PHARMACOLOGY EXAM 1 STUDY GUIDE(Download For Excellent Scores)

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PHARMACOLOGY EXAM 1 STUDY GUIDE • Drugs that PRODUCE a response? • Drugs that PREVENT a response? • Therapeutic WINDOW is what? • The time it takes for ½ of the drug concentration... to be eliminated from the body is called? • What is a patient on two highly protein bound drugs at risk for • What is it called for drugs to share many common features • What makes drugs fit into the same “class” • Another name for antagonist? • Who do you not give antagonist or adrenergic blocker to? • Beta blockers commonly seen in what clients? • Antagonist suffix • Antagonist S/S • Agonist S/S • Before administering antagonist what do you check • Cholinergic • Anticholinergic • What type of drug is Reglan? • How do you treat cholinergic crisis • Cholinergic crisis S/S • Anticholinergic drugs are contraindicated in who? • CNS stimulant drugs are contraindicated in who? • Hemorrhagic stroke • Anorexiants can lead to what? • Most common side effects of Ritalin o Irritability o Insomnia ▪ Weight loss ▪ Decrease appetite • Benzodiazepines increase activity to what neurotransmitter (PAM & LAM) o GABA • Reversal to benzodiazepines o Flumazenil • Ambien side effects o Sedative/hypnotic o Suicidal ideation o Dependence o Abnormal behavior • Drug choice for treating status epilepticus o Diazepam’s • Dilantin can do what? o Cause gum disease o Treat seizures o Cause high BP o Cause birth defects o Decrease effectiveness of anticoagulants • When a client is on Dilantin what are some nursing interventions? o Monitor for narrow therapeutic index (freq blood test) o Take as prescribed o Oral care o Teach pt to use barrier contraceptives along with oral • What is therapeutic level for Depakote? o 40-100 • If Depakote levels are high (>100) what needs to be done? o Hold meds o Check liver function with blood test o Discuss with DR o Neuro assessment o Check vitals • What does Depakote treat? o Epilepsy o Migraine • Bipolar disorder • Benzodiazepines can lead to what? o Tolerance o Dependence o Withdrawal • Barbiturates reversal treatment o Activated charcoal • Example of barbiturates o Phenobarbital • What disease process goes with “dopamine depletion”, rigidity, acetylcholine accumulation, acetylocholinerase inhibitor drugs, facial masking, motor neuron degeneration and anticholinergic drugs o Parkinson’s disease • What disease goes with confusion, bradykinesia, memory loss, amyloid plaques, and neurofibrillary tangles o Alzheimer’s disease • Aricept improves what? o Cholinergic function • What is SLUD o Salivation, lacrimation, urination, defecation • You CANNOT crush CONTIN, POTASSIUM and IRON o You CAN crush calcium antacids • What disease process goes with “lack of Ach receptor sites”? o Myasthenia Gravis • What disease process goes with “respirator muscle weakness”? o Myasthenia gravis • What disease process goes with “anticholinesterase inhibitor drugs”? o Myasthenia gravis • What should you avoid while taking cyclobenzaprine (flexeral)? o Driving and alcohol • A patient is taking an MAOI and eating blue cheese and red wine with dinner, what should you tell them that they are at risk for? o Hypertensive crisis • A patient is taking Lithium, you should advise them to avoid what other drugs? o Ibuprofen, ACE inhibitor, HCTZ • Serotonin syndrome S/S o Agitation, confusion, rigidity, fever • Extrapyramidal (EPS) effects are most common with which class of antidepressants? o Tricyclics • What to keep in mind with lithium? o It has a narrow therapeutic range, do not crush, check serum levels, take same time every day, and lab range is .4-.8 MeQ/L • What drugs contain acetaminophen? o Vicodin, Tylenol, Lortab, Norco, Excedrin, Nyquil, fioricet, Percocet, alka seltzer plus • What drugs do not contain acetaminophen? o Tramadol, gabapentin, flexeril, ketorolac, Motrin, dilaudid, Advil • What drug should not be given during an acute gout flare up? o Probenecid • What is an injectable NSAID? o Toradol • Ibuprofen should always be taken with? o Food or milk • All opioids can be reversed by what? o Narcan/naloxone • Max daily dose of acetaminophen for adults? o 3 grams/2 grams for elderly or liver/kidney damage • Common side effect of opioids are? o Respiratory depression, hypotension, increase intracranial pressure • Extra pyramidal symptoms? o Tardive dyskinesia, akathisia, acute dystonia • Neuroleptic malignant syndrome? o Sudden high fever, tachycardia, BP fluctuations, altered mental status, acute renal failure • The ONLY non-sedating anti-anxiety med is? o Buspar • Typical antipsychotics may be prescribed for short term use why? o It is faster working • Extra pyramidal side effects are most commonly seen in which class of medications? o Typical antipsychotics • How do you know if a neuroleptic is working? o Positive change in behavior • What do you need to teach with DMARDS? o Good hygiene • What is pharmaceutics? o Applies only to tablets or capsules given by mouth (PO). The process in which the tablet or capsule becomes a solution so that it can cross the biologic membrane of the stomach or small intestine • Drugs generally disintegrate and are absorbed faster in what? o Very acidic fluids • Very old and very young people have less gastric acidity? o Lower/slower absorption>drug in the system longer • If a drug is enteric coated and meant to be absorbed in where? o Small intestine, absorbed in the stomach • Pharmacokinetic phase o This is the process of drug movement to achieve drug action. Sometime referred to as what the body does to the drug • 4 processes o Absorption, distribution, metabolism, excretion • Protein bound drugs are destroyed by? o Digestive enzymes • Insulin is a protein bound drug, so CANNOT be given by which route? o Oral • Absorption drugs absorbed most easily are? o Fat soluble and non-ionized • What is the first pass effect? o The liver can inactive or change drugs into different forms • Bioavailability is what? o The % of the administered dose that reaches systemic circulation • Bioavailability for IV administered drugs is what %? o 100% because of the bloodstream/vein contact • After a pill is taken by mouth, what organ has a major impact on its bioavailability? o Absorption, most oral drugs are absorbed through the action of mucosal villi in the small intestine. If the villi are damaged by disease or surgical intervention, the absorption of the drug is delayed or does not occur • High fat foods increase what? o Absorption time • Exercise can decrease drug absorption because? o Blood flow is in peripheral muscles instead of the GI tract • Protein binding is what? o As drugs circulate in the blood and plasma, some of them have a high affinity for binding to the plasma proteins. Drugs that are stuck onto the proteins aren’t free to go to their target receptor sites and do their jobs • If a patients in on 2 drugs that are both strongly protein bound, what happens? o The compete for binding sites on the protein, which means more free drugs will be released into active circulation, which can lead to accumulation and toxicity • The blood brain barrier is what? o A filtering mechanism of the capillaries that carry blood to the brain and spinal cord tissue, blocking the passage of certain substances • Excretion/elimination are accomplish mainly where? o Kidneys • Peak is what? o When a drug reaches its highest plasma or blood concentration • Pharmacodynamics phase I what? o The way the drug affects the body • Onset is what? o The time until minimum effective action • Duration of action is what? o The length of time the drug has a pharmalogic effect • Receptor theory is? o Drugs act through receptors to produce or block a response. The better a drug fits at the receptor site, the more biologically active it is, like a key fitting into a lock • Agonist’s examples? o Drugs that produce a response are agonists, epinephrine • Antagonist examples? o Drugs that prevent or block a response are called antagonists, histamine receptor antagonist, and atropine • Peak is what? o The point at which plasma drug levels are highest • Trough is what? o Point at which plasma drug levels are lowest • Loading dose is what? o Given to achieve a rapid minimum effective concentration in the plasma. After the loading dose is given a prescribed daily dose is provided • Brand names are what? o Drug manufactures choose the brand names of their products, there can be many brands of a particular drug • Additive effects? o When two drugs with similar action are administered • Additive effect BAD example? o Undesired effect- hydralazine and nitroglycerine • Additive effect GOOD example o Desired effect, beta blocker & diuretic or aspirin and codeine • Synergistic effect o When two or more drugs are given together and the combined effect is substantially greater than the combined effect of the two • Synergistic effect BAD example o Undesired effect, diazepam and alcohol • Synergistic effect GOOD example o Desired effect amoxicillin and clavulanate, antagonistic effect • Antagonistic effect BAD example o Undesirable effects, bet stimulant, isoproterenol and beta blocker • Antagonistic effect GOOD example o Desirable effects, morphine and naloxone • Some drugs like MAOI antidepressants have specific food interactions such as tyramine (aged cheese, blue cheese, cured meat, summer sausage, pepperoni, salami, smoked/processed meats, pickled foods, sauces, soybeans, pop, peas, dried fruit, meat tenderizers yeast and alcoholic foods) • OTC cough and cold o Should not be taken by patients with hypertension or thyroid disease without talking to their DR first • Sleep Aids o Should not be taken with CNS depressant medications due to increase CNS depression • CNS brain and spinal cord o Peripheral nervous system • Somatic vs autonomic o Somatic ▪ Mostly voluntary, skeletal muscle movement o Autonomic o Mostly involuntary, acts on smooth muscles and glands, autonomic nervous system, sympathetic (adrenergic) parasympathetic (cholinergic) • Sympathetic o Norepinephrine, receptors alpha 1&2, beta 1&2, fight or flight • Parasympathetic o Acetylcholine, receptors (nicotinic and muscarinic), rest and digest • Adrenergic agonists o Increase BP, increase HR, bronchodilation, increase blood sugar, pupil dilation, and alertness • Adrenergic agonist drugs o Epinephrine and albuterol • Beta blockers o Specifically block beta receptor site, also inhibit the release of norepinephrine and epinephrine • Beta blocker effects o Decrease blood pressure, decrease heart rate, bronchoconstriction • Beta blocker drugs o Atenolol (Tenormin), metoprolol (Lopressor) used to treat hypertension, migraine prophylaxis, angina, myocardial infarction, heart failure • Beta blocker side effects o Depression, sexual dysfunction, cool extremities • Indirect aching o Inhibit the action of the enzyme cholinesterase, permitting ach to persist and attach to the receptor • Cholinergic drugs o Bethanechol chloride, metoclopramide hcl • Anticholinergics drugs DRY DRY DRY DRY o Atropine for bradycardia, reduces salivation, dilates pupils • Benzotropine for Parkinson’s o Tolterodine tartrate decreases urinary frequency, urgency and incontinence • Who to caution giving anticholinergic meds to? o Glaucoma and urinary retention • Amphetamines o Stimulates the release of norepinephrine and dopamine from the brain and sympathetic nervous system • Amphetamines common side effects o Insomnia, restlessness, nervousness, tremors, irritability, tachycardia, hypertension, weight loss • Amphetamine drugs o Methylphenidate (Ritalin), dexmethylphenidate (Focalin) used to treat ADHD and Narcolepsy • Amphetamines drug adverse reactions o Tachycardia, hypertension, palpitations, weight loss, hepatoxicity • Insomnia treatments o Non pharmalogic, antihistamines, sedative hypnotics • Insomnia drugs o Zolpidem (Ambien) • Insomnia drugs adverse reactions o Tolerance, dependence, hypotension, suicidal ideation • Benzodiazepines do what? o Increase the action of the inhibitory neurotransmitter GABA to the GABA receptors • Benzodiazepines drugs o Lorazepam (Ativan) - treats anxiety/seizures, diazepam (valium) treats anxiety and is a muscle relaxer, and alprazolam (Xanax) treats anxiety and insomnia • Benzodiazepine side effects o Lethargy, memory impairment dizziness, decrease libido, drowsiness • Benzodiazepine reversal agent o Flumazenil (Romazicon) • Epilepsy o Seizure disorder results from abnormal electrical discharges from the cerebral neurons, and causes a loss of consciousness and involuntary muscle contractions • Epilepsy drugs o Anticonvulsants (hydantoins, barbiturates, benzodiazepines, balproate) • Hydantoins side effects/adverse reactions o Slurred speech, confusion, depression, elevated blood sugar, fetal abnormalities • Benzodiazepines Lorazepam (Ativan treat what o Anxiety and seizure • Diazepam treats what o Anxiety and muscle relaxer • Valproate drugs (valproic acid “Depakote) treat what? o Manic bipolar Check liver enzymes • What is Parkinson’s caused by? o Imbalance of neurotransmitters dopamine and acetylcholine • Treatment for Parkinson’s? o Anticholinergics. Dopamine replacements, dopamine agonists, MOA-B inhibitors, COMT inhibitors • Parkinson’s drug? o Carbidopa/levodopa • Alzheimer’s disease is what? o Incurable dementia by chronic, progressive neurodegenerative conditions with marked cognitive dysfunction • Alzheimer’s disease symptoms o Memory loss, confusion, inability to communication, aggressive behavior, depression • Alzheimer disease acetylcholinesterase inhibitor o Prevents the breakdown of acetylcholine • Myasthenia gravis is what? o A lack of nerve impulses and muscle responses at nerve and muscle junctions: autoimmune disease • Myasthenia crisis? o Not enough acetylcholine, severe generalized weakness, may involve respiration muscles • Cholinergic crisis? o Too much acetylcholine, muscle weakness, increase salivation • Multiple sclerosis is what? o An autoimmune disorder that attacks the myelin sheath of nerve fibers in the brain and spinal cord, causing lesions called plaques • Multiple sclerosis treatments o Glucocorticoids, biological immune modifiers, immunosuppressant cyclophosphamide • MS symptom management o Skeletal muscle relaxer (diazepam, baclofen, tizanidine, methacarbamol) • Cyclobenzaprine side effects o Dizziness, headaches • Histamine o Causes dilation of arterioles and increases capillary permeability, allowing fluid into the injured areas • Kinins o Such as bradykinin increase capillary permeability and the sensation of pain • Prostaglandins o Increase vasodilation, capillary permeability and pain/fever • Aspirin o Decrease inflammation, decreases platelet aggregation, higher doses are usually enteric coated to protect the stomach • Ibuprofen-nonsteroidal anti-inflammatory o Fewer side effects than aspirin, can still cause GI upset, should not be taken during pregnancy • Celecoxib-NSAID o COX2 inhibitor, requires a prescription, adverse reaction is peripheral edema, used to treat osteoarthritis, rheumatoid arthritis • DMARDS (disease modify antirheumatic drugs) o Includes immunosuppressive agents, immunodulators, antimalarials • Rheumatoid arthritis o A chronic inflammatory disorder that typically affects the joints of the hands and feet • Immunomodulators: infiximb (remicade) o Tumor necrosis factor blocker, treats Rheumatoid arthritis and crohns disease, report dizziness, chills, depression, seizures, fatigue, rash • Gout o Inflammatory condition in which uric acid accumulates and urate crystals form in tissues, tendons, joints. Most commonly affects the big toe o Colchicine is the anti-inflammatory used to treat gout • Urocosurics, probenecid o Promotes excretion of uric acid, should not be given during acute attack, increase fluid intakes, lab tests may be needed • Uric acid inhibitor, allopurinol o Inhibits uric acid synthesis, prevents acute attacks • Analgesia o Relief from pain • Mild to moderate pain is usually relieved with the use of nonopiod analgeiscs • Moderate to severe pain usually requires an opioid • Non opioid analgesics o Aspirin, ibuprofen, ketorolac, cox2 inhibitors, acetaminophen, naproxen • Acetaminophen o Analgesic, antipyretic, not an NSAID, not an anti-inflammatory, hepatoxicity at high doses, no more than 650mg per dose, max 3,000mg per day • High purine foods o Alcoholic beverages, some seafood/fish, some meats (turkey, bacon, liver) • Ketorolac (toradol) o NSAID, analgesic, anti-inflammatory, commonly given IV or IM, treats moderate to severe pain, not to exceed 5 total days of treatment • Cox1 inhibitor o Can still cause GI bleed even if given IV, can cause fetal abnormalities in first trimester of pregnancy • Opioid analgesics o Morphine and codeine, true opiates, derived from opium o Act primarily on MU receptors of the CNS, suppress pain impulses, suppress respiration, suppress cough, antidiarrheal effects • Morphine sulfate adverse reactions o Life threatening respiratory depression (all opioids), increase intracranial pressure, hypotension, seizures, constipation • Other opioids o Hydromorphonr, fentanyl patch, oxycodone, oxycontin, hydrocodone, tramadol • The half-life of naloxone is shorter than the half-life of most opioids meaning what? o They many need a second dose of naloxone • Buprenorphrine/naloxone (suboxone) o Combination of opioid and opioid antagonists, used to help patients taper off heroin and other opioid drugs when addicted, if the pills are crushed for snorting or injecting, the naloxone capsules break open and cancel out the opioid effects at the receptor sites • Migraines o Caused by inflammation and dilation of the blood vessels in the cranium o Drugs: beta blockers, anticonvulsants, antidepressants, triptans, NSAIDS/naproxen • Triptans: sumatriptan (imitrex) o Rescue drug from migraine attack, causes vasoconstriction of cranial arteries • Mood stabilizers o Lithium, used to curb mania, narrow therapeutic range, blood levels must be monitored closely, avoid ACE inhibitors, HCTZ and NSAIDS • Bipolar treatment o Mood stabilizers, antidepressants, anticonvulsants • Bipolar affective disorder o A brain disorder that causes unusual shifts in mood, energy, activity levels and the ability to carry out daily tasks • Serotonin syndrome o Occurs when you take medication that causes high levels of the chemical serotonin to accumulate in your body • GABA o When reduced can lead to anxiety • Serotonins does what? o Regulates sleep, wakefulness, mood, delusions • Dopamine does what o Involved in the regulation of cognition, emotional responses, motivation • Norepinephrine does what o Associated with the control of arousal, attention, vigilance, mood, affect and anxiety • Neuroleptics o Refers to any drug that modifies psychotic behavior and exerts and antipsychotic effect • Anxiolytics o Anti-anxiety, sedatives, hypnotics • Psychosis o Losing contact with reality, commonly seen in schizophrenia, includes difficulty processing information and coming to a conclusion, delusions, illusions, hallucinations, incoherence, aggressive behavior or catatonia • What nursing education is needed for Dilantin o Take good care of oral hygiene and Dilantin can interfere with birth control, watch liver • aspirin therapy can cause what concern to watch for o increased risk for bleeding including with GI tract • sympathetic medications trigger o fight or flight, increases blood flow to muscle, dilates pupils, increase HR & RR, increases perspiration and arterial BP • How long does it take atypical neuroleptics to be effective o 2-3 weeks • what route of absorption is fastest o IV • myasthenia gravis is caused by o autoimmune issues, weakness of skeletal muscles, neuromuscular disease • used to reverse opiate overdose o narcan/naloxone • In epilepsy what does benzodiazepines do o Sustains GABA, benzos enhance effect causing sedative hytonic, muscle relaxant, gamma aminobutynic acid • when giving narcotic pain medications remember to always assess what system o respiratory system (rate, quality, o2 needs, o2 saturation) • What are the 4 stages in order of pharmakinetcs o Absorption, distribution, metabolism, excretion • when would you consider a medication effective o symptoms are improved, no signs or symptoms of toxicity • List characteristics of MS o Comes and goes, weakness, spasticity and double vision (diplopia) • what medication reverses benzodiazepines o romazicon/Flumazenil • CNS stimulates approved for o ADHD narcolepsy and respiratory distress • When do you give Ritalin o Before breakfast or lunch • Benzodiazepines mechanism of action o Interacts with GABA to decrease excitability • what nursing intervention may you do for side effects of anticholinergics o watch urine output, may have retention of urine that needs catheter use to void • What are the side effects of lithium o Seizures, fatigue, headache, ECG changes, muscle weakness, drowsiness, sedation, weight gain, rigidity, tremors, abdominal pain, nausea, polyuria • What are the two stages of sleep o REM and NREM • Urinary retention is due to what type of medication o Anticholinergic • Valproic acid is toxic to what system o Liver, if serum level is high check liver enzymes, check neruro status and call DR with findings • Sedative hypnotics when do you take o 15-45 mins before bed • what are the two types of anesthetics o general and local • what category of medication cannot be faxed and require med counts o C2-hydromorphone, methadone, oxycodone, fentanyl, morphine, codeine, opium, cocaine, hydrocodone, amphetamine o High potential for abuse • dextroamphetamine is also known as o Adderall, dexedine o Manages ADHD and narcolepsy • what is a medication washout o period of time to clear the medication-needed to prevent toxic side effect from overlapping medications in the body • cholinesterase inhibitors can cause o urgency with bowel and bladder • Pregnancy category D. Is this medication safe while pregnant o No due to birth defect risk • Is timing between sinement dosing of importance o Yes, must keep dosing evenly spaced out to maintain serum therapeutic levels • what class of medications do you avoid with asthmatics o beta blockers • Can Valproic acid - depakote be crushed o No, use the sprinkles • What are symptoms of serotonin syndrome o Agitation, confusion, rigidity, fever, dilated pupils, rapid HR and BP and can be life threatening • Any narcotic can cause constipation. What nursing interventions might you consider o drink water, stool softener, high fiber foods • metabolism primarily occurs where for medications o liver • benzodiazepine nursing instruction o do not stop this med without DR ok, do not stop suddenly, do not share, keep away from kids, tolerance may develop, serious side effects such as seizure can happen with sudden withdrawal • what are the acute medications for seizures o valium/Ativan • What is the best thing to do with any allergy or suspected allergy o Avoid the triggering agent • What should a nurse watch for with the use of traditional neuroleptics o Extrapyramidal movements • what are the side effects of tricyclics o increased HR, sleepiness, long half-life, slows down GI system • What does APAP stand for o Tylenol, do not exceed max dose • what medication class do you avoid in Parkinson’s o neuroleptics, they block dopamine receptors, worsening Parkinson symptoms • what medication may be tried to help with nerve pain o gabapentin, Lyrica, Cymbalta • MAOI medications can cause elevated blood pressure with what foods o Tyramine rich foods • peaks and troughs of medications are the o high and low levels in the blood • Benzodiazepines increase risk of what o falling • Neuroleptic syndrome causes what signs o High fever, confusion, rigidity, unstable walking, seizures, fever, renal failure, coma and can lead to death • anticholinergics can cause o dry mouth, increase HR, reduced bronchial secretions, blurred vision, decrease sweating, confusion, delirium, cognitive decline • increased suicide risk for patients on antidepressants occur when o initiation, full effects not for 2-3weeks, care if switching (serotonin syndrome) • what is a common side effect of beta blockers Decrease HR • when using patches what must you always remember o remove the old patch and wear gloves • what does the half-life mean of medication o time for half of the med to leave the body • agonist define o mimics receptor activity • antagonist define o blocks normal receptor activity • what is given for Tylenol (APAP) over dose o mucomyst • overdose of phenobarbital - what medication do you use o activated charcoal • Therapeutic range for Dilantin o 10-20 mcg/ml • therapeutic range for phenobarbital is o 20-40 mcg/ml • What are the side effects of sinement - carbidopa-levodopa o Fatigue, insomnia, dry mouth, orthostatic BP, palpitations, urinary retention, nausea, vomiting, dyskinesia and depression • Antipsychotic agents are either typical or a typical and block what o dopamine • what is the treatment for neuroleptic syndrome o remove antipsychotics, hydration, cooling blankets, benzodiazepines • risperidone - Risperdal is used for o psychosis, schizophrenia • what group of meds is used for anxiety o benzodiazepines • what are the three types of depression o reactive, major, bipolar • What is the therapeutic range for lithium o 1.0-1.5 mEq/l • What are the three chemical mediators in inflammation o Histamine, serotonin, lysosomal enzymes • Mechanism of action of NSAIDS o Inhibit biosynthesis of prostaglandins • Remember Cholinergic effects are either muscarinic or nicotinic • sympathetic causes what to heart rate o acceleration • parasympathetic causes what to eyes o constriction • sympathetic does what to kidneys o stimulates epinephrine and norepinephrine release • know your drug classes and side effects known for the classes along with nursing interventions o • what foods have tyramine in them o strong cheeses, cured meats, beers on tap, soy products, beans • What is EPS - describe and what causes o Extrapyramidal symptoms- akathisia(feeling of restlessness), parkinsonism (tremor, slow thought process, slow movement, rigid muscles, difficulty speaking, facial stiffness, DO NOT HAVE PARKINSONS, JUST SIMILAR SYMPTOMS FROM MEDICATION), tardive dyskinesia (uncontrollable facial movements), dystonia (involuntary muscle movement, contract and contort) • what is malignant hyperthermia and what is the treatment o disease that causes fast rise in body temp and severe muscle contractions o medication is dantrolene, a skeletal muscle relaxant • Review FDA oversight o Emerging drug safety issues • nursing intervention/teaching for patients started on antidepressants • know the difference between acute vs chronic treatment medications o acute is short, chronic is long o Acute include Antibiotics (germ-killing medicine), Anti-diarrhea medicine, Pain medicine, Cough, cold and allergy medicines, Medicines used in an emergency, such as for a heart attack. o Chronic include Diabetes medicine, Heart medicine, Osteoporosis medicine, High blood pressure medicine, Cholesterol medicine o Acute and chronic medicines may be used to treat the same problems. For example, you may take pain medicine when you have a headache. Once the headache goes away, you stop taking the medicine. This would be an acute medicine. But if you take medicine each day to prevent headaches, this would be a chronic medicine. • know your rights and your patients’ rights o NURSE ▪ Right patient ▪ Right drug ▪ Right dose ▪ Right time/frequency ▪ Right route ▪ Right to refuse ▪ Right documentation ▪ Right response o PATIENT ▪ Right to a medical record and to keep them private ▪ Right to make decisions on medical care ▪ Right to accept or refuse care ▪ Right to advanced directives • what does a culture of safety look like in nursing o promote safety o prevent injury - know their strengths, can they stand o be aware of the development level o be aware of the patient's lifestyle (ex. smoker) o identify potential hazards (look at what they bring in) • It important to access the patient and inquire of what for every patient o All medications including herbs, otc and alternative health care treatments they are receiving, these can interact with medications • Does the FDA regulate OTC and herbs o Yes but different regulation • Pain level is o Whatever the patient says it is • you can measure someone’s pain by observation o No! • Content Guide Exam 1 • 1) Medication Classification: • Schedule 1: • Schedule II: • Schedule III: • Schedule IV: • Schedule V: • 2) Opioid and non-opioid medications • Examples: Morphine, Tylenol, Percocet, Ibuprofen Aspirin • Assessment of the pain • Assessment of the patient • Commodities: COPD, Asthma, Pneuomonia • Dosage, Orders, active ingredients, Medication side-effects • 4) Antianxiety medications Benzodiazepines: Xanax Examples • Nursing Assessment: • Side Effects: • Adverse effects: • Dependency: • Hyponotics: Zolpidem • Anti-cholinergic • Know the Pathophysiology of PNS and SNS • Exemplar: • 5) Anorexants: Phentermine • 6) Stimulants: Adderall, indication for use, dosage, indications • 7) Neuroleptic Malignant Syndrome • 8) Serotonin Syndrome • 9) Neuroleptics: Examples, know side-effects, indication for use. • 10) Medications Review the mechanism of action, contraindication, indication for use, assessment on whether it is effective, safe dosing, adverse effects, pregnancy schedule, antidote • Flexeril • Cogentin • Phenytoin • Morphine • Buspar • Valium Chapter 1: Drug Development and Ethical Considerations Drug Names- ▪ The Generic Name: is the official, nonproprietary name for the drug; this name is not owned by any drug company and is universally accepted. Generic names are given in lowercase letters ▪ The Brand (Trade) Name: also known as the proprietary name is chosen by the drug company and it usually a registered trademark. Brand names always begin with a capital letter. Over-the-Counter Drugs- ▪ Over the Counter (OTC): drugs have been found to be safe and appropriate for use without the direct supervision of a healthcare provider. They are available for purchase without a prescription in many retail locations. OTC drugs include vitamin supplements, cold remedies, analgesics, antacids, laxatives, antihistamines, sleep aids, nasal sprays, weight control drugs, drugs for dermatitis and fungal infections, fluoride toothpaste, corn and callous removal products, and herbal products. Chapter 2: Pharmacokinetics, Pharmacodynamics, and Pharmacogenetics Pharmacokinetics- ▪ Pharmacokinetics: . Is the process of drug movement throughout the body that is necessary to achieve drug action. The 4 processes are absorption, distribution, metabolism (or biotransformation), and excretion (or elimination). ▪ Drug Absorption: is the movement of the drug into the bloodstream after administration. Approximately 80% of drugs are taken by the mouth (enteral). For the body to utilize drugs taken by mouth, drug and solid form must disintegrate into small pieces and combined with liquid to form a solution, a process known as dissolution, in order to be absorbed from the gastrointestinal track into the bloodstream. o Unlike drugs taken by mouth parenteral drug such as eyedrops, eardrops, nasal sprays, respiratory inhalants, transdermal drugs, and sublingual drugs do not pass through the G.I. tract. o Blood flow, pain, stress, hunger, fasting, food, and pH affects drug absorption. o Drugs given intramuscularly are observed faster and muscles that have increased blood flow (e.g. deltoid) than those that do not (e.g. gluteus maximus). o Subcutaneous tissue has decreased blood flow when compared to muscles, so absorption is slower when drugs are given subcutaneously. However, drugs that are given subcutaneously have a more rapid and predictable rate of absorption than those given by mouth. o Drugs given rectally are absorbed slower than drugs administered by oral route. Absorption is slower because the surface area in the rectum is smaller than the stomach, and there are no villi. o Following absorption of oral drugs from the G.I. tract, they pass from the intestinal lumen to the liver via the portal vein. In the liver some drugs are metabolized to a in active form and are excreted, thus reducing the amount of active drug available to exert a pharmacological effect. This is referred to as The First Pass Effect. Affected to some degree by 1st pass metabolism. o Bioavailability refers to the percentage of administered drug available for activity. The bioavailability of intravenous drugs is 100%. The bioavailability of oral drugs is always less than 100% and varies based on the rate of 1st pass metabolism. ▪ Drug Distribution: distribution is the movement of the drug from the circulation of body tissues. Drug distribution is influenced by the rate of blood flow to the tissue, the drugs affinity to the tissue, and protein binding. o Protein Binding- as drugs distribute in the plasma, many bind with plasma proteins. The portion of the drug bone to protein is inactive because it is not available to interact with tissue receptors and therefore is unable to exert a pharmacological effect. The portion that remains unbound is free, active drug. Free drugs are able to exit blood vessels and reach their site of action, causing a pharmacological response. ▪ When 2 highly protein bound drugs are administered together, they compete for protein binding sites, leading to an increase in free drug being released into the circulation. In this situation it is possible for drug accumulation to occur and for toxicity to result. ▪ Another factor that may alter protein binding is low plasma protein levels, which potentially decrease the number of available binding sites and can lead to an increase in the amount of free drug available, resulting in drug accumulation and toxicity. Patients with liver kidney disease and those who are malnourished may have significantly lower serum albumin levels. Additionally, older adults are more likely to have low albumin levels, particularly if they have multiple chronic illnesses. ▪ Drug Metabolism: metabolism or biotransformation, is the process by which the body chemically changes drugs into a form that can be excreted. The liver is the primary site of metabolism. o Liver disease such as cirrhosis and hepatitis alter drug metabolism by inhibiting the drug metabolizing enzymes in the liver. When the drug metabolism rate is decreased, excess drug accumulation can occur and can lead to toxicity. o The drug half-life is the time it takes for the amount of drug in the body to be reduced by half. The amount of drug administered, the amount of the drug remaining in the body from previous doses, metabolism, and elimination affect the half-life of a drug. o By knowing the half-life, the time it takes for the drug to reach a steady state (plateau drug level) can be determined. A steady-state occurs when the amount of drug being administered is the same as the amount of drug being eliminated; a steady state of drug concentration is necessary to achieve optimal therapeutic benefit. This takes about 4 half-life’s, if the size of all doses are the same. o Loading Dose- in the case of drugs with long half-life’s, it may not be acceptable to wait for steady-state to be achieved. For example a person with seizures receiving phenytoin. The half-life of phenytoin is approximately 22 hours; if all doses of the drug were the same, steady-state would not be achieved for about 3 ½ days. By giving a large initial dose, known as a loading dose, that is significantly higher than maintenance dosing, therapeutic effects can be obtained while a steady state is reached. ▪ Drug Excretion: the main route of drug excretion, elimination of drugs from the body, is through the kidneys. Drugs are also excreted through bile, the lungs, saliva, sweat, and breast milk. The kidneys filter free drugs (in healthy kidneys, drugs bound to protein are not filtered), water- soluble drugs, and drugs that are unchanged. Pharmacodynamics- ▪ Pharmacodynamics: is the study of the effects of drugs on the body. Drugs act within the body to mimic the action of the body’s own chemical messengers. Drug response can cause a primary or secondary physiological effect or both. A drugs primary effect is the desirable response, and the secondary effect may be desirable or undesirable. ▪ Onset: is the time it takes for a drug to reach the maximum effective concentration after administration. ▪ Peak: a drugs peak occurs when it reaches its highest concentration in the blood. ▪ Duration of Action: is the length of time the drug exerts a therapeutic effect ▪ Peak Drug Level: is the highest plasma concentration of drug at a specific time, and it indicates the rate of drug absorption. If the peak is too low, effective concentration has not been reached. If the drug is given orally, the peak is usually 2 to 3 hours after drug administration. If the drug is given intravenously, the peak time is usually 30 to 60 minutes after the infusion is complete. If the drug is given intramuscularly the peak time is usually 2 to 4 hours after injection. ▪ Through Drug Level: is the lowest plasma concentration of a drug, and it measure the rate at which the drug is eliminated. Troughs levels are drawn just prior to the next dose of drug regardless of route of administration. Most drugs only require trough concentration levels to be drawn ▪ Agonist: drugs that activate receptors and produce a desired response ▪ Antagonists: drugs that prevent receptor activation and block a response. Blocking receptor activation either increases or decreases cellular action, depending on the androgynous action of the chemical messenger that is blocked. ▪ Side Effect: our secondary effects of drug therapy. All drugs have side effects. Even with correct drug dosage, side effects occur that can be predictable and range from inconvenient to severe or life-threatening. In some instances, the side effects may be desirable (e.g. using diphenhydramine at bedtime, when it side effect of drowsiness is beneficial). Chronic illness, age, weight, gender, and ethnicity all play a part in drug side effects. ▪ Adverse Drug Reactions (ADRs): are unintentional, unexpected reactions to drug therapy that occur at normal drug dosages. The reactions may be mild to severe and include anaphylaxis. Adverse drug reactions are always undesirable and must be reported and documented because they represent variances from plant therapy. ▪ Drug Toxicity: occurs when drug levels exceed the therapeutic range; toxicity may occur secondary to overdose of drug accumulation. Factors that influence drug toxicity include disease, genetics, and age. Pharmacogenetics- ▪ Pharmacogenetics: refers to the study of genetic factors that influence an individual’s response to a specific drug. Genetic factors can alter drug metabolism, resulting in either enhanced or diminished drug response. ▪ Tolerance: refers to a decreased responsiveness to a drug over the course of therapy; an individual’s drug tolerance requires a higher dosage of drug to achieve the same therapeutic response. Chapter 4: Complementary and Alternative Therapies ▪ Herbal Medicine: Chapter 8: The Nursing Process and Patient-Centered Care The Nursing Process- ▪ Assessment: gathering information from the patient about the patient’s health and lifestyle. Always perform a complete, systematic assessment of the patient’s body systems. In this assessment, the nurse asked the patient questions about illness and about the drug regimen. o Subjective Data- ▪ current health history ▪ swallowing problems (dysphasia) ▪ current concerns ▪ allergies o Objective Data- ▪ physical health assessment ▪ laboratory and diagnostic test results ▪ measurement of vital signs ▪ patient’s body language ▪ Diagnosis: is made based on analysis of the assessment data, and is determines the type of care the patient will receive. When data show a abnormality during the assessment, it can serve as the defining characteristic of a problem to support the appropriate nursing diagnosis. Common nursing diagnosis is related to drug therapy include: o pain, acute or chronic, related to surgery o confusion, acute related to an adverse reaction to a medication o health maintenance, ineffective related to not receiving recommended preventative care o knowledge, deficit related to effects of anticoagulant education o noncompliance related to forgetfulness o health management, ineffective related to lack of finances ▪ Planning: the nurse uses the data collected to set goals or expected outcomes and interventions. Goals or expected outcomes should address the problems in the patient’s nursing diagnosis. Goals are patient centered, described the specific activity, and include a timeframe for achievement and reevaluation. ▪ Implementation of Nursing Interventions: is the part of the nursing process in which the nurse provides education, drug administration, patient care, and other interventions necessary to assist the patient in accomplishing the established goals. In most practice settings, administration of drugs and assessment of the drug’s effectiveness are important nursing responsibilities. o Patient Teaching- the following are important principles to remember when teaching patients about their medications: ▪ Gen.-instruct the patient to take the drug as prescribed. • Name of drug • reason for taking the drug • time to take the drug • possible side effects • possible adverse effects ▪ Side effects ▪ self-administration ▪ diet ▪ cultural considerations ▪ Evaluation: the nurse determines whether the goal and teaching objectives are being met. If the objectives and goals are not met, the nurse will revise the objectives, goals, and interventions to ensure success. If the objectives, goals, and interventions are met the nurse will document the success attained in the nursing plan of care. Chapter 9: Safety and Quality ▪ Five-plus-Five Rights of Medication Administration: o Right Patient o Right Drug o Right Dose o Right Time o Right Route ▪ Right Assessment ▪ Right Documentation ▪ Right Education ▪ Right Evaluation ▪ Right to Refuse ▪ Pregnancy Categories: Unit IV: Autonomic Nervous System Drugs ▪ The Central Nervous System: is the body’s primary nervous system and consists of the brain and spinal cord. ▪ The Peripheral Nervous System: located outside the brain and spinal cord, is made up of 2 divisions the autonomic and somatic. After interpretation by the CNS, the PNS receive stimuli and initiates responses to the stimuli. o Autonomic Nervous System- also called the visceral system, axon smooth muscles and glands. It functions include control and regulation of heart, respiratory system, gastrointestinal tract, bladder, eyes, and glands. The ANS is a involuntary nervous system, over which we have little to no control: the breeze, our hearts beat, and peristalsis continues without our realizing it. ▪ Afferent (Sensory) Neurons: send impulses to the CNS, where they are interpreted. ▪ Efferent (Motor) Neurons: receives the impulses (information) from the brain and transmit these impulses through the spinal cord to the effector organ cells. The efferent pathways in the ANS are divided into 2 branches: the sympathetic and parasympathetic nerves. • Sympathetic Nervous System- the sympathetic nervous system is also called the adrenergic system because at one time, it was believed that adrenaline was the neurotransmitter that innervated smooth muscle. However, that neurotransmitter is norepinephrine • Parasympathetic Nervous System- the parasympathetic nervous system is called the cholinergic system because the neurotransmitter at the end of the neuron that innervates the muscle is acetylcholine. o Somatic Nervous System- is a voluntary system that innervates skeletal muscles, which there is control. Chapter 15: Adrenergic Agonists and Antagonists ▪ Adrenergic Agonists (Sympathomimetics)- drugs the stimulate the sympathetic nervous system are called adrenergic agonists, adrenergics, sympathomimetics because they mimic the sympathetic neurotransmitters norepinephrine and epinephrine. They act on one or more adrenergic receptor sites located in the effector cell of muscles such as the heart, bronchiole walls, gastrointestinal tract, urinary bladder, and ciliary muscles of the eye. o The 4 main receptor sites are alpha-1, alpha-2, beta-1, and beta-2 which mediate the major responses. o Fight or Flight ▪ What happens in each system? ▪ Diversion of blood to skeletal muscles ▪ mobilizing energy o Classifications of Sympathomimetics- drugs that stimulate adrenergic receptors are classified into 3 categories according to their effects on organ cells. ▪ Direct acting sympathomimetics: which directly stimulate the adrenergic receptors (e.g. epinephrine or norepinephrine) ▪ Indirect acting sympathomimetics: which stimulate the release of norepinephrine from the terminal nerve ending (e.g. amphetamine) ▪ Mixed acting (both direct and indirect acting) sympathomimetics: which stimulate the adrenergic receptor sites and stimulate the release of norepinephrine from the terminal nerve endings (e.g. ephedrine) o Side Effects and Adverse reactions- ▪ Hypertension ▪ Tachycardia ▪ Palpitations ▪ Restlessness ▪ Tremors ▪ Dysrhythmia ▪ Dizziness ▪ urinary retention ▪ nausea and vomiting ▪ Dyspnea ▪ pulmonary edema ▪ Adrenergic Antagonists (Adrenergic Blockers)- is a block the effects of adrenergic neurotransmitters are called adrenergic antagonists, adrenergic blockers, or sympatholytics. They act as antagonists to adrenergic agonists by blocking the alpha and beta receptor sites. Most adrenergic antagonists block either the alpha receptor or the beta receptor. They block the effects of the neurotransmitter either directly by occupying the receptors or indirectly by inhibiting the release of the neurotransmitter norepinephrine and epinephrine. o Alpha-Adrenergic Antagonists: drugs that block or inhibit the response at the alpha adrenergic receptor site are called alpha adrenergic antagonists, adrenergic blockers, or alpha blockers. Alpha blocking agents are divided into 2 groups: ▪ selective- alpha blockers block alpha 1 ▪ nonselective- alpha blockers that block alpha-1 and alpha-2 o Because alpha adrenergic antagonists can cause orthostatic hypotension and reflects tachycardia, many of these drugs are not as frequently prescribed as beta antagonists. o Alpha antagonists (alpha blockers): promote vasodilation, causing a decrease in blood pressure. If vasodilation is long-lasting, orthostatic hypotension can result. Dizziness may also be a symptom of a drop in blood pressure. As blood pressure decreases, pulse rate usually increases to compensate for the low blood pressure and inadequate blood flow. Alpha antagonists can be used to treat peripheral vascular disease. Vasodilation occurs, permitting more blood flow to the extremities. These drugs are also helpful in decreasing symptoms of benign prostate hyperplasia. o Beta-Adrenergic Antagonists: more commonly called beta blockers, decreased heart rate and a decrease in blood pressure usually follows. Some beta blockers are nonselective, blocking both beta-1 and beta-2 receptors. Not only does the heart rate decrease because of beta-1 blocking, bronchial constriction also occurs. Nonselective beta blockers block both beta-1 and beta-2 and should be used with extreme caution in any patient who has chronic obstructive pulmonary disease (COPD) or asthma. ▪ Atenolol- a selective beta-1 blocker, is one of the most frequently prescribed drugs in the United States. Atenolol decreases sympathetic outflow to the periphery and suppresses the renin angiotensin aldosterone system response. ▪ Beta blockers are useful in treating mild to moderate hypertension, angina, heart failure, and myocardial infarctions. Beta blockers should not be abruptly discontinued but rather should be tapered off over 1 to 2 weeks to avoid tachycardia, hypertension, severe angina, dysrhythmia, and MI. Chapter 16: Cholinergic Agonists and Antagonists ▪ Cholinergic Agonists- drugs that stimulate the parasympathetic nervous system are called cholinergic agonists, or parasympathomimetics, because they mimic the parasympathetic neurotransmitter acetylcholine. There are 2 types of cholinergic agonists: o direct acting cholinergic agonists- act on receptors to activate a tissue response o Indirect acting cholinergic agonists- inhibit the action of the enzyme cholinesterase also called acetylcholinesterase, by forming a chemical complex that allows acetylcholine to persist and attached to the receptor. Indirect acting cholinergic agonists do not act on receptors; instead they inhibit or inactivate the enzyme cholinesterase, permitting acetylcholine to accumulate at the receptor sites. ▪ Cholinergic Antagonists- drugs that inhibit the actions of acetylcholine by occupying the acetylcholine receptors are called cholinergic antagonists (blocking agents), anticholinergics, cholinergic blocking agents,. The major body tissues and organs affected by the anticholinergic group of drugs are the heart, respiratory tract, G.I. tract, urinary bladder, eyes, and exocrine glands. By blocking the parasympathetic nerves, the sympathetic (adrenergic) nervous system dominates. Anticholinergics and adrenergic agonists produce many of the same responses. ▪ Antiparkinson-Anticholinergic Drugs- studies indicate that anticholinergics affect the CNS as well as the parasympathetic nervous system. Anticholinergics affect the CNS by suppressing the tremors and muscular rigidity of Parkinsonism, but they have little effect on mobility and muscle weakness. ▪ Antichlinergics: Gastrointestinal or Cholinergic Blockers: ▪ Anticholinergics for Treating Motion Sickness: Unit V: Central and Peripheral Nervous System Drugs Chapter 17: Stimulants ▪ numerous drugs can stimulate the central nervous system, which involve the brain and spinal cord and regulates body functions. Medically approved use of CNS stimulants is limited to the treatment of attention deficit/hyperactivity disorder in children, narcolepsy, and the reversal of respiratory distress. ▪ The major groups of CNS stimulants include amphetamines and caffeine, which stimulate the cerebral cortex of the brain; analeptics and caffeine, which act on the brainstem and Medusa to stimulate respiration; and anorexiants which are thought to suppress appetite by stimulating the satiety center of the hypothalamus and limbic areas of the brain. ▪ Long-term use of in fat amines can produce psychological dependence or tolerance, conditions in which larger and larger dose of the drug are needed to reproduce the initial response. ▪ Amphetamines: stimulate the release of neurotransmitters norepinephrine and dopamine from the brain and sympathetic nervous system and inhibit the reuptake of these transmitters. Amphetamines ordinarily cause euphoria and increased alertness, but they can also cause insomnia, restlessness, tremors, irritability, and weight loss. Cardiovascular problems such as increased heart rate, palpitations, cardiac dysrhythmia, and increase blood pressure can result from cardiac stimulation and vasoconstriction with continuous use of amphetamines. o Side effects and adverse reactions- ▪ Amphetamines can cause adverse effects on the CNS and the cardiovascular, gastrointestinal, and endocrine systems. Side effects and adverse reactions include dizziness, headaches, euphoria, confusion, blurred vision, restlessness, insomnia, tachycardia, hypertension, heart palpitations, dysrhythmia, dry mouth, anorexia, weight loss, diarrhea, constipation, seizures, tremors, and erectile dysfunction. ▪ Amphetamine -like drugs: o Methylphenidate and dexmethylphenidate, classed as a phentermine like drugs, are given to increase a child’s attention span and cognitive performance and to decrease impulsiveness, hyperactivity, and restlessness. Methylphenidate is also used to treat narcolepsy. Because of the potential for abuse of methylphenidate, it is classified as a controlled substance schedule (CSS)II drug. Chapter 18: Depressants ▪ Drugs that are central nervous system depressants cause varying degrees of depression (reduction in functional activity) within the CNS. The degree of depression depends primarily on the drug and the amount of drug taken. The broad classification of CNS depressants include sedative-hypnotics, general anesthetics, analgesics, opioid and non-opioid analgesics, anticonvulsants, antipsychotics, and antidepressants. ▪ Barbiturates: were introduced as a sedative in the early 1900s. They are classified as long, intermediate, short, and ultrashort acting. o Long-acting- includes phenobarbital and mephobarbital, which are used to control seizures in epilepsy. o Intermediate acting- such as butabarbital, are useful in sleep sustainers for maintaining long periods of sleep. Because these drugs take approximately one hour for the onset of sleep, they are not prescribed for those who have trouble getting to sleep. Vital signs should be closely monitored in persons who take intermediate acting barbiturates. o Short acting- secobarbital may be used for procedure sedation. Vital signs should be closely monitored in persons who take short acting barbiturates. o Barbiturates should be restricted for short-term use (2 weeks or less) because of their numerous side effects, including tolerance to the drug. In the United States, barbiturates are classified under the controlled substance act as a schedule II for short acting, schedule III for intermediate acting, and schedule IV for long-acting hypnotics. o Many drug interactions are associated with barbiturates. I’ll call, narcotics, and other sedative hypnotics used in combination with barbiturates may further depress the CNS. Pentobarbital increases hepatic enzyme action, causing an increased metabolism and decrease effect of drugs such as oral anticoagulants, glucocorticoid, tricyclic antidepressants, and quinidine. Pentobarbital may cause hepatotoxicity if taken with large doses of acetaminophen. ▪ Benzodiazepines: selected benzodiazepines, minor tranquilizers and anxiolytics, where introduced with chlordiazepoxide in the 1960s as antianxiety agents. This drug group is ordered as the date of hypnotics for inducing sleep. Increased anxiety might be the cause of insomnia for some patients, so lorazepam and diazepam can be used to alleviate the anxiety. These drugs are classified as schedule IV according to the controlled substance act. The benzodiazepines increase the action of the inhibitory neurotransmitter GABA to the GABA receptors. Neuron excitability is reduced. Chapter 19: Antiseizure Drugs ▪ Drugs used for epileptic seizures are called antiseizure drugs, anticonvulsants, or antiepileptic drugs. Antiseizure drugs stabilize nerve cell membranes and suppress the abnormal electrical impulses in the cerebral cortex. These drugs prevent seizures but do not eliminate the cause or provide a cure. Antiseizure drugs are classified as central nervous system depressants. ▪ Hydantoins: the 1st antiseizure drug used to treat seizures was phenytoin, a hydantoin discovered in 1938 and still commonly used for controlling seizures. Hydantoins inhibit the sodium influx, stabilize cell membranes, reduce repetitive neurological firing, and limit seizures. By increasing the electrical stimulation threshold in cardiac tissue, it also acts as an anti-dis- rhythmic. It has a slight effect on general sedation, and it is non-addicting. However, this drug should not be used during pregnancy because it can have a teratogenic effect on the fetus. o Drug-Drug interactions- ▪ drug interaction is common with hydantoins because they are highly protein bound. Hydantoins compete with other drugs (e.g. anticoagulants, aspirin) for plasma protein binding sites. The hydantoins displace anticoagulants and aspirin, causing more free drug availability and increasing their activity. Barbiturates, rifampin, and chronic ingestion of ethanol increases hydantoins metabolism. Drugs like sulfonamides and cimetidine can increase the action of hydantoins by inhibiting liver metabolism, which is necessary for drug excretion. Antacid, calcium preparations, sucralfate, and antineoplastic drugs also decrease the absorption of hydantoins. Antipsychotics and certain herbs can lower the seizure threshold, the level at which seizure may be induced, and they increased seizure activity. ▪ Barbiturates: phenobarbital, a long acting barbiturates is prescribed to treat tonic-clonic, partial, and myoclonic seizures and status epilepticus, a rapid succession of epileptic seizures. Barbiturates reduce seizure by enhancing the activity of GABA, an inhibitory neurotransmitter. Possible teratogenic effects and other side effects related to phenytoin are less pronounced with the phenobarbital. The therapeutic serum range of phenobarbital is 20 to 40 mcg/mL. Risks associated with the use of phenobarbital include sedation and tolerance to the drug. Discontinuance of phenobarbital should be gradual to avoid reoccurrence of seizures ▪ Benzodiazepines: the benzodiazepine that have antiseizure effects are clonazepam, clorazepate dipotassium, lorazepam, and diazepam. Clonazepam is effective in controlling abscess and myoclonic seizures, but tolerance may occur 6 months after drugs therapy starts; consequently, clonazepam dosage must be adjusted. Clorazepate dipotassium is administered for treating partial seizures. o Diazepam is administered by IV to treat status epilepticus. The drug has a short-term effect; thus other antiseizure drugs, such as phenytoin or phenobarbital, must be given during or immediately after administration of diazepam. ▪ Valproate Acid: is prescribed for tonic-clonic, absence, and mixed type seizures, although the safety and efficiency of this drug has not been established for children younger than 2 years of age. Care should be taken when giving this drug to very young children and to patients with liver disorders because hepatotoxicity is one of the possible adverse reactions. Liver enzymes should be monitored. The therapeutic serum range for patients with seizures is 50-100 mcg/mL Chapter 20: Drugs for Parkinson’s Disease and Alzheimer Disease ▪ ▪ Anticholinergics: anticholinergic drugs reduce the rigidity and some of the tremors characteristic of Parkinson’s disease but have a minimal effect on bradykinesia. The anticholinergic’s are parasympatholytics that inhibit the release of acetylcholine. Anti-cholinergic’s are still used to treat drug-induced parkinsonism, or pseudo-parkinsonism, a side effect of antipsychotic phenothiazine drug group. Examples of anticholinergics use for Parkinson’s disease include trihexyphenidyl and benztropine. o Patient Teaching- ▪ avoid alcohol, cigarettes, caffeine, and aspirin to decrease gastric acidity ▪ encourage patients to relieve a dry mouth with hard candy, ice chips, or sugar list chewing gum. Anticholinergics decrease elevation ▪ suggest that patients use sunglasses in direct sunlight because of possible photophobia ▪ advise patients to avoid before taking the drug to minimize urinary retention ▪ counsel patients who take a anticholinergic for control of symptoms of Parkinson’s disease to have routine eye examinations because anticholinergics are contraindicated in patients with glaucoma. ▪ Dopaminergics: the 1st dopaminergic drug was levodopa, which was introduced in 1961 but is no longer available in the United States. When introduced, levodopa was effective in diminishing symptoms of Parkinson’s disease and increasing mobility; this is because the blood brain barrier admits levodopa but not dopamine. The enzyme dopa decarboxylase converts levodopa to dopamine in the brain, but this enzyme is also found in the peripheral nervous system and allows 99% of levodopa to be converted to dopamine before it reaches the brain. Therefore about 1% of levodopa taken is available to be converted to dopamine once it reaches the brain, a large dose is needed to achieve pharmacological response. These high doses could cause many side effects, including nausea, vomiting, dyskinesia, orthostatic hypotension, cardiac dysrhythmias, and psychosis. ▪ Because of the side effects of levodopa and the fact that so much levodopa is metabolized before it reaches the brain, alternative drug, carbidopa, was developed to inhibit the enzyme dopa carboxylase. By inhibiting the enzyme in the peripheral nervous system, more levodopa reaches the brain. The carbidopa is combined with levodopa in a ratio of one part carbidopa to 10 parts levodopa. ▪ The advantages of combining levodopa with carbidopa are that more dopamine reaches the basal ganglia and that smaller doses of levodopa are required to achieve the desired effects. The disadvantage of the carbidopa levodopa combination is that with more available levodopa, more side effects may occur, which may include nausea, vomiting, dystonic movement (involuntary abnormal movement), and psychotic behavior. The peripheral side effects of levodopa are not as prevent; however, angioedema, palpitations, and orthostatic hypotension may occur. ▪ Precautions for Drugs Used to Treat Parkinson’s Disease: o Side Effects and Adverse Reactions- the common side effects of anticholinergics include dry mouth and dry secretions, urinary retention, constipation, blurred vision, and increased heart rate. Mental effects such as restlessness and confusion may occur in older adults. o Contraindications-anticholinergic or any drugs that have anticholinergic effects are contraindicated for patients with glaucoma. Those with severe cardiac, renal, or psychiatric health problems should avoid levodopa drugs because of adverse reactions. Patients with chronic obstructive lung disease such as emphysema can have dry, thick mucus secretions caused by large doses of antics energy drugs. o Drug-Drug interactions- antipsychotic drugs block the receptors for dopamine. Carbidopa-levodopa taken with a monoamine oxidase inhibitor (MAOI) antidepressant can cause a hypertensive crisis. Chapter 21: Drugs for Neuromuscular Disorders and Muscle Spasms ▪ Skeletal Muscle Relaxants: muscle relaxants relieve muscular spasms and pain associated with traumatic injuries and spasticity from chronic debilitating disorders (e.g. MS, stroke, cerebral palsy, head and spinal cord injuries). Spasticity results from increased muscle tone from hyper excitable neuron; this is caused by increased stimulation from the cerebral neurons or lack of inhibition in the spinal cord or at the skeletal muscles. The centrally acting muscle relaxants depress neuron activity in the spinal cord or brain, or the enhanced neural inhibition on the skeletal muscles. o Centrally Acting Muscle Relaxants: the mechanism of action of centrally acting muscle relaxants is not fully known. Centrally acting muscle relaxants are used in case of spasticity to suppress hyperactive reflex and for muscle spasms that do not respond to anti-inflammatory agents, physical therapy, or other forms of therapy. ▪ Spasticity- skeletal muscle specificity is muscular hyperactivity that causes contraction of muscles, resulting in pain and limited mobility. Centrally acting muscle relaxants act on the spinal cord. ▪ Muscle Spasms- various centrally acting muscle relaxants are used for muscle spasms to decrease pain and increase range of motion. They have a sedative effect and should not be taken concurrently with CNS depressants such as barbiturates, narcotics, and alcohol. These agents, with the exception of cyclobenzaprine, can cause drug dependence. In addition, dizziness and drowsiness are common side effects. ▪ Side Effects and Adverse Reactions- drowsiness, dizziness, lightheadedness, headaches, and occasional G.I. sensitivity (e.g. nausea, vomiting, abdominal distress). Chapter 22: Antipsychotics and Anxiolytics ▪ Typical Antipsychotics: introduced in 1952, are subdivided into the phenothiazines and non- phenothiazines. o Adverse Reactions- ▪ Extrapyramidal Syndrome (Pseudoparkinsonism): which resembles symptoms of Parkinsonism is a major side effect of typical antipsychotics. Symptoms of pseudoparkinsonism or EPS include stooped posture, masklike facies, rigidity, tremors at rest, shuffling gait, pill rolling motions of the hands, and bradykinesia. When patients take high potency typical antipsychotic drugs for extended periods, EPS is more pronounced. Patients who take low strength antipsychotics such as chlorpromazine are not as likely to have symptoms of pseudoparkinsonism as those who take fluphenazine. ▪ Acute Dystonia: usually occurs in 5% of patients within days of taking typical antipsychotics. Characteristics of the reaction include muscle spasms of the face, tongue, neck, and back; facial grimacing; abnormal or involuntary upward eye movement; and laryngeal spasms that can impair respiration. This condition is treated with a anticholinergic antiparkinson drugs such as an benztropine. The benzodiazepine lorazepam made also be prescribed. ▪ Akathisia: occurs in approximately 20% of patients who take atypical antipsychotic drug. With this reaction, the patient has trouble standing still, is restless, paces the 4, and is in constant motion (e.g. rocks back and forth). It is best treated with a benzodiazepine such as Lorazepam or a beta blocker such as propranolol. ▪ Tardive Dyskinesia: is a serious adverse reaction that occurs in approximately 20% to 30% of patients who have taken a typical antipsychotic drug for more than one year. The prevalence is higher in cigarette smokers. The likelihood of developing tardive dyskinesia depends on the dose and duration of the antipsychotic factor. Characteristics of tardive dyskinesia include protrusion and rolling of the tongue, sucking and smacking movements of the lips, chewing motion, and involuntary movement of the body and extremities. In older adults, these reactions are more frequent and severe. The antipsychotic drug should be stopped in all who experience and another antipsychotic agent should be substituted. Benzodiazepine, calcium channel blockers, and beta blockers are sometimes helpful in decreasing symptoms. ▪ Neuroleptic Malignant Syndrome: is a rare but potentially fatal condition associated with antipsychotic drugs. Predisposing factors include excess agitation, exhaustion, and dehydration. Neuroleptic malignant syndrome symptoms involve muscle rigidity, hyperthermia, altered mental state, profuse diaphoresis, blood pressure fluctuations, tachycardia, dysrhythmias, seizures, acute renal failure, respiratory failure, and coma. Treatment for NMS involves immediate withdrawal of antipsychotics, adequate hydration, hypothermic blankets, and administration of antipyretic’s, benzodiazepines, and muscle relaxants such as dantrolene. ▪ Atypical Antipsychotics: make up the 2nd category of antipsychotics. Klonopin, discovered in the 1960s and made available in Europe in 1971, was the 1st and atypical antipsychotic agent. Atypical antipsychotics are effective for treating schizophrenia and other psychotic disorders in patients who do not respond to or are intolerant of typical antipsychotics. Because of their decreased side effects, atypical antipsychotics are often used instead of traditional typical antipsychotics as first-line therapy. Chapter 23: Antidepressants and Mood Stabilizers ▪ Tricyclic Antidepressants: I used to treat major depression because they are effective and are less expensive than SSRIs and other drugs. The action of TCAs is to block the uptake of the neurotransmitters norepinephrine and serotonin in the brain. The clinical response of TCAs occurs after 2 to 4 weeks of drug therapy. If there is no improvement after 2 to 4 weeks, the antidepressant is slowly withdrawn and then another antidepressant is prescribed. Polydrug therapy, the practice of giving several antidepressants or antipsychotics together should be avoided if possible because of potential serious side effects. o The effectiveness of TCAs in treating major depression is well documented. This group of drugs elevates mood, increases interest in daily living and activities, and decreases insomnia. For agitated depressed persons, amitriptyline, doxepin, or trimipramine may be prescribed because of their highly sedate effects. TCAs are often given at night to minimize problems caused by their sedate of action. When discontinuing TCAs, the drug should be gradually decreased to avoid withdrawal symptoms such as nausea, vomiting, anxiety, and akathisia. Imipramine hydrochloride is used for the treatment of enuresis (involuntary discharge of urine during sleep in children). o The TCA drugs include amitriptyline, imipramine, trimipramine, doxepin, desipramine, nortriptyline, and protriptyline. o Side Effects and Adverse Reactions- the TCAs have many side effects: orthostatic hypotension, sedation, anticholinergic effects, cardio toxicity, and seizures. Rising from a sitting position to rapidly can cause dizziness and lightheadedness (orthostatic hypotension), so the patient should be instructed to rise slowly to a upright position. The TCAs block the histamine receptors, thus sedation is likely to occur initially but decreases with continuous use of the drug. Because TCAs block the cholinergic receptors, they can cause anticholinergic effects such as tachycardia, urinary retention, constipation, dry mouth, and blurred vision. Other side effects of TCAs include allergic reactions (skin rash, pruritus, and petechiae) that require close monitoring of blood cell counts. Amitriptyline may lead to symptoms of extrapyramidal syndrome (EPS). Clomipramine can cause neuroleptic malignant syndrome. Because this seizure threshold is decreased by TCAs, patients with seizure disorders may need TCA dose adjustment. The most serious adverse reaction to TCAs is cardio toxicity, such as dysrhythmias that may result from high doses of the drug. o Drug Interactions- alcohol, hypnotics, sedatives, and barbiturates potentiate central nervous system depression when taken with TCAs. Concurrent use of MAOIs with amitriptyline may lead to cardiovascular instability and toxic psychosis. Antithyroid medications taken with amitriptyline may increase the risk of dysrhythmias. ▪ Selective Serotonin Reuptake Inhibitors (SSRI): block the reuptake of serotonin into the nerve terminal of the CNS, thereby enhancing its transmission at the serotonergic synapsis. These drugs do not block the uptake of dopamine or norepinephrine, and they do not block cholinergic and alpha 1-adrenergic receptors. SSRIs are more commonly used to treat depression than are TCAs, and they have fewer side effects than TCAs. o The primary use of SSRIs is for major depressive disorder. They are also effective for treating anxiety disorders such as obsessive-compulsive disorder, panic disorders, phobias, posttraumatic stress disorder, and other forms of anxiety. Fluvoxamine is useful for treating OCD in children and adults. SSRIs have also been used to treat eating disorders and selected drug abuse. Miscellaneous uses for SSRIs include decreasing premenstrual tension syndrome, preventing migraine headaches, and preventing or minimizing aggressive behaviors in patients with borderline personality disorders. o The SSRIs include fluoxetine, fluvoxamine, sertraline, paroxetine, citalopram, and escitalopram. Fluoxetine has been effective in 50% to 60% of patients who fail to respond to TCA therapy. The US FDA approved a weekly delayed-release fluoxetine dose of 90 mg. However, before taking the weekly dose, the patient should respond to a daily maintenance dose of 20 mg per day without serious side effects. o Many SSRIs have a interaction with grapefruit juice that can lead to possible toxicity. It is recommended that daily intake be limited to 8 ounces of grapefruit juice or one half of a grapefruit. ▪ Monoamine Oxidase Inhibitors (MAOI): the enzyme monoamine oxidase (MAO) inactivates norepinephrine, dopamine, epinephrine, and serotonin. By inhibiting MAO, the levels of these neurotransmitters rise. 2 forms for of MAO enzyme exist in the body. For the treatment of depression, MAOIs are as effective as TCAs; however, because of adverse reactions, such as the risk of hypertensive crisis resulting from food and drug interactions, only 1% of patients who take antidepressants take a am AOI. Currently, MAOIs are not the antidepressant of choice and are usually prescribed when the patient does not respond to TCAs or second-generation antidepressants. However, MAOIs are still used for mild, reactive, and atypical depression (chronic anxiety, hypersomnia, fear). MAOIs and TCAs should not be taken together when treating depression. o Drug and Food Interactions- certain drug and food interactions with MAOIs can be fatal. Any drugs that are CNS stimulants or sympathomimetics, such as vasoconstrictor’s and cold medication that contain phenylephrine and pseudoephedrine, can cause a hypertensive crisis when taken with a MAOI. In addition foods that contain tyramine- aged cheese, cream, yogurt, coffee, chocolate, bananas, raisins, Italian green beans, liver, pickled foods, sausage, soy sauce, yeast, beer, and red wines-have symphomimetic like effects that can cause a hypertensive crisis. Am AOI users must avoid these types of food and drugs. Frequent blood pressure monitoring is essential, and patient teaching regarding foods and over-the-counter drugs to avoid is an important nursing responsibility. Because of the danger associated with hypertensive crisis, many psychiatrists will not prescribe MAOIs for depression unless other drugs have failed to be effective for the patient. However, this group of drugs is effective for treating depression if taken properly. o Side Effects and Adverse Reactions- side effects of MAOIs include CNS stimulation (agitation, restlessness, and insomnia), orthostatic hypotension and anticholinergic effects. ▪ Mood Stabilizers: mood stabilizers are used to treat bipolar affective disorder. Lithium was the 1st drug use to manage this disorder. Some refer to lithium as a anti-mania drug effective in controlling manic behavior that arises from underlying bipolar disorder. Lithium has a calming effect but may cause some memory loss and confusion. It controls any evidence of flight of ideas and hyperactivity. If the person stops taking lithium, manic behaviors may return. Lithium, carbamazepine, valproic acid and divalproex, and lamotrigine are currently first-line drugs for bipolar disorder. o Lithium is a inexpensive drug that must be closely monitored, and it has a narrow therapeutic serum range of 0.82 1.2 mEq/L. serum lithium levels greater than 1.5 may produce early signs of toxicity. The serum lithium level should be monitored by weekly and tell the therapeutic level has been obtained, and then it must be monitored at least every one to 2 months on the maintenance dose. Serum sodium levels also need to be monitored because lithium tends to deplete sodium. Lithium must be used with caution, if at all, by patients taking diuretics. o Side Effects and Adverse Reactions- the many side effects of lithium-dry mouth, thirst, increased urination (loss of water and sodium), weight gain, bloated feeling, metallic taste, and edema of the hands and ankles-can be annoying to the patient. If taken during pregnancy, with him may have teratogenic effects. ▪ Lithium and nonsteroidal anti-inflammatory drugs (NSAIDs) should not be given together, as NSAIDs may increase lithium levels. Caffeine and loop diuretics may decrease lithium levels. Lithium should be prescribed with extreme caution for patients who have a cardiovascular disease due to an increased risk of lithium toxicity. Frequent monitoring of lithium levels is necessary. Caution must be used with patients afflicted by thyroid disease, as hypothyroidism may occur. Chapter 24: Anti-inflammatories ▪ Nonsteroidal Anti-inflammatory Drugs: include aspirin and aspirin like drugs that inhibit the enzyme COX, which is needed for the biosynthesis of prostaglandins. These drugs may be called prostaglandin inhibitors with varying degrees of analgesic and antipyretic effects, but they are used primarily as anti-inflammatories to relieve inflammation and pain. There antipyretic effect is less than their anti-inflammatory effect. With several exceptions, NSAID preparations are not suggested for use in alleviating mild headaches and mild elevated temperature. Preferred drugs for headaches and fever are aspirin (adults only for fever), acetaminophen, and ibuprofen. NSAIDs are more appropriate for reducing swelling, pain, and stiffness in joints. o Most NSAIDs cost more than aspirin. Other than aspirin, only NSAIDs that can be purchased over-the-counter are ibuprofen and naproxen. All other NSAIDs require up his prescription. Examples of prescription products on the market that contain NSAIDs contents alone or in combination include celecoxib, meloxicam, oxaprozin, nabumetone, sulindac, and ketorolac. If a patient can take aspirin for the inflammatory process without gastrointestinal (GI) upset, salicylate products are usually recommended. ▪ There are 7 groups of NSAIDs: • Salicylates • Para-chlorobenzoic acid derivatives, or indoles • Phenylacetic acids • Propionic acid derivatives • Fenamates • Oxicams • Selective COX-2 inhibitors ▪ The 1st 6 NSAID groups on the list are known as first-generation NSAIDs, and the COX-2 inhibitors are called second-generation NSAIDs o Salicylates- aspirin comes from the family of Salicylates derived from salicylic acid. Aspirin is also called a acetylsalicylic acid after the acetyl group used in its composition. Aspirin was developed in 1899 making it the oldest anti-inflammatory agent. It was the most frequently used anti-inflammatory agent before the introduction of ibuprofen. Aspirin is a prostaglandin inhibitor that decreases the inflammatory process. It is also considered a antiplatelet drug for patients with cardiac or cerebrovascular disorders; aspirin decreases platelet aggregation, and thus blood clotting is decreased. Because high doses of aspirin are usually needed to relieve inflammation, gastric distress-which includes anorexia, dyspepsia, nausea, vomiting, diarrhea, constipation, abdominal pain, heartburn, and flatulence-is a common problem. In such cases, enteric coated tablets may be used. Aspirin should not be taken with other NSAIDs because a decrease the blood level and effectiveness of NSAIDs. ▪ Hypersensitivity to Salicylate Products: patients may have hypersensitivity to aspirin. Tinnitus (ringing in the ears), vertigo (dizziness), and bronchospasm’s- especially in asthmatic patients ▪ Warn patient not to administer aspirin for virus or flu symptoms in children. Reye syndrome (vomiting, lethargy, delirium, and coma) has been linked with aspirin and viral infections. Acetaminophen is usually prescribed for colds and flu symptoms. ▪ Direct patients to report side effects such as drowsiness, tinnitus, headaches, flushing, dizziness, G.I. distress, G.I. bleeding, visual changes, and seizure. ▪ Anti-gout Drugs: gout is an inflammatory condition that affects joints, tendons, and other tissues. It may be called gouty arthritis. The most common site of acute gouty inflammation is at the joint of the big toe. Gout is characterized by a uric acid metabolism disorder and a defect in purine (products of certain proteins) metabolism, which results in a increase in urates (a uric acid salts) and a accumulation of uric acid (hyperuricemia) or a ineffective clearance of uric acid by the kidneys. Uric acid solubility is poor in acid urine, and urate crystals may form, causing urate calculi. o To promote uric acid excretion and to prevent renal calculi, fluid intake should be increased while taking antigout drugs. Foods high in purine—such as organ meats, sardines, salmon, gravy, herring, liver, and meat soups—and alcohol, especially beer, should be avoided. Alcohol causes both an overproduction and underexcretion of uric acid. To reduce acidity, acetaminophen should be taken for discomfort instead of aspirin (salicylic acid). Chapter 25: Analgesics ▪ Nonopioid Analgesics: such as aspirin, acetaminophen, ibuprofen, and naproxen are less potent than opioid analgesics and are used to treat mild to moderate pain. Non-opioids are usually purchased over-the-counter, but cyclooxygenase 2 (COX-2) inhibitors require prescription. Non- opioids are effective for the dull, throbbing pain of headaches, dysmenorrhea (menstrual pain), inflammation, minor abrasions, muscular aches and pain, and mild to moderate arthritis. Most analgesics also have a antipyretic effect and will lower an elevated body temperature. Some, such as aspirin, will have anti-inflammatory and antiplatelet effects as well. o Nonsteroidal Anti-inflammatory Drugs- all NSAIDs have a analgesic effect as well as a antipyretic and anti-inflammatory action. NSAIDs such as aspirin, ibuprofen, and naproxen can be purchased over-the-counter. Aspirin, is the oldest non-opioid analgesic drug still in use. ▪ The CDC recommends aspirin products not be given to children and adolescents younger than 19 years of age during episodes of fever or viral illness because of the danger of Reye syndrome. Reye syndrome is a rare but serious condition associated with viral infections treated with salicylates that causes swelling of the brain and liver. In these circumstances, acetaminophen is recommended instead of aspirin. ▪ In addition to its analgesic, antipyretic, and anti-inflammatory properties, aspirin decreases platelet aggregation (clotting). Some healthcare providers made therefore prescribe one 81 mg, 162 mg, or 325 mg aspirin tablet every day or one 325 mg tablet every other day as a preventative measure against transient ischemic attacks (TIAs, or mini stroke), heart attacks, or any thromboembolic episode. ▪ Aspirin and other NSAIDs relieve pain by inhibiting biosynthesis of prostaglandins by different forms of the COX enzymes. Aspirin is the drug of choice for alleviating pain and inflammation in arthritic conditions, but when given in high doses, severe gastrointestinal irritation and possible ulceration develop and approximately 20% of patients. o Side Effects and Adverse Reactions- a common side effect of NSAIDs is gastric distress, including anorexia, nausea, vomiting, and diarrhea. These drugs should be taken with food, at mealtime, or with a full glass of fluid to help reduce this problem. Excessive bleeding might occur as a side effect if a NSAID is taken for dysmenorrhea during the 1st 2 days of menstruation. Adverse effects of salicylate toxicity includes tinnitus, vertigo, hyperventilation, and potential metabolic acidosis. ▪ Some patients are hypersensitive to aspirin. Dyspnea, bronchospasm, and urticarial are some of the symptoms that indicate anaphylaxis to salicylate products. Certain foods also contain salicylates: prunes, raisins, paprika, and licorice. ▪ Acetaminophen- the analgesic acetaminophen, a para-aminophenol derivative, was 1st marketed in the mid-1950s as an analgesic and antipyretic drug use for muscular aches and pains and 4 fever caused by viral infections in infants, children, adults, and older adults. Acetaminophen is a non-opioid drug, but it is not a NSAID . Because acetaminophen does not have the anti- inflammatory properties of aspirin, it is not the drug of choice for any inflammation process. Acetaminophen is a safe, effective drug when used at therapeutic doses, causes little to no gastric distress, and does not interfere with platelet aggregation. There is no link between acetaminophen and Reye syndrome, and unlike aspirin and NSAIDs, it does not increase the potential for excessive bleeding if taken for dysmenorrhea. o Side Effects and Adverse Reactions: an overdose of acetaminophen can be extremely toxic to liver cells; death can occur in 1 to 4 days from hepatic necrosis. If a child or adult ingest excessive amounts of acetaminophen tablets or liquid, a poison control center should be contacted immediately, and the child or adult should be taken to the emergency department. Early symptoms of hepatic damage include nausea, vomiting, diarrhea, and abdominal pain. ▪ Opioid Analgesics: opioid analgesics, called opioid agonists, are prescribed for moderate to severe pain. Morphine, a prototype opioid, is obtained from the sap of seedpods of the opium poppy plant. Codeine is another drug obtained from opium. In the past decades, many synthetic and semi synthetic opioids have been developed. o Although non-opioid analgesics act on the peripheral nervous system at the pain receptor sites, opioid analgesics act mostly on the central nervous system. Opioids act primarily by activating the μ-receptors, but they also exert a weak activation of the kappa (κ) receptors. Analgesia, respiratory depression, euphoria, and sedation are effects of μ-receptor activation. Activation of κ-receptors leads to analgesia and sedation but has no effect on respiratory depression and euphoria. o Opioids not only suppress pain impulses but also suppress respiration and coughing by acting on the respiratory and cost centers in the medulla of the brainstem. One example of such an opioid is morphine, a potential analgesic that can readily depress respirations. Codeine is not as potent as morphine, but it also relieves moderate to mild pain and suppresses cough, which allows it to be classified as a antitussive. Most opioids have a cough suppression effect. Pharmacokinetics: (what we do to drugs) the process of drug movement throughout the body that is necessary to achieve drug action. INCLUDES 4 PROCESSES: Absorption, Distribution, Metabolism, and Excretion. Absoption: the movement of the drug into the bloodstream after administration. Absoption/dissolution: drugs in solid form disintegrate into small particles and combine with a liquid to form a solution. This need to happen in order for the drug to be absorbed into the GI tract into the bloodstream. Parenteral drugs DO NOT pass through the GI tract these include: eye drops eardrops, nasal sprays, inhalents, transdermal, topical, and sublingual medications. Drugs are absorbed faster in in acidic fluids with a PH of 1 or 2 rather than alkaline fluids with a PH 7 or greater. Very young and very old have less gastric acidity so drug absorption is generally slower for drugs absorbed in the stomach. Excipients: fillers and inert substances: are used in drug preparation to allow drug to take on a particular size and shape and to enhance drug dissolution. Enteric coated drugs (EC): resist disintegration in the gastric acids of the stomach, disintegration takes place when it reaches the alkaline environment of the SMALL INTESINE – these drugs can remain in the stomach for a long period of time so their effect might be delayed. DO NOT CRUSH enteric coated and sustained release capsules because it will alter the place and time of absorption. Passive transport: (does not require ATP) includes diffusion and facilitated diffusion: Diffusion- drugs move across the cell membrane from higher concentration to lower concentration. Facilitated Diffusion_ relies on a carrier protein to move the drug from areas of higher concentration to lower concentration. Active Transport: (Requires ATP) requires a carrier, such as an enzyme or protein to move the drug against a concentration gradient this requires ATP. Includes the process of PINOCYTOSIS- a process by which cells carry a drug across their membrane by engulfing the drug particles in a vesicle. CELL EATING Lipid Soluble Drugs: mucous membrane in the GI tract is composed of lipids and proteins such that lipid soluble drugs are able to pass rapidly through the mucous membrane. Water Soluble Drug: Need a carrier(enzyme or protein) to pass through the mucous membrane. (DRUGS THAT ARE LIPID SOLUBLE AND NON-IONIZED ARE ALWAYS ABSORBED FASTER THAN WATER SOLUBLE DRUGS) Things that affect Absorption: BLOOD FLOW, PAIN, STRESS, HUNGER, FASTING, FOOD,AND PH. IM: are absorbed faster in the muscles that have increased blood flow (deltoid) then those that do not (gluteous maximus). Faster absorption than SUBQ SUB Q: tissue has decreased blood flow when compared w/ muscle, so absorption is slower. However, they have a more rapid and predictable rate of absorption than those given by mouth. Rectal dugs: absorbed slower than drugs given by oral route. First Pass Effect: following absorption form the GI tract they pass from the intestinal lumen to the liver via the portal vein. In the liver some drugs are metabolized to an inactive form and are excreted thus reducing the amount of active drug available to exert a pharmacologic effect this is referred to as first pass. Most oral drugs are effected to some degree by first pass metabolism. (lidocaine and nitroglycerins are not given orally because they have extensive first pass metabolism and most of the drug is inactivated. Bio Availability: refers to the percentage of administered drug available for activity. Orally administered drugs. Bio availability is affected by absorption and first pass metabolism. IV drugs always have 100% bio availability. Factors affecting Bio Availability: drug form, route of administration, Changes in liver metabolism caused by liver dysfunction or inadequate hepatic blood flow- a decrease in liver function or hepatic blood flow can increase the bio availability of a drug but only if the drug is metabolized by the liver. Less drug is destroyed by hepatic metabolism in the presence of a liver disorder. Distribution: the movement of the drug from circulation to the body tissue is influenced by the rate of blood flow to the tissue, the drugs affinity to the tissue and protein binding. Protein Binding: as proteins are distributed in the plasma many bind with plasma proteins. Drugs that are more than 90% bound to protein are known as highly protein bound drugs and if less than 10% are weakly protein bound. Free Drugs: the portion of rugs bound to protein is inactive because it is not available to interact with the tissue receptors and is not able to exert a pharmacologic effect. The portion that remains unbound is free active drug. Free drugs are able to exit blood vessels and reach their site of action causing a pharmacologic response. Highly Protein Bound: when 2 highly protein bound drugs are administered together they compete for protein binding sites leading to an increase in free drug being released into circulation. This could cause drug toxicity. Can also occur in patient with kidney or liver disease or malnourished may have lower serum albumin levels. Always be aware of patient albumin levels before administering medication. Blood Brain Barrier: blood vessels in the brain have a special endothelial lining where cells are pressed tightly together(tight Junction) this lining is referred to as the blood brain barrier. The BBB protects the brain from foreign substances which include about 98% of drug on the market. Drugs such as Benzodiazepines are highly lipid soluble and low of molecular weight and are able to cross the BBB through diffusion. Water soluble drugs and drugs that are not bound to transport proteins (free drugs) are not able to cross the BBB more difficult for these drugs to reach the brain. Metabolism: the process by which the body chemically changes the drugs into a form that can be excreted. THE LIVER IS THE PRIMARY SITE FOR METABOLISM. Majority of drugs are lipid soluble thus the liver metabolizes the lipid soluble drug substance to a water soluble substance for renal excretion. Liver disease such as cirrhosis or hepatitis alter drug metabolism by inhibiting the drug metabolizing enzymes in the liver. WHEN THE DRUG METABOLISM RATE IS DECREASED, EXCESS DRUG ACCUMULATION CAN OCCUR AND LEAD TO TOXICITY. Half Life: the time it takes for the amount of the drug in the body to be reduced by half. With liver or kidney dysfunction the half-life is prolonged. By knowing the half-life the time it takes for the drug to reach a steady state (plateau drug level) can be determined. Loading Dose: in the case of drugs with long half-lives, it may not be acceptable to wait for a steady state to be achieved. By giving a large initial dose (loading dose) that is significantly higher than maintenance dosing, therapeutic effects can be obtained while a steady state is reached. Drug Excretion: the main route of excretion is through the kidneys, drugs are also excreted through bile(liver), lungs, saliva, sweat, and breast milk. Kidneys filter free drugs, water soluble drugs, and drugs that are unchanged. Kidney disease or impairment may cause drug accumulation and result to toxicity and adverse drug reactions. Pharmacodynamics: (what drugs do to us) the study of the effects of drugs on the body. Drugs act within the body to mimic the actions of the bodys own chemical messengers. Dose response relationship: the bodys physiological response to changes in drugs concentration at the site of action. Potency: the amount of the drug needed to elicit a specific physiological response to a drug. Maximal efficacy: the point at which increasing the drug dosage no longer increases the desired therapeutic response. Therapeutic Index: level of the drug needed for the drug to be effective. Toxic Effect: too much of the drug build up in the system. Primary effect: desirable response. Secondary effect: desirable or undesirable side effect. Onset: The time it takes the drug to reach its minimal effective level. Peak: highest level of drug concentration. Duration: the length of time taken for the drug exerts a therapeutic effect. Receptor theory: to activate a receptor to produce a response or to inactivate a receptor blocking response. Agonist: activate receptors Antagonists: Prevent receptor activation and block response. Non-Specific drugs: drugs that affect multiple receptors Non-Selective: affect multiple receptors (both non-specific and non-selective effect multiple body systems) Mechanisms of action: stimulation, depression, irritation, replacement, cytotoxic (cancer drugs), antimicrobial, modification of immune system (vaccines). Pharmacogenetics: the study of genetic factors that influence an individual’s response to a specific drug. Tolerance: decreased responsiveness to a drug over the course of therapy requiring a higher dose to to achieve therapeutic response. Placebo Effect: a drug response not attributed to the chemical properties of the drug. Additive Effects: 2 drugs administered in combination, and the response is increased beyond what eith could produce alone. Adrenergic agents: Epinephrine, norepinephrine, Amphetamine, ephedrine. Direct-Acting: Epinephrine and nor-epinephrine directly stimulate adrenergic receptor. Indirect –Acting: Amphetamine stimulates release of norepinephrine from terminal nerve endings. Mixed – Acting: Ephedrine stimulates adrenergic receptor sites and stimulates release of norepinephrine. Adrenergic Antagonists: Beta Blockers inhibit the release of epinephrine and norepinephrine. Alpha 1 receptors: increase cardiac contractility, vasoconstriction, dilate pupils, decrease salivary gland secretions, increase bladder and prostate constriction. Alpha 2 Receptors: inhibit norepinephrine release, promote vasodilation, decrease BP, decrease GI motility and tone. Beta 1 Receptors: Increase cardiac contractility, Increase HR, increase Renin secretion, and increase BP. Beta 2 Receptors: decrease GI tone and motility, Bronchodilation, increase blood flow in skeletal muscles, relaxes the smooth muscles of the uterus, activates liver glycogenolysis increasing blood glucose. Adrenergic Agonist/sympathimimetics: epinephrine, albuterol. Catacholamines: produce sympathetic response , epinephrine, norepinephrine, dopamine. Non-Catacholamines: stimulate adgrenergic receptors, Albuterol. Epinephrine: alpha1 increase BP, Beta 1 increase HR, Beta 2 promote Bronchoditalion. Contraindicated in cardiac arrhythmias, HTN, hyperthyroidism, diabetes, pregnancy. (Antagonist-Beta Blockers / metoprolol, atenolol) (antidote-phentolomine mesylate for extravasation in IV dopamine) Albuterol: Acts on Beta 2 receptors promotes Bronchdilation. Sames contraindications as epinephrine may increase effect with other sympathomimetics. ( Antagonist- Beta Blockers/ metoprolol/ atenolol) do not use with MAOI’s and tricyclic antidepressants . Adrenergic agonists may result in rebound nasal congestion. Clonadine also an adrenergic agonist used to tx HTN. Cholinnergic Drugs: work on the parasympathetic NS enhance the action of acetycholine affects are increased salivation, active digestion, skeletal muscle relaxation, decreased HR, Decreased BP,Blood vessels relax. Anticholinergic drugs: work on the sympathetic NS block acetylcholine and cause a decrease in parasympathetic affects. Effects of anticholinergics are reduced smooth muscle spasm, decreased digestive tract movement, pupil dilation, decreased salivation, increased HR, increased airway relaxation. Cholinergic agonist- Bethanechol: tx of urinary retention, promotes contraction of the bladder. contraindicated in patients with asthma. adverse reaction –Bronchoconstriction. Assess lung sounds for rales and crackling sounds from fluid congestion in the lungs. Anticholinergic – Atropine: tx of sinus bradycardia or to dilate pupils for eye exam and pre-op reductions of salivation. action to increase HR or decrease GI and Respiratory secretions. Contraindicated patients with Glaucoma. Monitor I&O, bowel sounds, avoid hot environments, wear sunglasses. Anticholinergic-Benzotropine: Anticholinergics can also be used to treat parkinsonism used to treat EPS except tardive dyskinesia. Decreases involuntary symptoms. Cholinergic- Aricept: used to improve cognitive function in alzheimer’s disease. Increase acetylcholine in the brain and improves cognitive function. Antiseizure drugs: tx of seizure disorders (epilepsy) abnormal electric discharges from cerebral neurons. Action: stabilize nerve cell membrane suppress sodium influx, suppress calcium influx, enhance action of GABA, promote GABA release. Hydantions/ Phenytoin: therapeutic serem level 10-20 mcg/ml, contraindicated in pregnancy, interactions decreased effects with folic acid and anticoagulants and oral contraceptives. Barbiturates/ Phenobarbitol: enhances GABA activity therapeutic serum range 20-40mcg/ml Benzodiazepines/diazepam: tx status epilepticus short term effect IV administration given first before any other seizure drugs during and active seizure usually followed by phenytoin IV and if continued seizure give midazolam or propofol . Seizure drugs inhibit vitamin K and increase loss of folic acid and are not safe during pregnancy (teratogenic) patient are at risk for falls and phenytoin levels need to be monitored , thrombocytopenia is an adverse reaction Antipsychotics/ Haloperidol -nonphenothiazine: Blocks dopamine receptors. Contraindicated in Glaucoma, CNS depression, severe liver, kidney and cardiovascular disease. Avoid alcohol, and increased toxicity with anticholinergics. Antipsychotics/Fluphenazine-phenothiazine: blocks dopamine receptors, increased depression when taken with other CNS depressants, increase EPS Anxiolytics: Buspirone binds to serotonin and dopamine receptors, not a controlled substance does not effect GABA . Avoid Grafruit Juice. Mood Stabalizer/Lithium: increased receptor sensitivity to serotonin, serum lithium levels 1.0-1.5 greater can lead to toxicity. Levels must be monitored. Avoid caffeine and maintain adequate sodium intake. Monitor serum electrolytes. Stimulants: used for ADHD, narcolepsy, reversal of respiratory distress. Categories -Amphetamines ,Analeptics/caffeine, Anorexiants. Methylphenidate: modulates serotonergic pathways by affecting changes in dopamine transport. Caffeine may increase effects, decreased effects of antihypertensives, may alter insulin effects. Causes dry mouth use sugarless gum, take before meals, do not stop abruptly. Anti-Parkinson Drugs/ Carbadopa/Levodopa: converts to dopamine and increases mobility, should always be taken together carbidopa helps levodopa reach the brain. Monitor for agranulocytosis. Alzheimer Drugs/ Rivastigmine: allows more acetylcholine in neuron receptors. Take without food, assess for hx of glaucoma. Slows the progression of alzheimers disease. Neuromuscular Disorders/ Myasthenia Gravis: autoimmune disorder, causes skeletal weakness, respiratory muscle weakness, paralysis and arrest, MYASTHENIC CRISIS – treat with neostigmine. CHOLINERGIC CRISIS-treat with Atropine. To differentiate between Myasthenic or Cholinergic crisis administer Edrophnium symptons will worsen if its Cholinergic crisis. Neostigmine: helps increase muscle strength. Antiinflammatories/ Nsaid’s : inhibit biosynthesis of prostaglandins. Salicylates: ( aspirin) do not take with other Nsaid’s , avoid cold and flu meds, prolonged bleeding . monitor serum salicylate level. So not give to children for virus or flu symptoms to avoid reye syndrome. Ibuprofen: most widely used NSAID, inhibits prostaglandin synthesis. Causes Gastric distress and bleeding, monitor for black tarry stools, avoid alcohol, patients with peptic ulcer should not use. Antigout drugs/ Colchicine: inhibits migration of leukocytes to inflamed site. Alleviates gout symptoms, take with food to avoid GI distress, avoid alcohol especially beer. Purine containing foods. [Show More]

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