Pharmacology MDA 224 PHARMACOLOGY; Drug action, uses and caution 2020|2021

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ANTIBIOTICS 1) Cephalosporins Action: cephalexin (Keflex) 1st generation broad-spectrum active against gram(+) bacteria, poor distribution to CSF each generation has increasing bactericidal activi... ty to break down cefuroxime (Ceftin) 2nd generation gram(-) bacteria and anaerobes, and to reach the cerebrospinal fluid active against gram(+) and gram(-) bacteria, poor distribution to CSF strength increases with generation ceftriaxone (Rocephin) 3rd generation cephalosporins interfere/inhibit bacterial wall synthesis active against gram(-) bacteria, crosses into CSF the cell weakens, swells, bursts + dies from inc osmotic pressure inside the cell cefepime (Maxipime) 4th generation inc cephalosporin resistance is caused by production of beta-lactamases active against gram(+) and gram(-) bacteria, crosses into CSF 2) Tetracycline Action: tigecycline (Tygacil) broad-spectrum bacteriostatic abx that suppresses bacterial growth by inhbiting protein synthesis routes: IM, IV, PO inhibits growth of gram(-) and gram(+) bacteria 3) Metronidazole (Flagyl) Action: "Metallic bitter taste" interacts with anaerobic pathogens' + protozoa's DNA to cause strand breakage + loss of helical structure class: antibacterial the impairment of the DNA is responsible for the antimicrobial + mutagenic actions of the medication 4) Isoniazid (INH) Action: bacteriostatic to "resting organisms" class: antimycobacterial, antituberculosis agent bactericidal to actively dividing organisms routes: IM, PO interferes with biosynthesis of bacterial protein, nucleic acid + lipids 5) Aminoglycosides Action: amikacin (Amikin) narrow-spectrum abx effective against aerobic gram(-) bacteria gentamicin disrupts cell syntheis of protein kanamycin used for serious infections tobramycin routes: IV or topical, (poorly absorbed orally) 6) Aminoglycoside Toxicity ethacrynic acid (Edecrin) increases ototoxicity ethacrynic acid (Edecrin) is a diuretic, which is used to treat fluid retention (edema) 7) Fluoroquinolones Action: ciprofloxacin (Cipro) bactericidal ofloxacin (Floxin) broad-spectrum against gram(-) / gram(+) bacteria, but not against anaerobic infections moxifloxacin (Avelox) inhibits growth of gram(-) and gram(+) bacteria inhibits DNA enzyme that interferes with replication class: antibacterial "TWO QTs SAY NO TO OBs" abx contraindicated in pregnancy: MCAT Quinolones + Tetracyclines are Metronidazole CONTRAINDICATED during pregnancy Chloramphenicol Aminoglycoside Tetracycline 8) Penicillin (PCN) Action: narrow spectrum that are penicillinase sensitive bactericidal penicillin G (Bicillin), penicillin V disrupts + weakens cell wall, leading to cell lysis + death penicillinase-resistant (antistaphylococcal penicillins) nafcillin, oxacillin, dicloxacillin broad-spectrum (aminopenicillins) ampicillin, amoxicillin, amoxicillin/clavulanate (Augmentin) extended-spectrum penicillins (antipseudomonal penicillins) ticarcillin (Ticar), ticarcillin/clavulanate (Timentin), piperacillin/tazobactam (Zosyn) 9) Macrolides Action: "ACE" binds with ribosomal receptor sites in susceptible organisms to inhibit Azithromycin bacterial protein synthesis Clarithromycin Erythromycin routes: IV, PO 10) Vancomycin Action: ANTIRETROVIRALS Action: NRTI (nucleoside/nucleotide reverse transcriptase inhibitors) NRTI zidovudine (Retrovir) terminates/inhibits HIV replication NNRTI (non-nucleoside reverse transcriptase inhibitors) NNRTI efavirenz (Sustiva) blocks/disrupts enzyme activity PI (protease inhibitor) PI lopinavir/ritonavir (Kaletra) prevents/inhibits maturation of HIV CCR5 antagonist (chemokine receptor 5 antagonist) CCR5 antagonist maraviroc (Selzentry) blocks viral entry HIV-fusion inhibitor HIV-fusion inhibitor enfuvirtide (Fuzeon) blocks viral entry + replication into CD4-T cells Anticoagulants + Hematinics 1) Heparin Action: anticoagulants exert a direct effect on blood coagulation by enhancing the inhibitory routes: IV, subQ actions of antithrombin on several factors essential to normal blood clotting, thereby apply firm pressure for 1-2 minutes blocking the conversion of prothrombin to thrombin + fibrinogen to fibrin do not massage heparin prevents fibrin from forming a clot heparin helps prevent deep vein thrombosis (DVTs) + pulmonary emboli heparin does not break up a clot, it just keeps it from coming together 2) Enoxaparin (Lovenox) Action: low-molecular-weight heparin route: subQ has great affinity for factor Xa in providing anticoagulation action provides a predictable anticoagulant response 3) Warfarin Sodium (Coumadin) Action: warfarin (Coumdin) is an anticoagulant that antagonizes vitamin K vitamin K is necessary for the synthesis of clotting factors VII, IX, X + prothrombin as a result, it disrupts the coagulation cascade 4) Epoetin Alfa (Procrit) Action: Epoetin (Procrit) is synthetic erythropoietin, which increases RBC production routes: IV, subQ Epoetin (Procrit) helps the kidneys stimulate bones for their blood production 5) Iron Supplements Action: (Oral Ferrous Iron Salts) hematinic agent used in the production of normal hGb + RBCs for used for the tx + prevention of iron deficiency anemia transportation + utilization of oxygen ferrous sulfate (Feosol) ferrous gluconate (Fergon) 6) Thrombolytics Action: "clot busters" unclogs veins and arteries "ART" converts plasminogen to plasmin, an ezyme that acts to digest the fibrin matrix of clots Activase (Alteplase) (tPA: tissue plasminogen activator) dissolves existing thrombi rather than prevent them from occurring Reteplase Tenecteplase routes: IV, infusion pump 7) Clopidogrel (Plavix) Action: "when platelets gather together, use Plavix for crowd control" suppresses platelet aggregation in arterial circulation antiplatelet action occurs within 2 hours of administration class: antiplatelet 8) Argatroban Action: directly inhibits the action of thrombin in the clotting mechanism class: anticoagulant protects the pt + platelets from heparin-induced thrombocytopenia (HIT) route: IV Anticoagulants for ATRIAL FIBRILLATION Action: 9) Dabigatran (Pradaxa) prevents clots from forming when the heart is in a-fib direct thrombin inhibitor dabigatran (Pradaxa) 10) Rivaroxaban (Xarelto) directly inhibits thrombin formation direct factor Xa inhibitor prevents conversion of fibrinogen to fibrin prevents activation of factor XIII class: anticoagulants prevents the conversion of soluble fibrin into insoluble fibrin route: PO rivaroxaban (Xarelto) inhibits production of thrombin by binding directly with factor Xa CARDIAC 1) ANTIHYPERTENSIVES Action: antihypertensive drugs act on the Ace Inhibitors (end in -pril) vascular, cardiac, renal + sympathetic nervous systems blocks the conversion of angiotensin I to angiotensin II, a vasoconstrictor antihypertensive drugs act to this block causes vasodilation + dec PVR, resulting in dec BP lower BP, cardiac output + peripheral vascular resistance aldosterone is also blocked, causing a dec in sodium + water rentention Beta-Blockers (end in -lol) blood pressure is regulated by cardiac output + peripheral vascular resistance blocks the beta-1 receptors in the heart medications that influence either one of these systems lead to BP control this results in a dec in heart rate + dec force of contraction antihypertensive drugs that influence thse systems to lower BP are ACE inhibitors (angiotensin-converting enzyme) Calcium Channel Blockers Beta-Blockers (beta-adrenergic blockers) blocks calcium influx into beta-receptors, dec the force of myocardial contration, Calcium Channel Blockers reduces HR + dec PVR amlodipine (Norvasc) nifedipine (Procardia) verapamil (Calan Isoptin) diltiazem (Cardizem) 2) Ace Inhibitors Action: suppresses formation of angiotensin II from the renin-angiotensin-aldosterone system reduces peripheral vascular resistance improves cardiac output 9) Beta Blockers Action: block sympathetic nervous catecholamines, resulting in reduced renin + aldosterone release + fluid balance vasodilation of arterioles leads to a dec in pulm vascular resistance + BP [Show More]

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