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Antiarrhythmics: chem, class, MOA, AP, Pcol, SE, therapeutic
Antiarrhythmic drugs: med chem, class, mechanism of action, action potential effects, unique pharmacology, side effects, therapeutics
20
Pharmacology
Professional
04/07/2011

Additional Pharmacology Flashcards

 


 

Cards

Term
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Definition

Drug: Quinidine

Class: IA

MOA: block Na in, block K out

AP: increase 0, 1, 2, 3

Pcol: alpha block, antimuscarinic

SE: cinchonism = diarrhea, hypotension, ringing ears

Chem: antimalarial diastereomer, highly protein bound, DI w/ digoxin, basic charged tertiary amine

Forms: sulfate = oral IR & SR, gluconate = oral SR & injection, polygalacturonate = oral slow release

Term
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Definition

Drug: Procainamide

Class: IA

MOA: block Na in, block K out

AP: increase 0, 1, 2, 3

Pcol: ganglionic block, weak anticholinergic

SE: SLE, bone marrow suppression

Chem: aromatic N, amide, tertiary alkyl amine,

50% excreted unchanged = for good kidney & poor renal, procaine = ester analog,

aromatic acetylation = NAPA w/ increased K binding

Therapeutics: useful for atrial arrhythmias, do not use in renal pts., antihistone DNA Ab test

Term
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Definition

Drug: Disopyramide

Class: IA

MOA: block Na in, block K out

AP: increase 0, 1, 2, 3

Pcol: anticholinergic

SE: potent anti-DUMBBELSS (dry mouth, urine retention, constipation)

Chem: for life threatening arrhythmias, phosphate = H3PO4

Term
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Definition

Drug: Lidocaine

Class: IB

MOA: mild block Na in, increase K out

AP: mild increase 0, 1, 2, decrease 3

Pcol: local anesthetic

SE: paresthesias

Chem: N-dealk to active form then amide hydrolysis...inhibits its own metabolism = t1/2 increases with concentration

Therapeutics: ventricular arrhythmias, IV only, ok in renal pts., [tx] = 1.5-5 mg/L, dose = 1-1.5 mg/kg, max 3 mg/kg, gradually decrease dose if on it for >24h

Term
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Definition

Drug: Tocainide

Class: IB

MOA: mild block Na in, increase K out

AP: mild increase 0, 1, 2, decrease 3

Pcol:

SE: tremors

Chem: less N-dealk and amide hydrolysis, t1/2 = 12h, renal + hepatic CL

Therapeutics: not often used, pulmonary fibrosis, blood dyscrasias, same as mexiletine

Term
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Definition

Drug: Mexiletine

Class: IB

MOA: mild block Na in, increase K out

AP: mild increase 0, 1, 2, decrease 3

Pcol:

SE:

Chem: slow O-dealk but no ester hydrolysis, t1/2 = 12-16h, renal + hepatic CL

Therapeutics: very GI irritating, decrease ICD firing d/t frequent ventricular arrhythmias

Term
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Definition

Drug: Phenytoin

Class: IB

MOA: mild block Na in, increase K out

AP: mild increase 0, 1, 2, decrease 3

Pcol:

SE:

Chem: Na salt form of weak acid, less H2O soluble & uncharged at physio pH, slow IV push d/t 40% propylene glycol & 10% alcohol, IVPB in 0.9% NaCl

Term
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Definition

Drug: Flecainide

Class: IC

MOA: potent block Na in

AP: increase 0, 1, 2, 3

Pcol:

SE: proarrythmia, negative inotrope, CAST

Chem: several O-dealk active metabolite, accumulation increases proarrhythmia

Therapeutics: young Afib, atrial arrhythmias, Tambocor, pt. preference before shock, negative inotrope = careful in HF, only to convert, not for long term use, Afib conversion dose = 300mg, maintenance = 50-150 po q12h

Term
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Definition

Drug: Encainide

Class: IC

MOA: potent block Na in

AP: increase 0, 1, 2, 3

Pcol: PULLED FROM MARKET

SE: proarrythmia, negative inotrope, CAST

Chem: t1/2 2-4h, ODE to MODE with t1/2 = 12h

Term
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Definition

Drug: Propafenone

Class: IC

MOA: potent block Na in

AP: increase 0, 1, 2, 3, *4*

Pcol: BB, CCB (negative inotrope = proarrhythmic), block K out (Torsades unlikely though), anticholinergic

SE: proarrythmia, negative inotrope, anti-DUMBBELSS, taste loss

Chem: propyl-secondary amine-propanol = weak BB

Therapeutics: Rhythmol, increase [digoxin] & [warfarin] d/t 2D6 inhibition

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Term
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Definition

Drug: Moricizine

Class: IA/B/C

MOA: mild block Na in, increase K out

AP: mild increase 0, 1, 2, decrease 3

Pcol: weak D2 block, pheno-thi-az-ine derivative

SE: proarrythmia

Chem:"IC" pheno-thi-az-ine

Term
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Definition

Drug: Propranolol, Esmolol, Acebutolol

Class: II

MOA: BB slow SA & AV firing

AP: increase 3, 4

Pcol: propranol = beta 2

SE: cardiodepression, bronchospasm

Chem:

Term
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Definition

Drug: Sotalol

Class: III

MOA: BB slow SA & AV firing, blocks K out

AP: increase 3, 4

Pcol:

SE: cardiodepression, bronchospasm, Torsades

Chem: S = block K out, R = block K out & BB, aryl sulfonamide, phenethylamine

Therapeutics: Betapace, adjust for renal pts., not used often, a-fib & ventricular arrhythmias

Term
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Definition

Drug: Amiodarone

Class: III  MOA: blocks K out

AP: increase 0, 1, 2, 3, 4

Pcol: class I & III effects, CCB, alpha blocker

SE: pulmonary fibrosis, thyroid toxicity, corneal microdeposits, elevated LFTs, smurfism, Torsades

Chem: t1/2 = 15-100 DAYS, inhibits T3 to T4, I = big drug

ACLS: antiarrhythmic for pulseless arrest (VT/VF)

Therapeutics: Cordarone/Pacerone, DOC for (ventricular) arrhythmias in HF/CAD, increase [digoxin] & [warfarin], cut back/start lower on digoxin, 35% emperical reduction for warfarin, arrest dose = 300 mg IV bolus

Term
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Definition

Drug: Dronedarone

Class: similar to amiodarone (III)

MOA:

AP:

Pcol:

SE:

Chem: t1/2 = 13-19h, F = 4%, met by CYP, fecal elimination

Therapeutics: dose = 400mg BID with meals, CI: HF (but amiodarone ok), 2nd/3rd block, SSS, bradycardia, CYP3A4 inhibitors, QT prolonged, hepatic pts, pregnant/nursing

Term
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Definition

Drug: Ibutilide

Class: III

MOA: blocks K out

AP: increase 3

Pcol:

SE: QT prolongation, Torsades

Chem: unique agent b/c MOA was thought to be increase Na in to balance K out and increase APD, actually just nonselective K block, phenbutylamine

Therapeutics: Afib conversion = 1 mg IV over 10 min, may repeat once

Term
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Definition

Drug: Dofetilide

Class: III

MOA: blocks K out via inhibits inward rectifier K current

AP: increase 3

Pcol:

SE: QT prolongation, Torsades

Chem: eliminated primarily unchanged in urine, minimally metabolized, watch CYP3A4 inhibitors (grapefruit, ery), phenethylamine

Therapeutics: convert/maintain Afib, safe in HF/SHD, cimetidine, verapamil, HCTZ inhibit dofetilide secretion

Term
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Definition

Drug: Verapamil, Diltiazem

Class: IV

MOA: L type CCB

AP: increase 4

Pcol:

SE: cardiodepression

Chem: slow tissue = decrease rate, fast tissue = decrease coordination of impulse with contraction

Term
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Definition

Drug: Digoxin

Class:

MOA: slow AV conduction, vagomimetic

AP: increase 4

Pcol: Na/K ATPase inhibitor

SE: narrow therapeutic window

Chem: watch K, can be proarrhythmatic

Term
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Definition

Drug: Adenosine

Class:

MOA: decrease SA & AV nodal firing

AP: too short to affect

Pcol:

SE: dyspnea, flushing, chest pain, transient arrhythmia

Chem: inhibitory effect on cardiac tissue, t1/2 = 10s, dosing = 6/12/12, used for PSVT

ACLS: max 30mg, best in reentry, s-tach, a-tach, PSVT

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