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DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010

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Table 29–5

Pharmacokinetic Characteristics and Doses of Anti-Arrhythmic Drugs

BIOAVAILABILITY ELIMINATION USUAL DOSES c

Reduced PROTEIN THERAPEUTIC b

First-Pass BINDING ELIMINATION ACTIVE PLASMA Maintenance

DRUG Metabolism >80% Renal Hepatic Other t 1/2

METABOLITE(S) CONCENTRATION Loading Doses Doses

Adenosine d ✓ <10 s ✓ 6–12 mg (IV only)

Amiodarone ✓ ✓ wk ✓ 0.5-2 g/mL 800–1600 mg/d 400 mg/day

× 1–3 wk (IV: 1000 (IV: 0.5 mg/min)

mg over 24 h)

Digoxin 80% ✓ 36 h 0.5-2.0 ng/mL 0.6–1 mg over 0.0625–0.5 mg/

12–24 h 24 h

Diltiazem ✓ ✓ 4 h (x) 0.25 mg/kg over 5-15 mg/h (IV);

10 min (IV) 180-360 mg/d in

3-4 divided doses

(immediate

release); 120-180

mg/24 h

(extended

release) e

Disopyramide >80% ✓ ✓ 4-10 h (x) 2-5 g/mL 150 mg/6 h

(immediate

release);

300 mg

(controlled

release f

Dofetilide >80% ✓ (x) 7-10 h 0.5 mg/12 h

Dronedarone ✓ >98 % ✓ 13-19 h ✓ 400 mg/12 h

Esmolol ✓ 5-10 min 0.5 mg/kg over 0.05-0.3 mg/kg/

1 min (IV) min for 4 min (IV)

Flecainide >80% ✓ 10-18 h 0.2-1 g/mL 50-100 mg/12 h

Ibutilide ✓ ✓ 6 h 1 mg (IV) over 10

min; may repeat

once 10 min later

Lidocaine ✓ ✓ ✓ 120 min (x) 1.5-5 g/mL 50-100 mg 1-4 mg/min (IV)

administered at a

rate of 25-50 mg/

min (IV)

(Continued)

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