Macrolide類抗生素

Bacterial infections: Treatment of susceptible bacterial infections, including S. pyogenes, some S. pneumoniae, some S. aureus, M. pneumoniae, L. pneumophilai, diphtheria, pertussis, Chlamydia and erythrasma
Surgical (preoperative) prophylaxis: Colorectal decontamination, in conjunction with other agents, prior to surgical intervention

Antibiotic, Macrolide
Inhibits RNA-dependent protein synthesis at the chain elongation step; binds to the 50S ribosomal subunit resulting in blockage of transpeptidation

Absorption:
1. Effects of food: Cmax reduced by 73% and AUC reduced by 72%
2. Time to peak, serum: (Base) 4 hours; (Ethylsuccinate) 0.5-2.5 hours; (Stearate) 3 hours
Distribution:
1. Vd: 0.64 L/kg
2. Protein binding: 73-81%
Metabolism:
Demethylation primarily via hepatic CYP3A4
Excretion:
1. Primarily feces; urine (2% to 15% as unchanged drug)
2. Half-life elimination: (Neonates) 2.1 hours; (Adults) 1.5-2 hours; (End-stage renal disease) 5-6 hours

1. Concomitant therapy with astemizole, cisapride, dihydroergotamine, ergotamine, pimozide, or terfenadine
2. Hypersensitivity to erythromycin
3. Use with caution to patient with pre-existing liver disease

B [FDA]

Monitor breastfeeding infants for GI disturbances, such as thrush, dehydration, or diarrhea.

Diarrhea, Loss of appetite, Nausea, Stomach cramps, Vomiting, Cholestatic hepatitis

Usual dosage range:
250 to 500 mg every 6 to 12 hours; maximum: 4 g daily
Indication-specific dosing:
Legionnaire disease: 1-4 g daily in divided doses
Pertussis: 500 mg every 6 hours for 14 days
Rheumatic fever, secondary prophylaxis (alternative agent): 250 mg twice daily

General dosing:
30 - 50 mg/kg/day orally divided every 6 to 8 hours; maximum daily dose: 2,000 mg/day
Severe infection:
May double dose; maximum daily dose: 4,000 mg/day

There are no dosage adjustments provided in the manufacturer's labeling.
Dialysis: Slightly dialyzable (5% to 20%).

There are no dosage adjustments provided in the manufacturer's labeling; use with caution.