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BackRifapentine Data - Uses, Dosage, Drug class, Brand name, Warnings, etc
| Pharmacology | Rifapentine, a rifamycin antibiotic similar to rifampin and rifabutin, inhibits DNA-dependent RNA polymerase, exerting bactericidal activity against mycobacteria, particularly Mycobacterium tuberculosis. It is used in pulmonary tuberculosis treatment, with efficacy comparable to daily rifampin, though relapse rates may be higher. It is always used in combination regimens to prevent resistance. | ||||||||||||||||||||||||||||||||||||||||
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| Administration and Adult Dosage |
- PO for pulmonary tuberculosis: • Initial phase (2 months): 600 mg twice weekly (≥72 hr between doses) with other antitubercular drugs • Continuation phase (4 months): 600 mg once weekly with other antitubercular drugs - May be taken with food to reduce nausea, vomiting, or GI upset |
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| Dosage Forms | - Tablet: 150 mg | ||||||||||||||||||||||||||||||||||||||||
| Pharmacokinetics - Fate |
- Absorption: Peak serum levels 5–6 hr post-dose; food increases bioavailability and peak levels - Protein Binding: 93% to serum albumin - Distribution: Vd = 70 ± 1 L/kg - Clearance: Cl = 2.5 ± 0.14 L/hr/kg (males), 1.7 ± 0.41 L/hr/kg (females) - Metabolism: Hydrolyzed by esterase to active metabolite 25-desacetyl rifapentine - Excretion: Primarily fecal; minor urinary |
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| Pharmacokinetics - t¹⁄₂ | - ~13 hr (both rifapentine and 25-desacetyl rifapentine) | ||||||||||||||||||||||||||||||||||||||||
| Adverse Reactions & Side Effects |
Frequent (in combination regimens): - Neutropenia, leukopenia, increased liver enzymes, dyspepsia, anorexia Less Frequent (vs. rifampin regimens): - Pyuria, hematuria |
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| Contraindications | - Hypersensitivity to rifamycins | ||||||||||||||||||||||||||||||||||||||||
| Drug Interactions |
- Induces CYP2C8/9 and 3A4, increasing metabolism of drugs like indinavir (55% peak reduction, 70% AUC reduction), protease inhibitors, and others metabolized by these enzymes - Use with caution with CYP2C8/9 or 3A4 substrates |
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| Treatment of Latent Tuberculosis Infection Comparison Chart |
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References
Hand of Clinical Drug Data