Rifapentine

Information about Rifapentine

Rifampin (also referred to as rifampicin) is a macrocyclic antibiotic with major activity against mycobacteria, commonly used in combination with other agents as therapy of tuberculosis. Rifampin is associated with transient and asymptomatic elevations in serum aminotransferase and bilirubin levels and is a well known cause of clinically apparent, acute liver disease that can be severe and even fatal.

Mechanism of action of Rifapentine

Rifampin (rif am' pin) belongs to a class of medications know as rifamycins and is a synthetic derivative of natural products of the bacterium, S. mediterranei. Rifampin is a complex macrocyclic antibiotic that has activity against several bacteria, but most prominently inhibits growth of M. tuberculosis and several atypical mycobacterial species, probably as a result of inhibition of the DNA-dependent RNA polymerase of mycobacteria. Rifampin was approved for use in therapy of tuberculosis in the United States in 1971. Rifampin remains a mainstay of therapy of tuberculosis and atypical mycobacteria infections and is usually used in conjunction with isoniazid and/or pyrazinamide. Other approved uses of rifampin include chemoprophylaxis of meningococcal disease and meningitis due to H. influenza. Rifampin is used off-label as therapy of itching due to liver disease. Rifampin is available in multiple generic forms and under the trade names of Rimactane and Rifadin in capsules of 150 and 300 mg. Pediatric formulations are available as well, as are powdered preparations for parenteral administration. The recommended dose for therapy of tuberculosis in adults is 600 mg (~10 mg/kg) daily and in children 10-20 mg/kg, but no more than 600 mg daily. Fixed combinations of rifampin (300 mg) with isoniazid (150 mg) are available under the brand name Rifamate, and combinations of rifampin (120 mg) with both isoniazid (50 mg) and pyrazinamide (300 mg) under the brand name Rifater. Side effects of rifampin are uncommon, but include rash, fever, flu-like symptoms, gastrointestinal upset and orange discoloration of urine and sweat. Rifampin is a potent inducer of many hepatic enzymes including the drug metabolizing enzymes, CYP 1A2, 2C9, 2C19 and 3A4 for which reason use of concurrent medications (such as oral contraceptives, anticoagulants, some antiretroviral agents, cyclosporine, benzodiazepines, and macrolide antibiotics) should be carefully chosen and monitored. Rifabutin and rifapentine are two other rifamycins that can be used in place of rifampin, rifabutin being useful if drug-interactions are an issue and rifapentine if once weekly dosing is preferred.

The following are list of antituberculosis medications that are discussed individually:

• Bedaquiline
• Capreomycin
• Cycloserine
• Ethambutol
• Ethionamide
• Isoniazid
• Pyrazinamide
• Rifabutin
• Rifampin
• Rifapentine
• Streptomycin

• Dailymed label info on Rifapentine
• FDA Rifapentine

Information about Rifapentine

Rifapentine is a rifamycin antibiotic that is similar in structure and activity to rifampin and rifabutin and that is used in combination with other agents as therapy of tuberculosis, particularly in once or twice weekly regimens. Rifapentine is associated with transient and asymptomatic elevations in serum aminotransferase and is a likely cause of clinically apparent acute liver injury.

Mechanism of action of Rifapentine

Rifapentine (rif" a pen' teen) is a rifamycin antibiotic and a synthetic derivative of natural products of the bacterium, Amycolatopsis mediterranei. The rifamycins are complex macrocyclic antibiotics that have activity against several bacteria, but most prominently M. tuberculosis and several atypical mycobacterial species, probably as a result of inhibition of the DNA dependent RNA polymerase of mycobacteria. These agents are considered bactericidal and are active against both intracellular and extracellular organisms. Rifapentine has a longer half-life than rifampin and rifabutin, which allows for once or twice weekly dosing, which is its major advantage. Rifapentine was approved for use in treating active as well as latent tuberculosis in 1998. It is available as 150 mg film coated tablets under the trade names of Priftin. The recommended dose for active tuberculosis in adults is 600 mg twice weekly for 2 months, followed by 600 mg (~10 mg/kg) once weekly for 4 months as a part of directly observed therapy and in combination with isoniazid or other antituberculosis agents. The recommended regimen for latent tuberculsosis is a 12 week regimen of 600 mg once weekly in combination with isoniazid as directly observed therapy. Pyridoxine (vitamin B6) is commonly given with rifapentine and isoniazid to prevent neuropathy. Side effects of rifapentine are uncommon, but include rash, fever, flu-like symptoms, gastrointestinal upset and orange discoloration of urine and sweat. Rifapentine is intermediate between rifabutin and rifampin in activity as an inducer of the hepatic microsomal drug metabolizing P450 enzymes (CYP 1A2, 2C9, 2C19 and 3A4), the relative potencies being: rifampin (1.0), rifapentine (0.85) and rifabutin (0.4). For this reason, use of other medications (such as many antiretroviral agents, oral contraceptives, beta-blockers, benzodiazepines, cyclosporine, macrolide antibiotics and oral anticoagulants) with rifapentine should be carefully considered and monitored.

The following are list of antituberculosis medications that are discussed individually:

• Bedaquiline
• Capreomycin
• Cycloserine
• Ethambutol
• Ethionamide
• Isoniazid
• Pyrazinamide
• Rifabutin
• Rifampin
• Rifapentine
• Streptomycin

• Dailymed label info on Rifapentine
• FDA Rifapentine

• Rifapentine
  Rifapentine

• Rifapentine
  Rifapentine