Trade Names:Mycobutin- Capsules 150 mg
Inhibits DNA-dependent RNA polymerase in susceptible strains of bacteria.
Readily absorbed from GI tract (53%). C max is 375 ng/mL. T max is 3.3 h. Bioavailability is 20% (HIV-positive patients) or 85% (healthy patients). High fat meals slow the rate without influencing extent of absorption. Steady state is 9.3 L/kg.
High lipophilicity demonstrates a high propensity for distribution and intracellular uptake. Protein binding is about 85%. Vd is 9.3 L/kg.
In the liver, there are 5 metabolites identified, 25-0-desacetyl and 31-hydroxy are the most predominant.
Eliminated in the urine (53% excreted primarily as metabolites, 5% unchanged) and feces (30%; 5% unchanged). Systemic cl is 0.69 L/h/kg. Terminal t ½ is 45 h.
CrCl is less than 30 mL/min. AUC is increased 71%. Reduction in dosage is recommended.
Prevention of disseminated Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection.
Hypersensitivity to rifabutin or other rifamycins; active tuberculosis.
PO 300 to 450 mg once daily.Infants and Children
PO Up to 5 mg/kg/day.
Therapeutic efficacy may be decreased because of liver enzyme-inducing properties of rifabutin.Indinavir, itraconazole, ritonavir
May elevate rifabutin plasma levels, increasing the risk of side effects.Ketoconazole
May reduce rifabutin plasma levels, decreasing the therapeutic effects.Zidovudine
May decrease plasma levels of zidovudine.
None well documented.
Asthenia; headache; insomnia.
Anorexia; diarrhea; dyspepsia; abdominal pain; eructation; flatulence; nausea; vomiting.
Anemia; eosinophilia; leukopenia; neutropenia; thrombocytopenia.
Increased alkaline phosphatase, AST, and ALT.
Myalgia; fever; discolored saliva, sputum, tears, or skin.
Category B .
Unknown. Discontinue nursing or discontinue drug.
Safety and efficacy not established. Based on the limited data available, there is no evidence that doses higher than 5 mg/kg daily are useful.
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