Physiologically Based Pharmacokinetic Model of Rifapentine and 25-Desacetyl Rifapentine Disposition in Humans
نویسندگان
چکیده
منابع مشابه
Population pharmacokinetics of rifapentine and desacetyl rifapentine in healthy volunteers: nonlinearities in clearance and bioavailability.
Rifapentine is under active investigation as a potent drug that may help shorten the tuberculosis (TB) treatment duration. A previous rifapentine dose escalation study with daily dosing indicated a possible decrease in bioavailability as the dose increased and an increase in clearance over time for rifapentine and its active metabolite, desacetyl rifapentine. This study aimed to assess the effe...
متن کاملProtein binding of rifapentine and its 25-desacetyl metabolite in patients with pulmonary tuberculosis.
Rifapentine is highly protein bound in blood, but the free, unbound drug is the microbiologically active fraction. In this exploratory study, we characterized the free plasma fraction of rifapentine in 41 patients with tuberculosis. We found a lower total rifapentine concentration but significantly higher free rifapentine levels in African patients of black race compared to non-Africans. These ...
متن کاملDisposition and Metabolism of C-rifapentine in Healthy Volunteers
Rifapentine is a long-acting cyclopentyl-derivative of rifampin. This study was designed to investigate the mass balance and biotransformation of C-rifapentine in humans. Four healthy male volunteers received a single 600-mg oral dose of C-rifapentine in a hydroalcoholic solution. Whole blood, urine, and fecal samples were collected before and at frequent intervals after drug administration. Am...
متن کاملDisposition and metabolism of 14C-rifapentine in healthy volunteers.
Rifapentine is a long-acting cyclopentyl-derivative of rifampin. This study was designed to investigate the mass balance and biotransformation of 14C-rifapentine in humans. Four healthy male volunteers received a single 600-mg oral dose of 14C-rifapentine in a hydroalcoholic solution. Whole blood, urine, and fecal samples were collected before and at frequent intervals after drug administration...
متن کاملPharmacokinetic interaction of rifapentine and raltegravir in healthy volunteers.
OBJECTIVES Latent tuberculosis infection and tuberculosis disease are prevalent worldwide. However, antimycobacterial rifamycins have drug interactions with many antiretroviral drugs. We evaluated the effect of rifapentine on the pharmacokinetic properties of raltegravir. METHODS In this open-label, fixed-sequence, three-period study, 21 healthy volunteers were given: raltegravir alone (400 m...
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ژورنال
عنوان ژورنال: Antimicrobial Agents and Chemotherapy
سال: 2016
ISSN: 0066-4804,1098-6596
DOI: 10.1128/aac.00031-16