Trial reportAntimicrobial agents and chemotherapy2001
Pharmacokinetic Interaction between amprenavir and rifabutin or rifampin in healthy males.
Trial report in Antimicrobial agents and chemotherapy, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers, 1 of them a synthesis that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
28 citing papers in PubMed, 1 synthesis or guideline pooled it, 70 citations in OpenAlex.
- Intestinal Efflux Transporters P-gp and BCRP Are Not Clinically Relevant in Apixaban Disposition.Pharmaceutical research · 2020Pooled it
- Impact of Rifabutin or Rifampin on Bedaquiline Safety, Tolerability, and Pharmacokinetics Assessed in a Randomized Clinical Trial with Healthy Adult Volunteers.Antimicrobial agents and chemotherapy · 2018Trial
- Effect of SLCO1B1 Polymorphisms on Rifabutin Pharmacokinetics in African HIV-Infected Patients with Tuberculosis.Antimicrobial agents and chemotherapy · 2016Trial
- Randomized pharmacokinetic evaluation of different rifabutin doses in African HIV- infected tuberculosis patients on lopinavir/ritonavir-based antiretroviral therapy.BMC pharmacology & toxicology · 2014Trial
- Pharmacokinetics of darunavir/ritonavir and rifabutin coadministered in HIV-negative healthy volunteers.Antimicrobial agents and chemotherapy · 2010Trial
- Gefitinib-phenytoin interaction is not correlated with the C-erythromycin breath test in healthy male volunteers.British journal of clinical pharmacology · 2009Trial
- Interaction studies of tipranavir-ritonavir with clarithromycin, fluconazole, and rifabutin in healthy volunteers.Antimicrobial agents and chemotherapy · 2009Trial
- Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.Antimicrobial agents and chemotherapy · 2008Trial
- Amprenavir and efavirenz pharmacokinetics before and after the addition of nelfinavir, indinavir, ritonavir, or saquinavir in seronegative individuals.Antimicrobial agents and chemotherapy · 2005Trial
- Pharmacokinetic study of tenofovir disoproxil fumarate combined with rifampin in healthy volunteers.Antimicrobial agents and chemotherapy · 2005Trial
- Building Confidence in Physiologically Based Pharmacokinetic Modeling of CYP3A Induction Mediated by Rifampin: An Industry Perspective.Clinical pharmacology and therapeutics · 2025Review
- Lack of CYP3A4 protein induction despite mRNA induction in primary hepatocytes exposed to rifabutin as a possible explanation for its low interaction risk in vivo.Archives of toxicology · 2024Article
- An Overview of Various Rifampicin Analogs againstMedicinal chemistry (Shariqah (United Arab Emirates)) · 2024Review
- Pharmacology, Dosing, and Side Effects of Rifabutin as a Possible Therapy for Antibiotic-ResistantOpen forum infectious diseases · 2020Review
- Population pharmacokinetic drug-drug interaction pooled analysis of existing data for rifabutin and HIV PIs.The Journal of antimicrobial chemotherapy · 2016Article
- Chimeric mice with humanized livers: a unique tool for in vivo and in vitro enzyme induction studies.International journal of molecular sciences · 2013Article
- Stereoselective inhibition of CYP2C19 and CYP3A4 by fluoxetine and its metabolite: implications for risk assessment of multiple time-dependent inhibitor systems.Drug metabolism and disposition: the biological fate of chemicals · 2013Article
- Risk assessment of mechanism-based inactivation in drug-drug interactions.Drug metabolism and disposition: the biological fate of chemicals · 2012Article
- Pharmacokinetic drug interactions of antimicrobial drugs: a systematic review on oxazolidinones, rifamycines, macrolides, fluoroquinolones, and Beta-lactams.Pharmaceutics · 2011Article
- Nuclear receptor PXR, transcriptional circuits and metabolic relevance.Biochimica et biophysica acta · 2011Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
The objective of this study was to determine if there is a pharmacokinetic interaction when amprenavir is given with rifabutin or rifampin and to determine the effects of these drugs on the erythromycin breath test (ERMBT). Twenty-four healthy male subjects were randomized to one of two cohorts. All subjects received amprenavir (1,200 mg twice a day) for 4 days, followed by a 7-day washout period, followed by either rifabutin (300 mg once a day [QD]) (cohort 1) or rifampin (600 mg QD) (cohort 2) for 14 days. Cohort 1 then received amprenavir plus rifabutin for 10 days, and cohort 2 received amprenavir plus rifampin for 4 days. Serial plasma and urine samples for measurement of amprenavir, rifabutin, and rifampin and their 25-O-desacetyl metabolites, were measured by high-performance liquid chromatography. Rifabutin did not significantly affect amprenavir's pharmacokinetics. Amprenavir significantly increased the area under the curve at steady state (AUC(ss)) of rifabutin by 2.93-fold and the AUC(ss) of 25-O-desacetylrifabutin by 13.3-fold. Rifampin significantly decreased the AUC(ss) of amprenavir by 82%, but amprenavir had no effect on rifampin pharmacokinetics. Amprenavir decreased the results of the ERMBT by 83%. The results of the ERMBT after 2 weeks of rifabutin and rifampin therapy were increased 187 and 156%, respectively. Amprenavir plus rifampin was well tolerated. Amprenavir plus rifabutin was poorly tolerated, and 5 of 11 subjects discontinued therapy. Rifampin markedly increases the metabolic clearance of amprenavir, and coadministration is contraindicated. Amprenavir significantly decreases clearance of rifabutin and 25-O-desacetylrifabutin, and the combination is poorly tolerated. Amprenavir inhibits the ERMBT, and rifampin and rifabutin are equipotent inducers of the ERMBT.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.