Effects of rifampicin (rifampin) on the pharmacokinetics and safety of ambrisentan in healthy subjects: a single-sequence, open-label study.

Author: BoinpallyRamesh, DuftonChristopher, HarrisonBrooke, HendersonLinda S, MageeMindy H, MandagereArun, WalkerGennyne

Paper Details 
Original Abstract of the Article :
BACKGROUND: Ambrisentan is a once-daily, endothelin (ET) type A receptor-selective antagonist approved for the treatment of pulmonary arterial hypertension. Ambrisentan is primarily metabolized by glucuronidation and undergoes cytochrome P450 (CYP)-mediated oxidation to a lesser extent. OBJECTIVE: ...See full text at original site
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引用元:
https://doi.org/10.2165/11539110-000000000-00000

データ提供:米国国立医学図書館(NLM)

Investigating the Impact of Rifampicin on Ambrisentan Pharmacokinetics

This research examines the potential interaction between rifampicin (rifampin), a potent inducer of CYP3A4 and inhibitor of organic anion transporter polypeptides (OATPs), and ambrisentan, a drug used to treat pulmonary arterial hypertension. The study employed a 14-day, single-sequence, open-label study in healthy adults, analyzing the pharmacokinetic profiles of ambrisentan both when administered alone and in conjunction with rifampicin. The study found that while a transient increase in ambrisentan systemic exposure was observed during the initial days of co-administration with rifampicin, the overall steady-state pharmacokinetics of ambrisentan remained largely unaffected by rifampicin. These findings suggest that co-administration of ambrisentan and rifampicin is safe and does not necessitate dose adjustments for ambrisentan.

No Significant Impact of Rifampicin on Ambrisentan Pharmacokinetics

This study provides valuable information for healthcare professionals who prescribe ambrisentan. The researchers have demonstrated that rifampicin does not significantly alter the pharmacokinetics of ambrisentan, allowing for safe co-administration without the need for dose adjustments. This information can help ensure optimal treatment outcomes for patients taking both medications.

Optimizing Drug Therapy for Pulmonary Arterial Hypertension

This research contributes to our understanding of drug interactions and their impact on patient health. The study's findings help optimize drug therapy for pulmonary arterial hypertension, ensuring that patients receive effective treatment without unnecessary risks associated with drug interactions. It underscores the importance of ongoing research to identify potential drug interactions and develop safe and effective treatment regimens.

Dr. Camel's Conclusion

This research is like a compass guiding us through the complexities of drug interactions. The researchers have shown that rifampicin, a potent inducer of CYP3A4, does not significantly impact the pharmacokinetics of ambrisentan. This reassuring information can help ensure safe and effective treatment for patients with pulmonary arterial hypertension.

Date :
  1. Date Completed 2010-12-15
  2. Date Revised 2021-10-20
Further Info :

Pubmed ID

20923245

DOI: Digital Object Identifier

10.2165/11539110-000000000-00000

Related Literature

SNS
PICO Info
in preparation
Languages

English

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