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Question: Does telmisartan inhibit p-glycoprotein?
Does telmisartan inhibit p-glycoprotein?
Overview
Telmisartan, an angiotensin receptor blocker (ARB) used in the treatment of hypertension, has been shown to significantly inhibit p-glycoprotein (P-gp) activity.
Mechanism of Inhibition
Potent P-gp Inhibition
Telmisartan is identified as one of the most potent inhibitors of P-gp currently known (20222053). This inhibition occurs at relatively low concentrations, suggesting a high affinity for the transporter.
Comparison to Other ARBs
Among the ARBs, telmisartan stands out for its substantial ability to inhibit ABC transporters, including P-gp, which are relevant for drug pharmacokinetics and tissue defense (20222053).
Clinical Implications
Drug-Drug Interactions
The potent inhibition of P-gp by telmisartan may explain known interactions with other drugs, such as digoxin (20222053). This interaction potential suggests that telmisartan could modulate the bioavailability of drugs whose absorption is restricted by P-gp.
Potential for Altered Drug Disposition
Healthcare providers should be aware that telmisartan’s inhibition of P-gp could potentially alter the absorption, distribution, and excretion of other medications that are P-gp substrates (31571167).
Additional Transporter Interactions
BCRP and MRP2 Inhibition
In addition to P-gp, telmisartan also inhibits other ABC transporters, including:
- Human BCRP (Breast Cancer Resistance Protein)
- Human MRP2 (Multidrug Resistance-associated Protein 2) (20222053)
Considerations for Clinical Practice
Dosage Adjustments
While some ARBs may not require dosage adjustments when combined with other pharmacological agents, the unique inhibitory profile of telmisartan on P-gp and other transporters suggests that careful consideration should be given when prescribing it as part of a multi-drug regimen (27216792).
Monitoring
Patients taking telmisartan along with other medications that are P-gp substrates may require closer monitoring for potential drug-drug interactions and altered drug responses.
Conclusion
Telmisartan demonstrates a significant inhibitory effect on P-gp, distinguishing it from other ARBs in terms of its potential for transporter-mediated drug interactions. This characteristic should be considered when prescribing telmisartan, particularly in patients on multiple medications.
[Answer generated by www.DrOracle.ai]
