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How does probenecid affect tigecycline's bioavailability?

See the DrugPatentWatch profile for probenecid

Short answer: Probenecid will not meaningfully affect tigecycline’s bioavailability.

Rationale:
- Tigecycline is given IV and has essentially 100% systemic exposure when administered that way. It does not have meaningful oral bioavailability to begin with, so the concept of “increasing bioavailability” via probenecid doesn’t apply.
- Probenecid works by inhibiting renal tubular secretion, increasing levels of drugs that are mainly renally excreted. Tigecycline is eliminated mostly via hepatic/biliary routes with only a smaller renal component, so blocking renal clearance has little to no impact on its overall exposure.
- There is no well-established clinically significant interaction between probenecid and tigecycline reported.

Bottom line: Co-administration of probenecid is not expected to change tigecycline’s pharmacokinetics or “bioavailability.” If you’re monitoring for interactions, rely on up-to-date drug interaction resources or the product labeling, but a meaningful interaction with probenecid is unlikely.



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