Concentrations and effects of buspirone are considerably reduced by rifampicin.
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Lamberg TS, Kivisto KT, Neuvonen PJ
Concentrations and effects of buspirone are considerably reduced by rifampicin.
Br J Clin Pharmacol. 1998 Apr;45(4):381-5. doi: 10.1046/j.1365-2125.1998.t01-1-00698.x.
- PubMed ID
- 9578186 [ View in PubMed]
- Abstract
AIMS: The effects of rifampicin on the pharmacokinetics and pharmacodynamics of buspirone, a non-benzodiazepine anxiolytic agent, were investigated. METHODS: In a randomized, placebo-controlled cross-over study with two phases, 10 young healthy volunteers took either 600 mg rifampicin or matched placebo once daily for 5 days. On day 6, 30 mg buspirone was administered orally. Plasma buspirone concentrations and effects of buspirone were measured up to 10 h. RESULTS: The total area under the plasma buspirone concentration-time curve after rifampicin was 10.4% (95% CI, 6.3-14.5%) of that after placebo (1.64+/-0.35 ng ml(-1) h vs 22.0+/-15.1 ng ml(-1) h (mean+/-s.d.); P< 0.01). Rifampicin decreased the peak plasma concentration of buspirone from 6.6+/-3.7 ng ml(-1) to 0.84+/-0.23 ng ml(-1) (P< 0.01) and the half-life from 2.8+/-0.7 h to 1.3+/-0.5 h (P< 0.01). A significant (P<0.05) reduction in the effects of buspirone was observed in three of the six psychomotor tests employed (postural sway test with eyes closed, subjective drowsiness and overall drug effect) after rifampicin pretreatment. CONCLUSIONS: The strong interaction between rifampicin and buspirone is probably mostly due to enhanced CYP3A4-mediated first-pass metabolism of buspirone. Buspirone will most likely show a greatly reduced anxiolytic effect when used together with rifampicin or other potent inducers of CYP3A4 such as phenytoin and carbamazepine.
DrugBank Data that Cites this Article
- Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Buspirone Cytochrome P450 3A4 Protein Humans UnknownSubstrateDetails - Drug Interactions
Drugs Interaction Integrate drug-drug
interactions in your softwareBuspironeErythromycin The serum concentration of Buspirone can be increased when it is combined with Erythromycin. BuspironeItraconazole The serum concentration of Buspirone can be increased when it is combined with Itraconazole. BuspironeRifampicin The serum concentration of Buspirone can be decreased when it is combined with Rifampicin.