Lack of Interaction Between Cimetidine and Buspirone

Gammans, Richard E.; Pfeffer, Morris; Westrick, Mary L.; Faulkner, H.C.; Rehm, Klaus D.; Goodson, Peter J.

doi:10.1002/j.1875-9114.1987.tb03521.x

Cited by 12 publications

(3 citation statements)

References 15 publications

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“…However, based on the reported drug interactions, buspirone appears to be a substrate for CYP3A. Buspirone interactions with verapamil, [27] diltiazem, [27] erythromycin, [28] itraconazole, [28] diazepam, [29][30][31] cimetidine, [32] alcohol (ethanol), [29,33] rifampicin (rifampin), [34] alprazolam [35] and haloperidol [36] have been studied and are summarised in this section.…”

Section: Drug Interactionsmentioning

confidence: 99%

“…Since simultaneous administration of cimetidine and many benzodiazepine anxiolytics has resulted in decreased clearance of the drugs, [45,46] Gammans et al [32] investigated the effect of coadministration of cimetidine on the pharmacokinetics of buspirone. This study was of repeat design in 10 healthy men; all participants received all treatments in the same order.…”

Section: Cimetidinementioning

confidence: 99%

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Clinical Pharmacokinetics and Pharmacodynamics of Buspirone, an Anxiolytic Drug

Mahmood

Sahajwalla

1999

Clinical Pharmacokinetics

284

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Buspirone is an anxiolytic drug given at a dosage of 15 mg/day. The mechanism of action of the drug is not well characterised, but it may exert its effect by acting on the dopaminergic system in the central nervous system or by binding to serotonin (5-hydroxytryptamine) receptors. Following a oral dose of buspirone 20 mg, the drug is rapidly absorbed. The mean peak plasma concentration (Cmax) is approximately 2.5 micrograms/L, and the time to reach the peak is under 1 hour. The absolute bioavailability of buspirone is approximately 4%. Buspirone is extensively metabolised. One of the major metabolites of buspirone is 1-pyrimidinylpiperazine (1-PP), which may contribute to the pharmacological activity of buspirone. Buspirone has a volume of distribution of 5.3 L/kg, a systemic clearance of about 1.7 L/h/kg, an elimination half-life of about 2.5 hours and the pharmacokinetics are linear over the dose range 10 to 40 mg. After multiple-dose administration of buspirone 10 mg/day for 9 days, there was no accumulation of either parent compound or metabolite (1-PP). Administration with food increased the Cmax and area under the plasma concentration-time curve (AUC) of buspirone 2-fold. After a single 20 mg dose, the Cmax and AUC increased 2-fold in patients with renal impairment as compared with healthy volunteers. The Cmax and AUC were 15-fold higher for the same dose in patients with hepatic impairment compared with healthy individuals. The half-life of buspirone in patients with hepatic impairment was twice that in healthy individuals. The pharmacokinetics of buspirone were not affected by age or gender. Coadministration of buspirone with verapamil, diltiazem, erythromycin and itraconazole substantially increased the plasma concentration of buspirone, whereas cimetidine and alprazolam had negligible effects. Rifampicin (rifampin) decreased the plasma concentrations of buspirone almost 10-fold.

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Section: Drug Interactionsmentioning

confidence: 99%

Section: Cimetidinementioning

confidence: 99%

Clinical Pharmacokinetics and Pharmacodynamics of Buspirone, an Anxiolytic Drug

Mahmood

Sahajwalla

1999

Clinical Pharmacokinetics

284

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“…In clinical practice, specific studies failed to show any significant drug interaction when buspirone was co-prescribed either with tricyclic antidepressants (Napoliello, 1986) or with Hzreceptor antagonist drugs like cimetidine or ranitidine (Levine and Napoliello, 1988). In a study performed in 10 healthy volunteers receiving simultaneously buspirone (45 mg/day) and cimetidine (1 g/day), the results of both pharmacokinetic and pharmacodynamic evaluations also suggested the absence of clinically significant interaction between these drugs despite a slight increase (3 1 per cent) of buspirone metabolite I-PP after cimetidine (Gammans et al, 1987).…”

Section: Discussionmentioning

confidence: 99%

Repeated administration of buspirone: Absence of pharmacodynamic or pharmacokinetic interaction with triazolam

Boulenger

Gram

Jolicoeur

et al. 1993

Human Psychopharmacology

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The present study was designed to evaluate possible phannacokinetic and pharmacodynamic interactions between buspirone administered repeatedly and triazolam given acutely. Ten healthy male volunteers participated in the study and received 0.25 mg of triazolam orally after a one-week pretreatment with either placebo or buspirone 5 mg t.i.d. The study design was double-blind and crossover, the subjects receiving two times triazolam after the random administration of buspirone or placebo, each treatment period being separated by a washout period of 1 week. Plasma triazolam concentrations were measured by a radio-receptor assay using 'H-flunitrazepam as radioligand. Psychomotor effects of triazolam were measured through subjective self rating scales and various cognitive tests exploring concentration, memory and psychomotor skills.Overall, the results of the study failed to demonstrate any significant difference in triazolam subjective or objective effects as well as in triazolam plasma concentrations after a one-week pretreatment with either placebo or buspirone 15 mg daily. They do suggest that clinically relevant interactions are unlikely to appear when buspirone at moderate dosage is co-prescribed with acute doses of triazolam, though these data do not exclude the possibility of pharmacokinetic interactions between the two drugs. Finally our data also suggest the need for more specific studies in order to demonstrate a possible improvement of psychomotor functions after buspirone administration.

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