Clinical Pharmacokinetics and Pharmacodynamics of Buspirone, an Anxiolytic Drug

  title={Clinical Pharmacokinetics and Pharmacodynamics of Buspirone, an Anxiolytic Drug},
  author={Iftekhar Mahmood and Chandrahas Sahajwalla},
  journal={Clinical Pharmacokinetics},
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 20mg, the drug is rapidly absorbed. The mean peak plasma concentration (Cmax) is approximately 2.5 μg/L, and the time to reach the peak is under 1 hour. The absolute bioavailability… 

6-Hydroxybuspirone Is a Major Active Metabolite of Buspirone: Assessment of Pharmacokinetics and 5-Hydroxytryptamine1A Receptor Occupancy in Rats

Preclinical data suggest that 6-OH-buspirone probably contributes to the clinical efficacy of buspirone as an anxiolytic agent.

Systemic absorption of amitriptyline and buspirone after oral and transdermal administration to healthy cats.

Until supporting pharmacokinetic data are available, veterinarians and cat owners should not rely on the transdermal route of administration for treating cats with amitriptyline or buspirone.

Modulation of Cytochrome P450 Activity by 18β‐Glycyrrhetic Acid and its Consequence on Buspirone Pharmacokinetics in Rats

Results indicate that GLY can inhibit the in vitro CYP3A‐mediated drug metabolism in RLM via a mixed inhibition mechanism, and shows that GLy could function as merely a weak inhibitor for CYP1‐mediatedDrug metabolism in vivo.

Pharmacokinetics of Buspirone in Autistic Children

It is suggested that buspirone is rapidly absorbed and eliminated in young children with extensive metabolism to 1‐PP, and may be useful in developmental disorders in which brain serotonin synthesis is altered.

Pharmacokinetics and tolerability of buspirone during oral administration to children and adolescents with anxiety disorder and normal healthy adults

Buspirone was generally safe and well tolerated at doses up to 30mgbid in adolescents and adults and most of the children, and the most frequently reported adverse events in children and adolescents were lightheadedness, headache, and dyspepsia.

Selective effects of serotonergic psychoactive agents on gastrointestinal functions in health.

Buspirone, paroxetine, and venlafaxine-XR affect upper gastrointestinal functions in healthy humans and support the need for clinical and physiological studies of these agents in functional gastrointestinal disorders.

Understanding the pharmacokinetics of anxiolytic drugs

A need for a more balanced assessment of the benefits and risks associated with benzodiazepine use, particularly considering pharmacokinetic profile of the drugs to ensure that patients, who would truly benefit from these agents, are not denied appropriate treatment.



Concentrations and effects of buspirone are considerably reduced by rifampicin.

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.

Metabolism and disposition of buspirone.

Lack of Interaction Between Cimetidine and Buspirone

The results suggest that within the normal therapeutic dosage ranges for both drugs, it is unlikely that a clinically significant interaction between them will occur.

Dopaminergic effects of buspirone, a novel anxiolytic agent.

Interactions of buspirone with itraconazole and rifampicin: effects on the pharmacokinetics of the active 1-(2-pyrimidinyl)-piperazine metabolite of buspirone.

Itraconazole and rifampicin caused only relatively minor changes in the plasma concentrations of the active piperazine metabolite of buspir one, although they had drastic effects on the concentrations of parent buspirone.

The relationship between buspirone bioavailability and dose in healthy subjects.

It was concluded that buspirone exhibits linear pharmacokinetics following doses in the therapeutic range, and half-life did not change as a function of dose.

Evaluation of the alpha 2-adrenoceptor blocking properties of buspirone and ipsapirone in healthy subjects. Relationship with the plasma concentration of the common metabolite 1-(2-pyrimidinyl)-piperazine.

Clonidine decreased blood pressure, heart rate, oral body temperature, salivary excretion, plasma noradrenaline, 3,4-dihydroxyphenylglycol (DHPG) concentrations, increased plasma growth hormone but did not modify plasma insulin and C-peptide concentrations.

Dose of midazolam should be reduced during diltiazem and verapamil treatments.

If the administration of midazolam cannot be avoided, the dose of midAZolam should be reduced during concomitant treatment with diltiazem and verapamil, as these changes in the pharmacokinetics were associated with profound and prolonged sedative effects.

Lack of Pharmacokinetic Interaction Between Buspirone and Haloperidol in Patients with Schizophrenia

The results indicate that coadministration of buspirone does not markedly affect the pharmacokinetics or plasma concentrations of haloperidol.

Buspirone pharmacokinetics in patients with cirrhosis.

The pharmacokinetics of a single oral dose of buspirone (20 mg) were determined in 12 patients with cirrhosis and 12 normal subjects and on the kinetic evidence busPirone should be used with caution in liver disease.