Clear Search sequence regions
Bookmark Forward

QuickView for Buspirone (compound)


PubChem
Name: Buspirone
PubChem Compound ID: 10741074
Description: An anxiolytic agent and a serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the benzodiazepines, but it has an efficacy comparable to DIAZEPAM.
Molecular formula: C21H31N5O2
Molecular weight: 389.528 g/mol
DrugBank
Identification
Name: Buspirone
Name (isomeric): DB00490
Drug Type: small molecule
Description: An anxiolytic agent and a serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the benzodiazepines, but it has an efficacy comparable to DIAZEPAM.
Synonyms:
Buspirona [INN-Spanish]; Buspirone HCL; Buspironum [INN-Latin]
Brand: Narol, Ansial, Axoren, Buspinol, Buspimen, Anxiron, Buspisal, Ansiced, Travin, Lucelan, Wellbutrin XL, Buspar, Bespar, Censpar
Category: Serotonin Agonists, Anti-anxiety Agents, Anxiolytics sedatives and hypnotics
CAS number: 36505-84-7
Pharmacology
Indication: For the management of anxiety disorders or the short-term relief of the symptoms of anxiety, and also as an augmention of SSRI-treatment against depression.
Pharmacology:
Buspirone is used in the treatment of generalized anxiety where it has advantages over other antianxiety drugs because it does not cause sedation (drowsiness) and does not cause tolerance or physical dependence. Buspirone differs from typical benzodiazepine anxiolytics in that it does not exert anticonvulsant or muscle relaxant effects. It also lac...
show more »
Mechanism of Action:
Buspirone binds to 5-HT type 1A serotonin receptors on presynaptic neurons in the dorsal raphe and on postsynaptic neurons in the hippocampus, thus inhibiting the firing rate of 5-HT-containing neurons in the dorsal raphe. Buspirone also binds at dopamine type 2 (DA2) receptors, blocking presynaptic dopamine receptors. Buspirone increases firing in...
show more »
Absorption: Rapidly absorbed in man. Bioavailability is low and variable (approximately 5%) due to extensive first pass metabolism.
Protein binding: 95% (approximately 70% bound to albumin, 30% bound to alpha 1 -acid glycoprotein)
Biotransformation: Metabolized hepatically, primarily by oxidation by cytochrome P450 3A4 producing several hydroxylated derivatives and a pharmacologically active metabolite, 1-pyrimidinylpiperazine (1-PP)
Route of elimination: In a single-dose study using 14C-labeled buspirone, 29% to 63% of the dose was excreted in the urine within 24 hours, primarily as metabolites; fecal excretion accounted for 18% to 38% of the dose.
Half Life: 2-3 hours (although the action of a single dose is much longer than the short halflife indicates).
Toxicity: Oral, rat LD50 = 136 mg/kg. Symptoms of overdose include dizziness, drowsiness, nausea or vomiting, severe stomach upset, and unusually small pupils.
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Avoid alcohol.
Avoid taking grapefruit or grapefruit juice throughout treatment.
Always take at the same time with respect to meals.
Take with food.
Drug interaction:
ErythromycinThe macrolide, erythromycin, may increase the effect and toxicity of buspirone.
NefazodoneNefazodone increases the effect of buspirone
VerapamilVerapamil may increase the serum concentration of Buspirone. The likely occurs via Verapamil-mediated CYP3A4 inhibition resulting in decreased Buspirone metabolism. Monitor for changes in the therapeutic/adverse effects of Buspirone if Verpamil is initiated, discontinued or dose changed.
ZolmitriptanUse of two serotonin modulators, such as zolmitriptan and buspirone, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
TrimipramineIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
show more »

Targets


Enzymes


Transporters