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BuSpar: profile and news
STAR*D Preliminary Findings Provide Clearer Picture of Major ... Feb 27, 2006 Class-action suit filed against Omnicare Feb 6, 2006 Attorney General Announces BuSpar Settlement Jan 24, 2006 Class-action suit filed against Omnicare Feb 6, 2006 Drug Company Settlement To Help Mental Illness Group Jan 24, 2006 Omnicare subpoenaed in generic drug probe Jan 16, 2006 Update 1-Omnicare says gets subpoena from US Attorney Jan 13, 2006 Bristol-Myers establishes Vanlev fund Jan 23, 2006 Comorbid Tobacco Dependence and Psychiatric Disorders Jan 23, 2006 Extra-marital affairs: are women really to blame? (2) Nov 14, 2005 Extra-marital affairs: are women really to blame? Nov 9, 2005 Anxiety Disorders Discoverable by Blood Test Oct 10, 2005 Lexapro and Go Go GO! Sep 13, 2005 How to break teeth-grinding habit Sep 23, 2005 Doctor faces lawsuit over patient death Sep 25, 2005 Worrying all the time? Aug 31, 2005 Low-Dose Birth Control Pill Treats Severe PMS Aug 31, 2005 Drug-suit proceeds to benefit Medicaid Jul 8, 2005 Drug firm to pay $600,000 to state Jul 9, 2005 The Legislated Drugging of the American People Jul 14, 2005 Drug-suit proceeds to benefit Medicaid Jul 8, 2005 Drug firm to pay $600,000 to state Jul 9, 2005 Psychopharmacology of Autism Spectrum Disorders Jun 20, 2005 Multi-Modal Integrated Treatment for Youth With Bipolar Disorder Jun 20, 2005 Other information Indication For the management of anxiety disorders or the short-term relief of the symptoms of anxiety 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 lacks the prominent sedative effect that is associated with more typical anxiolytics. in vitro preclinical studies have shown that buspirone has a high affinity for serotonin (5-HT1A) receptors. Buspirone has no significant affinity for benzodiazepine receptors and does not affect GABA binding in vitro or in vivo when tested in preclinical models. Buspirone has moderate affinity for brain D2-dopamine receptors. Some studies do suggest that buspirone may have indirect effects on other neurotransmitter systems. 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 the locus ceruleus, an area of brain where norepinephrine cell bodies are found in high concentration. The net result of buspirone actions is that serotonergic activity is suppressed while noradrenergic and dopaminergic cell firing is enhanced. Drug Category Anti-anxiety Agents; Anxiolytics sedatives and hypnotics; ATC:N05BE01 Brand Names/Synonyms Ansial; Axoren; B119; B7148; Bespar; Buspar; Buspar Dividose; Buspimen; Buspinol; Buspirona [Inn-Spanish]; Buspirone; Buspirone Hcl; Buspironum [Inn-Latin]; Buspisal; Bustab; CHEMBANK1504; Censpar; Narol; Travin Dosage Forms in 5 and 10 mg tablets Absorption Rapidly absorbed in man and undergoes extensive first pass metabolism Interactions Interactions for Buspirone: It is recommended that buspirone hydrochloride not be used concomitantly with MAO inhibitors Because the effects of concomitant administration of buspirone HCl with most other psychotropic drugs have not been studied, the concomitant use of buspirone HCl with other CNS-active drugs should be approached with caution. There is one report suggesting that the concomitant use of trazodone hydrochloride (Desyrel) and buspirone HCl may have caused 3- to 6-fold elevations on SGPT (ALT) in a few patients. In a similar study, attempting to replicate this finding, no interactive effect on hepatic transaminases was identified. In a study in normal volunteers, concomitant administration of buspirone HCl and haloperidol resulted in increased serum haloperidol concentrations. The clinical significance of this finding is not clear. In vitro, buspirone does not displace tightly bound drugs like phenytoin, propranolol, and warfarin from serum proteins. However, there has been one report of prolonged prothrombin time when buspirone was added to the regimen of a patient treated with warfarin. The patient was also chronically receiving phenytoin, phenobarbital, digoxin, and levothyroxine sodium. In vitro, buspirone may displace less firmly bound drugs like digoxin. The clinical significance of this property is unknown. Chemical IUPAC Name 8-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-8-azaspiro[4.5]decane-7,9-dione Chemical Formula C21H31N5O2 Half Life 2-3 hours Drug Type Approved Drug # Accession No APRD00222 CAS Registry Number 36505-84-7 |
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