Buspirone resources

DRUG INFO
Buspirone

Drug Name: Buspirone

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-HT_1A) 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: DrugBank: Interactions for Buspirone

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

Buspirone News
(When available)

Class-action suit filed against Omnicare Feb 6, 2006
...of Fluoxetine, a generic form of the antidepressant Prozac; and substituting two 7.5 milligram tablets for a single 15 milligram tablet of Buspirone, a generic ... - Louisville Business First,

Omnicare Shares Skid on Downgrade Sparked by Raid Feb 5, 2006
...has been substituting antacid drug Ranitidine capsules for tablets; fluoxetine tablets for capsules; and switching one 15 milligram tablet of Buspirone, an anti ... - ChallengerNKY.com,

Probe News Punishes Omnicare Jan 17, 2006
Specifically, the filing indicates, the government is questioning whether Omnicare improperly substituted two 7.5-milligram Buspirone anti-anxiety tablets for ... - TheStreet.com

Omnicare subpoenaed in generic drug probe Jan 16, 2006
Substituting two 7.5 milligram tablets for a single 15 milligram tablet of Buspirone, a generic form of the anti-anxiety drug BuSpar. ... - Louisville Business First,

Omnicare drug 'relationships' come under federal scrutiny Jan 13, 2006
...substituting two 7.5 mg. tablets of buspirone for a single 15 mg. tablet. Buspirone is used to treat anxiety disorders. After a series of ... - Cincinnati Post,

Comorbid Tobacco Dependence and Psychiatric Disorders Jan 23, 2006
Cinciripini and colleagues (1995) found that smokers with high levels of trait anxiety taking buspirone (BuSpar) versus placebo were more likely to be ... - Psychiatric Times,

Update 1-Omnicare says gets subpoena from US Attorney Jan 13, 2006
Co's (LLY.N: Quote, Profile, Research) antidepressant Prozac; and the substitution of two 7.5 milligram tablets for one 15 mg tablet of Buspirone, a generic of ... - Reuters

Business digest Jan 17, 2006
...are investigating allegations of drug substitutions involving ranitidine (an anti-heartburn medication), fluoxetine (an antidepressant) and buspirone (an anti ... - Cincinnati Enquirer,

City Councilman resigns  Jan 12, 2006
...and July 5. Those drugs included hydrocodone, marijuana, OxyContin, Zyrtec 10, buspirone hydrochloride and ranitidine. He also is ... - Myrtle Beach Sun News, Update 1-Omnicare says gets subpoena from US Attorney  Jan 13, 2006
Reuters Prozac; and the substitution of two 7.5 milligram tablets for one 15 mg tablet of Buspirone, a generic of Bristol-Myers Squibb Co's BuSpar anti-anxiety drug.

New Medicare prescription program brings higher co-pays, confusing ...  Dec 28, 2005
San Jose Mercury News, He'll receive a larger-than-usual supply of Buspar, Lexapro and Seroquel, powerful psychiatric drugs that keep his schizophrenia and bipolar disorder in check. ...

DOJ: Lautenschlager Presents DOJ Grants to Five Wisconsin ...  Dec 20, 2005
Wisbusiness.com, The NAMI funds come from cy pres funds from the BuSpar antitrust case. Because the BuSpar drug treats anxiety disorders, the settlement ...

Option Fatigue  Dec 16, 2005
CBS News Or maybe a Valium, Antivan or BuSpar. Possibly a vodka martini, but with Grey Goose, Smirnoff, Stolichnaya, Absolut, Skyy, Belvedere, Finlandia or Ketel One. ...

Beware! Femme fatales on the prowl  Jan 13, 2006
Times of India, Little did he know that the 25-year-old woman who thumbed a ride on his bike on the Narol-Naroda highway would lead him to end his life. ...

In Dec, AMC collects Rs 50 crore as octroi  Dec 31, 2005
Ahmedabad Newsline, Modernisation of check-post should lead to generation of more revenue, he said, adding that tenders for modernisation of Narol-Sarkhej check-posts were being ...

BJP shelves Naroda flyover plan; others may be axed too  Jan 2, 2006
Ahmedabad Newsline, ...‘‘We have got complaints from locals that this would create nuisance to them...we are giving priority to the Narol-Naroda National Highway where two ...

3 charged in shooting at White Marsh Mall  Jan 6, 2006
Baltimore Sun, Police said Daniel Allen Brown, 19, of the 4000 block of Ridgecroft Road; Jonathan Derrell Parks, 19, of the 2100 block of E. Chase St.; and Travin Rashaad West ...

Recent Crime Wave In Baltimore County Not Typical  Jan 9, 2006
WJZ, Sears. Daniel Brown, Jonathan Parks, and Travin West are all charged with attempted murder and are being held without bail. Then ...

Shot fired at mall; police nab three  Jan 11, 2006
Maryland Northeast Booster, Police said in a news release that Daniel Allen Brown, Jonathan Derrell Parks and Travin Rashaad West, all 19, were charged immediately after the Jan. ...

Men Charged In Mall Food Court Shooting  Jan 6, 2006
WBAL Channel.com, Baltimore County police identified the three men as Daniel Allen Brown, Jonathan Derrell Parks and Travin Rashaad West, all 19 and of Baltimore. ...

Mosely’s journey to NFL tops Waynesville area sports year-in ...  Dec 29, 2005
Waynesville Daily Guide, Keeth tied for 17th. In the boys’ Class 2 State Golf Meet Dixon’s Travin Shelton tied for 15th. *Waynesville High’s Katie ...

Buspirone resources

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Buspirone