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Buspirone
drug data and news
Buspirone drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Buspirone | ||
| 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 | ||
| Indication | For the management of anxiety disorders or the short-term relief of the symptoms of anxiety | ||
| Sponsored links | Description | Not Available | |
| 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. | ||
| Buspirone News (When available) |
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| Dosage Forms | in 5 and 10 mg tablets | ||
| Drug_Category | Anti-anxiety Agents; Anxiolytics sedatives and hypnotics; ATC:N05BE01 | ||
| 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. | ||
| Toxicity | LD50=136 mg/kg(in rat) | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 8-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-8-azaspiro[4.5]decane-7,9-dione | ||
| Chemical Formula | C21H31N5O2 | ||
| Molecular Weight | 385.503 g/mol | ||
| Smiles String | C1CCC2(C1)CC(=O)N(C(=O)C2)CCCCN3CCN(CC3)C4=NC=CC=N4 | ||
| Melting Point | 201.5-202.5°C | ||
| Water Solubility | 21.35mg/L | ||
| State | white crystals (solid) | ||
| LogP/Hphobicity | 1.238 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Metabolized hepatically, primarily by oxidation producing several hydroxylated derivatives and a pharmacologically active metabolite, 1-pyrimidinylpiperazine (1-PP) | ||
| Half Life | 2-3 hours | ||
| Protein Binding [%] | 95% of buspirone is plasma protein bound | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Buspirone.html http://www.rxlist.com/cgi/generic/buspir.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00222 | ||
| CAS Registry Number | 36505-84-7 | ||
| KEGG Compound ID | C06861 | ||
| PubChem ID | SID:178830 | ||
| PharmGKB ID | PA448689 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2242149 |
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