Bespar - General Information: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. [PubChem]
Other Brand Names containing Buspirone
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Bespar - Pharmacology:
Bespar 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. Bespar also binds at dopamine type 2 (DA2) receptors, blocking presynaptic dopamine receptors. Bespar 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.
Bespar for patients
Buspirone is used for the treatment of nervousness and anxiety. Optimum results are usually seen after three to four weeks of treatment. This medication may be taken with or without food. Inform your physican if you are pregnant or nursing. Buspirone may cause dizziness and drowsiness; use caution while driving or operating hazardous machinery. Do not take any other sedating drugs or drink alcohol while taking this medication. Do not take this medication with a monoamine oxidase inhibitor. Notify physician if you develop muscle spasms, uncontrolled twitching in the face and body, or uncontrolled tongue movements.
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.
Buspirone HCl is contraindicated in patients hypersensitive to buspirone hydrochloride.
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