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Drug Information
Pharmacokinetics
| Indication
& Dosage | Action
| Interaction
Adverse
Effect & Precautions |
Brands available in Market
Pharmacokinetics
Buspirone hydrochloride is
rapidly absorbed from the gastrointestinal tract reaching peak plasma
concentrations within 40 to 90 minutes after administration by mouth.
Systemic bioavailability is low because of extensive first-pass
metabolism, but may be increased on administration with food as this
delays absorption from the gastrointestinal tract and thereby reduces
presystemic clearance. Buspirone is about 95% bound to plasma proteins.
Metabolism in the liver is extensive; hydroxylation yields several
inactive metabolites and oxidative dealkylation produces
1-(2-pyrimidinyl)-piperazine which is reported to be about 25% as potent
as the parent drug in one model of anxiolytic activity. The elimination
half-life of buspirone is usually about 2 to 3 hours but half-lives of
up to 11 hours have been reported. Buspirone is excreted mainly as
metabolites in the urine, and also in the faeces.
Indication and Dosage
Oral :
Anxiety disorders with or without depression : 5mg 2 or 3 times daily.
Increased by 5mg at 2-3 days interval. Maximum daily dose no to exceed
45mg/day.
Children : Not indicated
Action
Exerts anxiolytic and has no sedative, anticonvulsant or
muscle relaxing property. No affinity for benzodiazepine recator but high
affinity for serotonin (5HT1A) receptors, moderate affinity for brain
D2-dopamine receptor.
Interactions
Alcohol: Though it does not increase alcohol induced impairment in motor
and mental performace, still concomitant use should be avoided digoxin
levels causing toxicity.
Haloperidol: Enhaced serum haloperidol concentrations.
MAOIs: Concomitant use avoided because of elevation of blood pressure.
Adverse
& Effect
Headache, excitement, tachycardia, palpitation, nervousness, dizziness
drowsliness, confusion, fatigue, sweating and nausea
Precaution: Hepatic and renal disease. In alcocoholics.
Pregnancy: Contraindicated.
Breast Feeding: Contraindicated.
Man: May be given in reduced dose.
Anxipar
TAB
5mg
10
Tide
TAB
10mg
10
TIde
Busactil
TAB
5mg
10
Mejda
TAB
10mg
10
Mejda
Buscalm
TAB
5mg
10
Merind
TAB
10mg
10
Merind
Buson 5/10
TAB
5mg
10
Kramer
TAB
10mg
10
Kramer
Buspidac
TAB
5mg
10
Alidac
TAB
10mg
10
Alidac
Buspin
TAB
5mg
10
Intas
TAB
10mg
10
Intas
Tamspar
TAB
5mg
10
Sun Pharma
TAB
10mg
10
Sun Pharma
