Drug Information

 


  












     

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.

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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

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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.

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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.

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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.

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Brands
available in market

 
























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




Top    



                                                      






 

      


Drug Information
 

  

     
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.

Top  
 

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

Top  
  

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.

Top 
   
 

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.

Top   
  

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.

Top  

 

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


Top    

                                                      

 

By |2022-07-20T16:42:45+00:00July 20, 2022|Uncategorized|Comments Off on Buspirone

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