Benzodiazepines

Mechanism of action Benzodiazepines/Diazepam/Clobazem/Clonazepam/Loxazepum:

Benzodiazepines

Binds to specific,high affinity sites on the cell membrane that are adjacent to the GABA receptor(in brain)

↑ Affinity of GABA receptor for GABA.

When GABA binds with it’s receptor →Opening of  channel

Entry of  from ECF to ICF.

Hyper-polarization & stabilzation of the cell membrane.

Hypoexcitation.

CNS depression/sedation

 

Pharmacological effects of Benzodiazepines/Diazepam:

[A]On CNS:

  • Anasthesia
  • Sedation
  • Hypnosis
  • Anxiolysis
  • Muscle relaxation.

[B]On respiratory system:Respiartory depression by-

  • ↓ sensitivity to .
  • Medullary depression.

[C]On GIT:

  • Relief GIT disorder such as IBS.
  • Reduce nocturnal HCl secretion.

[D]On CVS:

  • No significant effect at theraputic dose.
  • IN high dose-↓BP.

Indication of Diazepam/Benzodiazepines/

Diazepum/Clonazepum:

  • Anxiety=as anxiolytic.
  • For insomnia.
  • Sedation=as sedative.
  • Hypnosis=as hypnotic.
  • Seizure disorder=Epilepsy.Tetanus,Eclampsia.
  • Muscle rigidity=as muscle relaxant.
  • As diagnostic aids or for treatment in psychiatry.
  • For control of ethanol or other sedative & hypnotic with drawal states.

Adverse effects of Benzodiazepines/Diazpam/Clonazepum:

[A] Over dose:Acute toxic effect (fatal)

[B] Normal dose:Undesired effect

  • Hange over effect.
  • Confusion

[C] Tolerance & dependency due to prolonged use:

  1. Pharmacokinetic tolerance:By barbiturate due to rapid metabolism by hepatic microsomal enz,induced by barbiturate.
  2. Pharmacodynamic tolerance:By BDZ due to down regulation of receptor.

Contraindication of diazepam: Myasthenia gravis.

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