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:
·
Sedation.
·
Hypnosis.
·
Anxiolysis.
·
Anasthesia.
·
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:
1)
Anxiety=as
anxiolytic.
2)
For insomnia.
3)
Sedation=as
sedative.
4)
Hypnosis=as
hypnotic.
5)
Seizure
disorder=Epilepsy.Tetanus,Eclampsia.
6)
Muscle
rigidity=as muscle relaxant.
7)
As diagnostic
aids or for treatment in psychiatry.
8)
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.
·
Confusioin.
[C]
Tolerance & dependency due to prolonged use:
a)
Pharmacokinetic
tolerance:By barbiturate due to rapid metabolism by hepatic microsomal
enz,induced by barbiturate.
b)
Pharmacodynamic
tolerance:By BDZ due to down regulation of receptor.
Contraindication
of diazepam: Myesthenia gravis.
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