ANXIOLYTIC & HYPNOTIC DRUGS - BENZODIAZEPENS, BENZODIAZEPENS ANTAGONIST, OTHER ANXIOLYTIC, BARBITURATE, ZOLPIDEM, DRUGS TO TREAT ETHANOL POISONING

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 Anxiety: unpleasant state of tension, apprehension, uneasiness,


Classification 

Benzodiazepens

Bezodiazepene=composed of α , β , γ..BZD binds to GABA receptor at specific site located at the interface of α & γ2 subunit...influx of Cl- ions...hyperpolarization... Θ action potential

Two BZD receptors

BZ1 & BZ2

Actions

 reduction of anxiety....sedation...Anticonvulsant....Muscle relaxant.

.Anterograde Amnesia..

T.E

 used in GAD(Generalized Anxiety Disorder), 

PTSD (Post Traumatic Stress Disorder), 

OCD(Obsessive Compulsive Disorder), 

Phobia, Social Anxiety,

 for Panic disorder Alprazolam is effective In Muscular Disorder Diazepam used. 

Midazolam induce Anaesthesia

Diazepam & Lorazepam DOC in Grand-Mal Epileptic disorder..

Clonazepam in Seizure Flurazepam (85hr t1/2) , Temazepam used in REM(Rapid Eye Movement)

Triazolam used in induction of sleep

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S.E

 drowsiness & confusion, Ataxia, weight gain, sexual dysfunction

Contraindicated in Pregnancy, Glaucoma, liver disease,

BZD ANTAGONIST

Flumazenil

 GABA receptor anatagonist...reverse the effects of BZD..i/v 1hr t1/2... withdrawl cause seizure

OTHER ANXIOLYTIC

Buspirone

 Act on Serotonin 5-HTA1 receptor & DA2 dopamine receptor... for chronic treatment of GAD..

S.E: Hypothermia, Prolactin enlargement, light headedness,

HYPNOTIC DRUGS/Barbiturates

Barbiturate

MOA:

 bind with GABA receptor...influx of CI- ion...hyperpolarization..... block Glutamate receptors..Block Na+ channels

Actions Sedation.. Hypnosis at high dose.. then Anaesthesia.. respiratory depression

by suppressing Hypoxic & response to CO2...Enzyme inducer

T.E:

in Anxiety, Anaesthesia, seizure...DOC in febrile seizure in children..

S.E

 drowsiness, drug hangover...interferes with porphyrin synthesis so contra in Acute

Intermittent porphyria ...physical dependence...poisoning occur

Zolpidem 

BZ1receptor... only Hypnosis lasts for 5hr..

Ramelton

Selective agonist of MT1,MT2 receptors..Melatonin receptors...produce sleep at dark

Ethanol

 CNS depressant...produce sedation & hypnosis at high dose..has a Shallow- Dose –Response curve...Metabolized into Acetaldehyde then Acetate by Aldehyde dehydrogenase...

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Drugs to treat Ethanol Poisoning

Disulfiram block oxidation of Acetaldehyde to acetate by Θ Aldehyde dehydrogenase..

Results into Hyperventillation, Tachycardia, Acetaldehyde in blood

Naltrexone Long-acting opiate antagonist used in supportive Psycotherapy..



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