Diazepam (Valium) - Uses, Mechanism Of Action, Pharmacology, Adverse Effects, And Contraindications

Sun, 17 Aug 2025 21:08:24 +0000

Diazepam is a fast-acting, long-lasting benzodiazepine medication used to treat a number of medical conditions.
Common indications of diazepam include the following.
In the treatment of anxiety & sleep disorders.
In alcohol detoxification.
As a long-term treatment for recurrent seizures.
In the treatment of severe muscle spasms, and spasticity-associated neurological disorders.
In acute alcohol withdrawal to relieve agitation, delirium tremors, and alcoholic hallucinations.
It is also used as a sedative in the ICU setting.
Gamma amino butyric acid, or GABA, is the principal inhibitory neurotransmitter in the nervous system.
Diazepam exerts its effects by facilitating the activity of GABA and reducing neuronal excitability.
Diazepam binds to an allosteric site at the interface between the alpha and gamma subunits on GABA-A receptor chloride ion channels in the excitatory neurons.
This binding will increase the frequency of chloride ion influx to the excitatory neurons, which leads to hyperpolarization and reduced neuronal excitability.
Diazepam action on the limbic system causes its anxiolytic effect.
Diazepam action in the spinal cord & motor neurons leads to muscle relaxation.
And the sedative, amnestic, and anticonvulsant effects are mediated by the action of diazepam on the cerebral cortex, thalamus, and cerebellum.
Diazepam is available as an oral tablet, intramuscular and intravenous injections, and as a rectal gel.
When administered orally, more than 90% of the drug is absorbed into the body.
Diazepam is metabolized by the liver into active metabolites, which are predominantly excreted by the kidneys.
Some common adverse effects of diazepam include the following.
Sedation.
Fatigue.
Confusion.
Ataxia.
Irritability.
Disinhibition.
Headache.
Tremors.
Dystonia.
Urinary retention and incontinence.
Nausea.
Constipation.
Diplopia.
Libido changes.
Rash.
And menstrual irregularities.
Serious adverse effects of diazepam include, Respiratory depression, Dependency and abuse, Withdrawal symptoms, Bradycardia, Hypotension, and cardiovascular collapse, and Syncope.
Diazepam is contraindicated in any person who has hypersensitivity to it.
Other contraindications include, age less than 6 months, severe respiratory insufficiency, myasthenia gravis, sleep apnea syndrome, and hepatic & renal impairment.

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