Diazepam Pharmacology

Diazepam

About Diazepam
A benzodiazepine derivative with CNS depressant, Anxiolytic, anticonvulsant, hypnotic, sedative, skeletal muscle relaxant and amnestic.
Mechanism of Action of Diazepam
Diazepam mainly acts on Limbic system and ascending reticular formation in the CNS and binds to the BZD receptor. The binding will facilitates GABA mediated chloride channel opening and produce hyperpolarisation. This will produce an increase in the concentration of the inhibitory neurotransmitter GABA and chloride ions and decreases firing rate of neuron. These in turn alters normal functions of the body.
Antivertigo action: Although intravenous diazepam has been used to abort acute attacks of vertigo of peripheral origin, it can prolong compensation and recovery from vestibular lesions
Pharmacokinets of Diazepam
Absorption: It is well absorbed after oral administration. Distribution: It is distributed widely in the body in protein bound form. Metabolism: It is metabolised to active metabolite (((Desmethyl diazepam))) in the liver. Excretion: Most metabolites are excreted in urine
Onset of Action for Diazepam
0.5 - 2 hour
Duration of Action for Diazepam
1 day
Half Life of Diazepam
20 - 100 hour
Side Effects of Diazepam
1.Ataxia
2.Drowsiness
3.Lethargy
4.Hallucination
5.Nausea
6.Constipation
7.Amnesia
8.Dependence
9. Tremor
10.Confusion
11.Light headedness
12.Mood changes
13.Muscle cramp
14. Drug dependence
15.Respiratory depression
Contra-indications of Diazepam
1.Hypersensitivity to Benzodiazepines
2.Acute narrow angle glaucoma.
Special Precautions while taking Diazepam
1.Renal impairment
2.Hepatic impairment
3.Open angle glaucoma
4.Depression
5.Pulmonary insufficiency
6.Epileptic patients
7.Driving vehicles, operating machines and other hazardous activities
Pregnancy Related Information
Contraindicated.
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated.
Children Related Information
Use with caution
NEONATES contraindicated:
Indications for Diazepam
1.Anxiety
2.Preanaesthetic medication
3.Insomnia
4.Treatment of Febrile seizure and Status epilepticus
5.Acute alcohol withdrawal syndrome,
6.Relief of muscle spasm
7.Tetanus
8.Eclampsia
9.General anaesthesia
10. Vertigo.
Interactions for Diazepam
Alcohol and other CNS depressants: Enhanced CNS effects.
Aminophylline: Antagonizes the sedative effect.
Cimetidine, Oral contraceptives, Disulfiram, Fluoxetine, Isoniazid, Ketoconazole, Metoprolol, Propoxyphene, Propranalol, Valproic Acid: Elimination of diazepam decreased due to inhibition of hepatic metabolism leading to enhanced activity.
Digoxin, Imipiramine & Desipramine: Enhanced activity of these drugs.
Levodopa: Decrease in antiparkinsonism efficacy.
Ranitidine: Decreases GI absorption of Diazepam.
Rifampicin: Decreases efficacy.
Typical Dosage for Diazepam
Adult: 4 - 30 mg/day in 2 - 4 divided doses
Anxiety: 2 -10 mg 2 - 3 times a day; depending on the severity of the disease.

Muscle spasm: 2 -10 mg every 2 - 3 times a day; depending on the severity of the disease.

Acute alcohol withdrawal syndrome: Initial dose: 30 - 40 mg / day in 3 - 4 divided doses; if needed the dose can be reduced to 15 - 20 mg / day in divided doses.

Status epilepticus : 0.2 - 0.5 mg/ kg body weight as IV infusion followed by repeated doses.

PAM (((IM))): 5 - 10 mg before surgery

Children:
Anxiety: 3 - 10 mg / day in 3 - 4 divided dose. As needed dose can be increased gradually

Tetanus (((IM/IV infusion))): 1- 10 mg; repeated every 3 - 4 hour; dose is selected depending on the age and severity of the disease.

Status epilepticus :Above 7 years: 5 mg IV over 5 minutes; the dose may be repeated every 2 - 4 hour as needed; maximum dose: 10 mg

Status epilepticus 1 - 7 years: 2.5 mg IV over 5 minutes; the dose may be repeated every 2 - 4 hour as needed; maximum dose: 5mg
Schedule of Diazepam
H
Storage Requirements for Diazepam
The drug should be kept at 15 - 30 degree C in a tightly closed container.
Effects of Missed Dosage of Diazepam
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose.
Effects of Overdose of Diazepam
Give support and symptomatic treatment. Flumazenil can be given as antagonist. Hypotension can be treated with vasopressors.If the patient is conscious induce emesis followed by charcoal administration

Home Delivery for Diazepam in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including diazepam.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for diazepam and other medicines and health products. Home delivery services for diazepam may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take diazepam only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for diazepam before they complete the sale. You can get this information while placing the order for diazepam with the pharmacy.

Diazepam is a generic medicine name and there are several brands available for it. Some of the brands for diazepam might be better known than diazepam itself. If the pharmacy that's willing to deliver medicines to your home doesn't have diazepam in stock, you can ask for one of the branded alternatives for diazepam.