Clinical Pharmacology Details


Diazepam


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Indications & Dose:

Muscle spasm of varied aetiology



Adult: 2–15 mg daily in divided doses, then increased if necessary to 60 mg daily, adjusted according to response, dose only increased in spastic conditions


Acute muscle spasm



Adult: 10 mg, then 10 mg after 4 hours if required, intravenous injection to be administered into a large vein at a rate of no more than 5 mg/minute


Tetanus



Child: 100–300 micrograms/kg every 1–4 hours


Adult: 100–300 micrograms/kg every 1–4 hours



Child: 3–10 mg/kg, adjusted according to response, to be given over 24 hours


Adult: 3–10 mg/kg, adjusted according to response, to be given over 24 hours


Muscle spasm in cerebral spasticity or in postoperative skeletal muscle spasm 



Child 1–11 months: Initially 250 micrograms/kg twice daily
Child 1–4 years: Initially 2.5 mg twice daily
Child 5–11 years: Initially 5 mg twice daily
Child 12–17 years: Initially 10 mg twice daily; maximum 40 mg per day

Anxiety



Adult: 2 mg 3 times a day, then increased if necessary to 15–30 mg daily in divided doses, for debilitated patients, use elderly dose Elderly: 1 mg 3 times a day, then increased if necessary to 7.5–15 mg daily in divided doses Insomnia associated with anxiety



Adult: 5–15 mg daily, to be taken at bedtime

Severe acute anxiety


Control of acute panic attacks


Acute alcohol withdrawal 



Adult: 10 mg, then 10 mg after at least 4 hours if required, intravenous injection to be administered into a large vein, at a rate of not more than 5 mg/ minute Acute drug-induced dystonic reactions



Adult: 5–10 mg, then 5–10 mg after at least 10 minutes as required, to be administered into a large vein, at a rate of not more than 5 mg/minute


Acute anxiety and agitation 



Adult: 500 micrograms/kg, then 500 micrograms/ kg after 12 hours as required Elderly: 250 micrograms/kg, then 250 micrograms/ kg after 12 hours as required

Premedication



Adult: 5–10 mg, to be given 1–2 hours before procedure, for debilitated patients, use elderly dose


Elderly: 2.5–5 mg, to be given 1–2 hours before procedure


Sedative cover for minor surgical and medical procedures



Adult: 10–20 mg, to be administered into a large vein over 2–4 minutes, immediately before procedure


Status epilepticus


Febrile convulsions


Convulsions due to poisoning


BY INTRAVENOUS INJECTION


Neonate: 300–400 micrograms/kg, then 300–400 micrograms/kg after 10 minutes if required, to be given over 3–5 minutes.


Child 1 month–11 years: 300–400 micrograms/kg (max. per dose 10 mg), then 300–400 micrograms/ kg after 10 minutes if required, to be given over 3– 5 minutes


Child 12–17 years: 10 mg, then 10 mg after 10 minutes if required, to be given over 3–5 minutes


Adult: 10 mg, then 10 mg after 10 minutes if required, administered at a rate of 1mL (5 mg) per minute



Neonate: 1.25–2.5 mg, then 1.25–2.5 mg after 10 minutes if required.


Child 1 month–1 year: 5 mg, then 5 mg after 10 minutes if required
Child 2–11 years: 5–10 mg, then 5–10 mg after 10 minutes if required
Child 12–17 years: 10–20 mg, then 10–20 mg after 10 minutes if required
Adult: 10–20 mg, then 10–20 mg after 10–15 minutes if required
Elderly: 10 mg, then 10 mg after 10–15 minutes if required


Life-threatening acute drug-induced dystonic reactions 



Child 1 month–11 years: 100 micrograms/kg, repeated if necessary, to be given over 3–5 minutes
Child 12–17 years: 5–10 mg, repeated if necessary, to be given over 3–5 minutes


Dyspnoea associated with anxiety in palliative care 



Adult: 5–10 mg daily 


Pain of muscle spasm in palliative care



Adult: 5–10 mg daily
NOTE: Only use intramuscular route when oral and intravenous routes not possible.


 


 

Contraindications:

Side Effects:

Cautions:

Precautions:

Elderly, debilitated, hepatic disease, renal disease, children, low serum albumin


PREGNANCY AND LACTATION:
Drug and metabolite enter breast milk; lethargy and loss of weight in nursing infant have been reported

Interaction:

Drugs


Carbamazepine: Markedly reduces effect of oral diazepam; parenteral diazepam less affected


Cimetidine: Inhibits hepatic metabolism of diazepam


Ciprofloxacin: Inhibits hepatic metabolism of diazepam; may also competitively inhibit gamma amino butyric acid receptors


Clarithromycin: Inhibits hepatic metabolism of diazepam


Clozapine: Additive respiratory and cardiovascular depression


Delavirdine: Inhibits hepatic metabolism of diazepam


Disulfiram: Inhibits hepatic metabolism of diazepam


Erythromycin: Inhibits hepatic metabolism of diazepam


Ethanol: Additive CNS effects


Fluconazole: Inhibits hepatic metabolism of diazepam


Fluoxetine: Inhibits hepatic metabolism of diazepam


Fluvoxamine: Inhibits hepatic metabolism of diazepam


Isoniazid: Inhibits hepatic metabolism of diazepam


Itraconazole: Inhibits hepatic metabolism of diazepam


Ketoconazole: Inhibits hepatic metabolism of diazepam


Levodopa: May reduce anti-Parkinsonian effect


Metoprolol: Inhibits hepatic metabolism of diazepam


Omeprazole: Inhibits hepatic metabolism of diazepam


Phenytoin: Markedly reduces effect of oral diazepam; parenteral diazepam less affected


Quinolones: Inhibits hepatic metabolism of diazepam; may also competitively inhibit gamma amino butyric acid receptors


Rifampin: Markedly reduces effect of diazepam


Troleandomycin: Inhibits hepatic metabolism of diazepam

Warnings:

Adverse Effects:

Lactations:

Special Precautions:

Counselling:

Side Effects Or Adverse Reactions:

CNS: Anxiety, confusion, depression, dizziness, drowsiness, fatigue; hallucinations, headache, insomnia, stimulation, tremors, withdrawal syndrome


CV: ECG changes, hypotension; orthostatIc hypotension, tachycardia, venous thrombosis, phlebitis, local irritation, swelling, and vascular impairment following IV inj into small veins on hand


EENT: Blurred vision, mydriasis, tinnitus


GI: Anorexia, constipation, diarrhea, dry mouth, increased ALT/ AST, nausea, vomiting


RESP: Respiratory depression


SKIN: Dermatitis, itching, rash

Patient And Carer Advice: