DIAZEPAM injectable

Therapeutic action

• Antiseizure (anticonvulsant), muscle relaxant, sedative, anxiolytic

Indications

• First-line treatment of convulsive status epilepticus
• Muscle spasms due to tetanus
• Severe agitation in adults

Forms and strengths, route of administration

• 10 mg in 2 ml ampoule (5 mg/ml) for IM injection, slow IV injection (3 to 5 minutes) or IV infusion in 0.9% sodium chloride or 5% glucose
• The injectable solution may be used rectally.

Dosage and duration 

Convulsive status epilepticus

• Child 1 month to 11 years:
  • Rectal route: one dose of 0.5 mg/kg (0.1 ml/kg); max. 10 mg (2 ml)
  • Slow IV injection: one dose of 0.2 to 0.3 mg/kg (0.04 to 0.06 ml/kg); max. 10 mg (2 ml)

• Child 12 years and over and adult:
  • Rectal route:  one dose of 10 to 20 mg (2 to 4 ml); one dose of 10 mg (2 ml) in older patients
  • Slow IV injection: one dose of 10 mg (2 ml); one dose of 5 mg (1 ml) in older patients

In children and adults, if seizures do not stop 5 minutes after the first dose, readminister the same dose, regardless of the route of administration. Do not administer more than 2 doses in total.

Muscle spasms due to tetanus
The dosage range is variable, depending on the severity of symptoms and clinical response. For information:

• Child 1 month and over and adult: 0.1 to 0.3 mg/kg by slow IV injection every 1 to 4 hours or 0.1 to 0.5 mg/kg/hour by IV infusion over 24 hours

Severe agitation

• Adult: 10 mg (2 ml) by IM injection, to be repeated once after 30 to 60 minutes if necessary

Rectal administration technique 

• Lay the patient on their side.
• For volumes up to 1 ml, use a 1 ml syringe. Withdraw the required dose. Remove the needle. Insert the syringe into the rectum for a length of 1 to 3 cm (depending on age) to administer the dose. For volumes greater than 1 ml, use a 2 ml syringe and attach to the tip of the syringe a nasogastric tube n°8 cut to a length of 2 to 3 cm to administer the dose.
• After administration, hold the buttocks together for at least one minute.

Contra-indications, adverse effects, precautions

• Do not administer to neonates (contains benzyl alcohol) and to patients with severe respiratory insufficiency or severe hepatic impairment.
• Administer with caution: 
  • to older patients and patients with renal or hepatic impairment (reduce the dose by half);
  • to patients with history of substance abuse or mental disorders.
• May cause:
  • pain at injection site;
  • hypotension, muscle weakness, ataxia, hypotonia, drowsiness, lethargy, confusional state;
  • respiratory depression, especially if injected rapidly by IV route and if large doses are administered;
  • coma in the event of overdose.
• Avoid or monitor in combination with:
  • opioid analgesics, antipsychotics, first-generation antihistamines (hydroxyzine, promethazine), antidepressants, other antiseizure medications, etc. (increased sedation);
  • enzyme inducers such as rifampicin, rifabutin, nevirapine, phenobarbital, phenytoin, carbamazepine, etc. (reduced effect of diazepam);
  • omeprazole, macrolides, ritonavir, isoniazid, fluconazole, itraconazole, etc. (increased diazepam toxicity);
  • phenytoin (increased phenytoin toxicity).
• Pregnancy and breast-feeding: avoid, except if vital (passage through the placenta and breast milk)

Remarks

• Diazepam is subject to international controls: follow national regulations.
• For administration by IV infusion, the concentration of diazepam in the solution should not exceed 0.25 mg/ml (e.g. 1 mg in at least 4 ml). 
• Diazepam slow IV is also used in delirium tremens (alcohol withdrawal) in adults: 10 to 20 mg every 4 to 6 hours under close supervision in intensive care unit.
• Do not mix with other drugs in the same syringe or infusion. 

Storage