Trade Names:Diastat- Gel, rectal 2.5 mg (pediatric)- Gel, rectal 10 mg- Gel, rectal 15 mg (adult)- Gel, rectal 20 mg (adult)
Trade Names:Diazepam- Solution, oral 1 mg/mL- Injection 5 mg/mL
Trade Names:Diazepam Intensol- Solution (intensol) 5 mg/mL
Trade Names:Valium- Tablets 2 mg- Tablets 5 mg- Tablets 10 mgApo-Diazepam (Canada)Diazemuls (Canada)Valium Roche Oral (Canada)
Potentiates action of GABA, inhibitory neurotransmitter, resulting in increased neural inhibition and CNS depression, especially in limbic system and reticular formation.
Slow and erratic absorption unless administered in the deltoid muscle; C max is lower than oral or IV administration.Rectal
T max is 1.5 h. Bioavailability is 90%.Oral
T max is 0.5 to 2 h.
95% to 98% protein bound. Highly lipophilic. Crosses the placenta and is excreted in breast milk.
Metabolized in the liver (involving CYP2C19 and CYP3A4) to desmethyldiazepam (active) and 2 minor active metabolites.
The t ½ is 20 to 80 h.
The t ½ is prolonged and Cl decreased in those with alcoholic cirrhosis.Elderly
The t ½ is increased and Cl is decreased.Children
The t ½ is longer in neonates and children younger than 2 yr of age; t ½ is shorter in children 2 to 16 yr of age.
Management of anxiety disorders; relief of acute alcohol withdrawal symptoms; relief of preoperative apprehension and anxiety and reduction of memory recall; treatment of muscle spasms, convulsive disorders (used adjunctively), and status epilepticus.
Treatment of irritable bowel syndrome; relief of panic attack.
Hypersensitivity to benzodiazepines; psychoses; acute narrow-angle glaucoma; use in children younger than 6 mo of age; lactation.
Individualize dosage; increase cautiously.Adults and Children
Usual recommended dose IM/IV 2 to 20 mg, depending on indication and severity. In acute conditions injection may be repeated within 1 h, but every 3 to 4 h is usually satisfactory. Dosage and route vary with indication and age.Children 6 mo of age and older
Usual daily dose PO 1 to 2.5 mg 3 or 4 times daily initially; increase gradually as needed and tolerated.Acute Alcohol WithdrawalAdults
PO 10 mg 3 to 4 times daily first 24 h, then 5 mg 3 to 4 times daily as needed. IM/IV 10 mg initially, then 5 to 10 mg in 3 to 4 h if needed.Anticonvulsant AdjunctAdults
PO 2 to 10 mg 2 to 4 times daily.Elderly or Debilitated Patients
PO Initial dose 2 to 2.5 mg once to twice daily; increase gradually.AnxietyAdults
PO 2 to 10 mg 2 to 4 times daily. IM/IV 2 to 10 mg; repeat in 3 to 4 h if needed.Cardioversion (Anxiety and Tension)Adults
IM/IV 5 to 15 mg 5 to 10 min before procedure.Endoscopic Procedures
IM/IV 10 to 20 mg IV or 5 to 10 mg IM approximately 30 min prior to procedure.Preoperative (Anxiety and Tension)Adults
IM 10 mg before surgery.Sedation/Muscle RelaxationAdults
IM/IV 2 to 10 mg/dose every 3 to 4 h as needed.Children 6 mo of age and older
PO 0.12 to 0.8 mg/kg/day in divided doses. IM/IV 0.04 to 0.2 mg/kg/dose every 2 to 4 h (max, 0.6 mg/kg in 8-h period).Skeletal Muscle SpasmAdults
PO 2 to 10 mg 3 to 4 times daily. IM/IV 5 to 10 mg initially, then 5 to 10 mg in 3 to 4 h if needed. Larger doses may be necessary in tetanus.Status Epilepticus and Severe Recurrent Convulsive DisordersAdults
IM/IV (IV preferred) 5 to 10 mg initially; then 5 to 10 mg at 10 to 15 min intervals (max total dose, 30 mg). If needed, repeat in 2 to 4 h.Children 5 yr of age and older
IM/IV 1 mg every 2 to 5 min (max total dose, 10 mg). If needed, repeat in 2 to 4 h.Infants and Children 1 mo to 5 yr of age
IM/IV 0.2 to 0.5 mg slowly every 2 to 5 min (max total dose, 5 mg).TetanusChildren 5 yr of age and older
IM/IV 5 to 10 mg; repeat every 3 to 4 h as needed.Infants and Children 1 mo to 5 yr of age
IM/IV 1 to 2 mg slowly; repeat every 3 to 4 h as needed.Rectal GelChildren 2 to 5 yr of age
Rectal 0.5 mg/kg.Children 6 to 11 yr of age
Rectal 0.3 mg/kg.Adults and Children 12 yr of age and older
Rectal 0.2 mg/kg.
A second dose, when required, may be given 4 to 12 h after the first dose.
Store tablets, oral solution, and injection at controlled room temperature (59° to 86°F). Protect from light. Protect tablets from moisture.
May increase diazepam plasma concentrations.Cimetidine, oral contraceptives, disulfiram
May increase effects of diazepam with excessive sedation and impaired psychomotor function.Digoxin
May increase serum digoxin concentrations.Omeprazole
May increase diazepam levels and enhance effects.Rifamycins
May decrease diazepam plasma concentrations.Theophyllines
May antagonize sedative effects of diazepam.
Diazepam interacts with plastic containers and IV tubing, significantly decreasing availability of drug delivered. Do not mix or dilute with other solutions or drugs in a syringe or infusion container.
None well documented.
CV collapse; bradycardia; tachycardia; hypertension; palpitations; edema; hypotension; phlebitis or thrombosis at IV sites.
Drowsiness; confusion; ataxia; dizziness; lethargy; fatigue; apathy; memory impairment; disorientation; anterograde amnesia; restlessness; headache; slurred speech; loss of voice; stupor; coma; euphoria; irritability; vivid dreams; psychomotor retardation; paradoxical reactions (eg, anger, hostility, mania, insomnia, muscle spasms); depression; dysarthria; hypoactivity; tremor; vertigo.
Urticaria; skin rash.
Visual or auditory disturbances; depressed hearing; blurred vision; diplopia; nystagmus.
Constipation; diarrhea; dry mouth; coated tongue; nausea; anorexia; vomiting.
Incontinence; changes in libido; urinary retention.
Blood dyscrasias including agranulocytosis, anemia, thrombocytopenia, leukopenia, neutropenia.
Hepatic dysfunction including hepatitis and jaundice; abnormal LFTs.
Ensure that CBC with differential and liver enzymes are evaluated periodically in patient on prolonged therapy.
Category D . Avoid drug especially during first trimester because of possible increased risk of congenital malformations.
Excreted in breast milk.
Oral form not recommended in patients younger than 6 mo of age; parenteral form not recommended in infants younger than 30 days of age.
Initial dose should be small and gradually increased. Give with extreme care to elderly patients with limited pulmonary reserve.
Observe caution to avoid accumulation of drug.
Observe caution to avoid accumulation of drug.
Prolonged use can lead to dependency. Withdrawal syndrome has occurred within 4 to 6 wk of treatment, especially if abruptly discontinued. For discontinuation after long-term treatment, use caution and taper dosage.
Reserved primarily for acute states.
Not intended for use in patients with primary depressive disorder, psychosis, or disorders in which anxiety is not prominent.
Tonic status epilepticus has been precipitated in patients treated with IV for petit mal or variant status.
Use drug with caution in patients with suicidal tendencies; do not allow access to large quantities of drug.
Hypotension, respiratory or cardiac arrest, drowsiness, confusion, somnolence, impaired coordination, diminished reflexes, lethargy, ataxia, hypotonia, hypnosis, coma, death.
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