Drug Profile

Name of Medicinal Product: Diazepam

Therapeutic Class: sedative/hypnotic

Chemical Class: Benzodiazepines

Pharmacologic Properties:
Mechanism of Diazepam is a benzodiazepine that exerts anxiolytic, sedative,
Action muscle- relaxant, anticonvulsant and amnestic effects. Most of these
effects are thought to result from a facilitation of the action of
gamma aminobutyric acid (GABA), an inhibitory neurotransmitter in
the central nervous system.
Indication Anxiety disorder, panic disorder, Sleep disorders, Amnesia, Seizures.
(primary and
secondary)
Contraindication Contraindicated in patients with increased eye pressure and
hypersensitivity.
Adverse Drug Drowsiness and confusion , Ataxia,, Cognitive impairment,
Reaction
Interactions Antibiotics and antihistamines
Precautions Ask the patient to avoid Driving and operating heavy machinery after
its use.
Pharmacokinetic Parameters:
Route Oral
Bioavailability After oral administration >90% of diazepam is absorbed and the
average time to achieve peak plasma concentrations is 1 – 1.5 hours
with a range of 0.25 to 2.5 hour. This results in an average decrease
in C max of 20% in addition to a 27% decrease in AUC
(range 15% to 50%) when administered with food.

Volume of Diazepam and its metabolites are highly bound to plasma proteins
Distribution (Vd) (diazepam 98%). In young healthy males, the volume of distribution
at steady-state is 0.8 to 1.0 L/kg.
Half Life (t1/2) half-life of approximately 1 hour, although it may range up to >3
hours.

Clearance (Cl) The clearance of diazepam is 20 to 30 mL/min inyoung adults.

Metabolism Diazepam is N-demethylated by CYP3A4 and 2C19 to the active
metabolite N desmethyldiazepam, and is hydroxylated by CYP3A4 to
the active metabolite temazepam. N-desmethyldiazepam and
temazepam are both further metabolized to oxazepam. Temazepam
and oxazepam are largely eliminated by glucuronidation.

Area Under AUC (range 15% to 50%) when administered with food.
Curve (AUC)
Mean Residence
Time (MRT)
Pharmaceutical Indication:
 Brand Market Company Strength Route of Dosage Form
Name Name Name Administration
Valium Valium 10mg oral tablet
Nicholas
Piramal India
Ltd.

anxol anxol 2ml intravenous injection

Nicholas
Pirama.

Dose:
Disease Pediatric Dose Adult Dose
Anxiety 2 mg
Symptomatic Relief in 10 mg, 2 to 4 times daily
Acute Alcohol
Withdrawal 10 mg, 3 or 4 times during
the first 24 hours,
Relief of Skeletal Muscle 5 mg, 3 or 4 times daily as
needed Adjunctively.
Convulsive Disorders 2 mg to 10 mg, 3 or 4 times
daily.

CNS-acting 1 mg to 2.5 mg, 3 or 4 times

daily
Note: Not for use in pediatric patients under 6 months
Preservatives:
Brands Preservatives and Excipients Used Concentration
Valium benzyl alcohol 2-50 ul
Pregnancy and Lactation: during the first and third trimesters may be associated with an increased risk
of teratogenicity and withdrawal symptoms in the newborn, respectively.

Overdose: >10mg
Shelf Life: (Plumb's, 6th edition page 372) Diazepam has a shelf life of five years for oral tablets and
three years for IV/IM solutions.
Storage: Store at room temperature 59º to 86ºF (15º to 30ºC). Dispense in tight, light-resistant
containers as defined in USP/NF.
References: 1) USP 2) NF
Lippincott pharmacology.