DIAZEPAM (VALIUM)

 DESCRIPTION

Valium (diazepam) is a benzodiazepine derivative developed through original Roche research.  Its molecular name is diazepam.  Its molecular formula is C16-H13-Cl-N2-O.  Valium is a colorless crystalline compound, insoluble in water and has a molecular weight of 284.74.


 
 

CLINICAL PHARMACOLOGY

In animals, diazepam appears to act on parts of the limbic system, the thalamus and hypothalamus, and induces calming effects.  Long-term experiments in rats revealed no disturbances of endocrine function.

Reproduction Studies:  A series of rats reproduction studies was performed with diazepam in oral dozes of 1, 10, 80 and 100 mg/kg.  At 100 mg/kg there was a decrease in the number of pregnancies and surviving offspring in these rats.  Neonatal survival of rats at doses lower than 100mg/kg was within normal limits.  Several neonates in these rat reproduction studies showed skeletal or other defects.  In humans, measurable blood levels of diazepam were obtained in maternal and cord blood, indicating placental transfer of the drug.

The mean time to maxium plasma diazepam concentrations after administration of 15 mg diazepam capsules to elevan subjects was 5.3 hours.  The mean half-life of diazepam was 36 hours.  The average minimum plasma diazepam concentrations during once-daily administration of 15-mg diazepam capsules to eleven normal subjects was 196 to 341 ng/ml.

INDICATIONS

Diazepam is indicated for the management of anxiety disorders or for the short-term relief of the symptoms of anxiety.  Anxiety or tension assoiated with the stress of every life usually does not require treatment of Valium.  Diazepam may also be useful in acute alcohol withdrawal situations.  It can be use to relieve symptoms of alcohol withdrawal such as acute agitation, tremor, delirium or hallucinations.

HOW DOES DIAZEPAM WORK?

When you are anxious, your brain becomes more active.  Your brain then make a chemical messenger (or "neurotransmitter") called GABA which makes you feel calmer.  GABA is the brain's own naturally occurring "calmer."  Diazepam makes the action of GABA more powerful and helps calm the brain down.

ADVERSE REACTIONS

Side effects most commonly reported were drowsiness and fatigue.  Less common were confusion, constipation, depression, heache, hypotension, changes in salivation, nausea, skin rash, slurred speech, tremor, urinary retention, and blurred vision.  Minor changes in EEG patterns, usually low-voltage fast activity, have been observed in patients during and after Valium therapy and are of no known significance.