Diazepam

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It became a blockbuster for Roche after its properties were described in 1961[1].

Contents

Indications

  • Short term relief of severe anxiety
  • Adjunctive therapy at the start of antidepressant therapy
  • Control of status epilepticus
  • Muscle relaxant
  • Adjunct in acute alcohol withdrawal syndrome
  • Perioperative

Pharmacology

Pharmacokinetics

Diazepam has a high lipid solubility. It shows a biphasic half-life, with an initial decrease in blood levels due to re-distribution. The subsequent half-life is between 20-100 hours.

However, metabolites of diazepam are also active and some, for instance desmethyldiazepam, have even longer half-lives than diazepam itself. Therefore, the effective half-life of diazepam and its metabolites can be considerable with a danger of accumulation in the elderly.

Dosage

5-30mg daily in divided doses

Can be given in similar doses intravenously as Diazemuls® (emulsified preparation - as otherwise irritant to veins).

Side-effects

  • Sedation
  • Addiction
  • Pneumonia[2].

References

  1. Randall L O, Heise G A, Schallek W, Bagdon R E, Banziger R, Boris A, Moe R A & Abrams W B. Pharmacological and clinical studies on Valium™ a new psychotherapeutic agent of the benzodiazepine class. Curr. Ther. Res. 3:405-25, 1961.
  2. The impact of benzodiazepines on occurrence of pneumonia and mortality from pneumonia: case-control and cohort study Thorax doi:10.1136/thoraxjnl-2012-202374
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