Diazepam chemical structure
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Diazepam

Diazepam (marketed under brand names Valium®, Seduxen® and, in Europe, Apozepam® and Diapam®) is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. more...

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History

Diazepam was the second benzodiazepine to be invented by Leo Sternbach around 1960. It is five times more potent than its predecessor, chlordiazepoxide (Librium®), which it quickly overtook when first marketed in 1963. The benzodiazepines gained popularity among medical professionals as an improvement upon barbiturates, which have a comparatively narrow therapeutic index. At first, diazepam was considered something of a "wonder-drug": it was America's top-selling pharmaceutical from 1969 to 1982, with peak sales in 1978 of 2.3 billion pills ($US600 million in sales).

However, it is now known that benzodiazepines carry a risk of dependency. In the autumn of 1973, a report aired on the television show 60 Minutes attesting to the drug's addictiveness. This can occur in as little as four weeks. Following a controversial and often polemic discussion, benzodiazepine prescriptions declined by nearly half in the 1980's and 1990's.

Psychiatrists and neurologists have recently discovered new off-label uses for this 'old' drug, such as adjunctive treatment of extrapyramidal disorders or spastic paresis. This is most likely due to the inhibitory effects of the benzodiazepines (see Pharmacology section below).

Pharmacology

In animal models, diazepam appears to act on areas of the limbic system, thalamus and hypothalamus, inducing anxiolytic effects. It is thought to bind to GABAA receptors, (a sub-type of GABA receptors). Due to the role of diazepam as a GABAminergic agonist, when it binds to GABA receptors it causes inhibitory effects. This arises from the hyperpolarization of the postsynaptic membrane, due to the control exerted over negative chloride ions by GABAA receptors.

Diazepam is redistributed into tissues and fat deposits, where there are similar types of benzodiazepine receptors. In humans, tolerance to the sedative effects may develop within weeks, but tolerance to the anxiolytic effects usually does not develop. Lorazepam, clonazepam and alprazolam show stronger anxiolytic effects compared to diazepam, but carry a higher risk of misuse, abuse, tolerance and dependence.

Pharmacokinetics

Diazepam can be administered orally, intravenously, intramuscularly, or as a suppository. When taken orally, diazepam is rapidly absorbed and shows a fast onset of action. Absorption is much slower and more erratic when diazepam is given as an intramuscular injection. Diazepam is highly lipid-soluble and therefore crosses the blood-brain barrier easily.

Diazepam is metabolised in the liver and has a biphasic half-life. The half-life (t1/2α) is 20-100 hours, and the main active metabolite, desmethyldiazepam, has a half-life of 36-200 hours. Diazepam's other active metabolites include, among others, temazepam and oxazepam. Diazepam and its metabolites are excreted into the urine.

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Treating Repetitive Seizures with Rectal Diazepam
From American Family Physician, 2/15/99 by Clarissa C. Kripke

Although rectal diazepam has been used on an outpatient basis in Europe for the treatment of severe, repetitive seizures for more than 20 years, such a formulation has only recently been labeled by the U.S. Food and Drug Administration for this purpose. Diazepam rectal gel is indicated for use in intermittent epilepsy to control bouts of increased seizure activity. Doses of diazepam rectal gel are individually packaged in pre- measured applicators for rectal insertion, ideal for use by caregivers in institutions or home settings. Cereghino and colleagues performed a multi-center, randomized, parallel, double-blind study to determine the safety and efficacy of the diazepam rectal formulation in patients with acute repetitive seizures.

In this study, caregivers were shown how to administer and monitor the medication by use of a video and illustrated written materials. Caregivers received close support and follow-up and had access to medical advice at all times. Response to the medication was measured by time until next seizure and seizure count, and through a global assessment completed by the caregivers and study investigators.

For study purposes, the epileptic seizure type included primary- generalized, complex-partial and simple-partial seizures with a motor component. These seizure types are believed to be the ones recognized more accurately by caregivers. Acute repetitive seizures were distinct from unpredictable seizures or those provoked by a specific cause in that they had a predictable pattern such as an aura or prodrome that distinguished them from other seizures in type, frequency, severity or duration. Most of the 114 patients included in the study were taking other seizure medications as well.

Analysis of seizure count showed that the median number of seizures in patients receiving diazepam was zero, whereas patients receiving placebo had a median of two seizures. In the 12-hour observation period following the administration of diazepam, 55 percent of patients were seizure free compared with 34 percent of those given placebo. The overall assessment by caregivers was also significantly higher in the diazepam group. Although no statistically significant difference in adverse events was found, there was an increased rate of somnolence in the patients receiving diazepam. No episodes of respiratory depression or withdrawal from the study because of adverse events occurred.

The authors conclude that it is possible for well-informed caregivers to predict and prevent acute repetitive seizures at home. The convenience and ease of use of diazepam gel treatment offers families more flexibility and control and may prevent costly emergency room visits and hospital stays.

Cereghino JJ, et al. Treating repetitive seizures with a rectal diazepam formulation. A randomized study. Neurology November 1998;51:1274-82.

COPYRIGHT 1999 American Academy of Family Physicians
COPYRIGHT 2000 Gale Group

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