Chlordiazepoxide

Chlordiazepoxide (marketed under the trade name Librium®) is a hypnotic drug which is a benzodiazepine derivative. It has sedative, anxiolytic and skeletal muscle relaxant properties. more...

History

Chlordiazepoxide was the first benzodiazepine to be synthesized and made commercially available. It was an accidental discovery made by Leo Sternbach of Roche Pharmaceuticals in 1960. It has a medium to long half life.

Sternbach later went on to develop diazepam, better known as Valium, in 1963. The huge success of Valium made Roche the market leader in benzodiazepine products, and the company went on to develop and market nitrazepam in 1965 and later flurazepam and flunitrazepam in 1975.

Other drug companies soon jumped on board the benzodiazepine band wagon, with Wyeth's lorazepam and Upjohn (now Pfizer)'s alprazolam.

As prescriptions for benzodiazepines sky-rocketed through the late 1960s and 1970s, the problem of dependency began to emerge. However, chlordiazepoxide is still a useful treatment for patients suffering from acute anxiety. It is still manufactured and prescribed today, along with a wide variety of other benzodiazepines, all of which have similar properties.

Pharmacology

Chlordiazepoxide is believed to act on the GABA_A receptor, thereby producing inhibitory effects similar to the other benzodiazepines.

Indications

Chlordiazepoxide is indicated for the treatment of insomnia, anxiety and panic attacks. It has also been used as a treatment for acute alcohol or opiate withdrawl.

Dosage

Chlordiazepoxide is available in dosages of 5mg, 10mg and 25mg.

Side Effects

Common side effects of chlordiazepoxide include:

• Drowsiness
• Depression
• Impaired motor function
  • Impaired coordination
  • Impaired balance
  • Dizziness
• Nervousness
• Anterograde amnesia (especially pronounced in higher doses)

Contraindications

Use of chlordiazepoxide should be avoided in individuals with the following conditions:

• Myasthenia gravis
• Acute intoxication with alcohol, narcotics, or other psychoactive substances
• Ataxia
• Severe hypoventilation
• Acute narrow-angle glaucoma
• Severe liver deficiencies (hepatitis and liver cirrhosis decrease elimination by a factor of 2)
• Severe sleep apnea
• Hypersensitivity or allergy to any drug in the benzodiazepine class

Overdose

An individual who has consumed too much chlordiazepoxide will display one or more of the following symptoms:

• Somnolence (difficulty staying awake)
• Mental confusion
• Hypotension
• Hypoventilation
• Impaired motor functions
  • Impaired reflexes
  • Impaired coordination
  • Impaired balance
  • Dizziness
  • Muscle Weakness
• Coma

In animal models, the oral LD₅₀ of chlordiazepoxide is 537 mg/kg.

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