Chlordiazepoxide

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Chlordiazepoxide
Systematic (IUPAC) name
9-chloro-5-hydroxy-N-methyl-6-phenyl- 2,5-diazabicyclo[5.4.0]undeca- 1,6,8,10-tetraen-3-imine
Identifiers
CAS number	58-25-3
ATC code	N05BA02
PubChem	2712
DrugBank	APRD00682
Chemical data
Formula	C16H14ClN3O
Mol. weight	299.8
Pharmacokinetic data
Bioavailability	?
Metabolism	Hepatic
Half life	5-25 hours
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	D (USA)
Legal status	Schedule IV(US)
Routes	Oral, parenteral

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.

Contents 1 History 2 Pharmacology 3 Indications 4 Dosage 5 Side effects 6 Contraindications 7 Overdose 8 Legal status 9 Alternative trade names 10 External links

[edit] History

Chlordiazepoxide was the first benzodiazepine to be synthesized and made commercially available. It was an accidental discovery made by Leo Sternbach in the mid-1950s, and brought to market by Roche Pharmaceuticals in 1960. It has a medium to long half life.

Sternbach later went on to develop diazepam, better known as Valium, sold by Roche since 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.

[edit] Pharmacology

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

[edit] 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 withdrawal.

[edit] Dosage

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

[edit] 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)

[edit] 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

[edit] 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.

Chlordiazepoxide overdose is considered a medical emergency and generally requires the immediate attention of medical personnel. The antidote for an overdose of chlordiazepoxide (or any other benzodiazepine) is flumazenil (Anexate®).

[edit] Legal status

Internationally, chlordiazepoxide is a Schedule IV drug under the Convention on Psychotropic Substances[1].

[edit] Alternative trade names

• Librax
• Librocol
• Librelease
• Libritabs
• Limbitrol
• Menrium
• Novo-Poxide
• Poxidium
• Risolid
• Defobin

[edit] External links

• Rx-List.com - Chlordiazepoxide
• Inchem.org - Chlordiazepoxide

Benzodiazepines edit

Adinazolam, Alprazolam, Bentazepam, Bromazepam, Brotizolam, Camazepam, Chlordiazepoxide, Cinolazepam, Clobazam, Clonazepam, Clorazepate, Clotiazepam, Cloxazolam, Cyprazepam, Diazepam, Doxefazepam, Estazolam, Ethyl loflazepate, Etizolam, Fludiazepam, Flunitrazepam, Flurazepam, Flutazolam, Flutoprazepam, Gidazepam, Halazepam, Haloxazolam, Ketazolam, Loprazolam, Lorazepam, Lormetazepam, Medazepam, Mexazolam, Midazolam, Nimetazepam, Nitrazepam, Nordazepam, Oxazepam, Oxazolam, Phenazepam, Pinazepam, Prazepam, Quazepam, Temazepam, Tetrazepam, Tofisopam, Triazolam, Zolazepam