Chlordiazepoxide
From Wikipedia, the free encyclopedia
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Chlordiazepoxide
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| 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 |
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| 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.
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[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 GABAA 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
