Chlordiazepoxide

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Chlordiazepoxide.jpg

[edit] MECHANISM OF ACTION

Chlordiazepoxide was the first benzodiazepine derivative made available for clinical use. Chlordiazepoxide, like other Benzodiazepines bind to specific sites on the gamma-aminobutyric acid-A (GABAA) receptors. This enhances the effects of GABA by increasing its affinity for the GABAA receptor.

Activation of the GABAA receptor, which is linked to a chloride channel (Cl-), results in an influx of Cl- into the neurone causing hyperpolarisation, which results in inhibitory effects on the central nervous system.

Benzodiazepines action on GABAA receptors appears to produce their anxiolytic, sedative, muscle relaxant, hypnotic and anticonvulsant actions.

Chlordiazepoxide is a long acting benzodiazepine, It takes several hours for peak blood levels to be reached and its half-life is between 24 and 48 hours

[edit] INDICATIONS

  • Management of anxiety disorders. Stress of everyday life usually does not require treatment with an anxiolytic.
  • Management of the withdrawal symptoms of acute alcoholism.

[edit] DOSAGE

Adults:

  • Anxiety Disorders
    • Mild and Moderate: 5-10 mg, 3 or 4 times daily
    • Severe: 20 mg, 3 or 4 times daily
    • Geriatric Patients: 5 mg, 2 to 4 times daily. (Benzodiazepines with long half-lives may cause prolonged sedation and increase the risk of falls and fracture. (Short- or intermediate-acting benzodiazepines are preferred in elderly patients)
  • Relief of withdrawal symptoms of acute alcoholism: the parenteral form is usually used initially. If the drug is administered orally, the suggested initial dose is 50 to 100 mg, to be followed by repeated doses as needed until agitation is controlled, up to 300mg per day. Dosage should then be reduced to maintenance levels

[edit] CONTRAINDICATIONS

  • Hypersensitivity to Chlordiazepoxide or to other benzodiazepines.
  • Pregnancy and breastfeeding
  • Myasthenia gravis (Chlordiazepoxide could increase the muscle weakness)
  • Acute narrow angle glaucoma.
  • Severe respiratory failure or sleep apnea syndrome
  • Severe liver failure
  • Acute intoxication with alcohol

[edit] WARNINGS AND PRECAUTIONS

  • Do not drive or do other dangerous activities after taking Chlordiazepoxide until you feel fully awake.
  • Avoid drinking alcohol
  • Respiratory depression may occur in benzodiazepine overdose
  • Use of benzodiazepines can lead to dependence. This risk increases with dose and duration of treatment and in patients with a history of alcohol or drug abuse.
  • Withdrawal symptoms like convulsions, tremor, abdominal and muscle cramps, vomiting, sweating, appetite decrease, weight loss, anxiety and insomnia occurred after the discontinuation of benzodiazepines. Chlordiazepoxide should be discontinued gradually.
  • Paradoxical reactions like restlessness, agitation, irritability, aggressiveness, increased muscle spasticity, insomnia have been reported when using benzodiazepines. Should this occur, the use of the drug should be discontinued.
  • Amnesia: Benzodiazepines may induce anterograde amnesia leading to a partial or complete inability to recall the recent past. Anterograde amnesia may occur using higher therapeutic dosages, the risk increasing at higher dosages.
  • Risk of Fetal Harm: Benzodiazepines can potentially cause fetal harm when administered to pregnant women

[edit] INTERACTIONS

  • Benzodiazepines, including Chlordiazepoxide, produce additive CNS depressant effects when co-administered with other medications which themselves produce CNS depression (e.g. barbiturates, alcohol, sedatives, tricyclic antidepressants, antipsychotics, skeletal muscle relaxants, antihistamines or narcotic analgesics and anesthetics).

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category D (US). An increased risk of congenital malformations associated with the use of minor tranquilizers (chlordiazepoxide, diazepam and meprobamate) during the first trimester of pregnancy has been suggested in several studies. Because use of these drugs is rarely a matter of urgency, their use during this period should almost always be avoided. The possibility that a woman of childbearing potential may be pregnant at the time of institution of therapy should be considered. Patients should be advised that if they become pregnant during therapy or intend to become pregnant they should communicate with their physicians about the desirability of discontinuing the drug.
  • Nursing mothers: Benzodiazepines are known to be excreted in human milk. Chronic administration of diazepam to nursing mothers has been reported to cause their infants to become lethargic and to lose weight. As a general rule, nursing should not be undertaken by mothers who must use Chlordiazepoxide.

[edit] SIDE EFFECTS

Side effects include: sedation and drowsiness, confusion, impaired concentration and ataxia (lack of voluntary coordination of muscle movements).

See also WARNINGS AND PRECAUTIONS section

[edit] RELATED LINKS

[edit] REFERENCES

Sedatives / Hypnotics / Anxiolytics
Benzodiazepines Benzodiazepines (Anxiolytics)‎ Alprazolam (Xanax)   Bromazepam (Lexotan, Lexotanil)   Chlordiazepoxide (Librium)   Clobazam (Frisium)   Clorazepate (Tranxene)   Clotiazepam (Rizen, Tienor)   Delorazepam (EN)   Diazepam (Valium)   Etizolam (Depas)   Ketazolam   Lorazepam (Ativan, Control, Lorans, Tavor, Temesta)   Lormetazepam (Noctamid)   Nordazepam (Nordaz)   Oxazepam (Serepax)   Prazepam (Demetrin, Lysanxia)
Benzodiazepines (Hypnotics) Brotizolam (Lendormin, Bondormin, Dormex, Sintonal, Noctilan)   Clobazam (Frisium)   Estazolam (Esilgan, ProSom)   Etizolam (Depas, Pasaden, Etilaam, Etizest)   Flunitrazepam (Rohypnol)   Flurazepam (Dalmadorm, Dalmane, Felison, Flunox, Valdorm)   Ketazolam (Anseren, Anxon)   Lorazepam (Ativan, Control, Lorans, Tavor, Temesta)   Lormetazepam (Loramet, Minias, Noctamid, Pronoctan, Evamyl)   Midazolam (Dormicum, Hypnovel)   Nitrazepam (Mogadon, Nitrados, Numbon, Radedorm, Alodorm)   Nordazepam (Madar, Nordaz, Stilny, Tranxilium N)   Temazepam (Normison, Restoril, Tenox, Temaze)   Triazolam (Halcion, Hypam, Rilamir)
Non-Benzodiazepine Hypnotics Eszopiclone (Lunesta)   Zolpidem (Ambien, Stilnox, Hypnogen, Sanval, Stilnoct, Zoldem, Zolsana)   Zopiclone (Imovane, Zimovane)
Melatonin agonists Melatonin (Circadin)   Ramelteon (Rozerem)
Orexin agonists Suvorexant (Belsomra)