Chlordiazepoxide/Clidinium bromide

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[edit] BRAND NAMES

[edit] STRUCTURE

[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.

Clidinium bromide: muscarinic antagonist drug with pronounced antispasmodic and antisecretory effect on the gastrointestinal tract. It improves symptoms of cramping and abdominal/stomach pain by decreasing stomach acid and by slowing the intestines.

[edit] INDICATIONS

Adjunctive management of irritable bowel syndrome, peptic ulcer and other gastrointestinal disorders associated with hypersecretion, hypermotility and spasm and accompanied by anxiety or tension states.

[edit] DOSAGE

The optimum dosage varies with the diagnosis and response of the individual patient. The dosage, therefore, should be individualized for maximum beneficial effects. The usual maintenance dose is 1 or 2 capsules ( chlordiazepoxide-5 mg, and clidinium bromide-2.5 mg), 3 or 4 times a day administered before meals and at bedtime.


Elderly: Avoid use in elderly patients due to anticholinergic adverse effects and uncertain effectiveness. 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).

[edit] CONTRAINDICATIONS

  • Hypersensitivity to Chlordiazepoxide and/or clidinium bromide.
  • Pregnancy and lactation
  • Myasthenia gravis (Chlordiazepoxide could increase the muscle weakness)
  • Acute narrow angle glaucoma.
  • Severe respiratory failure or sleep apnea syndrome
  • Severe liver failure
  • Patients with prostatic hypertrophy
  • Patients with benign bladder neck obstruction

[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 (Chlordiazepoxide) 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

  • 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

Common adverse effects:

  • Drowsiness, ataxia, confusion (especially in geriatric subjects)
  • Anticholinergic side effects: dryness of the mouth, blurring of vision, urinary hesitancy and constipation

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[edit] REFERENCES