KLORPO TABLET 5mg

Chlordiazepoxide

Source of information: Drugbank (External Link). Last updated on: 3rd July 18
*Trade Name used in the content below may not be the same as the HSA-registered product.

Active Ingredient / Synonyms

7-chloro-2-methylamino-5-phenyl-3H-1,4-benzodiazepin-4-oxide | CDP | Chloradiazepoxide | Chlordiazepoxidum | Clopoxide | Methaminodiazepoxide | Chlordiazepoxide |

Description

An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.

Indication

For the management of anxiety disorders or for the short-term relief of symptoms of anxiety, withdrawal symptoms of acute alcoholism, and preoperative apprehension and anxiety.

Mechanism of Action

Chlordiazepoxide binds to stereospecific benzodiazepine (BZD) binding sites on GABA (A) receptor complexes at several sites within the central nervous system, including the limbic system and reticular formation. This results in an increased binding of the inhibitory neurotransmitter GABA to the GABA(A) receptor.BZDs, therefore, enhance GABA-mediated chloride influx through GABA receptor channels, causing membrane hyperpolarization. The net neuro-inhibitory effects result in the observed sedative, hypnotic, anxiolytic, and muscle relaxant properties.

Pharmacodynamics

Chlordiazepoxide has antianxiety, sedative, appetite-stimulating and weak analgesic actions. The drug seems to block EEG arousal from stimulation in the brain stem reticular formation. The drug has been studied extensively in many species of animals and these studies are suggestive of action on the limbic system of the brain, which recent evidence indicates is involved in emotional responses. Hostile monkeys were made tame by oral drug doses which did not cause sedation. Chlordiazepoxide revealed a "taming" action with the elimination of fear and aggression. The taming effect of chlordiazepoxide was further demonstrated in rats made vicious by lesions in the septal area of the brain. The drug dosage which effectively blocked the vicious reaction was well below the dose which caused sedation in these animals.

Pharmacokinetics

Absorption:

Not Available

Distribution:

Not Available

Metabolism:

Hepatic.

Elimination:

Chlordiazepoxide is excreted in the urine, with 1% to 2% unchanged and 3% to 6% as conjugate.

Half-life

24-48 hours

Clearance

Not Available

Toxicity

LD50=537 mg/kg (Orally in rats). Signs of overdose include respiratory depression, muscle weakness, somnolence (general depressed activity).

References

  1. Health Science Authority of Singapore - Reclassified POM
  2. Drugbank

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Approval Information

KLORPO TABLET 5mg was registered with Health Science Authority of Singapore by BEACONS PHARMACEUTICALS PTE LTD. It is marketed with the registration number of SIN01085P with effective from 1988-12-05.

This product contains 5mg of Chlordiazepoxide in the form of TABLET, SUGAR-COATED.

The medicine was manufactured by BEACONS PHARMACEUTICALS PTE LTD in SINGAPORE

It is a Presciption Only Medicine which can only be obtained from a doctor or a dentist, or from a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Anatomical Therapeutic Chemical (ATC) Classification

ATC Code: N05BA02

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