Clomethiazole

ATC CodeN05CM02
CAS number533-45-9
PUB number10783
Drugbank IDDB06470
Empirical formulaC6H8ClNS
Molar mass (g·mol−1)161,652
Physical statesolid
Density (g·cm−3)1,2
Boiling point (°C)245,8
Solubility0.674 mg/mL

Basics

Clomethiazole is an active ingredient used to treat alcohol withdrawal, sleep disorders and confusion. It has a sedative, sleep-inducing and anticonvulsant effect. Clomethiazole belongs to the group of sedatives and interacts with the GABA receptors. Clomethiazole can be addictive and should therefore only be used for a short time. Interaction with the CYP450 enzymes can also lead to numerous side effects and interactions. Clomethiazole was used for many years up to the year 2000 as the most important drug to combat severe alcohol withdrawal symptoms. Clomethiazole has since been replaced by drugs with fewer side effects, such as diazepam, and is now only used very rarely.

Graphic structural formula of the active substance chlomethiazole

Effect

Clomethiazole works by imitating gamma-aminobutyric acid (GABA), which binds to the GABA-A receptors and enhances the effect of the inhibitory neurotransmitter GABA. This binding results in a calming, sleep-promoting and anticonvulsant effect.

The bioavailability of clomethiazole - i.e. the percentage of the active ingredient that is available in the blood - is very low (exact values are not known). The half-life, i.e. the time the body needs to excrete half of the active ingredient, is 4 hours.

Dosage

Always take clomethiazole exactly as described in the package leaflet or as advised by your doctor.

There is no usual recommended dose for clomethiazole, as an individual dose must be selected for each treatment.

It is important to note that clomethiazole has a high dependency potential.

Clomethiazole should always be phased out, i.e. the dose should be reduced slowly until the medication can be discontinued. It should never be stopped abruptly, as this can lead to severe withdrawal symptoms.

Side effects

CAUTION: Excessive doses of clomethiazole can lead to death from respiratory paralysis. Therefore, always take only the prescribed dosage or the dosage specified in the package leaflet.

The following side effects may occur

  • strong salivation
  • increased mucus secretion in the upper respiratory tract
  • stomach pain
  • heartburn
  • Nausea and vomiting
  • diarrhea
  • Burning in the throat and nose
  • Runny nose and coughing
  • drop in blood pressure
  • Inhibition of respiratory and circulatory function
  • Blistering rashes on the skin
  • Facial swelling
  • Hypersensitivity reactions
  • cardiac arrest
  • fatigue
  • drowsiness
  • headache
  • palpitations
  • Feeling of numbness or tingling
  • itching
  • conjunctivitis

Interactions

Interactions may occur if the following medicines are taken at the same time:

  • other drugs that have a dampening effect on the central nervous system - CAUTION:This can lead to an unpredictable increase in effect and thus to death due to respiratory paralysis
  • Carbamazepine - the effect may be weakened
  • Drugs that affect liver metabolism (e.g. cimetidine)
  • Propranolol - this can lead to an extremely slow heartbeat (bradycardia)
  • Chlorzoxazone - the effect of chlorzoxazone may be prolonged
  • Alcohol - also has a dampening effect on the central nervous systemCAUTION:Death may occur due to respiratory paralysis

Contraindications

Clomethiazole must not be taken in the following cases

  • if you are allergic to clomethiazole
  • in the case of sleep apnea syndrome, i.e. seizure-like breathing stops lasting more than 10 seconds
  • in the case of breathing disorders caused by a disorder of the central nervous system
  • in acute alcohol intoxication
  • acute intoxication caused by other substances that depress the central nervous system
  • alcohol dependence
  • addiction to psychotropic substances

Age restriction

Clomethiazole should NOT be used under the age of 18.

In older people, the availability of clomethiazole may be increased and at the same time the excretion of the active substance may be delayed. This can lead to an intensification of the effect and a prolonged duration of action.

Pregnancy & breastfeeding

Clomethiazole must NOT be taken during pregnancy and breastfeeding unless your doctor considers it absolutely necessary. Clomethiazole is placental, which means that the active substance can enter the bloodstream of the unborn baby, where it can also cause effects and side effects. The same applies to breast milk. Clomethiazole passes into breast milk and can therefore cause effects and side effects in the infant. If treatment with clomethiazole is necessary during breastfeeding, you should stop breastfeeding.

History of the active ingredient

Clomethiazole was originally researched as an active substance for the treatment of strokes. In the past, clomethiazole was also repeatedly abused as a depressant drug. However, this can lead to psychological or physical dependence.

Thomas Hofko

Thomas Hofko

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer



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