Products
Chloral hydrate was approved in many countries in 1954 and is commercially available as a solution (Nervifene). Other products such as Medianox and chloraldurate are no longer available.
Structure and properties
Chloral hydrate (C2H3Cl3O2, Mr = 165.4 g/mol) is in the form of colorless, transparent crystals that are very soluble in water. It has a bitter taste. The substance was synthesized as early as 1832 by Justus Liebig.
Effects
Chloral hydrate (ATC N05CC01) has sleep-inducing and sedative properties. The effects are rapid and the half-life is up to 8 hours. Chloral hydrate is a prodrug and is converted to the active form trichloroethanol in the body by alcohol dehydrogenase (Figure). The effects are based on interference with GABAA-ergic neurotransmission.
Indications
For short-term treatment of sleep and insomnia. In many countries, chloral hydrate is also approved for the treatment of nervous restlessness.
Dosage
According to the prescribing information. The solution is taken as a sleep aid diluted with cold water before sleep. Because of the potential for dependence, chloral hydrate should be administered only for short periods.
Contraindications
- Hypersensitivity
- Severe hepatic or renal insufficiency
- Heart disease
- Respiratory failure
- Porphyria
- Gastritis
- Obstructive sleep apnea
- Children and adolescents
- Pregnancy and lactation
- Chloral hydrate should not be combined with anticoagulants.
For complete precautions, see the drug label.
Interactions
Drug-drug interactions have been described with anticoagulants, furosemide, amitriptyline, alcohol, fluoxetine, MAO inhibitors, and central depressant drugs.
Adverse effects
Possible adverse effects include central and psychiatric disturbances such as headache, dizziness, confusion and paradoxical agitation, small pupils, drooping of the eyelid, cardiac arrhythmias (at high doses), and digestive disturbances. Prolonged administration can lead to dependence. Overdose is dangerous and can lead to respiratory depression, coma, and cardiac arrhythmias. The most famous victim of a chloral hydrate overdose is Marilyn Monroe, who died at age 36 from poisoning with Nembutal capsules (pentobarbital) and chloral hydrate.
