Chloral Hydrate

• Short-term Sedation and Hypnosis:
  Used primarily for short-term treatment of insomnia, especially when difficulty in falling asleep is prominent.
• Preoperative Sedation:
  Employed as a sedative before anesthesia or minor surgical procedures.
• Sedation in Pediatric Patients:
  Occasionally used for sedation prior to diagnostic procedures or dental work.
• Off-label Uses:
  Sometimes used for managing agitation or delirium in select cases under close supervision.

Adults:

• Oral dose for insomnia: 500 mg to 1 g at bedtime.
• Maximum dose usually not exceeding 2 g per day.
• Sedation dose before procedures: 1 g orally 30 minutes prior.

Pediatrics:

• Dose usually 25 to 50 mg/kg orally, max 1 g, given 30 to 60 minutes before procedure.

Elderly:

• Start at lower doses due to increased sensitivity and risk of adverse effects.

Special Populations:

• Renal or hepatic impairment: Use caution; no precise dosage adjustments established.
• Administer orally, preferably with water or juice.

Duration:

• Short-term use only; generally limited to 1–2 weeks.

Chloral hydrate is a sedative-hypnotic that is metabolized in the liver to trichloroethanol, its active metabolite, which acts on the central nervous system to produce sedation. It enhances the activity of gamma-aminobutyric acid (GABA), the major inhibitory neurotransmitter, by modulating GABA_A receptor function, leading to increased neuronal inhibition and CNS depression. This results in sedation, hypnosis, and anxiolysis.

• Absorption:
  Rapidly absorbed from the gastrointestinal tract.
• Distribution:
  Widely distributed throughout body tissues, crosses the blood-brain barrier.
• Metabolism:
  Extensively metabolized in the liver to active metabolite trichloroethanol and trichloroacetic acid.
• Elimination:
  Metabolites are excreted mainly via the kidneys.
• Half-life:
  Parent compound short (~8 hours); active metabolite trichloroethanol has a half-life of approximately 8 to 12 hours.

• Pregnancy:
  FDA Category C — Animal studies have shown adverse effects; no adequate human studies. Use only if potential benefit justifies risk.
• Lactation:
  Excreted in breast milk; potential CNS depression in infants. Use caution or avoid during breastfeeding.

• Sedative-hypnotic
• Non-benzodiazepine sedative

• Known hypersensitivity to chloral hydrate or its metabolites.
• Severe hepatic or renal impairment.
• Porphyria.
• Severe respiratory depression.
• Acute intoxication with alcohol, barbiturates, or other CNS depressants.

• Risk of respiratory depression, especially when combined with other CNS depressants.
• Potential for dependence and tolerance with prolonged use.
• Use with caution in elderly due to increased sensitivity and fall risk.
• Monitor for paradoxical excitation or behavioral changes.
• Avoid abrupt discontinuation after prolonged use to prevent withdrawal symptoms.

Common:

• Drowsiness
• Dizziness
• Headache
• Gastrointestinal upset (nausea, vomiting)

Serious/Rare:

• Respiratory depression
• Hypotension
• Confusion or agitation
• Allergic reactions including rash and angioedema
• Dependence and withdrawal symptoms with long-term use

• Additive CNS depression with alcohol, benzodiazepines, barbiturates, opioids, and other sedatives.
• May potentiate effects of other CNS depressants leading to respiratory depression.
• Enzyme inducers or inhibitors affecting liver metabolism may alter levels.

• Usage has declined due to safety concerns and availability of safer alternatives.
• Guidelines recommend limiting use to short-term treatment (less than 2 weeks).
• Emphasis on caution in elderly and patients with comorbidities.
• Avoid routine use in pediatric sedation due to variable response and safety concerns.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from light and moisture.
• Keep container tightly closed.
• Keep out of reach of children.