DrugindexOnline^{2nd edition}

Pronouncation: (KLOR-uhl HIGH-drate)
Class: Sedative, Hypnotic, Nonbarbiturate

Trade Names:
Aquachloral Supprettes
- Suppositories 324 mg
- Suppositories 648 mg

PMS-Chloral Hydrate (Canada)

Mechanism of Action

Pharmacology

Exact mechanism is unknown; can produce mild CNS depression.

Pharmacokinetics

Absorption

Readily absorbed.

Distribution

35% to 41% protein bound (trichloroethanol). Excreted in breast milk.

Metabolism

Metabolized to trichloroethanol (active), which is then converted in liver and kidney to trichloroacetic acid (inactive).

Elimination

The t _½ is 7 to 10 h (trichloroethanol). Metabolites are excreted in urine and bile.

Indications and Usage

Management of short-term insomnia; sedation; adjunctive to anesthesia, analgesia; prevention or suppression of alcohol withdrawal symptoms (rectal).

Unlabeled Uses

Conscious sedation in pediatric dentistry.

Contraindications

Hypersensitivity to chloral derivatives; severe renal or hepatic function impairment; gastritis (oral forms); severe cardiac disease.

Dosage and Administration

Insomnia
Adults

PO/PR 500 mg to 1 g 15 to 30 min before bedtime.

Children

PO/PR 50 mg/kg/day (up to 1 g per dose) for sleep.

Premedication
Adults

PO 500 mg to 1 g 30 min before surgery.

Sedation
Adults

PO 250 mg 3 times daily after meals.

Children

PO/PR 25 mg/kg/day; may be given in divided doses.

Dental Sedation
Children

75 mg/kg; supplementation with nitrous oxide may provide better sedation than manufacturer's recommended dosage.

General Advice

Administer syrup or capsules with full glass of water or fruit juice to help prevent GI upset problems. Chilling of syrup may lessen its unpleasant taste.

Storage/Stability

Store at room temperature in tightly closed, light-resistant container.

Drug Interactions

Alcohol and other CNS depressants

May produce additive CNS depression.

Furosemide (IV)

Administration within 24 h of chloral hydrate may lead to diaphoresis, hot flashes, tachycardia, and hypertension.

Oral anticoagulants

Anticoagulant effects may be increased, especially during first 2 wk.

Phenytoin

May reduce effects of phenytoin.

Laboratory Test Interactions

May cause false-positive urine glucose test results with Benedict solution or cupric sulfide tablets (eg, Clinitest ), but not with enzyme-based tests (eg, Clinistix , Tes-tape ); altered urinary 17-ketosteroid values when using the Reddy, Jenkins, and Thorn procedure; false-positive phentolamine test results; results of fluorometric tests for urine catecholamines may be altered (do not administer chloral hydrate 48 h before this test).

Adverse Reactions

CNS

Somnambulism; ataxia; dizziness; headache; “hangover” effect.

GI

Stomach pain; nausea; vomiting; diarrhea; flatulence; unpleasant taste in mouth.

Hematologic

Leukopenia; eosinophilia.

Respiratory

Respiratory depression.

Miscellaneous

Hypersensitivity (eg, rash, itching, erythema multiforme, fever).

Precautions

Pregnancy

Category C .

Lactation

Excreted in breast milk.

Tartrazine Sensitivity

Some products contain tartrazine, which can cause allergic-type reactions in some individuals.

Acute intermittent porphyria

Attacks may be precipitated in susceptible patients.

Drug dependency

May be habit forming. Use with caution in patients with history of drug or alcohol addiction.

GI disorders

Avoid use in patients with esophagitis, gastritis or gastric or duodenal ulcers.

Skin/Mucous membrane irritation

Irritates skin and mucous membranes.

Overdosage

Symptoms

Stupor, coma, pinpoint pupils, hypotension, slow or rapid and shallow respirations, hypothermia, muscle flaccidity; also: nausea, vomiting, gastritis, hemorrhagic gastritis, and gastric necrosis caused by drug's corrosive action.

Patient Information

• Instruct patient to take medication exactly as prescribed. Warn that taking doses too close together could result in overdose. Omit missed doses.
• Inform patient that effects of medication may not be noted until after 48 h.
• Advise that medication will be discontinued gradually to prevent withdrawal symptoms, including CNS excitation with tremor, anxiety, hallucinations or delirium.
• Instruct patient to report these symptoms to health care provider: visual changes, irregular heartbeats or palpitations, yellowing of skin or eyes, rash or unusual bleeding or bruising, abdominal pains or gastrointestinal problems.
• Advise patient that drug may cause drowsiness or dizziness and to use caution when driving or performing other tasks requiring mental alertness.
• Caution patient to avoid intake of alcoholic beverages and other CNS depressants such as barbiturates and narcotics.