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Chloral Hydrate

Pronunciation

Class: Anxiolytics, Sedatives, and Hypnotics; Miscellaneous
VA Class: CN309
CAS Number: 302-17-0
Brands: AquachloralSuprettes, Somnote

Warning(s)

Genotoxic and may be carcinogenic in mice; should not be used when less potentially dangerous agents would be effective.103

Introduction

Sedative and hypnotic.100 101 103 106

Uses for Chloral Hydrate

Hypnotic

Short term treatment of insomnia for <2 weeks; effective for inducing and maintaining sleep.100 101 103

Sedation

Used for routine sedation.100 101 106

Used preoperatively to relieve anxiety and to provide sedation100 101 without depressed respiration or cough reflex.103

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Also used to produce sleep prior to non-painful procedures (e.g., EEG, diagnostic imaging)104 105 to relieve anxiety and to provide sedation.100 101 103

Has been used for conscious sedation to relieve anxiety in young pediatric patients (usually <3 years of age) during procedures (e.g., diagnostic imaging).104 105 106

Used often in geriatric and pediatric patients, because many clinicians suggest that the drug is associated with paradoxical excitement less frequently than barbiturates; however, no well controlled studies confirmed this clinical impression.100 101

Postoperative Analgesia

Adjunct to opiates and analgesics for control of postoperative pain.103

Withdrawal

Reduction of anxiety associated with withdrawal of opiates or barbiturates.100 101 103

Used alone or in conjunction with paraldehyde for prevention of alcohol withdrawal symptoms and/or suppression of the syndrome once it develops.100 101

Chloral Hydrate Dosage and Administration

Administration

Administer orally100 101 or rectally.103

Withdraw chloral hydrate slowly after chronic administration to avoid possibility of precipitating withdrawal symptoms.101 c (See Withdrawal under Warnings and Precautions.)

Oral Administration

Administer capsules with a full glass of water or liquid after meals;101 dilute oral solution in 1/2 a glass of water or other liquid (e.g., fruit juice, ginger ale).100 101

Rectal Administration

Moisten finger and suppository with water before inserting suppository.103

Suppositories have been dissolved in cottonseed or olive oil and administered as a retention enema.c

Dosage

Pediatric Patients

Hypnotic
Oral

50 mg/kg or 1.5 g/m2 up to a maximum single dose of 1 g.100 101

Rectal

18 mg/kg (325 mg/18 kg) once daily before bedtime.103

Sedation
Routine Sedation
Oral

8 mg/kg or 250 mg/m2 3 times daily, up to a maximum of 500 mg 3 times daily.100 101

Some experts recommend a dosage of 25–50 mg/kg per 24 hours, (given in 3 or 4 doses; every 8 or 6 hours, respectively), up to 500 mg per dose.106

Rectal

9 mg/kg (325 mg/36 kg), do not exceed 1 dose in 24 hours.103

Some experts recommend a dosage of 25–50 mg/kg per 24 hours, (given in 3 or 4 doses; every 8 or 6 hours, respectively), up to 500 mg per dose.106

Preoperative Sedation
Oral

8 mg/kg or 250 mg/m2 3 times daily, up to a maximum of 500 mg 3 times daily.100 101

Rectal

9 mg/kg (325 mg/36 kg); do not exceed 1 dose in 24 hours.103

Procedural Sedation
Oral

20–25 mg/kg before procedure.100 101

Some experts recommend a 25- to 100-mg/kg dose before procedure; do not exceed a 1-g dose in infants or a 2-g dose in children.105 106

Rectal

Some experts recommend a 25- to 100-mg/kg dose before procedure; do not exceed a 1-g dose in infants or a 2-g dose in children.106

Conscious Sedation
Oral

Neonates: have been given 25–100 mg/kg once.104

Pediatric patients <3 years of age (excluding neonates): were given a dose of 25–100 mg/kg and a second dose of 25–50 mg/kg may be administered after 30 minutes; maximum total dosage has been 2 g or 100 mg/kg (whichever was lower).104 105

Rectal

Some experts recommend a 25- to 100-mg/kg dose before procedure; do not exceed a 1-g dose in infants or a 2-g dose in children.106

Adults

Hypnotic
Oral

0.5–1 g 15–30 minutes prior to bedtime.100 101

Some experts recommend a 0.5- to 1-g dose; do not exceed 2 g in 24 hours.106

Rectal

0.65–1.3 g 30 minutes prior to bedtime.103

Some experts recommend a 0.5- to 1-g dose; do not exceed 2 g in 24 hours.106

Sedation
Routine Sedation
Oral

250 mg 3 times daily after meals.100 101

Rectal

325–650 mg 3 times daily, up to a maximum total daily dosage of 1950 mg.103

Some experts recommend 250 mg 3 times daily.106

Preoperative Sedation
Oral

0.5–1 g 30 minutes prior surgery.c

Alcohol Withdrawal
Oral

0.5–1 g every 6 hours as needed, up to a maximum single dose or daily dosage of 2 g.100 101

Prescribing Limits

Pediatric Patients

Hypnotic
Oral

Maximum 1 g daily (as a single dose).100 101

Sedation
Oral

For routine sedation, maximum 500 mg 3 times daily.100 101 c

For procedural sedation, maximum 1-g dose in infants or a 2-g dose in children.106

For conscious sedation, maximum total dosage in children <3 years of age (excluding neonates) is 2 g or 100 mg/kg (whichever is lower).104 105

Rectal

For routine or preoperative sedation, maximum of one 9-mg/kg (325-mg/36 kg) dose daily.103

Adults

Oral

Maximum 2 g daily.100 101 c

Rectal

Maximum 1950 mg daily.103

Special Populations

No special population recommendations at this time.100 101 c 103 (See Contraindications under Cautions.)

Cautions for Chloral Hydrate

Contraindications

  • Marked hepatic impairment.100 101 c 103

  • Marked renal impairment. 100 101 c 103

  • Known hypersensitivity or idiosyncratic reaction to chloral hydrate.100 101 c 103

Warnings/Precautions

Warnings

Carcinogenicity

Although the manufacturer of Aquachloral suppositories warns about potential carcinogenicity of the drug, some experts state that the assumption that chloral hydrate is a reactive metabolite of trichloroethylene (an industrial solvent) responsible for the carcinogenicity of trichloroethylene is questionable.108 There is evidence that the carcinogenicity of trichloroethylene is due to a reactive intermediate epoxide metabolite rather than to chloral hydrate.108

Abuse Potential

Although uncommon, tolerance and psychologic dependence may occur following prolonged administration of the drug; use with caution in patients with a history of drug abuse.100 101 c 103

Symptoms of dependence are similar to those of chronic alcoholism100 101 c 103 (drowsiness, lethargy, hangover, slurring of speech, incoordination, tremulousness, and nystagmus).c

Withdrawal

Sudden withdrawal may cause delirium tremens (sometimes fatal) and hallucinations; following chronic use, withdraw slowly.100 101 c 103

Sensitivity Reactions

Hypersensitivity Reactions

Scarlatiniform or erythematous rash, urticaria, angioedema, purpura, eczema, bullous lesions, skin eruptions, and erythema multiforme reported, sometimes accompanied by fever.100 101 103

Tartrazine Sensitivity

Aquachloral 325 mg rectal suppositories contain tartrazine (FD&C yellow No. 5), which may cause allergic reactions including bronchial asthma in susceptible individuals.103 Incidence of tartrazine sensitivity is low, but it frequently occurs in patients who are sensitive to aspirin.103

General Precautions

CNS Effects

Use with caution in mentally depressed patients or those having suicidal tendencies.100 101 c 103

Rarely, somnambulistic reaction characterized by disorientation and incoherence reported.100 101 103

GI Effects

Avoid oral administration in patients with esophagitis, gastritis, or gastric or duodenal ulcers.100 101 c

Gastritis may develop following prolonged oral administration; minimize irritation by diluting oral syrup or administering other oral dosage forms with liquids.100 101 c (See Administration under Dosage and Administration.)

Cardiac Effects

Prolonged administration of therapeutic doses was not associated with adverse cardiac effects.100 101 103

Do not use high doses in patients with severe cardiac disease.100 101 103

Renal Effects

Following prolonged administration, parenchymatous renal damage reported.100 101

Porphyria

Attacks of acute intermittent porphyria reported; use caution in susceptible patients.101

Adequate Monitoring

Procedural sedation using chloral hydrate in pediatric patients should be performed only under the supervision of qualified clinicians experienced in cardiorespiratory complications.104 105 107

Specific Populations

Pregnancy

Category C.100 101 c 103

Lactation

Distributed into milk.103 Use with caution in nursing women.100 101 c 103

Pediatric Use

Used orally and rectally in pediatric patients for sedation and hypnosis.100 101 c 103 104 105 106 108

Geriatric Use

Geriatric patients may tolerate chloral hydrate even when intolerant to barbiturates.103

Common Adverse Effects

Nausea,100 101 c 103 vomiting, 100 101 c 103 diarrhea, 100 101 c 103 ataxia, 100 101 c 103 dizziness.100 101 c 103

Interactions for Chloral Hydrate

Specific Drugs

Drug

Interaction

Comments

CNS depressants (e.g., alcohol, barbiturates, paraldehyde )

Additive CNS depression100 101 103

Vasodilation (characterized by tachycardia, palpitations, facial flushing, and dysphoria) may occur when used with alcohol100 101 103

Use with caution to avoid overdosage100 101 103

Furosemide

Possible diaphoresis, flushing, variable BP, uneasiness, in patients with acute MI and CHF receiving IV furosemide within 24 hours of chloral hydrate100 101

Consider alternative hypnotic drug (e.g., a benzodiazepine) in patients receiving IV furosemide100 101 c

Warfarin

Potential for increased warfarin metabolism and decreased warfarin efficacy (hypoprothrombinemia)100 101 c 103

Consider alternative hypnotic drug e.g., benzodiazepine).100 101 c If used concomitantly, monitor prothrombin time closely100 101 c 103

Tests for Urine Glucose

Possible false-positive results in urine glucose test using cupric sulfate as Benedict’s solution and possibly with cupric sulfate tablets (Clinitest)100 101 c

May use glucose tests based on enzymatic glucose oxidase reactions (e.g., Clinistix, Tes-Tape)100 101 c

Urine Catecholamine Test (Fluorometric)

Possible interference 100 101

Do not administer chloral hydrate for 48 hours prior to test100 101 c

Urinary 17-hydroxycorticosteroids Test

Possible interference with Reddy, Jenkins, and Thorn procedures100 101 c

Chloral Hydrate Pharmacokinetics

Absorption

Bioavailability

Rapidly absorbed following oral or rectal administration.c

Onset

Following oral administration of 0.5–1 g, sedation occurs within 30–60 minutes.c 105

Following rectal administration, sedation occurs within 60 minutes.103

Duration

Following oral administration of 0.5–1 g : 4–8 hours.c 105

Distribution

Extent

Distributed into CSF, umbilical cord blood, fetal blood, amniotic fluid, and milk.100 101 c

Elimination

Metabolism

Metabolized to trichloroethanol (active metabolite), principally in the liver and erythrocytes, by alcohol dehydrogenase and other enzymes.c Small, but variable amounts of chloral hydrate metabolized to trichloroacetic acid (inactive metabolite) in liver and kidneys.c

Elimination Route

Active and inactive metabolites are slowly and variably excreted in the kidneys.c Trichloroethanol glucuronide (urochloralic acid), an inactive metabolite, may be secreted into the bile and excreted in feces.c

Eliminated by dialysis.103

Half-life

8–11 hours.c

Stability

Storage

Oral

Capsules

25°C (may be exposed to 15–30°C).101

Solution

Tight, light resistant containers at 20–25°C; protect from freezing.100

Rectal

Suppositories

15–30°C; do not refrigerate.c 103

Actions

  • Mechanism of action not fully elucidated; CNS depressant effect believed to result primarily from active metabolite trichloroethanol.c 103

  • CNS depressant effects similar to paraldehyde and barbiturates.c

  • Hypnotic doses produce mild cerebral depression and quiet, deep sleep.c

  • Higher doses may lead to general anesthesia and concurrent depression of respiratory and vasomotor centers; death may result from respiratory failure.c

  • Sedative or hypnotic doses have little anticonvulsant activity.c

  • Has little analgesic activity and may produce excitement or delirium in the presence of pain.c

Advice to Patients

  • Administer capsules with a full glass of water or liquid101 and oral solution with half glass of liquid (i.e., water, fruit juice, or ginger ale).100 (See Administration under Dosage and Administration)

  • Advise patients not to take CNS depressant drugs or alcohol concomitantly with chloral hydrate.100 101 103

  • Risk of dizziness or fatigue; potential for drug to impair mental alertness or physical coordination; use caution when driving or operating machinery until effects on the individual are known.100 101 c 103

  • Importance of informing clinicians of hypersensitivity to aspirin.103 (See Tartrazine Sensitivity under Warnings and Precautions.)

  • Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as concomitant illnesses.100 101 c 103

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed; breast-feeding may result in sedation of the infant.c 103

  • Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Chloral hydrate is subject to control under the Federal Controlled Substances Act of 1970 as a schedule IV (C-IV) drug.c

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Chloral Hydrate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Capsules, liquid-filled

500 mg*

Somnote (C-IV)

Breckenridge

Solution

500 mg/5 mL*

Chloral Hydrate Syrup (C-IV)

Pharmaceutical Associates

Rectal

Suppositories

325 mg

Aquachloral Supprettes (with tartrazine, C-IV)

Amerifit Pharma

500 mg

Chloral Hydrate Suppositories (C-IV)

G&W

650 mg

Aquachloral Supprettes (with tartrazine, C-IV)

Amerifit Pharma

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Somnote 500MG Capsules (BRECKENRIDGE): 50/$79.99 or 150/$229.98

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions April 1, 2009. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

100. Pharmaceutical Associates. Chloral hydrate syrup prescribing information. Greenville, SC; 2002 Oct.

101. Breckenridge Pharmaceutical. Somnote capsules prescribing information. Boca Raton, FL; 2004 Dec.

103. Amerifit Pharma. AquachloralSupprettes prescribing information. Woburn, MA; 2006 May.

104. Krauss B, Green SM. Sedation and analgesia for procedures in children. N Engl J Med. 2000; 342:938-45. [PubMed 10738053]

105. Sectish TC. Use of sedation and local anesthesia to prepare children for procedures. Am Fam Physician. 1997; 55:909-16. [PubMed 9048510]

106. Siberry GK, Iannone R, eds. The Harriet Lane handbook: a manual for pediatric house officers. 15th ed. Philadelphia, PA: Mosby: 2000:667.

107. American Academy of Pediatrics, American Academy of Pediatric Dentistry, Coté CJ, Wilson S, and the Work Group on Sedation. Guidelines for monitoring and management of pediatric patients during and after sedation for diagnostic and therapeutic procedures; an update. Pediatrics. 2006; 118::836-8.

108. American Academy of Pediatrics Committee on Drugs and Committee on Environmental Health. Use of chloral hydrate for sedation in children. Pediatrics. 1993; 92:471-3. [PubMed 8361811]

c. AHFS drug information 2007. McEvoy GK, ed. Chloral hydrate. Bethesda, MD: American Society of Health-System Pharmacists; 2007;2547-8.

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