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chloral [hydrate] (Noctec)

Tradename: Noctec. (trichloroacetaldehyde monohydrate) DEA-controlled substance: class 4. Indications: 1) short-term (< 2 weeks) sedative/hypnotic - 500 mg PO QHS 2) sedation, general anesthesia for dental & diagnostic procedures - 500 to 1000 mg 15-30 minutes prior to procedure 3) sedation prior to EEG 4) used as alcohol replacement in alcohol withdrawal - 500 to 1000 mg PO every 6 hours PRN Contraindications: recovered alcoholics Dosage: 25-50 mg/kg up to 1000 mg PO. Max 75 mg/kg. Tabs: 250 & 500 mg. Syrup: 250 & 500 mg/5 mL. Suppositories: 345, 500, 648 mg. Pharmacokinetics: 1) well absorbed after oral administration 2) peak effect within 30 minutes to 1 hour 3) duration of action 4-8 hours 4) metabolized by liver to active metabolite trichloroethanol (active metabolite) Adverse effects: 1) common (> 10%) - nausea/vomiting - stomach pain 2) less common (1-10%) - skin rash, clumbsiness, hallucinations, diarrhea, drowsiness, "hangover" 3) uncommon (< 1%) - confusion, disorientation, sedation, ataxia, paradoxical excitement, dizziness, fever, headache, gastric irritation, flatulence, leukopenia, eosinophilia, addiction (physical & psychological) may occur with prolonged use of large doses Drug interactions: 1) chloral hydrate may increase effects of: a) warfarin b) CNS depressants c) alcohol 2) concurrent use of furosemide (Lasix) may result in flushing, diaphoresis & changes in blood pressure 3) concurrent use of metronidazole (Flagyl) causes a disulfiram-like reaction Laboratory: 1) specimen: serum 2) methods: GLC, color 3) interferences: a) other chlorinated hydrocarbons may interfere with colorimetric assay b) substances metabolized to trichloroethanol will interfere with GLC assay Mechanism of action: CNS depressant

Interactions

drug adverse effects (more general classes)

General

aldehyde sedative/hypnotic (tranquilizer)

Properties

MISC-INFO: elimination route LIVER KIDNEY 1/2life 4 MIN 4-14 HOURS therapeutic-range 2-12 UG/ML toxic-range >20 UG/ML protein-binding 35% elimination by hemodialysis + hemoperfusion + pregnancy-category C safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  4. Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995