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triazolam (Halcion)

Tradename: Halcion. DEA-controlled substance: class 4. Indications: insomnia, difficulty initiating sleep Dosage: - 0.125-0.5 mg PO QHS [1]. - 0.125-0.25 mg PO QHS [2]. Tabs: 0.125 & 0.25 mg. Pharmacokinetics: 1) ultra short-acting benzodiazepine 2) metabolized in liver by cyt P450 3A4 a) primarily metabolized by hydroxylation b) principal metabolite is alpha-hydroxytriazolam c) metabolites are pharmacologically inactive [2] Adverse effects: 1) profound anterograde amnesia 2) early morning rebound & anxiety [6] Drug interactions: 1) any drug that inhibits cyt P450 3A4 may increase levels of triazolam 2) any drug that induces cyt P450 3A4 may diminish levels of triazolam Laboratory: 1) specimen: serum, plasma (EDTA), urine 2) methods: a) serum/plasma: GLC, HPLC b) urine: EIA, FPIA, GC-MS

Interactions

drug interactions drug adverse effects (more general classes)

Related

cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)

General

benzodiazepine

Properties

MISC-INFO: elimination route KIDNEY 1/2life 2-3 HOURS protein-binding 88-92% pregnancy-category X safety in lactation -

Database Correlations

PUBCHEM cid=5556

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996.
  2. Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 7
  3. Saunders Manual of Medical Practice, Rakel (ed), WB Saunders, Philadelphia, 1996, pg 1087-89
  4. Clinical Guide to Laboratory Tests, NW Tietz (ed) 3rd ed, WB Saunders, Philadelpha 1995
  5. Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: 220233 (subscription needed) http://www.prescribersletter.com
  6. Geriatrics Review Syllabus, American Geriatrics Society, 5th edition, 2002-2004

Component-of

alprazolam/triazolam