Names and pronunciation
(trye-ay′zoe-lam) Halcion
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Drug reference
(trye-ay′zoe-lam) Halcion
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Func. class.: Sedative-hypnotic, antianxiety
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Chem. class.: Benzodiazepine, short acting Controlled Substance Schedule IV (USA), Targeted (CDSA IV) (Canada)
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Do not confuse: Halcion/Haldol/halcinonide
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ACTION: Produces CNS depression at limbic, thalamic, hypothalamic levels of CNS; may be mediated by neurotransmitter γ-aminobutyric acid (GABA); results are sedation, hypnosis, skeletal muscle relaxation, anticonvulsant activity, anxiolytic action
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USES: Insomnia, sedative/hypnotic
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CONTRAINDICATIONS: Preg- nancy, breastfeeding, hypersensitivity to benzodiazepines Precautions: Children <15 yr, geriatric patients, anemia, renal/hepatic disease, suicidal individuals, drug abuse, psy- chosis, acute closed-angle glaucoma, seizure disorders, angioedema, respira- tory disease, depression, sleep-related behaviors (sleep walking), intermittent porphyria, myasthenia gravis, Parkin- son’s disease
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Black Box Warning: Coadministration with other CNS depressants, respiratory depression, abrupt discontinuation, sub- stance abuse Black Box Warning: Increase: action of both products—alcohol, CNS depres- sants Increase: triazolam levels—CYP2C19 inhibitors (fluconazole, ketoconazole, omeprazole, hormonal contraceptives, ticlopidine Decrease: triazolam levels—CYP3A4 inducers (carBAMazepine, phenobarbi- tol, phenytoin, rifamycins, valproate) Decrease: effect of antacids, theophyl- line, rifAMPin Drug/Herb Increase: CNS depression—chamomile, hops, kava, lavender, valerian Drug/Food • Grapefruit may increase action; avoid concurrent use Drug/Lab Test Increase: ALT, AST, serum bilirubin Decrease: RAI uptake False increase: urinary 17-OHCS Black Box Warning: Respiratory de- pression: may occur more frequently with coadministration of other CNS de- pressants; monitor respirations often • Blood studies: Hct, HB, RBC if blood dyscrasias suspected (rare) • Hepatic studies: AST, ALT, bilirubin if hepatic damage has occurred • Mental status: mood, sensorium, af- fect, memory (long, short term), insom- nia, withdrawal symptoms, excessive se- dation, impaired coordination • Blood dyscrasias: fever, sore throat, bruising, rash, jaundice, epistaxis (rare) • Type of sleep problem: falling asleep, staying asleep • Safety: Assistance with ambulation af- ter receiving dose • Pregnancy/breastfeeding: do not use in pregnancy; not recommended in breastfeeding • Beers: avoid use in older adults; in- creased sensitivity to benzodiazepines and decreased metabolism; may cause or worsen delirium Black Box Warning: To avoid alcohol in- gestion, sedatives, hypnotics • That effects may take 2 nights for ben- efits to be noticed; that product is for short-term use only; to use for 7-10 continuous nights • About alternative measures to improve sleep: reading, exercise several hours before bedtime, warm bath, warm milk, TV, self-hypnosis, deep breathing • That complex sleep-related behaviors (sleep eating/driving) may occur • That hangover is common in geriatric patients but less common than with bar- biturates; that rebound insomnia may occur for 1-2 nights after discontinuing product; to discontinue by decreasing dose by 50% q2nights until 0.125 mg for 2 nights, then stop
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SIDE EFFECTS CNS: Headache, lethargy, drowsiness, daytime sedation, dizziness, confusion, light-headedness, anxiety, irritability, amnesia, poor coordination, complex sleep-related reactions: sleep driving, sleep eating CV: Chest pain, pulse changes, ECG changes GI: Nausea, vomiting, diarrhea, heart- burn, abdominal pain, constipation, hepatic injury SYST: Severe allergic reactions
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INTERACTIONS • Smoking may decrease hypnotic effect Increase: triazolam levels—CYP3A4 inhibi- tors, protease inhibitors (dilTIAZem, FLUoxetine, fluvoxaMINE, macrolides) Increase: effects of cimetidine, disulfi ram, erythromycin, clarithromycin, pro benecid, isoniazid, oral contraceptives; do T not use concurrently
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TREATMENT OF OVERDOSE: Lavage; monitor electrolytes, VS, flumazenil
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DOSAGE AND ROUTES • Adult: PO 0.125-0.5 mg at bedtime, max 0.5 mg/day • Geriatric: PO 0.0625-0.125 mg at bedtime, max 0.25 mg/day
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Available forms: Tabs 0.125, 0.25 mg
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Administer: • After trying conservative measures for insomnia • 1⁄2 hr before bedtime for sleeplessness • On empty stomach for fast onset; may be taken with food if GI symptoms occur • Avoid use with CNS depressants; seri- ous CNS depression may result
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Assess: • Severe allergic reactions: may occur during any use
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Evaluate: • Therapeutic response: ability to sleep at night, decreased amount of early morning awakening if taking product for insomnia
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To use reliable contraception • That dependence is possible after long-term use • To avoid driving, other activities re- quiring alertness until product is stabi- lized
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PHARMACOKINETICS Onset 15-30 min, duration 6-8 hr, metabolized by liver, excreted by kid- neys (inactive metabolites), crosses pla- centa, excreted in breast milk, half-life 1.5-5.5 hr
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• Adult: PO 0.125-0.5 mg at bedtime, max 0.5 mg/day
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• Geriatric: PO 0.0625-0.125 mg at bedtime, max 0.25 mg/day
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