trye-AZ-oh-lam

Therapeutic Classification: sedative/hypnotics

Pharmacologic Classification: benzodiazepines

• Short-term management of insomnia.

• Acts at many levels in the CNS, producing generalized depression.
• Effects may be mediated by GABA, an inhibitory neurotransmitter.

• Relief of insomnia.

Absorption: Well absorbed following oral administration.

Distribution: Widely distributed, crosses blood-brain barrier.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A4 isoenzyme. Primarily excreted in urine as metabolites.

Half-life: 1.6–5.4 hr.

(sedation)

Contraindicated in:

• Hypersensitivity
• Cross-sensitivity with other benzodiazepines may occur
• Pre-existing CNS depression
• Uncontrolled severe pain
• Concurrent use of strong CYP3A4 inhibitors.

Use Cautiously in:

• Hepatic impairment (↓ dose)
• History of suicide attempt or drug addiction
• OB: Use late in pregnancy can result in sedation (respiratory depression, lethargy, hypotonia) and/or withdrawal symptoms (hyperreflexia, irritability, restlessness, tremors, inconsolable crying, and feeding difficulties) in neonates
• Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant
• Pedi: Safety and effectiveness in children not established
• Geri: Appears on Beers list. ↑ risk of cognitive impairment, delirium, falls, fractures, and motor vehicle accidents in older adults. If possible, avoid use in older adults.

Derm: rash.

EENT: blurred vision.

GI: constipation, diarrhea, nausea, vomiting.

Neuro: dizziness, excessive sedation, hangover, headache, abnormal thinking, anterograde amnesia, behavior changes, confusion, depression, hallucinations, lethargy, paradoxical excitation, sleep-driving.
Misc: physical dependence, psychological dependence, tolerance.

Drug-Drug:

• Strong CYP3A4 inhibitors, including, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, and lopinavir, may ↑ levels and risk of toxicity; concurrent use contraindicated.
• Erythromycin, clarithromycin, and cimetidine may ↑ levels; consider ↓ triazolam dose.
• Strong CYP3A inducers may ↓ levels and effectiveness.
• Use with opioids or other CNS depressants, including other benzodiazepines, non-benzodiazepine sedative/hypnotics, anxiolytics, general anesthetics, muscle relaxants, antipsychotics, and alcohol, may cause profound sedation, respiratory depression, coma, and death; reserve concurrent use for when alternative treatment options are inadequate.
• May ↓ effectiveness of levodopa.
• May ↑ toxicity of zidovudine.
• Isoniazid may ↓ excretion and ↑ effects of triazolam.
• Sedative effects may be ↓ by theophylline.

Drug-Natural Products:

• Concomitant use of kava-kava, valerian, chamomile, or hops can ↑ CNS depression.

Drug-Food:

• Grapefruit juice significantly ↑ levels and risk of toxicity.

• PO (Adults): 0.125–0.25 mg (up to 0.5 mg) at bedtime.
• PO (Geriatric Patients): 0.125 mg at bedtime initially; may be ↑ as needed.

(Generic available)

• Tablets: 0.125 mg; 0.25 mg;

• Assess sleep patterns prior to and periodically throughout therapy.
• Assess CNS effects and risk of falls. Institute falls prevention strategies.
• Prolonged high-dose therapy may lead to psychological or physical dependence. Restrict the amount of drug available to patient, especially if patient is depressed, suicidal, or has a history of substance use disorder.
• Assess risk for addiction, abuse, or misuse prior to administration.
• Geri: Assess risk of falls and institute fall prevention strategies.

• Flumazenil is an adjunct in the management of toxicity or overdose. Flumazenil may induce seizures in patients with a history of seizures disorder or who are on tricyclic antidepressants.

• Supervise ambulation and transfer of patients following administration. Remove cigarettes. Side rails should be raised and call bell within reach at all times.
• Use lowest effective dose. Gradually taper the dose when discontinuing the therapy to decrease withdrawal symptoms. Some patients may require longer taper periods (mo).
• PO: Administer right before going to bed. Do not take with or right after a meal.

• Instruct patient to take triazolam as directed. Discuss the importance of preparing environment for sleep (dark room, quiet, avoidance of nicotine and caffeine). If less effective after a few wk, consult health care professional; do not increase dose. Must be discontinued gradually. Do not suddenly stop taking triazolam without consulting health care professional; may cause unusual movements, responses or expressions, seizures, sudden and severe mental or nervous system changes, depression, seeing or hearing things that others do not see or hear, an extreme increase in activity or talking, losing touch with reality, and suicidal thoughts or actions.
• Advise patient to avoid grapefruit and grapefruit juice during therapy.
• Advise patient that triazolam is a drug with known abuse potential. Protect it from theft, and never give to anyone other than the individual for whom it was prescribed. Store out of sight and reach of children and in a location not accessible by others.
• May cause daytime drowsiness or dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known. Instruct patient and family how to reduce falls risk at home. Geri: Advise older adults of increased risk for CNS effects and potential for falls.
• Inform patient that after taking triazolam patient may get out of bed and perform activities (driving a car ["sleep-driving"], making and eating food, talking on the phone, having sex, sleepwalking) while unaware. You may not remember anything done during the night; increased risk with alcohol or other CNS depressants.
• Advise patient to avoid the use of alcohol and other CNS depressants and to consult health care professional prior to using OTC preparations that contain antihistamines or alcohol.
• Instruct patient to notify health care professional if an increase in daytime anxiety occurs. May occur after as few as 10 days of therapy. May require discontinuation of triazolam.
• Advise patient to inform health care professional if confusion, depression, or persistent headaches occur. Instruct family or caregiver to notify health care professional if personality changes occur.
• May cause fetal harm. Advise females of reproductive potential to contact health care professional immediately if pregnancy is planned or suspected. Monitor infants exposed to triazolam during pregnancy or labor for several wk or more prior to delivery for signs and symptoms of withdrawal (hypoactivity, hypotonia, hypothermia, respiratory depression, apnea, feeding problems, impaired metabolic response to cold stress). Monitor infants exposed to triazolam during breastfeeding for excessive sedation, poor feeding, and poor weight gain, and advise family or caregiver to seek medical attention if they notice these signs. There is a pregnancy registry that monitors pregnancy outcomes in women exposed to psychiatric medications, including triazolam, during pregnancy. Health care providers are encouraged to register patients by calling the National Pregnancy Registry for Psychiatric Medications at 1-866-961-2388 or online at womensmentalhealth.org/pregnancyregistry/.
• Emphasize the importance of follow-up appointments to monitor progress.

• Improvement in sleep patterns, which may not be noticeable until the 3rd day of therapy.

Halcion

Schedule IV (C-IV)