triazolam

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.

Adv. Reactions/Side Effects ⬆ ⬇

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

Interactions ⬆ ⬇

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 otherbenzodiazepines, 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.

Availability ⬆ ⬇

(Generic available)

Tablets: 0.125 mg; 0.25 mg

Route/Dosage ⬆ ⬇

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.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

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

Therapeutic effects:

Relief of insomnia.

Classifications ⬆ ⬇

Therapeutic Classification: sedative/hypnotics

Pharmacologic Classification: benzodiazepines

Pharmacokinetics ⬆ ⬇

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.

Contr. Subst. Schedule ⬆ ⬇

Time/Action Profile ⬆ ⬇

(sedation)

ROUTE	ONSET	PEAK	DURATION
PO	15–30 min	6–8 hr	unknown

Patient/Family Teaching ⬆ ⬇

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.
Rep: 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 https://womensmentalhealth.org/pregnancyregistry/.
Emphasize the importance of follow-up appointments to monitor progress.

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Indications ⬇

Contraind./Precautions ⬆ ⬇