Drug information of Triazolam

Triazolam

Drug group:

Triazolam is a short-acting benzodiazepine used in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges.

Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries.

Mechanism of effect

Depresses all levels of CNS, possibly by increasing membrane permeability to chloride ions, which in turn increases the inhibitory activity of GABA on neuronal excitability.

Pharmacodynamic

A short-acting benzodiazepine used as a hypnotic agent in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges.

 Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries. Triazolam has a shorter half-life than chlordiazepoxide, flurazepam, and prazepam and does not generate active metabolites.

Pharmacokinetics

  • Half-Life: 1.5-5.5 hr
  • Peak plasma time: 0.5-2 hr
  • Onset of action: 15-30 min
  • Vd: 0.8-1.8 L/kg
  • Protein binding: 89%
  • Duration: 6-7 hr
  • Peak plasma concentration: 1-6 ng/mL
  • Metabolism: CYP3A4, glucuronic acid conjugation
  • Metabolites: Inactive metabolites
  • Excretion: Urine

Drug indications

Insomnia

Dosage

Tablet: Schedule IV

0.125mg

0.25mg

Insomnia

0.125-0.25 mg PO qHS

Maximum dose: 0.5 mg PO qHS

Dosage Modifications

Hepatic impairment: Administer a lower dose; avoid use in cirrhosis

Renal impairment: Use with caution in patients with renal impairment.

Respiratory disease: Use with caution in patients with respiratory compromise, COPD or sleep apnea.

Drug contraindications

Myasthenia gravis , angle-closure glaucoma

Alerts

Concerns related to adverse effects:

Anterograde amnesia: Benzodiazepines have been associated with anterograde amnesia, particularly benzodiazepines with short half-lives such as triazolam.

CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).

CNS effects: Abnormal thinking and behavior changes including excessive aggressiveness and extroversion, bizarre behavior, agitation, hallucinations, and depersonalization have been reported with the use of benzodiazepine hypnotics. Some evidence suggests symptoms may be dose-related.

Hypersensitivity reactions: Reports of hypersensitivity reactions, including anaphylaxis and angioedema, have been reported with triazolam. Patients who develop angioedema should not be rechallenged with triazolam.

Paradoxical reactions: Paradoxical reactions, including hyperactive or aggressive behavior, have been reported with benzodiazepines, particularly in adolescent/pediatric or psychiatric patients.

Sleep-related activities: An increased risk for hazardous sleep-related activities such as sleep-driving, cooking and eating food, having sex, and making phone calls while asleep have also been noted. Concurrent use of alcohol and other CNS depressants as well as exceeding the maximum recommended dose may increase the risk of these behaviors. Patients will often not remember doing these activities. Consider discontinuation of therapy for patients who report sleep-driving episodes.

Disease-related concerns:

Depression: Use caution in patients with depression, particularly if suicidal risk may be present. Minimize risks of overdose by prescribing the least amount of drug that is feasible in suicidal patients. Worsening of depressive symptoms has also been reported with use of benzodiazepines.

Special populations:

Debilitated patients: Use with caution in debilitated patients; potential for oversedation, impaired coordination, and dizziness with use.

Elderly: Elderly patients experience greater sedation and increased psychomotor impairment.

Other warnings/precautions:

Tolerance: Triazolam is a short half-life benzodiazepine. Duration of action after a single dose is determined by redistribution rather than metabolism. Chronic use of this agent may increase the perioperative benzodiazepine dose needed to achieve desired effect.

Points of recommendation

Use with caution in patients with a history of drug abuse or acute alcoholism; potential for drug dependency exists. Tolerance, psychological and physical dependence may occur with prolonged use.

Rebound insomnia or withdrawal symptoms may occur following abrupt discontinuation or large decreases in dose. Use caution when reducing dose or withdrawing therapy; decrease slowly and monitor for withdrawal symptoms. An increase in daytime anxiety may occur after as few as 10 days of continuous use, which may be related to withdrawal reaction in some patients.

Prescriptions for Triazolam should be written for short-term use (7–10 days) and it should not be prescribed in quantities exceeding a 1-month supply.

Pregnancy level

X


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