Triazolam

Oral
Short-term management of insomnia

Debilitated patients: Initially, 125 mcg at bedtime. Max: 250 mcg.

Severe: Initially, 125 mcg.

May be taken with or without food.

Pregnancy. Concomitant use w/ CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, nefazodone, several HIV protease inhibitors).

Patient w/ signs and symptoms of depression, chronic pulmonary insufficiency and sleep apnoea. Patient w/ a history of alcoholism, drug abuse, or in patient w/ marked personality disorders. Long-term use may lead to dependence. Avoid abrupt withdrawal in long-term treatment. Renal and hepatic impairment. Elderly and debilitated patients. Lactation.

Anterograde amnesia, abnormal thinking, behavioural changes, agitation, hallucinations, bizarre behaviour, depersonalisation; hypersensitivity reactions (e.g. angioedema); paradoxical reactions (e.g. hyperactive or aggressive behaviour); sleep-related activities (e.g. sleep-driving); drowsiness, headache, dizziness, ataxia, lightheadedness, nervousness, nausea, vomiting, confusion, cramps, depression, dermatitis, dreaming/nightmares, dysaesthesia, euphoria, fatigue, hepatic failure (fulminant), memory impairment, pain, paraesthesia, tachycardia, violent acts, visual disturbance, weakness, xerostomia, burning tongue/glossitis/stomatitis, chest pain, dysarthria, jaundice, libido changes, menstrual irregularities, pruritus, sedation, slurred speech, urinary incontinence, urinary retention.
Potentially Fatal: Anaphylaxis.

PO: X

May impair ability to drive or operate machinery.

Monitor daytime alertness, resp rate and behaviour profile.

Symptoms: Somnolence, confusion, impaired coordination, slurred speech, and ultimately, coma; resp depression, apnoea, seizures. Management: Perform immediate gastric lavage w/ maintenance of adequate airway. IV fluids may be administered. Flumazenil may be used as antidote.

Increased plasma concentrations w/ macrolide antibiotics, cimetidine, isoniazid, OCs and ranitidine.
Potentially Fatal: CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, nefazodone, several HIV protease inhibitors) may significantly increase plasma concentrations of triazolam.

Alcohol may enhance the CNS effects of triazolam. Increased plasma concentrations w/ grapefruit juice.

Description: Triazolam binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites w/in the CNS, including the limbic system, reticular formation. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to Cl ions, which results in hyperpolarisation (a less excitable state) and stabilisation. Benzodiazepine receptors and effects appear to be linked to the GABA-A receptors.
Onset: 15-30 min.
Pharmacokinetics:
Absorption: Rapidly and nearly completely absorbed from the GI tract. Time to peak plasma concentration: W/in 2 hr.
Distribution: Volume of distribution: 0.6-1.7 L/kg. Plasma protein binding: Approx 89%.
Metabolism: Hepatically via hydroxylation by CYP3A4 isoenzyme.
Excretion: Via urine (approx 80%, mainly as conjugated metabolites and small amounts as unchanged drug). Plasma elimination half-life: 1.5-5.5 hr.

Source: National Center for Biotechnology Information. PubChem Database. Triazolam, CID=5556, https://pubchem.ncbi.nlm.nih.gov/compound/Triazolam (accessed on Jan. 23, 2020)

Store between 20-25°C.

Anxiolytics / Hypnotics & Sedatives

N05CD05 - triazolam ; Belongs to the class of benzodiazepine derivatives. Used as hypnotics and sedatives.

Anon. Triazolam. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 27/11/2014.

Buckingham R (ed). Triazolam. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 27/11/2014.

Halcion Tablet (Pharmacia and Upjohn Company). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 27/11/2014.

McEvoy GK, Snow EK, Miller J et al (eds). Triazolam. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 27/11/2014.