Triazolam

Debilitated patients: Initially, 0.125 mg once daily at bedtime; may increase dose to Max 0.25 mg once daily at bedtime, if needed.

Dose reduction may be needed.

Dose reduction may be needed.

Should be taken on an empty stomach. Avoid grapefruit juice.

Myasthenia gravis and depression with suicidal tendencies. Pregnancy and lactation. Concomitant administration with opioids and CYP3A inhibitors.

Patient with respiratory depression, pulmonary disease (e.g. COPD), sleep apnoea, convulsive disorder, acute narrow-angle glaucoma, history of alcohol or drug abuse or dependence. Patients at risk of falls. Patients in whom drop in blood pressure may result in cerebral or cardiac complications. Not recommended as primary treatment for patients with depression and psychosis. Continuous long-term use is not recommended. Avoid abrupt withdrawal. Renal and hepatic impairment. Elderly or debilitated patients.

Significant: CNS depression, respiratory depression, anterograde amnesia, worsening of depression with suicidal ideation, increased frequency and/or severity of seizures (after abrupt withdrawal); increased risk of falls (particularly in elderly); paradoxical reactions (e.g. excitement, agitation, sleep disturbances, hallucinations, paranoia, acute rage); hazardous sleep-related activities (e.g. sleep-driving, making phone calls, and cooking and eating food while asleep); drug dependence, abuse or tolerance; withdrawal syndrome (particularly after abrupt discontinuation), rebound insomnia (following withdrawal of therapy). Rarely, hypotension, bloody dyscrasias, increased liver enzymes.
Cardiac disorders: Palpitations, tachycardia.
Ear and labyrinth disorders: Tinnitus.
Eye disorders: Visual disturbance.
Gastrointestinal disorders: Nausea, vomiting, constipation, diarrhoea, dysgeusia, dry mouth.
General disorders and administration site conditions: Lethargy, weakness, pain.
Musculoskeletal and connective tissue disorders: Asthenia, muscle cramps.
Nervous system disorders: Headache, dizziness, drowsiness, somnolence, ataxia, paraesthesia, dysaesthesia.
Psychiatric disorders: Impaired concentration, euphoria, confusion, nervousness, anxiety, abnormal dreams, nightmares, memory impairment.
Renal and urinary disorders: Urinary retention or incontinence.
Reproductive system and breast disorders: Change in libido.
Skin and subcutaneous tissue disorders: Rash, pruritus, dermatitis.
Potentially Fatal: Rarely, severe hypersensitivity reactions including anaphylaxis or angioedema.

PO: X

This drug may cause drowsiness and impaired alertness, if affected, do not drive, or operate machinery.

Monitor respiratory rate. Assess for individual risk for abuse, misuse, and addiction before and during treatment.

Symptoms: Drowsiness, mental confusion, slurred speech, lethargy, diminished reflexes, and in more serious cases, ataxia, hypotonia, hypotension, respiratory depression, apnoea, occasional seizures, and coma. Management: Symptomatic and supportive treatment. Induce vomiting (within an hour) if the patient is conscious or perform immediate gastric lavage with the airway protected for an unconscious patient. May administer activated charcoal to reduce absorption if there is no advantage in emptying the stomach. Flumazenil may be cautiously given as an adjunct to supportive management; flumazenil must not be used in mixed overdoses.

Additive CNS depressant effects with barbiturates, sedatives, TCAs, non-selective MAOIs, phenothiazines, other antipsychotics, anaesthetics, antihistamines, narcotic analgesics, skeletal muscle relaxants. Increased plasma concentration with macrolide antibiotics (e.g. erythromycin, clarithromycin), disulfiram, cimetidine, verapamil, and diltiazem. Concomitant administration with anticonvulsants may cause changes in serum concentration of anticonvulsants or triazolam.
Potentially Fatal: Increased risk of sedation, respiratory depression, and coma with opioids. Increased serum concentrations with strong CYP3A Inhibitors (e.g. itraconazole, ketoconazole, lopinavir, ritonavir, indinavir, nelfinavir, saquinavir, nefazodone.

May enhance CNS depressant effects with alcohol. May increase serum concentration with grapefruit juice.

Description:
Mechanism of Action: Triazolam is a potent short-acting benzodiazepine. It binds to stereospecific benzodiazepine receptors on the postsynaptic γ-aminobutyric acid (GABA) neuron within the CNS (including the limbic system and reticular formation). It enhances the GABA inhibitory effect on neuronal excitability by increasing neuronal membrane permeability to chloride ions, thus resulting in hyperpolarisation and stabilisation.
Onset: Hypnotic: 15-30 minutes.
Duration: Hypnotic: 6-7 hours.
Pharmacokinetics:
Absorption: Rapidly and nearly completely absorbed from the gastrointestinal tract. Time to peak plasma concentration: Within 2 hours.
Distribution: Crosses the placenta. Plasma protein binding: Approx 89%.
Metabolism: Extensively metabolised in the liver via hydroxylation by CYP3A4 with subsequent glucuronide conjugation into 4-hydroxytriazolam and α-hydroxytriazolam (short-acting active metabolites).
Excretion: Via urine (approx 80% as metabolites; small amounts as unchanged drug). Elimination half-life: 1.5-5.5 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5556, Triazolam. https://pubchem.ncbi.nlm.nih.gov/compound/Triazolam. Accessed Feb. 28, 2024.

Store between 20-25°C. Protect from light.

Thuốc ngủ & thuốc an thần

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

Anon. Triazolam. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 05/12/2023.

Anon. Triazolam. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/12/2023.

Buckingham R (ed). Triazolam. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/12/2023.

Halcion Tablet (Pharmacia & Upjohn Company LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 05/12/2023.

Inzolam 0.25 mg Tablet (Duopharma [M] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 05/12/2023.

Triazolam. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 16/01/2024.

Viatris Ltd. Hypam 0.125 mg, 0.25 mg, Tablets data sheet 24 March 2022. Medsafe. http://www.medsafe.govt.nz. Accessed 05/12/2023.