Triazolamum
Triazolamum Uses, Dosage, Side Effects, Food Interaction and all others data.
Withdrawn in the United Kingdom due to risk of psychiatric adverse drug reactions. This drug continues to be available in the U.S. Internationally, triazolam is a Schedule IV drug under the Convention on Psychotropic Substances.
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. Triazolamum has a shorter half-life than chlordiazepoxide, flurazepam, and prazepam and does not generate active metabolites.
| Trade Name | Triazolamum |
| Availability | Prescription only |
| Generic | Triazolam |
| Triazolam Other Names | Triazolam, Triazolamum |
| Related Drugs | amitriptyline, lorazepam, melatonin, zolpidem, diphenhydramine, Ativan |
| Type | |
| Formula | C17H12Cl2N4 |
| Weight | Average: 343.21 Monoisotopic: 342.043901818 |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
How Triazolamum works
Benzodiazepines bind nonspecifically to bezodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
Toxicity
Symptoms of overdose include drowsiness, slurred speech, motor inco-ordination, coma, and respiratory depression.
Food Interaction
- Avoid alcohol. Ingesting alcohol may increase the risk of complex behaviors like sleep-driving, which the patient does not remember.
- Avoid grapefruit products. Grapefruit may reduce the CYP3A4 metabolism of triazolam, which increases the serum concentration of triazolam.
[Moderate] GENERALLY AVOID: The pharmacologic activity of oral midazolam, triazolam, and alprazolam may be increased if taken after drinking grapefruit juice.
The proposed mechanism is CYP450 3A4 enzyme inhibition.
In addition, acute alcohol ingestion may potentiate CNS depression and other CNS effects of many benzodiazepines.
Tolerance may develop with chronic ethanol use.
The mechanism may be decreased clearance of the benzodiazepines because of CYP450 hepatic enzyme inhibition.
Also, it has been suggested that the cognitive deficits induced by benzodiazepines may be increased in patients who chronically consume large amounts of alcohol.
MANAGEMENT: The manufacturer recommends that grapefruit juice should not be taken with oral midazolam.
Patients taking triazolam or alprazolam should be monitored for excessive sedation.
Alternatively, the patient could consume orange juice which does not interact with these drugs.
Patients should be advised to avoid alcohol during benzodiazepine therapy.
Triazolamum Drug Interaction
Major: acetaminophen / hydrocodoneModerate: zolpidem, duloxetine, cyclobenzaprine, escitalopram, pregabalin, quetiapine, alprazolam, sertraline, cetirizineUnknown: amphetamine / dextroamphetamine, rosuvastatin, omega-3 polyunsaturated fatty acids, esomeprazole, levothyroxine, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, lisdexamfetamine
Triazolamum Disease Interaction
Major: acute alcohol intoxication, closed-angle glaucoma, drug dependence, renal/liver disease, respiratory depression, seizuresModerate: depression, obesity, paradoxical reactions
Elimination Route
Bioavailability is 44% (oral) and 53% (sublingual).
Half Life
1.5-5.5 hours
Elimination Route
Triazolamum and its metabolites, principally as conjugated glucuronides, which are presumably inactive, are excreted primarily in the urine. Only small amounts of unmetabolized triazolam appear in the urine. The two primary metabolites accounted for 79.9% of urinary excretion.
Innovators Monograph
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