Triazolam is a short-acting benzodiazepine. The drug is usually used as a sleep aid. The active ingredient belongs to the group of benzodiazepines and is characterized by a sleep-promoting and sedative effect.
What is triazolam?
Triazolam is a short-acting benzodiazepine. The drug is commonly used as a sleep aid. The active ingredient triazolam is available on the market under the sales name Halcion. It is an oral benzodiazepine derivative characterized by a short half-life. This is usually between two and five hours. Triazolam is used as a sleep aid. The drug acts in a direct way by inhibiting certain regions in the brain. After only a short period of use, however, both physical and psychological withdrawal symptoms are within the realm of possibility. The risk of dependence on the active substance is therefore considerable. In addition, triazolam is also abused as a narcotic. For these reasons, the drug is subject to the Narcotics Act in Germany. Although it is considered marketable, it is always subject to prescription. Unauthorized use of the drug or its distribution without a doctor’s prescription is in principle punishable by law. An exception to these regulations are special preparations that do not contain any other anesthetics and contain a maximum of 0.25 milligrams of triazolam. Animal studies have shown that the active ingredient passes relatively quickly both into the fetal circulation and into breast milk. Because the onset of action of triazolam is relatively rapid, with an average absorption half-life of one-quarter hour, dependence on the substance is promoted.
Pharmacologic Effects
Metabolism of the active ingredient triazolam occurs in the liver, while excretion occurs in the urine. In principle, the active ingredient triazolam is one of the very rapidly and briefly acting benzodiazepines. The sedative effect sets in within 15 to 30 minutes after ingestion. The subsequent sleep duration is usually between six and seven hours. In the brain, the substance triazolam binds to specific receptors that are suitable for benzodiazepines. As a result, triazolam increases the inhibitory effect of the neurotransmitter GABA. In this process, various associations of nerve nodes are influenced. In this way, triazolam primarily exerts a sleep-inducing and sedative effect. It also exhibits excitation- and tension-relieving as well as anxiety-reducing effects. If triazolam is taken in higher doses, it sometimes reduces muscle tension and thus at the same time reduces the risk of epileptic convulsions. Because triazolam is a benzodiazepine, it acts as an allosteric modulator at GABA-A receptors. If the neurotransmitter GABA is present, it intensifies its effect. When increased chloride ions enter a cell, hypopolarization occurs. This makes the cell less sensitive to excitatory stimuli. Unlike those barbiturates that act independently of GABA on chloride influx, benzodiazepines are associated with a lower risk of respiratory depression. The drug reaches maximum plasma concentrations between 0.6 to 2.3 hours after oral ingestion. In contrast, the plasma half-life usually exhibits wide variations, ranging from 1.4 to 4.6 hours. The drug is metabolized by a specific hepatic system. Subsequently, the metabolites are largely eliminated renally.
Medical application and use
Triazolam is classically prescribed for the treatment of sleep disorders. In this context, both severe insomnia and jet lag are treated with triazolam. In certain diagnostic procedures, such as diagnostic MRI examinations, triazolam is sometimes administered as a short-acting anxiolytic. Due to its high dependence potential, this administration is controversial. The likelihood of paradoxical reactions is also increased. Because of its psychoactive properties, preparations containing triazolam are abused as intoxicants. The bioavailability of triazolam is less than 50 percent when taken orally, whereas the bioavailability is over 50 percent when taken sublingually. For this reason, preparations containing triazolam have a slightly stronger effect when patients allow them to dissolve under the tongue.Triazolam is used for the short-term treatment of severe sleep disorders. In this case, the tablets are taken shortly before bedtime.
Risks and side effects
Taking triazolam may be associated with various unwanted side effects in some circumstances. The most common side effects include dizziness, drowsiness, and impaired coordination. A drop in performance, memory impairment, and restlessness are also possible. Patients may suffer from drowsiness, balance disorders, muscle weakness and slowed reaction time. In addition, gastrointestinal disturbances, local skin reactions and allergies sometimes occur. Confusion, fatigue, visual disturbances, and respiratory depression may also occur as consequences of triazolam ingestion. The active ingredient triazolam should not be prescribed and taken in cases of hypersensitivity, severe respiratory disorders, myasthenia gravis, and serious mental illness. Strong CYP inhibitors, such as HIV protease inhibitors or azole antifungals, should also not be administered at the same time. This is because these inhibit the metabolism of triazolam, can increase its concentration and consequently trigger side effects. In principle, triazolam should not be taken during pregnancy or while breastfeeding.
