The active ingredient triazolam is available under the distribution name Halcion® on the market. It is an oral benzodiazepine derivative characterized by a low half-life. This is usually between two and five hours.
Triazolam is used as a sleeping aid. The remedy works directly by inhibiting certain regions of the brain. After a short period of use, however, both physical and mental withdrawal symptoms are in the range of the possible. The risk of dependence on the active ingredient is therefore significant.
In addition, triazolam is also abused as an intoxicant. For these reasons, the drug in Germany is under the Narcotics Act. Although it is considered as marketable, but always prescription. An unauthorized use of the drug or its distribution without presentation of a medical prescription are punishable in principle. An exception to these regulations are special preparations that contain no further anesthetics and contain a maximum of 0.25 milligrams of triazolam.
In animal experiments it has been shown that the active ingredient relatively quickly passes into both the fetal circulation and into breast milk. Since the action of triazolam starts relatively quickly with an average absorption half-life of one quarter of an hour, dependence on the substance is promoted.
Metabolism of the drug triazolam takes place in the liver, while urinary excretion occurs. In principle, triazolam is one of the very fast and short-acting benzodiazepines. The calming effect begins within 15 to 30 minutes after ingestion. The subsequent sleep period is usually between six and seven hours.
In the brain, the substance triazolam binds to specific receptors that are suitable for benzodiazepines. This triazolam increases the inhibitory effect of the messenger GABA. In this course, various associations of nerve nodes are affected. In this way, triazolam primarily exerts a sleep-inducing and calming effect. It also shows excitement and tension-releasing as well as anxiety-damping effects.
When taken in higher doses, triazolam sometimes reduces muscle tension and at the same time reduces the risk of epileptic seizures.
Since the drug triazolam is a benzodiazepine, it acts as a so-called allosteric modulator at the GABA-A receptors. If the neurotransmitter GABA is present, it intensifies its effect. If more chloride ions flow into a cell, it will lead to a hypopolarization. This makes the cell less susceptible to excitatory stimuli. Unlike barbiturates, which act on the chloride influx independently of GABA, benzodiazepines are associated with less risk of respiratory depression.
The maximum plasma concentrations are reached between 0.6 and 2.3 hours after oral administration. In contrast, the plasma half-life usually has large fluctuations ranging from 1.4 to 4.6 hours. The active substance is metabolised via a special hepatic system. Subsequently, the metabolites are largely eliminated renally.
Triazolam is classically prescribed for the treatment of sleep disorders. Both severe insomnia and jet lag are treated with triazolam.
In certain diagnostic procedures, for example in the context of diagnostic MRI examinations, triazolam is sometimes administered as a short-acting anxiolytic. Due to the high dependence potential, this administration is controversial. The likelihood of paradoxical reactions is also increased.
Because of its psychoactive properties, preparations containing triazolam as an intoxicant are abused. The bioavailability of triazolam is less than 50 percent when taken orally, while the bioavailability is more than 50 percent when taken sublingually. For this reason, preparations containing triazolam have a slightly stronger effect when patients let them melt under the tongue.
Triazolam is used for short-term therapy of severe sleep disorders. The tablets are taken shortly before bedtime.
The use of triazolam may be associated with various undesirable side effects. The most common side effects include dizziness, drowsiness, and coordination problems. Also, a drop in performance, memory disorders and restlessness are possible. Patients may experience drowsiness, balance disorders, muscle weakness, and a slower reaction time.
In addition, sometimes gastrointestinal disturbances, local skin reactions and allergies occur. Confusion, fatigue, blurred vision and respiratory depression can also occur as a result of taking triazolam.
The active substance triazolam should not be prescribed and used in case of hypersensitivity, severe respiratory distress, myasthenia gravis or serious mental illness. Also, non-simultaneous strong CYP inhibitors may be administered, such as HIV protease inhibitors or azole antifungals. Because these inhibit the metabolism of triazolam, can increase its concentration and thus trigger side effects.
Basically, a triazolam intake during pregnancy and lactation is foreseen.