Active Ingredients

Triazolam – Effect, Application & Risks

Triazolam

Triazolam is a short-acting benzodiazepine . The drug is commonly used as a sleep aid . The active ingredient belongs to the group of benzodiazepines and is characterized by a sleep-promoting and calming effect.

What is triazolam?

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 works directly by inhibiting certain regions in the brain . However, after only a short period of use, both physical and psychological withdrawal symptoms are possible. The risk of dependence on the active substance is therefore considerable.

In addition, triazolam is also abused as an intoxicant. For these reasons, the drug is subject to the Narcotics Act in Germany. Although it is considered marketable, it always requires a prescription. Unauthorized handling of the drug or its distribution without presentation of a doctor’s prescription are in principle punishable. An exception to these regulations are special preparations that do not contain any other narcotics and contain a maximum of 0.25 milligrams of triazolam.

Animal experiments have shown that the active ingredient passes relatively quickly both into the fetal circulation and into breast milk . Since the effect of triazolam sets in relatively quickly, with an average absorption half-life of a quarter of an hour, dependence on the substance is promoted.

Pharmacological action

Metabolism of the active substance triazolam takes place in the liver , while excretion occurs in the urine . In principle, the active ingredient triazolam is one of the very quickly and briefly effective benzodiazepines. The calming effect begins 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 messenger substance GABA . In this course, various associations of nerve nodes are influenced. In this way, triazolam primarily develops a sleep-inducing and calming effect. It also shows excitement and tension-relieving and anxiety-reducing effects.

When taken in higher doses, triazolam sometimes reduces muscle tension , thereby reducing the risk of epileptic seizures at the same time .

Since the active ingredient triazolam is a benzodiazepine, it acts as a so-called allosteric modulator on the GABA-A receptors. If the neurotransmitter GABA is present, it intensifies its effect. If more chloride ions flow into a cell , hypopolarization occurs. This makes the cell less sensitive to excitatory stimuli. Unlike such barbiturates, which affect chloride influx independently of GABA, benzodiazepines are associated with a lower risk of respiratory depression .

The active substance reaches its maximum plasma concentrations between 0.6 and 2.3 hours after oral administration. On the other hand, the plasma half-life usually shows large fluctuations, ranging between 1.4 and 4.6 hours. The active substance is metabolized via a special hepatic system. The metabolites are then largely eliminated via the kidneys.

Medical Application & Use

Triazolam is traditionally prescribed to treat insomnia. Both severe insomnia and jet lag are treated with triazolam.

In certain diagnostic procedures, such as diagnostic MRI scans, triazolam is sometimes administered as a short-acting anxiolytic. Due to the high potential for dependency, this administration is controversial. The probability 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, while the bioavailability when taken sublingually is over 50 percent. For this reason, preparations with triazolam have a slightly stronger effect when patients let them dissolve under the tongue .

Triazolam is used for short-term therapy of severe sleep disorders. The tablets are taken just before bedtime.

Risks & side effects

Taking triazolam can sometimes be associated with various undesirable side effects. The most common side effects include dizziness , drowsiness and incoordination . A drop in performance, memory disorders and restlessness are also possible. Patients may experience drowsiness , balance problems , muscle weakness , and a slowed reaction time .

In addition, gastrointestinal disorders, local skin reactions and allergies sometimes occur . Confusion , exhaustion , visual disturbances and respiratory depression can also occur as a result of taking triazolam.

The active substance triazolam should not be prescribed or taken in the case of hypersensitivity, severe respiratory disorders , myasthenia gravis or serious mental illnesses. Also, strong CYP inhibitors, such as HIV protease inhibitors or azole antimycotics, must not be administered at the same time. Because these inhibit the metabolism of triazolam, can increase its concentration and consequently trigger side effects.

Basically, you should refrain from taking triazolam during pregnancy and breastfeeding .

Lisa Newlon
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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.