Triazolam (anxiolytic): indications, uses and side effects

The benzodiazepines are drugs generally used to treat anxiety disorders and associated problems.

These drugs have sedative, hypnotic and relaxing effects on the nervous system, being like a kind of chemical remedy that gives us artificial tranquility.

However, there is an exception: triazolam. Due to its chemical peculiarities, this drug, which belongs to the group already mentioned, is used for the treatment of sleep problems, especially acute insomnia.

Let's see why it is such a peculiar benzodiazepine and how it differs from the rest.

What is triazolam?

Triazolam is a medication belonging to the group of benzodiazepines., which has a depressant effect on the central nervous system. It was patented in 1970 and approved for sale in the United States from 1982, having wide use and support worldwide until the early 1990s.

This drug, like the other drugs belonging to the previously mentioned group, has relaxing, anticonvulsant, hypnotic, sedative, and amnestic effects. However, it differs from this group of drugs in that it is normally indicated for

sleeping problems more than anxiety disorders.

Mechanism of action

Triazolam is a very short-acting benzodiazepine anxiolytic. Its way of acting on the body is to increase the activity of the GABA, an inhibitory neurotransmitter of the nervous system, facilitating its union with the GABA-ergic receptor.

When a greater amount of this substance is found in the synaptic space, a greater sensation of calm is generated and sleep is induced.

Administration

Triazolam is available in tablet form.. In healthy adults, amounts between 0.125 and 0.250 mg daily are recommended. In the case of elderly people, debilitated patients or with some type of liver problem, the dose should not exceed 0.125 mg.

The drug is taken before going to bed and never accompanied by food, since its effect may be reduced. Shortly after consuming the medication, you begin to feel very sleepy, being asleep between 7 and 8 hours.

Triazolam is consumed for short periods, between 7 and 10 days, never extending the treatment for more than 2-3 weeks. The reason for this is that, from the week after starting the consumption of this benzodiazepine, the body develops tolerance, decreasing its main therapeutic effects.

Indications

The main use of this benzodiazepine is short-term treatment of acute insomnia, as well as circadian cycle disorders such as jet lag. The indication for insomnia is only when the sleep disorder is severe, disabling, or causes extreme exhaustion.

Its use is ideal for this type of problem because it acts very quickly and has a long half-life. short, causing the person who has consumed it to fall asleep in no more than an hour and half. It should be noted that triazolam induces sleep, but does not maintain it because, as it has a very short half-life, it is metabolized very quickly.

Another of the uses that triazolam has is in medical procedures, in which anesthesia is required, thanks to its powerful hypnotic power. It can also be used to reduce anxiety symptoms in specific situations, such as short and medium-haul air travel, particularly if the person has a particularly hard time in this type of routes.

Adverse effects

Among the most common side effects reported by triazolam patients are: drowsiness, dizziness, lightheadedness, headaches, skin tingling, coordination problems, nervousness, nausea and vomiting.

If one of the following symptoms appears, considered less common and more serious for health, you should immediately talk to your health care professional. the health that prescribed the drug: rash, hives, swelling in the eyes, face, tongue or throat, euphoria, rapid heartbeat, tiredness, cramps, depression, visual problems itching, feeling that the throat is closed, difficulties in breathing and swallowing and hoarseness.

Although they are not more common than the symptoms mentioned above, they can also occur: constipation, changes in the sense of taste, diarrhoea, dry mouth, dreams and nightmares, paraesthesia, tinnitus, dysesthesia, weakness and congestion.

Triazolam, although it is a short-acting benzodiazepine, can cause certain effects the morning after it is taken. The patient may feel as if he has a hangover, feeling drowsy, motor incoordination and decreased cognitive functions. Confusion and amnesia can also occur, this being especially striking since the person can do everyday actions but later not remember what he has been doing at all.

Contraindications and precautions for use

Among the main contraindications we find some that are shared with other benzodiazepines, such as chlordiazepoxide:

• Allergies to benzodiazepines.
• Myasthenia gravis.
• Respiratory insufficiency
• narrow angle glaucoma
• Sleep apnea
• Liver failure
• Acute alcohol poisoning
• Eat
• Syncope

The reason why it is contraindicated for myasthenia and respiratory failure is, Mainly, due to its relaxing capacity on the muscles, making these symptoms worse. medical conditions.

Special care should be taken in cases where the patient has a history of drug addiction, since the prolonged use of triazolam or its administration in high doses can generate physical and psychological dependence.

This drug is eliminated mainly by the kidneys, which is why in case of renal failure it should be monitor the dose with which this drug is administered or, if it is possible to find a better hypnotic option, prescribe it.

1. Interactions with other substances

Triazolam may interact with other substances. It should be noted that this substance is extensively metabolized in the liver and eliminated via the kidneys.

Drugs that have some type of hepatic action, such as oral contraceptives, can cause the plasmatic levels of the benzodiazepine to increase, increasing its effect and toxicity.

Precautions should be taken if the patient is taking calcium antagonists, azole antifungals, macrolide antibiotics, cimetidine, indinavir, isoniazid, nefazodone, and omeprazole.

It has been seen that the combination of alcohol and triazolam contributes to potentiating the depressant effects of the drug on the central nervous system.

Benzodiazepines have inhibitory effects on levodopa, a drug used for Parkinson's.

As a notable feature, the consumption of grapefruit juice is contraindicated if you are under treatment with triazolam, since this fruit increases the plasma levels of the drug by acting on the liver.

2. Dependence

With prolonged use, dependency may develop. In addition, abrupt interruption of treatment can cause withdrawal syndrome, which may manifest anxiety, agitation, aggressiveness, tremor, muscle spasm and insomnia.

If during the treatment high doses had been administered, its sudden withdrawal can cause delusions and convulsions to manifest.

For this reason, discontinuation of treatment should be done gradually, decreasing the dose in a controlled manner over a period between 4 and 8 weeks.

3. Overdose

As with other benzodiazepines, overdosage of this substance implies potentiated depressant effects on the central nervous system. In themselves, they are not usually dangerous, unless they have been combined with alcohol consumption.

Among the milder symptoms that the person can manifest are drowsiness, confusion and lethargy.

In more serious cases, hypotonia, ataxia, hypotension, respiratory depression, coma can occur in a very rare situation, and death in extremely unlikely cases.

To treat overdose with triazolam, as with other benzodiazepines such as chlordiazepoxide, flumazenil is used as an antidote.

4. Pregnancy and lactation

It has been suggested that the consumption of this drug during pregnancy can cause congenital malformations in the fetus. Also, once the baby is born, it may suffer tremors and irritability associated with the benzodiazepine.

In animal studies with rats, triazolam and its metabolites have been shown to be excreted in milk. That is why it is recommended not to breastfeed the baby if you are undergoing treatment or suspend it.

Bibliographic references:

• Adam, a. and Prat, G. (2016). Psychopharmacology: Mechanism of action, effect and therapeutic management. Barcelona, ​​Spain. Marge Medical Books.
• Lui, C. AND.; Amidon, G. L.; Goldberg, A. (1991). "Intranasal absorption of flurazepam, midazolam, and triazolam in dogs". J Pharm Sci. 80 (12): 1125–9.
• Rickels K. (1986). "The clinical use of hypnotics: indications for use and the need for a variety of hypnotics". Acta Psychiatr Scand Suppl. 74(S332): 132–41.
• Vademecum. (2016). Triazolam.