Triazolam (anxiolytic): indications, uses and side effects

This type of benzodiazepine has a short action and is used to combat certain cases of anxiety.

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 a sort of chemical remedy that provides artificial tranquility.

However, there is one exception: triazolam.. This drug, which belongs to the aforementioned group, due to its chemical peculiarities 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 drug, belonging to the benzodiazepine group, which has a depressant effect on sleep.It has a depressant effect on the central nervous system. It was patented in 1970 and approved for sale in the United States as of 1982, having a wide use and support worldwide until the early 90's. This drug, like the other drugs belonging to the aforementioned group, has relaxing, anticonvulsant, hypnotic, sedative and amnesic effects.

This drug, like the other drugs belonging to the aforementioned group, has relaxing, anticonvulsant, hypnotic, sedative and amnesic effects. However, it differs from this group of drugs in that it is usually indicated for sleep problems rather than anxiety disorders.

Mechanism of action

Triazolam is a very short-acting benzodiazepine anxiolytic. Its way of acting on the organism consists of increasing the activity of GABA, an inhibitory neurotransmitter of the nervous system, facilitating its binding with the GABA-ergic receptor.

As a greater quantity of this substance is found in the synaptic space, a greater sensation of calmness is generated and sleep is induced.

Administration

Triazolam is marketed 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 those with some type of liver problem, the dose should not exceed 0.125 mg.

The drug is taken before going to bed and never with food, since its effect may be reduced. Shortly after taking the drug, you will start to feel very sleepy, being asleep for 7 to 8 hours.

Triazolam is taken for short periods of time, between 7 and 10 days, and the treatment should never be extended for more than 2-3 weeks. The reason for this is that, from one week after starting the consumption of this benzodiazepine, the organism develops tolerance, reducing 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 short half-life, causing the person who has consumed it to fall asleep in no more than an hour and a half. It should be noted that triazolam induces sleep, but does not maintain it because, having a very short half-life, it is metabolized very quickly.

Another use of triazolam is in medical procedures where anesthesia is required, thanks to its powerful hypnotic power. It can also be used to reduce anxiogenic symptomatology in specific situations, such as short and medium distance air travel, especially if the person has a particularly bad time during this type of journey.

Adverse effects

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

If one of the following symptoms, considered less common and more serious to your health, occur, you should immediately talk to the health care professional who prescribed the drug: rash; hives; swelling of the eyes, face, tongue or throat; euphoria; rapid heartbeat; tiredness; cramps; depression; visual problems; itching; closing of the throat; difficulty breathing and swallowing; and hoarseness.

Although not more common than the above symptoms, constipation, taste changes, diarrhea, dry mouth, dreams and nightmares, paraesthesia, tinnitus, dysesthesia, weakness and congestion may also occur.

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

Contraindications and precautions for use

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

• Allergies to benzodiazepines.
• Myasthenia gravis.
• Respiratory insufficiency
• Narrow angle glaucoma
• Sleep apnea
• Hepatic insufficiency
• Acute alcohol intoxication
• Coma
• Syncope

The reason why it is contraindicated for myasthenia and respiratory insufficiency is mainly because of its relaxing capacity on the musculature, making these medical conditions worse.

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

This drug is eliminated mainly through the kidneys, therefore, in case of renal insufficiency, the dose with which this drug is administered should be monitored or, if it is possible to find a better hypnotic option, it should be prescribed.

1. Interactions with other substances

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

Drugs that have some type of hepatic action, such as oral contraceptives, may increase the plasma levels of the benzodiazepine, 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.

The combination of alcohol and triazolam has been shown to contribute to the potentiation of the depressant effects of the drug on the central nervous system.

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

As a special 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, dependence may develop. In addition, abrupt discontinuation of treatment may cause withdrawal syndrome, which may manifest as anxiety, agitation, aggressiveness, tremor, muscle spasm and insomnia.

If high doses have been administered during treatment, sudden discontinuation of treatment may lead to delirium and convulsions.

For this reason, treatment should be discontinued progressively, decreasing the doses in a controlled manner over a period of 4 to 8 weeks.

3. Overdose

As with other benzodiazepines, overdosage of this substance involves 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 may manifest are drowsiness, confusion and lethargy.

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

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 may 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, it has been shown that triazolam and its metabolites are excreted through milk. For this reason, it is recommended not to breastfeed the baby in case of treatment or to discontinue treatment.

Bibliographic references:

• Adán, A. and Prat, G. (2016). Psychopharmacology: mechanism of action, effect and therapeutic management. Barcelona, Spain. Marge Medica Books.
• Lui, C. Y.; 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.