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 one exception: triazolam This drug, which belongs to the group already mentioned, 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 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 starting in 1982, having wide use and support worldwide until the early 90’s.
This drug, like the other medications belonging to the aforementioned group, has relaxing, anticonvulsant, hypnotic, sedative and amnesic effects. However, it differs from this group of medications 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 body 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 amount of this substance is found in the synaptic space, a greater feeling of calm is generated and sleep is induced.
Administration
Triazolam is sold in tablet form In healthy adults, amounts between 0.125 and 0.250 mg daily are recommended. In the case of elderly people, weakened 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 medication, he begins to feel very sleepy, sleeping between 7 and 8 hours.
The consumption of triazolam is carried out for short periods, between 7 and 10 days, and the treatment should never be extended for more than 2-3 weeks. The reason for this is that, starting a week after starting the consumption of this benzodiazepine, the body 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, 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-distance air travel, specifically if the person has a particularly bad time on this type of journey.
Adverse effects
Among the most common side effects reported by triazolam patients are: drowsiness, dizziness, lightheadedness, headaches, tingling skin, coordination problems nervousness, nausea and vomiting.
If one of the following symptoms occurs, considered less common and more serious for health, you should speak immediately with the health professional who prescribed the drug: rash, hives, swelling of the eyes, face, tongue or throat, euphoria, tachycardia, tiredness, cramps, depression, visual problems, itching, sensation of the throat closing, difficulties breathing and swallowing, and hoarseness.
Although they are not more common than the previously mentioned symptoms, they can also occur: constipation, changes in the sense of taste, diarrhea, dry mouth, dreams and nightmares, parasthesia, tinnitus, dysesthesia, weakness and congestion.
Triazolam, although a short-acting benzodiazepine, can cause certain effects the morning after being taken. The patient may feel as if he or she has a hangover, feeling drowsy, motor incoordination, and decreased cognitive functions. Confusion and amnesia can also occur, this being especially striking given that the person can do everyday actions but then not remember at all what they have been doing.
Contraindications and precautions for use
Among the main contraindications we find some that are shared with other benzodiazepines, such as chlordiazepoxide:
The reason why it is contraindicated for myasthenia and respiratory failure is, mainly, because of its relaxing ability on the muscles, making these medical conditions worse.
Special care should be taken in cases where the patient has a history of drug addiction given that prolonged use of triazolam or its administration in high doses can generate physical and psychological dependence.
This drug is eliminated mainly through the kidneys, which is why if you suffer from kidney failure, you should 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 widely metabolized in the liver and eliminated through the kidneys.
Drugs that have some type of hepatic action, such as oral contraceptives, can cause the plasma 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 the potentiation of the depressant effects of the drug on the central nervous system.
Benzodiazepines have inhibitory effects on levodopa, the 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. Dependency
With prolonged use, dependence may develop. Furthermore, abrupt interruption of treatment can cause withdrawal syndrome, which may cause anxiety, agitation, aggressiveness, tremor, muscle spasm and insomnia.
If high doses have been administered during treatment, sudden discontinuation may cause delirium and seizures to occur.
It is for this reason that the interruption of treatment should be done progressively, decreasing the doses in a controlled manner over a period between 4 and 8 weeks.
3. Overdose
As with other benzodiazepines, Overdosage of this substance implies enhanced 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 experience 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 breastfeeding
It has been suggested that Consumption of this drug during pregnancy can cause congenital malformations in the fetus Also, once the baby is born, he or she may suffer tremors and irritability associated with the benzodiazepine.
In animal studies with rats, triazolam and its metabolites have been shown to be excreted through milk. This is why it is recommended not to breastfeed your baby if you are undergoing treatment or to discontinue it.