Midazolam: uses and side effects of this anxiolytic

Anxiety is one of the most common problems today. In fact, a large majority of the Western population has had or will have an episode of anxiety or panic attack in their lives. And while for some it may be something that has happened at some point in time, for others it may become commonplace and require some type of treatment.

In this sense, at the pharmacological level we have substances that allow us to lower anxiety levels in specific situations. This is the most used and widespread group of psychoactive drugs among the population: anxiolytics. And within these, benzodiazepines stand out, with applications not only for anxiety itself but also for other conditions.

An example of this type of drug is midazolam., which we are going to talk about throughout this article.

• Related article: "Types of psychoactive drugs: uses and side effects"

Midazolam: what is it?

Midazolam is an anxiolytic drug, that is, a drug that through its action on the brain neurotransmission systems allows to treat conditions such as anxiety, agitation and extreme nervousness.

Within anxiolytics, it is part of the benzodiazepines, the most popular group of anxiolytics used in anxiety and whose appearance allowed unseat barbiturates (effective but much more dangerous and addictive) in addition to having multiple applications in different types of disorders.

Is about a sedative-hypnotic drug and also has anticonvulsant effect. Although it is not considered an anesthetic, it has a slight effect at this level which, together with sedation, means that it is often applied as a preparation for anesthesia and in conjunction with other drugs.

Midazolam is a short-lived benzodiazepine, which means that its effects take a short time to wear off (on average 2.3 hours, although it may range between 2.2 and 6.8 depending on body mass), although on the other hand its effects are almost immediate (it begins to have sedative effects at two minutes). It is metabolized in the liver and is excreted mainly via the kidneys.

On the other hand, midazolam is a well-known product with multiple applications, and it is available in various presentations for its administration by oral route (the most common in the form of tablets or tablets), intravenous or intramuscular (presentation as injection), intranasal or even rectal. It can be used in children older than 6 months, although it requires very controlled doses prescribed by the doctor. In the case of children under this age, there is a risk of respiratory depression.

Unfortunately, it is also famous for a controversial application in the United States: it is one of the drugs with a sedative effect that is applied to prisoners sentenced to prison. capital before subjecting them to lethal injection, in order to render them unconscious (high doses are used) before other substances are applied that will cause death. death.

Still, the drug has a weak anesthetic effect and is not approved as such, and in fact there have been judicial litigation so that it ceases to be applied in this way, since there have been cases of prisoners in which they did not it worked.

• You may be interested in: "Types of anxiolytics: drugs that fight anxiety"

Mechanism of action: how does it work?

Like many other benzodiazepines, midazolam acts on our body through a mechanism based on alteration of the GABAergic system. Specifically, midazolam is an indirect agonist of gamma-aminobutyric acid or GABA, which is one of the main inhibitory neurotransmitters in the brain.

This mechanism implies that the drug acts by activating the GABAergic receptors of the nervous system, something that has the effect of inhibiting the system and reduced level of brain activation. This action is especially relevant in the limbic system, which is linked to emotional responses, including anxiety.

Indications in pharmacological treatments

As we have seen, there are various different indications for this substance. Since it is a short-lived anxiolytic, it is especially indicated in those situations in which a sudden attack of anxiety and agitation appearssuch as an anxiety attack. It can also be used to induce sleep in people with conciliation insomnia (that is, they have trouble falling asleep).

Another of its main indications and uses is at the medical level, as a sedative drug to relax patients. before any type of surgical intervention or in a situation of being in the intensive care unit.

It is also applied at the level of anesthesia, mainly as a predrug or for the induction of the administration of other anesthetics. In addition, it is used as initial antiepileptic treatment in seizures, or in problems related to muscle spasticity as it can help relax the muscles.

Side effects

As with other drugs, midazolam also can cause side effects or side effects and undesirables. Among them is the presence of prolonged sedation, headaches, nausea and vomiting, erythema, fatigue, movements tremors, euphoria, agitation, confusion, incoordination, hallucinations, constipation, dry mouth, or allergic reactions.

Being sedative it can cause falls and fractures, especially in the elderly. Also hypotension and vasodilatation, respiratory disorders may appear which can lead to respiratory depression and arrest, decreased level of consciousness, tremors and aggressive behavior (a possible paradoxical effect).

Seizures have also been observed in some cases (especially in children or as an effect of withdrawal syndrome). The possible hypotension and slowing of the heart and respiratory rate are especially relevant.

Last but not least, this and other benzodiazepines They can generate dependency and be linked to abusive uses (in the case of midazolam it is easier as its action is quick and short) and even in overdoses that can lead to coma and even death, as well as withdrawal syndromes (something that makes its withdrawal must be gradual).

contraindications

Although the effects of this drug can be very useful, the truth is that midazolam can be Contraindicated for some population groups due to the risk that its effects on the body may entail.

These include all those people who are allergic or hypersensitive to this drug or any of its components. They also have it contraindicated people suffering from respiratory failure or depression, as well as those with heart problems, sleep apnea or have a serious chronic illness.

It is not recommended or great caution should be taken by those with renal or hepatic insufficiency. Neither should it be used by people with myasthenia or glaucoma, people in a coma, or those who are under the influence of alcohol or other depressants.

Concomitant use with other drugs should also be avoided, and their suitability should be consulted with the doctor since in some cases it can interact and see its effects enhanced or diminished. Among them we can find some antidepressants, antihypertensives, antihistamines, antiretrovirals (as in the case of some of the protease inhibitors used in HIV), ketoconazole, fluconazole, diltiazem or some antibiotics.

Pregnant and lactating women should not use it unless it is necessary, since it can cause effects on the fetus and even generate dependence.

Although it is applicable in children, its use must be carried out with special caution with this sector of the population (should be avoided as far as possible in children under six months unless necessary, and always with control and monitored).

Bibliographic references:

• Spanish Agency for Medicines and Health Products (2018). Technical Data Sheet Midazolam Accord 5 mg/ml. Solution for injection and infusion EFG. Ministry of Health, Social Policy and Equality. [On-line]. Available in: https://cima.aemps.es/cima/pdfs/es/ft/72016/FichaTecnica_72016.html.pdf.
• Vidal Vademecum Spain. (2016). Midazolam. Vademecum [Online]. Available in: https://www.vademecum.es/principios-activos-midazolam-n05cd08.
• Salazar, M.; Peralta, C.; Shepherd, J. (2011). Manual of Psychopharmacology. Madrid, Panamerican Medical Editorial.