Midazolam: uses and side effects of this anxiolytic drug

This anxiolytic drug has various medical and psychological applications.

Anxiety is one of the most common problems today. In fact, a large majority of the western population has had or will have in their lifetime an episode of anxiety or a crisis of anxiety. And while for some it may be something that has happened at some point in time, for others it may become a regular occurrence and may require some kind of treatment.

In this sense, at pharmacological level we have substances that allow lowering anxiety levels in specific situations. This is the most widely used and widespread group of psychotropic drugs among the population: anxiolytics. Among 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 will discuss in this article.of which we are going to speak along this article.

Midazolam: what is it?

The midazolam is an anxiolytic drug, that is to say, a drug that through its action on the systems of cerebral neurotransmission allows to treat conditions such as anxiety, agitation and extreme nervousness..

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

It is a sedative-hypnotic drug and also has an 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 used in preparation for anesthesia and together with other drugs.

Midazolam is a short-lived benzodiazepine, which means that its effects take a short time to disappear (on average 2.3 hours, although it can vary between 2.2 and 6.8 depending on body mass), although on the other hand its effects are almost immediate (it starts to have sedative effects after two minutes). It is metabolized in the liver and excreted mainly by the kidneys.

On the other hand, midazolam is a well-known product with multiple applications, and is available in various presentations for oral administration (most commonly in tablet or tablet form), intravenous or intramuscular (presentation as an injectable), intranasal or even rectal. It can be used in children older than 6 months, although very controlled doses prescribed by a doctor are required. controlled doses prescribed by the physician.. 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 death row inmates before lethal injection, in order to render them unconscious (high doses are used) before the application of other substances that will cause death.

Even so, the drug has a weak anesthetic effect and is not approved as such, and in fact there has been legal litigation to stop it from being applied in this way, since there have been cases of inmates in which it did not work.

Mechanism of action: how does it work?

Like many other benzodiazepines, midazolam acts on our body through a mechanism based on the alteration of the GABAergic system. a mechanism based on the 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 GABAergic receptors in the nervous system, which has the effect of inhibiting the system and reducing the level of brain activation. the reduction of the 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 different indications for this substance. Since it is a short-lived anxiolytic, it is especially indicated in the following cases those situations in which a sudden access of anxiety and agitation appears, such as an anxiety crisis.such as an anxiety crisis. It can also be used to induce sleep in people with insomnia of conciliation (i.e. who 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 surgery. before some type of surgical intervention or in situation of being or in situation of being in the intensive care unit.

It is also applied at anesthesia level, mainly as a drug prior to or for the induction of the administration of other anesthetics. In addition, it is used as initial antiepileptic treatment in crises, or in problems related to spasticity. problems related to muscular spasticity, as it can help to relax as it can help to relax the musculature.

Side effects

As with other drugs, midazolam can also can lead to side effects or adverse and undesirable and undesirable side effects. These include prolonged sedation, headaches, nausea and vomiting, erythema, fatigue, involuntary movements, tremors, euphoria, agitation, confusion, incoordination, hallucinations, constipation, dry mouth or allergic reactions.

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

In some cases, convulsions have also been observed (especially in children or as an effect of withdrawal syndrome). Of particular relevance are possible hypotension and slowing of the heart and respiratory rate.

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

Contraindications

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

These include all those who are allergic or hypersensitive to this drug or any of its components. It is also contraindicated for people suffering from respiratory insufficiency or depression, as well as those who suffer from heart problems, sleep apnea or have any of its components.sleep apnea or have a serious chronic disease.

It is not recommended or great caution should be exercised by people with renal or hepatic insufficiency. It should also not be used by people with myasthenia or glaucoma, people in coma or those under the effects of alcohol or other depressive substances.

The concomitant use with other drugs should also be avoided, and its suitability should be consulted with the doctor, since in some cases it may interact and its effects may be potentiated 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 women and breastfeeding mothers should not use it unless it is necessary, since it can cause effects in the fetus and even generate dependence.

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

Bibliographic references:

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