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Flumazenil: uses, characteristics and side effects

Flumazenil: uses, characteristics and side effects

September 15, 2022

Numerous media have reported the growing use and abuse of psychoactive drugs in our society . Benzodiazepines are the most commonly used medications to deal with anxiety disorders, serving a support function in many psychological treatments.

However, all that glitters is not gold: it has been documented that benzodiazepines can lead to physical and psychological dependence in the person (overdosing), excessive drowsiness and even depressive symptoms, interfering in the daily life of the consumer .

The flumazenil, protagonist of this article , is the medicine responsible for combating the drowsiness produced by benzodiazepines in very specific situations.


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

What is Flumazenil?

Flumazenil (trade names: Anexate, Lanexat, Mazicon, Romazicon) is a medicine that works as a GABA antagonist . It is responsible for blocking, by competitive inhibition, the effects produced by benzodiazepines in our Central Nervous System. At the moment it is the only benzodiazepine receptor antagonist available in the pharmaceutical market.

To this drug, as we will see, two basic properties are attributed to it. On the one hand, reverses sedation produced by benzodiazepines . On the other, it helps reduce psychomotor slowness.


Uses of Flumazenil

Flumazenil is used in adults to correct the sedative effects of benzodiazepines. It can be used in two main situations: anesthesia and palliative care .

In anesthesia, it is used to end the hypnosedating effects of general anesthesia maintained or induced in hospitalized patients. It is also used for the reduction and correction of sedation due to the use of benzodiazepines in diagnostic or therapeutic procedures in an outpatient or inpatient setting.

In intensive care, it is sought restore the spontaneous breathing of the patient , correcting the central effects of benzodiazepines. In addition, it is also used for the diagnosis and treatment of overdoses or poisonings resulting from the abuse of benzodiazepines.

Apart from these uses, there is evidence that flumazenil may be effective in treating prolonged withdrawal from benzodiazepines , with quite promising results, as well as to reduce tolerance to benzodiazepines, although more studies are needed.


In addition, it has been used to treat hepatic encephalopathy, although in this case the results have been contradictory and not as promising.

Its use is not suitable for the pediatric population, only for children over 1 year of age.

Method of administration and dose

This medicine can only be given intravenously, so it can only be applied by a professional person in the health field . Flumazenil can be administered as an injection or infusion, and it is possible to use it in parallel with other resuscitation techniques.

Regarding the dose, we will only focus on the adult population. In cases where the person has been anesthetized, the recommended dose is 0.2 milligrams, administered intravenously, for approximately 15 seconds. In cases where the required degree of consciousness has not been obtained, an additional dose of 0.1mg may be injected. In general terms, The usual dose that is required in these cases fluctuates between 0.3-0.6mg .

The dose is different in intensive care. You start with a dose of 0.3mg intravenously; if the required degree of consciousness is not obtained in 60 seconds , a dose of 0.1mg can be applied, up to a maximum dose of 2.0mg.

It could be that the person did not recover the desired degree of consciousness and that his breathing was not stable after the administration of the doses. In these cases it should be taken into consideration that the poisoning is possibly not caused by the consumption of benzodiazepines.

Side effects

As it happens in the vast majority of medicines marketed, a series of adverse reactions can be manifested, which we will detail below. However, many of the adverse reactions usually disappear quickly or progressively without the need to intervene in a special way on them.

Very frequent

  • Insomnia.
  • Drowsiness.
  • Vertigo and headaches.
  • Dry mouth and tremors .
  • Hyperventilation.
  • Convulsions

Frequent

Hypotension Nausea and vomiting . Sweating Fatigue. Pain in the area of ​​the injection.

Uncommon

  • Anxiety and fear .
  • Panic attacks in patients with a history of panic attacks.
  • Abnormal hearing
  • Palpitations .
  • Tachycardia or bradycardia.
  • Cough and nasal congestion .

Warnings and precautions

Before using flumazenil, a series of precautions should be taken into account.

Flumazenil has a shorter effect than benzodiazepines, so it is recommended that the patient be monitored in the intensive care unit until it is assumed that the effect of flumazenil has disappeared.

The use of flumazenil is not always the best option. For example, in patients with heart problems It is not always a good alternative for the patient to wake up quickly from anesthesia. In these cases it may be preferable to maintain a certain degree of sedation.

After major surgery, it is important to keep in mind that the patient will be sore during the postoperative period. Therefore, it may be preferable to keep the patient lightly sedated.

Special consideration should be given to the posology of flumazenil in people with preoperative anxiety or those with a history of anxiety disorders.

The use of flumazenil is not recommended in patients with epilepsy who have been previously treated with benzodiazepines for a prolonged period.

In the case of people treated for prolonged periods with high doses of benzodiazepines, the advantages of using flumazenil should be carefully evaluated against the risk of triggering withdrawal symptoms.

Flumazenil should be used with caution in patients suffering from alcoholism , due to the increase in tolerance and dependence of benzodiazepines in this population.

Contraindications

When should flumazenil not be administered? Its use is not recommended in patients with known hypersensitivity to flumazenil or to benzodiazepines. According to experts, it should not be used in patients who have been given a benzodiazepine to control a life-threatening condition (eg, endocranial pressure).


How to Give Your Child Nasal Midazolam (September 2022).


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