Flumazenil: uses, characteristics and side effects
Numerous media have reported the growing use and abuse that occurs in our society of psychotropic drugs. Benzodiazepines are one of the most widely used medications to deal with anxiety disorders, fulfilling a supportive role in many psychological treatments.
However, all that glitters is not gold: it has been documented that benzodiazepines can lead to physical and psychological dependence on person (leading to overdose), excessive drowsiness and even depressive symptoms, interfering with the person's daily life consumer.
Flumazenil, protagonist of this article, is the drug in charge of 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 on the pharmaceutical market.
As we will see, this drug is attributed two basic properties. On the one hand, reverses sedation produced by benzodiazepines. On the other hand, 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 hypnosedative effects resulting from 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 hospital setting.
In intensive care, it is sought restore spontaneous breathing of the patient, correcting the central effects of benzodiazepines. In addition, it is also used for the diagnosis and treatment of overdose or poisoning resulting from the abuse of benzodiazepines.
Apart from these uses, there is evidence that flumazenil could be effective in treating long-term withdrawal from benzodiazepines, with quite promising results, as well as to reduce tolerance to benzodiazepines, although more studies are needed in this regard.
In addition, it has been used to treat hepatic encephalopathy, although in this case the results have been contradictory and not so promising.
Its use is not suitable for the pediatric population, only for children over 1 year of age.
Method of administration and dosage
This medicine can only be given intravenously, so It can only be applied by a professional person in the health field. Flumazenil can be given as an injection or infusion, and can be used 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 can be injected. In general terms, the usual dose required in these cases fluctuates between 0.3-0.6mg.
The dose is different in intensive care. It begins with a dose of 0.3mg intravenously; if the required level 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 regain the desired level 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 may not be caused by the consumption of benzodiazepines.
Side effects
As is the case with the vast majority of marketed drugs, a series of adverse reactions can occur, which we are going to detail below. However, many of the adverse reactions usually disappear quickly or progressively without the need for special intervention on them.
Very frequent
- Insomnia.
- Drowsiness.
- Vertigo and headaches.
- Dry mouth and tremors.
- Hyperventilation
- Seizures.
Frequent
Hypotension Nausea and vomiting. Sweating Fatigue. Pain at the injection site.
Infrequent
- 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 cautions
Before using flumazenil, a number of precautions should be observed.
Flumazenil has a shorter effect than benzodiazepines, therefore it is recommended that the patient be monitored patient in the intensive care unit until the effect of flumazenil is assumed to have worn off.
Using flumazenil is not always the best option. For instance, in patients with heart problems, it is not always a good alternative for the patient to wake up quickly from anesthesia. In these cases, maintaining a certain degree of sedation may be preferable.
After major surgery, it is important to note that the patient will be in pain postoperatively. Therefore, it may be preferable to keep the patient lightly sedated.
Special consideration must be given to the dosage 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 previously received benzodiazepine treatment for a long period of time.
In the case of people treated for long periods with high doses of benzodiazepines, they should be carefully weigh the benefits of using flumazenil against the risk of triggering symptoms of abstinence.
Flumazenil should be used with caution in patients suffering from alcoholism, due to increased tolerance and dependence on benzodiazepines in this population.
Contraindications
When should flumazenil not be given? Its use is not recommended in patients with known hypersensitivity to flumazenil or benzodiazepines. According to experts, it should also not be used in patients who have been given a benzodiazepine to control a life-threatening condition (eg. g., intracranial pressure).