The high prevalence of problems related to anxiety means that different disciplines seek to develop different ways to address them. Among them we can find pharmacology, which throughout history has discovered and developed different substances that allow treating this type of problems.
Many are highly effective, although some of them and especially the first generations of anxiolytics have shown that despite this they can also cause dangerous side effects. In some cases the drug has even been recommended and even ended up being withdrawn in most of the world. A relatively recent case is that of meprobamate, which we are going to talk about throughout this article
The name meprobamate refers to an anti-anxiety or tranquilizer drug , which through its action on the body generates relief from anxiety and agitation. Among anxiolytics, it is part of the group of propanediols and carbomates.
It is one of the oldest types of tranquilizers or anxiolytic drugs, born in 1950 and applied as a psychotropic drug starting in 1955. It replaced barbiturates (with whom it shares pharmacological properties), but With the arrival of benzodiazepines, its use decreased largely to the one replaced by these.
This drug has muscle-relaxing, hypnotic and sedative effects, and its effectiveness and half-life is between six and seventeen hours (although there may be accumulation and prolongation of this in excessively prolonged treatments), similar to that of intermediate-action barbiturates. Its use is usually reserved for the short-term treatment of anxiety, given that this substance has a high addictive potential and dangerous side effects. It is metabolized in the liver and excreted through the kidneys, and is presented in the form of tablets, tablets and solutions for oral and intravenous administration.
But although it has a certain level of effectiveness, it also has a very narrow safety margin between therapeutic and toxic doses, making it relatively easy to suffer an involuntary overdose that can cause serious repercussions and even death. For this reason and given the existence of much safer therapeutic alternatives, in 2012 the European Union Medicines Agency recommended its withdrawal, and today it is withdrawn in much of the world.
Mechanism of action of this psychotropic drug
Meprobamate acts in the body causing the modification of the functioning of the nervous system, although in general the way in which it does this is little known. It is a drug that inhibits nervous functioning and reduces neuronal activation and activity in different brain nuclei
Thus, it is known that it acts by causing depression in the central nervous system of nuclei such as the limbic system and the thalamus (something that contributes to reducing anxiety), in addition to also affecting the spinal cord (something that is related to its action). as a muscle relaxant) affecting, among others, the interneurons that connect the different neurons that are part of the motor system.
What indications do you have?
As a hypnotic-sedative anxiolytic, meprobamate had as its main indications the short-term treatment of symptoms of anxiety and nervous agitation
In addition to this, another of the common indications for this drug has been the treatment of conditions linked to spasticity and muscle rigidity, given that, as we have said, it has positive effects on the relaxation of the muscles. Although it is not among its indications, it has anticonvulsant effects, something that can help control seizures typical of different disorders.
It also had as an indication treatment of primary insomnia , but in this aspect its effectiveness is rather limited. Last but not least, it should be noted that it has been used for the treatment of conditions such as high blood pressure, since it has a strong effect on its reduction.
Side effects
Meprobamate is a drug that may have some effectiveness, but whose consumption may have a significant risk of generating annoying and even dangerous side effects, to the point of having been withdrawn from many countries due to its lack of safety.
Some relatively common side effects are sedation, feeling of fatigue, headache, dizziness and motor incoordination Vomiting and diarrhea are also possible, as well as anorexia or loss of appetite. Others that are more serious and require medical attention are unexplained bleeding, problems and decreased ability to breathe and communicate, tachycardia and arrhythmias.
Likewise, it should be noted that it causes hypotension, something that, although it has been used medically, can be problematic and dangerous depending on the population sector. It can also cause cognitive impairment and episodes of confusion, urticaria, angioneurotic edema, bronchospasm or urination difficulties. It can also cause blood problems, including anemia, agranulocytosis, leukopenia, and thrombocytopenia.
Among these side effects highlights its addictive potential, something it shares to a large extent with barbiturates and that can lead to physical and psychological dependence on this substance and abusive use, in addition to withdrawal syndrome after cessation that can cause seizures, hallucinations, anxiety, vomiting, loss of appetite and lethargy. In the event of an overdose, it can even cause fatal respiratory arrest or a coma.
Although it is a withdrawn drug, it is also interesting to know which sectors of the population have it especially contraindicated, given that in some cases its consumption is dangerous and the probability of suffering serious medical problems increases.
First of all, it is contraindicated for people who are allergic to this drug or its components or to drugs from the carbamate group. It is also contraindicated for those subjects with underlying arterial hypotension, as well as for those who suffer from liver or kidney insufficiency or failure or for those who suffer from porphyria (it can worsen this condition). In epileptic patients it can cause seizures.
It is contraindicated (except when necessary) in pregnant and lactating women, since the drug is capable of crossing the placenta or being transmitted through breast milk and is capable of causing anomalies. Patients with diabetes, the elderly and children should be cautious. Subjects with depression and a history of suicide attempts are also contraindicated, as well as people with a history of dependence on any substance. It should not be mixed with alcohol or other depressant substances, as well as antidepressants, muscle relaxants, anticonvulsants or narcotics, among others.
