Moclobemide: uses and side effects of this psychotropic drug.
An Antidepressant drug that affects the brain's monoamine oxidase. Let's see what it looks like.
Moclobemide was the first antidepressant RIMA (Reversible Inhibitor of Monoamine oxidase Atype), i.e. the first reversible MAOI type A, which increases serotonin, dopamine and serotonin concentrations.
This drug is mainly used for depression and social anxiety. In this article we will learn about its characteristics, adverse effects and therapeutic indications, among others.
Moclobemide: general characteristics
Moclobemide is an antidepressant of the MAOI (monoamine oxidase inhibitor) group, specifically a benzamide (solid organic compound).
This drug is mainly used to treat major depression. and, to a lesser extent, social anxiety. Although clinical trials with moclobemide began in 1977, it is not currently approved for use in the United States.
The toxicity of moclobemide is low and it is very well tolerated. It is almost completely metabolized by the pancreas; less than 1% is excreted in the urine.
In contrast to traditional MAOIs, with moclobemide no signs of hepatic toxicity have been detected with moclobemide and to date there are no signs that moclobemide causes cardiotoxic effects (toxic to the heart).
Mechanism of action
As we have said, moclobemide is a reversible monoamine oxidase inhibitor, fundamentally of subtype A; that is to say, it reversibly and selectively inhibits monoamine oxidase type A..
This means that it decreases the metabolism of noradrenaline, serotonin and dopamine, and therefore increases the extracellular concentrations of these neurotransmitters.
Thus, the mechanism of action of moclobemide is similar to that of the classic MAOIs, but unlike the latter, its mechanism of action is similar to that of the MAOIs.However, unlike the latter, its effect on the aforementioned enzyme basically modifies noradrenergic and serotonergic transmission with little effect on dopaminergic transmission.
Therapeutic indications.
Moclobemide is indicated (and used) for major depression (major depressive episodes) (mainly) and social anxiety.
Contraindications
Moclobemide is contraindicated in acute confusional states, in children, when there is hypersensitivity to moclobemide, and as concomitant use in children.and as concomitant use with selegiline.
Dosage
In adults, the initial dose is usually 300 mg, and its administration is divided into several doses after meals. The tablets are administered orally. If necessary, the daily dose can be increased up to 600 mg/day.
Duration of treatment
Treatment with moclobemide should be administered for at least 4-6 weeks in order to evaluate the efficacy of moclobemide. Normally, treatment is intended to continue for an asymptomatic (symptom-free) period of 4-6 months.
We know that antidepressants, especially MAOIs, should be withdrawn gradually to reduce the risk of withdrawal symptoms..
Precautions
It should be borne in mind that moclobemide can exacerbate symptoms in depressive patients with schizophrenic or schizoaffective psychoses (therefore, if possible, it is recommended to continue treatment with long-acting neuroleptics).
On the other hand, it is warned that if moclobemide is used, no more than 100 mg/day of food containing tyramine should be consumed, especially in hypertensive patients. Tyramine is found in some foods such as Cheddar cheese, beans or Chianti wine. This is done in order to avoid an increase in blood pressure..
In addition, the use of moclobemide should be monitored in patients with suicidal tendencies, and its administration with 5-HT reuptake inhibitors (SSRIs) is not recommended.
Side effects
According to the World Health Organization (WHO), an adverse drug reaction is "any unintended harmful reaction occurring at doses normally used in humans for prophylaxis, diagnosis or treatment or to modify physiological functions".
In the case of moclobemide, its adverse reactions (rarely occurring) may include: agitation; sleep disorders; feelings of anxiety, confusion, irritability; dizziness; headaches; paresthesia; vertigo; visual disturbances; flushing; gastrointestinal discomfort; increased liver enzymes; rash; pruritus; urticaria.
Efficacy
Moclobemide has been evaluated in numerous clinical trials and has demonstrated antidepressant efficacy superior to placebo and similar to that of antidepressants. and similar to tricyclic antidepressants and serotonin reuptake inhibitors (SSRIs).
In terms of tolerance, it is well tolerated and has practically no interactions with other drugs.
On the other hand, it is safe in overdose (due to its reduced toxicity), and it is considered a good alternative (first choice) to current treatments for depression, especially in polymedicated patients and in those who require a non-sedative drug..
(Updated at Apr 13 / 2024)