Moclobemide: uses and side effects of this psychoactive drug

Moclobemide was the first RIMA antidepressant (Revesible Inhibitor of Monoamine oxidase Atype), that is, the first reversible MAOI type A, which increases the concentrations of serotonin, dopamine and serotonin.

This drug is mainly used for depression and social anxiety. In this article we will know its characteristics, adverse effects and therapeutic indications, among others.

• Related article: "Psychoactive drugs: drugs that act on the brain"

Moclobemide: general characteristics

Moclobemide is an antidepressant from the MAOI group (monoamine oxidase inhibitor), specifically it is a benzamide (solid organic compound).

This medication 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 metabolized by the pancreas practically completely; less than 1% is excreted, in the urine.

Unlike traditional MAOIs, with moclobemide

no signs of liver toxicity have been detected and to date, no evidence suggests that moclobemide causes cardiotoxic effects (toxic to the heart).

Mechanism of action

As we have said, moclobemide is a reversible monoamine oxidase inhibitor, mainly of subtype A; that is to say, reversibly and selectively inhibits monoamine oxidase type A.

This means that it decreases the metabolism of norepinephrine, serotonin and dopamine, and therefore that it increases the extracellular concentrations of these neurotransmitters.

So, the mechanism of action of moclobemide is similar to that of classic MAOIs, but unlike these, its effect on the aforementioned enzyme basically modifies noradrenergic and serotonergic transmission with little effect on dopaminergic transmission.

• You may be interested in: "Types of antidepressants: characteristics and effects"

Therapeutic indications

Moclobemide is indicated (and used) for major depression (major depressive episodes) (primarily) and social anxiety.

contraindications

Moclobemide It is contraindicated in acute confusional states, in children, when there is hypersensitivity, and as concomitant use with selegiline.

Dose

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.

Treatment duration

Treatment with moclobemide should be administered for at least 4-6 weeks in order to assess the efficacy of moclobemide. Treatment is normally 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 noted that moclobemide may exacerbate symptoms in depressed 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, more than 100 mg/day of foods containing tyramine should not 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 in suicidal patients should be controlled, 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 that appears at doses normally used in humans for prophylaxis, diagnosis or treatment or to modify physiological functions”.

In the case of moclobemide, your adverse reactions (which appear rarely) can be: agitation; sleep disorders; feelings of anxiety, confusion, irritability; dizziness; headaches; paresthesia; Vertigo; visual disturbances; blush; gastrointestinal discomfort; increased liver enzymes; rash; pruritus; urticaria.

Effectiveness

Moclobemide has been evaluated in numerous clinical trials and has demonstrated its antidepressant efficacy superior to placebo and similar to that of tricyclic antidepressants and selective serotonin reuptake inhibitors (SSRIs).

At the tolerance level, 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.