Clomipramine: characteristics and side effects of this drug.

A type of Antidepressant used in many psychological disorders beyond depression.

Antidepressants are the main pharmacological treatment for depression, although they are also used for other clinical conditions.although they are also used for other clinical conditions. On the other hand, there are different types of antidepressants, and each is used for certain types of depression.

In these lines we are familiar with clomipraminea tricyclic antidepressant. This drug is indicated for the treatment of depression, phobias, anxiety attacks, obsessive syndromes, nocturnal enuresis and certain types of narcolepsy.

Clomipramine: characteristics

Clomipramine is a tricyclic antidepressant with a structure similar to imipramine and desipramine (also tricyclics). (also tricyclics). More specifically, it is a derivative of imipramine.

It is a potent non-selective serotonin reuptake inhibitor, and its main active metabolite (desmetylomipramine) acts preferentially by inhibiting noradrenaline reuptake.and its main active metabolite (desmetylomipramine) acts preferentially by inhibiting the reuptake of norepinephrine.

In addition, it is the most specific drug (compared to all tricyclics) with respect to its ability to inhibit serotonin reuptake, when compared to norepinephrine reuptake. That is, its action is more noticeable on serotonin.

It is generally used for Obsessive-Compulsive Disorder, although it is also used for major depression.. It also has other indications, as we will see below. It is usually administered orally.

Mechanism of action

The mechanism of action of clomipramine is the inhibition of the neuronal reuptake of noradrenaline (NA) and serotonin (SA) released in the synaptic cleft.

Therapeutic indications

The indications of clomipramine are: depression of any etiology, symptomatology and severity, obsessive symptoms (it was the first drug approved for the treatment of Obsessive-Compulsive Disorder), phobias and anxiety crises. It is also used in narcolepsy syndrome with cataplexy crisis and premature ejaculation in adults.

In children, it is indicated for nocturnal enuresisbut only from the age of 5 years and after excluding the possibility of organic causes. In addition, it is also used for autism.

Contraindications

The contraindications of clomipramine (when it should not be taken) are mainly aimed at people with hypersensitivity or cross-sensitivity to tricyclic antidepressants (clomipramine, desomipramine, desalicyclic antidepressants). (clomipramine, desipramine, imipramine,...). It should also not be taken in combination, or in the 14-day period before or after treatment with MAOI antidepressants, or with a recent myocardial infarction or congenital long QT syndrome.

On the other hand, clomipramine is not recommended in children and adolescents in the treatment of: depression, obsessive disorders, phobias, anxiety crises, premature ejaculation, narcolepsy with cataplexy (in adults) and attention deficit disorder with or without hyperactivity.

In addition, it is not authorized, neither in children nor in adults, it is not authorized, neither in children nor in adolescents, the use of the intravenous or intramuscular route..

Side effects

The most frequent adverse effect of the central nervous system with tricyclic antidepressants is drowsiness. On the other hand, sedation may be a desirable effect at bedtime, which minimizes any undesirable drowsiness and sedation during the day.

Dizziness may also occur (due to orthostatic hypotension, i.e., the body's inability to regulate blood pressure rapidly), but can be minimized by having the patient change posture more slowly.

In addition to those mentioned, a wide variety of cardiovascular adverse or side effects may occur, due to the anticholinergic properties of tricyclics and their ability to potentiate norepinephrine.

Also may also cause ventricular tachycardia, palpitations, hypertension, and orthostatic hypotension, with the possibility of more severe reactions.with the possibility of more serious reactions such as myocardial infarction, congestive heart failure, or stroke.

Pharmacokinetics

In terms of pharmacokinetics, that is, the branch of pharmacology that studies the processes to which a drug undergoes during its passage through the body, clomipramine is well absorbed in the intestinal tract.. However, each person responds individually.

The effects usually take several weeks to stabilize, but adverse effects appear within the first few hours. Peak concentrations of the drug in the body are obtained between 2 and 6 hours after oral administration.

On the other hand, because tricyclic antidepressants are long-acting (i.e., their effect lasts for several hours), a single daily dose can be administered once the most appropriate dosage for the patient has been established.

Bibliographic references:

• Stahl, S.M. (2002). Essential psychopharmacology. Neuroscientific bases and clinical applications. Barcelona: Ariel.
• Clomipramine. (2013). Pediamécum.