Clomipramine: characteristics and side effects of this drug

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

In these lines we know clomipramine, a tricyclic antidepressant. This medicine is indicated for the treatment of depression, phobias, panic attacks, obsessive syndromes, nocturnal enuresis and certain types of narcolepsy.

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Clomipramine: characteristics

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

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

In addition, it is the most specific drug (compared to all tricyclics) regarding its capacity to inhibit serotonin reuptake, compared to norepinephrine reuptake. That is, its action is most notable on serotonin.

It is generally used for Obsessive-Compulsive Disorder, but also for major depression. In addition, it has other indications, as we will see later. Normally its route of administration is oral.

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Mechanism of action

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

Therapeutic indications

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

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

Contraindications

The contraindications of clomipramine (when not to take it) are mainly oriented to people with hypersensitivity or cross-sensitivity to tricyclic antidepressants (clomipramine, desipramine, imipramine, ...). It should also not be taken in combination, or in the period of 14 days 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 attack, premature ejaculation, narcolepsy with cataplexy (in adults) and attention deficit disorder with or without hyperactivity

What's more, The use of the intravenous or intramuscular route is not authorized, neither in children nor in adolescents.

Side effects

The most common central nervous system adverse effect with tricyclic antidepressants is the somnolence. On the other hand, sedation can be a desirable effect at bedtime, minimizing any undesirable drowsiness and sedation during the day.

Dizziness may also appear (from orthostatic hypotension, that is, the body's inability to regulate blood pressure rapidly), but can be minimized by making the patient change posture more slowly.

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

Too can cause ventricular tachycardia, palpitations, hypertension, and orthostatic hypotension, with the possibility of more serious reactions such as myocardial infarction, congestive heart failure, or a stroke.

Pharmacokinetics

As for pharmacokinetics, that is, the branch of pharmacology that studies the processes to which a drug is subjected through its passage through the body, clomipramine well absorbed from the intestinal tract. However, each person responds individually.

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

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

Bibliographic references:

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