Clomipramine: Characteristics And Side Effects Of This Drug

Clomipramine

Antidepressants are the main pharmacological treatment for depression, although they are also used for other clinical conditions. 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 medication is indicated for the treatment of depression, phobias, panic 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). More specifically, it is a derivative of imipramine.

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

In addition, it is the most specific drug (compared to all tricyclics) regarding its ability to inhibit the reuptake of serotonin, if we compare it with the reuptake of norepinephrine. 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.

Mechanism of action

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

Therapeutic indications

Indications for clomipramine They 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 panic attacks. It is also used in narcolepsy syndrome with cataplexy attacks and premature ejaculation in adults.

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

Contraindications

The contraindications of clomipramine (when it should not be taken) are aimed primarily at people with hypersensitivity or cross-sensitivity to tricyclic antidepressants (clomipramine, desipramine, imipramine,…). It should also not be taken in combination, or within 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 attacks, premature ejaculation, narcolepsy with cataplexy (in adults) and attention deficit disorder with or without hyperactivity.

Besides, 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 may be a desirable effect at bedtime, minimizing any undesirable drowsiness and sedation during the day.

Dizziness may also occur (due to orthostatic hypotension, that is, the body’s inability to regulate blood pressure quickly), but they can be minimized by having the patient change positions more slowly.+

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

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

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Pharmacokinetics

Regarding pharmacokinetics, that is, the branch of pharmacology that studies the processes to which a drug is subjected through its passage through the body, clomipramine is well absorbed from 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. Maximum 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 (that is, their effect lasts several hours), a single daily dose can be administered once the most appropriate dosage for the patient has been established.