Clomipramine: characteristics and side effects of this drug
Antidepressants are the main pharmacological treatment for depression , although they are also used for other clinical pictures. On the other hand, there are different types of antidepressants, and each is used for certain types of depression.
In these lines we know about 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.
Clomipramine is a tricyclic antidepressant with a similar structure to imipramine and desipramine (also tricyclic). More specifically, it is a derivative of imipramine.
It is a potent non-selective serotonin reuptake inhibitor , and its main active metabolite (demethyclomipramine) acts preferentially by inhibiting the reuptake of noradrenaline.
In addition, it is the most specific drug (compared to all tricyclics) with respect to its ability to inhibit the reuptake of serotonin, compared to norepinephrine reuptake. In other words, its action is more noticeable 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 the neuronal reuptake of noradrenaline (NA) and serotonin (SA) released into the synaptic cleft.
The indications for 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 attacks. It is also used in Narcolepsy Syndrome with cataplexy crisis and premature ejaculation in adults.
In children it is indicated for nocturnal enuresis , but only from the age of 5 and after excluding the possibility of organic causes. In addition, it is also used for autism.
The contraindications of clomipramine (when it should not be taken) are mainly aimed at people with hypersensitivity or cross-sensitivity to tricyclic antidepressants (clomipramine, desipramine, imipramine,…). Nor should it be taken in combination with, 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 attacks, premature ejaculation, narcolepsy with cataplexy (in adults) and attention deficit disorder with or without hyperactivity.
Furthermore, is not authorized, neither in children nor in adolescents, the use of the intravenous or intramuscular line .
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 sleepiness and sedation during the day.
Dizziness may also occur (from orthostatic hypotension, i.e. the body’s inability to regulate blood pressure quickly), but can be minimized by causing the patient to change position 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 cause ventricular tachycardia, palpitations, hypertension, and orthostatic hypotension , with the possibility of more serious reactions such as myocardial infarction, congestive heart failure, or stroke.
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 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. The maximum concentrations of the drug in the body are obtained between 2 and 6 hours after being administered orally.
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 a more suitable dosage has been established for the patient.
- Stahl, S.M. (2002). Essential Psychopharmacology. Neuroscientific bases and clinical applications. Barcelona: Ariel.
- Clomipramine. (2013). Pediamécum.