One of the most widely used antidepressants has been dosulepine, which has been shown to be effective in treating both major depression and neurological problems.

This drug, which is available by prescription, has had its ups and downs, so its use has been decreasing in recent years but has not stopped being prescribed.

Let’s take a closer look at the characteristics of dosulepine , what it is used for, as well as talk about its adverse effects and contraindications.

Dosulepine: general characteristics

Dosulepine, also called dotiepine, is a tricyclic antidepressant, used in the treatment of depression . It has been marketed under several names: Altapin, Depresym, Dopress, Dothapax, Dothep, Idom, Prepadine, Protiaden, Protiadene, Thaden, and Xerenal.

This psychoactive drug is available in several parts of Europe, New Zealand, Australia and Asia. Although it was once one of the most widely prescribed antidepressants in the United Kingdom, this is no longer the case because it has a relatively high level of toxicity if overdosed, and it has no major advantages over other tricyclic antidepressants.

Indications: what is it used for?

Dosulepine is used in the treatment of major depression . It is also used to treat pain of neurological origin, such as fibromyalgia, and as a preventive for migraines. There is scientific evidence that it is useful for treating atypical facial pain.

Mechanism of action

Dosulepine acts as a selective inhibitor of serotonin and noradrenaline , blocking the reuptake of these two neurotransmitters in the neuronal membrane. It is also an antagonist of the histamine H1, alpha-1-adrenergic, serotoninergic 5-HT2 and muscarinic receptors. It is also a blocker of potential-dependent sodium channels.

Administration

Dosulepine is taken orally and is marketed in 25mg and 75mg tablets. For depression it is usually prescribed between 75mg and 150mg per day, being the maximum recommended dose for this diagnosis 225mg per day . For the treatment of pain and prevention of migraines, the usual dose is around 75mg per day taken before going to sleep, the maximum dose being 150mg.

This drug causes drowsiness, for this reason it is recommended to take it once a day, especially before going to sleep. In case you feel sleepy when you wake up the next day, it is recommended to take the tablet a little earlier than you did the night before.

Sometimes, when treatment is started, low doses are prescribed about two or three times a day until the body gets used to the drug. The aim of this is to avoid overdose dependent side effects.

Dosulepine can be consumed with or without food , always taking it with a glass of water and without chewing the tablet.

Side effects

As with all psychotropic drugs, dosulepine may have some side effects , which are due to either an overdose of the drug or an allergic reaction to it. Most of these side effects go away once the body has become accustomed to the dosulepine.

Digestive effects

Dosulepine can cause some unwanted effects on the digestive tract, such as dry mouth, nausea, vomiting, diarrhea and constipation . If constipation is prolonged over time, it can cause stomach pain.

Effects on the circulatory system

One of the most dangerous effects this drug can produce is heart problems, especially arrhythmias and tachycardia . In addition, hypertension may occur. In the most severe cases, heart attacks and myocardial infarctions can occur.

Skin effects

Blisters may appear, in addition to hives, rashes and increased sensitivity to sunlight.

Liver problems

The liver can be damaged, resulting in hepatitis , which can cause the skin and whites of the eyes to turn yellow.

Due to poor liver regulation, blood glucose levels are altered.

Cognitive and psychiatric impairment

Dosulepine can cause drowsiness, dizziness, tiredness and general weakness . Headaches may also occur.

In more severe cases there may be disorientation, lack of concentration, hallucinations, over-excitement, insomnia and nightmares. Anxiety and hypomania may occur.

Other effects

Some of the most notable effects are impotence, gynecomastia, testicular swelling, blackening of the tongue, difficulty in urinating, weight loss and/or gain, and increased eye pressure.

Contraindications and precautions

These are the populations and situations where dosulepine is contraindicated.

Pregnancy and lactation

Dosulepine has been linked to a very low risk to the fetus. Even so, if you suspect that you are pregnant, it is recommended that you consult a professional to consider changing antidepressants to ensure that the unborn child develops smoothly.

During lactation, if no problems are noticed in the newborn, it is possible to continue taking dosulepine, since this medicine reaches the breast milk in very small quantities .

Driving

As this drug causes drowsiness, it is not recommended to drive or operate heavy machinery after having taken dosulepine.

Interactions with other substances

Dosulepine can interact with alcohol. Also, like other tricyclics, this drug potentiates the effects of barbiturates, anxiolytics and depressants of the central nervous system.

Dosulepine has anti-histamine and anti-cholinergic effects, which increase if it is combined with other drugs that also have these effects.

Dosulepine and St. John’s wort, a natural remedy for depression, are contraindicated because taken together they increase the risk of adverse effects.

Bibliographic references:

  • Adam, A. and Prat, G. (2016). Psychopharmacology: Mechanism of action, effect and therapeutic management. Barcelona, Spain. Marge Medica Books.
  • Lancaster S. G., Gonzalez J. P. (1989). Dothiepin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in depressive illness. Drugs. 38 (1): 123–47.
  • Donovan S., Dearden L., Richardson L. (1994). The tolerability of dothiepin: a review of clinical studies between 1963 and 1990 in over 13,000 depressed patients. Neuropsychopharmacol. Biol. Psychiatry. 18 (7): 1143–62.
  • Thanacoody H. K., Thomas S. H. (2005). Tricyclic antidepressant poisoning : cardiovascular toxicity. Toxicol Rev. 24 (3): 205-14.
  • Feinmann, C; Harris, M.; Cawley, R. (1984). “Psychogenic facial pain: presentation and treatment”. Br Med J (Clin Res Ed). 288 (6415): 436–8.
  • Vademecum. (2016). Dosulepine.