Desipramine is a tricyclic antidepressant. It is used as part of the therapy of depression. Currently, however, the drug is no longer available in numerous countries and can no longer be prescribed.
What is desipramine?
The drug desipramine is used for the therapy of depressive disorders. Desipramine is a drug that is usually administered orally and in the form of tablets. The active ingredients have a bioavailability of almost 92 percent. The subsequent metabolization of desipramine is primarily hepatic. The average plasma half-life is around 22 hours. Subsequently, the active ingredients contained are excreted by the kidneys or eliminated renally. The drug desipramine is used in the treatment of depressive disorders. Initially, the drug increases the patient’s drive and later has a mood-lifting effect. The active ingredient was launched on the German market in 1965 under the name Pertofran. In modern times, however, finished medicines containing desipramine are out of distribution in most of the world.
Pharmacologic action
The drug desipramine belongs to the so-called tri- and tetracyclic antidepressants. In this group, it is classified as a tricyclic antidepressant. In the brain, it primarily causes the uptake of the neurotransmitter norepinephrine. As a result, it increases the patient’s drive and improves mood. For this reason, a relatively successful therapy of depression is possible using desipramine. In the central nervous system, desipramine reduces the reuptake of monoamines into the presynaptic vesicles. This increases the concentrations of norepinephrine and serotonin in the synaptic cleft. As a result, the drug shows its antidepressant and mood elevating effects. At the same time, however, tricyclics also influence the cholinergic, histaminergic and adrenergic systems. This results in a variety of side effects. In principle, desipramine is the active metabolite of the substance imipramine. Its effect unfolds in the central nervous system, where it impairs the reuptake of certain neurotransmitters. This increases their concentration, which in turn reduces depressive symptoms. Desipramine also has a sedative effect, but this is only weak. In addition, desipramine is able to reduce the perception of pain. In principle, the absorption of desipramine from the intestine is relatively good. However, due to its high first-pass effect, bioavailability is reduced and can vary enormously. The plasma half-life of the active substance is between 15 and 25 hours. Desipramine passes the blood–brain barrier as well as the placental barrier. The active ingredient also passes into breast milk. Following biotransformation, it is excreted by the kidneys and liver.
Medicinal use and application
Depressive disorders represent the main indication of the drug desipramine. In this case, the active substance is usually administered in tablet form, and the patient must adhere to the dosage and time guidelines provided by the attending physician. Regular check-ups during therapy ensure that the dose is continuously adjusted to the patient’s condition. The antidepressant desipramine must not be prescribed in the event of hypersensitivity reactions to the active substance. If a patient has a history of intoxication with psychotropic drugs or sedatives, desipramine should also not be administered. Similarly, disorders of bladder emptying, cardiac conduction disorders, glaucoma, ileus, and pyloric stenosis are contraindications. In addition, desipramine should not be taken concomitantly with MAO inhibitors. In principle, desipramine should also not be prescribed during pregnancy and breastfeeding. In such cases, possible alternatives to the drug should be considered. When treating with desipramine, it should be noted that there are interactions with certain other substances. For example, the effects of desipramine and alcohol may reinforce each other. Other medications, such as painkillers, antipsychotics, barbiturates, and antihistamines, also sometimes produce such an effect. Desipramine also interacts with substances that dock onto the same receptors in the brain.These include, for example, serotonin reuptake inhibitors, anticholinergics or alpha-sympathomimetics. Under certain circumstances, they can impair the metabolism of desipramine.
Risks and side effects
The antidepressant desipramine can cause a variety of side effects, so therapy must be monitored by the treating physician. The most common side effects of taking it include dry mouth, dizziness, lightheadedness, blurred vision, sweating, tremors, rapid heartbeat, and lowered blood pressure. In addition, liver enzymes may increase and weight gain, constipation, and circulatory regulation problems may occur. Occasionally, discomfort during urination and sleep disturbances occur. Patients complain of inner restlessness, sexual problems, skin rashes, and thirst. Rare side effects of desipramine include circulatory collapse, confusional states, urinary retention, bowel obstruction, and changes in blood counts. Liver dysfunction, allergic reactions in the form of vascular inflammation and skin inflammation may occur, as well as cardiac arrhythmias. During therapy with desipramine, seizures, pneumonia, nervous disorders and movement disorders occur in isolated cases. In addition, acute attacks of glaucoma and Löffler’s syndrome up to delirium are possible. Basically, headaches and drowsiness sometimes occur while taking desipramine. In some cases, suicidal tendencies increase, while withdrawal symptoms may occur after desipramine is discontinued. Any side effects that occur must be reported immediately to the treating physician.
