The drug Lisuride belongs to the drug class of dopamine agonists. It also belongs to the serotonin antagonists and to the HT2B antagonists.
What is lisuride?
Mainly, the drug lisuride is used in the therapy of Parkinson’s disease. The ergoline derivative lisuride is used for various indications. However, the drug is mainly used in the therapy of Parkinson’s disease. In Germany, drugs containing the active ingredient lisuride are subject to medical prescription. Lisuride is a drug derived from ergot alkaloids. Ergot is a form of ergot fungus. It attacks food and feed grains and exhibits high toxicity due to the alkaloids it contains. The ergot-derived lisuride has an ergoline backbone. Ergoline is a nitrogen-containing organic chemical compound and the backbone of many ergot alkaloids. The ergoline of lisuride differs from naturally occurring ergolines in a special configuration of the ergoline backbone.
Pharmacological action
Lisuride is one of the so-called “dirty drugs.” The term dirty drug is used for drugs that can bind to different receptors in the brain. This results in a very wide range. However, side effects also occur more often. Lisuride has an affinity for serotonin receptors, dopamine receptors, adrenoreceptors, beta-adrenoreceptors, and for histamine receptors.
Medical application and use
The drug’s affinity for dopamine receptors is responsible for its effectiveness in Parkinson’s disease therapy. Parkinson’s disease is caused by a decline in dopamine-producing cells in the substantia nigra in the brain. Dopamine is a neurotransmitter that is essential for smooth movement. Dopamine deficiency causes symptoms such as poor movement, muscle stiffness, balance problems, tremors, or gait disturbances. Lisuride can bind to the dopamine receptors and stimulate them. As a result, a dopamine-like effect occurs. The symptoms of Parkinson’s disease are alleviated accordingly. However, since dopamine not only plays a role in motor function, but also has an inhibitory effect on the secretion of the hormone prolactin in the pituitary gland, Lisuride enhances prolactin inhibition. This has an effect on milk flow, for example. Lisuride is therefore used in individual cases to inhibit lactation during weaning. Prolactin-induced amenorrhea and abnormal milk flow (galactorrhea) are also indications for Lisuride. Other indications include restless legs syndrome and malignant neuroleptic syndrome. At higher doses, Lisuride acts at serotonin receptors as an antagonist. The receptors are inhibited. Because of this effect, lisuride was used for a long time for the prophylaxis of migraine before its use as an anti-parkinsonian agent. Today, the active ingredient no longer has approval for this purpose.
Risks and side effects
Side effects such as nausea, drowsiness, dizziness, sweating, or dry mouth often occur at the beginning of therapy. Side effects may also occur if the dose is too high, if the dose is increased, or if it is taken outside of meals. Rare side effects include a sudden drop in blood pressure and retroperitoneal fibrosis. These are also known as Ormond’s syndrome. These are connective tissue growths between the peritoneum and the spine. Vessels, nerves and ureters are literally walled in by the connective tissue. The disease manifests itself in the form of severe pain in the flanks, scrotum, lower abdomen and back. The narrowing of the ureter can cause urine to back up into the kidneys. Such fibrosis can occur not only in the retroperitoneal space, but also on the four heart valves. In animal studies, lisuride has been shown to induce premature ejaculation. Female rats responded to lisuride by developing male-like behavioral patterns. However, similar adverse effects have not yet been demonstrated in humans. The sedative effects of Lisuride may be enhanced by other depressant drugs. When Lisuride is taken together with neuroleptics or dopamine antagonists, the drugs attenuate each other. Contraindications to treatment with Lisuride are liver function disorders and cardiovascular diseases.Lisuride must also not be administered in cases of organ fibrosis, such as pulmonary fibrosis. Otherwise, increased pathological connective tissue remodeling of the organ functional tissue could occur. Lisuride may be used in pregnancy only in absolutely exceptional cases. In lactating women, the milk-inhibiting effect must be taken into account. Another contraindication to lisuride is cardiac arrhythmias.
