Lisurid

The drug Lisurid belongs to the drug class of dopamine agonists. It is also one of the serotonin antagonists and the HT2B antagonists.

What is lisuride?

The ergoline derivative lisuride is used for various indications. However, the drug is mainly used in the therapy of Parkinson's disease. Medicines with the active ingredient lisuride are subject to medical prescription in Germany.

Lisuride is a drug derived from ergot alkaloids. Ergot is a form of the ergot fungus.It attacks food and feed grain and is highly toxic because of the alkaloids it contains. The lisuride derived from ergot has a basic ergoline structure. Ergoline is a nitrogen-containing, organic chemical compound and the basic structure of many ergot alkaloids. The ergoline of the lisuride differs from the naturally occurring ergolines in a special configuration of the ergoline frame.

Pharmacological effect

Lisurid is one of the so-called "dirty drugs". The term dirty drug is used for drugs that can bind to various receptors in the brain. A very large bandwidth is thereby achieved. However, side effects are also more common. Lisuride has an affinity for serotonin receptors, dopamine receptors, adrenergic receptors, beta-adrenergic receptors, and histamine receptors.

Medical application & use

The affinity to the dopamine receptors is responsible for the effectiveness of the drug in Parkinson's therapy. Parkinson's is caused by the destruction of the dopamine-producing cells in the substantia nigra in the brain. Dopamine is a neurotransmitter that is essential for the smooth running of movement sequences. The dopamine deficiency leads to symptoms such as sedentary lifestyle, muscle stiffness, balance disorders, tremors or gait disorders. Lisuride can bind to and stimulate the dopamine receptors. This results in a dopamine-like effect. The symptoms of Parkinson's disease are alleviated accordingly.

Since dopamine not only plays a role in motor skills, but also has an inhibiting effect on the secretion of the hormone prolactin in the pituitary gland, lisuride strengthens the inhibition of prolactin. This has an effect on the flow of milk, for example. Lisuride is therefore used in individual cases to inhibit lactation during weaning. Prolactin-related amenorrhea and abnormal milk flow (galactorrhea) are also indications for lisuride. Further areas of application are the restless legs syndrome and the malignant neuroleptic syndrome.

In higher doses, lisuride acts as an antagonist on serotonin receptors. The receptors are inhibited. Because of this effect, lisuride was used long before its use as an anti-Parkinson agent for the prophylaxis of migraines. Today, the active ingredient is no longer approved for this.

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Risks & side effects

Side effects such as nausea, drowsiness, dizziness, sweating or dry mouth often occur at the beginning of therapy. Side effects can 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 Syndrome. It is an increase in connective tissue between the peritoneum and the spine. Vessels, nerves and ureters are literally walled up 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 in the kidneys. Such fibrosis can occur not only in the retroperitoneal space, but also on the four heart valves.

Animal experiments have shown that lisuride can trigger premature ejaculation. Female rats responded to lisuride by developing male behavior patterns. However, no similar undesirable effects have yet been demonstrated in humans. The sedative effects of lisuride can be increased by other sedative medicines. When Lisuride is taken together with neuroleptics or dopamine antagonists, the drugs weaken each other.

Contraindications for treatment with lisuride are disorders of liver function and cardiovascular diseases. Lisuride must also not be administered in the case of organ fibrosis, such as pulmonary fibrosis. Otherwise there could be an increased pathological connective tissue remodeling of the organ's functional tissue.

Lisuride may only be used during pregnancy in absolutely exceptional cases. The milk-inhibiting effect should be noted in breastfeeding women. Another contraindication for lisuride is cardiac arrhythmia.