A Look At Drugs Used For Restless Leg Syndrome

Concept

Restless legs syndrome is mainly manifested as indescribable paresthesia and discomfort in the lower limbs at rest or during sleep at night, with a strong desire to move the legs, and the patient is constantly forced to tap the lower limbs to relieve pain, often aggravated by rest at night , the symptoms relieved after the activity, and can reappear after the cessation. The disease can induce depression, schizophrenia, sleep disorders and other complications.

Classification

Restless legs syndrome is divided into primary and secondary. The specific cause of primary restless legs syndrome is not yet clear, but may be related to genetics and abnormal brain dopamine function; secondary restless legs syndrome has various causes, including spinocerebellar ataxia, peroneal muscular atrophy, Parkinson's disease, Rheumatic diseases, iron deficiency anemia, uremia, pregnancy, etc.

Early detection, early diagnosis, and early treatment of restless legs syndrome are extremely important for improving symptoms, delaying disease progression, and preventing complications. Here are a few drugs used for restless leg syndrome.

First class of drugs used for restless leg syndrome-Dopamine receptor agonists

The effect is better and can be used as the drugs used for restless leg syndrome of choice, such as rotigotine. Rotigotine belongs to a class of non-ergot selective dopamine receptor agonist drugs that work by stimulating dopamine receptors in the body and mimicking the neurotransmitter dopamine. Rotigotine can excite 5-HT1A receptors and produce anxiolytic effects similar to buspirone; it produces anti-dyskinetic effects by blocking adrenergic α2B receptors. Rotigotine has no affinity for the 5HT2b receptor. Rotigotine is used for the treatment of moderate-to-severe primary restless legs syndrome. It is transdermally administered, which can continuously release the drug, maintain the drug concentration in the blood and cerebrospinal fluid, and reduce the peak-to-trough effect of the drug. Compared with the abdomen and buttocks, the difference in bioavailability was less than 1%, with the shoulders having the highest bioavailability at 64%. Low-dose use before bed can improve symptoms, reduce periodic limb movements, and improve sleep quality. The main adverse reactions were nausea, dizziness, vertigo, fatigue, vomiting and insomnia. Other potential safety concerns include sudden somnolence, hallucinations, orthostatic hypotension, and peripheral edema.

Second class of drugs used for restless leg syndrome-Levodopa

L-dopa is an intermediate in the formation of catecholamine from tyrosine, a precursor of dopamine. About 95% of L-dopa absorbed into the blood is decarboxylated by dopa decarboxylase in peripheral tissues to form catecholamines, which are not easy to pass through the blood-brain barrier, but cause many adverse reactions. Only 1% of L-dopa enters the cerebral circulation, and reaches the central nervous system, where it is converted into catecholamines to play a therapeutic role. It has no significant pharmacological effect by itself, but exerts its curative effect indirectly through catecholamines. Oral administration before bed can significantly improve symptoms, reduce periodic limb movements, improve sleep quality, and reduce daytime drowsiness. Most patients tolerate it well. But there are also some side effects. Common adverse reactions are: nausea, vomiting, orthostatic hypotension, abnormal involuntary movements of head, face, tongue, upper extremities and upper body, mental depression, dysuria. Less common adverse reactions are: hypertension, arrhythmia, hemolytic anemia.

Third class of drugs used for restless leg syndrome-Anticonvulsants

If patients cannot tolerate dopamine agonists, gabapentin and carbamazepine can be considered, which are more effective for patients with pain symptoms.

Gabapentin has been shown to prevent epilepsy in various animal models, in addition, in animal models of spasticity, analgesia and amyotrophic sclerosis. Gabapentin has a high affinity for novel binding sites in brain tissue, it can pass through some barriers in the body through amino acid transfer bodies, and compared with other anticonvulsants, gabapentin has less behavioral and cardiovascular side effects. Gabapentin has a high affinity for a novel binding site in brain tissue, it can pass through some barriers in the body through amino acid transsomes, and is used in patients that are not satisfactorily controlled or tolerated by conventional drugs used for restless leg syndrome. 

Carbamazepine is mainly used for complex partial seizures and generalized tonic-twin seizures, and is also used as a drug for restless legs syndrome.

At the same time, it is necessary to cooperate with non-drug treatments, such as daily exercise to increase the body's ability to resist disease, not to be overtired, over-consumed, and quit smoking and drinking. Maintain balance and overcome anxiety and tension. Improve the living environment space and develop good living habits.