Nitsergoline, lyophilizate 4 mg 35 mg 5 pcs

Nicergoline is an alpha-adrenoblocking agent – a synthetic derivative of ergot alkaloids, with an attached bromosubstituted nicotinic acid residue. It has a vasodilator effect (including against the cerebral arteries). It improves microcirculation.

The contained residue of nicotinic acid has a direct myotropic spasmolytic effect on the muscular membrane of blood vessels, increases their permeability to glucose (leveling the opposite effect of the ergoline ring), which is most clearly seen in relation to the vessels of the brain and limbs. It improves cerebral, pulmonary and renal blood flow. It reduces the tone of the central vessels, increases arterial blood flow, increases oxygen and glucose delivery.

In therapeutic doses does not affect blood pressure; in patients with arterial hypertension it may cause a gradual moderate decrease in pressure. Reduces platelet aggregation and improves hemorheological parameters. It improves blood flow in the extremities, especially in circulatory insufficiency due to functional arteriopathies.

Pharmacokinetics

The bioavailability is about 60%. The maximum concentration is determined after 1-1.5 hours. 90% of the drug is metabolized by hydrolysis, demethylation and glucuronization to 1,6-dimethyl-8beta-oxymethyl-10alpha-methoxyergoline (1-MMDL), 1-hydroxymethyl-6-methyl-8beta-oxymethyl-10alpha-methoxyergoline (1-OHMMDL) and 6-methyl-8beta-oxymethyl-Ualpha-methoxyergoline (MDL – main active metabolite).

The kidneys excreted 70-80% of the drug and metabolites within 70-100 hours after administration. With the feces 20% of the drug is excreted. Period of half-life of the preparation is 2.5 hours, MDL – 12-17 hours, 1-MMDL – 2-4 hours.

Indications

Cerebral circulation disorders (atherosclerosis of cerebral vessels, thrombosis and thromboembolism of cerebral arteries, post-traumatic encephalopathy, psychoorganic syndrome); Vertigo, migraine;

Peripheral circulatory disorders (organic and functional), arteriopathy of the extremities: obliterating endarteritis, Raynaud’s disease, diabetic angiopathy; dystrophic diseases of the cornea, diabetic retinopathy, ischemic optic neuropathy.

Active ingredient

Composition

Active ingredient: nitergoline 4 mg

Associates:

Tartaric acid, 1.04 mg;

Lactose monohydrate (milk sugar), 30 mg

How to take, the dosage

Intramuscularly, pre-dissolved in the attached 0.9% sodium chloride solution, 2-4 mg 2 times a day.

The dose and duration of therapy depend on the nature of the disease.

Patients with impaired renal function (serum creatinine ≥2 mg/dL) are recommended to use in lower therapeutic doses.

Interaction

It enhances the effects of hypotensive drugs, anxiolytics and antipsychotics.

Antacids and colestyramine slow down absorption.

Adrenostimulants may cause idiosyncrasy when used together.

Contraindications

Hypersensitivity, arterial hypotension, organic heart disease, myocardial infarction, angina pectoris, pregnancy, lactation.

Side effects

Dyspepsia (nausea, vomiting, diarrhea, abdominal pain); hyperemia of the skin of the face and upper half of the trunk, fever, sleep disorders, decreased blood pressure, headache, dizziness, angina, symptoms of ergotism;

Cold extremities, pain in the extremities; skin itching, allergic reactions.

Overdose

Symptoms: increased severity of side effects, except for allergic reactions.

Treatment: symptomatic therapy.

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