Nicergoline, ampoules 4mg, 5ml, 5pcs

Composition

Active ingredient:

nicergoline 4 mg

Excipients:  

tartaric acid-1.04 mg;

lactose monohydrate (milk sugar) — 30 mg

Pharmacological action

Nicergoline is an alpha-adrenoblocking agent-a synthetic derivative of ergot alkaloids, with an attached bromo-substituted nicotinic acid residue. It has a vasodilating effect (including on the cerebral arteries). Improves microcirculation.

The contained nicotinic acid residue has a direct myotropic antispasmodic effect on the muscle membrane of blood vessels, increases their permeability to glucose (leveling the opposite effect of the ergoline ring), which is most clearly manifested in relation to the vessels of the brain and extremities. Improves brain, lung and kidney blood flow. Reduces the tone of central blood vessels, increases arterial blood flow, increases the delivery of oxygen and glucose.

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

Pharmacokinetics

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

70-80% of the drug and its metabolites are excreted by the kidneys within 70-100 hours after use. 20% is excreted in the feces. The half – life of the drug is 2.5 hours, MDL – 12-17 hours,1-MMDL – 2-4 hours.

Indications

Cerebral circulatory disorders (cerebral vascular atherosclerosis, cerebral artery thrombosis and thromboembolism, post-traumatic encephalopathy, psychoorganic syndrome);

vertigo, migraine;

peripheral circulatory disorders (organic and functional), limb arteriopathy: obliterating endarteritis, Raynaud’s disease, diabetic angiopathy;

corneal dystrophic diseases, diabetic retinopathy, ischemic optic neuropathy the nerve.

Contraindications

Hypersensitivity, hypotension, organic heart damage, myocardial infarction, tension angina, pregnancy, lactation.

Side effects

Dyspepsia (nausea, vomiting, diarrhea, abdominal pain);

hyperemia of the skin of the face and upper body,

fever, sleep disorders, decreased blood pressure, headache, dizziness, angina pectoris, symptoms of ergotism;

cold extremities, pain in the extremities; itching of the skin, allergic reactions.

Interaction

Increases the effects of antihypertensive agents, anxiolytics and antipsychotics.

Antacids and colestyramine slow absorption.

Adrenostimulants, when used together, can cause idiosyncrasy.

How to take, course of use and 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 lower therapeutic doses.

Overdose

Symptoms:  increased severity of side effects, with the exception of allergic reactions.

Treatment:  symptomatic therapy.

Product form

solution for injection

Storage conditions

In a dark place, at a temperature of 2-10 °C.

Shelf life

3 years

Active ingredient

Nicergoline

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection

Description

For adults as directed by your doctor

Indications

Cerebrovascular accident