Nicergoline (Lyophilisate) Instructions for Use

ATC Code

C04AE02 (Nicergoline)

Active Substance

Nicergoline (Rec.INN registered by WHO)

Clinical-Pharmacological Group

A drug that improves cerebral circulation

Pharmacotherapeutic Group

Peripheral vasodilators; ergot alkaloids

Pharmacological Action

Alpha-adrenoblocker. It improves cerebral circulation and activates brain metabolism.

It reduces cerebral vascular resistance, increases arterial blood flow and the consumption of oxygen and glucose by brain tissues.

It reduces pulmonary vascular resistance.

It increases the blood flow rate in the vessels of the upper and lower extremities, especially in cases of circulatory disorders.

It reduces platelet aggregation and improves hemorheological parameters.

In patients with arterial hypertension, it may cause a gradual decrease in blood pressure.

Pharmacokinetics

After oral administration, Nicergoline is rapidly and almost completely (90-100%) absorbed from the gastrointestinal tract.

The C_max of nicergoline in blood plasma is reached within 1-1.5 hours.

It is metabolized by hydrolysis, demethylation and glucuronidation.

Three metabolites of nicergoline are known, the main one being 6-methyl-8β-hydroxymethyl-10α-methoxyergoline.

70-80% of nicergoline and its metabolites are excreted by the kidneys within 70-100 hours after oral administration.

20% of nicergoline is excreted in the feces.

The T_1/2 of nicergoline in healthy volunteers is 2.5 hours, and that of the main metabolite is 12-17 hours.

Indications

Acute and chronic cerebral circulation insufficiency (including cerebral vascular atherosclerosis, dynamic disorders of cerebral circulation, thrombosis and embolism of cerebral vessels), migraine, obliterating diseases of limb vessels, Raynaud’s disease, arterial hypertension and hypertensive crisis (as an auxiliary agent).

ICD codes

Dosage Regimen

Lyophilisate

The dose is set individually.

Orally – 5-10 mg 3 times/day; the course of treatment is 2-3 months or more.

Intramuscularly – 2-4 mg 2 times/day.

The single dose for intravenous drip infusion is 4-8 mg, for intra-arterial administration – 4 mg.

In some cases, at the beginning of treatment, it is administered intramuscularly or intravenously, then orally as maintenance therapy.

Adverse Reactions

From the cardiovascular system orthostatic hypotension and dizziness (especially after intramuscular or intravenous administration), fainting, facial skin redness.

From the central nervous system sleep disorders, agitation, drowsiness, insomnia, anxiety, increased sweating.

From the digestive system nausea, diarrhea, increased gastric juice acidity, abdominal pain, decreased appetite.

Allergic reactions erythema, urticaria.

Contraindications

Acute bleeding, recent myocardial infarction, arterial hypotension, severe bradycardia, concurrent use of alpha- and beta-adrenoblockers, pregnancy, lactation, hypersensitivity to nicergoline.

Use in Pregnancy and Lactation

Nicergoline is contraindicated for use during pregnancy and during the lactation (breastfeeding) period.

Use in Renal Impairment

Patients with renal failure and a serum creatinine level of more than 2 mg/dL require a dosage regimen adjustment.

Geriatric Use

Elderly patients with a serum creatinine level of more than 2 mg/dL require a dosage regimen adjustment.

Special Precautions

Patients with renal failure and elderly patients with a serum creatinine level of more than 2 mg/dL require a dosage regimen adjustment.

After intramuscular or intravenous administration of nicergoline, the patient must remain in a horizontal position for several minutes.

During long-term therapy, patients should be examined at least once every 6 months for possible dose reduction or discontinuation of nicergoline.

Drug Interactions

With concurrent use with antihypertensive agents, the antihypertensive effect is enhanced.

With concurrent use, the effect of indirect anticoagulants and antiplatelet agents is enhanced.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.