Nitsergoline, 10 mg 30 pcs

Pharmacotherapeutic group

Alpha-adrenoblocker

Pharmacological properties
Produces alpha 1-adrenoblocking action

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Pharmacokinetics

After oral administration, nicergoline is rapidly and almost completely absorbed. The main products of metabolism of nicergoline are 1,6-dimethyl-8β-hydroxymethyl-10α-methoxyergoline (MMDL, hydrolysis product) and 6-methyl-8β-hydroxymethyl-10α-methoxyergoline (MDL, demethylation product by CYP2D6 isoenzyme). Ratios of the area under the concentration-time curve (AUC) values for MMDL and MDL when administered orally and intravenously with nicergoline indicate marked metabolism during the first passage.

After oral administration of 30 mg of nicergoline, maximum concentrations of MMDL (21 ± 14 ng/mL) and MDL (41 ± 14 ng/mL) were reached after approximately 1 and 4 hours, respectively, and then MDL concentrations decrease with a half-life of 13 to 20 hours. Food intake has no significant effect on the degree and rate of absorption of Nicerglin.

Nicergoline actively ( > 90%) binds to plasma proteins, with a greater degree of affinity for α-acid glycoprotein than for serum albumin. It has been shown that nicergoline and its metabolites can be distributed in blood cells. The pharmacokinetics of nicergoline at doses up to 60 mg are linear and do not vary with the age of the patient.

Nicergoline is excreted as metabolites, mainly in the urine (approximately 80% of the total dose) and in small amounts in the feces (10 – 20%). In patients with severe renal impairment a significant decrease in the degree of excretion of metabolites with urine is observed compared to patients with normal renal function.

Indications

Acute and chronic cerebral metabolic and vascular disorders (due to atherosclerosis, arterial hypertension, cerebral vascular thrombosis or embolism), including transient ischemic attack, vascular dementia and vasospasm-induced headache.

Acute and chronic (metabolic and vascular) peripheral disorders (organic and functional arteriopathies, Raynaud’s disease, syndromes caused by disorders of peripheral blood flow).

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Active ingredient

Nitsergoline

Composition

1 tablet contains:

Active ingredient:

• nicergoline – 10 mg

Associates

Lactose monohydrate – 70.0 mg

• Potato starch – 26.9 mg

• Colloidal silica (aerosil) – 2.0 mg

• magnesium stearate – 1.1 mg

Average weight of the tablet without the shell – 110 mg

Shell excipients

• sucrose (sugar) – 65.3 mg

• povidone – 1.967 mg

• magnesium hydroxycarbonate pentahydrate – 2.1 mg

• silicon dioxide colloid (aerosil) – 0.13 mg

• 0.016 mg of talcum powder

• titanium dioxide – 0.37 mg

• beeswax – 0.117 mg

Average weight of the coated tablet – 180 mg

Auxiliary substances – core:

• Potato starch,

• magnesium carbonate basic,

• milk sugar (lactose),

• stearic acid,

• magnesium stearate,

• Polyvinylpyrrolidone low molecular weight medical (povidone),

• coating:

• sucrose,

• magnesium carbonate basic, <

• aerosil (colloidal silicon dioxide),

• Low molecular weight polyvinylpyrrolidone medical (povidone),

• talc,

• beeswax,

• gelatin medical,

• titanium dioxide.

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