Nitsergolin

General characteristics. Structure:

Active ingredient: 10 mg of a nitsergolin in 1 tablet.

Excipients: lactoses monohydrate, potato starch, silicon dioxide colloid (aerosil), magnesium stearate.

 Excipients for a cover: sucrose (sugar), povidone, hydroxycarbonate magnesium pentahydrate, silicon dioxide colloid (aerosil), talc, titanium dioxide, beeswax.

Pharmacological properties:

Pharmacodynamics. Shows alpha 1-adrenoceptor blocking action.

Pharmacokinetics. After intake, ницерголин it is quickly and almost completely absorbed. Key products of metabolism of a nitsergolin 1,6–диметиë–8?–гидроксиметиë–10?–метоксиэрголин (MMDL, a hydrolysate) and 6–метиë–8бетà–гидроксиметиë–10альфà–метоксиэрголин (MDL, a demethylation product under the influence of CYP2D6 isoenzyme). Ratios of values of the area under a curve "concentration time" (AUC) for MMDL both MDL at intake and intravenous administration of a nitsergolin indicate the expressed metabolism at the first passing. After reception of 30 mg of a nitsergolin inside the maximum concentration of MMDL (21±14 ng/ml) and MDL (41±14 ng/ml) were reached approximately in 1 and 4 hours respectively, then concentration of MDL decreases with an elimination half-life of 13 - 20 h. Meal has no significant effect on degree and speed of absorption of a nitserglin. Nitsergolin it is active (> 90%) degree of his affinity contacts proteins of plasma, and to  ? - acid of a glycoprotein has more, than to a seralbumin. It is shown that ницерголин and its metabolites can be distributed in blood cells. The pharmacokinetics of a nitsergolin at use of doses to 60 mg has linear character and does not change depending on age of the patient.

Nitsergolin is brought in the form of metabolites, generally with urine (about 80% of the general dose) and in a small amount with a stake (10–20%). At patients with a heavy renal failure considerable decrease in extent of removal of products of metabolism with urine in comparison with patients with normal function of kidneys is observed.

Indications to use:

Acute and chronic cerebral metabolic and vascular disorders (owing to atherosclerosis, arterial hypertension, thrombosis or a vascular embolism of a brain), including the tranzitorny ischemic attack, vascular dementia and a headache caused by a vasospasm.

Acute and chronic (metabolic and vascular) peripheral disturbances (the organic and functional arteriopatiya, a Raynaud's disease, syndromes caused by disturbance of a peripheral blood-groove).

Route of administration and doses:

Inside, on 10 mg three times a day with identical intervals between receptions during a long span (up to several months).

At vascular dementia use of 30 mg 2 times a day is shown, at the same time each 6 months it is recommended to consult with the doctor about expediency of continuation of therapy.

The dose and duration of treatment depend on character, disease severity and efficiency of treatment. It is in certain cases preferable to begin therapy with parenteral administration, and then to pass to administration of drug inside for the supporting treatment.

At a renal failure (serumal creatinine ≥ 2 mg/dl) it is recommended to use drug in lower therapeutic doses.

Features of use:

Use at pregnancy and during breastfeeding. Nitsergolin it is necessary to apply, only if the expected advantage for mother exceeds possible risk for a fruit and the child.

In therapeutic doses ницерголин, as a rule, does not influence arterial pressure, however, drug can cause a gradual lowering of arterial pressure in patients with an arterial hypertension.

Drug works gradually therefore it should be accepted for a long time, at the same time the doctor has to periodically (at least each 6 months) to estimate effect of expediency of continuation of treatment.

Influence on ability to control of vehicles and to service of moving mechanisms. In spite of the fact that ницерголин improves reaction and concentration of attention, its impact on ability to drive the car and to use a difficult technique specially it was not studied. Anyway it is necessary to be careful, considering character of a basic disease.

Side effects:

Allergic reactions, lowering of arterial pressure, dizziness, feeling of heat, drowsiness or sleeplessness, dispeptic phenomena.

Increase in concentration of uric acid in blood is possible, and this effect does not depend on a dose and duration of therapy. Side effect is usually easy or moderately expressed.

If any of the side effects specified in the instruction are aggravated, or you noticed any other side effects which are not specified in the instruction, report about it to the doctor.

Interaction with other medicines:

Strengthens effects of hypotensive medicines. ницерголин it is metabolized under the influence of CYP450 2D6 isoenzyme therefore it is impossible to exclude a possibility of its interaction with drugs which are metabolized with the participation of the same enzyme.

Contraindications:

Hypersensitivity to a nitsergolin or other components of drug, recently postponed myocardial infarction, acute bleeding, the expressed bradycardia, disturbance of orthostatic regulation, deficit of invertase/isomaltase, deficit of lactase, a lactose intolerance, intolerance of fructose, glyukozo-galaktozny malabsorption, children's age up to 18 years.

With care. A hyperuricemia or gout in the anamnesis and/or in combination with medicines which break metabolism or removal of uric acid.

Overdose:

Symptoms: the passing expressed lowering of arterial pressure.

Treatment: special treatment usually is not required, it is enough to lay the patient in horizontal position on several minutes, in exceptional cases at sharp disturbance of blood supply of a brain and heart introduction of sympathomimetic means under constant control of arterial pressure is recommended.

Storage conditions:

In the dry place protected from light at a temperature not above 25 °C. In the place, unavailable to children! A period of validity - 3 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated, 10 mg. On 10, 15, 20 or 30 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1, 2, 3 or 5 blister strip packagings with the application instruction in a pack from a cardboard.