Nitsergolin

General characteristics. Structure:

Active ingredient: 5 mg, 10 mg or 30 mg of a nitsergolin in 1 tablet.

The drug possessing the alpha and adrenolytic, vazodilatiruyushchy and improving cerebral circulation action.

Pharmacological properties:

Pharmacodynamics. Renders both alpha and adrenoceptor blocking action, and myotropic spasmolytic action on resistive vessels (it is especially active concerning vessels of a brain and extremities), increases their permeability for glucose. Blocks the vasoconstrictive reactions of brain vessels caused by serotonin. Inhibits aggregation of thrombocytes. Improves a brain, pulmonary and renal blood stream, normalizes blood supply of extremities at spastic arteriopatiya. With arterial hypertension can cause gradual moderate pressure decrease in patients.

Pharmacokinetics. Quickly and almost completely (90–100%) it is soaked up. Bioavailability — about 60%. Cmax is defined by 1–1,5 h 90% of drug is metabolized by hydrolysis, demethylation and a glyukuronization to 1,6-dimetil-8beta-oksimetil-a 10alfa-metoksiergolina (1-MMDL), 1-gidroksimetil-6-metil-8beta-oksimetil-a 10alfa-metoksiergolina (1-OHMMDL) and 6-metil-beta-oksimetil-a 10alfa-metoksiergolina (MDL — the main active metabolite). Kidneys remove 70–80% of drug and metabolites during 70–100 h after reception. With a stake 20% are removed. Drug T1/2 — 2,5 h, MDL — 12–17 h, 1-MMDL — 2–4 h.

Indications to use:

Disturbances of cerebral circulation (including at atherosclerosis of vessels of a brain, a stroke, brain ischemia, effects of thrombosis and a thromboembolism of vessels of a brain, posttraumatic encephalopathy, a psychoorganic syndrome); migraine; vascular disorders of the peripheral blood circulatory system (an arteriopatiya of extremities, a Raynaud's disease), dementia, вертиго, an obliterating endarteritis, diabetic retino-and an angiopatiya, dystrophic diseases of a cornea, vascular disorders in mesh and vascular covers of an eye, ischemic neuropathy of an optic nerve, vestibular and labyrinth disturbances of vascular genesis; a prostatauxe, the disturbances of an urination connected with a neurogenic bladder.

Route of administration and doses:

Inside, before or during food, without chewing, washing down with enough liquid, 5–10 mg 3 times a day. At bounded function of kidneys (the size of serumal creatinine more than 2 mg/ml) — on 5 mg 2–3 times a day.

In/in kapelno on 4–8 mg on 100 ml of normal saline solution of sodium of chloride; 2 times, in oil on 2–4 mg, a day; in / and — on 4 mg in 10 ml of normal saline solution of sodium of chloride, within 2 min. A course of treatment — of 2–3 weeks to several months.

Features of use:

Use at pregnancy and feeding by a breast. Contraindicated at pregnancy. For the period of treatment it is necessary to stop breastfeeding.

At persistent bradycardia (ChSS at rest — less than 50 уд. / mines) administration of drug is possible only at careful medical control. At simultaneous use with anticoagulants and antiagregant control of parameters of coagulability of blood is necessary. With care apply with hypotensive drugs.

After parenteral administration for the prevention of orthostatic effect or when developing of the expressed hypotension it is recommended to accept horizontal position na10-15min.

The patient with a renal failure, and also to elderly patients the daily dose has to be reduced. It is not necessary to apply in operating time to drivers of vehicles and people whose profession is connected with the increased concentration of attention. For the period of treatment it is necessary to refrain from alcohol intake.

Side effects:

From a nervous system and sense bodys: headache, dizziness, drowsiness, feeling of fatigue, sleeplessness, excitement, concern, syncope.

From cardiovascular system and blood (a hemopoiesis, a hemostasis): orthostatic hypotension, stenocardia attack, reduction of viscosity of blood, cold snap of extremities.

From bodies of a GIT: nausea, vomiting, loss of appetite, diarrhea, abdominal pains, increase in acidity of a gastric juice.

From urinogenital system: disturbance of an ejaculation.

From integuments: perspiration.

Allergic reactions: itch and hyperemia of the person and upper half of a trunk, erythema, small tortoiseshell.

Others: extremity pain, heat.

Interaction with other medicines:

Strengthens effects of antihypertensives, anxiolytics and antipsychotic means. Antacids and холестирамин slow down absorption. It is necessary to avoid combined use with the drugs exciting TsNS alpha and beta-adrenergic agonists.

Contraindications:

Hypersensitivity, arterial hypotension, the expressed atherosclerosis of peripheral vessels, organic lesions of heart, recently postponed myocardial infarction, angina of exertion, bradycardia, acute bleeding, pregnancy, feeding by a breast.

Overdose:

Symptoms: decrease in the ABP.

Storage conditions:

To store at a temperature of 15-25 °C, in dry, protected from light and the place, unavailable to children. Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets of 5 mg, 10 mg or 30 mg. On 20 tablets in each blister, on one, two or three blisters together with the application instruction in cardboard packaging.