Nitserium

General characteristics. Structure:

Active ingredient: ницерголин 10 mg

Other ingredients: starch corn, lactoses monohydrate, povidone, silicon dioxide colloid anhydrous, magnesium stearate, methacrylate copolymer (type A), sucrose, talc, solution of glucose, calcium the carbonate, starch corn modified triethyl citrate, wax montaglikolevy, titanium dioxide (E171), a yellow decline of FCF (Е 110).

Pharmacological properties:

Pharmacodynamics. After reception active ingredient of drug Nitserium — ницерголин — is quickly and extensively metabolized with formation of metabolites which activity was observed in TsNS at several levels.

Nitserium has the following neuropharmacological effect: drug not only improves absorption and consumption of glucose in a brain, biosynthesis of proteins and nucleic acids, but also influences various systems of neurotransmitters.

Strengthening of activity of cholineacetyltransferase and density of muskarinovy receptors was also observed after long reception of Nitserium. Nitsergolin considerably increased activity of acetylcholinesterase. Both after one-time, and after long administration of drug exchange basal and an agonist - a sensitive fosfoinozitid amplifies. Nitserium also increases activity and moving to a membrane of Sa-zavisimykh of isoforms of a protein kinase of C. These enzymes participate in the mechanism of secretion of the soluble amyloid predecessor of a protein that leads to strengthening of its release and to decrease in products of pathological β-amyloid..........

The antioxidant effect and activation of enzymes of a detoxication drug Nitserium protect nervous cells from death owing to oxidizing loading and apoptosis.

Nitsergolin weakens the decrease in maintenance of a sintetaza of an oxide of MRNK nitrogen depending on age in neurons that can promote improvement of cognitive function.

Pharmacokinetics. Nitsergolin quickly and almost is completely absorbed after oral administration. Peak of serumal radioactivity after use of low doses (4–5 mg) it is radioactive a marked nitsergolin it was observed in 1,5 h. However at reception of therapeutic doses (30 mg) of a H3-marked nitsergolin the radioactivity peak in a blood plasma was observed in 3 h with Т½ about 15 h (healthy patients).

Absolute bioavailability of a nitsergolin after oral administration makes about 5% that is caused by high hepatic clearance and presistemny metabolism.

Drug is quickly and extensively distributed in fabrics. The volume of distribution of a nitsergolin is rather high (> 105 l) that, perhaps, is caused by metabolism in blood and distribution in blood cells and/or fabrics.

Nitsergolin extensively contacts proteins of a blood plasma with big affinity to a α-acid glycoprotein, than albumine in blood serum.

Removal with urine is the main way of excretion as 80% of the general dose of a nitsergolin, marked radioactive isotope, also only 10-20% — in Calais are defined in urine.

The pharmacokinetics has linear character at reception of 30-60 mg of a nitsergolin.

Nitsergolin is extensively metabolized before removal. At patients with heavy renal failures considerable decrease in secretion with urine is observed.

Indications to use:

Acute and chronic disorders of cerebrovascular metabolism owing to atherosclerosis, thrombosis and an embolism of cerebral vessels, tranzitorny disturbances of cerebral blood circulation.

Acute and chronic peripheral vascular metabolic disorders (organic and functional disturbances of arteries of extremities, Raynaud's disease and other syndromes which are associated with blood circulation disturbance).

As additional therapy at AG.

Route of administration and doses:

Before an initiation of treatment drug Nitserium it is necessary to exclude a possibility that disturbance is a consequence of a basic disease which demands special treatment.

For ensuring the best absorption of a tablet to swallow whole, washing down with a certain amount of liquid (for example a glass of water), to food.

The recommended dose — 5–10 mg 3 times a day with an identical interval, are desirable between meals, for a long time.

At purpose of a nitsergolin in a dose of 5 mg use drug in a necessary dosage.

The dosage, duration of use of drug depend on a specific clinical situation and are defined individually. It is in certain cases reasonable to begin treatment with parenteral administration with the subsequent continuation of treatment in the form of the supporting peroral therapy.

Patients of advanced age. Dose adjustment is not required.

Features of use:

In general in therapeutic doses drug does not cause changes of the ABP, however in the patients inclined to AG, drug can gradually reduce the ABP. In an initiation of treatment development of orthostatic hypotension is possible.

In case of slight bradycardia it is necessary to appoint drug with care.

With a hyperuricemia or gout in the anamnesis and/or at simultaneous treatment by the drugs influencing metabolism and excretion of uric acid ницерголин it is necessary to apply to treatment of patients with care.

As about 80% of metabolites of a nitsergolin are allocated with urine, it is desirable to reduce a drug dose to patients with a renal failure (creatinine of blood serum of ≥2 mg/dl or 175 mmol/l).

Nitserium's tablets contain dye a yellow decline (E110) which can cause reactions, similar allergic, including OH in persons with special sensitivity to this substance. The allergy to this dye meets at the persons sensitive to acetylsalicylic acid more often.

Drug contains sucrose therefore it do not follow to appoint to patients with rare hereditary forms of intolerance of a galactose, deficit of lactase, invertase-isomaltase or a syndrome of glyukozo-galaktozny malabsorption.

The effect of use of drug increases gradually. Therefore, drug needs to be accepted for a long time. It is desirable that each 6 months the doctor estimated effect and made the decision on expediency of continuation of use of drug.

During use of drug it is necessary to abstain from alcohol intake.

Use during pregnancy or feeding by a breast. Nitsergolin it is not necessary to appoint during pregnancy as experience of safety of its use during this period is absent. It is not necessary to use drug during feeding by a breast as it is unknown whether gets ницерголин to breast milk.

Children. Drug is not appointed to children.

Ability to influence speed of response at control of vehicles or work with other mechanisms 

During treatment emergence of side reactions from a nervous system is possible (namely — dizziness, drowsiness, etc.) therefore in such cases it is necessary to refrain from control of vehicles or work with mechanisms.

Side effects:

It was seldom reported about the following side effects.

From a GIT: lock, nausea, vomiting, increase in acidity of a gastric juice, diarrhea, abdominal pain.

From cardiovascular system: arterial hypotension, faints, stenocardia attacks, a cryesthesia in extremities, tachycardia.

From a nervous system: dizziness, headache, confusion of consciousness, drowsiness, sleeplessness.

Allergic reactions: Quincke's disease, itch, skin rashes.

Reproductive disturbances at men: disturbances of an ejaculation.

General frustration: feeling of heat, inflows, the increased sweating, extremity pain, fervescence.

Increase in level of uric acid in blood was observed that did not depend neither on a dose, nor on treatment duration.

Interaction with other medicines:

With care drug is used with:

anti-hypertensive means (ницерголин can exponentiate their effects);

drugs which are metabolized by system of P450 2D6 cytochrome because it is impossible to exclude interaction with these means (such as quinidine sulfate, the majority of antipsychotic means, including clozapine, рисперидон, a haloperidol, thioridazine);

acetylsalicylic acid (the bleeding time can be extended);

drugs which influence metabolism of uric acid (metabolism and excretion of uric acid can change).

Nitsergolin it is impossible to apply at the same time with means which excite TsNS, α-and β-adrenomimetikam.

At simultaneous use with anticoagulants and antiagregant it is necessary to control blood coagulation parameters.

Drug can strengthen effects of cholinomimetic means.

Contraindications:

Overdose:

Simtoma: considerable decrease in the ABP, ataxy, asthma and tremor.

Treatment: a gastric lavage, reception of absorbent carbon and the corresponding symptomatic treatment for maintenance of function of vitals and systems. In case of decrease in the ABP — introduction of indirect or direct α-sympathomimetics, in case of a vasospasm — use of vazodilatator (depending on a situation and signs — antagonists of calcium, a papaverine, theophylline). Monitoring of cardiovascular system is always necessary.

Storage conditions:

At a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

Tablets п / Sakha. cover of 10 mg blister, No. 50.