Nitserium 30 UNO

General characteristics. Structure:

Active ingredient: nitsergolina of 30 mg;

excipients: sugar spherical, macrogoal 4000, polyacrylate dispersion, talc;

cover: gelatin, titanium dioxide (E171), ferrous oxide yellow (E172).

Pharmacological properties:

Pharmacodynamics. Nitserium 30 UNO — a peripheral vazodilatator. Blocks α-adrenoceptors, thanks to what renders vasodilating effect, reduces OPSS and the ABP. Slows down aggregation of thrombocytes, reduces viscosity of blood. Pharmakodinamichesky properties of a nitsergolin are based on its ability to influence cellular metabolism — to increase utilization of glucose and oxygen, to increase the content of ATP, proteins and synthesis of nucleic acids. Nitserium 30 UNO improves cerebral blood circulation, provides protection of a brain against damage to conditions of a hypoxia and ischemia. Positively influences neural transfer, increases intensity of exchange of a dopamine and noradrenaline, increases the tsAMF level. The digital analysis of data of EEG confirms positive influence of a nitsergolin on bioelectric activity of a brain and strengthening of its adaptation opportunities. Nitsergolin renders positive effect on cognitive function, improves memory, psychomotor activity, prevents affective disturbances and somatic dysfunctions (increased fatigue, anorexia, dizziness).

In the clinical relation preliminary researches using a low daily dose (30 mg of a nitsergolin) showed statistically reliable improvement only of dementia syndrome monosymptoms. In therapeutic researches of the last time more expressed and more extensive improvements of a syndrome of dementia on average for 25% it was reached at use of a daily dose of 60 mg (2×30 mg) during the 3-6-month period of observation. Therapeutic success grew gradually and became noticeable in comparison with an initial situation after 3 months of treatment.

At patients with dementia and positive reaction on ницерголин improvement of a clinical state continued till 6th month of treatment.

Pharmacokinetics. Absorption. Nitsergolin quickly and almost is completely soaked up in a GIT. It is subject to considerable effect of primary passing through a liver. Degree of system availability is unknown. After introduction of 70 mkg/kg of body weight it is radioactive a marked nitsergolin its concentration in a blood plasma made 100–200 ng/ml.

Distribution. Nitsergolin actively contacts proteins of a blood plasma, at the same time his affinity to albumine is about 4 times lower, than to α1-кислому to a glycoprotein. The percent of binding remains rather constant at physiological concentration of a protein in plasma, even when concentration of a nitsergolin is increased. As concentration α1-кислого a glycoprotein in a blood plasma at patients of advanced age at morbid conditions, for example at acute inflammatory processes, oncological diseases or in case of a stress can increase, that is all bases to believe that effective concentration of active ingredient under such circumstances can be reduced.

Metabolism. Nitsergolin is almost completely metabolized by hydrolysis of radio communication and N-demethylation. Active metabolites which at the same time are formed, conjugated with glucuronic acid.

Elimination. Metabolites of a nitsergolin are excreted for 80% by kidneys and for 10% — with a stake.

Т½ the nitsergolina makes 2,5 h, its main metabolite — 10-metoksi-digidrolizergola — 12–17 h, other metabolite — 1-methyl-10-metoksi-digidrolizergola — from 2 to 4 h.

Given concerning excretion in cases of bounded function of a liver or kidneys is not present.

Indications to use:

For treatment of the states which are characterized by deterioration in cognitive function, states after a stroke, vascular dementia (multiinfarctive dementia), degenerative states connected with dementia (senile and presenile dementia of altsgeymerovsky type, dementia at Parkinson's disease) as drug favorably influences not only on a condition of cognitive function, but also disturbance of mood and behavior — positively influences the cheerfulness level, ability to concentration and an emotional state.

Route of administration and doses:

For ensuring the best absorption of the capsule it is necessary to swallow whole, washing down with a glass of water, to food. Before an initiation of treatment drug Nitserium 30 UNO it is necessary to exclude a possibility that complaints of the patient are caused by primary disease which demands specific treatment.

Usual daily dose — 1 capsule a day (30 mg of a nitsergolin). If at use of this dose the desirable effect is not reached, the daily dose can be raised to 2 capsules (60 mg of a nitsergolin a day).

After noticeable improvement of symptomatology in many cases the dose decline is possible.

Patients with an impaired renal function (creatinine level in blood serum> 2 mg / 100 ml) need to lower a dose.

As the effect of use of drug increases gradually, it is recommended to accept drug for a long time. Through the corresponding periods, but at least every 6 month, it is necessary to estimate need for further treatment by drug Nitserium 30 UNO.

Features of use:

In general in the recommended therapeutic doses ницерголин does not cause changes of the ABP; at the patients inclined to AG, drug can gradually reduce the ABP level. 

At weak bradycardia ницерголин it is possible to apply only with extra care.

Or with hyper uraemia in the anamnesis or during treatment by the drugs influencing metabolism and excretion of uric acid ницерголин it is necessary to apply to treatment of patients with gout with care. 

Proceeding from a research of pharmacokinetics and portability, there is no need to change a drug dose for patients of advanced age.

Nitsergolin it is impossible to apply at the same time with the means exciting TsNS, α-and β-adrenomimetikam. At simultaneous use with anticoagulants and antiagregant it is necessary to control blood coagulation parameters.

Patients with rare hereditary intolerance of fructose, a syndrome of reduced absorption of glucose galactose or deficit of invertase-isomaltase should not accept Nitserium 30 UNO. 

During treatment nitsergoliny it is impossible to take alcoholic beverages.

Use during pregnancy or feeding by a breast. Nitsergolin it is not necessary to appoint during pregnancy as experience concerning 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 ницерглин to maternal milk.

Children. Drug is not appointed to children.

Ability to influence speed of response at control of vehicles or work with other mechanisms. Before clarification of individual reaction on ницерголин during treatment it is necessary to be careful at control of vehicles and occupations other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Undesirable effects arise seldom and are usually connected with vasodilating effect of drug. Insignificant decrease in the ABP, dizziness, especially at patsiyet with arterial hypotension are possible. Temporary erubescence, the passing, poorly expressed blood inflow, feeling of compression of the head, fatigue, stenocardia attacks, a cryesthesia in extremities, the increased sweating, increase in acidity of a gastric juice, nausea, vomiting, diarrhea, an abdominal pain, extremity pain, disturbance of an ejaculation, skin rash, drowsiness, sleeplessness is sometimes observed.

Insignificant gastric frustration which can be prevented are in some cases possible, accepting drug together with food.

Interaction with other medicines:

As ницерголин oppresses aggregation of thrombocytes and reduces viscosity of blood, it is necessary to control to a thicket blood coagulation parameters, especially at the patients predisposed to such disturbances.

At a concomitant use Nitserium 30 UNO can strengthen cordial effects of β-adrenoblockers and effect of drugs, the reducing ABP. Efficiency of the sympathomimetics stimulating α-or β-receptors, can be weakened if to accept them along with nitsergoliny.

Antacids and Colestyraminum slow down drug absorption.

As ницерголин it is metabolized by means of CYP 2D6 enzyme, it is impossible to exclude interactions with drugs (such as quinidine sulfate, the majority of antipsychotic means, including clozapine, рисперидон, a haloperidol, thioridazine) which are metabolized by this enzyme too.

Contraindications:

Hypersensitivity to a nitsergolin, other alkaloids of an ergot or any of drug ingredients. Recently postponed myocardial infarction, acute bleedings, heavy bradycardia (<50 уд. / mines), arterial hypotension, orthostatic dysregulation, simultaneous treatment by the sympathomimetics stimulating α-or β-receptors.......... Period of pregnancy and feeding by a breast. Children's age.

Overdose:

Till this time about cases of overdose of drug it was not reported. In case of overdose considerable decrease in the ABP can be observed. 

Treatment — symptomatic. In case of overdose or intoxication it is necessary to stop at once administration of drug, to wash out a stomach.

The doctor estimates weight of overdose and makes the decision of rather necessary measures. In treatment the priority is given to symptomatic actions. If the patient in consciousness, it is necessary to cause as soon as possible in it vomiting for the purpose of reduction of amount of rezorbirovanny drug.

Further actions for reduction of a resorption: gastric lavage, reception of absorbent carbon and acceleration of a passage of gastrointestinal contents (sodium sulfate).

In case of decrease in the ABP it is necessary to carry out in/in administration of liquid, introduction indirect, and it is possible as well direct α-sympathomimetics;;;;;;;;;; in case of a vasospasm — vazodilatator (depending on a situation and signs — blockers of β-adrenoceptors, antagonists of calcium, a papaverine, theophylline). Always monitoring of cardiovascular system is necessary.

The specific antidote is unknown.

Storage conditions:

In original packaging at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 capsules in the blister, on 3 (3 x 10) blister in a cardboard box.