Instruction for use
international and chemical name: nicergoline; 1,6-dimethyl-8ß-(5-promontories-oxymethyl)-10α-methoxyergoline.
basic physical and chemical properties: tablets of 5 mg: round, convex tablets of orange color, covered in sugar coated tablets 10 mg: round, convex tablets white sugar coated shell;
tablets 30 mg – 1 tablet contains 30 mg nargana;
excipients: cellulose microcrystalline, calcium phosphatidyl dibasic, sodium carboxym ethyl cellulose, magnesium stearate; shell: acacia resin, the resin of the sandarac, rosin, talc, magnesium carbonate, titanium dioxide (E 171), Carnauba wax, sucrose;
Form of issue. Tablets, film-coated.
Pharmacotherapeutic group. Peripheral vasodilators. Ergot alkaloids. ATC code 04 And E-02.
Pharmacodynamics. Sermion is used to improve metabolism and hemodynamics of the brain. The effect of sermion has effects on platelets and helps to improve the rheological properties of blood. Nargan is derived Ergoline with alpha-1-adrenalin action when applied parenterally. After oral administration, the drug undergoes rapid metabolism with the formation of a number of metabolites that also affect different levels of the CNS.
After oral administration of Sermion causes numerous neuropharmacologic effects: in fact not only is increased consumption of glucose by brain tissues and increases the biosynthesis of proteins and nucleic acids, but the drug affects different neurotransmitter system.
The study of pharmacodynamics in humans were performed using a computerized EEG in young and elderly healthy volunteers and in elderly patients with impaired
of cognitive functions. Sermion had normalso whose influence on EEG in elderly patients and adults after hypoxia, which was manifested in the increase in α - and β-activity in the reduction of δ - and θ-activity. Long-term use (2 to 6 months) Sermon few significant positive effects in patients with mild and moderate manifestations of dementia of different origin. Sermion is used to improve metabolism and hemodynamics of the brain. The drug has a effect effect on platelets and helps to improve the rheological properties of blood.
Pharmacokinetics. Oral use Sermion rapidly absorbed (as shown by radioisotope study, the maximum concentration level is reached after about 3 hours). The absolute bioavailability nargana that was studied after oral and internally tively the introduction of [3H]nargana from 3 healthy volunteers was < 5%. The same effect was observed in the major metabolites of the drug. Very low nargana in plasma (< 1 ng/ml) was observed after oral administration of [3H]nargana. After eating nargana at a dose of 30 mg orally, the peak concentrations of the main metabolites of the drug in plasma was observed after 1 – 4 hours. After reaching peak concentration, plasma concentration of metabolites decreased with a half-life period of 13 – 20 hours. The absorption of the drug is not dependent on concurrent food intake and form of the drug (solution or tablet is covered.) The volume of distribution nargana was 105 l, which may reflect metabolism of the drug in the blood and drug penetration into red blood cells and/or tissues. Nargan widely associated with the blood protein (> 90%) with a greater affinity to the α-acid glycoprotein than to albumin serum. The ratio of concentration of labelled [14C]nargana blood plasma concentration was > 0.5 in. This suggests that nargan and its metabolites can penetrate the blood cells in humans. As a result of long research it was determined that the pharmacokinetics nargana in elderly patients has no differences from the pharmacokinetics in adult patients.
The selection of the drug is in the form of metabolites in urine and in smaller quantities – with feces. After a single reception nargana 30 mg orally in patients with slight, moderate and severe impaired renal function was observed a decrease in the concentration of drug metabolites in urine at 32 and 59% in comparison with patients with normally functioning kidneys.
Indications for use. Sermion is used for the treatment of easy and moderately severe of Alzheimer's disease and vascular dementia. The drug is also used for the treatment of syndrome senling cognitive disorder, which is characterized by the appearance of intellectual, emotional, behavioral and somatic disorders such as memory loss, deterioration of attention and concentration, mood changes, dizziness, and asthenia.
Method of application and doses. Recommended dose - 5 - 10 mg three times a day with equal interval between doses for a long time. For improving the absorption of the drug should be taken in between meals. The tablet is taken whole with a small amount of liquid.
Side effects. Adverse events are rare, are not clinically heavy and, in General, may be associated with the vasoactive effect of the drug. Side-effects may have the following manifestations: hypotension and dizziness, hot flashes, angina, cold extremities, sweating, increased gastric acidity, nausea, vomiting, diarrhea, abdominal pain, pain in extremities, abnormal ejaculation, skin rash, drowsiness, insomnia. During studies of drug action, an increase in the level of uric acid in the blood, but this effect did not require changes to the dose or duration of treatment.
Contraindications. Sermion is contraindicated in patients in such cases: recent myocardial infarction, symptoms of acute bleeding, severe bradycardia, impaired orthostatic regulation, hypotension, angina burden, virginoa atherosclerosis, Hyper sensitivity to nargana or other tablet components.
Overdose. High-dose Sermon occasionally can cause a fast transient decrease in blood pressure. Of course this condition does not require special treatment, it is sufficient that the patient lay for a few minutes. In exceptional cases of severe insufficiency of cerebral and cardiac blood circulation can be assigned to symptomatic therapy and blood pressure monitoring.
Features of the application. In General, the recommended therapeutic dose of Sermion does not cause changes in blood pressure, patients who are prone to hypertension, the drug can gradually reduce the level of blood pressure. For the treatment of patients with gout or gpereira in history or during a treatment with drugs that affect the metabolism and excretion of uric acid, Sermion should be used with caution.
Because approximately 80% of nargana metabolites excreted in the urine, it is advisable to reduce the dose of the drug to patients with impaired renal function (serum creatinine ≥ 2%).
The effect of the drug increases gradually. Therefore, the drug should be taken for a long time. It is desirable that every 6 months the doctor assessed the effects and made the decision about whether to continue use of the drug.
Given the indications for use of this form Sermon, the appointment of its children is not expected. Based on the studies of pharmacokinetics and tolerability, no need to change the dose for elderly patients. Sermion cannot be applied simultaneously with the means that excite the Central nervous system, α - and betaadrenergic ticks. At the time of treatment contraindicated use of alcohol. While the use of anticoagulants and antiplatelet agents is necessary to control the parameters of blood coagulation.
Effects on ability to drive and operate moving mechanisms
Although clinical effects Sermone used to improve attention and concentration, its effect on ability to drive and operate moving mechanisms has never been studied.
Pregnancy and lactation. Despite the fact that during Toxicological studies Sermion had tertogennogo effect, pregnant this drug should be administered only in cases of real necessity for strict medical reasons.
Interaction with other medicinal products. Sermion may increase the effect of antihypertensive and antiholinesteraznah funds. Antacids and holestiramin slow down smokotina of the drug.
As Sermion is metabolized by the enzyme CYTP450 2D6, we cannot exclude interactions with drugs (such as HND, most antipsychotics, including clozapine, risperidone, haloperidol, thioridazine), which are also metabolized by this enzyme.
The conditions and duration of storage. Store in a dry, protected from light and inaccessible to children at temperature not above 25 ºc.
Shelf life - 36 months.
Packing. Of 30 tablets in blisters made of aluminium foil in a cardboard box.
Manufacturer. Pfizer Italy S. G. L., Italy.
Address. 63046 Marino Del Tronto, Ascoli Piceno, Italy.