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medicalmeds.eu Medicines Alpha adrenoblocker. Sermion

Sermion

Препарат Сермион. Pfizer (Пфайзер) США


Producer: Pfizer (Pfayzer) of the USA

Code of automatic telephone exchange: C04AE02

Release form: Firm dosage forms. Tablets.

Indications to use: Atherosclerosis of vessels of a brain. Arterial hypertension. Tranzitorny ischemic attack. Brain vascular embolism. Vascular dementia. Headache. Arteriopatiya. Raynaud's disease.


General characteristics. Structure:

Tablets, coated 5 mg Active agent: ницерголин 5 mg; Excipients: calcium hydrophosphate dihydrate of 100 mg, microcrystallic cellulose of 22,4 mg, magnesium stearate of 1,3 mg, sodium carboxymethylcellulose of 1,3 mg; sugar cover: sucrose of 33,35 mg, talc of 10,9 mg, acacias pitch of 2,7 mg, sandarac pitch of 1 mg, magnesium a carbonate of 0,7 mg, titanium dioxide (E171) of 0,7 mg, rosin of 0,6 mg, karnaubsky wax of 0,06 mg, sanst yellow (E110) of 0,05 mg.

Tablets, coated 10 mg Active agent: ницерголин 10 mg; Excipients: calcium hydrophosphate dihydrate of 94,3 mg, microcrystallic cellulose of 22,4 mg, magnesium stearate of 2 mg, sodium carboxymethylcellulose of 1,3 mg; sugar cover: sucrose of 33,4 mg, talc of 10,9 mg, acacias pitch of 2,7 mg, sandarac pitch of 1 mg, magnesium carbonate of 0,7 mg, titanium dioxide (E171) of 0,7 mg, rosin of 0,6 mg, karnaubsky wax of 0,06 mg.

Tablets, coated 30 mg Active agent: ницерголин 30 mg; Excipients: calcium hydrophosphate dihydrate of 72,69 mg, microcrystallic cellulose of 22,4 mg, magnesium stearate of 3,61 mg, sodium carboxymethylcellulose of 1,3 mg; film cover:  gipromelloza of 2,8985 mg, titanium dioxide (E171) of 0,7246 mg, mg polyethyleneglycol 6000 0,2899, ferrous oxide yellow (E172) of 0,0725 mg, silicone of 0,0145 mg.




Pharmacological properties:

Pharmacodynamics. Nitsergolin – derivative an ergolina, improves metabolic and hemodynamic processes in a brain, reduces aggregation of thrombocytes and improves haemo rheological indicators of blood, increases blood-groove speed in upper and lower extremities. Nitsergolin shows α1-адреноблокирующее the action leading to improvement of a blood-groove and makes direct impact on cerebral neyrotransmitterny systems — noradrenergichesky, dofaminergichesky and atsetilkholinergichesky. Against the background of use of drug activity of noradrenergichesky, dofaminergichesky and atsetilkholinergichesky cerebral systems increases that promotes optimization of cognitive processes. As a result of long therapy nitsergoliny observed permanent improvement of cognitive function and reduction of expressiveness of the behavioural disturbances connected with dementia.

Pharmacokinetics. After intake, ницерголин it is quickly and almost completely absorbed. Key products of metabolism of a nitsergolin: 1,6-диметил-8-гидроксиметил-10-метоксиэрголин (MMDL, a hydrolysate) and 6-метил-8-гидроксиметил-10-метоксиэрголин (MDL, a demethylation product under the influence of CYP2D6 isoenzyme). The ratio of values of the area under a curve "concentration – time" for MMDL and MDL at reception of a nitsergolin inside indicates (AUC) the expressed metabolism at "the first passing" through a liver. 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 decreased with an elimination half-life of 13 - 20 h. Researches confirm lack of accumulation of other metabolites (including MMDL) in blood. Meal or a dosage form have no significant effect on degree and speed of absorption of a nitsergolin. Nitsergolin it is active (> 90%) contacts proteins of plasma, and degree of his affinity to α1-кислому to a glycoprotein is 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 by kidneys (about 80% of the general dose), and in a small amount (10–20%) – through intestines. 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 was 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 cerebral attack, vascular dementia and a headache caused by a vasospasm);

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


Route of administration and doses:

At chronic disturbances of cerebral circulation, vascular cognitive disturbances, postinsultny states ницерголин назначаютвнутрь on 10 mg 3 times a day. The therapeutic effectiveness of drug develops gradually and the course of treatment has to be not less than 3 months. At vascular dementia use in 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). At acute disorders of cerebral circulation, an ischemic stroke owing to  atherosclerosis, thrombosis and an embolism of cerebral vessels, passing disturbances of cerebral circulation (the tranzitorny ischemic attacks, hypertensive cerebral crises) it is preferable to begin a course of treatment with parenteral administration of drug, then to continue administration of drug inside. At disturbances of peripheric circulation ницерголин appoint внутрьпо 10 mg 3 times a day  during a long span (up to several months). Patients with a renal failure (serumal creatinine ≥ 2 mg/dl) are recommended to apply Sermion® in lower therapeutic doses.


Features of use:

In therapeutic doses of Sermion®, as a rule, does not influence the ABP, however it can cause his gradual decrease in patients with 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 treatment and expediency of its continuation. Influence on ability to drive the car and other mechanisms In spite of the fact that Sermion® 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:

The expressed lowering of arterial pressure (ABP), in the main ambassador of parenteral administration, dizziness, the dispeptic phenomena, a sensation of discomfort in a stomach, skin rashes, feeling of heat, drowsiness or sleeplessness. Increase in concentration of uric acid in blood is possible, and this effect does not depend on a dose and duration of therapy.


Interaction with other medicines:

Сермион® can strengthen action of antihypertensives. Сермион®метаболизируется under the influence of CYP2D6 isoenzyme therefore it is impossible to exclude a possibility of its interaction with drugs which are metabolized with the participation of the same enzyme. At use of a nitsergolin with acetylsalicylic acid, increase in a bleeding time is possible.


Contraindications:

Recently postponed myocardial infarction, acute bleeding, vyrazhennayabradikardiya, disturbance of orthostatic regulation, hypersensitivity to a nitsergolin or other components of drug, deficit of invertase/isomaltase, intolerance of fructose, glyukozo-galaktozny malabsorption, age up to 18 years, pregnancy, the breastfeeding period.


Overdose:

Symptoms: the passing expressed decrease in the ABP. Special treatment usually is not required, the patient has enough to accept horizontal position for several minutes. In exceptional cases at sharp disturbance of blood supply of a brain and heart introduction of sympathomimetic means under constant control of the ABP is recommended.


Storage conditions:

At a temperature not above 25 °C.


Issue conditions:

According to the recipe


Packaging:

- tablets, coated 5 mg: on 15 tablets in the blister (PVC / ПВДХ-алюминиевая foil/PVDH). On 2 blisters together with the application instruction place in a cardboard pack.

- tablets, coated 10 mg: on 25 tablets in the blister (PVC / ПВДХ-алюминиевая foil/PVDH). On 2 blisters together with the application instruction place in a cardboard pack.

- tablets, coated 30 mg. On 15 tablets in the blister (PVC / ПВДХ-алюминиевая foil/PVDH). On 2 blisters together with the application instruction place in a cardboard pack.



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