Sergolin

Sergolin is a drug that affects the work of the CAS. Included in the group of peripheral vasodilators.

Indications Sergolina

It is used for therapy in such conditions:

• Alzheimer's disease, with moderate or mild severity;
• vascular dementia;
• cognitive impairment of the presenile or senile nature, against which there is a deterioration of intellectual abilities, behavioral as well as emotional disorders, deterioration of the ability to concentrate, mood lability, fatigue, dizziness, and in addition, cochlear and vestibular disorders (ear ring and auditory frustration) ;
• disturbances of peripheral circulation processes (Raynaud's syndrome).

Release form

The release of the drug produced in tablets, in the amount of 14 pieces inside a blister pack; The box contains 2 or 4 of these packages.

Pharmacodynamics

Nicergoline is a semi-synthetic derivative of ergot alkaloids; has the ability to pass inside the central nervous system. This component has anti-aggregation, vasodilator and α-adrenolytic effect, and in addition contributes to the improvement of metabolic processes within the central nervous system.

Nicergoline helps to improve the dynamics of peripheral as well as cerebral circulation and strengthens it, and at the same time weakens vascular resistance. It also reduces blood viscosity, slowing down platelet aggregation, reduces the formation of microthrombus, and contributes to the improvement of the movement of oxygen, especially within the brain tissue.

The medication has a number of neuropharmacological properties. It potentiates the capture and utilization of glucose, and with it the processes of biosynthesis of nucleic acids with proteins within the brain tissue; besides it influences systems of various mediators and transformation mechanisms. Nicergoline helps to improve the cholinergic activity of the brain, enhances the transformation of dopamine, especially within the mesolimbic regions (modulating dopamine endings), and at the same time improves the mechanisms of signal transmission through cells (potentiates the conversion of phosphoinositide, and also increases the translocation of calcium-dependent protein kinase isoforms within the membrane departments).

Impact on mental activity.

Nicergoline stabilizes electroencephalography readings in both elderly and younger patients with hypoxia. The substance increases α- and β-activity, and with it reduces δ- and τ-activity.

In individuals with moderate dementia of various origins (vascular dementia or Alzheimer's disease), prolonged therapy using Sergolin (for 2-6 months) causes positive changes in the bioelectric cerebral activity of the brain.

Pharmacokinetics

Nicergoline consumed is absorbed almost completely and at a high speed (by 90-100%) and also undergoes a significant presystemic metabolism. The most important metabolic products of nicergoline, which are formed during the presystemic metabolism, are the components of MDL and MDL. Plasma Cmax of the drug is noted after 1-1.5 hours, MMDL - after 60 minutes, and MDL - after 4 hours. Food products do not have a significant impact on the severity and rate of absorption.

More than 90% of the substance is synthesized with protein (most of it with glycoproteins). Plasma values of glycoproteins increase with age, and in addition, due to acute inflammation caused by malignant tumors or stress. Similar conditions lead to a decrease in nicergoline plasma levels.

Approximately 90% of the used portion undergoes metabolic processes - to a greater extent desmethylation and hydrolysis. Desmethylation occurs indirectly due to the catalytic effect of the enzyme CYP2D6.

Approximately 80% of the active element and its metabolic products are excreted in the urine, and the remainder in the feces. Nicergolin and MMDL have a high elimination rate (half-life is 2.5 hours for nicergolin and 2-4 hours for MMDL), while MDL is excreted more slowly (half-life is about 10-12 hours).

Dosing and administration

The size of a standard adult portion is 30 mg of nicergoline 1 times per day. You can increase the dosage to 60 mg, with a 2-time use per day (this is the maximum allowable adult portion) - in the morning and in the evening. When using drugs in 1-fold dosage per day (30 mg), it must be taken in the morning.

Drug exposure develops only with prolonged therapy, because of which the treatment cycles with the use of drugs are quite long. Evaluation of the results of therapy occurs 1-fold in the first half of the year - at the end of this period, the doctor must evaluate the feasibility of subsequent treatment.

People with disorders in the kidneys need to lower the dosage of Sergolin.

The use of pills occurs before meals; they should not be chewed, but swallowed, washed down with plain water. In case of problems with the digestive process, it is allowed to take the medicine with food.

[2]

Use Sergolina during pregnancy

The use of Sergolin during pregnancy is prohibited, because the experience of therapy in this category of patients is not enough to draw conclusions about its safety.

Nicergolin is able to pass into the mother's milk, and therefore it is not taken when breastfeeding - because this can lead to the appearance of severe negative symptoms.

Contraindications

Among the contraindications:

• the presence of strong sensitivity with respect to the active drug element or its other components;
• porphyria;
• acute bleeding;
• exertional angina;
• recent myocardial infarction;
• bradycardia, which is pronounced (heart rate is <50 beats / minute);
• significantly lower blood pressure values;
• severe atherosclerosis.

Side effects Sergolina

Often, negative signs have a mild severity and are transient.

There may appear redness or burning sensation on the skin, a feeling of apathy or fatigue, dryness of the oral mucosa, ear ringing and dizziness. It is also possible the development of disorders of the gastrointestinal tract (vomiting, abdominal pain, nausea, constipation and diarrhea) or sleep, headaches, tachycardia, anxiety or nervousness, as well as increased heart rate. In addition, ejaculatory disorders, orthostatic disturbances, a feeling of nasal congestion and uric acid blood values may occur.

[1]

Overdose

With intoxication, a decrease in blood pressure indicators.

The drug does not have an antidote; symptomatic events are being held

Interactions with other drugs

Nicergolin potentiates the effects of antihypertensive drugs and anticoagulants for oral administration.

It is forbidden to combine the drug with α- or β-blockers.

Combination with sympathomimetics can lead to significant fluctuations in blood pressure.

Nicergoline metabolism occurs with the participation of CYP450 2D6. Therefore, we can not exclude the possibility of the development of interaction with drugs, whose metabolism is developing in a similar way:

• analgesic drugs - methadone with pethidine and phenacetin, and in addition morphine and tramadol with oxycodone;
• anorectic substances - dexfenfluramine with fenfluramine;
• antiarrhythmic drugs - amiodarone together with quinidine and enkainid, as well as propafenone and flekainid with meksiletin;
• antihistamine - chlorpheniramine;
• antidepressants - bupropion, fluvoxamine, maprotiline, amitriptyline, and in addition doxepin with citalopram and clomipramine; In addition, desipramine, trazodone, escitalopram, minaprine with fluoxetine, moclobemide with imipramine, and paroxetine, venlafaxine and nortriptyline with sertraline;
• anticoagulants - tyclophidins;
• antiemetic drugs - ondansetron with metoclopramide;
• antimalarial substance - halofantrine;
• anti-inflammatory drug celecoxib;
• antihypertensive drugs - prehexylin, alprenolol, mibefradil with carvedilol, bisoprolol, debrisoquine with bufuralol, propranolol with captopril and metoprolol;
• antitussive drugs - codeine, and besides dextromethorphan with hydrocodone;
• miorelaxant - cyclobenzaprine;
• antiulcer drugs - cimetidine with ranitidine;
• antiviral drug - ritonavir;
• cytostatics - tamoxifen with doxorubicin;
• antidiabetic drug for oral administration - phenformin;
• antimycotic - terbinafine;
• local anesthetic - lidocaine;
• antipsychotics - haloperidol with risperidone, flufenazine with clozapine, perphenazine with chlorpromazine and levomepromazine with thioridazine;
• eye drops - a means of thymol;
• psihostimulyator - donepezil.

The antihypertensive effect of nicergoline is potentiated when combined with alcoholic beverages.

[3], [4]

Storage conditions

Sergolin is required to be kept in a place closed from access of children and penetration of sunlight. Temperature values - maximum 25 ° С.

Shelf life

Sergolin can be used within 36 months from the moment of release of the medicine.

Application for children                                  

There is no information about drug efficacy and safety when using drugs in pediatrics, which is why it is not prescribed to children.

Analogs

Analogues of the drug are such means as Nitsergolin, Nitseromaks and Nitserium with Sermion.