Sergolin

Sergolin is a medication that affects the functioning of the cardiovascular system. It belongs to the group of peripheral vasodilators.

Indications Sergolina

It is used for therapy in the following conditions:

• Alzheimer's disease, which is moderate or mild;
• vascular dementia;
• cognitive impairment of a presenile or senile nature, which is accompanied by a deterioration in intellectual abilities, behavioral and emotional disorders, a deterioration in the ability to concentrate, mood lability, a feeling of fatigue, dizziness, and in addition cochlear and vestibular disorders (tinnitus and hearing impairment);
• peripheral circulatory disorders (Raynaud's syndrome).

Release form

The medicine is released in tablets, in the amount of 14 pieces inside a blister pack; a box contains 2 or 4 such packs.

Pharmacodynamics

Nicergoline is a semi-synthetic derivative of ergot alkaloids; it has the ability to penetrate into the central nervous system. This component has an antiaggregatory, vasodilatory and α-adrenolytic effect, and in addition, it helps improve metabolic processes within the central nervous system.

Nicergoline helps improve the dynamics of peripheral and cerebral blood circulation and enhances it, and at the same time weakens vascular resistance. It also reduces blood viscosity, slowing down platelet aggregation, reduces the formation of microthrombi and helps improve oxygen transport processes, especially within brain tissue.

The drug has a number of neuropharmacological properties. It potentiates the capture and utilization of glucose, and along with this, the processes of biosynthesis of nucleic acids with proteins inside brain tissues; in addition, it affects the systems of various mediators and transformation mechanisms. Nicergoline improves cholinergic activity of the brain, enhances the transformation of dopamine, especially inside the mesolimbic areas (modulating dopamine endings), and at the same time improves the mechanisms of signal transmission through cells (potentiates the transformation of phosphoinositide, and also increases the translocation of calcium-dependent isoforms of protein kinase type C inside membrane sections).

Impact on mental activity.

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

In individuals with moderate dementia of various origins (vascular dementia or Alzheimer's disease), long-term therapy using Sergolin (over 2-6 months) causes positive changes in bioelectrical brain activity.

Pharmacokinetics

Nicergoline is absorbed almost completely and at a high rate (90-100%) after consumption, and also undergoes significant presystemic metabolism. The most important metabolic products of nicergoline, formed during presystemic metabolism, are the components of MMDL, as well as 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 effect on the expression and rate of absorption.

More than 90% of the substance is synthesized with protein (mostly with glycoproteins). Plasma glycoprotein values increase with age, and also due to acute inflammation caused by malignant tumors or stress. Such conditions lead to a decrease in the plasma level of nicergoline.

Approximately 90% of the used portion undergoes metabolic processes - mainly demethylation and hydrolysis. Demethylation 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. Nicergoline and MMDL have a high elimination rate (half-life of 2.5 hours for nicergoline and 2-4 hours for MMDL), while MDL is excreted more slowly (half-life of about 10-12 hours).

Dosing and administration

The standard adult dose is 30 mg of nicergoline taken once a day. The dosage can be increased to 60 mg, taken twice a day (this is the maximum permissible adult dose) – in the morning and in the evening. When taking the drug in a single dose per day (30 mg), it must be taken in the morning.

The drug effect develops only with prolonged therapy, which is why treatment cycles using drugs are quite long. The evaluation of the therapy results occurs once every six months - at the end of this period, the doctor must evaluate the feasibility of further treatment.

People with kidney problems need to reduce the dosage of Sergolin.

The tablets are taken before meals; they should not be chewed, but swallowed with plain water. If problems with the digestive process occur, the medicine can be taken with food.

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Use Sergolina during pregnancy

The use of Sergolin during pregnancy is prohibited, because there is insufficient experience with therapy in this category of patients to draw conclusions about its safety.

Nicergoline is able to pass into breast milk, and therefore it is not taken during breastfeeding - because this can lead to the appearance of severe negative symptoms.

Contraindications

Among the contraindications:

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

Side effects Sergolina

Often, negative symptoms are mild and transient.

Redness or burning of the skin, a feeling of apathy or fatigue, dry mouth, tinnitus and dizziness may occur. It is also possible to develop gastrointestinal disorders (vomiting, abdominal pain, nausea, constipation and diarrhea) or sleep disorders, headaches, tachycardia, anxiety or nervousness, and increased heart rate. In addition, ejaculation disorders, orthostatic disorders, a feeling of nasal congestion and increased blood uric acid levels may occur.

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Overdose

In case of intoxication, a decrease in blood pressure is observed.

The drug has no antidote; symptomatic measures are taken.

Interactions with other drugs

Nicergoline potentiates the effects of antihypertensive drugs and anticoagulants taken orally.

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

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

Nicergoline is metabolized by CYP450 2D6. Therefore, the possibility of interaction with medications whose metabolism occurs in a similar way cannot be ruled out:

• analgesic drugs - methadone with pethidine and phenacetin, as well as morphine and tramadol with oxycodone;
• anorexigenic substances - dexfenfluramine with fenfluramine;
• antiarrhythmic drugs – amiodarone together with quinidine and encainide, as well as propafenone and flecainide with mexiletine;
• antihistamine - chlorpheniramine;
• antidepressants - bupropion, fluvoxamine, maprotiline, amitriptyline, as well as doxepin with citalopram and clomipramine; in addition, desipramine, trazodone, escitalopram, minaprine with fluoxetine, moclobemide with imipramine, as well as paroxetine, venlafaxine and nortriptyline with sertraline;
• anticoagulant – ticlopidine;
• antiemetic drugs - ondansetron with metoclopramide;
• antimalarial substance - halofantrine;
• anti-inflammatory drug - celecoxib;
• antihypertensive drugs - prehexilin, alprenolol, mibefradil with carvedilol, bisoprolol, debrisoquine with bufuralol, propranolol with captopril and metoprolol;
• cough suppressants - codeine, and also dextromethorphan with hydrocodone;
• muscle relaxant - cyclobenzaprine;
• antiulcer drugs – cimetidine with ranitidine;
• antiviral drug - ritonavir;
• cytostatics – tamoxifen with doxorubicin;
• antidiabetic drug for oral administration - phenformin;
• antimycotic – terbinafine;
• local anesthetic - lidocaine;
• neuroleptics - haloperidol with risperidone, as well as fluphenazine with clozapine, perphenazine with chlorpromazine and levomepromazine with thioridazine;
• eye drops - thymol;
• psychostimulant – donepezil.

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

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Storage conditions

Sergolin should be kept in a place closed to children and sunlight. Temperature values are maximum 25°C.

Shelf life

Sergolin can be used within 36 months from the date of release of the drug.

Application for children

There is no information on the medicinal efficacy and safety of the drug when used in pediatrics, which is why it is not prescribed to children.

Analogues

Analogues of the drug include such products as Nicergoline, Niceromax and Nicerium with Sermion.