Components:
Method of action:
Treatment option:
Medically reviewed by Militian Inessa Mesropovna, PharmD. Last updated on 26.03.2022
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Ceborin
Nicergoline
acute and chronic cerebral metabolic and vascular disorders (due to atherosclerosis, arterial hypertension, thrombosis or embolism of the brain vessels, including transient ischemic attack, vascular dementia and headache caused by vasospasm),
acute and chronic peripheral metabolic and vascular disorders (organic and functional limb arteriopathies, Raynaud's disease, syndromes caused by peripheral blood flow disorders),
as an additional tool in the treatment of hypertensive crises.
acute and chronic cerebral metabolic and vascular disorders (due to atherosclerosis, arterial hypertension, thrombosis or embolism of the brain vessels, including transient cerebral attack, vascular dementia and headache caused by vasospasm),
acute and chronic peripheral metabolic and vascular disorders (organic and functional limb arteriopathies, Raynaud's disease, syndromes caused by peripheral blood flow disorders),
as an additional means in the treatment of hypertensive crises (parenterally).
acute and chronic cerebral metabolic and vascular disorders (due to atherosclerosis, arterial hypertension, thrombosis or embolism of the brain vessels, including transient ischemic attack, vascular dementia and headache caused by vasospasm),
acute and chronic peripheral metabolic and vascular disorders (organic and functional limb arteriopathies, Raynaud's disease, syndromes caused by peripheral blood flow disorders),
as an additional tool in the treatment of hypertensive crises.
Coated tablets
Inside.
Chronic disorders of cerebral circulation, vascular cognitive disorders, post-stroke conditions: nicergoline is prescribed at a dose of 10 mg 3 times a day. The therapeutic effectiveness of the drug develops gradually, and the course of treatment should be at least 3 months.
Vascular dementia: the use of 30 mg 2 times a day is indicated (at the same time, every 6 months it is recommended to consult a doctor about the feasibility of continuing therapy).
Acute disorders of cerebral circulation, ischemic stroke due to atherosclerosis, thrombosis and cerebral embolism, transient disorders of cerebral circulation (transient ischemic attacks, hypertensive cerebral crises): it is preferable to start the course of treatment with parenteral administration of the drug, then continue taking the drug orally.
Peripheral circulatory disorders: nicergoline is prescribed orally at 10 mg 3 times a day for a long period of time (up to several months).
Lyophilizate for preparation of solution for injection
In/m. 2-4 mg (2-4 ml) 2 times a day.
V/v, by slow infusion. 4-8 mg in 100 ml of 0.9% sodium chloride solution or 5-10% dextrose solution, as prescribed by a doctor, this dose can be administered several times a day.
In/a. 4 mg in 10 ml of 0.9% sodium chloride solution, the drug is administered for 2 minutes.
The reconstituted solution is recommended to be used immediately after preparation.
The dose, duration of therapy and method of administration depend on the nature of the disease. In some cases, it is preferable to start therapy with parenteral administration, and then switch to taking the drug orally for maintenance treatment.
Special patient groups
Impaired renal function (serum creatinine ≥2 mg/dl). Ceborin® it is recommended to use in lower therapeutic doses.
hypersensitivity to nicergoline or other components of the drug,
recent myocardial infarction,
bleeding,
severe bradycardia,
orthostatic hypotension,
galactose intolerance,
lactose deficiency or glucose-galactose malabsorption,
pregnancy,
breastfeeding,
children under 18 years of age (due to lack of data).
With caution - a history of hyperuricemia or gout in combination with drugs that interfere with the metabolism or excretion of uric acid.
Common for all dosage forms
hypersensitivity to nicergoline and / or other components of the drug,
acute bleeding,
acute myocardial infarction,
orthostatic hypotension,
severe bradycardia.
Optional for coated tablets
sucrose/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption,
pregnancy,
breastfeeding period,
age up to 18 years.
With caution: hyperuricemia or gout in the anamnesis and / or in combination with drugs that interfere with the metabolism or excretion of uric acid.
hypersensitivity to Ceborin or other components of the drug,
recent myocardial infarction,
bleeding,
severe bradycardia,
orthostatic hypotension,
galactose intolerance,
lactose deficiency or glucose-galactose malabsorption,
pregnancy,
breastfeeding,
children under 18 years of age (due to lack of data).
With caution - a history of hyperuricemia or gout in combination with drugs that interfere with the metabolism or excretion of uric acid.
Rarely-a marked decrease in blood pressure, mainly after parenteral administration, dizziness, dyspeptic phenomena, a feeling of discomfort in the abdomen, skin rashes, a feeling of heat, drowsiness or insomnia. It is possible to increase the concentration of uric acid in the blood, and this effect does not depend on the dose and duration of therapy. Side effects are usually mild or moderate.
Symptoms: transient marked decrease in blood pressure.
Treatment: special treatment is usually not required, the patient only needs to take a horizontal position for a few minutes. In exceptional cases, with a sharp violation of the blood supply to the brain and heart, it is recommended to administer sympathomimetic agents under constant control of blood pressure.
Nicergoline-a derivative of ergoline-improves metabolic and hemodynamic processes in the brain, reduces platelet aggregation and improves blood hemorheological parameters, increases the speed of blood flow in the upper and lower extremities, shows alpha1- adrenoblocking effect. In patients with arterial hypertension, it can cause a gradual moderate decrease in blood pressure.
Nicergoline-a derivative of ergoline, improves metabolic and hemodynamic processes in the brain, reduces platelet aggregation and improves blood hemorheological parameters, increases the speed of blood flow in the upper and lower extremities. Nicergoline exhibits α1- adrenoblocking effect, leading to improved blood flow, and has a direct effect on the cerebral neurotransmitter systems — adrenergic, dopaminergic and cholinergic. Against the background of the use of the drug, the activity of the adrenergic, dopaminergic and cholinergic cerebral systems increases, which contributes to the optimization of cognitive processes. As a result of long-term therapy with nicergoline, a persistent improvement in cognitive functions and a decrease in the severity of behavioral disorders associated with dementia were observed.
Ceborin-a derivative of ergoline-improves metabolic and hemodynamic processes in the brain, reduces platelet aggregation and improves blood hemorheological parameters, increases the speed of blood flow in the upper and lower extremities, shows alpha1- adrenoblocking effect. In patients with arterial hypertension, it can cause a gradual moderate decrease in blood pressure.
The main products of nicergoline metabolism are 1,6-dimethyl-8β-hydroxymethyl-10α-methoxyergoline (MMDL, a product of hydrolysis) and 6-methyl-8β-hydroxymethyl-10α-methoxyergoline (MDL, a product of dimethylation under the action of CYP2D6). Nicergoline is actively (>90%) bound to plasma proteins, and the degree of its affinity for alpha1- more acidic glycoprotein than serum albumin. It has been shown that nicergoline and its metabolites can be distributed in blood cells. The pharmacokinetics of nicergoline is linear and does not change depending on the age of the patient. Nicergoline is excreted in the form of metabolites, mainly through the kidneys (approximately 80% of the total dose) and in small amounts (10-20 %) - through the intestines. In patients with severe renal insufficiency, there was a significant decrease in the degree of excretion of metabolic products in the urine compared to patients with normal renal function.
After oral administration, nicergoline is rapidly and almost completely absorbed. The main products of nicergoline metabolism: 1,6-dimethyl-8β-hydroxymethyl-10α-methoxyergoline (MMDL, hydrolysis product) and 6-methyl-8β-hydroxymethyl-10α-methoxyergoline (MDL, the product of demethylation under the action of the CYP2D6 isoenzyme). Ratio of AUC values for MMDL and MDL when taken orally and in / in the administration of nicergoline indicates a pronounced metabolism at the first pass. After taking 30 mg of nicergoline orally CmaxMMDL — (21±14) ng / ml and MDL — (41±14) ng / ml, Tmax — 1 and 4 hours, respectively, then the concentration MDL decreased from T1/2 13-20 hours. Studies confirm the absence of accumulation of other metabolites (including MMDL) in the blood. Food intake or dosage form does not significantly affect the degree and rate of absorption of nicergoline. Nicergoline is actively (>90%) bound to plasma proteins, and the degree of its affinity for the alpha-acid of the glycoprotein is greater than for serum albumin. It has been shown that nicergoline and its metabolites can be distributed in blood cells. The pharmacokinetics of nicergoline at doses up to 60 mg is linear and does not change depending on the age of the patients.
Nicergoline is excreted in the form of metabolites, mainly in the urine (approximately 80% of the total dose), and in small amounts (10-20%) - with feces. In patients with severe renal insufficiency, there was a significant decrease in the degree of excretion of metabolic products in the urine compared to patients with normal renal function.
The main products of Ceborin metabolism are 1,6-dimethyl-8β-hydroxymethyl-10α-methoxyergoline (MMDL, a product of hydrolysis) and 6-methyl-8β-hydroxymethyl-10α-methoxyergoline (MDL, a product of dimethylation under the action of CYP2D6). Ceborin is actively (>90%) bound to plasma proteins, and the degree of its affinity for alpha1- more acidic glycoprotein than serum albumin. It has been shown that Ceborin and its metabolites can be distributed in blood cells. The pharmacokinetics of Ceborin are linear and do not change depending on the age of the patient. Ceborin is excreted in the form of metabolites, mainly through the kidneys (approximately 80% of the total dose) and in small amounts (10-20 %) - through the intestines. In patients with severe renal insufficiency, there was a significant decrease in the degree of excretion of metabolic products in the urine compared to patients with normal renal function.
- Alpha-blocker [Alpha-blockers]
- Alpha-adrenoblocker [Correctors of cerebral circulatory disorders]
Increases the effect of antihypertensive drugs. Nicergoline is metabolized under the action of CYP2D6, so it is impossible to exclude the possibility of its interaction with drugs that are metabolized with the participation of the same enzyme.
Ceborin® may increase the effect of antihypertensive agents.
Ceborin® it is metabolized under the action of the isoenzyme CYP2D6, so it is impossible to exclude the possibility of its interaction with drugs that are metabolized with the participation of the same enzyme.
When using nicergoline with acetylsalicylic acid, it is possible to increase the bleeding time.
Increases the effect of antihypertensive drugs. Ceborin is metabolized under the action of CYP2D6, so it is impossible to exclude the possibility of its interaction with drugs that are metabolized with the participation of the same enzyme.
