Nitsergoline, 10 mg 30 pcs

Pharmacotherapeutic group: alpha-adrenoblocker.

ATX code: CO4AE02

Pharmacological properties:

Pharmacodynamics:

Nicergoline is an ergoline derivative, improves metabolic and hemodynamic processes in the brain, reduces platelet aggregation and improves hemorheological blood parameters, increases blood flow rate in the upper and lower extremities. Nitsergoline exhibits alpha-1-adrenoblocking effect that leads to improved blood flow and has a direct effect on cerebral neurotransmitter systems – noradrenergic, dopaminergic and acetylcholinergic. Against the background of using the drug the activity of noradrenergic, dopaminergic and acetylcholinergic cerebral systems increases, which promotes optimization of cognitive processes.

As a result of long-term therapy with nicergolin there is a steady improvement in cognitive function and reduction of behavioral disorders associated with dementia.

Pharmacokinetics:

After oral administration, nicergoline is quickly and almost completely absorbed. The main products of metabolism of nicergoline are 1,6-dimethyl-8β-hydroxymethyl-10α-methoxyergoline (MMDL, hydrolysis product) and 6-methyl-8β-hydroxymethyl-10α-methoxyergoline (MDL, dimethylation product under the action of CYP2D6 isoenzyme). The ratio of the area under the concentration-time curve (AUC) for MMDL and MDL when nicergoline is taken orally indicates marked metabolism “at first passage” through the liver. After oral administration of 30 mg of nicergoline, maximum concentrations of MMDL
(21±14 ng/mL) and MDL (41±14 ng/mL) were reached after approximately 1 and 4 hours, respectively, and then MDL concentrations declined with a half-life of 13 to 20 hours. Studies confirm the absence of accumulation of other metabolites (including MMDL) in the blood. Food intake or dosage form has no significant effect on the degree and rate of absorption of nicergoline.

Nicergoline actively (>90%) binds to plasma proteins, with a greater degree of affinity for α1-acid glycoprotein 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 are linear and do not vary with the age of the patient.

Nicergoline is excreted in the form of metabolites, mainly by the kidneys (about 80% of the total dose), and in small amounts (10-20%) – through the intestine. In patients with severe renal insufficiency, there is a significant decrease in the degree of excretion of metabolites with urine compared to patients with normal renal function.

Indications

Symptomatic therapy of cognitive disorders, including dementia in chronic cerebrovascular and organic brain lesions accompanied by decreased memory, concentration, thinking, activity, increased fatigability, emotional disorders.

Note: Before starting therapy with nicergolin it is necessary to make sure that these symptoms are not a manifestation of another disease (such as internal diseases, psychiatric or neurological diseases) and do not require specific therapy.

Active ingredient

Nitsergoline

Composition

Composition per tablet:

Active substance:

Nicergoline (in terms of 100% substance) – 10.0 mg.

Excipients: potato starch – 26.9 mg, colloidal silica – 2.0 mg, magnesium stearate – 1.1 mg, lactose monohydrate – until making an uncoated tablet weighing 110.0 mg.

Shell excipients up to 180.0 mg coated tablet: sucrose – 48.1159 mg, magnesium carbonate (light) – 19.8800 mg, povidone K-17 – 1.0000 mg, beeswax – 0.3880 mg, titanium dioxide – 0.3036 mg, talc – 0.2990 mg, colloidal silicon dioxide – 0.0135 mg.

How to take, the dosage

Oral. Tablets should be taken with meals, with a small volume of liquid, without chewing. The recommended daily dose is 30-60 mg, depending on the severity of the symptoms and the individual patient’s response to treatment. The daily dose of 30 mg is recommended to be taken at breakfast. Patients with impaired renal function (serum creatinine ≥2 mg/dL) are recommended to use nicergolin in lower therapeutic doses.

Interaction

Nitsergoline may increase the effect of hypotensive drugs.

Nitsergoline is metabolized by CYP2D6 isoenzyme, so we cannot rule out the possibility of its interaction with drugs that are metabolized with the participation of the same enzyme.

When using nitsergoline with acetylsalicylic acid, you may increase bleeding time.

Nitsergoline affects the metabolism and excretion of uric acid, and therefore caution should be exercised when using it with drugs that affect uric acid metabolism.

Nitsergoline potentiates the effect of beta-adrenoblockers on the heart.

Nitsergoline has antagonistic action in relation to the vasoconstrictor effect of sympathomimetics through its alpha-adrenoblocking effect.

Special Instructions

In clinical studies, it has been shown that single or repeated use of nicergolin can decrease systolic and to a greater extent diastolic blood pressure in patients with normal and elevated blood pressure. These results may vary because other studies have shown no change in blood pressure values.

The drug works gradually, so it should be taken over a long period of time, with the physician periodically (at least every 6 months) evaluating the effect of treatment and whether it should be continued.

The development of fibrosis (e.g., pulmonary, cardiac, heart valve, and retroperitoneal) has been associated with the use of ergot alkaloids with antagonistic activity to 5HT2β serotonin receptors.
Symptoms of ergotism (including nausea, vomiting, diarrhea, abdominal pain, and peripheral vasoconstriction) have been reported with some ergot alkaloids and their derivatives.
Clinicians should be aware of the possible symptoms of ergot overdose before prescribing this class of drugs.

Impact on ability to drive and operate machinery:

While nicergoline improves reaction and concentration, its effects on the ability to drive and operate complex machinery have not been specifically studied. In any case, caution should be exercised given the nature of the underlying disease, especially given that dizziness or drowsiness may develop in some cases.

Synopsis

Round, biconvex tablets, coated with a white or almost white coating; two layers are visible on the cross section: a white or almost white core and a white or almost white coating.

Contraindications

Recent myocardial infarction, acute bleeding, marked bradycardia, orthostatic dysregulation, hypersensitivity to nicergoline, other ergotamine derivatives or other drug components, sucrose/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption, age under 18, pregnancy, breastfeeding.

With caution:
Hyperuricemia or gout in the history and/or in combination with drugs that impair uric acid metabolism or excretion.
Concurrent use with sympathomimetic agonists (alpha- and beta-).

Side effects

.

.

.p> * Adverse reactions identified during post-registration use of nicergoline.
An association has been noted with the development of fibrosis (e.g., pulmonary, cardiac, heart valve, and retroperitoneal) when using ergot alkaloids that have antagonistic activity to 5HT2β serotonin receptors.

Overdose

Symptoms: transient marked decrease in BP. No special treatment is usually required, the patient only needs to take a horizontal position for a few minutes. In exceptional cases with acute impairment of blood supply to the brain and heart it is recommended to administer sympathomimetic drugs under constant control of blood pressure.

Pregnancy use

Due to the lack of special studies, nicergolin is contraindicated during pregnancy. Breastfeeding should be avoided while taking the drug, since nicergolin and its metabolic products penetrate into the mother’s milk. No effect of nicergolin on fertility has been observed in animal studies.

Similarities

Sermion, Nitsergoline