Nicheromax lyophilizate for a solution of 4 mg of No. 4

NICEROMAX instructions for use

Composition

active ingredient: nicergoline; 1 bottle contains 4 mg of nicergoline;
excipients: lactose, acid should.

Dosage form

Lyophilizate for solution for injection.

Pharmacological group

Peripheral vasodilators. Alkaloids of ergot. The code of automatic telephone exchange С04А Е02.

Indications

Acute and chronic cerebrovascular disorders of metabolism due to atherosclerosis, thrombosis and embolism of cerebral vessels, transient disorders of cerebral circulation (transient ischemic attacks).

Headache.

Additional therapy for the treatment of hypertension.

Additional therapy for hypertensive crisis.

Contraindications

Hypersensitivity to the active substance, ergot alkaloids or to any component of the drug. Recently suffered myocardial infarction, acute bleeding, orthostatic hypotension, severe bradycardia. Simultaneous reception of sympathomimetics (alpha or beta receptor agonists).

Dosing and Administration

Intramuscular injections of 2-4 mg (2-4 ml) twice a day (lyophilizate diluted with water for injection or physiological saline solution to 2-4 ml).

Slow infusion of 4-8 mg dissolved in 100 ml of 0.9% sodium chloride solution or 5% glucose solution. According to the doctor's decision, the dose can be reused during the day.

If necessary, the drug can be used intraarterially: 4 mg dissolved in 10 ml of 0.9% sodium chloride solution, slowly, for 2 or more minutes.

The dose, duration of treatment and the route of administration depend on the severity of the clinical manifestations of the disease. In some cases, it is advisable to begin treatment with the introduction of the drug parenterally, and then switch to oral administration.

Patients of advanced age. According to the results of pharmacokinetic studies and drug tolerability studies, elderly patients do not need to adjust the dosage.

Adverse Reactions

Rarely were reported the following non-tapering side effects.

From the digestive tract: constipation, nausea, vomiting, increased acidity of gastric juice, diarrhea, abdominal pain.

From the cardiovascular system: arterial hypotension, dizziness, attacks of stenocardia, cold extremities, tachycardia.

From the nervous system: dizziness, headache, confusion, drowsiness, insomnia, agitation.

Allergic reactions: angioedema, itching, skin rashes.

Reproductive disorders in men with ejaculation disorder.

General disorders: sensation of fever, hot flashes, sweating, pain in the limbs, fever.

During clinical trials, there was an increase in the level of uric acid in the blood, which did not depend on the prescribed dose and on the duration of treatment.

Overdose

When using nicergoline in high doses, there may be a temporary decrease in blood pressure. Special treatment is usually not required, it is enough to put the patient in a prone position. In exceptional cases of insufficiency of blood supply to the brain and heart, sympathomimetics and constant monitoring of arterial pressure indices are recommended.

Use during pregnancy and lactation

Toxicological studies have not revealed a teratogenic effect of nicergoline. Given the indications of the drug Niteromax, its administration to pregnant women and women breastfeeding is unlikely. If the indication for the purpose of treatment is justified treatment should start only after assessing the ratio of "risk / benefit."

It is unknown, penetrates nicergoline into breast milk, so Nitzeromax should not be used breast-feeding.

Children

The drug should not be used in pediatric practice.

Application features

In total, at recommended therapeutic doses, Niteromax does not cause changes in blood pressure. In patients prone to hypertension, the drug can gradually reduce the level of blood pressure.

At the beginning of treatment, orthostatic hypotension may develop.

The drug should be used with caution in patients with angina pectoris and severe atherosclerosis.

Nicergoline should be administered with caution to patients with hyperuricemia or gout in history or in the treatment of drugs that affect metabolism and excretion of uric acid.

Since approximately 80% of nicergoline metabolites are excreted in the urine, it is desirable to reduce the dose to patients with impaired renal function (serum creatinine ≥ 2 mg / dL or 175 mmol / l).

For the duration of the drug should refrain from drinking alcohol.

The onset of fibrosis (eg, fibrosis of the lungs, heart, heart valves and retroperitoneal fibrosis) was associated with the use of certain ergot alkaloids with agonist activity up to 5-HT serotonin receptors.

It has been reported that symptoms of ergotism (including nausea, vomiting, diarrhea, abdominal pain and narrowing of peripheral vessels) occur with the use of certain ergot alkaloids and their derivatives.

Before prescribing this class of medicines, doctors should familiarize themselves with the signs and symptoms of a horn overdose.

The ability to influence the reaction rate when driving vehicles or other mechanisms

Although the clinical effects of Nitzeromax aimed at improving care and concentration, the effect of taking the drug on the reaction rate when driving or working with other mechanisms has not been investigated.

In any case, care must be taken, taking into account the underlying disease of the patient and bearing in mind that sometimes dizziness and fatigue can occur when the drug is used, especially at the beginning of the application.

Interaction with other drugs and other interactions

Use with caution with:

• antihypertensives (Nicheromax may enhance their effects);
• drugs are also metabolized by the cytochrome P450 2D6 system, because it is impossible to exclude interaction with these agents (such as quinidine, most antipsychotics, including clozapine, risperidone, haloperidol, thioridazine);
• acetylsalicylic acid (bleeding time may be prolonged);
• drugs that affect the metabolism of uric acid (can change metabolism and excretion of uric acid).

Nitzeromax can not be used simultaneously with the drugs that excite the central nervous system, α- and β-adrenomimetics. Since nicergoline increases the effect of anticoagulants and antiplatelet agents, when combined with Nicergoline, it is necessary to control the parameters of blood coagulation.

The drug may enhance the effects of cholinomimetic drugs.

Nicergoline can enhance the effect of β-blockers on the heart.

Pharmacological properties

Pharmacodynamics.

Nicergoline is a derivative of ergoline with alpha-1-adrenergic blocking activity.

In studies in vitro and in vivo, nicergoline significantly increased the activity of acetylcholinesterase. In these experimental studies, neurochemical effects were observed simultaneously with a steady improvement in behavioral responses, for example, in a test with a labyrinth, in mature animals that used nicergoline for a long time observed the development of reactions similar to those in young animals.

When using nicergoline in animals, it was also possible to reduce the manifestations of cognitive deficiency, which was induced by several agents (hypoxia, electroconvulsive therapy (ECT), scopolamine).

Nicergoline also increases the activity and transfer to the site of the membrane of calcium-dependent protein kinase C isoforms. These enzymes are involved in the secretion of the soluble amyloid precursor protein, which leads to increased release and a decrease in the production of pathological beta-amyloid, as demonstrated in the culture of human neuroblastoma.

Thanks to the antioxidant effect and the ability to activate detoxification enzymes, nicergoline prevents the death of nerve cells caused by oxidative stress and apoptosis in in vitro and in vivo experimental models. Nicergoline reduces the age-related decrease in mRNA expression of neuronal nitric oxide synthase, and can also affect the improvement of cognitive function.

Pharmacokinetics.

Nicergoline rapidly hydrolyzed as a result of binding by ethers after administration, which leads to the formation of 1,6-dimethyl-8b-hydroxymethyl-10a-methoxyergoline (MMDL). The following biotransformation leads to the formation of a metabolite of 6-methyl-8b-hydroxymethyl-10a-methoxyergoline (MDL).

The distribution of the drug in the tissues is rapid and wide, which is reflected by a short phase of the distribution of radioactivity in blood serum. The volume of distribution of nicergoline is high enough (> 105 L), which is possibly due to metabolism in the blood and distribution in blood cells and / or tissues. Nicergoline in a significant amount binds to human blood plasma proteins, with a greater affinity for a-acid glycoprotein than for serum albumin.

Excretion in the urine is the main way of excretion, since 80% of the total dose of nicergoline, labeled with a radioactive isotope, is detected in urine and only 10-20% in feces.

In patients with severe renal dysfunction, there is a significant decrease in MDL secretion in the urine. In the secondary metabolic pathway, 1-dimethyl-nicergoline is formed by demethylation (1-DN), which is then metabolized to MDL by hydrolysis of ester bonds.

Basic physical and chemical properties:

lyophilized white porous mass or white powder.

Incompatibility

Do not mix with other medicines. Use only recommended solvents.

Shelf life

2 years.

Storage conditions

Store in the original packaging at a temperature not higher than 25 ° C. Keep out of the reach of children.

Packaging

For 1 or 4 vials with lyophilizate in a contiguous cell package, 1 contour squamute in a cardboard bundle.

Category of leave

On prescription.