Nemotan

Nemotan selectively blocks the action of Ca channels, mainly affecting the vessels. The drug is a derivative of dihydropyridine and contains the component nimodipine.

Nimodipine demonstrates pronounced selective activity in certain areas of the brain. The medicinal effect of the drug develops under the influence of calcium ions - slowing down of contractile processes inside smooth muscle cells.

It has been established that the drug reduces the intensity of memory impairment and helps improve concentration in people with problems in the functioning of the brain.

Indications Nemotana

It is used for the treatment and prevention of neurological disorders of an ischemic nature associated with vascular spasms inside the brain, arising from the development of subarachnoid hemorrhage after the rupture of an aneurysm.

It is prescribed for disorders of brain activity accompanied by intense symptoms in elderly people.

Release form

The medicine is released in tablets - 10 pieces inside a cell package; 3 or 10 packages inside a pack.

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Pharmacodynamics

Nimodipine helps to normalize the work of neurons and protects them from negative influences. At the same time, it has a positive effect on cerebral blood supply and increases tolerance to ischemia, interacting with cerebrovascular and neuronal endings that are associated with Ca channels.

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Pharmacokinetics

The active substance of the drug is almost completely absorbed after oral administration. The values of plasma Cmax, as well as AUC, increase in accordance with the increase in dosage (studies were conducted up to a dose of 90 mg).

The distribution volume (Vss, 2-chamber type) values for intravenous injection are 0.9-1.6 l/kg. The total clearance rate is 0.6-1.9 l/hour/kg.

It is synthesized with blood protein by 97-99%.

Nimodipine excretion is realized during metabolic processes through the structure of hemoprotein P450 3A4.

Intensive presystemic metabolic processes (approximately 85-95%) create bioavailability rates of 5-15%.

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Dosing and administration

Use in disorders of brain function.

Elderly people with such pathologies are required to take 1 tablet of the drug 3 times a day (30 mg of the substance 3 times a day).

For individuals with significantly weakened renal function (the rate of CF is below 20 ml per minute), it is prescribed very carefully, with regular examinations of the patient during therapy.

Therapy and prevention of neurological disorders of ischemic nature associated with cerebral vascular spasms developing due to rupture of an aneurysm with subsequent subarachnoid hemorrhage.

After a course of treatment with infusions, 60 mg of the drug (2 tablets) is taken orally 6 times a day.

If negative symptoms appear, the dosage is reduced or the use of the drug is stopped (if necessary).

Liver problems (especially liver cirrhosis) may increase the bioavailability of the drug due to a decrease in metabolic clearance values and a weakening of primary metabolic processes. In these cases, negative symptoms may increase (for example, a decrease in blood pressure values), so the dosage is reduced or the drug is discontinued.

Combination with substances that induce or inhibit the action of the CYP 3A4 component may require a change in portion size.

The tablets are swallowed whole, without chewing, with plain water. The medicine can be taken without reference to food intake, with at least 4-hour intervals. It is forbidden to drink grapefruit juice during therapy.

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Use Nemotana during pregnancy

There have been no tests performed on the use of the drug during pregnancy. If it is necessary to use it during this period, it is necessary to carefully evaluate the risks and benefits, taking into account the severity of the clinical symptoms.

It has been determined that the values of nimodipine and its metabolic components in mother's milk correspond to plasma values. For this reason, breastfeeding is prohibited during the period of Nemotan use.

Contraindications

Main contraindications:

• use of the drug in case of personal intolerance associated with nimodipine or other components of the drug;
• administration in combination with rifampicin (in such cases, the therapeutic effect of Nemotan is significantly weakened) and anticonvulsants, including phenytoin and phenobarbital with carbamazepine (these substances significantly reduce the level of bioavailability of nimodipine);
• administration to persons with myocardial infarction or unstable angina (also within 1 month from the moment of their development);
• during ongoing therapy for disorders of brain activity;
• liver dysfunction (especially liver cirrhosis), because this may provoke an increase in the bioavailability of nimodipine due to a weakening of metabolic clearance and primary metabolic processes.

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Side effects Nemotana

Side effects include:

• blood and lymphatic disorders: thrombocytopenia or changes in blood laboratory test results;
• immune disorders: allergy symptoms, acute manifestations of intolerance and rashes;
• lesions affecting the nervous system: headaches and cerebrovascular symptoms of a non-specific nature;
• problems with the heart: tachycardia, non-specific types of arrhythmia and bradycardia;
• vascular symptoms: decreased blood pressure, non-specific cardiovascular signs, and vasodilation;
• gastrointestinal disorders: nausea, gastrointestinal dysfunction and intestinal obstruction;
• liver and biliary tract problems: temporary increase in liver enzyme activity and moderate to mild liver-related symptoms.

Adverse reactions found during clinical trials of nimodipine in accordance with the indication for the treatment of disorders in brain function:

• problems with the functioning of the nervous system: vertigo;
• neurological manifestations of a non-specific nature: hyperkinesia, dizziness or tremor;
• cardiac dysfunction: palpitations;
• vascular lesions: swelling or syncope;
• problems with the gastrointestinal tract: diarrhea, bloating or constipation.

Overdose

Acute poisoning with Nemotan causes bradycardia or tachycardia, nausea, a sharp decrease in blood pressure, and gastrointestinal disorders.

In case of acute intoxication, the use of the drug should be stopped immediately. In addition, symptomatic actions are carried out, as well as gastric lavage and administration of activated carbon.

If blood pressure continues to decrease, dopamine or norepinephrine should be administered intravenously. Since the drug has no antidote, symptomatic procedures are performed in the event of other side effects.

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Interactions with other drugs

The processes of nimodipine metabolism are associated with the action of the hemoprotein system P450 ZA4, located inside the liver and intestinal mucosa. Because of this, medications that affect this enzymatic structure are capable of changing the level of drug clearance and its primary metabolic processes.

Experience with other Ca channel antagonists shows that rifampicin can potentiate the metabolic processes of nimodipine because it induces enzyme activity. The combination of these drugs results in a significant weakening of the therapeutic effect of nimodipine, which is why they are not used together.

Anticonvulsants (including phenytoin with phenobarbital and carbamazepine) significantly reduce the bioavailability of Nemotan, which is why it is not used with these substances.

Co-administration with the following agents that inhibit the activity of the hemoprotein P450 3A4 system requires monitoring of blood pressure values and consideration of options for changing the nimodipine dosage, if necessary.

No interaction testing of the drug and macrolides has been performed, but it is known that certain macrolides (for example, erythromycin) are capable of slowing down the effect of hemoprotein P450 3A4, so they may interact with the drug at this stage. Therefore, such a combination cannot be used.

No interaction studies have been performed when the drug is combined with anti-HIV protease inhibitors (e.g. ritonavir). Substances in this category are thought to have a strong inhibitory effect on the hemoprotein P450 3A4. There is a possibility of a significant and clinically important increase in plasma nimodipine levels when administered together with protease inhibitors.

There is no information regarding the effects that develop when using the drug and ketoconazole. There is information that azole antifungals slow down the activity of hemoprotein P450 3A4, and also interact with other dihydropyridine antagonists of Ca channels. Because of this, when combined with nimodipine, a noticeable increase in the level of its overall bioavailability may be observed (due to the weakening of primary metabolic processes).

No testing has been performed on the combined use of the drug and nefazodone. There is evidence that the antidepressant has a strong inhibitory effect on hemoprotein P450 3A4. There is a risk of increasing plasma levels of nimodipine when combined with nefazodone.

Long-term combination of the drug with fluoxetine leads to an increase in plasma nimodipine values by almost 50%. The effectiveness of fluoxetine was significantly weakened, but the effect of its active metabolic element norfluoxetine was not.

Use of the drug together with dalfopristin or quinupristin causes an increase in plasma levels of nimodipine.

The introduction of Nemotan together with the H2-termination antagonist cimetidine or valproic acid causes an increase in plasma values of the drug.

Long-term combination of the drug and nortriptyline slightly increases plasma levels of nimodipine (while nortriptyline levels do not change).

The drug is capable of potentiating the antihypertensive activity of the following antihypertensive drugs: β-blockers, α-adrenoblockers, diuretics, α1-antagonists and other Ca antagonists, as well as ACE inhibitors, α-methyldopa and PDE-5 inhibitors. If there is a strict need to use such combinations, the patient's condition should be closely monitored.

Testing in monkeys revealed that when the drug is used intravenously with zidovudine, there is a significant increase in the AUC of zidovudine, as well as a decrease in its clearance and distribution volume.

Grapefruit juice slows down the action of hemoprotein P450 ZA4. When used together with this juice, the plasma values of the drug increase and its effect is prolonged. Such an effect can enhance the antihypertensive activity of the drug. This effect can continue for about 4 days from the moment of taking grapefruit juice, which should be taken into account when using nimodipine.

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Storage conditions

Nemotan must be stored in a place closed to small children. Temperature indicators - maximum 25°C.

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Shelf life

Nemotan can be used for a period of 5 years from the date of manufacture of the therapeutic substance.

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Application for children

The drug cannot be used in pediatrics.

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Analogues

Analogues of the drug are Vazokor, Amlorus, Nimotop with Nimodipe Sandoz, Nitopin with Nimodipexal, and in addition Amlodipine, Nimodipine and Phenigidine.

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Reviews

Nemotan gets mostly good reviews – it helps to significantly improve the quality of life of older people who experience age-related disorders in the brain: irritability, memory loss and insomnia.

The drug's sustained restorative effect was noted during rehabilitation in individuals who had suffered an active phase of ischemic stroke. The drug's effectiveness in eliminating vascular spasms inside the brain was also positively assessed in forum comments.