Smooth

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

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

It is established that the drug reduces the intensity of memory disorders and helps to improve concentration of attention in individuals with problems in the brain.

Indications Nemontana

It is used to treat and prevent neurological disorders of the ischemic nature associated with vascular spasms inside the brain, resulting from the developed subarachnoid hemorrhage after aneurysm rupture.

Appointed with the accompanying intense symptoms of brain disorders in the elderly.

Release form

The release of the drug produced in tablets - 10 pieces inside the cell packaging; 3 or 10 packs inside a pack.

[1], [2], [3], [4]

Pharmacodynamics

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

[5], [6], [7], [8], [9], [10]

Pharmacokinetics

The active element of the drug is almost fully absorbed after ingestion. The values of plasma Cmax, as well as AUC increase in accordance with the increase in dosage (studies were carried out to a portion of 90 mg).

Distribution volume (Vss, 2-chamber type) for intravenous injection equal to 0.9-1.6 l / kg. The level of total clearance is 0.6-1.9 l / h / kg.

With blood protein, it is synthesized at 97-99%.

Nimodipine excretion is realized in metabolic processes through the structure of hemoprotein P450 ZA4.

Intense presystemic metabolic processes (approximately 85-95%) create bioavailability indicators equal to 5-15%.

[11], [12], [13], [14]

Dosing and administration

Use in disorders of brain function.

Older people with similar pathologies are required to apply 3 times a day for the first tablet of drugs (30 mg of the substance 3 times a day).

Persons with significantly impaired renal activity (the CF rate is below 20 ml per minute) are prescribed very carefully, with regular examinations of the patient during therapy.

Therapy and prevention of neurological disorders of the ischemic nature associated with cerebral vascular spasms that develop due to aneurysm rupture followed by subarachnoid hemorrhage.

After the course of treatment with the introduction of infusions, oral administration of 60 mg of the drug (2 tablets) is carried out 6 times a day.

With the appearance of negative signs, a portion reduces or stops the use of drugs (if necessary).

Problems with the functioning of the liver (especially hepatic cirrhosis) can increase the bioavailability of the drug due to a decrease in metabolic clearance values and a weakening of the primary metabolic processes. In these cases, negative symptoms may increase (for example, a decrease in blood pressure values), therefore, dosage reduction or medication cancellation is performed.

Combination with substances that induce or slow down the action of the CYP 3A4 component may require changing the portion size.

Tablets are swallowed whole, without chewing, squeezed with plain water. You can take medicine without reference to food intake, with at least 4-hour intervals. It is forbidden to drink grapefruit juice during therapy.

[19], [20], [21], [22], [23], [24]

Use Nemontana during pregnancy

Testing was not performed regarding the use of drugs during pregnancy. In the case of the need to use it in the specified period, you need to carefully assess the risks and benefits, given the severity of clinical symptoms.

It was determined that the indices of nimodipine and its metabolic components inside the mother's milk correspond to plasma values. Because of this, during the use of Nemotana, breastfeeding is prohibited.

Contraindications

The main contraindications:

• the use of drugs for personal intolerance associated with nimodipine or other elements of the drug;
• administration in combination with rifampicin (in such cases, the therapeutic effects of Nemotan are significantly weakened) and anticonvulsants, including phenytoin and phenobarbital with carbamazepine (these substances significantly lower the level of bioavailability of nimodipine);
• introduction to persons with myocardial infarction or angina of unstable nature (also during the 1st month from the moment of their development);
• with ongoing therapy of brain disorders;
• disorders in the liver (especially hepatic cirrhosis), because it can provoke an increase in the bioavailability values of nimodipine due to the weakening of metabolic clearance and primary metabolic processes.

[15], [16], [17], [18]

Side effects Nemontana

Among the adverse events:

• disorders associated with blood and lymph: thrombocytopenia or a change in the indications of laboratory blood tests;
• immune disorders: symptoms of allergies, acute manifestations of intolerance and rashes;
• lesions affecting NS: headaches and cerebrovascular signs that are non-specific;
• heart problems: tachycardia, non-specific types of arrhythmias and bradycardia;
• vascular-related symptoms: a decrease in blood pressure values, non-specific cardiovascular signs, and vasodilation;
• disorders of the gastrointestinal tract function: nausea, gastrointestinal disorders and intestinal blockage;
• problems with liver and gallbladder activity: a temporary increase in the activity of the liver enzymes and moderate or mild signs associated with the liver.

Negative manifestations found in clinical testing of nimodipine in accordance with the indications for the treatment of disorders in the brain:

• problems with the work of the National Assembly: vertigo;
• neurological manifestations of a non-specific nature: hyperkinesia, dizziness or tremor;
• impaired cardiac function: palpitation;
• vascular lesions: swelling or syncope;
• problems with the work of the digestive tract: diarrhea, bloating or obstipation.

Overdose

Acute poisoning with Nemotan causes bradycardia or tachycardia, nausea, a strong decline in blood pressure, as well as disorders of gastrointestinal function.

In the case of acute intoxication, you must immediately cancel the use of the drug. In addition, symptomatic actions are performed, as well as gastric lavage and intake of activated carbon.

If the blood pressure indicators continue to decrease, you need to enter in / in the method of dopamine or norepinephrine. Because the drug does not have an antidote, in the case of the development of other side signs, symptomatic procedures are performed.

[25], [26], [27], [28]

Interactions with other drugs

The metabolism of nimodipine is associated with the action of the hemoprotein P450 ZA4 system, which is located inside the liver and intestinal mucosa. Because of this, drugs that affect this enzyme structure can change the level of drug clearance and its primary metabolic processes.

The experience of using other Ca channel antagonists shows that rifampicin is able to potentiate the metabolism of nimodipine, because it induces the activity of enzymes. As a result of the combination of these drugs, there is a significant weakening of the therapeutic effect of nimodipine, which is why they are not used together.

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

Introduction together with the following agents, slowing down the activity of the hemoprotein P450 ZA4 system, requires tracking blood pressure values and considering options with changing the dosage of nimodipine, if needed.

Testing of the interaction of drugs and macrolides has not been performed, but it is known that individual macrolides (for example, erythromycin) can slow down the effect of hemoprotein P450 ZA4, so they can interact with the drug at this stage. In this regard, this combination can not be used.

Testing investigating interactions with a combination of drugs and agents that slow down the activity of anti-HIV protease (for example, ritonavir) has not been performed. It is believed that substances from this category have a strong inhibitory effect on hemoprotein P450 ZA4. There is a possibility of an increase in the plasma values of nimodipine, which is intense and important for the clinical picture, when administered together with drugs that slow down the action of protease.

There is no information regarding the effects that develop when using the drug and ketoconazole. There is information that azolic type antimycotics slow down the activity of hemoprotein P450 ZA4, and also interact with other dihydropyridine Ca channel antagonists. Because of this, with a combined administration with nimodipine, a noticeable increase in the level of its general bioavailability can be observed (due to the weakening of the primary metabolic processes).

Testing regarding drug sharing and nefazodone was not conducted. There is evidence that the antidepressant has a strong inhibitory effect on hemoprotein P450 ZA4. There is a risk of increasing plasma indices of nimodipine if it is combined with nefazodone.

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

Using the drug together with dalfopristin or quinupristin causes an increase in plasma indices of nimodipine.

The administration of Nemotan together with the H2-terminal antagonist cimetidine or with valproic acid causes an increase in the plasma values of drugs.

Prolonged combination of the drug and nortriptyline does not significantly increase the plasma level of nimodipine (while the values of nortriptyline do not change).

The drug is able to potentiate the antihypertensive activity of the following antihypertensive drugs: β-blockers, α-adrenergic blocking agents, diuretics, α1 antagonists and other Ca antagonists, and in addition, ACE inhibitors, α-methyldopa and PDE-5 inhibitors. With a strict need to use such combinations, you need to carefully monitor the patient's condition.

Testing with the participation of monkeys revealed that when combined with / in the use of the drug with zidovudine, there is a significant increase in the AUC indicators 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 along with this juice, the plasma values of the drug increase and prolongation of its effect. This 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 must be considered when using nimodipine.

[29], [30], [31]

Storage conditions

Nemotan is required to be kept in a place closed from the penetration of small children. Temperature indicators - a maximum of 25 ° C.

[32]

Shelf life

Nemotan can be used for a 5-year term since the production of the therapeutic substance.

[33]

Application for children

You can not use the drug in pediatrics.

[34], [35]

Analogs

Analogs of drugs are drugs Vazokor, Amlorus, Nimotop with Nimodip Sandoz, Nitopin with Nimodipheksalom, and in addition Amlodipine, Nimodipin and Fenigidin.

[36], [37], [38], [39], [40]

Reviews

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

The sustained regenerative effect of the drug was noted during the rehabilitation of individuals who have undergone an active phase of ischemic stroke. The comments on the forums also positively evaluated the effectiveness of drugs in the elimination of vascular spasms inside the brain.