Nimotop - Instructions For Use, Analogs, Price, Tablets, Solution

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Nimotope

Nimotop: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Nimotop

ATX code: C08CA06

Active ingredient: nimodipine (Nimodipine)

Manufacturer: Bayer, AG (Bayer, AG) (Germany)

Description and photo update: 2019-20-09

Nimotop is a drug that affects the vessels of the brain.

Release form and composition

Nimotop is available in the following dosage forms:

• Film-coated tablets: yellow, biconvex, round, engraved with the inscription "SK" on one side and the Bayer cross on the other (10 pcs. In blisters, 3 or 10 blisters in a cardboard box);
• Solution for infusion: transparent, slightly yellowish (50 ml in dark glass bottles, 1 or 5 bottles in a cardboard box, complete with a connecting tube).

Each pack also contains instructions for using Nimotop.

Composition of 1 tablet:

• Active ingredient: nimodipine - 30 mg;
• Auxiliary components: corn starch - 37.5 mg, microcrystalline cellulose - 142.5 mg, crospovidone - 44.4 mg, povidone - 75 mg, magnesium stearate - 0.6 mg;
• Film shell: hypromellose - 5.4 mg, yellow iron oxide - 0.54 mg, macrogol - 1.8 mg, titanium dioxide - 1.26 mg.

The composition of 1 bottle of solution for infusion includes:

• Active ingredient: nimodipine - 10 mg;
• Auxiliary components: 96% ethanol - 10,000 mg, macrogol 400 - 8500 mg, anhydrous citric acid - 15 mg, sodium citrate - 100 mg, water for injection - 31.225 mg.

Pharmacological properties

Pharmacodynamics

The active ingredient of Nimotop is nimodipine, a calcium channel blocker with a highly selective antispasmodic effect on the vessels of the brain. Able to prevent or eliminate vasoconstriction caused by various vasoactive substances (including serotonin, prostaglandins and histamine). Possesses psycho- and neurotropic activity.

In acute disorders of cerebral circulation, nimodipine dilates the vessels of the brain, as a result of which cerebral circulation improves. The increase in perfusion is, as a rule, more pronounced in the damaged areas of the brain and areas that received insufficient blood supply. Nimotop significantly reduces the incidence of ischemic brain damage and mortality in patients with subarachnoid hemorrhage.

By acting on the receptors of the blood vessels of the brain associated with calcium channels, nimodipine stabilizes the function of nerve cells and has a protective effect on them, improves the tolerance of ischemia by nerve cells and improves blood flow to the brain. At the same time, it does not cause the development of the stealing syndrome.

Nimotope has a positive effect on disorders of concentration and memory in patients with impaired brain function. Helps to improve the results of psychometric functional tests, personality and behavioral reactions.

Pharmacokinetics

After taking Nimotop tablets inside, the drug is almost completely absorbed. Nimodipine and its primary metabolites are found in blood plasma after 10-15 minutes. In young patients, after a single dose of 30 and 60 mg, the maximum concentration is 16 ± 8 ng / ml and 31 ± 12 ng / ml, respectively. With repeated administration of the drug (30 mg three times a day), the maximum concentration in elderly patients is reached after 0.6-1.6 hours and is 7.3-43.2 ng / ml. The increase in the maximum concentration and the area under the concentration-time curve is dose-dependent.

Nimodipine has the effect of the first passage through the liver (85–95%), therefore its absolute bioavailability is about 5–15%.

With continuous infusion of Nimotop at a rate of 0.03 mg / kg / h, the average stable plasma concentration of nifedipine is 17.6–26.6 ng / ml. After an intravenous bolus infusion, a two-phase decrease in the plasma level of the drug is observed: 1 - after 5-10 minutes, 2 - after about 60 minutes. The volume of distribution is 0.9-1.6 l / kg, the total clearance is 0.6-1.9 l / h / kg.

Nifedipine is characterized by intense binding to plasma proteins (97–99%). Penetrates through the placental barrier and into breast milk. At the same time, in mother's milk, the concentrations of nimodipine and its metabolites significantly exceed plasma concentrations.

With oral administration of Nimotop, the concentration of the drug in the cerebrospinal fluid is about 0.5% of the plasma level.

Nimodipine is metabolized mainly by dehydrogenation of the dihydropyridine ring and oxidative degradation of esters. Three main metabolites are found in the blood, which do not have clinically significant pharmacological activity.

The effect of nimodipine on the activity of liver enzymes has not been studied. The drug is excreted: with kidneys - 50%, with bile - 30%.

The initial phase of the half-life for film-coated tablets is 1.1-1.7 hours, the final phase is 5-10 hours.

Indications for use

• Ischemic neurological disorders caused by cerebral vasospasm against the background of subarachnoid hemorrhage associated with rupture of an aneurysm (for treatment and prevention);
• Severe functional disorders of the brain in elderly patients, manifested in the form of decreased concentration of attention and memory, emotional instability (pills).

Contraindications

Absolute:

• Age under 18;
• Hypersensitivity to drug components.

Additional contraindications to the use of Nimotop tablets are:

• Severe functional disorders of the liver (for example, cirrhosis of the liver);
• Simultaneous use with rifampicin or antiepileptic drugs (phenytoin, phenobarbital, carbamazepine);
• Pregnancy and lactation.

Relative (Nimotop should be used with caution in the presence of the following diseases / conditions):

• Arterial hypotension (with systolic pressure less than 100 ml Hg);
• Unstable angina pectoris or the period of the first 4 weeks after acute myocardial infarction (before prescribing the drug, it is necessary to correlate the benefits of therapy with the possible risk of decreased coronary artery perfusion and myocardial ischemia);
• Elderly age in combination with severe renal impairment (with glomerular filtration less than 20 ml per minute (for tablets));
• Alcoholism with impairment of alcohol metabolism, liver disease, epilepsy, pregnancy and lactation period (for infusion solution, due to the presence of 23.7 vol.% Ethanol in the drug);
• Severe bradycardia, myocardial ischemia, severe heart failure, increased intracranial pressure, generalized cerebral edema, hepatic and renal failure (for infusion solution).

Elderly patients with severe heart failure who are taking Nimotop for the treatment of functional disorders of the brain require regular examinations.

Nimotop, instructions for use: method and dosage

Pills

Nimotop tablets are taken orally, regardless of food intake, swallowing whole and drinking a small amount of liquid. The intervals between single doses should be at least 4 hours.

In case of subarachnoid hemorrhage caused by a rupture of an aneurysm, pills are taken after 5-14 days of intravenous therapy with an infusion solution. The recommended single dose is 2 tablets (60 mg), the frequency of administration is 6 times a day. The duration of the course is 7 days.

For functional disorders of the brain, elderly patients are recommended to take 1 tablet 3 times a day.

Infusion solution

At the beginning of therapy, Nimotop is administered as an intravenous infusion over 2 hours at 1 mg (5 ml) per hour, approximately 0.015 mg / kg per hour. After 2 hours, with good tolerance (first of all, in the absence of a noticeable decrease in blood pressure), the dose is doubled. The initial dose for patients weighing up to 70 kg or labile blood pressure should be 0.5 mg per hour.

Nimotop infusion solution is used for continuous intravenous infusion through a central catheter using a three-channel stopcock and an infusion pump simultaneously with one of such solutions as: 5% dextrose, 0.9% sodium chloride, dextran solution 40, Ringer's solution with magnesium, Ringer's solution or a solution of 6% hydroxyethylated starch in a ratio of about 1: 4 (Nimotop / other solution). Mannitol, blood, or human albumin can also be used as a concomitant infusion.

The solution should not be mixed with other drugs or added to the infusion vessel. It is recommended to continue the administration of Nimotop during anesthesia, angiography and surgery.

In ischemic neurological disorders caused by vasospasm due to subarachnoid hemorrhage, infusion therapy is started as early as possible and is carried out for 5-14 days, after which they switch to taking the drug inside.

For prophylaxis, the use of the infusion solution should be started no later than 4 days after the hemorrhage. Therapy continues throughout the entire period of maximum risk of developing vasospasm (10-14 days after subarachnoid hemorrhage). At the end of the course, treatment should be continued by taking Nimotop inside.

If during the use of the drug with a therapeutic or prophylactic purpose, surgical treatment of hemorrhage is performed, intravenous administration of Nimotop should be continued for at least 5 days after the surgery.

When performing a surgical intervention, a freshly prepared infusion solution heated to an average body temperature (1 ml of Nimotop and 19 ml of Ringer's solution) can be injected into the cisterns of the brain. In the event of adverse reactions to the ongoing therapy, it is necessary to reduce the dose or cancel the administration of the drug.

Nimotop infusion solution is sensitive to light, therefore, direct sunlight should be avoided. For this, the use of glass syringes and connecting tubes in brown, black, red or yellow is recommended. It is also advisable to wrap the tubing and infusion pump with opaque paper. In diffused daylight or artificial light, without special protective measures, Nimotop can be used for 10 hours.

The active substance of Nimotop, nimodipine, is absorbed by polyvinyl chloride, and therefore only systems with polyethylene tubes can be used for its parenteral administration.

Side effects

In the treatment of ischemic neurological disorders during the use of Nimotop, the following disorders may develop (≥ 1/10 - very often; from ≥ 1/100 to <1/10 - often; from ≥ 1/1000 to <1/100 - infrequently; from ≥ 1/10 000 to <1/1000 - rarely; <1/10 000 - very rare):

• Digestive system: infrequently - nausea; rarely - intestinal obstruction;
• Cardiovascular system: infrequently - lowering blood pressure, tachycardia, vasodilation; rarely - bradycardia;
• Nervous system: infrequently - headache;
• Hepatobiliary system: rarely - a transient increase in the level of hepatic enzymes;
• Immune system: infrequently - rash, allergic reactions;
• Hematopoietic systems: infrequently - thrombocytopenia;
• Local reactions (with intravenous administration): rarely - reactions at the site of infusion or injection, thrombophlebitis at the injection site.

When using Nimotop in elderly patients during the therapy of severe brain dysfunctions, side effects may develop:

• Nervous system: rarely - vertigo, headache, hyperkinesia, dizziness, tremor;
• Digestive system: rarely - diarrhea, constipation, flatulence;
• Cardiovascular system: infrequently - vasodilation, lowering of blood pressure; rarely - a feeling of palpitations, fainting, tachycardia, edema;
• Immune system: rarely - rash, allergic reactions.

Overdose

Regardless of the dosage form, an overdose of Nimotop can be manifested by a pronounced decrease in blood pressure, tachycardia or bradycardia. When taking the drug in tablets, pain in the epigastric region, vomiting, symptoms of impaired activity of the central nervous system are also possible.

The drug is canceled. If an overdose is caused by Nimotop tablets, gastric lavage should be performed and activated charcoal should be taken. Treatment is symptomatic. With a significant decrease in blood pressure, dopamine or norepinephrine is administered intravenously. The specific antidote for the drug has not been established.

special instructions

The appointment of Nimotop to elderly patients with a large number of concomitant diseases, severe cardiovascular diseases and severe renal failure (with a glomerular filtration rate of less than 20 ml per minute) should be especially carefully justified. Such patients during therapy and after its completion require regular medical supervision.

With severe functional disorders of the liver, especially with cirrhosis of the liver, the bioavailability of Nimotop increases. As a result, it is possible to aggravate the side effects of the drug, including the development of hypotensive action. In this case, based on the degree of decrease in blood pressure, the dose of the drug should be reduced. If necessary, therapy is interrupted.

In some cases, during in vitro fertilization against the background of the use of Nimotop, reversible chemical changes were observed in the sperm head, which can lead to impaired sperm function.

Influence on the ability to drive vehicles and complex mechanisms

During therapy, the ability to drive vehicles may be impaired due to the occurrence of dizziness and a decrease in blood pressure.

Application during pregnancy and lactation

Nimotop tablets are contraindicated for use during pregnancy and lactation.

Solution for infusion in pregnant / lactating women can be used if the expected benefits of therapy are higher than the potential risks.

Pediatric use

Nimotop is not used in pediatric practice (under 18 years of age).

With impaired renal function

Solution for infusion should be used with caution in renal impairment.

For violations of liver function

In tablets, Nimotop is contraindicated in patients with severely impaired liver function (for example, with liver cirrhosis).

The solution for infusion should be used with caution in liver disease, liver failure and alcoholism.

Use in the elderly

In the form of tablets, Nimotop should be prescribed with caution to elderly patients if they have severe renal dysfunction (glomerular filtration rate <20 ml / min) or severe heart failure, as well as if the drug is prescribed to them in connection with brain dysfunctions. During the treatment period, these patients should be examined regularly.

Drug interactions

With the simultaneous use of Nimotop with certain drugs, the following effects may occur:

• Nortriptyline (long-term combined use): a slight decrease in the concentration of nimodipine in the blood plasma without changing the concentration of nortriptyline;
• Rifampicin: accelerating metabolism and decreasing the effectiveness of nimodipine;
• Fluoxetine (long-term combined use): a significant increase in the concentration of nimodipine in the blood plasma (usually by 50%) with a significant decrease in the concentration of fluoxetine and the unchanged content of the active metabolite of fluoxetine (norfluoxetine);
• Medicines that inhibit or induce the activity of liver enzymes: changes in the concentration of nimodipine in plasma;
• Antiepileptic drugs that induce the isoenzyme CYP3A4 (phenytoin, phenobarbital, carbamazepine): a significant decrease in the bioavailability of nimodipine (the combination of drugs is contraindicated);
• Diuretics, beta-blockers, angiotensin-converting enzyme inhibitors, AT1-receptor blockers, other calcium antagonists, alpha-blockers, methyldopa, phosphodiesterase inhibitors: lowering blood pressure (requires careful monitoring);
• Drugs that induce the activity of the CYP3A4 isoenzyme (macrolides (eg erythromycin), azole antifungals (eg ketoconazole), HIV protease inhibitors (eg ritonavir), antidepressants nefazodone and fluoxetine, dalfopristin / quinopristinic acid concentration, c nimodipine in plasma (it is recommended to reduce its dose and monitor blood pressure);
• Zidovudine (intravenous administration): a significant increase in its AUC (total concentration of the drug in blood plasma) and a decrease in its volume of distribution and clearance;
• Calcium preparations: decrease in the effectiveness of nimodipine;
• Potentially nephrotoxic drugs (for example, aminoglycosides, cephalosporins, furosemide): impaired renal function (when used together, as well as when Nimotop is prescribed to patients with renal failure, careful monitoring of the condition is necessary; with the development of functional renal disorders, therapy is canceled);
• Grapefruit juice: increased plasma concentration of nimodipine.

Analogs

Nimotop's analogs are: Breinal, Dilceren, Nimodipin, Nimopin.

Terms and conditions of storage

Store in a dark, dry place out of reach of children at temperatures up to 30 ° C.

Shelf life:

• Tablets - 5 years;
• Infusion solution - 4 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Nimotop

Reviews about Nimotop are mostly positive: the drug is effective when used according to indications, it is well tolerated. Of the side effects, the most often mentioned are a feeling of heat, redness of the skin, a decrease in blood pressure.

Price for Nimotop in pharmacies

Approximate prices for Nimotop: film-coated tablets of 30 mg - 1240 rubles. per pack of 100 pcs., solution for infusion 0.2 mg / ml - 2967–3316 rubles. per pack of 5 bottles.

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!