Nimopine
Nimopine: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Nimopine
ATX code: C08CA06
Active ingredient: nimodipine (Nimodipine)
Manufacturer: Simpex Pharma Pvt. Ltd. (Simpex Pharma Pvt. Ltd.) (India)
Description and photo update: 09.10.2019
Prices in pharmacies: from 642 rubles.
Buy
Nimopine is a drug that affects the vessels of the brain, used for ischemic neurological lesions in patients with subarachnoid hemorrhage (SAH) due to ruptured aneurysm.
Release form and composition
Dosage forms of Nimopine:
- solution for infusion: clear, slightly yellowish liquid (50 ml each in a brown glass bottle sealed with a rubber stopper, rolled up with an aluminum ring and a plastic cap; in a cardboard box 1 bottle complete with a connecting tube for an infusion pump);
- film-coated tablets: biconvex oval, with a line on one side, pale yellow film shell, at the break - a yellowish-white mass (10 pcs. in a blister, in a cardboard box 1, 2, 3, 5 or 10 blisters).
Each pack also contains instructions for the use of Nimopin.
1 ml of solution contains:
- active substance: nimodipine - 0.2 mg;
- additional components: propylene glycol, ethanol 96%, water for injection.
1 tablet contains:
- active substance: nimodipine - 30 mg;
- additional components: microcrystalline cellulose, crospovidone, corn starch, povidone K-30, magnesium stearate;
- film shell: propylene glycol, FMC yellow (titanium dioxide, macrogol-400, hypromellose, macrogol-6000, dye iron oxide yellow).
Pharmacological properties
Pharmacodynamics
Nimopine is a derivative of 1,4-dihydropyridine, a slow calcium channel blocker (BMCC). Nimodipine demonstrates predominantly cerebrovasodilating and anti-ischemic effects. Able to prevent or relieve vasospasm caused by exposure to various vasoactive substances, including prostaglandins, serotonin, histamine. As a result of high lipophilicity, the active substance passes well through the blood-brain barrier, has almost no effect on conductivity in the atrioventricular and sinoatrial nodes, and on myocardial contractility. Nimopine reflexively increases the heart rate (HR) due to vasodilation.
Against the background of acute disorders of cerebral circulation, leading to the expansion of the vessels of the brain, Nimopine helps to improve cerebral circulation. Moreover, additional perfusion is usually most pronounced in the area of damaged and previously insufficiently supplied with blood areas of the brain. The therapy can significantly reduce the incidence of ischemic neurological disorders and the mortality rate associated with SAH.
Pharmacokinetics
After oral administration of Nimopine, there is an almost complete absorption of nimodipine. Its bioavailability can vary from 8 to 12%, which demonstrates a pronounced effect of the first passage through the liver. The maximum concentration (C max) of nimodipine is 31 ng / ml, and the time to reach it (T Cmax) is 0.5–1 h. After 0.6–1.6 h after the next oral administration of the drug, its equilibrium concentration (C ss) in plasma is 26 ng / ml in the elderly and 12.3-17.5 ng / ml in young people. With an increase in a single dose to 90 mg, a proportional increase in the level of nimodipine in plasma is recorded.
In the case of a long-term infusion intravenous (IV) infusion at a rate of 0.03 mg / kg / h, the average plasma concentration of the active substance in the blood is 17.6–26.6 ng / ml. The volume of distribution (V d) is 0.9-1.6 l / kg, the total clearance is 0.6-1.9 l / h / kg.
Nimodipine binds to plasma proteins almost completely - by 97–99%. It crosses the placental barrier and is excreted during lactation, the level of the drug and its metabolites in human milk significantly exceeds the level in blood plasma.
After intravenous jet injection, a two-phase decrease in the concentration of nimodipine in plasma is observed - after 5-10 minutes and after approximately 60 minutes. The concentration of the drug in the cerebrospinal fluid after intravenous infusion is about 0.5% of the plasma concentration in the blood.
Nimodipine is metabolized by the cytochrome CYP3A4 system through dehydrogenation of the dihydropyridine ring and oxidative degradation of esters. The 3 main metabolites formed as a result of the biotransformation of the drug have practically no pharmacological activity. The drug is excreted in the form of metabolites by the kidneys (by 50%) and with bile. Elimination kinetics are linear.
Indications for use
- ischemic neurological disorders due to cerebral vasospasm against the background of SAH caused by rupture of an aneurysm - for the purpose of prevention and treatment;
- emotional lability, decreased memory and ability to concentrate, and other pronounced dysfunctions of the brain in the elderly (for tablets).
Contraindications
Absolute contraindications for all dosage forms of Nimopine:
- age up to 18 years;
- individual intolerance to any of the components of the drug.
Additional absolute contraindications for film-coated tablets:
- severe functional disorders of the liver (in the treatment of disorders of brain function);
- combination therapy with antiepileptic drugs or rifampicin;
- pregnancy and lactation.
Relative (Nimopine should be used with extreme caution):
- severe heart failure;
- arterial hypotension - systolic blood pressure (BP) less than 100 ml Hg. Art.;
- myocardial ischemia, severe bradycardia;
- chronic hepatic failure, severe;
- severe chronic kidney failure, with a glomerular filtration rate (GFR) less than 20 ml / min;
- generalized edema of brain tissue;
- intracranial hypertension;
- combined use with flecainamide and disopyramide, due to a possible increase in the severity of negative inotropic action (for tablets);
- old age, due to the greatest risk of age-related disorders of kidney function (for tablets).
Since the solution for infusion Nimopin contains ethyl alcohol, it should also be used with caution in patients with a slowdown in ethanol metabolism, alcoholism, people with epilepsy, liver disease, pregnant and lactating women.
Nimopin, instructions for use: method and dosage
Solution for infusion
Solution for infusion Nimopine is administered by infusion into a vein.
At the beginning of treatment, the solution should be administered over 2 hours at a rate of 1 mg / h, (on average 0.015 mg / kg / h). If the drug is well tolerated, primarily in the absence of a significant decrease in blood pressure, after 2 hours the rate of administration can be increased to 2 mg / h (approximately 0.03 mg / kg / h).
For patients with labile blood pressure or body weight significantly below 70 kg, it is recommended to administer Nimopine with an initial rate of 0.5 mg / h.
Continuous IV infusion of Nimopine is performed through a central catheter using an infusion pump and a three-channel stopcock, simultaneously with one of the following solutions: sodium chloride 0.9%, dextrose 5%, Ringer's solution, hydroxyethyl starch 6% or dextran with an average molecular weight 35000-45000 Da (the ratio of Nimopine / other solution should be 1 ÷ 4). Mannitol, human albumin, or blood may also be given as a concomitant infusion.
For patients with hepatic and / or renal insufficiency, the dose should be selected individually, depending on the readings of heart rate and blood pressure.
For prophylaxis, starting intravenous administration of the solution is required no later than 4 days after hemorrhage, and continue using Nimopin during the entire period of maximum threat of vasospasm development, that is, up to 10-14 days after subarachnoid hemorrhage.
In case of already existing ischemic neurological disorders caused by vasospasm due to SAH, it is necessary to start infusion therapy as early as possible and carry it out within 5–14 days. After the end of the course of intravenous infusion of the solution, prescribed for both prophylaxis and therapy, for the next 7 days, it is recommended to take the oral form of the drug.
If, during the therapeutic or prophylactic use of Nimopin, surgical treatment of hemorrhage is prescribed, infusion of the solution after the operation must be carried out for at least 5 days.
When introducing the drug into the cisterns of the brain, in the process of surgery, a solution of nimodipine prepared immediately before use (infusion solution at a dose of 1 ml and Ringer's solution at a dose of 19 ml), warmed up to body temperature, can be administered intracisternally.
Patients who experience adverse events may need to reduce the dose of Nimopine or discontinue treatment.
Film-coated tablets
Nimopine tablets are intended for oral administration. They are swallowed whole with a small amount of liquid, regardless of the time of the meal, observing the interval between doses of at least 4 hours.
The recommended dosage regimen of Nimopine (in the absence of other prescriptions):
- hemorrhage in the subarachnoid space after rupture of the aneurysm: upon completion of infusion therapy with solution, 6 times a day, 60 mg (2 tablets), course - 7 days;
- dysfunction of the brain in elderly patients: 3 times a day, 30 mg (1 tablet).
Side effects
- cardiovascular system: facial flushing, decreased blood pressure, arrhythmias, tachycardia or bradycardia, development / aggravation of concomitant heart failure and myocardial ischemia (especially in the presence of severe obstructive coronary artery disease);
- hematopoietic system: agranulocytosis, asymptomatic thrombocytopenia;
- nervous system: insomnia, agitation, increased physical activity, aggressiveness and other symptoms of arousal of the central nervous system; drowsiness, excessive fatigue, dizziness, headache, asthenia, depression; extrapyramidal disorders such as mask-like face, ataxia, tremors, muscle rigidity, difficulty swallowing;
- respiratory system: stridor breathing, cough, difficulty breathing;
- digestive tract: gingival hyperplasia (soreness, bleeding, swelling), increased appetite, dry mouth, nausea, diarrhea / constipation, in some cases - paralytic intestinal obstruction;
- musculoskeletal system: swelling and soreness of the joints;
- changes in laboratory parameters: increased activity of alkaline phosphatase (ALP), gamma-glutamyltransferase (GGT), hepatic transaminases; functional disorders of the kidneys with an increase in the content of urea and / or creatinine in the blood plasma;
- others: increased sweating, peripheral edema, decreased renal activity (increased urea levels, hypercreatininemia), increased body weight, galactorrhea;
- allergic reactions: rash, itchy skin;
- local reactions: phlebitis (when the solution is injected into the peripheral veins, mainly without infusion with concomitant solutions).
Overdose
With an acute overdose of Nimopine, the following symptoms may appear: a pronounced decrease in blood pressure, bradycardia or tachycardia, various neurological disorders and (for tablets) epigastric pain.
In case of signs of an acute overdose, the drug therapy should be stopped immediately. Emergency measures to relieve intoxication are determined by its symptoms. With a significant decrease in blood pressure, intravenous dopamine or norepinephrine should be prescribed. Since the specific antidote of nimodipine is unknown, further treatment of other manifestations of overdose should be symptomatic.
special instructions
Against the background of severe violations of the liver, especially in patients with cirrhosis of the liver with severe portal hypertension, the bioavailability of nimodipine obtained orally may be increased due to a weakening of the metabolic rate in the liver. As a result, there may be an increase in the main action of the drug and its side reactions, including the hypotensive effect. In such cases, the dose of Nimopine should be reduced, taking into account the degree of decrease in blood pressure, or, if necessary, interrupt therapy.
Despite the fact that BMCC does not have a withdrawal syndrome, before completing the course of treatment with the oral form of the drug, it is recommended to slowly reduce the doses received.
If during the period of Nimopin therapy the patient needs surgery under general anesthesia, the anesthesiologist should be informed about the treatment.
Due to the fact that nimodipine is absorbed by polyvinyl chloride, only infusion systems with polyethylene tubes can be used to administer the solution.
Nimodipine is sensitive to the action of light, therefore, direct sunlight should be avoided on the infusion solution. For the implementation of parenteral administration of Nimopine, glass syringes and connecting tubes of red, yellow, brown or black color are required; wrap the infusion pump and tubing with opaque paper or foil. If the solution is used under artificial lighting or diffused daylight, then no special protective measures are needed for 10 hours.
Influence on the ability to drive vehicles and complex mechanisms
During the period of treatment with Nimopin, due to the possible occurrence of dizziness, care should be taken when driving vehicles and operating other complex and potentially dangerous mechanisms.
Application during pregnancy and lactation
Pills are contraindicated for pregnant and lactating women. The solution during pregnancy is allowed to be used only if the expected benefit to the woman outweighs the possible threat to the fetus.
During therapy with all dosage forms of Nimopine, breastfeeding must be discontinued.
Pediatric use
Nimopine treatment is contraindicated in patients under 18 years of age.
With impaired renal function
Against the background of severe chronic kidney failure, with a GFR below 20 ml / min, Nimopine should be used with extreme caution.
For violations of liver function
In the presence of severe functional disorders of the liver, it is contraindicated to use Nimopin tablets for the treatment of disorders of brain function. Patients with decompensated chronic liver failure are advised to use both dosage forms of Nimopine with caution.
Use in the elderly
The use of Nimopine in the elderly with numerous concomitant diseases, including severe cardiovascular lesions and severe renal failure (GFR less than 20 ml / min), should be especially carefully justified. During and after treatment, such patients require regular medical supervision, including neurological.
Drug interactions
- rifampicin: the metabolism of nimodipine is accelerated due to an increase in the activity of liver enzymes caused by rifampicin, with a corresponding decrease in the effectiveness of nimodipine;
- xenobiotics affecting the activity of cytochrome CYP3A4: a change in the metabolic clearance of nimodipine is possible;
- fluoxetine: an increase in the plasma concentration of nimodipine (by 50%) and a simultaneous significant decrease in the content of fluoxetine are recorded, while the concentration of its active metabolite, norfluoxetine, is not subject to changes;
- phenytoin, phenobarbital, carbamazepine and other inducers of microsomal oxidation: against the background of long-term previous use of these drugs, the metabolism of nimodipine is activated;
- cimetidine, valproic acid: an increase in the concentration of nimodipine in plasma is possible;
- grapefruit juice: suppression of the metabolism of dihydropyridines is noted; this combination should be avoided, since an unpredictable increase in the content of nimodipine in plasma may be recorded against its background;
- haloperidol: long-term treatment with this substance does not determine drug interactions with nimodipine;
- nortriptyline: with prolonged combination therapy, a slight decrease in the plasma level of nimodipine is possible, while the concentration of nortriptyline does not change;
- lithium preparations, cardiac glycosides, cyclosporine, theophylline, quinidine, carbamazepine, valproic acid: the threat of unwanted effects of these drugs is aggravated;
- drugs that promote the excretion of potassium ions: their arrhythmogenic effect is enhanced;
- inhalation anesthetics: the hypotensive effect increases;
- cephalosporins, aminoglycosides, furosemide and other potentially nephrotoxic drugs: increased risk of renal dysfunction; if combined treatment is necessary, it should be carried out with careful monitoring of renal function, in case of detection of impaired renal function, it is required to stop using nimodipine;
- non-steroidal anti-inflammatory drugs, sympathomimetics, estrogens: the hypotensive effect decreases;
- diuretics, α-adrenergic blockers, angiotensin-converting enzyme inhibitors, β-adrenergic blockers, other BMCCs, angiotensin II receptor antagonists, sympatholytics, methyldopa and other antihypertensive drugs: the degree of hypotensive action increases; during treatment with nimodipine, intravenous administration of β-blockers is contraindicated;
- zidovudine: with simultaneous intravenous administration with a solution, the area under the concentration-time curve (AUC) of a given substance significantly increases and its volume of distribution and clearance decreases;
- flecainide, procainamide, disopyramide, quinidine and other agents leading to prolongation of the QT interval: the likelihood of increased negative inotropic effect and prolongation of the QT interval increases; these funds should be combined with nimodipine with caution.
Analogs
Nimopin's analogs are Nimodipine-native, Nimotop, Nimodipine, Cinnarizin Avexima, Cinnarizin Sopharma, Cinnarizin.
Terms and conditions of storage
Store in a place protected from light and moisture, out of reach of children, at a temperature not exceeding 25 ° C.
The shelf life of the solution for infusion is 2 years, film-coated tablets - 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Nimopine
Currently, there are no reviews on Nimopine left by patients on medical sites, which could objectively assess the effectiveness of the drug and the disadvantages of its use.
Price for Nimopine in pharmacies
The price of Nimopine can be:
- film-coated tablets (30 mg): 30 pcs. in the package - 600-650 rubles, 100 pcs. in the package - 1500-1660 rubles;
- solution for infusion (0.2 mg / ml): 1 bottle of 50 ml complete with a connecting tube - 600-740 rubles.
Nimopine: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Nimopin 30 mg film-coated tablets 30 pcs. 642 RUB Buy |
|
Nimopine 0.2 mg / ml solution for infusion 50 ml 1 pc. 686 r Buy |
|
Nimopin 30 mg film-coated tablets 100 pcs. 1679 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, 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!
