Active substanceNimodipineNimodipine
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  • Nimodipine-native
    solution d / infusion 
    NATIVA, LLC     Russia
  • Nimopin
    pills inwards 
  • Nimopin
    solution in / in d / infusion 
  • Nimotop®
    pills inwards 
    Bayer Pharma AG     Germany
  • Nimotop®
    solution in / in d / infusion 
    Bayer Pharma AG     Germany
  • Dosage form: & nbspsolution for infusions
    Composition:

    One bottle with 50 ml infusion The solution contains 0.01 g of nimodipine

    (active substance).

    Excipients: ethanol 96% - 10 g, macrogol 400 - 8.5 g,

    sodium citrate - 0.1 g, lemon acid anhydrous - 0.015 g, water for

    injections - 31.225 g.

    Description:

    Transparent, slightly yellowish solution.

    Pharmacotherapeutic group:The blocker of "slow" calcium channels (BCCI).
    ATX: & nbsp

    C.08.C.A   Dihydropyridine derivatives

    C.08.C.A.06   Nimodipine

    Pharmacodynamics:

    Nimodipin has cerebrovazodilatiruyuschim action, prevents or eliminates the spasm of blood vessels, provoked by various vasoactive substances (including serotonin, prostaglandins and histamine), has neuro- and psychotropic activity.

    In patients with acute disorders of the cerebral circulation nimodipine, expanding the vessels of the brain, the brain, improves cerebral circulation. Moreover, additional perfusion, as a rule, is more pronounced in the area of ​​damaged and previously insufficiently perfused blood regions of the brain.The use of nimodipine significantly reduces the mortality rate and the incidence of ischemic neurological disorders that occur as a result of subarachnoid hemorrhage.

    Pharmacokinetics:

    Suction. With continuous infusion at a rate of 0.03 mg / kg / h, the average stable concentration of nifedipine in the blood plasma is 17.6-26.6 ng / ml. After intravenous bolus infusion, there is a two-phase reduction in nimodipine plasma concentration after 5-10 min and after about 60 min. The volume of distribution is 0.9-1.6 l / kg of weight, the total clearance is 0.6-1.9 l / h / kg.

    Distribution. Nimodipine intensively binds to blood plasma proteins (97-99%). Penetrates through the placental barrier. The concentration of nimodipine and its metabolites in breast milk is significantly higher than the concentration in the blood plasma.

    After intravenous administration, the concentration of nimodipine in the spinal fluid is about 0.5% of the concentration in the blood plasma.

    Metabolism and excretion. Nimodipine metabolized by dehydrogenation of the dihydropyridine ring and oxidative cleavage of esters. The three main metabolites found in the blood plasma do not have clinically significant pharmacological activity.

    CCDS 4 (aSAH), 19-09-2007

    The effect of nimodipine on the activity of liver enzymes has not been studied. At the person metabolites on 50% are deduced by kidneys and on 30% with bile.

    Indications:Prophylaxis and treatment of ischemic neurological disorders caused by spasm of cerebral vessels on the background of subarachnoid hemorrhage due to aneurysm rupture.
    Contraindications:In view of the seriousness of the indications, the only absolute contraindication is individual intolerance, age to 18 years.
    Carefully:

    With caution Nimotop is prescribed in the following situations: pronounced bradycardia, arterial hypotension (systolic pressure less than 100 ml.Hg), myocardial ischemia, severe heart failure, increased intracranial pressure, generalized cerebral edema, hepatic and renal insufficiency.

    Preperate contains 23.7% by volume of ethanol, this should be taken into account when appointing alcoholism sufferers with deterioration of alcohol metabolism, pregnant and lactating women and patients with liver diseases, epilepsy.

    Pregnancy and lactation:The use of Nimotop during pregnancy always requires a careful assessment of the relationship between the factors of benefit and risk, taking into account the severity of the clinical picture.
    Dosing and Administration:

    The following dosing regimen is recommended:

    Intravenous infusion. At the beginning of the therapy, 1 mg of nimodipine per hour (5 ml of the Nimotop infusion solution), approximately 15 μg / kg / h, is administered within 2 hours. With good tolerability (especially in the absence of a marked decrease in blood pressure), after 2 hours the dose is increased to 2 mg of nimodipine per hour (approximately 30 μg / kg / h). The initial dose for patients weighing well below 70 kg or labile blood pressure should be 0.5 mg nimodipine per hour.

    Infusion solution Nimotop is used for continuous intravenous infusion through the central catheter> using an infusion pump and a three-channel stopcock simultaneously with one of the following solutions: 5% dextrose, 0,9% sodium chloride, Ringer's solution, Ringer's solution with magnesium, a solution of dextran 40 or 6% hydroxyethyl starch in a ratio of approximately 1: 4 (Nimotope / other solution). As a concomitant infusion can also be used mannitol, human albumin or blood.

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

    To connect the polyethylene tube, which receives the Nimotop solution, the channel of the concomitant solution and the central catheter, a three-channel stopcock must be used.

    Preventive use. Intramuscular therapy with nimodipine should begin no later than 4 days after hemorrhage, and continue throughout the period of maximum risk of vasospasm development, that is, up to 10-14 days after subarachnoid hemorrhage.

    After the end of the infusion therapy for the next 7 days, oral intake of the tablet form of nimodipine at a dose of 60 mg x 6 times a day with intervals of 4 hours is recommended.

    Therapeutic use. If there are already ischemic neurologic disorders due to vasospasm due to subarachnoid hemorrhage, infusion therapy should be started as early as possible and conducted for at least 5, but not more than 14 days.

    After the end of the infusion therapy for the next 7 days, oral intake of the tablet form of nimodipine at a dose of 60 mg 6 times a day (every 4 hours) is recommended.

    If, during the therapeutic or prophylactic use of the Nimotop solution, surgical treatment for hemorrhage is performed, intravenous therapy with nimodipine should be continued for at least 5 days after surgery. Introduction to the cistern of the brain. During the surgical intervention, a freshly prepared solution of nimodipine (1 ml of Nimotop infusion solution and 19 ml of Ringer's solution), warmed to the average body temperature, can be administered intracistrically. The solution should be used immediately after preparation.

    If a patient develops adverse reactions to the drug, either reduce the dose or stop treatment with nimodipine. In severe liver function disorders, especially with liver cirrhosis, the bioavailability of nimodipine can be increased due to a decrease in the intensity of primary metabolism and a slowing of metabolic inactivation. A consequence of this may be an aggravation of the main and side effects of the drug, in particular, its hypotensive effect. In such cases, the dose of the drug should be reduced, based on the degree of reduction in blood pressure; If necessary, treatment should be interrupted.

    Nimodipine is sensitive to light, so you should avoid direct exposure to sunlight: use glass syringes and connecting tubes black, brown, yellow or red; In addition, it is advisable to wrap the infusion pump and tubes with opaque paper. With diffused daylight or artificial lighting, Nimotop can be used for 10 hours without special protective measures.

    Nimodipine, the active substance of the Nimotop infusion solution, is absorbed by polyvinyl chloride, only systems with polyethylene tubes can be used for its parenteral administration.

    Side effects:

    Allergic reactions: itching, rash.

    From the gastrointestinal tract: dyspeptic disorders, nausea, diarrhea, dry mouth, changes in appetite, in rare cases - ileus.

    From the nervous system: headache, with the taking of tablets - dizziness.

    From the side of the cardiovascular system: a significant reduction in blood pressure, especially with increased baseline values, "hot flushes" to the face, bradycardia, a feeling of heat in the head, increased sweating,tachycardia, the development or aggravation of existing heart failure and myocardial ischemia.

    On the part of the hematopoiesis system: thrombocytopenia.

    Impact on laboratory performance: increased activity of transaminases, alkaline phosphatase and gamma-glutamyltransferase, impaired renal function with an increase in the concentration of urea and / or creatinine in the blood plasma. In the treatment, it should be taken into account that the preparation contains 23.7% by volume of alcohol (200 mg of alcohol per 1 ml of solution) and 17% of polyethylene glycol 400.

    Local Reactions: phlebitis (with the introduction of the Nimotop infusion solution into the peripheral veins without the concomitant solution).

    Overdose:

    In acute Nimotop overdose, the following symptoms may occur: significant lowering of blood pressure, tachycardia, or bradycardia.

    When symptoms of acute overdose occur, the use of nimodipine should be stopped immediately. Measures for emergency care in case of an overdose are determined by its symptoms. If there is a significant drop in blood pressure, you should enter intravenously dopamine or norepinephrine. Since the specific antidotes of nimodipine are not known, further therapy of other side effects should be symptomatic.
    Interaction:

    Prolonged use of nimodipine with fluoxetine leads to an increase in the concentration of nimodipine in blood plasma by an average of 50%. The concentration of fluoxetine is significantly reduced, while the active metabolite content of fluoxetine - norfluoxetine does not change.

    Simultaneous long-term use of nimodipine and nortriptyline leads to a slight decrease in the concentration of nimodipine (the concentration of nortriptyline in blood plasma does not change). In patients on long-term therapy with haloperidol, no drug interaction of nimodipine with haloperidol was observed.

    Simultaneous intravenous administration of zidovudine and nimodipine results in a significant increase AUC for zidovudine and a decrease in the volume of its distribution and clearance.

    In combination with drugs that reduce blood pressure:

    - diuretics

    - beta-blockers

    - with ACE inhibitors

    - blockers of AT-1 receptors

    - other calcium antagonists

    - alpha-blockers

    - methyldopa

    - inhibitors of phosphodiesterase

    Nimotop can strengthen the hypotensive effect.

    Simultaneous therapy with potentially nephrotoxic drugs (eg, aminoglycosides, cephalosporins, furosemide) can cause renal dysfunction.In the case of such treatment, as well as in patients with renal insufficiency, treatment should be carried out under careful control. If you find a violation of the kidneys reception of nimodipine should be discontinued. Infusion solution Nimotopa contains 23.7 vol% alcohol, it is necessary to take into account the possible interaction of alcohol with other medicinal products.

    In the monkey study, simultaneous administration of zidovudine and intravenous bolus administration of nimodipine led to a decrease in zidovudine clearance.

    Special instructions:

    Effect on the ability to drive transp. cf. and fur:

    Due to the possible development of dizziness, the use of nimodipine may impair the ability to drive vehicles and mechanisms. When using the Nimotope infusion solution, this factor usually does not matter.

    Form release / dosage:

    Solution for infusions, 0.2 mg / ml.

    50 ml in bottles of brown glass; 1 bottle together with

    instructions for use and polyethylene connecting

    tube for infusion into cardboard pack.

    50 ml in bottles of brown glass, 1 bottle together with

    instructions for use and polyethylene connecting

    tube for infusion into cardboard pack of 5 cardboard packs

    packed in polyethylene film.

    Packaging:[solution for infusion, 0.2 mg / ml (bottle) 50 ml x 1 + (tube for infusion) x 1] x 1 (cardboard pack); [solution for infusion, 0.2 mg / ml (bottle) 50 ml x 1 + (tube for infusion) x 1] x 5 (polyethylene film)
    Storage conditions:

    At a temperature of no higher than 30 ° C in a place protected from light and inaccessible to children.

    Shelf life:

    4 years. Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N013667 / 02
    Date of registration:14.03.2008
    The owner of the registration certificate:Bayer Pharma AGBayer Pharma AG Germany
    Manufacturer: & nbsp
    Representation: & nbspBAYER, AOBAYER, AO
    Information update date: & nbsp17.08.2015
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