Nimopine
Xenobiotics that affect the activity of cytochrome CYP3A4 may alter the metabolic clearance of nimodipine.
Based on the experience of using nifedipine, it can be expected that rifampicin, by inducing the activity of liver enzymes, can accelerate the metabolism of nimodipine and, when used simultaneously, the effectiveness of nimodipine is reduced.
Previous long-term administration of microsomal oxidation inducers (phenobarbital, phenytoin or carbamazepine) increases the metabolism of nimodipine.
Grapefruit juice inhibits the metabolism of dihydropyridines. The combination of grapefruit juice and nimodipine should be avoided because this may result in unpredictable increases in nimodipine plasma concentrations. Concomitant use of nimodipine with cimetidine or valproic acid may also lead to increased plasma concentrations of nimodipine.
The combined use of nimodipine and fluoxetine is accompanied by an increase in the concentration of nimodipine in plasma (by 50%), while the concentration of fluoxetine is significantly reduced, and the concentration of its active metabolite norfluoxetine remains unchanged.
Simultaneous long-term use of nimodipine and nortriptyline leads to a slight decrease in the concentration of nimodipine (while the concentration of nortriptyline in the blood plasma does not change). In patients on long-term therapy with haloperidol, no drug interactions between nimodipine and haloperidol were detected.
Nimodipine, when administered intravenously with zidovudine, leads to a significant increase in the area under the concentration-time curve (AUC) of the latter and a decrease in its volume of distribution and clearance.
Suppresses the metabolism of prazosin and other alpha-blockers, as a result of which the hypotensive effect may be enhanced.
In patients taking antihypertensive drugs (diuretics, beta-blockers, angiotensin-converting enzyme inhibitors, angiotensin II receptor antagonists, other BMCCs, alpha-blockers, methyldopa, sympatholytics, etc.), the administration of Nimopin increases the severity of the hypotensive effect. Because of this, intravenous administration of beta-blockers is not permissible during the use of nimodipine.
Caution should be used concomitantly with disopyramide, flecainide, procainamide, quinidine and other drugs that cause prolongation of the QT interval (possible increased severity of negative inotropic effects and prolongation of the QT interval).
The simultaneous administration of potentially nephrotoxic drugs (for example, aminoglycosides, cephalosporins, furosemide) with nimodipine can lead to impaired renal function. If their simultaneous use is necessary, as well as in patients with renal failure, treatment should be carried out under careful monitoring of renal function. If renal dysfunction is detected, nimodipine should be discontinued.
Strengthens the arrhythmogenic effect of drugs that promote the excretion of potassium ions. Increases the risk of developing side effects of cardiac glycosides, quinidine, carbamazepine, cyclosporine, theophylline, valproic acid, lithium preparations.
The hypotensive effect is enhanced when administered simultaneously with inhalational anesthetics.
The hypotensive effect is reduced by sympathomimetics, non-steroidal anti-inflammatory drugs (suppression of prostaglandin synthesis, sodium and fluid retention in the body), estrogens (fluid retention in the body).
Nimopin 30 mg, 30 film-coated tablets
1 tab. nimodipine 30 mg
[PRING] corn starch - 68 mg, microcrystalline cellulose - 90 mg, povidone K30 - 70 mg, crospovidone - 80 mg, magnesium stearate - 2 mg.
Film shell composition: FMC yellow (hypromellose, macrogol 400, macrogol 6000, titanium dioxide, iron oxide yellow dye) - 9 mg, propylene glycol - 1 g.
10 pieces. - blister (1) - cardboard packs. 10 pieces. - blister (2) - cardboard packs. 10 pieces. - blister (3) - cardboard packs. 10 pieces. - blister (5) - cardboard packs. 10 pieces. - blister (10) - cardboard packs.
Indications
- prevention and treatment of ischemic neurological disorders caused by spasm of cerebral vessels against the background of subarachnoid hemorrhage due to aneurysm rupture (after IV therapy with an infusion solution);
- severe dysfunction of the brain in elderly patients (including decreased memory and ability to concentrate, emotional lability).
Contraindications for use
- severe liver dysfunction (for the treatment of brain dysfunction);
- pregnancy;
- lactation period;
- age under 18 years;
- therapy with antiepileptic drugs;
- simultaneous use with rifampicin;
- individual intolerance to the components of the drug.
With caution: arterial hypotension (systolic blood pressure less than 100 mm Hg), severe bradycardia, myocardial ischemia, severe heart failure, severe chronic renal (GFR less than 20 ml/min) and/or liver failure, intracranial hypertension, generalized tissue edema brain.
Caution should be prescribed simultaneously with disopyramide and flecainamide (possible increased severity of negative inotropic effect).
Caution should be exercised in elderly patients due to the greater likelihood of age-related renal impairment.
pharmachologic effect
A slow calcium channel blocker (SCBC), a 1,4-dihydropyridine derivative, has a predominantly cerebrovasodilating and anti-ischemic effect. May prevent or eliminate vasospasm caused by various vasoactive substances (including serotonin, prostaglandins, histamine). Due to its high lipophilicity, it penetrates the BBB.
It has virtually no effect on conductivity in the sinoatrial and atrioventricular nodes, as well as myocardial contractility. Reflexively increases heart rate in response to vasodilation.
In patients with acute cerebrovascular accidents, nimodipine, by dilating cerebral vessels, improves cerebral circulation. In this case, additional perfusion is usually expressed in damaged areas and in areas of the brain with insufficient blood supply. The use of nimodipine can significantly reduce mortality and the incidence of ischemic neurological disorders associated with subarachnoid hemorrhage.
Drug interactions
Xenobiotics that affect the activity of the CYP3A4 isoenzyme may alter the metabolic clearance of nimodipine.
Based on the experience of using nifedipine, it can be expected that rifampicin, by inducing the activity of liver enzymes, can accelerate the metabolism of nimodipine and, when used simultaneously, the effectiveness of nimodipine is reduced.
Previous long-term administration of microsomal oxidation inducers (phenobarbital, phenytoin or carbamazepine) increases the metabolism of nimodipine.
Grapefruit juice inhibits the metabolism of dihydropyridines. The combination of grapefruit juice and nimodipine should be avoided because this may result in unpredictable increases in nimodipine plasma concentrations.
Concomitant use of nimodipine with cimetidine or valproic acid may also lead to increased plasma concentrations of nimodipine.
The combined use of nimodipine and fluoxetine is accompanied by an increase in the concentration of nimodipine in plasma (by 50%), while the concentration of fluoxetine is significantly reduced, and the concentration of its active metabolite norfluoxetine remains unchanged.
Simultaneous long-term use of nimodipine and nortriptyline leads to a slight decrease in the concentration of nimodipine (while the concentration of nortriptyline in the blood plasma does not change).
In patients on long-term therapy with haloperidol, no drug interactions between nimodipine and haloperidol were detected.
Nimodipine, when administered simultaneously intravenously with zidovudine, leads to a significant increase in the AUC of the latter and a decrease in its Vd and clearance.
Suppresses the metabolism of prazosin and other alpha-blockers, as a result of which the hypotensive effect may be enhanced.
In patients taking antihypertensive drugs (diuretics, beta-blockers, ACE inhibitors, angiotensin II receptor antagonists, other BMCCs, alpha-blockers, methyldopa, sympatholytics and others), the appointment of Nimopin enhances the severity of the hypotensive effect. Because of this, intravenous administration of beta-blockers is unacceptable during the use of nimodipine.
Caution should be used concomitantly with disopyramide, flecainide, procainamide, quinidine and other drugs that cause prolongation of the QT interval (possible increased severity of negative inotropic effects and prolongation of the QT interval).
Co-administration of potentially nephrotoxic drugs (for example, aminoglycosides, cephalosporins, furosemide) with nimodipine can lead to impaired renal function. If their simultaneous use is necessary, as well as in patients with renal failure, treatment should be carried out under careful monitoring of renal function. If renal dysfunction is detected, nimodipine should be discontinued.
Strengthens the arrhythmogenic effect of drugs that promote the excretion of potassium ions.
Increases the risk of developing side effects of cardiac glycosides, quinidine, carbamazepine, cyclosporine, theophylline, valproic acid, lithium preparations.
The hypotensive effect is enhanced when administered simultaneously with inhalational anesthetics.
The hypotensive effect is reduced by sympathomimetics, NSAIDs (suppression of prostaglandin synthesis, sodium and fluid retention in the body), estrogens (fluid retention in the body).
Dosage regimen
The drug is taken orally, regardless of food intake. The tablets should be swallowed whole with a small amount of liquid. The intervals between doses should be at least 4 hours.
In the absence of other prescriptions, it is recommended to follow the following dosage regimen:
- subarachnoid hemorrhage after aneurysm rupture: the recommended dose is 60 mg 6 times a day for 7 days (after infusion therapy with nimodipine solution).
- impaired brain function in elderly patients: the recommended dose is 30 mg 3 times a day.
Overdose
In case of an acute overdose of the drug, the following symptoms may occur: a significant decrease in blood pressure, tachycardia or bradycardia, epigastric pain, various neurological disorders.
Treatment: if symptoms of acute overdose appear, the use of nimodipine should be stopped immediately. Emergency measures for overdose are determined by its symptoms. If there is a significant decrease in blood pressure, dopamine or norepinephrine should be administered intravenously. Because Specific antidotes for nimodipine are unknown; further treatment of other symptoms of overdose should be symptomatic. First aid includes gastric lavage and activated charcoal.
Side effect
Allergic reactions: skin itching, rash.
From the cardiovascular system: decreased blood pressure, bradycardia or tachycardia, arrhythmias, facial skin flushing, development or worsening of existing heart failure and myocardial ischemia (especially in patients with severe obstructive lesions of the coronary arteries).
From the digestive system: nausea, diarrhea or constipation, flatulence, dry mouth, changes in appetite (usually increased), gum hyperplasia (bleeding, pain, swelling), in rare cases - paralytic ileus.
From the nervous system: headache, dizziness, asthenia, extrapyramidal disorders (ataxia, masked face, muscle rigidity, tremor, difficulty swallowing), symptoms of central nervous system arousal (insomnia, increased motor activity, agitation, aggressiveness), depression, excessive fatigue, drowsiness .
From the hematopoietic system: thrombocytopenia, agranulocytosis.
From the respiratory system: difficulty breathing, cough, wheezing.
From the musculoskeletal system: pain and swelling of the joints.
Effect on laboratory parameters: increased activity of liver transaminases, alkaline phosphatase and GGT, increased urea concentration in blood plasma, hypercreatininemia.
Other: peripheral edema, increased sweating, decreased renal function, galactorrhea, weight gain.
special instructions
The prescription of nimodipine to elderly patients with a large number of concomitant diseases, severe renal failure (GFR less than 20 ml/min) and severe cardiovascular diseases should be especially carefully justified. During therapy and after its completion, such patients require regular medical supervision (including neurological).
In patients with impaired liver function, due to a decrease in the intensity of the pronounced “first pass” effect through the liver and a slowdown in metabolic inactivation, the bioavailability of nimodipine may increase. As a result, the main and side effects of nimodipine, in particular its hypotensive effect, may increase. In such cases, the dose of the drug should be reduced depending on the degree of reduction in blood pressure, and if necessary, the use of nimodipine should be discontinued.
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