1 film-coated tablet contains:
nifedipine 10 mg
Excipients: lactose monohydrate, potato starch, microcrystalline cellulose, povidone K25, magnesium stearate
Film shell: hypromellose, macrogol 6000, macrogol 35000, quinoline yellow dye (E 104), titanium dioxide (E 171), talc.
ATC: C.08.CA05 Nifedipine
Selective blocker of "slow" calcium channels (BMCC), a derivative of 1,4-dihydropyridine. It has antianginal and hypotensive effects. Reduces the flow of extracellular Ca2 + into cardiomyocytes and smooth muscle cells of coronary and peripheral arteries; in high doses inhibits the release of Ca2 + from intracellular stores. In therapeutic doses, it normalizes the transmembrane Ca2 + current, impaired in a number of pathological conditions, primarily in arterial hypertension. Does not affect the tone of the veins.
Strengthens coronary blood flow, improves blood supply to ischemic zones of the myocardium without the development of the phenomenon of "steal", activates the functioning of collaterals. By expanding the peripheral arteries, it reduces the total peripheral vascular resistance, myocardial tone, afterload, and myocardial oxygen demand. Virtually no effect on the sinoatrial and atrioventricular nodes, has a weak antiarrhythmic activity. Increases renal blood flow, causes moderate natriuresis.
Negative chrono-, dromo- and inotropic effects are overridden by reflex activation of the sympathoadrenal system and an increase in heart rate in response to peripheral vasodilation.
The onset of the clinical effect was 20 minutes. and its duration is 4-6 hours.
Absorption - high (over 90%). Bioavailability is 50-70%. Food intake increases bioavailability. Has a "first pass" effect through the liver. The maximum concentration of nifedipine in blood plasma after a single oral intake of 2 tablets (corresponds to 20 mg of nifedipine) is reached after 1-3 hours and its value is on average 28.3 mg / ml Penetrates through the blood-brain and placental barriers, is excreted in breast milk. Communication with blood plasma proteins (albumin) - 95%. It is completely metabolized in the liver and excreted by the kidneys as an inactive metabolite (60-80% of the dose taken). 20% with bile. The half-life (T1 / 2) is 2-5 hours.
There is no cumulative effect. Chronic renal failure, hemodialysis and peritoneal dialysis do not affect pharmacokinetics.
In patients with hepatic impairment, total clearance decreases and T1 / 2 increases.With prolonged use (2-3 months), tolerance to the drug develops.
- Chronic stable angina pectoris (exertional angina),
- Prinzmetal's angina (variant angina),
- arterial hypertension.
Application during pregnancy and lactation
Corinfar is contraindicated in pregnancy.
If it is necessary to use Corinfar during lactation, the issue of stopping breastfeeding should be resolved.
- Hypersensitivity to nifedipine and other derivatives of 1,4-dihydropyridine or to other components of the drug,
- arterial hypotension (systolic blood pressure below 90 mm Hg),
- cardiogenic shock, collapse,
- chronic heart failure in the stage of decompensation,
- pronounced aortic stenosis,
- unstable angina,
- acute myocardial infarction (first 4 weeks),
- pregnancy (1 trimester),
- lactation period,
- combined use with rifampicin.
Mitral valve stenosis, hypertrophic obstructive cardiomyopathy, severe bradycardia or tachycardia, sick sinus syndrome, malignant arterial hypertension, hypovolemia, severe cerebrovascular accidents, myocardial infarction with left ventricular failure, intestinal obstruction and gastrointestinal obstruction (due to the risk of arterial hypotension), pregnancy (2nd and 3rd trimesters), age up to 18 years (efficacy and safety have not been established), concomitant use of beta-blockers, digoxin.
From the side of the cardiovascular system: tachycardia, palpitations, arrhythmias, peripheral edema (ankles, feet, legs), manifestations of excessive vasodilation (asymptomatic decrease in blood pressure, development or worsening of heart failure, "flushing" of blood to the skin of the face, hyperemia of the egg skin, feeling of heat), marked decrease in blood pressure (rarely), syncope. In some patients, especially at the beginning of treatment or with an increase in the dose, angina attacks may occur and, in isolated cases, the development of myocardial infarction, which requires discontinuation of the drug.
From the side of the central nervous system: headache, dizziness, general weakness, increased fatigue, drowsiness. With prolonged use of the drug in high doses - paresthesia of the extremities, tremors, extrapyramidal (parkinsonian) disorders (ataxia, "mask-like" face, shuffling gait, tremors of the hands and fingers, difficulty swallowing), depression.
From the digestive system: dyspepsia (nausea, diarrhea or constipation), dry mouth, flatulence, increased appetite. Rarely - gingival hyperplasia, completely disappearing after drug withdrawal. With prolonged use - liver dysfunction (intrahepatic cholestasis, increased activity of hepatic transaminases).
From the side of the musculoskeletal system: arthritis, myalgia, joint swelling, convulsions of the upper and lower extremities.
Allergic reactions: rarely - pruritus, urticaria, exanthema, autoimmune hepatitis, exfoliative dermatitis, photodermatitis, anaphylactic reactions
From the side of hematopoiesis: anemia, leukopenia, thrombocytopenia, thrombocytopenic purpura, agranulocytosis.
From the urinary system: increased daily urine output, deterioration of renal function (in patients with renal failure).
Others: rarely - visual impairment (including transient blindness with a maximum concentration of nifedipine in the blood plasma), gynecomastia (in elderly patients, completely disappearing after withdrawal), galactorrhea, hyperglycemia, pulmonary edema, bronchospasm, weight gain.
With the simultaneous use of other antihypertensive drugs, as well as tricyclic antidepressants, nitrates, cimetidine, inhalation anesthetics, diuretics, the hypotensive effect of nifedipine may increase. BMCCs can further enhance the negative inotropic effect of antiarrhythmic drugs such as amiodarone and quinidine. When combining nifedipine with nitrates, tachycardia increases.
Diltiazem inhibits the metabolism of nifedipine in the body, which may require a reduction in the dose of nifedipine while prescribing these drugs. Reduces the concentration of quinidine in blood plasma. Increases the concentration of digoxin and theophylline in blood plasma. Rifampicin accelerates the metabolism of nifedipine, co-administration is not recommended.
With simultaneous administration with cephalosporins (for example, cefixime), the concentration of cephalosporins in the blood may increase. Sympathomimetics, NSAIDs (suppression of PG synthesis in the kidneys and the retention of sodium ions and fluid in the body), estrogens (fluid retention in the body) reduce the hypotensive effect.
Nifedipine can displace drugs with a high degree of binding from the connection with proteins (including indirect anticoagulants - coumarin and indandione derivatives, anticonvulsants, NSAIDs, quinine, salicylates, sulfinpyrazone), as a result of which their concentration in blood plasma may increase.
Nifedipine inhibits the metabolism of prazosin and other alpha-blockers, which can lead to an increase in the hypotensive effect. Reduce the dose of vincristine if necessary. nifedipine inhibits its excretion from the body, which can cause increased side effects.
Lithium preparations can increase toxic effects (nausea, vomiting, diarrhea, ataxia, tremors, tinnitus). With the simultaneous administration of procainamide, quinidine and other drugs that cause prolongation of the QT interval, the risk of a significant prolongation of the QT interval increases.
Grapefruit juice inhibits the metabolism of nifedipine in the body, therefore it is contraindicated during treatment with nifedipine. Nifedipine is metabolized by the cytochrome P450 3A system; therefore, the simultaneous use of drugs that inhibit this system can lead to the interaction of this drug and nifedipine: for example, macrolides, antiviral drugs (for example, amprenavir, indinavir, nelfinavir, ritonavir or saquinavir); antifungal agents of the azole group (ketoconazole, itraconazole or fluconazole) cause an increase in the concentration of nifedipine in the blood plasma.
Taking into account the experience of using BMCC nimodipine, it is impossible to exclude similar interactions with nifedipine: carbamazepine, phenobarbital can cause a decrease in the concentration of nifedipine in the blood plasma; and valproic acid - an increase in the concentration of nifedipine in the blood plasma.
How to take, course of administration and dosage
Inside after eating, without chewing and drinking plenty of fluids.
The dose of the drug is selected by the doctor individually in accordance with the severity of the disease and the patient's sensitivity to the drug. For patients with concomitant severe cerebrovascular diseases and in elderly patients, the dose should be reduced.
Simultaneous food intake delays, but does not reduce the absorption of the active substance from the gastrointestinal tract.
Recommended dosing regimen for adults:
Chronic stable and vasospastic angina
The initial dose is 10 mg (1 tablet) 2-3 times a day. In case of insufficiently pronounced clinical effect, the dose of the drug is gradually increased to 2 tablets (20 mg) 1-2 times a day. The maximum daily dose is 40 mg (4 tablets per day).
The average daily dose is 10 mg (1 tablet) 2-3 times a day.
In case of insufficiently pronounced clinical effect, it is possible to gradually increase the dose of the drug to 20 mg (2 tablets) 2 times a day.
The maximum daily dose is 40 mg (4 tablets per day).
With a 2-fold appointment, the minimum interval between doses of the drug should be at least 4 hours.
The duration of the course of treatment is determined by the attending physician.
Symptoms: headache, facial flushing, prolonged marked decrease in blood pressure, depression of sinus node function, bradycardia / tachycardia, bradyarrhythmia.
In severe poisoning - loss of consciousness, coma. Treatment: symptomatic. In severe poisoning (collapse, oppression of the sinus node), the stomach is washed (if necessary, the small intestine), activated charcoal is prescribed. The antidote is calcium preparations, it is shown in / in the introduction of 10% calcium chloride or calcium gluconate, followed by transfer to a long infusion.
With a pronounced decrease in blood pressure, slow intravenous administration of dopamine, dobutamine, adrenaline or norepinephrine is indicated. It is recommended to monitor glucose (insulin release may decrease) and blood electrolytes (K +, Ca2 +). With the development of heart failure - in / in the introduction of strophanthin. In case of conduction disorders - atropine, isoprenaline or an artificial pacemaker. Hemodialysis is ineffective, plasmapheresis is recommended.
Caution should be exercised when prescribing Corinfar to patients with severe arterial hypotension (systolic blood pressure less than 90 mm Hg), chronic heart failure in the decompensation phase, as well as patients with severe forms of arterial hypertension and irreversible renal failure and hypovolemia, who are on hemodialysis (from - for the high risk of a sharp drop in blood pressure).
Corinfar should be canceled gradually, since with a sudden discontinuation of the drug (especially after prolonged treatment), withdrawal syndrome may develop.
When drinking alcohol against the background of Corinfar therapy, it is possible to slow down the speed of psychomotor reactions associated with a decrease in blood pressure.
Application for violations of liver function: Corinfar should be prescribed under close supervision to patients with impaired liver function. If necessary, the dose of the drug should be reduced.
When taking Corinfar, especially at the beginning of treatment and when changing the drug, it is possible to slow down the speed of psychomotor reactions associated with a decrease in blood pressure. This must be taken into account by persons engaged in potentially hazardous activities that require increased attention and speed of psychomotor reactions.