Corinfar retard: instructions for use. Corinfar: instructions for use and reviews From the respiratory system
Description of the dosage form
Round, biconvex yellow film-coated tablets.
View in the fracture - a homogeneous mass of yellow.
Pharmacodynamics
Selective BPC, a derivative of 1,4-dihydropyridine. It has antianginal and hypotensive effects.
Reduces the current of extracellular Ca 2+ inside cardiomyocytes and smooth muscle cells of the coronary and peripheral arteries; in high doses inhibits the release of Ca 2+ from intracellular depots. In therapeutic doses, it normalizes the transmembrane Ca 2+ current, which is disturbed in a number of pathological conditions, primarily in arterial hypertension. Does not affect the tone of the veins.
It enhances coronary blood flow, improves blood supply to ischemic areas of the myocardium without the development of the "steal" phenomenon, activates the functioning of collaterals. By expanding the peripheral arteries, it reduces peripheral vascular resistance, myocardial tone, afterload and oxygen demand. Virtually no effect on the sinoatrial and AV nodes, has a weak antiarrhythmic activity. Enhances renal blood flow, causes moderate natriuresis. Negative chrono-, dromo- and inotropic action is blocked by reflex activation of the sympathoadrenal system and an increase in heart rate in response to peripheral vasodilation.
The onset of the clinical effect is 20 minutes, its duration is 12 hours.
Pharmacokinetics
Absorption - high (more than 90%). Bioavailability - 50-70%. Eating increases bioavailability. It has the effect of the first passage through the liver. With max nifedipine in plasma after a single oral dose of 1 table. (20 mg of nifedipine) is achieved after 0.9-3.7 hours and averages 28.3 ng / ml. Penetrates through the BBB and the placental barrier, excreted in breast milk. Communication with blood plasma proteins (albumins) - 95%. Completely metabolized in the liver.
Excreted by the kidneys as an inactive metabolite (60-80% of the dose), with bile (20%). T 1/2 is 2-5 hours.
There is no cumulative effect. Chronic renal failure, hemodialysis and peritoneal dialysis do not affect the pharmacokinetics.
In patients with hepatic insufficiency, the total clearance decreases and T 1/2 increases.
With prolonged use (2-3 months), tolerance to the action of the drug develops.
Corinfar retard: Indications
chronic stable angina pectoris (angina pectoris);
vasospastic angina (Prinzmetal's angina, variant angina);
arterial hypertension.
Corinfar retard: Contraindications
hypersensitivity to nifedipine and other derivatives of 1,4-dihydropyridine, or other components of the drug;
arterial hypotension (SBP below 90 mm Hg);
cardiogenic shock, collapse;
severe aortic stenosis;
chronic heart failure in the stage of decompensation;
unstable angina;
acute myocardial infarction (first 4 weeks);
pregnancy (I trimester);
lactation period;
co-administration with rifampicin.
Carefully: severe mitral valve stenosis; hypertrophic obstructive cardiomyopathy; severe bradycardia or tachycardia; sick sinus syndrome; malignant arterial hypertension; hypovolemia; severe disorders of cerebral circulation; myocardial infarction with left ventricular failure; obstruction of the gastrointestinal tract; renal and liver failure; hemodialysis; pregnancy (II and III trimesters); age up to 18 years; simultaneous reception of beta-blockers, digoxin.
Dosage and administration
inside, after eating, without chewing and drinking plenty of liquid. Simultaneous food intake delays, but does not reduce the absorption of the active substance from the gastrointestinal tract.
The dose of the drug is selected by the doctor individually in accordance with the severity of the disease and the sensitivity of the patient to the drug. For patients with concomitant severe cerebrovascular disease and in elderly patients, the dose should be reduced.
Chronic stable and vasospastic angina:
Essential hypertension: 20 mg (1 tab.) 2 times a day. With an insufficiently pronounced clinical effect, the dose of the drug is gradually increased to 40 mg (table 2) 2 times a day. The maximum daily dose is 80 mg (4 tablets).
With a 2-fold administration of the drug per day, the interval between doses should be an average of 12 hours. The minimum interval between doses of the drug is at least 4 hours.
The duration of the course of treatment is determined by the attending physician.
In cases where the drug is taken in large doses and / or for a long time, treatment should be stopped gradually in order to avoid a withdrawal syndrome.
Corinfar retard side effects
From the side of the cardiovascular system: tachycardia, arrhythmia, palpitations, peripheral edema (ankles, feet, legs), manifestation of excessive vasodilation (asymptomatic decrease in blood pressure, development or aggravation of heart failure, flushing of the face, skin flushing, feeling hot), marked decrease in blood pressure (rarely), syncope . In some patients, especially at the beginning of treatment or with an increase in dose, angina attacks may occur, and in rare cases, the development of myocardial infarction, which requires discontinuation of the drug.
From the nervous system: headache, dizziness, general weakness, fatigue, drowsiness; with prolonged use of the drug - paresthesia of the extremities, tremor, extrapyramidal (parkinsonian) disorders (ataxia, mask-like face, shuffling gait, tremor of the hands and fingers, difficulty swallowing), depression.
From the digestive system: dyspepsia (nausea, diarrhea or constipation), dry mouth, increased appetite; rarely - gingival hyperplasia, completely disappearing after discontinuation of the drug; with prolonged use - a violation of liver function (intrahepatic cholestasis, increased activity of transaminases.)
From the musculoskeletal system: arthritis, myalgia, swelling of the joints.
Allergic reactions: rarely - itching, urticaria, exanthema, autoimmune hepatitis, photodermatitis, anaphylactic reactions, exfoliative dermatitis.
From the side of the hematopoietic organs: anemia, leukopenia, thrombocytopenia, thrombocytopenic purpura, agranulocytosis.
From the urinary system: increase in daily diuresis in the first weeks of admission, deterioration of kidney function (in patients with renal insufficiency).
Others: rarely - visual impairment (including transient blindness at the maximum concentration of nifedipine in plasma), gynecomastia (in elderly patients, completely disappearing after withdrawal), galactorrhea, hyperglycemia, pulmonary edema, weight gain.
Overdose
Symptoms: headache, flushing of the skin of the face, prolonged pronounced decrease in blood pressure, inhibition of sinus node function, bradycardia / tachycardia, bradyarrhythmia. In severe poisoning - loss of consciousness, coma.
Treatment: symptomatic. In case of severe poisoning (collapse, suppression of the sinus node), the stomach is washed (if necessary, the small intestine), activated charcoal is prescribed. Calcium preparations are an antidote, IV administration of 10% calcium chloride or calcium gluconate is indicated, followed by switching to a long-term infusion.
With a pronounced decrease in blood pressure, a slow intravenous administration of dopamine, dobutamine, adrenaline or noradrenaline is indicated. It is recommended to monitor the content of glucose (the release of insulin may decrease) and electrolytes in the blood (K +, Ca 2+).
With the development of heart failure - in / in the introduction of strophanthin.
For conduction disorders - atropine, isoprenaline or an artificial pacemaker.
Caution is required when used in patients with malignant arterial hypertension and irreversible renal failure who are on hemodialysis, tk. possibly a significant drop in blood pressure due to vasodilation.
Interaction
With the simultaneous use of other antihypertensive drugs, as well as tricyclic antidepressants, nitrates, cimetidine, inhalation anesthetics, diuretics, the hypotensive effect of nifedipine may be enhanced.
CCBs may further enhance the negative inotropic effect of antiarrhythmics such as amiodarone and quinidine.
When combining nifedipine with nitrates, tachycardia increases.
Diltiazem inhibits the metabolism of nifedipine in the body, which may require, while prescribing these drugs, a reduction in the dose of nifedipine.
Reduces the concentration of quinidine in plasma.
Increases the concentration of digoxin and theophylline in plasma.
Rifampicin accelerates the metabolism of nifedipine; co-administration is not recommended.
With simultaneous administration with cephalosporins (for example, cefixime), the bioavailability of cephalosporins may increase by 70%.
Sympathomimetics, NSAIDs (suppression of prostaglandin synthesis in the kidneys and 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 protein binding (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 may lead to an increase in the hypotensive effect.
If necessary, the dose of vincristine is reduced, because. nifedipine inhibits its excretion from the body, which can cause an increase in side effects.
Lithium preparations can increase toxic effects (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
With the simultaneous appointment of procainamide, quinidine and other drugs that cause a 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, so 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 may lead to the interaction of this drug and nifedipine: for example, macrolides, antiviral drugs (for example, amprenavir, indinavir, nelfinavir, ritonavir or saquinavir), antifungals azole groups (ketoconazole, itraconazole or fluconazole) cause an increase in plasma concentrations of nifedipine.
Taking into account the experience of using CCB nimodipine, similar interactions with nifedipine cannot be excluded: 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.
special instructions
During the period of treatment, it is necessary to refrain from taking ethanol.
It should be borne in mind that angina pectoris may occur at the beginning of treatment, especially after the recent abrupt withdrawal of beta-blockers (the latter should be canceled gradually).
The simultaneous appointment of beta-blockers should be carried out under conditions of close medical supervision, since this may cause an excessive decrease in blood pressure, and in some cases, aggravation of symptoms of heart failure.
With severe heart failure, the drug is dosed with great care.
Diagnostic criteria for prescribing the drug for vasospastic angina are: the classic clinical picture, accompanied by an increase in the ST segment, the occurrence of ergonovine-induced angina or spasm of the coronary arteries, the detection of coronary spasm during angiography or the detection of an angiospastic component without confirmation (for example, with a different threshold of tension or with unstable angina, when ECG data indicate transient angiospasm).
For patients with severe obstructive cardiomyopathy, there is a risk of an increase in the frequency, severity of manifestation and duration of angina attacks after taking nifedipine; in this case, it is necessary to cancel the drug.
In patients with irreversible renal failure, who are on hemodialysis, who have high blood pressure and a reduced total amount of blood, the drug should be used with caution, because. a sharp drop in blood pressure is possible.
Patients with impaired liver function are closely monitored; if necessary, the dose of the drug is reduced and / or other dosage forms of nifedipine are used.
If surgery is required under general anesthesia, it is necessary to inform the anesthesiologist about the patient's treatment with nifedipine.
In in vitro fertilization, in some cases, BCC caused changes in the head of the spermatozoa, which can lead to dysfunction of the spermatozoa. In cases in which in vitro fertilization has not been performed for an unclear reason, the use of CCBs, including nifedipine, can be considered a possible cause of failure.
During treatment, it is possible to obtain a false positive result of the direct Coombs test and laboratory tests for antinuclear antibodies.
In the spectrophotometric determination of vanillylmandelic acid in urine, nifedipine can cause a falsely high result, however, nifedipine does not affect the results of tests performed using HPLC.
With caution, simultaneous treatment with nifedipine, disopyramide and flecainamide should be carried out due to a possible increase in the inotropic effect.
Influence on the ability to drive a car and other mechanisms. During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.
Calcium channel blocker
pharmachologic effect
Selective blocker of slow calcium channels (BCCC), a derivative of 1.4-dihydropyridine. It has antianginal and hypotensive effects. Reduces the current of extracellular Ca 2+ inside cardiomyocytes and smooth muscle cells of the coronary and peripheral arteries; in high doses inhibits the release of Ca 2+ from intracellular depots. In therapeutic doses, it normalizes the transmembrane Ca 2+ current, which is disturbed in a number of pathological conditions, primarily in arterial hypertension. Does not affect the tone of the veins. Enhances coronary blood flow, improves blood supply to ischemic areas of the myocardium without the development of the "steal" phenomenon, activates the functioning of collaterals. By expanding the peripheral arteries, it reduces the total peripheral vascular resistance, myocardial tone, afterload and oxygen demand. Virtually no effect on the sinoatrial and atrioventricular nodes, has antiarrhythmic activity. Enhances renal blood flow, causes moderate natriuresis. Negative chrono-, dromo- and inotropic action is blocked by reflex activation of the sympathoadrenal system and an increase in heart rate in response to peripheral vasodilation.
The time of onset of the clinical effect is 20 minutes, the duration is 12 hours.
With prolonged use (2-3 months), tolerance to the action of the drug develops.
Pharmacokinetics
Suction and distribution
Absorption is high (more than 90%). Bioavailability - 50-70%. Eating increases bioavailability. It has the effect of "first pass" through the liver. Cmax of nifedipine after a single dose of 1 tablet (20 mg of nifedipine) is achieved after 0.9-3.7 hours and averages 28.3 ng / ml.
Binding to plasma proteins (albumin) - 95%.
Penetrates through the BBB and the placental barrier, excreted in breast milk.
Metabolism and excretion
Completely metabolized in the liver.
Excreted by the kidneys as an inactive metabolite (60-80% of the dose taken). 20% - with bile. T 1/2 is 2-5 hours. There is no cumulative effect.
Pharmacokinetics in special clinical situations
Chronic renal failure, hemodialysis and peritoneal dialysis do not affect the pharmacokinetics. In patients with hepatic insufficiency, the total clearance decreases and T 1/2 increases.
Chronic stable angina (angina pectoris);
Vasospastic angina (Prinzmetal's angina, variant angina);
Arterial hypertension.
Hypersensitivity to nifedipine and other derivatives of 1,4-dihydropyridine or to other components of the drug;
Arterial hypotension (systolic pressure below 90 mm Hg);
Cardiogenic shock, collapse;
Severe aortic stenosis;
Chronic heart failure in the stage of decompensation;
Unstable angina;
Acute myocardial infarction (first 4 weeks);
I trimester of pregnancy;
lactation period;
Co-administration with rifampicin.
Caution: severe mitral valve stenosis, hypertrophic obstructive cardiomyopathy, severe bradycardia or tachycardia, SSS, malignant arterial hypotension, hypovolemia, severe cerebrovascular accident, myocardial infarction with left ventricular failure, gastrointestinal obstruction, renal and liver failure, hemodialysis, II and III trimesters of pregnancy, children and adolescence up to 18 years, the simultaneous use of beta-blockers, digoxin.
From the side of the cardiovascular system: tachycardia, arrhythmias, palpitations, peripheral edema (ankles, feet, legs), manifestations of excessive vasodilation (asymptomatic decrease in blood pressure, development or worsening of heart failure, flushing of the face, flushing of the skin of the face, a feeling of heat), a pronounced decrease in blood pressure (rarely) , syncope. In some patients, especially at the beginning of treatment or with an increase in dose, angina attacks may occur, and in isolated cases, the development of myocardial infarction, which requires discontinuation of the drug.
From the nervous system: headache, dizziness, general weakness, fatigue, drowsiness. With prolonged use of the drug in high doses - paresthesia of the extremities, tremor, extrapyramidal (parkinsonian) disorders (ataxia, mask-like face, shuffling gait, tremor 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 discontinuation of the drug. With prolonged use - abnormal liver function (intrahepatic cholestasis, increased activity of hepatic transaminases).
From the musculoskeletal system: arthritis, myalgia, swelling of the joints.
Allergic reactions: rarely - itching, urticaria, exanthema, autoimmune hepatitis, photodermatitis, anaphylactic reactions, exfoliative dermatitis.
From the hematopoietic system: anemia, leukopenia, thrombocytopenia, thrombocytopenic purpura, agranulocytosis.
From the urinary system: increase in daily diuresis in the first weeks of admission, deterioration of kidney function (in patients with renal insufficiency).
Others: rarely - visual disturbances (including transient blindness with C max nifedipine in plasma), gynecomastia (in elderly patients, completely disappearing after withdrawal), galactorrhea, hyperglycemia, pulmonary edema, weight gain.
Overdose
Symptoms: headache, flushing of the skin of the face, prolonged pronounced decrease in blood pressure, inhibition of sinus node function, bradycardia / tachycardia, bradyarrhythmia. In severe poisoning - loss of consciousness, coma.
Treatment: conducting symptomatic therapy.
In case of severe poisoning (collapse, suppression of the sinus node), the stomach is washed (if necessary, the small intestine), activated charcoal is prescribed. Calcium preparations are an antidote, IV administration of 10% calcium chloride or calcium gluconate is indicated, followed by switching to a long-term infusion.
With a pronounced decrease in blood pressure, a slow intravenous administration of dopamine, dobutamine, adrenaline or norepinephrine is indicated. It is recommended to control the content of glucose (insulin release may decrease) and electrolytes (K +, Ca 2+).
With the development of heart failure - in / in the introduction of strophanthin.
For conduction disorders, atropine, isoprenaline, or an artificial pacemaker.
Caution is required when used in patients with malignant arterial hypertension and irreversible renal failure who are on hemodialysis, tk. possibly a significant drop in blood pressure due to vasodilation.
special instructions
During the treatment period, patients should refrain from taking ethanol.
It should be borne in mind that angina pectoris may occur at the beginning of treatment, especially after the recent abrupt withdrawal of beta-blockers (the latter should be canceled gradually).
The simultaneous appointment of beta-blockers should be carried out under conditions of careful medical supervision, since this may cause an excessive decrease in blood pressure, and in some cases, aggravation of symptoms of heart failure.
With severe heart failure, the drug is dosed with great care.
Diagnostic criteria for prescribing the drug for vasospastic angina are: the classic clinical picture, accompanied by an increase in the ST segment, the occurrence of ergonovine-induced angina or spasm of the coronary arteries, the detection of coronary spasm during angiography or the detection of an angiospastic component without confirmation (for example, with a different threshold of tension or with unstable angina, when electrocardiogram data indicate transient angiospasm).
For patients with severe obstructive cardiomyopathy, there is a risk of an increase in the frequency, severity of manifestation and duration of angina attacks after taking nifedipine; in this case, it is necessary to cancel the drug.
In patients with irreversible renal failure who are on hemodialysis, with high blood pressure and reduced BCC, the drug should be used with caution, because. a sharp drop in blood pressure is possible.
Patients with impaired liver function require careful monitoring; if necessary, the dose of the drug is reduced and / or other dosage forms of nifedipine are used.
If surgery is required under anesthesia, it is necessary to inform the anesthesiologist about the patient's treatment with nifedipine.
During in vitro fertilization, in some cases, BMCC caused changes in the head of the spermatozoa, which can lead to dysfunction of the spermatozoa. In cases in which in vitro fertilization has not been performed for an unclear reason, the use of CBCC, including nifedipine, can be considered a possible cause of failure.
During treatment, it is possible to obtain a false positive result of the direct Coombs test and laboratory tests for antinuclear antibodies.
In the spectrophotometric determination of vanillyl-mandelic acid in urine, nifedipine can cause a falsely high result, however, nifedipine does not affect the results of HPLC tests.
With caution, simultaneous treatment with nifedipine, disopyramide and flecainamide should be carried out due to a possible increase in the inotropic effect.
Influence on the ability to drive vehicles and control mechanisms
During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.
With kidney failure
Use with caution in case of impaired renal function, in case of renal insufficiency.
In patients with irreversible renal failure who are on hemodialysis, with high blood pressure and a reduced total amount of blood, the drug should be used with caution, since a sharp drop in blood pressure is possible.
In violation of the functions of the liver
Use with caution in violations of liver function, in liver failure.
Patients with impaired liver function are closely monitored; if necessary, the dose of the drug is reduced and / or other dosage forms of nifedipine are used.
Use during pregnancy and lactation
It is contraindicated to use during pregnancy of the first trimester and during lactation. With caution: pregnancy (II and III trimesters).
drug interaction
With the simultaneous use of other antihypertensive drugs, as well as tricyclic antidepressants, nitrates, cimetidine, inhalation anesthetics, diuretics, the hypotensive effect of nifedipine may be enhanced.
Calcium channel blockers may further enhance the negative inotropic effect of antiarrhythmics 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 plasma.
Increases the concentration of digoxin and theophylline in plasma.
Rifampicin accelerates the metabolism of nifedipine in the body; co-administration is not recommended.
With simultaneous administration with cephalosporins (for example, cefixime), the bioavailability of cephalosporins may increase by 70%.
Sympathomimetics, NSAIDs (suppression of prostaglandin synthesis in the kidneys and 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 protein binding (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 may lead to an increase in the hypotensive effect.
If necessary, the dose of vincristine is reduced, because. nifedipine inhibits its excretion from the body, which can cause an increase in adverse reactions.
Lithium preparations can increase toxic effects (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
With the simultaneous appointment of procainamide, quinidine and other drugs that cause a 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, so it is contraindicated during treatment with nifedipine.
Nifedipine is metabolized with the participation of isoenzymes of the cytochrome P450 3A system, in connection with this, 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) ; azole antifungal agents (ketocanazole, itraconazole or fluconazole) cause an increase in plasma concentrations of nifedipine.
Taking into account the experience of using BMCC nimodipine, a similar interaction with nifedipine cannot be excluded: 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.
Inside, after eating, without chewing and drinking plenty of liquid.
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 disease 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.
Chronic stable and vasospastic angina
Essential hypertension
The drug is prescribed 20 mg (1 tab.) 2 times / day. With an insufficiently pronounced clinical effect, the dose of the drug is gradually increased to 40 mg (2 tablets) 2 times / day. The maximum daily dose is 80 mg (4 tablets / day).
With a 2-fold administration of the drug per day, the interval between doses should be an average of 12 hours. The minimum interval between doses of the drug is at least 4 hours.
The duration of the course of treatment is determined by the attending physician.
In cases where the drug is used in high doses and / or for a long time, treatment should be stopped gradually in order to avoid a withdrawal syndrome.
Storage conditions and shelf life
The drug should be stored out of the reach of children, protected from light, at a temperature not exceeding 25°C. Shelf life - 5 years.
Selective calcium channel blocker class II, dihydropyridine derivative. Causes antianginal and hypotensive effects. Relaxes the smooth muscles of blood vessels. Stops a spasm and expands coronary and peripheral arteries. Reduces peripheral resistance and slightly - myocardial contractility, reduces afterload on the heart and myocardial oxygen demand. Improves coronary blood flow, post-stenotic circulation in atherosclerotic obstructions.
Does not inhibit automatism and myocardial conduction, can cause reflex tachycardia.
Pharmacokinetics Corinfar retard
Suction
Quickly and almost completely (90-100%) is absorbed from the gastrointestinal tract. Systemic bioavailability is 50-70%.
Distribution
It binds to plasma proteins (albumin) by 95%. Cumulation is not observed.
Metabolism
Almost completely metabolized in the liver with the formation of inactive metabolites.
breeding
T 1 / 2 is 2-5 hours. 60-80% of nifedipine in the form of metabolites is excreted in the urine, the rest with feces. Less than 0.1% of the active substance is found in the urine unchanged.
Pharmacokinetics in special clinical situations
In case of impaired liver function, an increase in T 1/2 and a decrease in total plasma clearance occur.
Indications Corinfar retard
- stable angina pectoris (angina pectoris);
- angiospastic angina (Prinzmetal's angina, variant angina);
- essential arterial hypertension.
Dosing regimen Corinfar retard
Set individually.
The average dose is 20 mg 2 times / day. With insufficient severity of the clinical effect, a gradual increase in the dose of Corinfar retard to 40 mg 2 times / day is possible.
The maximum daily dose is 80 mg.
The interval between doses should not be less than 4 hours. When prescribing the drug 2 times / day, the recommended interval for taking is approximately 12 hours (morning and evening).
Tablets are taken after meals, without chewing and drinking plenty of liquid.
Side effects Corinfar retard
From the side of the cardiovascular system: at the beginning of treatment - hyperemia of the face and skin of the upper body with a feeling of heat, an increase in the frequency, duration and severity of angina pectoris; possible occurrence of a state of stupor, tachycardia, lowering blood pressure, swelling of the legs; in isolated cases - the development of myocardial infarction.
From the digestive system: rarely - nausea, feeling of fullness in the epigastrium, diarrhea; in isolated cases - an increase in the level of hepatic transaminases, allergic hepatitis, gingival hyperplasia.
From the urinary system: rarely (shortly after taking the drug at the beginning of treatment) - possibly increased urine output; in patients with impaired renal function, a temporary deterioration in renal function is possible.
Allergic reactions: skin itching, urticaria, exanthema; in isolated cases - the occurrence of exfoliative dermatitis.
From the side of the central nervous system and peripheral nervous system: at the beginning of treatment, often - transient headaches; sometimes - a state of stupor, dizziness, a feeling of fatigue, paresthesia; in isolated cases - the occurrence of tremor, mild visual impairment (especially when using the drug in high doses).
From the hematopoietic system: anemia, leukopenia, thrombocytopenia (sometimes with manifestations of purpura).
Others: transient increase in plasma glucose levels; in some cases - myalgia (especially when using the drug in high doses). Isolated cases of gynecomastia have been described (in elderly patients, especially with prolonged use of the drug).
Contraindications Corinfar retard
– cardiogenic shock;
- severe stenosis of the aortic orifice;
- unstable angina;
- acute period of myocardial infarction (during the first 4 weeks);
- pregnancy;
- lactation period (breastfeeding);
- Hypersensitivity to nifedipine.
Pregnancy and lactation Corinfar retard
Corinfar retard is contraindicated for use during pregnancy.
Nifedipine is excreted in breast milk. Data on the effect of nifedipine on an infant is not enough. Therefore, if it is necessary to use Corinfar retard during lactation, breastfeeding should be stopped.
Special instructions Corinfar retard
Caution should be exercised when prescribing Corinfar retard to patients with severe arterial hypotension (systolic blood pressure less than 90 mm Hg), chronic heart failure in the decompensation phase, as well as elderly patients over the age of 60 years and patients with severe arterial hypertension and irreversible renal failure and hypovolemia on hemodialysis (due to the high risk of a sharp drop in blood pressure).
Patients with impaired liver function Corinfar retard is prescribed only with careful medical supervision, if necessary, dose adjustment should be carried out.
Corinfar retard should be canceled gradually, since with a sudden discontinuation of the drug (especially after prolonged treatment), a withdrawal syndrome may develop, which is expressed in a sharp increase in blood pressure or in the development of myocardial ischemia.
When drinking alcohol during therapy with Corinfar retard, it is possible to slow down the speed of psychomotor reactions associated with a decrease in blood pressure.
Pediatric use
Clinical experience with the drug in children is insufficient.
Influence on the ability to drive vehicles and control mechanisms
When taking Corinfar retard, 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.
Overdose Corinfar retard
Symptoms: loss of consciousness up to the development of coma, drop in blood pressure, tachycardia or bradycardia, hyperglycemia, metabolic acidosis, hypoxia.
Treatment: artificial vomiting, gastric lavage, symptomatic therapy aimed at maintaining the activity of the cardiovascular system.
Drug interaction Corinfar retard
With the simultaneous use of Corinfar retard with other antihypertensive drugs, as well as with tricyclic antidepressants, an increase in the hypotensive effect of Corinfar retard is noted.
With the simultaneous use of Corinfar retard with nitrates, an increase in the effect of Corinfar retard on blood pressure and heart rate is noted.
With the simultaneous use of Corinfar retard with beta-blockers, a sharper drop in blood pressure may occur, in addition, cases of weakening of cardiac activity have been observed.
With the simultaneous use of Corinfar retard and cimetidine (to a lesser extent ranitidine), it is possible to enhance the effects of Corinfar retard.
With the simultaneous use of Corinfar with quinidine, in some cases, there was a decrease in the concentration of quinidine in the blood plasma, and after the abolition of Corinfar retard, a sharp increase in the concentration of quinidine in the plasma.
With the simultaneous use of Corinfar with digoxin and theophylline, in some cases, changes in the concentration of the latter in the blood plasma were noted.
Terms and conditions of storage Corinfar retard
The drug should be stored in a place protected from light. Shelf life - 3 years.
Terms of dispensing from pharmacies
The drug is released by prescription.
