Composition, form of production and packaging
The tablets covered with a film cover of yellow color, round, biconcave.
1 tab.
nifedipine 10 mg
Auxiliary substances: potato starch, gelatin, lactose, microcrystalline cellulose, magnesium stearate, talc.
Sheath composition: hypromellose, macrogol 6000, quinoline yellow (E104) varnish, titanium dioxide, talc, propylene glycol.
25 pcs. - blisters (2) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2012.
PHARMACHOLOGIC EFFECT
Selective blocker of "slow" calcium channels, derivative of 1,4-dihydropyridine. Has vasodilating, antianginal and hypotensive action. Reduces the current of calcium ions in cardiomyocytes and smooth muscle cells of the coronary and peripheral arteries; in high doses, suppresses the release of calcium ions from the intracellular depot. Reduces the number of functioning channels, without affecting the time of their activation, inactivation and recovery. Separates the processes of excitation and contraction in the myocardium mediated by tropomyosin and troponin, and in smooth muscles of vessels, mediated by calmodulin. In therapeutic doses normalizes the transmembrane current of calcium ions, disrupted in a number of pathological conditions, especially in hypertension. Does not affect the tone of the veins. Strengthens the coronary blood flow, improves the blood supply of the ischemic zones of the myocardium without the development of the phenomenon of "stealing", activates the functioning of collaterals. Expanding the peripheral arteries, reduces the overall peripheral vascular resistance, myocardial tone, postload, myocardial oxygen demand and prolongs the diastolic relaxation of the left ventricle (LV). Virtually does not affect the sinouauricular and atrioventricular nodes and does not have antiarrhythmic activity. It enhances kidney blood flow, causes a moderate natriuresis. Negative chrono-, dromo- and inotropic action is blocked by reflex activation of the sympathoadrenal system and an increase in the heart rate in response to peripheral vasodilation. The effect occurs after 20 minutes - when taking the drug inside, the duration of the effect is 4-6 hours.
PHARMACOKINETICS
Nifedipine is almost completely absorbed into the digestive tract (more than 90%). Absolute bioavailability is 40 - 70%. Nifedipine undergoes intensive metabolism during the "first passage" through the liver (40-60%). After ingestion of 1 tablet 10 mg the maximum concentration of the drug in the blood plasma is reached after 30 - 60 minutes. Half-life is 2 to 4 hours. The association of nifedipine with plasma proteins (albumins) is 94 - 97%. The active substance penetrates the placental barrier and is excreted into breast milk. Less than 5% of the administered dose penetrates the blood-brain barrier. Nifedipine is generally metabolized to 3 pharmacologically inactive metabolites, and in this form, approximately 60-80% of the administered dose is excreted in the urine. The rest of the dose is excreted through the bile ducts and with feces.
INDICATIONS
- ischemic heart disease - for the prevention of seizures with various forms of angina pectoris, including vasospastic angina (Prinzmetal angina);
- arterial hypertension (monotherapy or in combination with other antihypertensive drugs).
DOSING MODE
Kordafen В® tablets are for oral use. Accepted regardless of food intake. Tablets should be swallowed whole, washed down with a small amount of liquid.
The initial dose is 10 mg (1 tablet) 3 times a day. If necessary, the dose can be increased to 20 mg 2 times a day under the control of blood pressure. The maximum daily dose is 40 mg.
In elderly patients or patients receiving combined (antianginal or antihypertensive) therapy, as well as in violation of liver function, in patients with severe impairment of cerebral circulation, the dose should be reduced. In patients requiring higher doses of nifedipine, the drug should be used in long-acting dosage forms.
SIDE EFFECT
From the side of the cardiovascular system: manifestations of excessive vasodilation (asymptomatic decrease in blood pressure, development or exacerbation of heart failure, "flushing" of blood to the skin of the face, hyperemia of the skin of the face, a feeling of heat), tachycardia, palpitation, arrhythmia, peripheral edema, retrosternal pain; rarely - excessive reduction in blood pressure, fainting, in some patients, especially at the beginning of treatment, there may be angina attacks, which requires the withdrawal of the drug. Single cases of myocardial infarction are described.
From the side of the central nervous system: headache, dizziness, fatigue, weakness, drowsiness. With prolonged ingestion in high doses - paresthesia of the extremities, depression, anxiety, extrapyramidal (parkinsonian) disorders (ataxia, "masky" face, shuffling gait, stiffness of the arms and legs movements, tremor of hands and fingers, difficulty swallowing).
On the part of the digestive system: dry mouth, increased appetite, indigestion (nausea, diarrhea, or constipation); rarely - gingival hyperplasia (bleeding, soreness, swelling), with prolonged admission - violations of the liver (intrahepatic cholestasis, increased activity of "liver" enzymes).
On the part of the organs of hematopoiesis: anemia, asymptomatic agranulocytosis, thrombocytopenia, thrombocytopenic purpura, and leukopenia.
Allergic reactions: rarely - skin itching, hives, exanthema, exfoliative dermatitis, photodermatitis; very rarely - autoimmune hepatitis.
From the musculoskeletal system: arthritis, rarely - arthralgia, swelling of the joints, myalgia, convulsions of the upper and lower extremities.
On the part of the urinary system: an increase in daily diuresis, impaired renal function (in patients with renal insufficiency).
Other: rarely - difficulty breathing, cough; very rarely - visual impairment (including transient blindness with maximum concentration of nifedipine in blood plasma), gynecomastia (in elderly patients, completely disappearing after drug discontinuation), hyperglycemia, galactorrhea, pulmonary edema, bronchospasm, weight gain.
CONTRAINDICATIONS
- hypersensitivity to nifedipine (and other dihydropyridine derivatives) or other components of the drug;
- cardiogenic shock, collapse, severe aortic stenosis, unstable angina;
- after a previous myocardial infarction (the first 4 weeks);
lactose intolerance;
- age under 18 years (efficiency and safety not established);
- arterial hypotension (systolic blood pressure less than 90 mm Hg), chronic heart failure in the stage of decompensation, syndrome of weakness of the sinus node, pregnancy (up to 20 weeks), lactation.
With caution: severe stenosis of the aortic or mitral valve mouth, hypertrophic obstructive cardiomyopathy, severe bradycardia or tachycardia, sinus node weakness syndrome, malignant hypertension, myocardial infarction with left ventricular failure, unstable angina, simultaneous administration of beta-blockers or cardiac glycosides, simultaneous reception of rifampicin , severe disorders of cerebral circulation, impaired liver and / or kidney function, hemodialysis (risk of arterial hypotension), advanced age.
PREGNANCY AND LACTATION
The administration of nifedipine to pregnant women is only indicated if the intended benefit to the mother exceeds the potential risk to the fetus. Nifedipine is not recommended in the 1st trimester of pregnancy (up to 20 weeks). The drug is excreted in breast milk, so it is recommended to stop breastfeeding while taking the drug.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution should apply the drug for violations of kidney function, with the dose should be reduced.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should apply the drug for violations of liver function, with the dose should be reduced.
APPLICATION FOR CHILDREN
Contraindicated for children under 18 years of age (efficacy and safety not established).
APPLICATION IN ELDERLY PATIENTS
Caution should be used in elderly people, and the dose should be reduced.
SPECIAL INSTRUCTIONS
The drug can enhance the symptoms of IHD, cause manifestations of acute myocardial infarction, especially in patients, at the beginning of treatment or with an increase in the dose of the drug.
Patients who took beta-blockers should not abruptly discontinue treatment with these drugs (prior to initiation of nifedipine therapy), in view of the possibility of increasing the symptoms of myocardial ischemia.
It should be used with caution in patients with heart failure, aortic stenosis, especially with concomitant treatment with beta-blockers. nifedipine may accelerate the manifestation or worsen the already existing symptoms of heart failure. Pay attention to peripheral edema.
Nifedipine, reducing the overall vascular peripheral resistance, can cause severe arterial hypotension, so you should carefully monitor blood pressure, especially in the initial period of treatment and after increasing the dose of the drug.
Nifedipine, used for a long time, can enhance the symptoms of coronary heart disease, cause myocardial infarction, and increase the death rate of patients with arterial hypertension or chronic coronary heart disease.
Nifedipine can be used in patients with intolerance or resistance to organic nitrates.
If during the therapy the patient is required to undergo surgery under general anesthesia, it is necessary to inform the anesthetist about the nature of the therapy.
Influence of the drug on driving and management of vehicles
When taking Cordafen В® , especially at the beginning of treatment, it is possible to slow down the reaction rate associated with lowering blood pressure.
This should be taken into account by persons engaged in potentially hazardous activities requiring increased attention and speed of psychomotor reactions.
OVERDOSE
Symptoms: headache, hyperemia of the facial skin, prolonged pronounced decrease in blood pressure, inhibition of sinus node function, bradycardia, bradyarrhythmia.
Treatment: with severe poisoning (collapse, suppression of the sinus node), gastric lavage is performed, activated charcoal is administered. Antidote are preparations of calcium ions: a slow intravenous injection of a 10% solution of calcium chloride or calcium gluconate is shown, followed by a switch to a long infusion. With a pronounced decrease in blood pressure - iv injection of dopamine or dobutamine. In conduction disorders - atropine, isoprenaline or an artificial pacemaker. With the development of heart failure - in / in the introduction of strophanthin. Catecholamines should be used only with a life threat (due to their reduced efficacy, a high dosage is required, which increases the risk of arrhythmia). It is recommended to monitor the concentration of glucose in the blood (insulin release may decrease) and electrolytes (potassium and calcium ions). Hemodialysis is ineffective.
DRUG INTERACTION
The severity of lowering blood pressure is enhanced by the simultaneous use of other antihypertensive agents, nitrates, cimetidine (to a lesser extent ranitidine), inhalational anesthetics and tricyclic antidepressants.
Drugs from the group of "slow" calcium channel blockers can further increase the negative inotropic effect (reducing the force of cardiac contraction) of antiarrhythmics such as amiodarone and quinidine. Nifedipine causes a decrease in the concentration of quinidine in the blood plasma, after the withdrawal of nifedipine, a sharp increase in the concentration of quinidine can occur. Increases the plasma concentration of digoxin and theophylline, and therefore it is necessary to monitor the clinical effect and the content of digoxin and theophylline in the blood plasma.
Inductors of microsomal liver enzymes (rifampicin, etc.) reduce the concentration of nifedipine.
In combination with nitrates, tachycardia increases. The hypotensive effect is reduced by sympathomimetics, non-steroidal anti-inflammatory drugs (suppression of Pg synthesis in the kidneys and retention of Na + and fluid in the body), estrogens (fluid retention in the body). Calcium preparations can reduce the effect of blockers of "slow" calcium channels.
Nifedipine can displace drugs that are highly binding (including indirect anticoagulants, coumarin and indanedione derivatives, anticonvulsant drugs, nonsteroidal anti-inflammatory drugs, quinine, salicylates, sulfinpyrazone) from the association with proteins, and as a result, their concentration in the blood plasma can increase .
Suppresses the metabolism of prazosin and other alpha-adrenoblockers, as a result of which the hypotensive effect may increase.
Nifedipine inhibits the excretion of vincristine from the body and may cause an increase in side effects of vincristine, if necessary, reduce the dose of vincristine.Lithium preparations can enhance toxic effects (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
Procainamide, quinidine and other drugs that cause prolongation of the Q-T interval may increase the risk of a significant prolongation of the Q-T interval. Grapefruit juice inhibits the metabolism of nifedipine in the body, in connection with which, their simultaneous reception is contraindicated.
TERMS OF RELEASE FROM PHARMACY
On prescription.
TERMS AND CONDITIONS OF STORAGE
In a dry, protected from light place at a temperature of no higher than 25 В° C. Keep out of the reach of children.
Shelf life - 3 years.
