Calzigard retard - instructions for use, dose, side effects, contraindications

Core tablet: active substance: nifedipine 20 mg; Excipients: lactose monohydrate 20.00 mg, starch 13.44 mg, microcrystalline cellulose 15.00 mg, polysorbate 80 mg 1.00 mg, macrogol 6000 1.00 mg, stearic acid 1.00 mg, povidone (K-30) 6, 00 mg, magnesium stearate 1.56 mg, sodium lauryl sulfate 2.00 mg.

Film coat: hypromellose (15 cps) 2.66 mg, ethyl cellulose 0.40 mg, diethyl phthalate 0.26 mg, titanium dioxide 0.26 mg, chocolate-brown varnish 0.40 mg, talc 0.02 mg.

Description:Round biconvex tablets are brown, film-coated, with a notch on one side.

Pharmacotherapeutic group:The blocker of "slow" calcium channels

ATX: & nbsp

C.08.C.A.05 Nifedipine

Pharmacodynamics:

Selective blocker of "slow" calcium channels, 1,4-dihydropyridine derivative. Has vasodilating, antianginal and hypotensive action.Reduces the current of Ca²⁺ in cardiomyocytes and smooth muscle cells of the coronary and peripheral arteries; in high doses inhibits the release of Ca²⁺ 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 Ca²⁺, disturbed 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 resistance of the vessels, myocardial tone, postload, the need for myocardium in oxygen and prolongs the duration of diastolic relaxation of the left ventricle. Virtually no effect on sinoatrial 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 SIM of the pathoadrenal system and an increase in the number of cardiac contractions in response to peripheral vasodilation.

Time of onset of the effect - 20 minutes with oral administration; duration of the effect - 12-24 hours (prolonged form of "retard").

Pharmacokinetics:Absorption is high (more than 92-98%). Bioavailability is 40-60%. Eating increases bioavailability. Has the effect of "first pass" through the liver.

Penetrates through the blood-brain barrier, excreted in breast milk.

It is completely metabolized in the liver. In the metabolism of prepaRTA isoenzymes involved SRS_3A4, SRM_3A5 and SRM_3A7. Half-life (T_1/2) is 3.8-16.9 hours. In patients with hepatic insufficiency the overall clearance decreases and increases T_1/2.

There is no cumulative effect. Chronic renal failure, hemodialysis and peritoneal dialysis do not affect the pharmacokinetics. With long-term use, tolerance to the action of the drug develops. Plasmapheresis can enhance elimination.

Indications:

Ischemic heart disease - angina of tension and rest (including - variant).

Arterial hypertension (in the form of monotherapy or in combination with other antihypertensive drugs).

Contraindications:

Hypersensitivity to nifedipine or other dihydropyridine derivatives, other components of the drug, cardiogenic shock (risk of myocardial infarction), collapse, severe aortic valve stenosis, chronic heart failure (in decompensation stage), severe arterial hypotension (systolic blood pressure below 90 mm Hg. ), acute period of myocardial infarction (within the first 4 weeks), pregnancy (within the first 20 weeks), lactation period, age under 18 (efficacy and safety not established are displayed).

Carefully:

Severe stenosis of the aortic or mitral valve mouth, hypertrophic obstructive cardiomyopathy, severe bradycardia or tachycardia, sinus node weakness syndrome, malignant hypertension, mild or moderate arterial hypotension, myocardial infarction with left ventricular failure, unstable angina,simultaneous administration of beta-blockers or cardiac glycosides, simultaneous administration of rifampicin, severe disorders of cerebral circulation, impaired liver and / or kidney function, hemodialysis (risk of arterial hypotension), advanced age, gastrointestinal obstruction, pregnancy after 20 weeks.

Pregnancy and lactation:

Nifedipine is indicated to pregnant women only if the intended benefit to the mother exceeds the potential risk to the fetus. Nifedipine not recommended for the first 20 weeks of pregnancy.

The drug is excreted in breast milk, so it is recommended to stop breastfeeding while taking the drug. Data on the use of Kalzigard retard lactating women are absent.

Dosing and Administration:

The dosage regimen is set individually, depending on the severity of the disease and the response to ongoing therapy. It is recommended to take the drug during or after a meal, with a small amount of water.

Initial dose: 1 tablet (20 mg) twice a day. If necessary, the dose may be increased.The maximum daily dose of the drug is 120 mg.

In elderly patients or patients receiving combined (antianginal or antihypertensive) therapy, if liver function is impaired, in patients with severe impaired cerebral circulation dose should be reduced.

Side effects: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 facial skin, a feeling of heat), tachycardia, palpitation, arrhythmia, peripheral edema, chest pain. Rarely - excessive decrease in blood pressure, fainting, in some patients, especially at the beginning of treatment, there may be angina attacks, which requires the drug to be withdrawn; single cases of myocardial infarction are described.

From the central nervous system: Headache, dizziness, fatigue, weakness, drowsiness. With prolonged ingestion in high doses of paresthesia of the extremities, depression, anxiety, extrapyramidal (parkinsonian) disorders (ataxia, "masky" face, shuffling gait, stiffness of the arms and legs, tremor of hands and fingers, difficulty swallowing).

From the digestive system: Dry mouth, increased appetite, indigestion (nausea, diarrhea, or constipation). Rarely, gingival hyperplasia (bleeding, soreness, swelling). With long-term admission - violations of the liver (intrahepatic cholestasis, increased activity of hepatic enzymes).

From the 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, arthralgia (rarely), puffiness of the joints, myalgia, convulsions of the upper and lower extremities.

From 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 number - transitory blindness at the maximum concentration of nifedipine in blood plasma), gynecomastia (in elderly patients, completely disappearing after drug discontinuation), hyperglycemia, galactorrhea, pulmonary edema, bronchospasm, weight gain.

Overdose:

Symptoms: headache, hyperemia of the facial skin, lowering blood pressure, suppressing the activity of the sinus node, bradycardia, arrhythmia.

Treatment: gastric lavage with the appointment of activated charcoal, symptomatic therapy aimed at stabilizing the activity of the cardiovascular system. The antidote is calcium, a slow intravenous injection of 10 % a solution of calcium chloride or calcium gluconate, followed by a switch to a long infusion.

With a marked decrease in blood pressure - intravenous dopamine or dobutamine. In conduction disorders, the administration of atropine, isoprenaline or the establishment of an artificial pacemaker is indicated. With the development of heart failure - intravenous strophanthin. Catecholamines should be used only in the case of circulatory insufficiency, life-threatening (due to their reduced efficacy, a high dosage is required, which increases the risk of an increase in the tendency to arrhythmia due to intoxication). It is recommended to monitor the blood glucose and electrolytes (potassium, calcium ions), as the release of insulin is impaired.Hemodialysis is not effective.

Interaction:

The severity of lowering blood pressure is enhanced by the simultaneous use of other antihypertensive drugs, 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 (decrease in 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, which is why monitor the clinical effect and the content of digoxin and theophylline in the blood plasma.

Inductors of microsomal liver enzymes (rifampicin and others) reduce the concentration of nifedipine.

In combination with nitrates, tachycardia increases. Hypotensive effect reduces sympathomimetics, non-steroidal anti-inflammatory drugs (suppression of synthesis Pg in kidney and delay 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 lengthening of the interval Q - T, may increase the risk of significant lengthening of the interval Q - T. Grapefruit juice inhibits the metabolism of nifedipine in the body, in connection with which, their simultaneous reception is contraindicated.

Special instructions:

During the treatment it is necessary to refrain from taking ethanol.

Discontinue drug treatment is recommended gradually.

It should be borne in mind that at the beginning of treatment angina may occur, especially after the recent abrupt cancellation of beta-blockers (the latter should be abolished gradually).

Simultaneous administration of beta-blockers should be carried out in conditions of careful medical control, as this can lead to an excessive decrease in blood pressure, and in some cases, to worsening of symptoms of heart failure.

With severe heart failure, the drug is dosed with great care.

Diagnostic criteria for prescribing the drug with vasospastic angina are: a classic clinical picture, accompanied by an increase in the segment ST, appearance ergonovine-induced angina, or coronary artery spasm, coronary spasm detection by angiography or detection angiospastic component without acknowledgment (e.g., with different threshold voltage or unstable angina, when electrocardiogram data demonstrate transient vasoconstriction).

For patients with severe obstructive cardiomyopathy, there is a risk of increased frequency, severity, and duration of angina attacks after taking nifedipine; in this case, it is necessary to cancel the drug.

In patients who are on hemodialysis, with high blood pressure, irreversible kidney deficiency, with a reduced total amount of blood, the drug should be used cautiously, there may be a sharp drop in blood pressure.

Patients with impaired liver function are carefully monitored and, if necessary, reduce the dose of the drug and / or use other dosage forms of nifedipine.

If during the therapy the patient is required to undergo surgical intervention under general anesthesia, it is necessary to inform the anesthesia doctor about the nature conducted therapy.

During treatment, positive results are possible with a direct Coombs reaction and laboratory tests on antinuclear antibodies.

Caution should be given concomitantly with disopyramide and flecainamide because of the possible increase in inotropic effect.

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

In some patients, especially at the beginning of treatment, the drug may cause dizziness, which reduces the ability to drive or other mechanisms. Further, the degree of restriction is determined depending on the individual tolerability of the preparation.

Form release / dosage:

The tablets of the prolonged action covered with a film cover of 20 mg.

Packaging:10 tablets in a blister of PVC film and aluminum foil. 3, 6 or 10 blisters for 10 tablets with instructions for use in a cardboard box.

Storage conditions:

List B. At a temperature of no higher than 30 ° C in a dry, dark place.

Keep out of the reach of children.

Shelf life:3 years. Do not use after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N014793 / 01

Date of registration:25.11.2008 / 10.07.2014

Expiration Date:Unlimited

The owner of the registration certificate:Torrent Pharmaceuticals Co., Ltd.Torrent Pharmaceuticals Co., Ltd. India

Manufacturer: & nbsp

TORRENT PHARMACEUTICALS, Ltd. India

Representation: & nbspTORRENT PHARMACEUTICALS LTD. TORRENT PHARMACEUTICALS LTD. India

Information update date: & nbsp25.11.2017

Illustrated instructions

Instructions

Calzigard® retard (Calcigard retard)