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

Excipients: lactose monohydrate 31.60 mg, potato starch 31.40 mg, microcrystalline cellulose 31.00 mg, povidone K 25 5.40 mg, magnesium stearate 0.60 mg; film sheath: hypromellose 5,188 mg, macrogol 6000 0.861 mg, macrogol 35000 0.393 mg, quinoline yellow (E 104) dye 0.143 mg, titanium dioxide (E 171) 1.377 mg, talc 1.038 mg.

Description:Round, biconcave film-coated tablets yellow color. View at break: homogeneous mass of yellow colors.

Pharmacotherapeutic group:The blocker of "slow" calcium channels

ATX: & nbsp

C.08.C.A.05 Nifedipine

Pharmacodynamics:

Selective blocker of "slow" calcium channels (BCCC), a derivative of 1,4-dihydropyridine. Has antianginal and hypotensive effect. Reduces the current of extracellular Ca²⁺ inside cardiomyocytes and smooth muscle cells of the coronary and peripheral arteries; in high doses inhibits the release of Ca²⁺ from the intracellular depot. 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 vascular resistance, myocardial tone, postnagruzku and the need for oxygen. Virtually does not affect the sinoatrial and atrioventricular nodes, has a weak 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.

Time of onset of clinical effect is 20 min. and its duration is 12 hours.

Pharmacokinetics:Absorption is high (more than 90%).Bioavailability is 50-70%. Eating increases bioavailability. Has the effect of "first pass" through the liver. The maximum concentration of nifedipine in the blood plasma after a single dose 1 tablet (20 mg of nifedipine) is achieved after 0.9-3.7 hours and its value is on average 28.3 mg / ml. Penetrates through blood-brain and placental barriers, excreted in breast milk. The connection with blood plasma proteins (albumins) is 95%. It is completely metabolized in the liver.

It is excreted by the kidneys in the form of an inactive metabolite (60-80% of the dose taken). 20% - withfritter. The half-life (T1 / 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 overall clearance decreases and increases T1 / 2.

At long reception (2-3 months) tolerance to action of a preparation develops.

Indications:

- Chronic stable angina (stress angina),

- vasospastic angina (Prinzmetal angina, variant angina),

- arterial hypertension.

Contraindications:

- Hypersensitivity to nifedipine and other 1,4-dihydropyridine derivatives, 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);

- pregnancy (1 trimester);

- lactation period;

- combined use with rifampicin.

Carefully:Severe mitral valve stenosis, hypertrophic obstructive cardiomyopathy, severe bradycardia or tachycardia, sinus node weakness syndrome, malignant hypertension, giupovolemia, severe circulatory disorders, myocardial infarction with left ventricular failure, gastrointestinal obstruction, renal and hepatic insufficiency, hemodialysis, pregnancy (2 and 3 trimesters), age to 18 years, simultaneous reception of beta-adrenoblockers, digoxin.

Dosing and Administration:

Inside after eating, without chewing and washing down with a sufficient amount of liquid.

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.

Simultaneous intake of food 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:

Essential hypertension:

The drug is prescribed for 20 mg (1 tablet) 2 times a day. With an insufficiently pronounced clinical effect, the dose of the drug is gradually increased to 40 mg (2 tablets) 2 times a day. The maximum daily dose is 80 mg (4 tablets per 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 is not less than 4 hours.

The duration 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 discontinued gradually to avoid withdrawal syndrome.

Side effects:

From the side of the cardiovascular system: tachycardia, arrhythmias, palpitations, peripheral edema (ankles, feet, shins), manifestations of excessive vasodilation (asymptomatic decrease in blood pressure, development or aggravation of heart failure, flushing of the skin to the skin of the face, skin hyperemia, heat), marked decrease in blood pressure ), syncope. In some patients, especially at the beginning of treatment or with an increase in the dose, there may be angina attacks, and in some cases - the development of myocardial infarction, which requires the withdrawal of the drug.

From the nervous system: headache, dizziness, general weakness, increased fatigue, drowsiness. With long-term use of the drug in high doses - paresthesia of limbs, tremor, extrapyramidal (parkinsonian) disorders (ataxia, masky face, shuffling gait, tremor of 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 admission - violations of the liver (intrahepatic cholestasis, increased activity of transaminases).

From the musculoskeletal system: arthritis, myalgia, puffiness of the joints Allergic reactions: rarely - itching, urticaria, exanthema, autoimmune hepatitis, photodermatitis, anaphylactic reactions, exfoliative dermatitis.

From the hematopoiesis: anemia, leukopenia, thrombocytopenia, thrombocytopenic purpura, agranulocytosis.

From the urinary system: an increase in daily diuresis in the first weeks of admission, impaired renal function (in patients with renal insufficiency).

Other: rarely - visual impairment (ie transient blindness with a maximum concentration of nifedipine in plasma), gynecomastia (in elderly patients, completely disappearing after withdrawal), galactorrhea, hyperglycemia, pulmonary edema, weight gain.

Overdose:

Symptoms: headache, hyperemia of the facial skin, prolonged pronounced decrease in blood pressure, suppression 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), gastric lavage is performed (if necessary, the small intestine), appoint Activated carbon. Antidote are calcium preparations, shown in / in the administration of 10% calcium chloride or calcium gluconate, followed by a switch to a long infusion.

With a marked decrease in blood pressure, a slow intravenous injection of dopamine, dobutamine, epinephrine, or norepinephrine is indicated. It is recommended to monitor the glucose content (insulin release may decrease) and electrolytes in the blood (K +, Ca2 +).

With the development of heart failure - in / in the introduction of strophanthin.

In the case of conduction disturbances - atropine, isoprenaline or an artificial pacemaker.

Hemodialysis is not effective, plasmapheresis is recommended.

Caution is required when used in patients with malignant hypertension and irreversible renal failure on hemodialysis, since a significant drop in arterial pressure due to vasodilation is possible.

Interaction:

- With the simultaneous use of other antihypertensive drugs,as well as tricyclic antidepressants, nitrates, cimetidine inhalational anesthetics, diuretics, the hypotensive effect of nifedipine may be enhanced.

- The blockers of "slow" calcium channels can further increase 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 the simultaneous administration of these drugs to reduce the dose of nifedipine.

- Reduces the concentration of quinidine in the blood plasma.

- Increases the concentration of digoxin and theophylline in the blood plasma.

- Rifampicin accelerates the metabolism of nifedipine, joint use is not recommended.

- With concomitant administration with cephalosporins (eg, cefixime) can increase the bioavailability of cephalosporins by 70%.

- Sympathomimetics, non-steroidal anti-inflammatory drugs (suppression of prostaglandin synthesis in the kidneys and retention of sodium and liquid ions in the body), estrogens (fluid retention in the body) reduce the hypotensive effect.

- Nifedipine can displace from the bond with proteins preparations with a high degree of binding (including indirect anticoagulants - coumarin derivatives and. indandion, anticonvulsant, non-steroidal anti-inflammatory drugs, quinine, salicylates, sulfinpyrazone), so that their concentration in the blood plasma can increase.

- Nifedipine inhibits the metabolism of prazosin and other alpha-adrenoblockers, which can lead to an increase in the hypotensive effect.

- If necessary, the dose of vincristine is reduced, because nifedipine inhibits its removal from the body, which can cause increased side effects.

- Lithium preparations can enhance toxic effects (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).

- With the simultaneous administration of procainamide, quinidine and other drugs that cause lengthening of the interval QT, risk of significant lengthening of the interval QT 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, so 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); 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 BIMC nimodipine, it is impossible to exclude similar interactions with nifedipine: carbamazepine, phenobarbital can cause a decrease in the concentration of nifedipine in blood plasma; a valproic acid - Increase in the concentration of nifedipine in blood plasma.

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, the occurrence of ergon-induced angina pectoris or spasm of the coronary arteries, the detection of coronarospasm in angiography or the detection of an angiospastic component without confirmation (for example, at a different threshold of stress, or in unstable angina when the electrocardiogram data indicate transient angiospasm).

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 with irreversible renal failure who are on hemodialysis, who have high blood pressure and reduced total blood, the drug should be used cautiously, since it is possible a sharp drop in blood pressure.

For patients with impaired liver function, careful monitoring is established; if necessary, the dose of the drug is reduced and / or used by other dosage forms of nifedipine.

If surgical intervention is required under general anesthesia, the anesthetist should be informed of the patient's treatment with nifedipine.

In case of in vitro fertilization, in some cases BCCC caused changes in the head part of spermatozoa, which can lead to a disruption of the functions of spermatozoa. In cases in which repeated in vitro fertilization has not been carried out for an unclear reason, the use of BCCC, including nifedipine, can be considered a possible cause of failure.

During treatment, it is possible to obtain a false positive result of the Coombs direct reaction and laboratory tests for antinuclear antibodies.

When spectrophotometric determination of vanillyl-mandelic acid in the urine nifedipine may be the reason for obtaining a false-overestimated result, however, the results of tests performed with HPLC, nifedipine influence does not render.

Caution should be given to simultaneous treatment with nifedipine,disopyramide and flecainamide because of the possible enhancement of the inotropic effect.

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

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets of prolonged action of 20 mg, film-coated.

Packaging:

For 10 tablets per blister (PVC / aluminum).

For 3 blisters in a cardboard box together with instructions for use.

For 50 or 100 tablets in a bottle of brown glass with a white stopper made of PE of low density with a relief inscription "AWD".

1 bottle per cardboard pack together with instructions for use.

Storage conditions:

List B.

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:5 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N015327 / 01

Date of registration:14.05.2009 / 11.09.2012

Expiration Date:Unlimited

The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel

Manufacturer: & nbsp

PLIVA HRVATSKA, d.o.o. Croatia

Representation: & nbspTeva Teva Israel

Information update date: & nbsp04.02.2018

Illustrated instructions

Instructions

Corinfar® retard (Corinfar® retard)