Cordaflex - instructions for use, dose, side effects, contraindications

Each tablet, coated with a shell, contains active ingredient: nifedipine 10 mg. and Excipients: polyvinyl butyral, magnesium stearate, talc, hydroxypropyl cellulose, croscarmellose sodium, lactose monohydrate, microcrystalline cellulose, titanium dioxide, iron oxide yellow, hypromellose.

Description:Biconvex round, covered with a matte or slightly shiny coating tablets, yellow, with a weak characteristic odor.

Pharmacotherapeutic group:The blocker of "slow" calcium channels

ATX: & nbsp

C.08.C.A.05 Nifedipine

Pharmacodynamics:Nifedipine is a selective blocker of "slow" calcium channels, the 1,4-dihydropyridine derivative. Has antihypertensive and antianginal action. Reduces the current of extracellular calcium ions inside cardiomyocytes and smooth muscle cells of the coronary and peripheral arteries.In therapeutic doses normalizes the transmembrane current of calcium ions, disrupted in a number of pathological conditions, especially in hypertension. Reduces spasm and dilates coronary and peripheral arterial vessels, reduces overall peripheral resistance, reduces afterload and myocardial oxygen demand. At the same time it improves the blood supply of the ischemic zones of the myocardium without the development of the syndrome of "stealing", and also increases the number of functioning collaterals. Practically nc affects the sinoatrial and atrioventricular nodes and does not have both pro- and antiarrhythmic effects. Does not affect the tone of the veins. Nifedipine strengthens the renal blood flow, causing a moderate sodium naresis. In high doses, it inhibits the release of calcium ions from intracellular stores. Reduces the number of functioning rope cables, without affecting the time of their activation, inactivation and recovery.

Pharmacokinetics:

Nifedipine is almost completely absorbed in the gastrointestinal tract (more than 90%). Absolute bioavailability is 40 - 70%. Nifedipine is subjected to intensive metabolism at 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 -2-4 hours. The association of nifedipine with plasma proteins (albumins) is 94 - 97%. Studies with labeled nifedipine in animals have shown that unrelated nifedipine distributed in all organs and tissues. It was found that the concentration of nifedipine is higher in the myocardium than in the skeletal muscles. There is no cumulative effect.

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 completely metabolized into inactive metabolites and in this form 60-80% of the dose taken internally is excreted in the urine, the rest - with bile and feces. The half-life of nifedipine from plasma is approximately 2 hours.

Indications:

Arterial hypertension, including hypertensive crises

Ischemic heart disease: stable angina (stress angina), vasospastic angina (Prinzmetal angina)

Contraindications:

Hypersensitivity to nifedipine or any other component of the drug, other 1,4-dihydropyridine derivatives.

Severe arterial hypotension (systolic blood pressure is lower than 99 mm Hg).

Unstable angina.

Acute myocardial infarction (first 4 weeks).

Severe aortic stenosis, idiopathic subaortic stenosis.

Chronic heart failure in the stage of decompensation.

Carefully:

Severe mitral valve stenosis, hypertrophic obstructive cardiomyopathy, chronic heart failure, severe circulatory disorders, sinus node weakness syndrome, severe tachycardia, advanced age, renal and hepatic insufficiency (especially patients on hemodialysis - a high risk of excessive and unpredictable lowering of blood pressure) , age under 18 years (efficacy and safety not established), lactose intolerance.

Pregnancy and lactation:

The use of nifedipine in pregnant women is recommended when it is not possible to use other drugs that do not have limitations.

Because the nifedipine excreted in breast milk, should refrain from prescribing during lactation, or stop breastfeeding during treatment.

Dosing and Administration:

The dosage regimen is set individually, depending on the degree of severity of the disease and the patient's response to ongoing therapy.

The tablets covered with a cover, it is necessary to swallow entirely before meal, without chewing, with a small amount of water.

Initial dose: 1 tablet (10 mg) 3 times a day. If necessary, the dose of the drug can be increased to 2 tablets (20 mg) - 1-2 times a day.

Between the two methods of the drug should take at least 2 hours.

The maximum daily dose of the drug is 40 mg.If you need to increase the dose to 80 - 120 mg for the treatment of angina or hypertension, it is recommended to transfer the patient to the drug Kordaflex tablets prolonged action, coated, 20 mg.

To accelerate the effect of the drug at the beginning of the development of an attack of angina or hypertensive crisis, the tablet should be chewed, held for a while in the mouth, and then swallowed with a small amount of water.

In elderly patients, the pharmacokinetics of nifedipine is altered, so that, in order to maintain a sufficient therapeutic effect, lower dose.

When reducing renal or hepatic function, it is recommended to use with caution the same doses as with normal kidney or liver function (tolerance development is possible). With a significant decrease in liver function, it is not recommended to take a dose of more than 40 mg during the day.

Side effects:

Side effects often occur early in the course of treatment and may disappear over a further course.

The cardiovascular system: hyperemia of the facial skin, pronounced lowering of arterial pressure, tachycardia, peripheral edema (ankles, feet, shins); rarely - the appearance of attacks of angina (which is typical for other vasodilators and requires the withdrawal of the drug), heart failure, syncope.

Central nervous system: headache, dizziness, fatigue, sleep disturbances (drowsiness or insomnia), extremely rarely: mood lability. With prolonged use in high doses - paresthesia in the extremities, tremor.

Digestive system: nausea, heartburn, diarrhea, or constipation; rarely with long-term administration of the drug - dry mouth, increased formation of gases in the intestines, intrahepatic cholestasis, increased activity of "liver" enzymes that occur after drug withdrawal; very rarely - gingival hyperplasia, inflammation of the gingival mucosa, anorexia.

The system of hematopoiesis: rarely - thrombocytopenia, thrombocytopenic purpura, leukopenia; very rarely anemia.

Urinary system: an increase in daily diuresis; rarely - impaired renal function (in patients with renal insufficiency); night urination.

Musculoskeletal system: myalgia; very rarely - arthritis, arthralgia.

Allergic reactions: rarely - hives, exanthema, itchy skin; very rarely - photodermatitis.

Other: feeling of heat; very rarely - visual impairment, weakness, sweating, fever, chills, gynecomastia, hyperglycemia, completely passing after drug withdrawal; change in body weight, galactorrhea.

Overdose:

Symptoms

Depending on the severity of intoxication, there may be a significant reduction in blood pressure, tachycardia, chest pain (angina), collapse, loss of consciousness, nodular or ventricular extrasystole due to suppression of sinus function node and delayed atrial-ventricular conduction, bradycardia, or fainting. In severe cases, there may be a violation of consciousness with a transition to coma, hyperkalemia, metabolic alkalosis, hypoxia, cardiogenic shock with pulmonary edema.

Treatment

In the early stages after detecting an overdose as a first aid rinse the stomach and give Activated carbon. If necessary, a small bowel flushing can be done, which is more appropriate in case of an overdose of controlled release preparations. When appointing laxatives, it should be borne in mind that the reception of blockers of "slow" calcium channels suppresses intestinal motility to full atony.

As nifedipine is largely associated with blood plasma proteins, hemodialysis is not effective, and plasmapheresis can be effective.

In connection with the absence of a specific antidote, symptomatic therapy is indicated. Symptoms of heart rhythm disturbances with bradycardia can be eliminated by the administration of beta-adrenomimetics and / or atropine. In the life-threatening bradycardia, an artificial pacemaker should be used.

With a marked decrease in blood pressure, infusion of usual doses of norepinephrine (noradrenaline) or adrenaline is indicated, dopamine can be used (maximum dose of 25 mcg / kg body weight per minute), dobutamine (maximum dose 15 μg / kg body weight per minute), isoprenaline and 10% calcium gluconate solution (10-20 ml IV).

When developing symptoms of heart failure, intravenous rapid-acting glycosides of digitalis are recommended.

Interaction:

Rational in terms of antihypertensive and antianginal effects, is the combination of Cordaflex® beta-adrenoblockers, diuretics, angiotensin-converting enzyme (ACE) inhibitors, nitrates. All of the above combinations are safe and effective in most clinical situations, since they lead to summation or potentiation of effects, however, in some cases there is a risk of a marked decrease in blood pressure and an increase in symptoms of heart failure. Combination with clonidine, methyldopa, octadine, prazosin according to the indications is possible, however it can cause strong orthostatic hypotension.

Strengthening of the hypotensive effect is also observed with combined therapy with cimetidine, ranitidine and tricyclic antidepressants.

Nifedipine increases the concentration of digoxin and theophylline, and therefore the clinical effect and / or the content of digoxin and theophylline in the blood plasma should be monitored.

Procaine, quinidine and other drugs that cause lengthening of the interval QT, increase the negative inotropic effect and increase the risk of lengthening the interval QT. Under the influence of nifedipine, the concentration of quinidine in the blood serum is significantly reduced, which is apparently due to a decrease in its bioavailability, as well as induction of enzymes that inactivate quinidine. With the withdrawal of nifedipine, there is a transient increase in the concentration of quinidine (approximately 2-fold), which reaches a maximum level of 3-4 days. Care should be taken when using such combinations, especially in patients with left ventricular dysfunction.

Nifedipine can displace from the bond with proteins preparations characterized by a high degree of binding (incl.indirect anticoagulants - derivatives of coumarin and indanedione, non-steroidal anti-inflammatory drugs), so that their concentration in the blood plasma can increase.

With simultaneous administration with rifampicin, fenitoin and calcium preparations, the effect of nifedipine is weakened.

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.

Diltiazem suppresses the metabolism of nifedipine in the body, careful monitoring is necessary, if necessary, reduce the dose of nifedipine.

Grapefruit juice, erythromycin and azole antimycotics (fluconazole, intraconazole, ketoconazole) can suppress the metabolism of nifedipine and therefore enhance its effects. Similarly, the simultaneous use of nifedipine and cimetidine increases the level of nifedipine in blood plasma and enhances its effects; However, simultaneous administration with ranitidine does not lead to a significant increase in the level of nifedipine in blood plasma. Because the nifedipine metabolized by enzyme CYP3A4, any inhibitor or inducer of this enzyme can affect the metabolism of nifedipine. Cyclosporin is also an enzyme substrate CYP3A4; so when combined administration of cyclosporine and nifedipine, each can increase the duration of the effect of another.

Special instructions:

The antihypertensive effect of Cordaflex® is enhanced with hypovolemia. Reduction of pressure in the pulmonary artery and hypovolemia after dialysis can also enhance the effects of the drug, and therefore, it is recommended to reduce its dose.

In rare cases, at the beginning of a course of treatment with Cordaflex® or with an increase in its dose, pain in the chest (angina due to paradoxical ischemia) may occur soon after taking the drug. If there is a causal relationship between taking the drug and stenocardia, treatment should be discontinued.

Patients with diabetes need to be closely monitored during Cordaflex therapy.

In the presence of arterial hypertension or coronary artery disease, abrupt withdrawal of nifedipine may cause hypertensive crisis or myocardial ischemia (the phenomenon of "bounce").

During treatment, the use of alcoholic beverages is not recommended because of the risk of excessive lowering of blood pressure.

If during the therapy the patient requires surgical intervention under general anesthesia, it is necessary to inform the anesthetist about the therapy.

Effect on the ability to drive transp. cf. and fur:In the initial individually defined period of treatment, it is necessary to refrain from potentially dangerous activities requiring the speed of psychomotor reactions. In the process of further treatment, the degree of restriction is determined depending on the individual tolerability of the drug.

Form release / dosage:

Tablets, coated with a coating, 10 mg.

Packaging:For 100 tablets in a bottle of brown glass. 1 bottle is placed in a cardboard box together with instructions for use.

Storage conditions:

At a temperature of 15-25 ° C, in a place protected from light.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N012475 / 01

Date of registration:18.08.2010 / 08.10.2014

Expiration Date:Unlimited

The owner of the registration certificate:EGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Manufacturer: & nbsp

SERDIK, LLC Russia

Representation: & nbspEGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Information update date: & nbsp04.02.2018

Illustrated instructions

Instructions

Cordaflex® (Cordaflex®)