KORDIPIN HL

Active material: Nifedipine
When ATH: C08CA05
CCF: Kalьcievыh channel blocker. Antianginal and antihypertensive drug.
ICD-10 codes (testimony): I10, i20, I20.1
When CSF: 01.03.02
Manufacturer: KRKA d.d. (Slovenia)

Pharmaceutical form, composition and packaging

Pills, Film-coated, Modified release russet, round, lenticular.

Excipients: microcrystalline cellulose, cellulose, lactose, gipromelloza (methylhydroxypropylcellulose), magnesium stearate, Colloidal anhydrous silica.

The composition of the shell: gipromelloza (methylhydroxypropylcellulose), macrogol 6000, macrogol 400, iron oxide red dye (E172), Titanium dioxide (E171), talc.

10 PC. – blisters (2) – packs cardboard.

Pharmacological action

Kalьcievыh channel blocker. It inhibits calcium ion current across the membrane of cardiac muscle cells and vascular smooth muscle, which reduces the accumulation of intracellular calcium. This causes the expansion of the coronary arteries, peripheral blood vessels, reduction in systemic vascular resistance and, Consequently, reduction in cardiac afterload, reduction in myocardial contractility and reduction in myocardial oxygen demand.

Mostly at the beginning of therapy may decrease the heart rate and cardiac output as a result of the activation of baroreceptor reflex.

When long-term therapy with nifedipine heart rate and cardiac output returns to the, that existed before treatment.

In patients with hypertension there is a more pronounced reduction in blood pressure.

Mostly at the beginning of therapy, heart rate and cardiac output may be reduced as a result of the activation of baroreceptors. When long-term therapy with nifedipine heart rate and cardiac output returned to the values, they had before treatment. In patients with hypertension there is a more pronounced reduction in blood pressure.

The duration of drug action – 24 no.

Pharmacokinetics

Absorption and distribution

The release of nifedipine from tablets cordipin^® CL slow and almost linear, providing drug action during a day. After the release of nifedipine is rapidly and almost completely absorbed from the gastrointestinal tract. Simultaneous ingestion accelerates absorption.

C_ss^min achieved after the first dose cordipin CL (through 24 no), C_ss^max nifedipine in the blood observed after 5.0 ± 2.7 hours.

The binding of nifedipine plasma proteins – 94-99%.

Metabolism and excretion

Nifedipine is almost completely metabolized.

T_1/2 was 14.9 ± 6 hours. Less 1% the dose is excreted in the urine as unchanged, 70-80% dose – as metabolites.

Pharmacokinetics in special clinical situations

If the kidney function may slow excretion of nifedipine.

Testimony

- Arterial hypertension;

- Stable angina (angina);

- Angiospastic (vasospastic) angina.

Dosage regimen

Establish individually.

The drug is prescribed in high doses 40 mg (1 tab.) 1 times / day at the start of therapy, and when prolonged treatment. If necessary, increase the dose to a maximum – 80 mg (2 tab.)/sut 1 or 2 admission.

In the case of missing reception the next dose, next admission should not double the dose.

The drug should be taken after meals. The tablets are completely, without breaking or chewing, with a glass of water.

Side effect

Cardio-vascular system: symptoms of excessive vasodilatation (asymptomatic decrease in blood pressure, rush of blood to the face, facial flushing, feeling the heat), tachycardia, heartbeat, arrhythmia, peripheral edema, development or exacerbation of congestive heart failure (often worsening the already existing), retrosternal pain; rarely – excessive reduction of blood pressure, fainting; in some cases (especially at the beginning of treatment) – angina (It requires removal of the drug); in rare cases - myocardial infarction.

From the central and peripheral nervous system: headache, dizziness, fatigue, weakness, drowsiness; long-term use in high doses – paresthesias in extremities, depression, anxiety, extrapyramidal (parkinsonian) infringement (ataxia, mask-like face, shuffling gait, stiffness of arms and legs, tremors of the hands and fingers, difficulty swallowing).

From the digestive system: dry mouth, decreased appetite, dyspepsia (nausea, diarrhea or constipation); rarely – giperplaziya right (angiostaxis, soreness, puffiness); Propafenone – abnormal liver function (intrahepatic cholestasis, increase in liver transaminases).

From the side of hematopoiesis: anemia, asymptomatic agranulocytosis, thrombocytopenia, trombotsitopenicheskaya purpura, leukopenia.

On the part of the musculoskeletal system: arthritis; rarely – arthralgia, swelling of joints, myalgia, fits upper and lower extremities.

From the urinary system: increase in daily diuresis, worsening of renal function (in patients with renal insufficiency).

The respiratory system: rarely – difficulty breathing, cough; rarely – pulmonary edema, bronchospasm.

From the senses: rarely – blurred vision (in t. no. Transient blindness at maximal concentration in plasma nifedipine).

On the part of the endocrine system: rarely – gynecomastia (in elderly patients, completely disappears after drug withdrawal), galactorrhea.

Metabolism: rarely – giperglikemiâ, weight gain.

Allergic reactions: rarely – itching, exfoliative dermatitis; rarely – autoimmune hepatitis.

Dermatological reactions: rarely – rash, photodermatoses.

Contraindications

- Cardiogenic shock (the risk of myocardial infarction);

- The acute phase of myocardial infarction (during the first 4 weeks);

- Vыrazhennыy aortic stenosis;

- Congestive heart failure (decompensated);

- Severe hypotension (systolic BP below 90 mmHg.);

- Porphyria;

- I trimester of pregnancy;

- Lactation;

- Up to 18 years (efficacy and safety have not been established);

- Lactase deficiency, galactosemia, malabsorption;

- Hypersensitivity to nifedipine or other components of the drug;

- Hypersensitivity to other dihydropyridine derivatives;

FROM caution should use the drug in patients with severe aortic stenosis or mitral valve, hypertrophic obstructive cardiomyopathy, bradycardia and tachycardia, SSS, malignant hypertension, myocardial infarction with left ventricular failure, chronic heart failure, unstable angina, obstruction of the digestive tract, in the II and III trimesters of pregnancy, with mild to moderate hypotension, severe violations of cerebral circulation, hepatic dysfunction and / or kidney, gemodialize (the risk of hypotension); simultaneously with the beta-blockers, cardiac glycosides, rifampicin; in elderly patients.

Pregnancy and lactation

The appointment of the drug cordipin^® CL I trimester of pregnancy is contraindicated. In II and III trimesters of application is possible only in case, if the expected benefit of therapy for mother, outweighs the potential risk to the fetus.

Nifedipine is excreted in breast milk, therefore, if necessary, use during lactation should stop breastfeeding.

Cautions

Discontinue treatment with cordipin^® CL is recommended to gradually.

It will be appreciated, at the beginning of treatment may develop angina, especially after the recent abrupt withdrawal of beta-blockers (the past should be withdrawn gradually). Appointment of beta-blockers by patients, receiving cordipin^® HL, should be under close medical supervision, because it is possible excessive reduction of blood pressure, and in some cases – worsening symptoms of heart failure.

Diagnostic criteria for the appointment of the drug in vasospastic angina are: classical clinical picture, accompanied by ST-segment elevation, the occurrence of ergonovine-induced angina or coronary artery spasm, identification of coronary spasm during angiography or detection of a component without confirmation angiospastic (eg, at different threshold voltage or unstable angina, when ECG data indicate transient vasoconstriction).

For patients with severe obstructive cardiomyopathy, there is a risk to increase the frequency, the severity of symptoms and duration of angina attacks after taking nifedipine; in this case the necessary removal of the drug cordipin^® HL.

Patients, hemodialysis, high blood pressure, and irreversible renal failure with reduced BCC drug should be used with caution, tk. can occur a sharp drop in blood pressure.

You should carefully monitor the condition of patients with impaired liver function and, if necessary, reduce the dose and / or to use other formulations of nifedipine.

If during therapy the patient required surgery under general anesthesia, you must inform the anesthesiologist about the nature of the therapy.

During treatment, the positive results are possible during the direct reaction of Coombs and laboratory tests for antinuclear antibodies.

Precautions should be prescribed cordipin^® HL simultaneously with disopyramide and flecainide.

Effects on ability to drive vehicles and management mechanisms

Some patients, especially at the beginning of treatment, the drug may cause dizziness. Therefore, until, until you have established an individual patient's response to treatment, should refrain from driving and other activities potentially hazardous activities.

Overdose

Symptoms: drug causes peripheral vasodilation with marked and, perhaps, prolonged hypotension: headache, facial flushing, long marked reduction of blood pressure, inhibition activity of the sinus node, bradycardia and / or tachycardia, ʙradiaritmija. In severe poisoning – loss of consciousness, coma.

Treatment: standard measures, aimed at the elimination of the drug from the body (appointment of activated carbon, gastric lavage), hemodynamic stabilization; careful monitoring of the heart, lungs and excretory system.

An antidote is a calcium supplement. It is shown in / introduction 10% solution of calcium chloride or calcium gluconate, followed by switching to the long-term infusion.

Due to the high degree of binding to plasma proteins, Hemodialysis is not effective.

It is recommended to control blood glucose (may decrease the release of insulin) electrolytes and (Potassium, Calcium).

Clearance of nifedipine is increased in patients with hepatic insufficiency.

Drug Interactions

The hypotensive effect is enhanced by simultaneous application cordipin^® CL with other antihypertensives, beta-blockers, nitratami, cimetidine (to a lesser extent - Ranitidine), Anesthetic, Diuretics, tricyclic antidepressants.

The hypotensive effect is reduced while the application cordipin^® HL with sympathomimetic, NSAIDs, Estrogen, calcium supplementation.

In an application with enhanced nitrate tachycardia.

In an application cordipin^® HL (as well as other calcium channel bokatorov) antiarrhythmics such as amiodarone, quinidine, disopyramide, flekainid, procainamide is amplified negative inotropic effect. Drugs, causing prolongation of the QT interval, may significantly increase the risk of QT prolongation. Nifedipine quinidine causes a decrease in concentration in the blood plasma, after the abolition of nifedipine may be a sharp increase in the concentration of quinidine.

Nifedipine increases the plasma concentration of digoxin and theophylline (in combination requires control and clinical effect of theophylline and digoxin concentrations in plasma).

Inductors of microsomal liver enzymes (incl. rifampicin) reduce the concentration of nifedipine in the blood plasma.

Nifedipine is able to displace from its association with the plasma protein preparations, characterized by a high degree of binding (incl. indirect anticoagulant coumarin derivatives, and indandiona, anticonvulsants, NSAIDs, quinones, salicilaty, sulfinpirazon), thereby increasing their concentrations in blood plasma.

Nifedipine slow excretion of vincristine from the body and may cause increased side effects of vincristine (when this combination if necessary, reduce the dose of vincristine).

The drugs lithium may increase the side effects of nifedipine (nausea, vomiting, diarrhea, ataksiyu, tremor, noise in ears).

In clinical studies, while the appointment of cephalosporins (eg, cefixime) and increase the bioavailability of nifedipine in the cephalosporin 70%.

Nifedipine inhibits the metabolism of prazosin and other alpha-blockers, as a consequence may increase the hypotensive effect.

Grapefruit juice inhibits the metabolism of nifedipine, therefore during treatment cordipin^® CL its use is contraindicated.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 3 year.