Кордипин®

General characteristics. Structure:

Active ingredient: 10,0 mg of nifedipine.

Excipients: starch corn, lactoses monohydrate, povidone, sodium lauryl sulfate, talc, starch prezhelatinizirovanny, silicon dioxide colloid, anhydrous. 

Cover: methacrylic acid copolymer, talc, titanium dioxide (E 171),  macrogoal, dye quinolinic yellow (E104).

Kordipin is the antagonist of calcium blocking calcium channels in muscle cells of heart and blood vessels. Possesses hypotensive (lowers pressure), vazodelatiruyushchy, anti-anginal and antiischemic action.

Pharmacological properties:

Pharmacodynamics. Nifedipine concerns to group of blockers of "slow" calcium channels, derivative 1,4 dihydropyridines. Has anti-anginal and anti-hypertensive activity. Expands coronary and peripheral arterial vessels, reduces the need of a myocardium for oxygen due to reduction of an afterload by heart and deliveries of oxygen. Strengthens a coronary blood stream, improves blood supply of ischemic zones without development of a phenomenon of "burglarizing", activates functioning of collaterals. Expanding peripheral arteries, reduces the general peripheric resistance of vessels (GPRV), a myocardium tone, an afterload, the need of a myocardium for oxygen and increases duration of diastolic relaxation of the left ventricle (LV). Has no antiarrhytmic activity.

In response to peripheral vasodilation: negative hrono-, dromo-and inotropic action is blocked by reflex activation of sympathoadrenal system and increase in ChSS.

Pharmacokinetics. Nifedipine is almost completely soaked up in digestive tract (more than 90%). Absolute bioavailability makes 40 - 70%. Nifedipine is exposed to intensive metabolism at "the first passing" through a liver (40-60%).

After intake of 1 tablet of 10 mg the maximum concentration of drug in a blood plasma is reached in 30 - 60 min. An elimination half-life - 2 - 4 hours. Communication with proteins of a blood plasma (albumine) makes 94 - 97%.

Active ingredient gets through a placental barrier and is emitted in breast milk. Less than 5% of the entered dose get through a blood-brain barrier.

Nifedipine is generally metabolized to the 3rd pharmacological inactive metabolites, and in such view with urine about 60 - 80% of the entered dose are removed. Other dose is removed through intestines.

After intake 50-60% of nifedipine are absorbed. The maximum levels of concentration of nifedipine in a blood plasma after reception of a tablet with the slowed-down release of 20 mg it is reached in 2-4 hours.

Nifedipine is well distributed in fabrics, more than 90% contact proteins of a blood plasma, generally albumine. Nifedipine is almost completely metabolized in a liver, turning into inactive metabolites. 80% of inactive metabolites are removed by kidneys, other part through intestines. The elimination half-life of Kordipina®  makes 8-10 hours. Elimination can be slowed down at patients with a renal failure.

Nifedipine gets through a blood-brain and placental barrier, is emitted with breast milk. The cumulative effect is absent. The chronic renal failure, a hemodialysis and peritoneal dialysis do not influence pharmacokinetics. At prolonged use development of tolerance to nifedipine can be observed.

Indications to use:

Кордипин® apply to treatment:

• Stable stenocardia, alternative stenocardia (Printsmetal's stenocardia);
• Arterial hypertension;
• Raynaud's disease.

Route of administration and doses:

Doses of Kordipina® have to be selected individually. Drug is accepted inside, washing down with a small amount of water.

The initial dose makes 10 mg (1 tablet) 2-3 times a day. If necessary the dose of drug can be increased to 2 tablets (20 mg) 1-2 times a day. The maximum daily dose makes 40 mg.

Nifedipine is generally metabolized in a liver therefore the dose should be selected according to a condition of a liver of the patient. At a renal failure Kordipin's dose is not required to be adjusted.

Features of use:

 It is recommended to stop treatment by the drug Kordipin® gradually. It must be kept in mind that in an initiation of treatment there can be stenocardia, especially after recent sharp cancellation of beta adrenoblockers (the last should be cancelled gradually).

Co-administration of beta adrenoblockers needs to be carried out in the conditions of careful medical control as it can cause an excessive lowering of arterial pressure, and in certain cases - aggravation of symptoms of heart failure.

At the expressed heart failure drug is dosed carefully.

Diagnostic criteria of purpose of drug at vasospastic stenocardia are: the classical clinical picture which is followed by increase in a segment of ST, developing of the ergonovin-induced stenocardia or a spasm of coronary arteries, identification of a coronary spasm at an angiography or identification of an angiospastic component without confirmation (for example, at a different threshold of tension or at unstable stenocardia when these electrocardiograms confirm a passing vasomotor spasm).

For patients with a heavy subaortic stenosis there is a risk of increase in frequency, weight of manifestation and duration of attacks of stenocardia after nifedipine reception; in this case drug withdrawal is necessary.

At the patients who are on a hemodialysis with the high ABP and irreversible insufficiency of kidneys with the reduced total quantity of blood drug should be used carefully, there can be a sharp falling of the ABP.

For patients with the broken function of a liver careful observation is established and if necessary reduce a dose of drug and/or use other dosage forms of nifedipine.

If during therapy the patient needs to carry out surgical intervention under the general anesthesia, it is necessary to inform the anesthesiologist on the nature of the carried-out therapy.

During treatment positive takes when carrying out forward reaction of Koombs and laboratory tests on antinuclear antibodies are possible.

With care it is necessary to appoint along with Disopyramidum and flekainamidy owing to possible strengthening of an inotropic effect.

Purpose of nifedipine is shown to pregnant women only if the estimated advantage for mother, exceeds potential risk for a fruit. It is not recommended to appoint nifedipine in the 1st trimester of pregnancy.
Drug is emitted with breast milk therefore during administration of drug it is recommended to stop breastfeeding.

At some patients, especially in an initiation of treatment, drug can cause dizziness that reduces ability to driving or other mechanisms. Further extent of restrictions is defined depending on individual portability of drug.

Side effects:

From cardiovascular system: manifestations of an excessive vazodilatation (asymptomatic decrease in the ABP, development or aggravation of the heart failure (HF), "inflows" of blood to face skin, a dermahemia of the person, feeling of heat), tachycardia, heartbeat, arrhythmia, peripheral hypostases, retrosternal pains; seldom - the excessive lowering of arterial pressure (ABP), a syncope, a syncope, at some patients, especially in an initiation of treatment, is possible emergence of attacks of stenocardia that demands drug withdrawal. Isolated cases of a myocardial infarction are described.

From the central nervous system: headache, dizziness, increased fatigue, weakness, drowsiness. At chronic ingestion in high doses - paresthesias of extremities, a depression, feeling of alarm, extrapyramidal (parkinsonichesky) disturbances (the ataxy, a "masklike" face shuffling gait, constraint of movements of hands and legs, a tremor of brushes and fingers of hands, the complicated swallowing).

From the alimentary system: dryness in a mouth, increase in appetite, dyspepsia (nausea, diarrhea or a lock); seldom - a hyperplasia of gums (bleeding, morbidity, puffiness), at long reception - abnormal liver functions (an intra hepatic cholestasia, increase in activity of "hepatic" enzymes).

From bodies of a hemopoiesis: anemia, asymptomatic agranulocytosis, thrombocytopenia, Werlhof's disease, leukopenia.

Allergic reactions: seldom - a skin itch, a small tortoiseshell, a dieback, exfoliative dermatitis, a photodermatitis; very seldom - autoimmune hepatitis.

From a musculoskeletal system: arthritis, it is rare - an arthralgia, puffiness of joints, a mialgiya, spasms of upper and lower extremities.

From an urinary system: increase in a daily urine, deterioration in function of kidneys (at patients with a renal failure).

Others: seldom – breath difficulty, cough; very seldom - a vision disorder (including a tranzitorny blindness at the maximum concentration of nifedipine in a blood plasma), a gynecomastia (at elderly patients, completely disappearing after drug withdrawal), a hyperglycemia, a galactorrhoea, a fluid lungs, a bronchospasm, increase in body weight.

Interaction with other medicines:

Expressiveness of decrease in the ABP amplifies at simultaneous use of other antihypertensives, beta adrenoblockers, nitrates, Cimetidinum (to a lesser extent ranitidine), inhalation anesthetics, diuretics and tricyclic antidepressants.

Medicines from the BMKK group can strengthen even more the negative inotropic effect (lowering force of cordial reduction) of such antiarrhytmic means as Amiodaronum and quinidine.

Nifedipine causes decrease in concentration of quinidine in a blood plasma, after cancellation of nifedipine there can be a sharp increase in concentration of quinidine.

Increases plasma concentration of digoxin and theophylline in this connection it is necessary to control clinical effect and content of digoxin and theophylline in a blood plasma.

Inductors of microsomal enzymes of a liver (rifampicin, etc.) reduce concentration of nifedipine.

In combination with nitrates tachycardia amplifies. The hypotensive effect is reduced by sympathomimetics, non-steroidal anti-inflammatory drugs, estrogen, calcium drugs.

Nifedipine can force out from communication with proteins the drugs which are characterized by high extent of binding (including indirect anticoagulants – derivatives of coumarin and an indandion, anticonvulsants, non-steroidal anti-inflammatory drugs, quinine, salicylates, Sulfinpyrazonum) owing to what their concentration in a blood plasma can increase.

Nifedipine slows down removal of Vincristinum from an organism and can cause strengthening of side effects of Vincristinum, if necessary the dose of Vincristinum is reduced.

Drugs of lithium can strengthen toxic effects (nausea, vomiting, diarrhea, an ataxy, a tremor, a sonitus).

Grapefruit juice suppresses metabolism of nifedipine in an organism in this connection, their concomitant use is contraindicated.

Contraindications:

Hypersensitivity to nifedipine or other derivatives of dihydropyridine, other components of drug, cardiogenic shock (risk of development of a myocardial infarction), a collapse, the expressed stenosis of the aortal valve, chronic heart failure (in a decompensation stage), the expressed arterial hypotension (systolic arterial pressure is lower than 90 mm hg), the acute period of a myocardial infarction (within the first 4 weeks), pregnancy (the I trimester), the lactation period, age up to 18 years (efficiency and safety are not established).

With care: the expressed stenosis of the mouth of an aorta or the mitral valve, a hypertrophic subaortic stenosis, the expressed bradycardia or tachycardia, a sick sinus syndrome, malignant arterial hypertension, a myocardial infarction with a left ventricular failure, unstable stenocardia, co-administration of beta adrenoblockers or cardiac glycosides, a concomitant use of rifampicin, heavy disturbances of cerebral circulation, abnormal liver function and/or kidneys, a hemodialysis (risk of developing of arterial hypotension).

Overdose:

Symptoms: causes a peripheral vazodilatation with expressed and, perhaps, the prolonged system arterial hypotension: a headache, a dermahemia of the person, the long expressed decrease in the ABP, oppression of activity of a sinus node, bradycardia and/or tachycardia, a bradyarrhythmia. At a serious poisoning a loss of consciousness, a coma.

Treatment of overdose consists in standard procedures of removal of drug from an organism (purpose of absorbent carbon, a gastric lavage), recovery of stable indicators of a hemodynamics, careful control of action of the heart, lungs and secretory system.

Antidote are calcium drugs, is shown in/in introduction of 10% of solution of Calcii chloridum or calcium of a gluconate, with the subsequent switching to long infusion.

Owing to high extent of linkng with proteins of a blood plasma, the hemodialysis is not effective.

It is recommended to carry out control of the content of glucose to blood (insulin release can decrease) and electrolytes (potassium, calcium).

The clearance of nifedipine increases at patients with insufficiency of function of a liver.

Storage conditions:

To store in the dry, protected from light place, at a temperature not above 25 °C.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated 10 mg. On 10 tablets in a strip. 5 strips in a cardboard pack together with the application instruction.