Cordaflex, pills 10mg 100pcs

Composition

of 1 tab. :

– nifedipine 10 mg

Auxiliary substances:

polyvinyl butyral,

magnesium stearate,

talc,

hydroxypropylcellulose,

sodium croscarmellose,

lactose monohydrate,

microcrystalline cellulose,

titanium dioxide,

iron oxide yellow,

hypromellose.

Pharmacological action

Pharmgroup:

blocker of “slow” calcium channels.

Pharmaceutical action:

 Kordaflex is a selective slow calcium channel blocker, a 1,4-dihydropyridine derivative. It has antihypertensive and antianginal effects. Nifedipine reduces the flow of extracellular calcium ions into cardiomyocytes and smooth muscle cells of coronary and peripheral arteries. In therapeutic doses, it normalizes the transmembrane flow of calcium ions, which is disturbed in a number of pathological conditions, primarily in arterial hypertension. Reduces spasm and dilates coronary and peripheral arterial vessels, reduces OPSS, reduces afterload and myocardial oxygen demand. At the same time, it improves blood supply to ischemic areas of the myocardium without the development of “stealing” syndrome, and also increases the number of functioning collaterals.

Nifedipine has virtually no effect on the sinoatrial and AV nodes and does not have either pro-or antiarrhythmic effects. It does not affect the tone of the veins. Nifedipine increases renal blood flow, causing moderate natriuresis. In high doses, it inhibits the release of calcium ions from intracellular depots. Reduces the number of functioning calcium channels, without affecting the time of their activation, inactivation and recovery.

After a single dose of Kordaflex in the form of long-acting tablets, the clinical effect develops in 20 minutes, the duration of the clinical effect is 12-24 hours

. Pharmacokinetics:  

Absorption When taken orally, it is rapidly and almost completely (more than 90%) absorbed from the gastrointestinal tract. Bioavailability – 40-70%. After oral use of Kordaflex in the form of a 10 mg tablet, Cmax in the blood is reached 0.5-1 h after use. After oral use of 1 tablet of prolonged action 20 mg, the therapeutic concentration of nifedipine in blood plasma is reached in 1 hour and remains at a constant level for up to 6 hours (prolonged action plateau), and gradually decreases in the next 30-36 hours.

Distribution Binding to plasma proteins (albumins) is 94-97%. Unbound nifedipine is distributed to all organs and tissues.

Penetrates through the BBB (less than 5%), through the placental barrier, is excreted in breast milk. It doesn’t accumulate.

Metabolism Nifedipine is extensively metabolized in the liver to form 3 metabolites that do not have pharmacological activity.

Excretion After oral use of Kordaflex in the form of a tablet of 10 mg T1/2 nifedipine is 2 hours, after taking a tablet with a prolonged action of 20 mg – about 3.8-16.9 hours

.60-80% of the oral dose of the drug is excreted in the urine in the form of inactive metabolites, the remainder – with bile and feces.

Pharmacokinetics in special clinical cases

In elderly patients, nifedipine metabolism in the liver is reduced.

In patients with hepatic insufficiency, the total clearance decreases and the T1/2 of nifedipine increases. Chronic renal failure, hemodialysis, and peritoneal dialysis do not affect the pharmacokinetics of nifedipine.

Indications

-arterial hypertension of various origins, including hypertensive crises (for 10 mg tablets); – IHD: for the prevention of seizures in various forms of angina pectoris, including angiospastic (Prinzmetal angina pectoris);- Raynaud’s syndrome (for long-acting tablets).

Use during pregnancy and lactation

Kordaflex® is contraindicated for use in the first trimester of pregnancy.

The use of Kordaflex in pregnant women is indicated only in cases where normalization of blood pressure is impossible with the use of other antihypertensive drugs.

Since nifedipine is excreted in breast milk, you should avoid using Kordaflex during lactation or stop breastfeeding during treatment with the drug.

Contraindications

-acute stage of myocardial infarction;- cardiogenic shock; – severe arterial hypotension (systolic blood pressure below 90 mm Hg)— – severe aortic or mitral stenosis, idiopathic hypertrophic subaortic stenosis;— severe heart failure— – I trimester of pregnancy; – lactation (breastfeeding);— children and adolescents under 18 years of age;- hypersensitivity to nifedipine and other components of the drug Kordaflex.

Kordaflex® should be used with caution in patients with chronic heart failure, hypertrophic obstructive cardiomyopathy, severe cerebral circulatory disorders, SSR, severe tachycardia, severe liver and/or kidney function disorders, malignant arterial hypertension, in patients undergoing hemodialysis (due to the risk of severe arterial hypotension on the background of peripheral vasodilation), lactose intolerance, as well as in elderly patients.

Side effects

From the cardiovascular system: hyperemia of the facial skin, severe hypotension, peripheral edema, tachycardia; rarely-increased angina attacks (drug withdrawal is required), increased heart failure, fainting.

From the central nervous system and peripheral nervous system: headache, dizziness, fatigue, sleep disorders (drowsiness or insomnia); in isolated cases – lability of mood, visual disturbances; with prolonged use in high doses – paresthesia in the extremities, tremor.

From the digestive system: diarrhea, constipation, nausea, heartburn; rarely (with prolonged use of the drug) – dry mouth, flatulence, intrahepatic cholestasis, increased activity of hepatic transaminases; in some cases – gum hyperplasia, gingivitis, anorexia.

From the hematopoietic system: rarely-thrombocytopenia, thrombocytopenic purpura, leukopenia; in some cases-anemia.

From the urinary system: increased daily diuresis; rarely-deterioration of renal function in patients with chronic renal failure.

From the musculoskeletal system: myalgia; in some cases – arthritis.

From the endocrine system: in isolated cases – gynecomastia, hyperglycemia (completely disappear after discontinuation of the drug), changes in body weight, galactorrhea.

Allergic reactions: rarely-urticaria, exanthema, pruritus; in some cases-autoimmune hepatitis.

Other: feeling hot; in isolated cases – weakness, sweating, fever, chills, photodermatitis.

Interaction

The combination of Kordaflex with beta-blockers, diuretics, ACE inhibitors, nitrates is rational from the point of view of enhancing the antihypertensive and antianginal effects. All of the above combinations are safe and effective in most clinical situations, since they lead to a summation or potentiation of the effects, but in some cases there is a risk of a pronounced decrease in blood pressure and increased symptoms of heart failure.

The combination of Kordaflex with clonidine, methyldopa, octadine, prazosine is possible according to indications, but may cause severe orthostatic hypotension.

An increase in the hypotensive effect is also observed in combination therapy with cimetidine, ranitidine and tricyclic antidepressants.

Nifedipine increases the concentration of digoxin and theophylline in the blood plasma, 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 prolongation of the QT interval increase the negative inotropic effect and increase the risk of prolongation of the QT interval. Under the influence of nifedipine, the concentration of quinidine in the blood serum decreases significantly, which is probably due to a decrease in its bioavailability, as well as the induction of enzymes that inactivate quinidine. When nifedipine is discontinued, there is a transient increase in the concentration of quinidine (approximately 2 times), which reaches its maximum level on day 3-4. Caution should be exercised when using such combinations, especially in patients with left ventricular dysfunction.

Nifedipine can displace drugs with a high degree of binding from protein binding (including indirect anticoagulants-coumarin and indandione derivatives, NSAIDs), as a result of which their plasma concentrations may increase.

When administered concomitantly with rifampicin, phenytoin and calcium supplements, the effect of nifedipine is weakened. Nifedipine inhibits the elimination of vincristine from the body and may cause an increase in the side effect of vincristine, if necessary, the dose of vincristine is reduced.

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

Grapefruit juice, erythromycin, and azole antifungal medications (fluconazole, intraconazole, and ketoconazole) can inhibit nifedipine metabolism and therefore enhance its effects.

Similarly, the simultaneous use of Cordaflex and cimetidine increases the concentration of nifedipine in blood plasma, increases its effects

Since nifedipine is metabolized by the CYP3A4 isoenzyme, any inhibitor or inducer of this enzyme can affect the metabolism of nifedipine. Cyclosporine is also a substrate of the CYP3A4 isoenzyme; therefore, when cyclosporine and nifedipine are used together, each can increase the duration of the other’s effect.

How to take it, course of use and dosage

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

Adults Kordaflex® in the form of coated tablets are prescribed 10 mg (1 tab) 3 times a day. If necessary, the dose of the drug can be increased to 20 mg (2 tablets) 1-2 times / day. The maximum daily dose is 40 mg. The interval between doses of the drug is at least 2 hours.

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

If necessary, increase the dose to 80-120 mg / day. for the treatment of angina pectoris or arterial hypertension, it is recommended to transfer the patient to take the drug in the form of long-acting tablets.

During the course of therapy, it is recommended to use Kordaflex® in the form of long-acting tablets. The initial dose is 20 mg (1 tab) 2 times / day. with an interval of 12 hours. If necessary, the dose of the drug is gradually increased until the optimal clinical effect is achieved. For long-term maintenance therapy, as a rule, it is sufficient to take 20-40 mg (1-2 tablets) 2 times a day. The maximum daily dose is 120 mg.

In elderly patients, the pharmacokinetics of nifedipine changes, and therefore the initial dose of the drug is reduced by 2 times and lower doses may be required to maintain the therapeutic effect.

No dosage adjustment is required for moderate hepatic or renal impairment. With severe hepatic impairment, the maximum daily dose should not exceed 40 mg.

The drug in the form of tablets containing 10 mg of nifedipine is taken orally before meals.

Overdose

Symptoms: severe hypotension, tachycardia, chest pain (angina pectoris), headache, collapse, loss of consciousness, nodular or ventricular extrasystole due to sinus node depression, bradycardia, fainting. In severe cases, there may be impaired consciousness with the transition to a coma, hyperkalemia, metabolic alkalosis, hypoxia, cardiogenic shock with pulmonary edema.

Treatment: given the absence of a specific antidote, in cases of early detoxification, gastric lavage is performed with the appointment of activated charcoal. If necessary, small bowel lavage can be performed, which is more appropriate in the case of an overdose of controlled-release drugs. When prescribing laxatives, it should be borne in mind that taking slow calcium channel blockers suppresses intestinal motility to complete atony. Since nifedipine is largely bound to plasma proteins, hemodialysis is not effective, and plasmapheresis may be effective.

Symptomatic therapy is indicated. Symptoms of cardiac arrhythmias with bradycardia can be treated with beta-adrenomimetics and / or atropine. For life-threatening bradycardia, an artificial pacemaker should be used. With a marked decrease in blood pressure, infusion of conventional doses of norepinephrine (norepinephrine) or epinephrine (epinephrine) is indicated, dopamine (maximum dose 25 mcg/kg body weight/min), dobutamine (maximum dose 15 mcg/kg body weight/min), isoprenaline and 10% calcium gluconate solution (10-20 ml IV) can be used. If symptoms of heart failure develop, intravenous use of fast-acting cardiac glycosides is recommended.

Special instructions

The antihypertensive effect of Kordaflex increases with hypovolemia. Reduced pulmonary artery pressure and hypovolemia after dialysis may also increase the effects of the drug, and therefore a dose reduction is recommended.

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

In patients with arterial hypertension or coronary vascular disease, abrupt withdrawal of nifedipine can cause a hypertensive crisis or myocardial ischemia (the “rebound” phenomenon).

If the patient needs surgery under general anesthesia during therapy, it is necessary to inform the anesthesiologist about the treatment with Cordaflex.

Elderly patients are more likely to have decreased cerebral blood flow due to severe peripheral vasodilation. During the course of treatment with Kordaflex, the use of alcoholic beverages is not recommended due to the risk of excessive lowering of blood pressure.

Use in pediatrics

Due to the lack of sufficient clinical data, the drug is not recommended for use in children and adolescents under the age of 18 years.

Influence on the ability to drive motor vehicles and manage mechanisms

During the initial, individually determined period of application of Kordaflex, driving vehicles and engaging in other potentially dangerous activities that require rapid psychomotor reactions are not allowed. In the course of further treatment, the degree of restrictions is determined depending on the individual patient’s reaction to the drug.

Form of production

Pills.

Storage conditions

In a dark place, at a temperature of 15-25 °C

Shelf life

4 years

Active ingredient

Nifedipine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets