Corinfar sustained release pills 10mg, 100pcs

Composition

1 film-coated tablet contains:

Active ingredient:

nifedipine 10 mg

Auxiliary substances:  lactose monohydrate, potato starch, microcrystalline cellulose, povidone K 25, magnesium stearate

Film shell:  hypromellose, macrogol 6000, macrogol 35000, quinoline yellow dye (E 104), titanium dioxide (E 171), talc.

Pharmacological action

Blocker of “slow” calcium channelsath: C. 08. C. A. 05 Nifedipine Pharmacodynamics :

Selective slow calcium channel blocker (BMCC), a 1,4-dihydropyridine derivative. It has antianginal and antihypertensive effects. Reduces the flow of extracellular Ca2+ into cardiomyocytes and smooth muscle cells of coronary and peripheral arteries; in high doses, it inhibits the release of Ca2+ from intracellular depots. In therapeutic doses, it normalizes the transmembrane current of Ca2+, which is disturbed in a number of pathological conditions, primarily in arterial hypertension. It does not affect the tone of the veins.

Increases coronary blood flow, improves blood supply to ischemic areas of the myocardium without the development of the phenomenon of “stealing”, activates the functioning of collaterals. Dilating peripheral arteries reduces total peripheral vascular resistance, myocardial tone, afterload, and myocardial oxygen demand. Practically does not affect the sinoatrial and atrioventricular nodes, has a weak antiarrhythmic activity. Increases renal blood flow, causes moderate natriuresis.

The negative chrono -, dromo -, and inotropic effects are overlaid by reflex activation of the sympathoadrenal system and increased heart rate in response to peripheral vasodilation.

The time of onset of the clinical effect is 20 minutes and its duration is 4-6 hours.

Pharmacokinetics: Absorption is high (more than 90%). Bioavailability – 50-70%. Food intake increases bioavailability. It has a “first pass” effect through the liver. The maximum concentration of nifedipine in blood plasma after a single oral use of 2 tablets (corresponding to 20 mg of nifedipine) is reached in 1-3 hours and its value averages 28.3 mg / ml. Penetrates through the blood-brain and placental barriers, is excreted in breast milk. Binding to plasma proteins (albumins) is 95%. It is completely metabolized in the liver. It is excreted by the kidneys as an inactive metabolite (60-80% of the dose taken).20% with bile. 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, total clearance decreases and T1 / 2 increases.

With prolonged use (2-3 months), tolerance to the drug develops.

Indications

-Chronic stable angina (tension angina),

– Prinzmetal angina (variant angina),

– arterial hypertension.

Use during pregnancy and lactation

Corinfar is contraindicated for use during pregnancy.

If it is necessary to use Corinfar during lactation, the question of stopping breastfeeding should be decided.

Contraindications

– Hypersensitivity to nifedipine and other derivatives of 1,4 – dihydropyridine or to other components of the drug,

– hypotension (systolic blood pressure below 90 mm Hg. calendar),

– cardiogenic shock, collapse,

chronic heart failure in the stage of decompensation,

severe aortic stenosis,

unstable angina,

acute myocardial infarction (first 4 weeks)

pregnancy (1 trimester),

– lactation,

– concomitant use with rifampin.

With caution: Mitral valve stenosis, hypertrophic obstructive cardiomyopathy, severe bradycardia or tachycardia, sinus node weakness syndrome, malignant arterial hypertension, hypovolemia, severe cerebral circulatory disorders, myocardial infarction with left ventricular insufficiency, gastrointestinal obstruction, renal and hepatic insufficiency, hemodialysis (due to the risk of hypotension), pregnancy (2 and 3 trimesters), age up to 18 years (efficacy and safety have not been established), simultaneous use of beta-blockers, digoxin.

Side effects

From the cardiovascular system: tachycardia, palpitations, arrhythmias, peripheral edema (ankles, feet, shins), manifestations of excessive vasodilation (asymptomatic decrease in blood pressure, development or aggravation of heart failure, “hot flashes” of blood to the skin of the face, hyperemia of the skin of the egg, a feeling of heat), a pronounced decrease in blood pressure (rarely), syncope. In some patients, especially at the beginning of treatment or with an increase in the dose, angina attacks may occur and in some cases-the development of myocardial infarction, which requires discontinuation of the drug.

From the central nervous system: headache, dizziness, general weakness, fatigue, drowsiness. Long-term use of the drug in high doses – paresthesia of the extremities, tremor, extrapyramidal (Parkinsonian) disorders (ataxia, “masklike” face, shuffling gait, tremor of the hands and fingers, difficulty swallowing), depression.

From the digestive system: dyspepsia (nausea, diarrhea or constipation), dry mouth, flatulence, increased appetite. Rarely-gum hyperplasia, which completely disappears after discontinuation of the drug. With prolonged use-impaired liver function (intrahepatic cholestasis, increased activity of hepatic transaminases).

From the musculoskeletal system: arthritis, myalgia, swelling of the joints, cramps of the upper and lower extremities.

Allergic reactions: rarely-pruritus, urticaria, exanthema, autoimmune hepatitis, exfoliative dermatitis, photodermatitis, anaphylactic reactions

Hematopoietic disorders: anemia, leukopenia, thrombocytopenia, thrombocytopenic purpura, agranulocytosis. From the urinary system: increased daily diuresis, deterioration of renal function (in patients with renal insufficiency).

Other: rarely-visual disturbances (including transient blindness at the maximum concentration of nifedipine in blood plasma), gynecomastia (in elderly patients, polyp disappears after discontinuation), galactorrhea, hyperglycemia, pulmonary edema, bronchospasm, weight gain.

Interaction

With the simultaneous use of other antihypertensive agents, as well as tricyclic antidepressants, nitrates, cimetidine, inhaled anesthetics, diuretics, the hypotensive effect of nifedipine may increase. BMCs may further enhance the negative inotropic effects of antiarrhythmic drugs such as amiodarone and quinidine. When nifedipine is combined with nitrates, tachycardia increases.

Diltiazem inhibits the metabolism of nifedipine in the body, which may require a reduction in the dose of nifedipine with simultaneous use of these drugs. Reduces the concentration of quinidine in the blood plasma. Increases the concentration of digoxin and theophylline in blood plasma. Rifampicin accelerates the metabolism of nifedipine, co-use is not recommended.

Concomitant use with cephalosporins (e. g. cefixime) may increase the concentration of cephalosporins in the blood. Sympathomimetics, NSAIDs (suppression of PG synthesis in the kidneys and retention of sodium ions and body fluids), estrogens (fluid retention in the body) reduce the hypotensive effect.

Nifedipine can displace drugs with a high degree of protein binding (including indirect anticoagulants-coumarin and indanedione derivatives, anticonvulsants, NSAIDs, quinine, salicylates, sulfinpyrazone), as a result of which their concentration in blood plasma may increase.

Nifedipine inhibits the metabolism of prazosin and other alpha-blockers, which may lead to an increased hypotensive effect. If necessary, the dose of vincristine is reduced, because nifedipine inhibits its elimination from the body, which can cause increased side effects.

Lithium preparations may increase toxic effects (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus). Concomitant use of procainamide, quinidine, and other drugs that cause prolongation of the QT interval increases the risk of significant prolongation of the QT interval.

Grapefruit juice suppresses the metabolism of nifedipine in the body, so it is contraindicated during treatment with nifedipine. Nifedipine is metabolized by the cytochrome P-3A system, and therefore the simultaneous use of drugs that inhibit this system may lead to an 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 plasma blood.

Taking into account the experience of using BMCC nimodipine, it is impossible to exclude similar interactions with nifedipine: carbamazepine, phenobarbital may cause a decrease in the concentration of nifedipine in blood plasma; and valproic acid-an increase in the concentration of nifedipine in blood plasma.

How to take it, course of use and dosage

Inside after eating, without chewing and 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 patient’s sensitivity to the drug. For patients with concomitant severe cerebrovascular diseases and in elderly patients, the dose should be reduced.

Simultaneous food intake delays, but does not reduce the absorption of the Active ingredient from the gastrointestinal tract.

Recommended dosage regimen for adults:

Chronic stable and vasospastic angina pectoris

The initial dose is 10 mg (1 tablet) 2-3 times a day. If the clinical effect is not sufficiently pronounced, the dose of the drug is gradually increased to 2 tablets (20 mg) 1-2 times a day. The maximum daily dose is 40 mg (4 tablets per day).

Essential hypertension:

The average daily dose is 10 mg (1 tablet) 2-3 times a day.

If the clinical effect is not sufficiently pronounced, it is possible to gradually increase the dose of the drug to 20 mg (2 tablets) 2 times a day.

The maximum daily dose is 40 mg (4 tablets per day).

With a 2-fold appointment, the minimum interval between doses of the drug should be at least 4 hours.

The duration of treatment is determined by the attending physician.

Overdose

Symptoms: headache, hyperemia of the facial skin, prolonged marked decrease in blood pressure, sinus node depression, bradycardia/tachycardia, bradiarrhythmia.

With severe poisoning — loss of consciousness, coma. Treatment: symptomatic. In case of severe poisoning (collapse, sinus node depression), gastric lavage (if necessary, small intestine) is performed, activated charcoal is prescribed. The antidote is calcium preparations, intravenous use of 10% calcium chloride or calcium gluconate is indicated, followed by transfer to a long-term infusion.

With a marked decrease in blood pressure, slow intravenous use of dopamine, dobutamine, epinephrine or norepinephrine is indicated. It is recommended to monitor glucose levels (insulin release may decrease) and blood electrolytes (K+, Ca2+). With the development of heart failure — intravenous use of strophanthin. For conduction disorders — atropine, isoprenaline, or an artificial pacemaker. Hemodialysis is ineffective; plasmapheresis is recommended.

Special instructions

Caution should be exercised when prescribing Corinfar to patients with severe hypotension (systolic blood pressure less than 90 mm Hg), chronic heart failure in the decompensation phase, as well as patients with severe forms of arterial hypertension and irreversible renal failure and hypovolemia who are on hemodialysis (due to the high risk of a sharp drop in blood pressure).

Discontinue Corinfar gradually, since sudden discontinuation of the drug (especially after prolonged treatment) may lead to withdrawal symptoms.

When drinking alcohol on the background of Corinthar therapy, it is possible to slow down the speed of psychomotor reactions associated with a decrease in blood pressure.

Use in patients with impaired liver function: Corinfar should be prescribed under close supervision to patients with impaired liver function. If necessary, reduce the dose of the drug.

When taking Corinfar, especially at the beginning of treatment and when changing the drug, it is possible to slow down the speed of psychomotor reactions associated with a decrease in blood pressure. This should be taken into account by persons engaged in potentially dangerous activities that require increased attention and speed of psychomotor reactions.

Form of production

Coated tablets.

Storage conditions

In a dark place, at a temperature not exceeding 25 °C

Shelf life

5 years

Active ingredient

Nifedipine

Conditions of release from pharmacies

By prescription

Dosage form

long-acting tablets