Cardilopin, tablets 5 mg 30 pcs

Cardilopin is an antihypertensive drug with antianginal effect. Its active substance, amlodipine, is a slow calcium channel blocker (calcium antagonist), inhibits incoming transmembrane flow of calcium ions into vascular smooth muscle cells and the heart.

The direct relaxant effect of amlodipine on vascular smooth muscle cells helps to reduce peripheral vascular resistance and provides the drug with hypotensive effect. Antianginal effect of Cardilopin is a consequence of dilation of peripheral arterioles and reduction of PASS (total peripheral vascular resistance) that results in decreased energy and oxygen consumption by myocardium, decreased strain on heart. Dilation of large coronary arteries and arterioles increases the flow of oxygen to normal and ischemic areas of the myocardium. Amlodipine does not cause reflex tachycardia, myocardial oxygen supply improves, including in spasm of the coronary arteries (unstable angina, Prinzmetal angina).

The administration of amlodipine once daily for arterial hypertension provides reduction of blood pressure (BP) in the prone and standing position, which maintains clinical stability for 24 hours. Due to gradual slow dilation of vessels, the development of acute arterial hypotension against the background of Cardilopin administration is unlikely. In patients with angina pectoris, taking the drug once a day increases the total time of possible physical activity before an angina attack and the time before a significant lowering of ST interval. In addition, the frequency of angina attacks and the need to take nitroglycerin are reduced.

Amlodipine has no adverse effect on metabolism and has no effect on plasma lipid levels, serum uric acid levels and blood glucose concentrations. The results of the study showed that use of amlodipine in patients with heart failure of II-III stages according to NYHA classification (New York Heart Association) does not worsen clinical symptoms, does not decrease patients’ tolerance of physical activity and left ventricular ejection fraction.

In NYHA stage III-IV heart failure, no increased incidence of cardiovascular events or mortality has been noted when combined with diuretics, ACE (angiotensin converting enzyme) inhibitors or digoxin. The use of Cardilopin in patients with bronchial asthma is indicated.

Indications

– Arterial hypertension (as monotherapy or, if necessary, as part of combination therapy with other antihypertensive agents).
– Stable angina pectoris (as monotherapy or as part of combination therapy with other antianginal agents).
– Angiospastic angina pectoris (Prinzmetal angina) (as monotherapy or in combination therapy with other antianginal agents).

Active ingredient

Composition

1 tablet contains:

Active substances:

amlodipine 5 mg;

Auxiliary substances:

MCC;

sodium starch glycolate;

magnesium stearate;

colloidal anhydrous silicon dioxide.

How to take, the dosage

For treatment of arterial hypertension or angina pectoris, the usual starting dose is 5 mg once daily (preferably at the same time). Taking into account the reaction of the patient, the initial dose may be increased to 10 mg once daily.

The dose of Cardilopin is not changed if it is used simultaneously with diuretics from the thiazide group, beta-adrenoblockers or ACE inhibitors.

Interaction

Possible concomitant use of amlodipine with thiazide diuretics, beta-adrenoblockers, long-acting nitrates, nitroglycerin sublinguals, NSAIDs, antibiotics and oral hypoglycemic agents.

Thiazide and “loop” diuretics, beta-adrenoblockers, verapamil, ACE inhibitors and nitrates enhance the antianginal and hypotensive effects of amlodipine.

Amiodarone, quinidine, alpha 1-adrenoblockers, antipsychotic drugs (neuroleptics) and slow calcium channel blockers may increase the hypotensive effects of amlodipine.

Calcium preparations may decrease the effect of slow calcium channel blockers (including amlodipine).

Microsomal oxidation inhibitors, by increasing the plasma concentration of amlodipine, increase the risk of side effects, and inducers of microsomal liver enzymes decrease it.

The hypotensive effect of amlodipine is weakened by NSAIDs, especially indomethacin (due to sodium retention and blockade of prostaglandin synthesis by kidneys), alpha-adrenomimetics, estrogens (due to sodium retention), sympathomimetics.

Procainamide, quinidine and other drugs that cause QT interval prolongation increase the negative inotropic effect of amlodipine and may increase the risk of significant QT interval prolongation.

Cimetidine does not affect the pharmacokinetics of amlodipine.

Amlodipine has no effect on the pharmacokinetic parameters of digoxin and warfarin.

Grapefruit juice may slightly increase serum amlodipine levels, but this does not result in significant changes in BP.

Special Instructions

Studies in patients with NYHA stage II and III heart failure when taking amlodipine have shown no decrease in exercise tolerance, left ventricular ejection function or worsening of clinical symptoms. Results of clinical studies with patients with NYHA stage III-IV heart failure have shown that amlodipine does not increase incidence of cardiovascular events or mortality when combined with ACE inhibitors, diuretics or digoxin.

Tooth hygiene and dental visits are necessary during treatment (to prevent soreness, bleeding, and gum hyperplasia).

The dosing regimen for the elderly is the same as for patients in other age groups. Careful monitoring of elderly patients is necessary when increasing the dose. The vasodilator effect of amlodipine develops gradually. Therefore, acute arterial hypotension after its use is very rare, but a gradual reduction in doses is recommended before discontinuing treatment.

Amlodipine does not affect plasma concentrations of potassium, glucose, triglycerides, total cholesterol, LDL, uric acid, creatinine and uric acid nitrogen.

Contraindications

Unstable angina.
– Clinically significant aortic stenosis.
– Severe arterial hypotension.
– Child and adolescent age under 18 years (due to lack of clinical experience).
– Pregnancy.
– Lactation period (breastfeeding).
– Hypersensitivity to amlodipine and other components of the drug.

The drug should be prescribed with caution when:

– Impaired liver function.
– CCSU (marked bradycardia, tachycardia).
– Chronic heart failure in decompensation.
– Mild or moderate degree of arterial hypotension.
– Aortic stenosis.
– Mitral stenosis.
– Hypertrophic obstructive cardiomyopathy.
– Acute myocardial infarction (and within 1 month after).
– Diabetes mellitus.
– Patients of elderly age.

Side effects

Frequent side effects (>1%), dose-dependent (in %): peripheral edema (incidence for 5 mg dose 3.0% and 10 mg 10.8%); dizziness (incidence for 5 mg and 10 mg dose 3.4%); hot flashes (for 5 mg 1.4% and for 10 mg 2.6%); palpitation (for 5 mg 1.4% and for 10 mg 4.5%).

Frequent side effects (>1%), independent of dose (in %): headache (7.3%); abdominal pain (1.6%); increased fatigue (4.5%); drowsiness (1.4%); nausea (2.9%).

Other rare side effects: skin rash, gum hyperplasia, dyspepsia, asthenia, arthralgia, myalgia, muscle cramps, sexual disorders (in both men and women), dyspnea, itching, polylakiuria.

Very rare side effects: liver dysfunction, jaundice, erythema multiforme, gynecomastia.

Other side effects: as with other BCIs, patients with severe occlusive coronary disease may experience progression of angina symptoms, myocardial infarction, and arrhythmias (atrial fibrillation and ventricular tachycardia – which, however, cannot be differentiated from underlying disease).

Overdose

Symptoms: marked BP decrease, tachycardia, excessive peripheral vasodilation.
Treatment: the patient should be given a horizontal position with elevated legs. Gastric lavage, administration of activated charcoal, maintenance of cardiovascular function, control of cardiac and pulmonary function parameters, control of BOD and diuresis are performed. Intensive symptomatic therapy is carried out. To restore vascular tone vasoconstrictors are indicated (if there are no contraindications for their use); to eliminate the effects of calcium channel blockade – intravenous injection of calcium gluconate. Hemodialysis is not effective.

Pregnancy use

With due to insufficient clinical experience of amlodipine use in pregnancy and lactation, the drug should not be administered to pregnant women and women of reproductive age who do not use effective contraceptive methods, unless the therapeutic benefit of the drug justifies the possible risk.

Breast-feeding should be stopped if the drug has to be used during lactation.

Similarities