Cardilopin tablets 10mg, No. 30

• Treatment of arterial hypertension as monotherapy or (if necessary) in combination with other antihypertensive drugs.

• Stable angina pectoris and vasospastic angina pectoris (Prinzmetala) - as monotherapy or in combination with other antianginal drugs.

Inside. With arterial hypertension and angina pectoris, the initial dose is 5 mg once a day, preferably always at the same time of the day. Depending on the response to the drug, the initial dose can be increased to 10 mg per day (maximum daily dose).
No dose adjustment is required in case of concomitant use of thiazide diuretics, beta-blockers or angiotensin-converting enzyme blockers.
Elderly patients and those with renal impairment can be given the usual dose.
In case of impaired liver function, the dose should be reduced (up to 2.5 mg per day) due to the lengthening of the half-life of the drug.

Active ingredient: each tablet contains 10 mg of amlodipine (respectively in the form of 13.9 amlodipine besylate).
Excipients: microcrystalline cellulose, sodium carboxymethyl starch (type A), magnesium stearate, anhydrous colloidal silicon dioxide.

• Hypersensitivity to amlodipine and / or any other component of the drug.

• Children under 18 years of age (due to lack of clinical experience).

• Unstable angina (excluding Prinzmetal's angina).

• Clinically significant aortic stenosis.

• Severe arterial hypotension.

• Pregnancy and lactation (see section 'Pregnancy and lactation').

Carefully:

Liver dysfunction, sick sinus syndrome (severe bradycardia, tachycardia), chronic heart failure in the stage of decompensation, mild or moderate arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after) , diabetes mellitus, old age.

Trade name of the drug:

Cardilopin Ѓ

INN:

amlodipine

Dosage form:

pills

Composition:

Active ingredient: each tablet contains 2.5 mg, 5 mg or 10 mg of amlodipine (respectively in the form of 3.475 mg, 6.95 mg or 13.9 amlodipine besylate).
Excipients: microcrystalline cellulose, sodium carboxymethyl starch (type A), magnesium stearate, anhydrous colloidal silicon dioxide.

Description:

2.5 mg tablets: Round, flat, beveled tablets engraved with УEФ on one side and У251Ф on the other, white, off-white or off-white.
Tablets 5 mg: Round, flat, beveled tablets engraved with 'E' on one side and '252' on the other, white, off-white or off-white.
Tablets 10 mg: Round, flat, beveled tablets engraved with 'E' on one side and '253' on the other, white, off-white or off-white.

Pharmacotherapeutic group:

slow calcium channel blocker

Pharmacological properties

Mechanism of action:
Amlodipine inhibits the transmembrane incoming flow of calcium ions into smooth muscle cells of the heart and blood vessels (it blocks slow calcium channels, i.e., is a calcium antagonist).
The antihypertensive effect of amlodipine is due to a direct relaxing effect on vascular smooth muscle cells, which leads to a decrease in peripheral vascular resistance.
The mechanism of antianginal action is not fully understood, however, it is most likely associated with the following two effects:
1. Expansion of peripheral arterioles reduces total peripheral resistance, ie, afterload. Since amlodipine does not cause reflex tachycardia, myocardial energy and oxygen consumption is reduced.
2. Dilation of large coronary arteries and coronary arterioles improves oxygen supply to both normal and ischemic areas of the myocardium. Thanks to these effects, the oxygen supply to the myocardium is improved, even with spasm of the coronary arteries (Prinzmetal's angina or unstable angina).

Pharmacodynamics
In patients with arterial hypertension, taking the drug once a day causes a clinically significant decrease in blood pressure in the supine position and standing throughout the entire 24-hour interval between doses of the drug. Due to the slow development of the effect of amlodipine, it does not cause acute arterial hypotension.
In patients with angina pectoris, taking the drug once a day increases the total time for performing possible physical activity before the development of an angina attack, as well as the time until a significant decrease in the ST interval, and also reduces the frequency of angina attacks and the need for sublingual nitroglycerin intake.
There was no negative effect of amlodipine on metabolism. The drug does not affect plasma lipids, blood glucose and serum uric acid levels. It is safe for asthma patients.

Pharmacokinetics:

Absorption:
Amlodimine is well absorbed after oral administration. The maximum concentration in blood plasma is observed after 6-12 hours. Taking the drug with food does not affect its absorption. Absolute bioavailability is 64 - 80%.

Distribution: The
apparent volume of distribution is 21 l / kg. Equilibrium plasma concentration (5-15 ng / ml) is achieved 7-8 days after starting the drug. Studies in vitro have shown that circulating amlodipine approximately 93 - 98% bound to plasma proteins.

Biotransformation and excretion:
Amlodipine is extensively metabolized in the liver. Approximately 90% of the dose taken is converted to inactive pyridine derivatives. Approximately 10% of the dose taken is excreted in the urine unchanged. Approximately 60% of the amount of inactive metabolites is excreted by the kidneys and 20-25% through the intestines. The plasma concentration-time curve is biphasic. The final half-life is approximately 35-50 hours, which allows the drug to be administered once a day. The clearance of the drug and the whole body is 7 ml / min / kg (25 l / h in a patient weighing 60 kg). In elderly patients, the clearance of the drug from the whole body is 19 l / h.
The pharmacokinetics of amlodipine does not change in renal failure or in elderly patients.
Due to the decrease in clearance, patients with hepatic impairment should be given lower initial doses.

Indications for use:

• Treatment of arterial hypertension as monotherapy or (if necessary) in combination with other antihypertensive drugs.

• Stable angina pectoris and vasospastic angina pectoris (Prinzmetala) - as monotherapy or in combination with other antianginal drugs.

Contraindications:

• Hypersensitivity to amlodipine and / or any other component of the drug.

• Children under 18 years of age (due to lack of clinical experience).

• Unstable angina (excluding Prinzmetal's angina).

• Clinically significant aortic stenosis.

• Severe arterial hypotension.

• Pregnancy and lactation (see section 'Pregnancy and lactation').

Carefully:

Liver dysfunction, sick sinus syndrome (severe bradycardia, tachycardia), chronic heart failure in the stage of decompensation, mild or moderate arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after) , diabetes mellitus, old age.

Pregnancy and lactation

Given the limited clinical experience with the use of amlodipine during pregnancy and lactation, it should not be prescribed to pregnant women, as well as women of reproductive age who do not use effective methods of contraception, unless the beneficial effects of the drug justify the possible risk.
Amlodipine should not be taken during pregnancy unless absolutely necessary or when the therapeutic benefit of the drug justifies the potential risk. If a breastfeeding woman is taking amlodipine due to the lack of other drugs, it is recommended to stop breastfeeding.

Method of administration and dosage:

Inside. With arterial hypertension and angina pectoris, the initial dose is 5 mg once a day, preferably always at the same time of the day. Depending on the response to the drug, the initial dose can be increased to 10 mg per day (maximum daily dose).
No dose adjustment is required in case of concomitant use of thiazide diuretics, beta-blockers or angiotensin-converting enzyme blockers.
Elderly patients and those with renal impairment can be given the usual dose.
In case of impaired liver function, the dose should be reduced (up to 2.5 mg per day) due to the lengthening of the half-life of the drug.

Side effect

From the nervous system: headache, dizziness, excessive fatigue, drowsiness, mood changes, convulsions; rarely - loss of consciousness, hypesthesia, paresthesia, tremor, asthenia, malaise, insomnia, nervousness, depression, unusual dreams, anxiety; very rarely - ataxia, apathy, agitation, amnesia.

From the digestive system: nausea, abdominal pain; rarely hyperbilirubinemia, jaundice, increased activity of 'hepatic' transaminases, dry mouth, anorexia, vomiting, constipation or diarrhea, dyspepsia, flatulence, gingival hyperplasia; very rarely - gastritis, increased appetite, pancreatitis.

From the cardiovascular system: palpitations, swelling of the ankles and feet, shortness of breath, flushing of blood to the face, rarely - rhythm disturbances (bradycardia, ventricular tachycardia, atrial flutter), chest pain, excessive decrease in blood pressure, orthostatic hypotension; very rarely - development or worsening of heart failure, extrasystole, migraine.

From the genitourinary system: rarely - pollakiuria, painful urge to urinate, nocturia, sexual dysfunction (including decreased potency); very rarely - dysuria, polyuria.

From the side of the musculoskeletal system: rarely - arthralgia, arthrosis, myalgia (with prolonged use); very rarely - myasthenia gravis.

On the part of the skin: very rarely - xeroderma, alopecia, dermatitis, purpura.

Allergic reactions: pruritus, rash (including erythematous, maculopapular rash, urticaria).

Others: rarely - visual impairment, conjunctivitis, diplopia, eye pain, impaired accommodation, xerophthalmia, ringing in the ears, gynecomastia, back pain, fever, chills, weight gain, dyspnea, epistaxis, increased sweating, thirst; very rarely - cold clammy sweat, cough, rhinitis, parosmia, taste perversion, hyperglycemia.

Overdose

Symptoms: marked decrease in blood pressure, tachycardia, excessive peripheral vasodilation.
Treatment: gastric lavage, the appointment of activated charcoal, maintaining the function of the cardiovascular system, monitoring the indicators of the function of the heart and lungs, elevated position of the limbs, monitoring the volume of circulating blood and diuresis.
Intensive symptomatic therapy. To restore vascular tone - the use of vasoconstrictor drugs (in the absence of contraindications to their use); to eliminate the consequences of calcium channel blockade - intravenous administration of calcium gluconate. Hemodialysis is not effective.

Interaction with other medicinal products

The use of amlodipine has proven to be safe in combination with thiazide diuretics, beta-blockers, long-acting nitrates, sublingual nitroglycerin preparations, non-steroidal anti-inflammatory drugs, antibiotics and oral hypoglycemic agents.

Thiazide and 'loop' diuretics, beta-blockers, verapamil, ACE inhibitors and nitrates enhance antianginal and hypotensive effects.

Amiodarone, quinidine, alpha 1-blockers, antipsychotic drugs (antipsychotics) and blockers of 'slow' calcium channels can enhance the hypotensive effect.

Calcium supplements can reduce the effect of slow calcium channel blockers.

Inhibitors of microsomal oxidation increase the concentration of amlodipine in the blood plasma, increasing the risk of side effects, while inducers of microsomal liver enzymes decrease.

The antihypertensive effect is weakened by non-steroidal anti-inflammatory drugs, especially indomethacin (sodium retention and blockade of kidney prostaglandin synthesis), alpha-adrenostimulants, estrogens (sodium retention), sympathomimetics.

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

Cimetidine does not affect the pharmacokinetics of amlodipine.

Does not affect the pharmacokinetic parameters of digoxin and warfarin.

Grapefruit juice may slightly increase serum amlodipine levels, but this does not lead to significant changes in blood pressure.

special instructions

Studies in patients with NYHA stage II / III heart failure while taking amlodipine did not reveal a decrease in exercise tolerance, left ventricular ejection function, or worsening of clinical symptoms. Clinical trials in patients with NYHA stage III-IV heart failure ('PRAISE') have shown that amlodipine does not increase the incidence of cardiovascular disease or mortality when used with ACE inhibitors, diuretics, or digoxin.
During the treatment period, it is necessary to maintain dental hygiene and visit the dentist (to prevent soreness, bleeding and gingival hyperplasia).
The dosage regimen for the elderly is the same as for patients in other age groups.
When the dose is increased, careful monitoring of elderly patients is necessary.
The vasodilating effect of amlodipine develops gradually. Therefore, acute arterial hypotension after its use is very rare, however, a gradual dose reduction is recommended before stopping treatment.
Amlodipine does not affect plasma concentrations of K +, glucose, triglycerides, total cholesterol, LDL, uric acid, creatinine and uric acid nitrogen.

Influence on the ability to drive a car and mechanisms

There were no reports of the effect of amlodipine on driving or operating machinery. However, in some patients, drowsiness and dizziness may occur mainly at the beginning of treatment. If they occur, the patient must observe special precautions when driving and working with mechanisms.

Release form:

Tablets 2.5 mg, 5 mg, 10 mg.
10 tablets in a PVC / PVDC / aluminum foil blister.
1, 2 or 3 blisters in a cardboard box along with instructions for medical use.

Shelf life:

5 years. Do not use after the expiration date stated on the package.

Storage conditions:

Store at a temperature of 15 to 25 ? C, protected from light.
Keep out of the reach of children.

Terms of dispensing from pharmacies:

On prescription.