Kalchek tablets 10mg, # 30

- Arterial hypertension (in monotherapy or in combination with other antihypertensive drugs);
- stable exertional angina, vasospastic angina (Prinzmetal's angina) (in monotherapy or in combination with other antianginal drugs).

Inside, the initial dose for the treatment of hypertension and angina pectoris is 5 mg of the drug 1 time per day. The maximum dose can be increased to 10 mg once a day.
With arterial hypertension, the maintenance dose may be 5 mg per day.
No dose change is required when administered simultaneously with thiazide diuretics, beta-blockers or angiotensin-converting enzyme (ACE) inhibitors.
No dose change is required in patients with renal impairment.
In patients with impaired liver function, dose adjustment is usually not required.
In elderly patients, it is recommended to use in an average therapeutic dose; dose adjustment is not required.

Each tablet contains as an active substance: amlodipine besylate, which is equivalent to 10 mg amlodipine.
Excipients: corn starch, calcium hydrogen phosphate, talc, colloidal silicon dioxide, sodium carboxymethyl starch, magnesium stearate.

- hypersensitivity to amlodnpin and / or other components of the drug, as well as to other derivatives of dihydropyridine;
- severe arterial hypotension (systolic blood pressure less than 90 mm Hg);
- unstable angina (except for Prinzmetal's angina);
- severe stenosis of the aortic mouth;
- age up to 18 years (efficacy and safety have not been established).

With care: impaired liver function, sick sinus syndrome (severe bradycardia, tachycardia), chronic heart failure of non-ischemic etiology (NYHA functional class III-IV), arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after), advanced age.

Trade name of the drug: KalchekЃ

International non-proprietary name:

amlodipine

Dosage form:

pills

Composition:

each tablet contains as an active substance: amlodipine besylate, which is equivalent to amlodipine 5 mg and 10 mg.
Excipients: corn starch, calcium hydrogen phosphate, talc, colloidal silicon dioxide, sodium carboxymethyl starch, magnesium stearate.

Description:
White to off-white round, flat tablets with beveled edges, scored on one side.

Pharmacotherapeutic group:

blocker of 'slow' calcium channels (BMCC).

ATX code: —08—ј01

Pharmacological properties
Pharmacodynamnka
Amlodipine is a dihydropyridine derivative. By binding to dihydropyridine receptors, it blocks 'slow' calcium channels, inhibits the transmembrane transition of calcium into the cells of the smooth muscle of the heart and blood vessels (to a greater extent - into the smooth muscle cells of the vessels than into the cardiomyocytes). It has a hypotensive and antianginal effect.
The mechanism of the hypotensive action of amlodipine is due to a direct relaxing effect on vascular smooth muscles.
Amlodipine reduces myocardial ischemia in the following two ways:
1. Expands the arterioles and, thus, reduces the total peripheral resistance (afterload), while the heart rate remains practically unchanged, which leads to a decrease in energy consumption and myocardial oxygen demand.
2. Expands the coronary and peripheral arteries and arterioles in both normal and ischemic zones of the myocardium, which increases the flow of oxygen into the myocardium in patients with vasospastic angina (Prinzmetal angina) and prevents the development of coronary spasm caused by smoking.
In patients with arterial hypertension, a single daily dose of KalchekЃ provides a decrease in blood pressure (BP) for 24 hours (both in the 'lying' and 'standing' positions). Due to the slow onset of action, amlodipine does not cause a sharp decrease in blood pressure.
In patients with angina pectoris, a single daily dose of the drug increases the time of physical activity, delays the development of the next attack of angina pectoris and ST segment depression (by 1 mm) against the background of physical exertion, reduces the frequency of angina attacks and the consumption of nitroglycerin.
Use in patients with coronary artery disease (IHD)
In patients with cardiovascular diseases (including coronary atherosclerosis with damage to one vessel and up to stenosis of 3 or more arteries and carotid artery atherosclerosis) who have undergone myocardial infarction, percutaneous transluminal angioplasty of coronary arteries (TPA) or suffering from angina pectoris, the use of KalchekЃ prevents the development of thickening of the intima-media of the carotid arteries, stroke, TLP, coronary artery bypass grafting, leads to a decrease in the number of hospitalizations for unstable angina pectoris and progression of chronic heart failure (CHF), reduces the frequency of interventions aimed at restoring coronary flow.
Use in patients with heart failure
KalchekЃ does not increase the risk of death or complications and deaths in patients with chronic heart failure (CHF) of functional class III Ц IV (according to NYHA) during therapy with digoxin, diuretics and ACE inhibitors. In patients with CHF III Ц IV functional class according to TNRF of non-ischemic etiology, when using KalchekЃ, there is a possibility of pulmonary edema. KalchekЃ does not have any adverse effect on metabolism and plasma lipid concentration.

Pharmacokinetics
After oral administration, amlodipine is slowly absorbed (about 90%) from the gastrointestinal tract. The absolute bioavailability is 64Ц80%, the maximum concentration in the blood serum is observed after 6Ц9 hours. Equilibrium concentrations are reached after 7Ц8 days of drug therapy. Food intake does not affect the absorption of amlodipine. The average volume of distribution is 21 l / kg body weight, which indicates that most of the drug is in the tissues, and relatively less in the blood.
Most of the drug in the blood (97%) binds to blood plasma proteins.
Amlodipine is metabolized in the liver to form inactive metabolites.
After a single oral administration, the half-life (T1 / 2) is an average of 35 hours. About 60% of the dose taken orally is excreted by the kidneys mainly in the form of metabolites, 10% - unchanged, and 20-25% - with bile through the intestines.
In patients with arterial hypertension T1 / 2 - 48 hours, in elderly patients (over 65 years old), the excretion of amlodipine is slowed down (T1 / 2 - 65 hours) compared with young patients, but this border has no clinical significance.
In patients with hepatic insufficiency, an extension of T1 / 2 is expected, and with prolonged administration, the cumulation of the drug in the body will be higher (T1 / 2 up to 60 hours).
Renal failure does not significantly affect the kinetics of amlodipine.
The drug crosses the blood-brain barrier. It is not removed during hemodialysis.

Indications for use
- Arterial hypertension (in monotherapy or in combination with other antihypertensive drugs);
- stable exertional angina, vasospastic angina (Prinzmetal's angina) (in monotherapy or in combination with other antianginal drugs).

Contraindications
- hypersensitivity to amlodinpin and / or other components of the drug, as well as to other derivatives of dihydropyridine;
- severe arterial hypotension (systolic blood pressure less than 90 mm Hg);
- unstable angina (except for Prinzmetal's angina);
- severe stenosis of the aortic mouth;
- age up to 18 years (efficacy and safety have not been established).

With care: impaired liver function, sick sinus syndrome (severe bradycardia, tachycardia), chronic heart failure of non-ischemic etiology (NYHA functional class III-IV), arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after), advanced age.

Use during pregnancy and lactation The
safety of amlodipine during pregnancy has not been established, therefore, use during pregnancy is possible only if the benefit to the mother outweighs the risk to the fetus.
There are no data indicating the excretion of amlodipine in breast milk.
However, it is known that other BMCCs, dihydropyridine derivatives, are excreted in breast milk. If it is necessary to prescribe amlodipine during lactation, the question of stopping breastfeeding should be resolved.

Dosage and administration
Inside, the initial dose for the treatment of hypertension and angina pectoris is 5 mg of the drug 1 time per day. The maximum dose can be increased to 10 mg once a day.
With arterial hypertension, the maintenance dose may be 5 mg per day.
No dose change is required when administered simultaneously with thiazide diuretics, beta-blockers or angiotensin-converting enzyme (ACE) inhibitors.
No dose change is required in patients with renal impairment.
In patients with impaired liver function, dose adjustment is usually not required.
In elderly patients, it is recommended to use in an average therapeutic dose; dose adjustment is not required.

Side effect
From the side of the cardiovascular system: palpitations, marked decrease in blood pressure, peripheral edema (swelling of the ankles and feet), rarely - cardiac arrhythmias (bradycardia, ventricular tachycardia, atrial flutter), myocardial infarction, chest pain, orthostatic hypotension, vasculitis, very rarely - the development or worsening of heart failure, extrasystole, migraine.
From the side of the central nervous system:headache, dizziness, increased fatigue, a feeling of heat and 'flushes' of blood to the skin of the face, drowsiness, mood changes, convulsions, rarely - loss of consciousness, hypesthesia, nervousness, paresthesia, peripheral neuropathy, tremor, vertigo, asthenia, malaise, fainting, insomnia, emotional lability, depression, anxiety, unusual dreams, very rarely - ataxia, apathy, agitation, amnesia.
From the digestive system: nausea, vomiting, epigastric pain, rarely - increased activity of 'hepatic' transaminases, hyperbilirubinemia, jaundice (caused by cholestasis), pancreatitis, dryness of the oral mucosa, thirst, hepatitis, flatulence, gingival hyperplasia, constipation, diarrhea , anorexia, very rarely - gastritis, increased appetite.
From the side of the hematopoietic organs:very rarely - thrombocytopenic purpura, leukopenia, thrombocytopenia.
Respiratory system: shortness of breath, rhinitis, very rarely - cough.
From the genitourinary system: rarely - pollakiuria, painful urge to urinate, nocturia, sexual dysfunction (including decreased potency); very rarely - dysuria, polyuria.
On the part of the skin: very rarely - xeroderma, dermatitis, purpura, skin pigmentation disorders.
Allergic reactions: pruritus, rash (including erythematous, maculopapular rash, urticaria), angioedema, erythema multiforme.
From the side of the musculoskeletal system:rarely - arthralgia, muscle cramps, arthrosis, back pain, myalgia (with prolonged use); very rarely - myasthenia gravis.
Others: rarely - gynecomastia, gyneuricemia, weight gain / loss, hyperglycemia, visual impairment, diplopia, conjunctivitis, eye pain, ringing in the ears, dyspnea, nosebleeds, increased sweating; very rarely - cold sticky sweat, parosmia, violation of taste, violation of accommodation, xerophthalmia.

Overdose
Symptoms: marked decrease in blood pressure, tachycardia, excessive peripheral vasodilation (risk of severe and persistent arterial hypotension, including shock).
Treatment: gastric lavage, the appointment of activated charcoal (especially in the first 2 hours after an overdose), maintaining the function of the cardiovascular system, monitoring the indicators of heart and lung function, elevated position of the limbs, monitoring the volume of circulating blood and diuresis. To restore vascular tone - the use of vasoconstrictor agents (in the absence of contraindications to their use); to eliminate the consequences of calcium channel blockade - intravenous administration of calcium gluconate. Hemodialysis is ineffective.

Interaction with other drugs
It can be expected that inhibitors of liver microsomal enzymes will increase the concentration of amlodipine in the blood plasma, increasing the risk of side effects, and inducers of liver microsomal enzymes will decrease.
Unlike other BMCCs, there is no clinically significant interaction with non-steroidal anti-inflammatory drugs, especially with indomethacin.
Thiazide and 'loop' diuretics, beta-blockers, verapamil, ACE inhibitors and nitrates enhance the antianginal and hypotensive effect of amlodipine.
Amiodarone, quinidine, inhalation anesthetics (hydrocarbon derivatives), alpha-1-blockers, antipsychotics (neuroleptics) and BMCC can increase the hypotensive effect.
Amlodipine has no effect on the pharmacokinetic parameters of digoxin and warfarin.
Cimetidine: with the simultaneous use of amlodipine with cimetidine, the pharmacokinetics of amlodipine does not change.
With the combined use of amlodipine with lithium preparations, it is possible to increase the manifestations of their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
Calcium supplements can reduce the effect of BMCC.
Antiviral drugs (ritonavir) increase plasma concentrations of BMCC, including amlodipine.
Isoflurane - enhancement of the hypotensive effect of dihydropyridine derivatives.
With the combined use of BMCC with lithium preparations, an increase in neurotoxicity is possible.
Repeated use of amlodipine at a dose of 10 mg and atorvastatin at a dose of 80 mg is not accompanied by significant changes in the pharmacokinetics of atorvastatin.
The simultaneous intake of 240 ml of grainfruit juice and 10 mg of amlodipine is not accompanied by significant changes in the pharmacokinetics of amlodipine.
Concomitant administration of 100 mg of sildenafil in patients with essential hypertension does not affect the pharmacokinetic parameters of amlodipine.

Special instructions
During the period of treatment, it is necessary to control the body weight and sodium intake, the appointment of an appropriate diet.
Maintaining dental hygiene and frequent visits to the dentist is necessary (to prevent soreness, bleeding and gingival hyperplasia).
The dosage regimen for elderly patients is the same as for patients in other age groups. When the dose is increased, careful monitoring of elderly patients is necessary.
Despite the absence of a 'withdrawal' syndrome in BMCC, a gradual dose reduction is recommended before discontinuing treatment.
Amlodipine does not affect the plasma concentrations of potassium ions, glucose, triglycerides, total cholesterol, low density lipoproteins, uric acid, creatinine and uric acid nitrogen.
Patients with low body weight, patients of short stature and patients with severe liver dysfunction may require a lower dosage.
The efficacy and safety of using the drug KalchekЃ in hypertensive crisis has not been established.

Influence on the ability to drive vehicles and mechanisms
During the period of treatment, care should be taken when driving vehicles and engaging in other activities that require concentration of attention and speed of psychomotor reactions, due to the possibility of dizziness and drowsiness.

Release form
10 or 14 tablets in a blister made of aluminum foil and PVC film. 2 blisters containing 14 tablets, or 3 blisters containing 10 tablets, in a cardboard box, complete with instructions for use.

Storage conditions
List B.
Store in a dry, dark place at a temperature not exceeding 25 ? C.
Keep out of the reach of children.

Shelf life is
3 years.
Do not use after the expiration date printed on the package.

Terms of dispensing from pharmacies
Prescription.