Calchek, pills 5mg, 30pcs

Composition

Each tablet contains as an Active ingredient:

amlodipine bezylate, which is equivalent to amlodipine 5 mg.

Auxiliary substances:

corn starch,

calcium hydrophosphate,

talc,

colloidal silicon dioxide,

sodium carboxymethyl starch,

magnesium stearate.

Pharmacological action

Amlodipine is a dihydropyridine derivative. Binding to dihydropyridine receptors, it blocks “slow” calcium channels, inhibits the transmembrane transfer of calcium into the smooth muscle cells of the heart and blood vessels (to a greater extent – into vascular smooth muscle cells than into cardiomyocytes). It has antihypertensive and antianginal effects.

The mechanism of antihypertensive action of amlodipine is due to the direct relaxing effect on vascular smooth muscles. Amlodipine reduces myocardial ischemia in the following two ways:

1. Dilates the arterioles and, thus, reduces the total peripheral resistance (afterload), while the heart rate practically does not change, which leads to a decrease in energy consumption and myocardial oxygen demand.

2. Dilates the coronary and peripheral arteries and arterioles in both normal and ischemic areas of the myocardium, which increases oxygen supply to 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 Calchek ® provides a reduction 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 another angina attack and ST-segment depression (by 1 mm) against the background of physical activity, reduces the frequency of angina attacks and nitroglycerin consumption.

Use in patients with coronary heart disease (CHD)

In patients with cardiovascular diseases (including coronary atherosclerosis with a single vessel lesion and before stenosis of 3 or more arteries and carotid artery atherosclerosis), who have had a myocardial infarction, percutaneous transluminal angioplasty of the coronary arteries (TLP), or who suffer from angina pectoris, the use of Calchek® 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 and the progression of chronic heart failure (CHF), reduces the frequency of interventions aimed at restoring coronary flow.

Use in patients with heart failure

Calchek® It does not increase the risk of death or the development of complications and deaths in patients with chronic heart failure (CHF) of functional class III–IV (NYHA) during therapy with digoxin, diuretics and ACE inhibitors. In patients with CHF of functional class III–IV according to TNFR of non-ischemic etiology, when using Calchek®, there is a possibility of pulmonary edema. Calchek® it does not have any adverse effect on the metabolism and concentration of plasma lipids.

Pharmacokinetics

After oral use, amlodipine is slowly absorbed (about 90%) from the gastrointestinal tract. Absolute bioavailability is 64-80%, the maximum concentration in the blood serum is observed after 6-9 hours. Steady-state concentrations are reached after 7-8 days of drug therapy. Food intake does not affect the absorption of amlodipine. The average volume of distribution is 21 l / kg of 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 plasma proteins.

Amlodipine is metabolized in the liver to form inactive metabolites.

After a single oral dose, the half-life (T1/2) is an average of 35 hours. About 60% of the oral dose 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, T 1/2 — 48 hours, in elderly patients (older than 65 years), the elimination of amlodipine is slowed (T1/2 — 65 hours) compared to young patients, but this limit is not clinically significant.

In patients with hepatic insufficiency, T1/2 is expected to be prolonged, and with prolonged use, the accumulation of the drug in the body will be higher (T 1/2 to 60 hours).

Renal failure does not significantly affect the kinetics of amlodipine.

The drug penetrates the blood-brain barrier. It is not removed during hemodialysis.

Indications

-Arterial hypertension (in monotherapy or in combination with other antihypertensive agents); – stable tension angina, vasospastic angina (Prinzmetal angina) (in monotherapy or in combination with other antianginal agents).

Use during pregnancy and lactation

The safety of using amlodipine during pregnancy has not been established, so use during pregnancy is possible only if the benefit to the mother exceeds the risk to the fetus.

There are no data indicating the excretion of amlodipine in breast milk.

However, other BMCC derivatives of dihydropyridine are known to be excreted in breast milk. If it is necessary to prescribe amlodipine during lactation, the question of stopping breastfeeding should be decided.

Contraindications

— hypersensitivity to amlodipine and/or other components of the drug, as well as other derivative of dihydropyridine; — severe hypotension (systolic BP less than 90 mm Hg. St); — unstable angina (with the exception of prinzmetals angina); a pronounced stenosis of the mouth of the aorta; — age under 18 years (effectiveness and safety not established).

With caution:  impaired liver function, sinus node weakness 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), elderly age.

Side effects

From the cardiovascular system:  palpitations, marked decrease in blood pressure, peripheral edema (swelling of the ankles and feet), rarely-cardiac arrhythmia (bradycardia, ventricular tachycardia, atrial flutter), myocardial infarction, chest pain, orthostatic hypotension, vasculitis, very rarely — development or aggravation of heart failure, extrasystole, migraine.

From the central nervous system:  headache, dizziness, increased fatigue, 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 (due to cholestasis), pancreatitis, dry oral mucosa, thirst, hepatitis, flatulence, gum hyperplasia, constipation, diarrhea, anorexia, very rarely — gastritis, increased appetite.

From the side of hematopoietic organs:  very rarely — thrombocytopenic purpura, leukopenia, thrombocytopenia.

Respiratory system disorders:  shortness of breath, rhinitis, very rarely — cough.

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

From the side of the skin:  very rarely — xeroderma, dermatitis, purpura, skin pigmentation disorder.

Allergic reactions:  skin pruritus, rash (including erythematous, maculopapular rash, urticaria), angioedema, erythema multiforme.

From the musculoskeletal system:  rarely-arthralgia, muscle cramps, arthrosis, back pain, myalgia (with prolonged use); very rarely-myasthenia gravis.

Other services:  rarely-gynecomastia, gineruricemia, weight gain/loss, hyperglycemia, visual impairment, diplopia, conjunctivitis, eye pain, tinnitus, dyspnoea, nosebleeds, increased sweating; very rarely-cold sticky sweat, parosmia, impaired taste, accommodation disorders, xerophthalmia.

Interaction

It can be expected that inhibitors of microsomal liver enzymes will increase the concentration of amlodipine in blood plasma, increasing the risk of side effects, and inducers of microsomal liver enzymes will decrease. Unlike other BMCs, there is no clinically significant interaction with nonsteroidal anti-inflammatory drugs, especially indomethacin.

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

Amiodarone, quinidine, inhaled anesthetics (hydrocarbon derivatives), alpha-1-blockers, antipsychotics (neuroleptics), and BMCC may enhance the hypotensive effect.

Amlodipine does not affect the pharmacokinetic parameters of digoxin and warfarin.

Cimetidine: the pharmacokinetics of amlodipine do not change when amlodipine is co-administered with cimetidine. When amlodipine is co-administered 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 agents (ritonavir) increase plasma concentrations of BMCC, including amlodipine. Isoflurane increases the hypotensive effect of dihydropyridine derivatives.

When BMCC is co-administered with lithium preparations, neurotoxicity may increase.

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.

Concomitant use of 240 ml of grapefruit juice and 10 mg of amlodipine is not accompanied by significant changes in the pharmacokinetics of amlodipine.

Concomitant use of 100 mg of sildenafil in patients with essential hypertension does not affect the pharmacokinetics of amlodipine.

How to take, course of use and dosage

Inside, the initial dose for the treatment of arterial 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.

In arterial hypertension, the maintenance dose may be 5 mg per day.

No dose adjustment is required when co-administered with thiazide diuretics, beta-blockers, or angiotensin-converting enzyme (ACE) inhibitors.

No dose adjustment is required in patients with renal insufficiency.

In patients with hepatic impairment, no dose adjustment is usually required.

In elderly patients, it is recommended to use at an average therapeutic dose, no dose adjustment is required.

Overdose

Symptoms: marked decrease in blood pressure, tachycardia, excessive peripheral vasodilation (risk of severe and persistent arterial hypotension, including with the development of shock).

Treatment: gastric lavage, use of activated charcoal (especially in the first 2 hours after an overdose), maintenance of the cardiovascular system, monitoring of heart and lung function indicators, elevated position of the extremities, control of the volume of circulating blood and diuresis. To restore vascular tone — the use of vasoconstrictors (in the absence of contraindications to their use); to eliminate the consequences of calcium channel blockade — intravenous use of calcium gluconate. Hemodialysis is ineffective.

Special instructions

During the treatment period, it is necessary to monitor body weight and sodium intake, prescribe an appropriate diet. It is necessary to maintain dental hygiene and frequent visits to the dentist (to prevent soreness, bleeding and gum hyperplasia).

The dosage regimen for elderly patients is the same as for patients of other age groups. When increasing the dose, careful monitoring of elderly patients is necessary.

Despite the absence of “withdrawal” syndrome in BMCC, a gradual dose reduction is recommended before discontinuing treatment. Amlodipine does not affect plasma concentrations of potassium, glucose, triglycerides, total cholesterol, low-density lipoproteins, uric acid, creatinine, and uric acid nitrogen.

Patients with low body weight, short stature and patients with severe hepatic impairment may require a lower dosage.

The efficacy and safety of Calchek® in hypertensive crisis has not been established.

Influence on the ability to drive vehicles and mechanisms

During treatment, caution should be exercised 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.

Form of production

Round, flat tablets with beveled edges, white to almost white in color, with a risk on one side.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

3 years

Active ingredient

Amlodipine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets