Kalchek

General characteristics. Structure:

Active agent: an amlodipina безилат that is equivalent to an amlodipin of 2,5 mg; 5 mg and 10 mg.

Excipients: starch corn, calcium hydrophosphate, talc, silicon dioxide colloid, carboxymethylstarch of sodium, magnesium stearate.

Pharmacological properties:

Pharmakodinamnka. Amlodipin — derivative dihydropyridine. Contacting dihydropyridinic receptors, blocks "slow" calcium channels, inhibits transmembrane transition of calcium in cells of an unstriated muscle of heart and vessels (more — in smooth muscle cells of vessels, than in cardiomyocytes). Renders hypotensive and anti-anginal effect.
The mechanism of hypotensive action of an amlodipin is caused by the direct weakening impact on unstriated muscles of vessels.
Amlodipin reduces myocardium ischemia the next two ways:
1. Expands arterioles and, thus, reduces the general peripheric resistance (afterload), at the same time heart rate practically does not change that leads to decrease in consumption of energy and need of a myocardium for oxygen.
2. Expands coronary and peripheral arteries and arterioles both in normal, and in ischemic zones of a myocardium that increases intake of oxygen in a myocardium at patients with vasospastic stenocardia (Printsmetal's stenocardia) and prevents development of the coronary spasm caused by smoking.
At patients with arterial hypertension the single daily dose of Kalcheka® provides a lowering of arterial pressure (ABP) for 24 hours (as in situation "lying", and "standing"). Thanks to the slow beginning of action амлодипин does not cause sharp decrease in the ABP.
At patients with stenocardia the single daily dose of drug increases time of performance of an exercise stress, development of the next attack of stenocardia and depression of a segment of ST detains (on 1 mm) against the background of an exercise stress, reduces the frequency of attacks of stenocardia and consumption of nitroglycerine.
Use for patients with the coronary heart disease (CHD)
At the patients with cardiovascular diseases (including coronary atherosclerosis with defeat of one vessel and to a stenosis of the 3rd and more arteries and atherosclerosis of a carotid artery) who had a myocardial infarction, chrezkozhny transluminal angioplasty of coronary arteries (TLP) or having stenocardia, use of Kalcheka® prevents development of a thickening erotic-medii of carotid arteries, a stroke, TLP, aortocoronary shunting, leads to decrease in number of hospitalization concerning unstable stenocardia and progressing of the chronic heart failure (CHF), reduces the frequency of the interventions directed to recovery of a coronary flow.
Use for patients with heart failure
Калчек® does not increase risk of death or development of complications and deaths at patients with the chronic heart failure (CHF) of the III-IV functional class (on NYHA) against the background of therapy by digoxin, diuretics and APF inhibitors. Sick HSN III-IV of a functional class on TNRF not of an ischemic etiology at use of Kalcheka® have a probability of emergence of a fluid lungs. Калчек® does not exert any adverse impact on a metabolism and concentration of lipids of a blood plasma.

Pharmacokinetics. After intake амлодипин it is slowly absorbed (about 90%) from digestive tract. Absolute bioavailability makes 64–80%, the maximum concentration in blood serum is observed in 6–9 hours. Equilibrium concentration are reached after 7–8 days of therapy by drug. Meal does not influence absorption of an amlodipin. The average volume of distribution makes 21 l/kg of body weight that indicates that the most part of drug to be in fabrics, and rather smaller — in blood.
The most part of the drug which is in blood (97%) contacts proteins of a blood plasma.
Amlodipin is metabolized in a liver with formation of inactive metabolites.
After a single dose inside the elimination half-life (T1/2) averages 35 hours. About 60% of the dose accepted inside are removed by kidneys preferential in the form of metabolites, 10% — in not changed look, and 20–25% — with bile through intestines.
Patients with arterial hypertension of T1/2 have 48 hours, at elderly patients (65 years are more senior) removal of an amlodipin is slowed down (T1/2 is 65 h) in comparison with young patients, however this border has no clinical value.
At patients with a liver failure lengthening of T1/2 is supposed, and at long appointment cumulation of drug in an organism will be higher (T1/2 to 60 h).
The renal failure has no significant effect on kinetics of an amlodipin.
Drug gets through a blood-brain barrier. At a hemodialysis is not removed.

Indications to use:

— Arterial hypertension (in monotherapy or in a combination with other anti-hypertensive means);
— a stable angina of exertion, vasospastic stenocardia (Printsmetal's stenocardia) (in monotherapy or in a combination with other anti-anginal means).

Route of administration and doses:

Inside, the initial dose for treatment of arterial hypertension and stenocardia makes 5 mg of drug of 1 times a day. The dose as much as possible can be increased to 10 mg once in days.
At arterial hypertension the maintenance dose can be 5 mg a day.
Change of a dose at co-administration with thiazide diuretics, beta adrenoblockers or inhibitors of an angiotensin-converting enzyme (APF) is not required.
Change of a dose is not required from patients with a renal failure.
With a dose adjustment abnormal liver function usually it is not required from patients.
At elderly patients it is recommended to apply in an average therapeutic dose, dose adjustment is not required.

Features of use:

During treatment control of body weight and consumption of sodium, purpose of the corresponding diet is necessary.
Maintenance of hygiene of teeth and frequentation of the stomatologist is necessary (for prevention of morbidity, bleeding and a hyperplasia of gums).
The dosing mode for elderly patients same, as well as for patients of other age groups. At increase in a dose careful observation of elderly patients is necessary.
Despite the absence of at BMKK of a syndrome of "cancellation", before the termination of treatment gradual reduction of doses is recommended.
Amlodipin does not influence plasma concentration of potassium ions, glucose, triglycerides, the general cholesterol, lipoproteids of low density, uric acid, creatinine and nitrogen of uric acid.
To patients of low growth and patients with the expressed abnormal liver functions the smaller dosage can be required by patients with small body weight.
Efficiency and safety of use of the drug Kalchek® at hypertensive crisis is not established.

Influence on ability to control of vehicles and mechanisms
During treatment it is necessary to be careful during the driving of motor transport and occupation other types of activity demanding concentration of attention and speed of psychomotor reactions in connection with possibility of dizziness and drowsiness.

Side effects:

From cardiovascular system: heartbeat, the expressed decrease in the ABP, peripheral hypostases (puffiness of anklebones and feet), is rare — disturbance of a heart rhythm (bradycardia, ventricular tachycardia, an atrial flutter), a myocardial infarction, thorax pain, orthostatic hypotension, a vasculitis, is very rare — development or aggravation of heart failure, premature ventricular contraction, migraine.
From the central nervous system: a headache, dizziness, increased fatigue, feeling of heat and "inflows" of blood to face skin, drowsiness, change of mood, a spasm, it is rare — a loss of consciousness, hypesthesias, nervousness, paresthesias, peripheral neuropathy, a tremor, вертиго, an adynamy, an indisposition, a faint, sleeplessness, emotional lability, a depression, alarm, unusual dreams, it is very rare — an ataxy, apathy, agitation, amnesia.
From the alimentary system: nausea, vomiting, pains in epigastriums, it is rare — the increase in activity of "hepatic" transaminases, a hyperbilirubinemia, jaundice (caused by a cholestasia), pancreatitis, dryness of a mucous membrane of an oral cavity, thirst, hepatitis, a meteorism, a hyperplasia of gums, a lock, diarrhea, anorexia, is very rare — gastritis, increase in appetite.
From bodies of a hemopoiesis: very seldom — a Werlhof's disease, a leukopenia, thrombocytopenia.
From respiratory system: short wind, rhinitis, it is very rare — cough.
From urinogenital system: seldom — a pollakiuria, painful desires on an urination, a nocturia, disturbance of sexual function (including decrease in a potentiality); very seldom — a dysuria, a polyuria.
From integuments: very seldom — a xerodermia, dermatitis, a purpura, disturbance of a xanthopathy.
Allergic reactions: skin itch, rash (including erythematic, makulopapulezny rash, small tortoiseshell), Quincke's disease, multiformny erythema.
From a musculoskeletal system: seldom — an arthralgia, myotonia, arthrosis, a dorsodynia, a mialgiya (at prolonged use); very seldom — a myasthenia.
Others: seldom — a gynecomastia, a ginerurikemiya, increase/decrease in body weight, a hyperglycemia, a vision disorder, a diplopia, conjunctivitis, eye pain, a ring in ears, диспноэ, nasal bleeding, the increased sweating; very seldom — a cold clammy sweat, a parosmiya, disturbance of flavoring feelings, accommodation disturbance, a xerophthalmia.

Interaction with other medicines:

It is possible to expect that inhibitors of microsomal enzymes of a liver will increase concentration of an amlodipin in a blood plasma, strengthening risk of development of side effects, and inductors of microsomal enzymes of a liver — to reduce.
Unlike other BMKK clinically significant interaction with non-steroidal anti-inflammatory drugs, especially with indometacin is not noted.
Thiazide and "loopback" diuretics, beta adrenoblockers, verapamil, APF inhibitors and nitrates strengthen anti-anginal and hypotensive effect of an amlodipin.
Amiodaronum, quinidine, means for inhalation anesthesia (derivatives of hydrocarbons), alfa1-adrenoblockers, antipsychotic means (neuroleptics) and BMKK can strengthen hypotensive action.
Amlodipin does not exert impact on pharmacokinetic parameters of digoxin and warfarin.
Cimetidinum: at simultaneous use of an amlodipin with Cimetidinum the pharmacokinetics of an amlodipin does not change.
At combined use of an amlodipin with drugs of lithium strengthening of manifestations of their neurotoxicity (nausea, vomiting, diarrhea, an ataxy, a tremor, a sonitus) is possible.
Drugs of calcium can reduce effect of BMKK.
Antiviral means (ритонавир) increase plasma concentration of BMKK, including amlodipin.
Izofluran — strengthening of hypotensive action of derivatives of dihydropyridine.
At combined use of BMKK with drugs of lithium strengthening of a neurotoxicity is possible.
Repeated use of an amlodipin in a dose of 10 mg and an atorvastatina in a dose of 80 mg is not followed by considerable changes of indicators of pharmacokinetics of an atorvastatin.
The concomitant use of 240 ml of greynfrutovy juice and 10 mg of an amlodipin is not followed by essential changes of pharmacokinetics of an amlodipin.
The concomitant use of 100 mg of a sildenafil at patients with essential hypertensia does not exert impact on parameters of pharmacokinetics of an amlodipin.

Contraindications:

— hypersensitivity to an amlodnpin and/or other components of drug, and also to other derivatives of dihydropyridine;
— the expressed arterial hypotension (systolic the ABP less than 90 мм.рт.ст);
— unstable stenocardia (except for Printsmetal's stenocardia);
— the expressed stenosis of the mouth of an aorta;
— age up to 18 years (efficiency and safety are not established).

With care: an abnormal liver function, a sick sinus syndrome (the expressed bradycardia, tachycardia), chronic heart failure of not ischemic etiology (the III-IV functional class on NYHA classification), arterial hypotension, an aortal stenosis, a mitral stenosis, a hypertrophic subaortic stenosis, an acute myocardial infarction (and within 1 month after), advanced age.

Use at pregnancy and a lactation
Safety of use of an amlodipin at pregnancy is not established therefore use at pregnancy is possible only in that case when the advantage for mother exceeds risk for a fruit.
Are absent this, testimonial of excretion of an amlodipin with breast milk.
However it is known that other BMKK — dihydropyridine derivatives, are excreted with breast milk. In need of purpose of an amlodipin in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

Overdose:

Symptoms: the expressed decrease in the ABP, tachycardia, an excessive peripheral vazodilatation (risk of development of the expressed and persistent arterial hypotension, including with development of shock).

Treatment: a gastric lavage, purpose of absorbent carbon (especially in the first 2 hours after overdose), maintenance of function of cardiovascular system, control of indicators of function of heart and lungs, sublime position of extremities, control of volume of the circulating blood and a diuresis. For recovery of a tone of vessels — use of vasoconstrictors (in the absence of contraindications to their use); for elimination of effects of blockade of calcium channels — intravenous administration of calcium of a gluconate. The hemodialysis is inefficient.

Storage conditions:

List B.
To store in the dry, protected from light place at a temperature not above 25 °C.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 10 or 14 tablets in a blister strip packaging (blister) from aluminum foil and a film of PVC. On 2 blisters containing 14 tablets or on 3 blisters containing 10 tablets in a pack cardboard, complete with the application instruction.