Kalchek - instructions for use, dose, side effects, contraindications

Excipients: starch corn 66.72 / 101.1 mg, calcium hydrophosphate 150.88 / 235.70 mg talc 2.00 / 3.50 mg. silicon dioxide colloid 2.00 / 3.00 mg, sodium carboxymethyl starch 0.24 / 0.50 mg. magnesium stearate 1.00 / 2.00 mg.

Description:

Round, flat tablets with bevelled edges, from white to almost white, with a risk on one side.

Pharmacotherapeutic group:The blocker of "slow" calcium channels

ATX: & nbsp

C.08.C.A.01 Amlodipine

Pharmacodynamics:

Amlodipine is a dihydropyridine derivative. Linking with dihydropyridine receptors, blocks "slow" calcium channels, inhibits the transmembrane transition of calcium into the cells of the smooth muscle of the heart and blood vessels (mostly to the smooth muscle cells of the vessels,than in cardiomyocytes). Has hypotensive and antianginal effect.

The mechanism of hypotensive action of amlodipine is due to a direct relaxing effect on the smooth muscles of the vessels.

Amlodipine reduces myocardial ischemia in the following two ways:

1 Expands the arterioles and, thus, reduces the overall peripheral resistance (afterload), with the heart rate practically unchanged, which leads to a reduction in energy consumption and myocardial oxygen demand.

2 Expands coronary and peripheral arteries and arterioles in both normal and ischemic zones of the myocardium, which increases oxygen supply to the myocardium in patients with vasospastic angina (Prinzmetal angina) and prevents the development of coronarospasm caused by smoking.

In patients with arterial hypertension, a single daily dose of Kalcheck® provides a reduction in blood pressure (BP) for 24 hours (both in the "lying" and "standing" positions). Due to the slow start of action amlodipine does not cause a sharp decrease in blood pressure.

In patients with angina, a single daily dose of the drug increases the time of exercise, delays the development of another attack of angina and depression of the segment ST (by 1 mm) against the background of physical activity, reduces the frequency of angina attacks and the consumption of nitroglycerin.

Application v patients with ischemic heart disease (CHD)

In patients with cardiovascular diseases (including coronary atherosclerosis with single vessel damage and up to stenosis of 3 or more arteries and carotid artery atherosclerosis) who underwent myocardial infarction, percutaneous transluminal angioplasty of coronary arteries (TPL) or those suffering from angina, the use of Kalcheck® warns development of intima-media thickening of carotid arteries, stroke, TLO, coronary artery bypass surgery, reduces the number of hospitalizations for unstable angina and progression of chronic ce Cardiac insufficiency (CHF), reduces the frequency of interventions aimed at restoring the coronary flow.

Use in patients with heart failure

Kalchek® does not increase the risk of death or the development of complications and fatalities in patients with chronic heart failure (CHF) III-IV functional class (by NYHA) on the background of therapy with digoxin, diuretics and ACE inhibitors. In patients with CHF III-1V functional class on NYHA is not ischemic etiology in the application of Kalcheck® there is a possibility of pulmonary edema. Kalchek® ns exerts any adverse effect on the metabolism and concentration of plasma lipids.

Pharmacokinetics:

After oral administration amlodipine is slowly absorbed (about 90%) from the gastrointestinal tract. Absolute bioavailability is 64-80%, the maximum concentration in serum is observed after 6-9 hours. Equilibrium concentrations are achieved 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 body weight, indicating that most of the drug is in tissues, and relatively less in the blood. Most of the drug in the blood (97%) binds to blood plasma proteins. Amlodipine metabolized in the liver with the formation of inactive metabolites.

After a single oral intake, the half-life period (T_1/2) is an average of 35 hours. About 60% of the dose taken internally is excreted by the kidneys mainly in the form of metabolites, 10% - unchanged, and 20-25% - with bile through the intestine.

In patients with hypertension T_1/2) - 48 hours, in elderly patients (over 65 years of age) excretion of amlodipine is slowed down (T_1/2) - 65 h) compared with young patients, but this border has no clinical significance.

In patients with hepatic insufficiency, an extension T_1/2), and with prolonged administration, the cumulation 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. When hemodialysis is not removed.

Indications:

- Arterial hypertension (in monotherapy or in combination with other antihypertensive agents);

- stable angina of tension, vasospastic angina (Prinzmetal angina) (in ionotherapy or in combination with other antianginal agents).

Contraindications:

- Hypersensitivity to amlodipine and / or other components of the drug, as well as to other dihydropyridine derivatives;

- severe arterial hypotension (systolic blood pressure less than 90 mm Hg);

- unstable angina (with the exception of Prinzmetal's stenocardia);

- pronounced stenosis of the aortic aorta;

- age to 18 years (efficacy and safety not established).

Carefully:

Violation of the liver function, syndrome of weakness of the sinus node (pronounced bradycardia, tachycardia), chronic heart failure non-ischemic etiology (III-IV functional class by classification NYHA), arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after), elderly age.

Pregnancy and lactation:

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

There is no evidence of excretion of amlodipine in breast milk. However, it is known that other BCCC - dihydropyridine derivatives are excreted in breast milk. If it is necessary to prescribe amlodipine during lactation, the question of stopping breastfeeding should be resolved.

Dosing and Administration:

Inside, the initial dose for the treatment of hypertension and angina is 5 mg once a day.The maximum dose can be increased to 10 mg once a day.

With hypertension, the maintenance dose can be 5 mg per day.

Do not require dose changes with concomitant administration with thiazide diuretics, beta-blockers, or angiotensin-converting enzyme (ACE) inhibitors. Do not require dose changes in patients with renal insufficiency.

In patients with impaired liver function, dose adjustment is usually not required.

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

Side effects:

From the cardiovascular system: palpitations, marked reduction in blood pressure, peripheral edema (swelling of the ankles and feet), rarely - a violation of cardiac rhythm (bradycardia, ventricular tachycardia, atrial flutter), heart attack, chest pain, orthostatic hypotension, vasculitis, very rarely - the development or exacerbation of congestive heart insufficiency, extrasystole, migraine.

From the central nervous system: headache, dizziness, fatigue, a feeling of heat and "tides" of blood to the skin of the face, drowsiness, mood changes, seizures,rarely - loss of consciousness, hypoesthesia, 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 hematopoiesis: very rarely - thrombocytopenic purpura, leukopenia, thrombocytopenia.

From the respiratory system: shortness of breath, rhinitis, very rarely - cough.

From the genitourinary system: rarely - pollakiuria, painful urge to urinate, nocturia, violation of sexual function (including a decrease in potency); very rarely - dysuria, polyuria.

From the skin: very rarely - xeroderma, dermatitis, purpura, a violation of skin pigmentation.

Allergic reactions: itching, rash (including erythematous, maculopapular rash, urticaria), angioneurotic edema, erythema multiforme.

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

Other: rarely - gynecomastia, hyperuricemia, increase / decrease in body weight, hyperglycemia, impaired vision, diplopia, conjunctivitis, eye pain, ringing in the ears, dyspnoea, epistaxis, increased sweating; very rarely - cold sticky sweat, parosmia, a violation of taste sensations, disruption of accommodation, xerophthalmia.

Overdose:

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

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

Interaction:

It can be expected that inhibitors of microsomal liver enzymes will increase the concentration of amlodipine in the blood plasma, increasing the risk of side effects, and inductors of microsomal liver enzymes - reduce.

Unlike other BCCI, there is no clinically significant interaction with non-steroidal anti-inflammatory drugs, especially with indomethacin. Thiazide and "loop" diuretics, beta-ad rep about locators, verapamil, ACE inhibitors and nitrates increase the antianginal and hypotensive effect of amlodipine.

Amiodarone, quinidine, agents for inhalation anesthesia (derivatives of hydrocarbons), alpha 1-adrenosine blockers, antipsychotics (antipsychotics) and BCCC can enhance hypotensive action.

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

Cimetidine: with the simultaneous use of amlodipine with cimetidine, the pharmacokinetics of amlodipine does not change.

When amlodipine is used together with lithium preparations, it is possible to intensify the manifestations of their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, and tinnitus). Calcium preparations can reduce the effect of BCCC.

Antiviral drugs (ritonavir) increase plasma concentrations of BCCC, including amlodipine.

Isoflurane - strengthening of hypotensive action of dihydropyridine derivatives.

With the joint use of BCCC with lithium preparations, neurotoxicity may be enhanced.

The repeated use of amlodipine in a dose of 10 mg and atorvastatin at a dose of 80 mg is not accompanied by significant changes in the pharmacokinetics of atorvastatin. Simultaneous intake of 240 ml of grapefruit juice and 10 mg of amlodipine is not accompanied by significant changes in the pharmacokinetics of amlodipine.

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

Special instructions:

During the period of treatment, it is necessary to control the body weight and sodium intake, the appropriate diet.

It is necessary to maintain dental hygiene and frequent visits to the dentist (to prevent soreness, bleeding and gingival 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 the "cancellation" syndrome in BCC, before the cessation of treatment a gradual reduction of doses is recommended.

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, low growth patients and patients with severe liver function impairment may need a lower dosage. The effectiveness and safety of the use of the drug Kalchek® in hypertensive crisis is not established.

Effect on the ability to drive transp. cf. and fur:

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

Form release / dosage:

Tablets 5 mg, 10 mg.

Packaging:For 10 or 14 tablets in a planar cell packaging (blister) from aluminum foil and PVC film. 2 blisters containing 14 tablets or 3 blisters containing 10 tablets in a pack of cardboard, complete with instructions for use.

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N013168 / 01

Date of registration:25.12.2008 / 19.10.2015

Expiration Date:Unlimited

The owner of the registration certificate:Ipka Laboratories Ltd.Ipka Laboratories Ltd. India

Manufacturer: & nbsp

IPCA LABORATORIES, Ltd. India

Representation: & nbspIPKA LABORATORIES LTD. IPKA LABORATORIES LTD. India

Information update date: & nbsp26.11.2017

Illustrated instructions

Instructions

Calcheck® (Calchek®)