Active substanceAmlodipineAmlodipine
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  • Dosage form: & nbsppills
    Composition:

    One tablet contains active substance Amlodipine besylate in terms of amlodipine - 5 mg or 10 mg (7.4 mg or 14.6 mg of amlodipine besylate, respectively); Excipients: Copucidone 4.0 mg (8.0 mg), calcium dihydrogen phosphate (anhydrous) 60.0 mg (120.0 mg), microcrystalline cellulose 121.8 mg (243.8 mg), sodium carboxymethyl starch 4.0 mg (8, 0 mg), magnesium stearate 2.0 mg (4.0 mg), silicon dioxide colloid 0.8 mg (1.6 mg).

    Description:

    Tablets 5 mg - white, round, biconvex.

    Tablets 10 mg - round, white, flat-cylindrical, with a facet and a risk.
    Pharmacotherapeutic group:The blocker of "slow" calcium channels
    ATX: & nbsp
  • Amlodipine
  • Pharmacodynamics:

    The dihydropyridine derivative blocking the "slow" calcium channels (BCCI) has an antianginal and hypotensive effect.Linking with dihydropyridine receptors, blocks calcium channels, reduces the transmembrane transition of calcium ions into the cell (mostly in smooth muscle cells of blood vessels, rather than in cardiomyocytes). Antianginal effect is due to the expansion of coronary and peripheral arteries and arterioles: with angina decreases the severity of myocardial ischemia; expanding peripheral arterioles, reduces the overall peripheral vascular resistance, reduces preload on the heart, reduces the need for myocardium in oxygen. Expanding the main coronary arteries and arterioles in unchanged and ischemic zones of the myocardium, increases the flow of oxygen into the myocardium (especially with vasospastic angina); prevents the development of constriction of the coronary arteries (including caused by smoking). In patients with angina, the daily dose increases the time until the onset of the first ischemic episode during exercise, reduces the incidence of angina attacks and the consumption of nitroglycerin and other nitrates.

    Has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to a direct vasodilating effect on smooth muscle vessels.When hypertension single dose provides a clinically significant decrease in blood pressure (BP) over 24 hours (with the patient "lying" and "standing"). Does not cause a sharp decrease in blood pressure, a decrease in exercise tolerance, a fraction of the ejection of the left ventricle. Reduces the degree of myocardial hypertrophy of the left ventricle.

    In patients with coronary artery disease (CAD) (including coronary atherosclerosis with a lesion of the vessel and to the stenosis 3 or more arteries and carotid atherosclerosis), myocardial infarction, percutaneous transluminal angioplasty of coronary arteries (PTCA) or angina pectoris, amlodipine It prevents the development of a thickening of intima-media carotid arteries, reduces mortality from myocardial infarction, stroke, PTCA, coronary artery bypass surgery, reduces the number of hospitalizations for unstable angina and progression of chronic heart failure, reduces the frequency of interventions aimed at restoring coronary blood flow. Amlodipine does not increase the risk of death or development of complications leading to fatal outcomes in patients with chronic heart failure (CHF) (III-IV functional class by classification NYHA) on the background of therapy with digoxin, diuretics and angiotensin-converting enzyme (ACE) inhibitors. In patients with CHF (III-IV functional class by classification NYHA) non-ischemic etiology in the use of amlodipine, there is a possibility of pulmonary edema. Does not affect the contractility and conductivity of the myocardium, does not cause a reflex increase in the frequency of cardiac (HR), inhibits platelet aggregation, increases the rate of glomerular filtration, and has a weak natriuretic effect. When diabetic nephropathy does not increase the severity of microalbuminuria. Does not have adverse effects on the metabolism and concentration of lipids in the blood plasma. The time of onset of the effect is 2-4 hours, the duration of the effect is 24 hours.

    Pharmacokinetics:

    After oral administration amlodipine is slowly absorbed from the gastrointestinal tract. The average absolute bioavailability is 64 %, the maximum concentration in serum is observed after 6-9 hours. Equilibrium serum concentrations are achieved after 7-8 days of 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 the tissues, and relatively less in the blood. Most of the drug in the blood (95%), binds to blood plasma proteins. Amlodipine is subjected to a slow but active metabolism in the liver in the absence of a significant "primary transmission" effect. Metabolites do not have significant pharmacological activity.

    After a single administration, the half-life period (T1 / 2) varies from 31 to 48 hours, with a repeated appointment of T1 / 2 it is approximately 45 hours. About 60% of the dose taken internally is excreted by the kidneys mainly in the form of metabolites, 10% - unchanged, and 20-25% through the intestines with bile. The total clearance of amlodipine is 0.116 ml / s / kg (7 ml / min / kg, 0.42 l / h / kg).

    In elderly patients (over 65 years), amlodipine withdrawal is slowed (T1 / 2 65 h) compared with young patients, but this difference is not clinically significant.

    In patients with hepatic insufficiency, an elongation of T1 / 2 is assumed, and with prolonged administration the cumulation of the drug in the body will be higher (T1 / 2 to 60 h). 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 (monotherapy or combinations with others hypotensive drugs).

    Stenocardia of tension, vasospastic angina (angina pectoris Prinzmetal) (in monotherapy or in combination with other antianginal agents).

    Contraindications:
    • Hypersensitivity to amlodipine, other components of the drug and other dihydropyridine derivatives;
    • severe arterial hypotension (systolic blood pressure less than 90 mm Hg);
    • clinically significant aortic stenosis; collapse, cardiogenic shock;
    • unstable angina (with the exception of Prinzmetal angina);
    • pregnancy and lactation;
    • age to 18 years (efficacy and safety not established).
    Carefully:

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

    Pregnancy and lactation:

    In experimental studies fetotoxic and embryotoxic effects of the drug have not been established, but use in pregnancy is possible only if the benefit to the mother exceeds the potential 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. In this connection, when it is necessary to prescribe the drug Amlodipine During the lactation period, the issue of stopping breastfeeding should be addressed.

    Dosing and Administration:

    Inside, once a day, regardless of food intake, with a sufficient amount of water (100 ml). The initial dose for arterial hypertension and angina is 5 mg 1 time per day. The maximum dose can be increased to 10 mg once a day. It is recommended to increase the dose 7-14 days after the start of therapy (a faster increase in the dose requires careful monitoring of the patient). In elderly patients, T1 / 2 amlodipine may increase and creatinine clearance (CC) decrease. Dose changes are not required, but more careful monitoring of patients is necessary.Do not require dose changes when used simultaneously with thiazide diuretics, beta-blockers and angiotensin-converting enzyme (ACE) inhibitors. Do not require dose changes in patients with renal insufficiency.

    Side effects:

    The incidence of adverse reactions listed below was determined according to the following (World Health Organization classification): very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%, including individual reports.

    Co cardiovascular system: often - peripheral edema (ankles and feet), a feeling of palpitations, a sensation of heat and a "tide" of blood to the skin of the face; infrequently - excessive reduction of blood pressure, orthostatic hypotension, vasculitis; rarely - development or exacerbation of heart failure; very rarely - shortness of breath, heart rhythm disturbances (including bradycardia, ventricular tachycardia and atrial fibrillation), myocardial infarction, chest pain, pulmonary edema.

    From the central nervous system: often - headache (especially at the beginning of treatment), dizziness,increased fatigue, drowsiness; infrequent - general malaise, hypoesthesia, asthenia, paresthesia, tremor, insomnia, emotional lability, unusual dreams, nervousness, depression, increased sweating; rarely - convulsions, vertigo, fainting, apathy, agitation; very rarely - ataxia, amnesia.

    From the digestive system: often - nausea, pain in the abdomen; infrequent - vomiting, flatulence, constipation or diarrhea, dryness of the oral mucosa, thirst; rarely - gingival hyperplasia, increased appetite; very rarely - pancreatitis, gastritis, jaundice (usually cholestatic), increased activity of "liver" transaminases, hepatitis.

    From the hematopoiesis: very rarely - leukopenia, thrombocytopenia.

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

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

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

    From the skin: rarely - dermatitis; very rarely - alopecia, xeroderma, purpura, cold sticky sweat, a violation of skin pigmentation.

    Allergic reactions: rarely - skin itching, rash (including erythematous, maculopapular rash); very rarely - hives, angioedema, erythema multiforme.

    From the sense organs: infrequent - ringing in the ears, impaired vision, diplopia, accommodation disorder, xerophthalmia, conjunctivitis, pain in the eyes, perversion of taste; very rarely - parosmia.

    From the side of metabolism: very rarely - hyperglycemia.

    Other: infrequently - weight loss, weight gain, chills.

    Overdose:

    Symptoms: a marked decrease in blood pressure, tachycardia, excessive peripheral vasodilation.

    Treatment: gastric lavage, the appointment of activated charcoal, maintenance of cardiovascular function, control of heart and lung function, elevated position of the lower extremities, control of the volume of circulating blood and diuresis. To restore the vascular tone - the use of vasoconstrictive drugs (in the absence of contraindications to their use); to eliminate the effects of calcium channel blockade - intravenous calcium gluconate.

    Hemodialysis is not effective.

    Interaction:

    Inhibitors of microsomal oxidation increase the concentration of amlodipine in the blood plasma, increasing the risk of side effects, and inductors of microsomal liver enzymes reduce.

    Hypotensive effect weakens non-steroidal anti-inflammatory drugs, especially indomethacin (sodium retention and blockade of prostaglandin synthesis by the kidneys), alpha-adrenostimulants, estrogens (sodium retention), sympathomimetics. Thiazide and "loop" diuretics, beta-blockers, verapamil, ACE inhibitors and nitrates increase antianginal and hypotensive effects.

    Erythromycin in a joint application increases CmOh Amlodipine in young patients by 22%, and in the elderly by 50%.

    A single dose of 100 mg of sildenafil in patients with arterial hypertension does not affect the pharmacokinetics of amlodipine.

    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.

    Ethanol (drinks containing alcohol): amlodipine at a single and repeated application in a dose of 10 mg does not affect the pharmacokinetics of ethanol.

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

    Amiodarone, quinidine, alpha 1-adrenoblockers, antipsychotic drugs (neuroleptics) and blockers of "slow" calcium channels can enhance hypotensive action.

    Does not affect the pharmacokinetic parameters of digoxin and warfarin. Cimetidine does not affect the pharmacokinetics of amlodipine.

    When combined with preparations of lithium may be increased manifestations of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).

    Calcium preparations can reduce the effect of blockers of "slow" calcium channels.

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

    Grapefruit juice can reduce the concentration of amlodipine in the blood plasma, but this decrease is so small that it does not significantly alter the effect of amlodipine.

    Special instructions:

    During the treatment period it is necessary to control the body weight and sodium intake.

    It is necessary to maintain oral hygiene and frequent visits to the dentist (to prevent soreness,bleeding and gingival hyperplasia).

    When using the drug Amlodipine in patients with chronic heart failure III and IV functional class by classification NYHA possibly the development of pulmonary edema.

    Dosage regimen for the elderly is the same as for patients of other age groups. When increasing the dose, careful monitoring of elderly patients is necessary. Despite the lack of "slow" calcium channels of the syndrome of "cancellation" in blockers, a gradual decrease in doses is recommended before cessation of treatment. Amlodipine does not affect the potassium content and plasma concentrations of glucose, triglycerides, total cholesterol, low density lipoprotein (LDL), uric acid, creatinine and uric acid nitrogen. Amlodipine can be used to treat arterial hypertension in combination with thiazide diuretics, alpha-blockers, beta-blockers or ACE inhibitors. In patients with stable angina, the drug can be combined with other antianginal agents, for example, with prolonged or short-acting nitrates, beta-blockers.

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

    There were no reports of Amlodipine's influence on driving or working with machinery. However, some patients may experience drowsiness and dizziness at the beginning of treatment. When they occur, the patient should refrain from driving and working with machinery.

    Form release / dosage:

    Tablets of 5 or 10 mg.

    Packaging:

    For 10 tablets of 5 mg or 10 mg per blister.

    For 2 or 3 blisters together with instructions for use in a cardboard box.
    Storage conditions:

    In a dry, the 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 time specified on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-002020
    Date of registration:14.10.2011
    Expiration Date:Unlimited
    The owner of the registration certificate:REPLEK FARM Skopje, OOOREPLEK FARM Skopje, OOO Macedonia
    Manufacturer: & nbsp
    Representation: & nbspPharm Company Sotex CJSC Pharm Company Sotex CJSC Russia
    Information update date: & nbsp11.08.2017
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