Active substanceAmlodipineAmlodipine
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  • Dosage form: & nbsppills
    Composition:

    1 tablet 5 mg contains: active substance: amlodipine besylate - 7.0 mg, which corresponds to 5 mg of amlodipine base; Excipients: povidone To 30 - 20.0 mg, microcrystalline cellulose - 60.0 mg, calcium hydrophosphate - 113.0 mg, crospovidone - 17.0 mg, magnesium stearate - 3.0 mg.

    1 tablet of 10 mg contains: active substance: amlodipine besylate-14.0 mg, which corresponds to 10 mg of amlodipine base; Excipients: povidone To 30 - 20.0 mg, microcrystalline cellulose - 60.0 mg, calcium hydrophosphate - 106.0 mg, crospovidone - 17.0 mg, magnesium stearate - 3.0 mg.

    Description:

    Tablets 5 mg - white or almost white round biconvex tablets.

    Tablets 10 mg - white or almost white round biconvex tablets, with a risk on both sides;

    Pharmacotherapeutic group:The blocker of "slow" calcium channels
    ATX: & nbsp

    C.08.C.A.01   Amlodipine

    Pharmacodynamics:

    The dihydropyridine derivative blocking the "slow" calcium channels of the second generation, 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 pectoris The daily dose increases the time of exercise, slows the development of angina pectoris and the "ischemic" depression of the segment ST, reduces the incidence of angina attacks and consumption of nitroglycerin.

    Has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to a direct vasodilating effect on smooth muscle vessels. With arterial hypertension, a single dose provides a clinically significant reduction in blood pressure over a 24-hour period (in the "lying" and "standing" position). Does not cause a sharp decrease in blood pressure (BP), a decrease in exercise tolerance, or a fraction of the left ventricular ejection. Reduces the degree of myocardial hypertrophy of the left ventricle, has antiatherosclerotic and cardioprotective effect in coronary heart disease. Does not affect the contractility and conductance of the myocardium, does not cause a reflex increase in the heart rate (HR), inhibits platelet aggregation, increases the rate of glomerular filtration, has a weak natriuretic effect. When diabetic nephropathy does not increase the severity of microalbuminuria.Does not have adverse effects on the metabolism and lipids of 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 serum concentration is observed after 6-9 hours. The concentration of stable equilibrium is reached after 7 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 extensive metabolism (90%) in the liver with the formation of inactive metabolites, has the effect of a "first pass" through the liver. Metabolites do not have significant pharmacological activity.

    After a single oral intake, the half-life period (T1 / 2) varies from 31 to 48 hours, with the repeated appointment of T1 / 2 is approximately 45 hours.About 60% of the dose taken internally excreted by the kidneys mainly in the form of metabolites, 10% unchanged, and 20-25% through the intestine, as well as breast milk. 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 of age) the excretion of amlodipine is slowed (T1/2 65 hours) compared with young patients, but this difference is not of clinical significance. Patients with hepatic impairment are expected to have T1 / 2 lengthening, and with long-term administration, the accumulation 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 penetrates the blood-brain barrier. When hemodialysis is not removed.

    Indications:

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

    Stenocardia of tension, vasospastic angina (Prinzmetal angina).

    Contraindications:

    - Hypersensitivity to amlodipine and other dihydropyridine derivatives;

    - severe arterial hypotension;

    - collapse, cardiogenic shock;

    - unstable angina (with the exception of Prinzmetal angina)

    - pronounced anterior aortic stenosis

    - pregnancy and lactation;

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

    Carefully:

    Dysfunction of the liver, syndrome of weakness of the sinus node (severe bradycardia, tachycardia), chronic heart failure in the stage of decompensation, mild or moderate degree of arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after), advanced age, simultaneous use of beta- adrenoblockers and digoxin.

    Dosing and Administration:

    Inside, the initial dose for treatment arterial hypertension and angina pectoris is 5 mg of the drug 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.

    When angina pectoris and vasospastic angina pectoris - 5 - 10 mg per day, once.

    Do not require dose changes with simultaneous administration with thiazide diuretics, beta-blockers and angiotensin-converting enzyme inhibitors.

    Do not require dose changes in patients with renal insufficiency.

    Patients with low body weight or low growth, as well as with severe hepatic insufficiency, may require smaller doses.

    Side effects:

    From the side of the cardiovascular system, palpitations, dyspnea, marked decrease in blood pressure, fainting, vasculitis, peripheral edema (swelling of the ankles and feet), "tides" of blood to the skin of the face, rarely - rhythm disturbances (bradycardia, ventricular tachycardia, atrial flutter), myocardial infarction, chest pain , orthostatic hypotension, very rarely - development or aggravation of heart failure, extrasystole, migraine.

    From the central nervous system: headache, dizziness, fatigue, drowsiness, mood lability, convulsions, rarely - loss of consciousness, hypoesthesia, peripheral neuropathy, paresthesia, tremor, vertigo, asthenia, malaise, insomnia, depression, unusual dreams, very rarely - ataxia, apathy, agitation, amnesia.

    From the digestive system: nausea, vomiting, epigastric pain, rarely - increased activity of "liver" transaminases and jaundice (caused by cholestasis), pancreatitis, dry mouth, thirst, hepatitis, flatulence, gingival hyperplasia,constipation or diarrhea, very rarely - gastritis, increased appetite, anorexia, hyperbilirubinemia.

    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, alopecia, dermatitis, purpura, a violation of skin pigmentation.

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

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

    Other: rarely - gynecomastia, hyperuricemia, increase / decrease in body weight, thrombocytopenia, leukopenia, hyperglycemia, impaired vision, diplopia, conjunctivitis, eye pain, ringing in the ears, back pain, dyspnoea, epistaxis, increased sweating, thirst; very rarely - cold sticky sweat, cough, rhinitis, parosmia, taste disorders, accommodation disorder, xerophthalmia.

    Overdose:

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

    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 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.

    Unlike other BCCI, 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 increase the antianginal and hypotensive effect.

    Amiodarone, quinidine, alpha1-adrenoblockers, antipsychotics (antipsychotics) and BCCC may increase the hypotensive effect.

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

    Cimetidine does not affect the pharmacokinetics of amlodipine.

    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.

    Neuroleptics and isoflurane - Increased hypotensive effect of dihydropyridine derivatives.

    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 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).

    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 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.

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

    There were no reports of the effects of amlodipine on driving or working with machinery. However, some patients may experience drowsiness and dizziness at the beginning of treatment. When they occur, the patient must observe special precautions when driving and working with machinery.

    Form release / dosage:

    Tablets of 5 and 10 mg.

    Packaging:

    10 tablets per blister of PVC/ PVDC- AI .

    By 3, 5, 10 and 30 blisters together with instructions for use in a cardboard box.
    Storage conditions:

    List B.

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use the drug after the date shown on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-000378
    Date of registration:25.02.2011
    Expiration Date:25.02.2016
    Date of cancellation:2016-03-10
    The owner of the registration certificate:Wörwag Pharma GmbH & Co. KG. KGWörwag Pharma GmbH & Co. KG. KG Germany
    Manufacturer: & nbsp
    Representation: & nbspVEVWAG PHARMA GmbH & Co. KG VEVWAG PHARMA GmbH & Co. KG Germany
    Information update date: & nbsp13.09.2017
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