Active substanceAmlodipineAmlodipine
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    Active substance:

    Amlodschina besylate (amlodipine) - 6.944 mg (5.00 mg).

    Amlodipine besylate (amlodipine) -13.888 mg (10.00 mg).

    Excipients: Microcrystalline cellulose, calcium hydrophosphate (anhydrous), sodium carboxymethyl starch (type A), magnesium stearate.

    Description:

    Tablets 5 mg. Round biconvex tablets of white color. On one side is engraving "АВ 5". The other side is smooth.

    Tablets 10 mg. Round biconvex tablets of white color. On one side is the dividing risk and the engraving "AB 10". The other side is smooth.

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

    C.08.C.A.01   Amlodipine

    Pharmacodynamics:

    The blocker of the "slow" calcium channels, the dihydropyridine derivative, the "slow" calcium channel blocker (BCCI) of the second generation,has antianginal and hypotensive action. Blocking calcium channels, reduces the transmembrane passage of calcium ions into the cell (mainly in vascular smooth muscle cells than cardiac myocytes).

    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 (OISS), reduces afterload on the heart, reduces the need for myocardium in oxygen. Expanding 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 spasm of the coronary arteries (including caused by smoking). In patients with stable angina, a single daily dose increases exercise tolerance, increases the time until the onset of an attack of angina and "ischemic" depression of the segment ST, reduces the incidence of angina attacks and the consumption of nitroglycerin in other nitrates. 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 decrease in blood pressure (BP) for 24 hours (in the patient's "lying" and "standing ".) Orthostatic hypotension in the appointment of amlodipine is rare, does not cause a decrease in the left ventricular ejection fraction, reduces the degree of left ventricular myocardial hypertrophy, does not affect myocardial contractility and conductivity, 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 any adverse effect on metabolism and lipid concentration plasma and can be used in the treatment of patients with bronchial asthma, diabetes and gout. A significant decrease in blood pressure is observed after 6-10 hours, the duration of the effect is 24 hours.

    In patients with diseases of the cardiovascular system,including coronary atherosclerosis with one vessel and up to stenosis of 3 or more arteries, atherosclerosis of carotid arteries after myocardial infarction, percutaneous transluminal angioplasty (PTCA) of coronary arteries or patients with angina, the use of amlodipine prevents the development of thickening of intima-media of carotid arteries, reduces mortality from myocardial infarction, stroke, PTCA, aorto-coronary bypass; leads to a decrease in the incidence of unstable angina and the progression of chronic heart failure (CHF); reduces the frequency of interventions aimed at restoring coronary blood flow.

    Does not increase the risk of death or development of complications and deaths in patients with CHF (III-IV functional class by classification NYHA) on the background of therapy with digoxin, diuretics and inhibitors of anthotensin-converting enzyme (ACE). 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.

    Pharmacokinetics:

    After oral administration amlodipine slowly absorbed from the gastrointestinal tract (GIT).The average absolute bioavailability is 64%, the maximum concentration (Cmax) in the serum is observed after 6-9 hours. The equilibrium concentrations (CSS) 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 the smaller - 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 "first passage" effect. Metabolites do not have significant pharmacological activity. After a single administration, the half-life period (T1 / 2) varies from 35 to 50 hours, with repeated application 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 of age), amlodipine excretion is slowed (T1 / 2 hours 65 hours) compared with young patients, but this difference is not clinically significant.Elongation of T1 / 2y patients with liver failure suggests that with prolonged use, cumulation 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. In patients with impaired renal function, changes in amlodipine concentration in the blood plasma do not correlate with the degree of renal failure. Perhaps a slight increase in T1 / 2.

    Amlodipine penetrates the blood-brain barrier. When hemodialysis is not removed.

    Indications:

    - arterial hypertension.

    - stable angina pectoris and vasospastic angina.

    Contraindications:

    - hypersensitivity to amlodipine, other derivatives of dihydropyridine and other components of the drug;

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

    - cardiogenic shock;

    - acute myocardial infarction (within the first 28 days);

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

    - obstruction of the outflow tract of the left ventricle;

    - clinically significant aortic stenosis;

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

    Carefully:violations of liver function, syndrome of weakness of the sinus node (pronounced bradycardia, tachycardia), CHF of non-ischemic etiology-IV functional class by classification NYHA, arterial hypotension, aortic stenosis, mitral stenosis, acute myocardial infarction (after the first 28 days), elderly age, impaired renal function.
    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 connection with this, if it is necessary to prescribe Amlodipine-Teva during lactation, the question of stopping breastfeeding should be resolved.

    Dosing and Administration:

    Inside, once a day, washing down with the necessary amount of water (100 ml).

    With arterial hypertension and angina, the initial dose is 5 mg once a day.In the absence of therapeutic effect for 2-4 weeks, the dose of the drug can be increased to 10 mg / day. once.

    Have elderly patients

    Correction of the dose is not required.

    Have patients with impaired liver function

    Despite the fact that T1 / 2 amlodipine, like all BCCCs, increases in patients with impaired liver function, dose adjustment is usually not required (see section "Special instructions").

    Have patients with renal insufficiency

    It is recommended to use Amlodipine-Teva in usual doses (see section "Special instructions").

    Side effects:

    The frequency of adverse reactions listed below was determined according to the following (classification of the World Health Organization): 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.

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

    From the digestive system: often - nausea, pain in the abdomen; infrequently - vomiting, anorexia, dryness of the oral mucosa, thirst; rarely - gingival hyperplasia, increased appetite; very rarely - pancreatitis, gastritis, jaundice (usually cholestatic), hyperbilirubinemia, increased activity of "hepatic" transaminases, hepatitis.

    From the cardiovascular system: often - peripheral edema (ankles and feet), palpitations, "hot flashes" of blood to the skin of the face; infrequently - excessive reduction of blood pressure, orthostatic hypotension, vasculitis; rarely - development or aggravation of the course of CHF; very rarely - fainting, shortness of breath, heart rhythm disturbances (including bradycardia, ventricular tachycardia and atrial fibrillation), myocardial infarction, pain in a difficult cage, pulmonary edema.

    From the hematopoietic and lymphatic systems: rarely - thrombocytopenic purpura, leukopenia, thrombocytopenia.

    From the stroma of the urinary system: infrequently - pollakiuria, painful urge to urinate, nocturia; very rarely - dysuria, polyuria.

    From the country of the reproductive system and mammary glands: infrequently - gynecomastia, impotence.

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

    From the musculoskeletal system: infrequently - muscle cramps, myalgia, arthralgia, back pain, arthrosis; rarely - myasthenia gravis.

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

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

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

    From the side of metabolism: very rarely - hyperglycemia.

    Other: infrequently - weight loss, weight gain, taste distortion, epistaxis, chills.

    Overdose:

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

    Treatment: gastric lavage, the use of activated charcoal (especially in the first 2 hours after an overdose), maintaining the function of the cardiovascular system, elevating the position of the lower limbs, monitoring the heart and lung function, monitoring the volume of circulating blood (BCC) 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:

    Amlodipine can be safely used for the therapy of arterial hypertension along with thiazide diuretics, alpha-adrenoblockers or ACE inhibitors. In patients with stable angina pectoris amlodipine can be combined with other antianginal agents, for example, with nitrates of prolonged or short-acting.

    In contrast to other BCCC, the clinically significant interaction of amlodipine (II generation BCCI) was not detected in a joint application with anti-inflammatory drugs (NSAIDs), including indomethacin.It is possible to increase the anti-anginal and hypotensive effect of BCCC when combined with thiazide and loop diuretics, ACE inhibitors and nitrates, as well as enhance their hypotensive effect when combined with alpha1-blockers.

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

    Beta-adrenoblockers with simultaneous application with amlodipine can cause an exacerbation of the course of heart failure.

    Although no negative inotropic effects were usually observed in the study of amlodipine, nevertheless, some BCCCs can increase the severity of the negative inotropic effect of antiarrhythmic agents that cause lengthening of the interval QT (eg, amiodarone and quinidine).

    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.

    Antiretroviral agents (ritonavir) increases plasma concentrations of BCCC, including amlodipine.

    Neuroleptics and isoflurane - strengthening of hypotensive action of derivatives dihydropyridine.

    Calcium preparations can reduce the effect of BCCC.

    When amlodipine is used together with lithium preparations, it is possible to intensify manifestations of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus). Amlodipine does not change the pharmacokinetics of cyclosporine.

    Does not affect the concentration of serum digoxin and its renal clearance.

    Has no significant effect on the effect of warfarin (prothrombin time). Cimetidine does not affect the pharmacokinetics of amlodipine.

    In studies in vitro Amlodipine does not affect the binding of blood proteins to digoxin, phenytoin, warfarin and indomethacin.

    Grapefruit juice: simultaneous single intake of 240 mg of grapefruit juice and 10 mg of amlodipine inwards is not accompanied by a significant change in the pharmacokinetics of amlodipine.

    Aluminum- or magnesium-containing antacids: their single administration does not have a significant effect on the pharmacokinetics of amlodipine.

    Special instructions:

    During the period of therapy with the drug Amlodipine-Teva it is necessary to control body weight and sodium intake, the purpose of the appropriate diet is indicated.

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

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

    In acute myocardial infarction, amlodipine-Teva is prescribed after stabilization of hemodynamic parameters (see section "Contraindications").

    Patients with hepatic insufficiency if necessary to take Amlodipine-Teva should be supervised doctor.

    In elderly patients, T1 / 2 may increase and the clearance of the drug may decrease. Dose changes are not required, but more careful monitoring of patients of this category is necessary.

    In patients with impaired renal function, monitoring of the condition is necessary. The effectiveness and safety of the drug Amlodipina-Teva with hypertensive crisis is not established.

    Despite the absence of the "cancellation" syndrome in BCC, it is advisable to stop the treatment with Amlodipine-Teva, gradually reducing the dose of the drug.

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

    Although amlodipine-Teva did not have any negative effect on the ability to drive vehicles or other complex mechanisms, however, due to the possible excessive decrease in blood pressure, development of dizziness, drowsiness and other adverse reactions, caution should be exercised in the listed situations, especially at the beginning of treatment and with increasing doses.

    Form release / dosage:

    Tablets 5 mg and 10 mg.

    Packaging:

    For 10 tablets per blister of A1 / PVC / PVDC.

    For a dosage of 5 mg. 1 or 3 blisters per pack of cardboard along with the instructions for use.

    For the dosage of 10 ml of 1, 2 or 3 blisters per pack of cardboard along with the instructions for use.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children!

    Shelf life:

    5 years.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-005772/10
    Date of registration:23.06.2010
    The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel
    Manufacturer: & nbsp
    Representation: & nbspTeva Teva Israel
    Information update date: & nbsp09.07.2010
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