Active substanceAmlodipineAmlodipine
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  • Dosage form: & nbsppills
    Composition:

    One tablet contains active substance: amlodipine besilata in terms of amlodipine - 5 mg or 10 mg;

    Excipients: milk sugar (lactose), cellulose microcrystalline, potato starch, calcium stearate, magnesium stearate.

    Description:

    Tablets are white, flat-cylindrical with a bevel.

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

    C.08.C.A.01   Amlodipine

    Pharmacodynamics:

    A selective calcium antagonist from the dihydropyridine group. 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).Under its action, the tone of the smooth muscle of the vessels (arterioles) decreases, the peripheral vascular resistance decreases, which leads to a decrease in blood pressure (BP). The hypotensive effect is due to a direct relaxing effect on the smooth muscle of the vessels. When angina decreases the severity of myocardial ischemia (due to the expansion of peripheral arterioles and a decrease in OPSS against the background of a slightly changing heart rate). Reducing the load on the heart leads to a decrease in myocardial oxygen demand; on the other hand, due to the expansion of the main coronary arteries and coronary arterioles both in the unchanged and in the ischemic zones of the myocardium, oxygen supply to the myocardium increases (especially with vasospastic angina). Prevents the development of constriction of the coronary arteries (including caused by smoking). With arterial hypertension, a single daily dose provides a clinically significant decrease HELL for 24 hours (both in the prone position and in the standing). Due to the slow onset of action does not cause a sharp decrease in blood pressure, a decrease in exercise tolerance, a fraction of the ejection of the left ventricle.In patients with angina, a single daily dose increases the time of exercise, slows the rate of development of angina and "ischemic" depression of the segment ST, reduces the incidence of angina attacks and consumption of nitroglycerin. Does not have adverse effects on the metabolism and lipids of blood plasma. The time of onset of clinical effect is 2-4 hours, duration - 24 hours.

    Pharmacokinetics:

    Slowly and almost completely absorbed from the gastrointestinal tract (absorption - 90%). Eating does not affect the absorption of the drug. The maximum concentration of the drug in the plasma is observed 6-9 hours after use. Bioavailability is 60-80%, the connection with plasma proteins is 90-97%.

    Amlodipine undergoes 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 elimination half-life (T1/2) varies from 31 to 48 hours, with a reappointment T1/2 is approximately 45 hours. About 60% of the dose taken internally excreted by the kidneys mainly in the form of metabolites, 10% in unchanged form, and 20-25% through the intestine, as well as with breast milk.

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

    Indications:

    Arterial hypertension (monotherapy or in combination with other antihypertensive agents), angina pectoris, vasospastic angina.

    Contraindications:

    - Hypersensitivity to amlodipine and other dihydropyridine derivatives;

    - arterial hypotension;

    - collapse, vascular and cardiogenic shock;

    - unstable angina;

    - pregnancy and lactation;

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

    Carefully:

    Prenal failure, sinus node weakness syndrome (severe bradycardia, tachycardia), chronic heart failure in decompensation stage, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after), diabetes mellitus, violations of the lipid profile, elderly age.

    Pregnancy and lactation:Contraindicated.
    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 - 5 - 10 mg per day, once. Thin patients, patients of low height, elderly patients, patients with impaired liver function as an antihypertensive drug are prescribed in an initial dose of 2.5 mg; as an antianginal agent - 5 mg.

    There is no need for dose changes with simultaneous administration with thiazide diuretics, beta-blockers and angiotensin-converting enzyme (ACE) inhibitors. Do not require dose changes in patients with renal insufficiency.

    Side effects:

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

    From the central nervous system: headache, dizziness, fatigue, drowsiness, mood changes, convulsions, rarely - loss of consciousness, hypnosis, nervousness, 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 levels of "liver" transaminases and jaundice (caused by cholestasis), pancreatitis, dry mouth, 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, discoloration.

    Allergic reactions: skin itching, rash (including erythematous, maculopapular rash, urticaria), angioedema.

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

    Other: rarely - gynecomastia, polyuricemia, 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 - excessive peripheral vasodilation, pronounced and prolonged decrease in blood pressure, tachycardia.

    Treatment - gastric lavage, maintenance of cardiovascular function, monitoring of heart and lung function, elevated limb position, control of circulating blood volume and diuresis, iv gluconate administration of calcium and dopamine. Hemodialysis is not effective.

    Interaction:

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

    Hypotensive effect weakens non-steroidal anti-inflammatory drugs (NSAIDs), especially indomethacin and estrogens. Means for inhalation anesthesia, amiodarone, quinidine and others, calcium antagonists can increase the hypotensive effect.

    Thiazide and "loop" diuretics, beta-blockers, ACE inhibitors, nitrates increase antianginal and antihypertensive effects.

    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 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 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 plasma concentrations of K+, glucose, triglycerides, total cholesterol, LDL, 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 5 mg and 10 mg.

    Packaging:

    10 tablets per contour cell pack.

    For 3, 5 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

    For 30 or 50 tablets in a can of polymer.Each bank along with the instruction for use is placed in a pack of cardboard.
    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:

    2 years. Do not use after the time specified on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-001785/08
    Date of registration:17.03.2008 / 06.02.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:ROSFARM, LLC ROSFARM, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp10.08.2017
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