Expiration date: 03/2025
Amlodipine
International name: Amlodipine (Amlodipine)
Group affiliation: bmkk
Description of active ingredient (INN): Amlodipine
Dosage form:
capsules, tablets
Pharmacological action:
A derivative of dihydropyridine - down BCCI II generation, has antianginal and hypotensive action. Communicating with digidropiridinovmi receptors, does calzieve channels, lowers transmembranny transition of Ca2+ into the cell (more in gladkomyshechne cells receptacles, than cardiomiotita). Antianginal effect is due to the expansion of the coronary and peripheral arteries and arterioles: with angina reduces the severity of myocardial ischemia, expanding peripheral arterioles, reduces OPSS, reduces preload on the heart, reduces myocardial oxygen demand. Expanding the main coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, increases the flow of oxygen to the myocardium (especially in vasospastic angina), prevents the development of coronary artery constriction (including Smoking). In patients with angina, a single daily dose increases the time of physical activity, slows the development of angina and "ischemic" s-T segment depression, reduces the frequency of angina attacks and nitroglycerin consumption. It has a long dose-dependent hypotensive effect. Hypotensive effect due to direct vasodilating effect on the smooth muscles of blood vessels. In hypertension, a single dose provides a clinically significant decrease in blood PRESSURE for 24 hours (in the patient's "lying" and "standing"). Does not cause a sharp decrease in blood PRESSURE, reduced tolerance to physical activity, the fraction of LV release. Reduces the degree of myocardial hypertrophy of the left ventricle, exerts anti-atherosclerotic and cardioprotective action in coronary heart disease. Does not increase the risk of death in patients with CHF (III-IV NYHA class), during treatment with digoxin, diuretics and ACE inhibitors. It does not affect the contractility and conductivity of the myocardium, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases glomerular filtration rate, has a weak natriuretic effect. In diabetic nephropathy does not increase the severity of microalbuminuria. It has no adverse effects on the metabolism and plasma lipids. The time of onset of effect - 2-4 h, duration - 24 h
Indications:
Hypertension, angina pectoris, vasospastic angina, silent myocardial ischemia, decompensated CHF (as adjuvant therapy).
Contraindications:
Hypersensitivity (including to other dihydropyridines), severe hypotension, pregnancy, lactation.With caution. With caution-hypotension, aortic stenosis, CHF, hepatic insufficiency, acute myocardial infarction (and within 1 month after), age up to 18 years (efficacy and safety are not installed), old age. When assigning amlodipine (similar to other dihydropyridines) in patients with HACMP, SSSU and mitral stenosis, care must be taken.
Side effect:
From the nervous system: headache, dizziness, excessive fatigue, drowsiness, mood changes, convulsions, rarely - loss of consciousness, hyperesthesia, paresthesia, tremor, asthenia, malaise, insomnia, nervousness, depression, extraordinary dreams, anxiety, very rarely - ataxia, apathy, agitation, amnesia. From the digestive system: nausea, abdominal pain, hyperbilirubinemia, jaundice, increased activity of "hepatic" transaminases, rarely - dry mouth, anorexia, vomiting, constipation or diarrhea, dyspepsia, flatulence, hyperplasia of the gums, very rarely - gastritis, increased appetite, pancreatitis. From the CCC: heartbeat, swelling of the ankles and feet, shortness of breath, "tides" of blood to the face, rarely - arrhythmia (bradycardia, ventricular tachycardia, atrial flutter), chest pain, decreased blood PRESSURE, orthostatic hypotension, very rarely - the development or aggravation of CH, extrasystole, increased blood PRESSURE, migraine. On the part of the genitourinary system: rarely-pollakiuria, painful urge to urinate, nicturia, violation of sexual function (including decreased potency), very rarely - dysuria, polyuria. From the musculoskeletal system: rarely-arthralgia, arthrosis, myalgia (with prolonged use), very rarely - myasthenia gravis. From the skin: very rarely-xeroderma, alopecia, dermatitis, purpura. Allergic reactions: itching, rash (including erythematous, maculopapular rash, urticaria). Other: rare - impaired vision, conjunctivitis, diplopia, eye pain, disturbance of accommodation, xerophthalmia, ringing in the ears, gynecomastia, back pain, feeling of heat "tides" of blood to the face, chills, increase in body weight, dyspnea, nasal bleeding, increased sweating, the thirst; very rarely-cold clammy sweat, cough, rhinitis, parosmia, taste perversion, hyperglycemia.
Overdose:
Symptoms: excessive peripheral vasodilation, decreased blood pressure, tachycardia. Treatment: gastric lavage, the appointment activated carbon, the maintenance of the functions of the cardiovascular system, monitoring of indicators of function of heart and lungs, exalted position of extremities, control of the BCC and diurezom, symptomatic and supportive therapy, in/with the introduction of calcium gluconate and dopamine. Hemodialysis is ineffective.
Dosage and administration:
Inside, the initial dose-5 mg / day at a time with a gradual increase for 7-14 days to 10 mg/day once, with hypertension supporting dose - 2.5-5 mg/day. In angina pectoris and vasospastic angina-5-10 mg / day once, for the prevention of angina attacks-10 mg / day. Thin patients, patients of small stature, elderly patients, patients with impaired liver function as anti-hypertensive drugs administered in an initial dose of 2.5 mg, as antianginalnogo LS - 5 mg. With CHF, the initial dose is 2.5 mg 1 time per day, with good tolerability, the dose is gradually increased to 10 mg 1 time per day.
Special instruction:
Safety of use during pregnancy and lactation is not established. Experience of application in children is absent. During treatment, it is necessary to control the body weight and be observed at the dentist (to prevent pain, bleeding and hyperplasia of the gums). Amlodipine does not affect plasma concentrations of K+, glucose, triglycerides, total cholesterol, LDL, uric acid, creatinine and urea nitrogen. Despite the absence of "withdrawal" syndrome in bmcc, a gradual reduction of doses is recommended before discontinuation of treatment.
Interaction:
Inhibitors of microsomal oxidation increase the concentration of amlodipine in plasma, increasing the risk of side effects, and inducers of microsomal liver enzymes reduce. Weaken hypotensive effect of NSAIDs, especially indometacin (delay of Na+ and blockade of Pg synthesis by the kidney), alpha-agonists, estrogens (delay of Na+), simpatomimetiki. Thiazide and loop diuretics, beta-blockers, verapamil, ACE inhibitors and nitrates enhance antianginal and hypotensive effects. Amiodarone, quinidine, alpha1-adrenoblokatora, antipsychotic drugs (neuroleptics) and bmkk may increase the hypotensive action. It has no effect on the pharmacokinetic parameters of digoxin and warfarin. Cimetidine does not affect the pharmacokinetics of amlodipine. When combined with drugs Li+ may increase the manifestations of their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus). Preparations of Ca2+ can reduce the effects bmkk. Procainamide, quinidine, etc. LS, causing an extension of the q-T interval, increase the negative inotropic effect and may increase the risk of a significant extension of the q-t interval.
