Pharmacological action Amlodipine 5 mg:
Dihydropyridine derivative – BCCI II generation, has antianginal and hypotensive action. Dihydropyridine binding to receptors, blocking calcium channels, reduces the transmembrane passage of Ca2 + in the cell (to a greater extent in vascular smooth muscle cells than in cardiomyocytes). Antianginal effect is due to the expansion of the coronary and peripheral arteries and arterioles: angina reduces the severity of myocardial ischemia extending peripheral arterioles, reduces the PR, reduces preload on the heart, reducing myocardial oxygen demand. Expanding the major coronary arteries and arterioles in the unaltered and in the ischemic zone myocardium, increases oxygen to the myocardium (especially in vasospastic angina), prevents the development of constriction of the coronary arteries (including caused by smoking). In patients with angina single daily dose increases the run-time physical activity slows the development of angina and “ischemic” segment depression ST, reduces the frequency of angina attacks and nitroglycerin consumption. Has a long dose-dependent hypotensive effect. Hypotensive effect due to the direct vasodilating effect on vascular smooth muscle. When hypertension single dose provides clinically significant reductions in blood pressure over 24 hours (in the patient’s “lying” and “standing”). There is no sharp decrease in blood pressure, reduce exercise tolerance, left ventricular ejection fraction. Reduces the degree of hypertrophy, left ventricular, has anti-atherosclerotic and cardioprotective action in coronary artery disease. Does not increase the risk of death in patients with chronic heart failure (III-IV class NYHA), during therapy with digoxin, diuretics and ACE inhibitors. No effect on contractility and myocardial conduction, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases the glomerular filtration rate, has a weak natriuretic properties. In diabetic nephropathy does not increase the severity of microalbuminuria. It has no adverse effects on metabolism and plasma lipids. Time of onset of effect – 2-4 hours, duration – 24 hours
Uses Amlodipine 5 mg:
Hypertension, angina, vasospastic angina, painless myocardial ischemia, decompensated heart failure (as adjuvant therapy).
Contraindications Amlodipine 5 mg:
Hypersensitivity (including to other dihydropyridine), severe hypotension, pregnancy, lactation. Caution – hypotension, aortic stenosis, heart failure, liver failure, acute myocardial infarction (and within 1 month after), age 18 years (effectiveness and safety have not been established), advanced age. In the appointment of amlodipine (like other dihydropyridine) in patients with GOKMP, SSS and mitral stenosis should be careful.
Side effects Amlodipine 5 mg:
Nervous system disorders: headache, dizziness, excessive fatigue, drowsiness, mood changes, seizures, rare – loss of consciousness, hyperesthesia, paresthesia, tremor, fatigue, malaise, insomnia, nervousness, depression, unusual dreams, anxiety, very rarely – ataxia , apathy, agitation, amnesia. Part of the digestive system: nausea, abdominal pain, hyperbilirubinemia, jaundice, increased activity of “liver” enzymes, rarely – dry mouth, anorexia, vomiting, constipation or diarrhea, dyspepsia, flatulence, gingival hyperplasia, very rarely – gastritis, increased appetite , pancreatitis. From the CCC: heart rate, swelling of the ankles and feet, shortness of breath, “tides” of blood to the face, rarely – arrhythmias (bradycardia, ventricular tachycardia, atrial flutter), chest pain, lower blood pressure, orthostatic hypotension, very rarely – the development or worsening heart failure, arrythmia, increased blood pressure, migraine. Genitourinary: rare – thamuria, painful urge to urinate, nocturia, violation of sexual function (including reduced potency), very rarely – dysuria, polyuria. On the part of the musculoskeletal system: rarely – arthralgia, arthrosis, myalgia (with prolonged use), very rarely – myasthenia gravis. For the skin: very rare – dermatoxerasia, alopecia, dermatitis, purpura. Allergic reactions: itching, rash (including erythematous, maculopapular rash, urticaria). Other: rarely – blurred vision, conjunctivitis, diplopia, eye pain, disturbance of accommodation, xerophthalmia, tinnitus, gynecomastia, back pain, hot flashes and “tides” of blood to the face, chills, weight gain, dyspnea, epistaxis , increased sweating, thirst, very rarely – a cold clammy sweat, cough, rhinitis, parosmiya, taste perversion, гипергликемия.Передозировка. Symptoms: excessive peripheral vasodilation, reduced blood pressure, tachycardia. Treatment: gastric lavage, activated charcoal assignment, the maintenance functions of the SSA, the control performance of the heart and lungs, elevation of extremities, monitoring the BCC and diuresis, symptomatic and supportive therapy, in / to the introduction of calcium gluconate and dopamine. Hemodialysis is ineffective.
Dosage and administration Amlodipine 5 mg:
Inside, the initial dose – 5 mg / day at a time with a gradual increase within 7-14 days and 10 mg / day once, hypertension maintenance dose – 2.5-5 mg / day. If angina and vasospastic angina – 5.10 mg / day once, to prevent strokes – 10 mg / day. Thin patients, patients with a short, elderly patients, patients with impaired liver function as antihypertensive drugs administered in an initial dose of 2.5 mg as antiangialnogo PM – 5 mg. In CHF, the initial dose – 2.5 mg 1 time a day, if tolerated dose gradually increased to 10 mg 1 time per day.
Cautions:
Safety of pregnancy and lactation has not been established. Experience in children is missing. During the treatment necessary to control body weight and observed with a dentist (to prevent soreness, bleeding and gingival hyperplasia). Amlodipine did not affect the plasma concentrations of K +, glucose, triglycerides, total cholesterol, LDL cholesterol, uric acid, creatinine and urea nitrogen. Despite the lack of BCCI syndrome “cancel” before the termination of treatment recommended a gradual reduction in dose.
Interaction:
Inhibitors of microsomal oxidation increase the concentration of amlodipine in plasma, increasing the risk of side effects, and inducers of microsomal liver enzymes decrease. Antihypertensive effect of weakening the NSAIDs, especially indomethacin (delay of Na + and the blockade of the synthesis of Pg by the kidneys), alpha-adrenostimulyatorov, estrogens (delay Na +), sympathomimetic. Thiazide and “loop” diuretics, beta blockers, verapamil, ACE inhibitors and nitrates enhance the antianginal and antihypertensive effects. Amiodarone, quinidine, alpha 1-blockers, anti-psychotic drugs (neuroleptics) and the BCCI may increase the hypotensive effect. It has no effect on the pharmacokinetic parameters of digoxin and warfarin. Cimetidine does not affect the pharmacokinetics of amlodipine. In a joint application with preparations Li + may increase neurotoxicity manifestations (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus). Preparations of Ca2 + can reduce the effect of BCCI. Procainamide, quinidine and other drugs causing prolongation of the interval QT, reinforce the negative inotropic effect and may increase the risk of significant prolongation QT.
