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Active ingredients
Amlodipine
Release form
Pills
Composition
Amlodipine (in the form of besylate) 5 mg adjuvants: lactose, microcrystalline cellulose, calcium stearate, croscarmellose sodium, aerosil.
Pharmacological effect
Derivative of dihydropyridine - BPC II generation, has antianginal and hypotensive effects. Communicating with dihydropyridine receptors, it blocks calcium channels, reduces the transmembrane transition of calcium ions into the cell (to a greater extent - into vascular smooth muscle cells than into cardiomyocytes). expanding peripheral arterioles, reduces the round focal disease, reduces the preload on the heart, reduces the need for myocardium in oxygen. Expanding the main coronary arteries and arterioles in unchanged and ischemic areas 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, a single daily dose increases exercise time, slows the development of angina and ischemic depression of the ST segment, reduces the frequency of strokes and nitroglycerin consumption. It has a long dose-dependent hypotensive effect. The hypotensive effect is due to the direct vasodilating effect on vascular smooth muscle. In case of arterial hypertension, a single dose provides a clinically significant decrease in blood pressure for 24 hours (in the patient's position "lying" and "standing"). It does not cause a sharp decrease in blood pressure, a decrease in exercise tolerance, or a left ventricular ejection fraction. Reduces the degree of hypertrophy of the left ventricular myocardium, has anti-atherosclerotic and cardioprotective effect in IHD. Does not affect the contractility and conductivity of the myocardium, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases the glomerular filtration rate, has a weak natriuretic effect. In diabetic nephropathy does not increase the severity of microalbuminuria. It has no adverse effects on metabolism and blood plasma lipids.The onset of the effect is 2-4 hours, the duration of the effect is 24 hours.
Indications
Arterial hypertension (as monotherapy or in combination with other antihypertensive agents). Angina, vasospastic angina (Prinzmetal's angina).
Contraindications
Hypersensitivity to amlodipine and other dihydropyridine derivatives. Severe arterial hypotension. Collapse, cardiogenic shock. Pregnancy. Lactation period. Age up to 18 years (efficacy and safety have not been established). With caution: impaired liver function; sick sinus syndrome (severe bradycardia, tachycardia); decompensated chronic heart failure; mild or moderate hypotension; aortic stenosis; mitral stenosis; hypertrophic obstructive cardiomyopathy; acute myocardial infarction (and within 1 month after the disease); diabetes; lipid profile disorder; elderly age.
Precautionary measures
Application for violations of liver functionWith caution, you should prescribe the drug for violations of the liver.It is not necessary to change the dose in case of renal dysfunction. The concentration of amplodipine in the blood plasma does not depend on the degree of reduction of renal function. Use in children It is contraindicated in children and adolescents under the age of 18. Application in elderly patients With caution in elderly patients.
Use during pregnancy and lactation
Contraindicated in pregnancy and lactation.
Dosage and administration
Inside, 1 time per day, regardless of the meal, drinking plenty of water (100 ml). Arterial hypertension and angina: the initial dose is 5 mg. Depending on the individual response of the patient, the maximum dose can be increased to 10 mg. It is recommended to increase the dose 7–14 days after the start of therapy (a more rapid dose increase requires careful observation of the patient). The initial dose of 2.5 mg can also be used when amlodipine is added to other antihypertensive drugs. Particular patient groups, patients with low body mass, short stature, elderly patients, patients with impaired liver function: amlodipine is prescribed as an antihypertensive agent in an initial dose of 2.5 mg (1/2 table. 5 mg), 5 mg is used as an antianginal agent. x with renal insufficiency dose adjustment is required.
Side effects
Since the cardiovascular system: palpitations, shortness of breath, marked reduction in blood pressure, fainting, vasculitis, swelling (swelling of the ankles and feet), flushing of the face, rarely - rhythm disturbances (bradycardia, ventricular tachycardia, atrial flutter), chest pain , orthostatic hypotension, very rarely - development or aggravation of heart failure, extrasystole, migraine. For the central nervous system: headache, dizziness, fatigue, drowsiness, mood changes, convulsions, rarely - loss of consciousness, hypesthesia, nervousness, steam strasia, 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 hepatic transaminases and jaundice ( caused by cholestasis), pancreatitis, dry mouth, flatulence, gingival hyperplasia, constipation or diarrhea, very rarely - gastritis, increased appetite. From the genitourinary system: rarely pollakiuria, painful urination to urinate, nocturia, impaired sexual function (in including decrease in potency); very rarely - dysuria, polyuria. From the skin: very rarely - xerodermia, alopecia, dermatitis, purpura, discoloration of the skin. Allergic reactions: itchy skin, rash (including erythematous, maculopapular rash, urticaria), angioneurotic, rash, . On the part of the musculoskeletal system: rarely - arthralgia, arthrosis, myalgia (with prolonged use); very rarely - myasthenia. Others: rarely - gynecomastia, urecemia, weight gain / loss, thrombocytopenia, leukopenia, hyperglycemia, blurred vision, diplopia, conjunctivitis, pain in the eyes, tinnitus, back pain, dyspnea, nasal bleeding, increased sweating, thirst; very seldom - cold sticky sweat, cough, rhinitis, parosmia, disturbance of taste, disturbance of accommodation, xerophthalmia.
Overdose
Symptoms: pronounced decrease in blood pressure, tachycardia, excessive peripheral vasodilation. Treatment: gastric lavage, the appointment of activated carbon, maintaining the function of the cardiovascular system, monitoring indicators of heart and lung function, elevated position of the extremities, control of the BCC and diuresis.To restore vascular tone - the use of vasoconstrictor drugs (in the absence of contraindications to their use); to eliminate the effects of calcium channel blockade, intravenous administration of calcium gluconate. Hemodialysis is not effective.
Interaction with other drugs
Inhibitors of microsomal oxidation increase the concentration of amlodipine in the blood plasma, increasing the risk of side effects, and inducers of microsomal liver enzymes decrease. The antihypertensive effect weakens NSAIDs, especially indomethacin (sodium retention and blockade of GHG synthesis by the kidneys), alpha-adrenostimulyatory, estrogens (sodium retention), sympathomimetics. Thiazide and “loop” diuretics, beta-blockers, verapamil, ACE inhibitors and nitrates increase antianginal and hypotensive effects. Amiodarone, quinidine, alpha-blocker tori, antipsychotic drugs (neuroleptics) and BPC can enhance the hypotensive effect. It does not affect the pharmacokinetic parameters of digoxin and warfarin. Cimetidine does not affect the pharmacokinetics of amlodipine. When used together with lithium preparations, it is possible that their neurotoxicity may increase (nausea, vomiting, diarrhea, diarrhea, and vomiting can be increased (nausea, vomiting, diarrhea). , tremor, tinnitus). Calcium preparations can reduce the effect of CCA. Procainamide, quinidine and other drugs that cause prolongation of the QT interval, increase the negative inotropic effect and may increase the risk nachitelnogo extension QT.Greypfrutovy interval juice can reduce the concentration of amlodipine in plasma, but this decrease is so small that it does not significantly alter the effect of amlodipine.
special instructions
During the period of treatment, control over body weight and sodium consumption, the appointment of an appropriate diet is necessary. Maintain dental hygiene and frequent visits to the dentist (to prevent pain, bleeding and gum hyperplasia). The dosing regimen for the elderly is the same as for patients of other age groups. With increasing doses, careful monitoring of elderly patients is necessary. Despite the lack of withdrawal syndrome, a gradual decrease in dose is recommended before stopping treatment. Amlodipine does not affect a Plasma concentration of K +, triglycerides, total cholesterol, LDL,Creatinine and uric nitrogen However, in some patients, drowsiness and dizziness may occur predominantly at the beginning of treatment. When they occur, special precautions must be taken when driving and working with machinery.