Description
Pharmacological action
Derivative of dihydropyridine. It has antihypertensive, antianginal action. It blocks the flow of calcium ions through cell membranes into smooth muscle cells of the myocardium and blood vessels.
The antianginal effect is due to the expansion of the coronary and peripheral arteries and arterioles: with angina pectoris it reduces the severity of myocardial ischemia by expanding peripheral arterioles, reduces OPSS, reduces afterload on the heart, and reduces myocardial oxygen demand. Expanding the main coronary arteries and arterioles in unchanged and in ischemic zones of the myocardium increases the flow of oxygen into the myocardium (especially with vasospastic angina pectoris) and prevents the development of coronary artery constriction (including that caused by smoking). In patients with angina pectoris, a single daily dose increases exercise tolerance, slows the development of angina pectoris and ischemic depression of the ST segment, reduces the frequency of angina attacks and consumption of nitroglycerin.
Has a prolonged dose-dependent hypotensive effect. The antihypertensive effect is due to a direct vasodilating effect on the smooth muscles of blood vessels. With arterial hypertension, a single dose provides a clinically significant reduction in blood pressure over 24 hours (in the patient ² ¢s position, lying and standing). Does not cause a sharp decrease in blood pressure, reduce exercise tolerance, LV ejection fraction. Reduces the degree of LV myocardial hypertrophy, has antiatherosclerotic and cardioprotective effects in coronary heart disease. It does not increase the risk of death in patients with heart failure (III-IV class according to NYHA) during therapy with digoxin, diuretics and ACE inhibitors.
Does not affect myocardial contractility and conductivity, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases glomerular filtration rate, has a weak natriuretic effect. With diabetic nephropathy does not increase the severity of microalbuminuria. It has no adverse effects on metabolism and plasma lipids, suitable for the treatment of patients with concomitant bronchial asthma, diabetes mellitus.
Pharmacokinetics:
Absorption is slow, does not depend on food intake, is about 90%, bioavailability is 60-65%. TCmax for oral administration is 6-12 hours. With continuous administration, Css is created after 7-8 days. Distribution volume – 21 l / kg. Communication with plasma proteins -90-97%. Penetrates through the BBB.
Intensively (90%) is metabolized in the liver with the formation of inactive metabolites, has the effect of the first passage through the liver. T1 / 2 on average -35 hours. The total clearance is 500 ml / min.
T1 / 2 in patients with arterial hyperesis – 48 hours in elderly patients increases to 65 hours, with liver failure – up to 60 hours, similar parameters of T1 / 2 increase are also observed in severe heart failure, with impaired renal function – does not change. With hemodialysis, it is not removed.
It is excreted by the kidneys-60% in the form of metabolites, 10% unchanged with bile and through the intestines-20-25% in the form of metabolites, as well as with breast milk.
Indications
Arterial hypertension, exertional angina, vasospastic angina pectoris.
Contraindications
Hypersensitivity to the drug and other derivatives of dihydropyridine, severe arterial hypotension, collapse, unstable angina (except for Prinzmetal angina), pregnancy, lactation.
Precautions:
Arterial hypotension, aortic stenosis, chronic heart failure, liver failure, acute myocardial infarction (and within 1 month after), hypertrophic obstructive cardiomyopathy (GOKMP), sinus node weakness syndrome (SSS) and mitral stenosis, age before 18 years old (efficacy and safety of use not established), old age.
Special instructions
During treatment, it is necessary to control the body weight observed by the dentist (to prevent soreness, bleeding and gingival hyperplasia).
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 dose reduction is recommended before discontinuation of treatment.
Composition
One tablet contains amlodipine (as amlodipine besilate) 10,000 -13,869 mg.
Excipients:
lactose monohydrate,
magnesium stearate,
microcrystalline cellulose.
Dosage and administration
Inside, the initial daily dose is 5 mg per dose with a gradual increase over the course of 7-14 days to 10 mg / day once with arterial hypertension, the maintenance dose is 2.5-5 mg / day.
With angina pectoris and vasospastic angina, the dose is 5-10 mg / day once for the prevention of angina attacks -10 mg / day.
The elderly and debilitated patients with impaired liver function as an antihypertensive drug are prescribed an initial dose of 2.5 mg as an antianginal drug – 5 mg.
Any dose adjustment of amlodipine while using thiazide diuretics, beta-blockers, or angiotensin-converting enzyme inhibitors is not required.
Side effects of the
From the nervous system: headache, dizziness, excessive fatigue, drowsiness, mood changes, cramps rarely – loss of consciousness, hypesthesia, paresthesia, tremor, asthenia, malaise, insomnia, nervousness, depression, unusual dreams, very unusual dreams rarely – ataxia, apathy, agitation, amnesia.
From the digestive system: nausea, abdominal pain hyperbilirubinemia, jaundice, increased activity of hepatic transaminases rarely – dry mouth, vomiting, anorexia, constipation or diarrhea, dyspepsia, flatulence, gum hyperplasia is very rare – gastritis, pancreatitis.
From the CCC side: palpitations, swelling of the ankles and feet, shortness of breath, flushing, rarely – rhythm disturbances (bradycardia, ventricular tachycardia, atrial flutter), chest pain, marked decrease in blood pressure, orthostatic hypotension is very rare – development or aggravation heart failure, extrasystole, vasculitis, migraine.
From the genitourinary system: rarely – pollakiuria, painful urination, nocturia, sexual dysfunction (including decreased potency) very rarely – dysuria, polyuria.
From the musculoskeletal system: rarely – arthralgia, arthrosis, myalgia (with prolonged use) is very rare – myasthenia gravis.
From the skin: very rarely – xeroderma, alopecia, dermatitis, purpura. Allergic reactions: skin itch, rash (including erythematous, maculopapular rash, urticaria).
Other: rarely – visual impairment, conjunctivitis, diplopia, eye pain, disturbance of accommodation, xerophthalmia, tinnitus, gynecomastia, back pain, sensation of fever and flushing, chills, weight gain, dyspnea, nosebleeds, increased sweating, thirst, very rarely, cold, sticky sweat, cough, rhinitis, parosmia, taste perversion.
Overdose
Symptoms: excessive peripheral vasodilation, marked decrease in blood pressure, tachycardia.
Treatment: gastric lavage, administration of activated charcoal, maintenance of CCC functions, monitoring of heart and lung function, elevated limbs, circulating blood volume (BCC) and urine output, symptomatic and supportive therapy, intravenous administration of calcium gluconate and dopamine. Hemodialysis is ineffective.
Storage conditions
In a dark place at a temperature of 15 to 25 ° C, inaccessible to children.
Expiration
3 years.
Deystvuyuschee substances
amlodipine
drugstore terms
drugstore
dosage form
tablets
Appointment
Adult prescription
