Amlodipine Alkaloid, pills 10mg, 30pcs

Composition

One tablet contains 10,000 -13,869 mg of amlodipine (as amlodipine bezylate).

Auxiliary substances:

lactose monohydrate,

magnesium stearate,

microcrystalline cellulose.

Pharmacological action

A dihydropyridine derivative. It has an antihypertensive, antianginal effect. Blocks the flow of calcium ions through cell membranes to smooth muscle cells of the myocardium and blood vessels. Antianginal action is caused by the expansion of coronary and peripheral arteries and arterioles: with angina, it reduces the severity of myocardial ischemia; expanding peripheral arterioles, reduces OPSS, reduces afterload on the heart, reduces the need for myocardial oxygen. Dilating the main coronary arteries and arterioles in unchanged and ischemic areas of the myocardium increases oxygen supply to the myocardium (especially in vasospastic angina); prevents the development of coronary artery constriction (including caused by smoking). In patients with angina pectoris, a single daily dose increases exercise tolerance, slows down the development of angina and “ischemic depression” in the S-T segment, reduces the frequency of angina attacks and nitroglycerin consumption. It has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to the direct vasodilating effect on vascular smooth muscles. In arterial hypertension, a single dose provides a clinically significant reduction in blood pressure for 24 hours ( in the patient’s “lying” and “standing” positions). It does not cause a sharp decrease in blood pressure, reduced exercise tolerance, or LV ejection fraction. Reduces the degree of LV myocardial hypertrophy, has anti-atherosclerotic and cardioprotective effects in CHD. It does not increase the risk of death in patients with CHF (NYHA class III-IV) treated with digoxin, diuretics, and ACE inhibitors. It does not affect the contractility and conduction of the myocardium, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases the glomerular filtration rate, and has a weak natriuretic effect. In diabetic nephropathy, it does not increase the severity of microalbuminuria. It has no adverse effects on the metabolism and plasma lipids, and is suitable for the treatment of patients with concomitant bronchial asthma and diabetes mellitus. Pharmacokinetics: Absorption – slow, does not depend on food intake, is about 90%, bioavailability-60-65%. TSMAKH with oral use-6-12 hours. If it is constantly accepted, Css is created in 7-8 days. The volume of distribution is 21 l / kg. Binding to plasma proteins is 90-97%. Penetrates through the BBB. Intensively (90%) metabolized in the liver with the formation of inactive metabolites, has the effect of “first pass” through the liver. T1 / 2 on average -35 h. Total clearance-500 ml / min. T1 / 2 in patients with arterial hypertension-48 h in elderly patients increases to 65 h, with hepatic insufficiency-up to 60 h, similar parameters of increase in T1 / 2 are observed in severe CHF, with impaired renal function-does not change. It is not removed during hemodialysis. Excreted by the kidneys-60% in the form of metabolites,10% in unchanged form; 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.

Contraindications

Hypersensitivity to the drug and other dihydropyridine derivatives, severe hypotension, collapse, unstable angina (with the exception of Prinzmetal angina), pregnancy, lactation.

With caution:

Arterial hypotension, aortic stenosis, chronic heart failure, hepatic insufficiency, acute myocardial infarction (and within 1 month after), hypertrophic obstructive cardiomyopathy (HOCMP), sinus node weakness syndrome (SSS) and mitral stenosis, age up to 18 years (efficacy and safety of use have not been established), elderly age.

Side effects

From the nervous system: headache, dizziness, excessive fatigue, drowsiness, mood swings, convulsions; rarely-loss of consciousness, hypesthesia, paresthesia, tremor, asthenia, malaise, insomnia, nervousness, depression, unusual dreams, anxiety; very rarely – ataxia, apathy, agitation, amnesia. From the digestive system: nausea, abdominal pain; hyperbilirubinemia, jaundice, increased activity of “liver” transaminases; rarely-dry mouth, vomiting, anorexia, constipation or diarrhea, dyspepsia, flatulence, gum hyperplasia; very rarely – gastritis, pancreatitis. From the cardiovascular system: palpitations, swelling of the ankles and feet, shortness of breath, “flushes” of blood to the face, rarely – rhythm disorders (bradycardia, ventricular tachycardia, atrial flutter), chest pain, marked decrease in blood pressure, orthostatic hypotension; very rarely – development or aggravation of 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); very rarely-myasthenia gravis. From the skin: very rarely – xeroderma, alopecia, dermatitis, purpura. Allergic reactions: pruritus of the skin, rash (including erythematous, maculopapular rash, urticaria). Others: rarely-visual impairment, conjunctivitis, diplopia, eye pain, accommodation disorders, xerophthalmia, tinnitus, gynecomastia, back pain, feeling hot and “hot” in the face, chills, weight gain, dyspnoea, nosebleeds, increased sweating, thirst; very rarely-cold sticky sweat, cough, rhinitis, parosmia, taste distortion.

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. The antihypertensive effect is weakened by NSAIDs, especially Indometacin (Na + delay and blockade of Pg synthesis by the kidneys), alpha-adrenostimulants, estrogens (Na+ delay), sympathomimetics. Thiazide and loop diuretics, beta-blockers, verapamil, ACE inhibitors, and nitrates enhance the antianginal and hypotensive effects. Amiodarone, quinidine, alpha-1-adrenoblockers, antipsychotic drugs (neuroleptics) and BMCC may enhance the hypotensive effect. It has no effect on the pharmacokinetic parameters of digoxin and warfarin. Cimetidine does not affect the pharmacokinetics of amlodipine. When combined with Li+ preparations, it is possible to increase the manifestations of their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus). Ca2+ preparations can reduce the effect of BMCC. Procainamide, quinidine, etc. drugs that cause prolongation of the Q-T interval increase the negative inotropic effect and may increase the risk of significant prolongation of the Q-T interval.

How to take, course of use and dosage

Inside, the initial daily dose is 5 mg at a time with a gradual increase over 7-14 days to 10 mg / day once; in arterial hypertension, the maintenance dose is 2.5-5 mg/day. For exertional angina and vasospastic angina, the dose is 5-10 mg / day once; for the prevention of angina attacks-10 mg/day. Elderly and debilitated patients, patients with impaired liver function as a hypotensive drug are prescribed at an initial dose of 2.5 mg; as an antiangial drug-5 mg. No dose adjustment of amlodipine is required with concomitant use of thiazide diuretics, beta-blockers, or angiotensin converting enzyme inhibitors.

Overdose

Symptoms: excessive peripheral vasodilation, marked decrease in blood pressure, tachycardia. Treatment: gastric lavage, use of activated charcoal, maintenance of CVS functions, monitoring of heart and lung function, elevated position of the limbs, monitoring of circulating blood volume (BCC) and diuresis, symptomatic and supportive therapy, intravenous use of calcium gluconate and dopamine. Hemodialysis is ineffective.

Special instructions

During treatment, it is necessary to monitor body weight and see a dentist ( to prevent soreness, bleeding and gum 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 discontinuing treatment.

Storage conditions

In a place protected from light, at a temperature of 15 to 25 °C, out of the reach of children.

Shelf

life is 3 years.

Active ingredient

Amlodipine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets