2010/09/20

Amlodipine

Composition, structure and packing

Tablets are white, ploskotsilindricheskie, with bevel.

1 tab.

amlodipine (in the form bezilata) 5 mg.

- - 10 mg.

Excipients: potato starch, lactose, microcrystalline cellulose, magnesium stearate, calcium stearate.

Clinico-pharmacological group: Calcium channel blockers.

Pharmacological action

Dihydropyridine derivative - BCCI II generation, has antianginal and hypotensive action. Communicating with the dihydropyridine receptors, blocking calcium channels, reduces the transmembrane passage Ca2 + into the cell (to a greater extent in vascular smooth muscle cells than in cardiomyocytes). Antianginal due to increased coronary and peripheral arteries and arterioles: angina reduces the severity of myocardial ischemia, increasing peripheral arterioles, reduces TPVR, reduces preload on the heart, reduces the need for myocardial oxygen. Expanding the major coronary arteries and arterioles in the unaltered and in the ischemic myocardial areas, increases oxygen to the myocardium (especially in vasospastic angina), prevents the development of constriction of the coronary arteries (including those caused by smoking).

In patients with angina and single daily dose increases the run-time physical activity slows the development of angina and coronary "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 a clinically significant reduction in blood pressure over 24 h (in the position of the patient "lying" and "standing"). There is no sharp decline in blood pressure, reduce exercise tolerance, left ventricular ejection fraction. Reduces the degree of left ventricular hypertrophy, has antiateroskleroticheskoe and cardioprotective effect in ischemic heart disease. Do not increase the risk of death in patients with chronic heart failure (III-IV class NYHA), during therapy with digoxin, diuretics and ACE inhibitors. It has no effect on myocardial contractility and conductivity, does not cause a reflex increase in heart rate, inhibits platelet aggregation, improves 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 plasma lipids. Time of onset of effect - 2-4 h duration - 24 hours

Statement
hypertension,
angina,
vasospastic angina
silent myocardial ischemia,
decompensated CHF (as adjuvant).

Dosage regimen

Inside, the initial dose - 5 mg / day at a time with a gradual increase during the 7-14 days to 10 mg / day once, with arterial hypertension maintenance dose - 2.5-5 mg / day.

If angina and vasospastic angina - 5-10 mg / day once, for the prevention of angina attacks - 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 LS - 5 mg. In CHF, the initial dose - 2.5 mg 1 time per day, with good endurance gradually increase the dose to 10 mg 1 time per day.

Side effect

Of the nervous system: headache, dizziness, excessive fatigue, drowsiness, mood changes, seizures, rare - loss of consciousness, hyperesthesia, paresthesia, tremor, asthenia, malaise, insomnia, nervousness, depression, unusual dreams, anxiety, and very rarely - ataxia , apathy, agitation, amnesia.

On the part of the digestive system: nausea, abdominal pain, hyperbilirubinemia, jaundice, increase in activity of "liver" transaminase; rarely - dry mouth, anorexia, vomiting, constipation or diarrhea, dyspepsia, flatulence, gingival hyperplasia, 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 - arrhythmias (bradycardia, ventricular tachycardia, atrial flutter), chest pain, decrease blood pressure, orthostatic hypotension, and very rarely - the development or worsening HF, beats, increased blood pressure, migraines.

On the part of the urogenital system: rarely - thamuria, tenesmus, nocturia, violation of sexual function (including reduction of potency), very rarely - dysuria, polyuria.

From the musculoskeletal system: rarely - arthralgia, arthrosis, myalgia (with prolonged use), very rarely - myasthenia gravis.

On the part of the skin: very rarely - dermatoxerasia, alopecia, dermatitis, purple.

Allergic reactions: itching, rash (including erythematous, maculopapular rash, urticaria).

Other: rarely - blurred vision, conjunctivitis, diplopia, eye pain, disruption of accommodation, xerophthalmia, tinnitus, gynecomastia, back pain, sensation of heat 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, hyperglycemia.

Contraindications
Hypersensitivity (including to other dihydropyridine),
severe arterial hypotension,
pregnancy
lactation.

Be wary - hypotension, aortic stenosis, CHF, hepatic failure, acute myocardial infarction (and within 1 month after), the age of 18 years (efficacy and safety have not been established), advanced age.

In the appointment of amlodipine (like other dihydropyridine) patients with GOKMP, SSS and mitral stenosis should be careful.

Pregnancy and lactation

Use of the drug is contraindicated.

Cautions

Safety of pregnancy and lactation not established.

Experience with 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, uric acid, creatinine and urea nitrogen. Despite the lack of BCCI syndrome "cancel" before the termination of treatment is recommended a gradual reduction in dose.

Overdose

Symptoms: excessive peripheral vasodilation, reduced blood pressure, tachycardia.

Treatment: gastric lavage, the appointment of activated carbon, the maintenance functions of the SSA, the control performance of the heart and lungs, an elevated position of the limbs, the control of BCC and diuresis, symptomatic and supportive therapy, in / to the introduction of calcium gluconate and dopamine. Hemodialysis is ineffective.

Drug Interactions

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 increase antianginal and hypotensive effects. Amiodarone, quinidine, alpha 1-blockers, antipsychotic drugs (neuroleptics) and the BCCI might enhance the hypotensive effect. It has no effect on the pharmacokinetic parameters of digoxin and warfarin. Cimetidine has no effect on the pharmacokinetics of amlodipine.

When combined with the use of drugs Li + may gain manifestations of neurotoxicity (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 lengthening of the interval QT.

Terms and Conditions of storage

Store in a dry place protected from light.