medicalmeds.eu Medicines Anti-hypertensive means. Blockers of calcium channels. Dihydropyridine derivatives. Amlodipin

Amlodipin

Producer: RUP of Belmedpreparata Republic of Belarus

Code of automatic telephone exchange: C08CA01

Release form: Firm dosage forms. Tablets.

Indications to use: Arterial hypertension. Stable stenocardia.

General characteristics. Structure:

Active ingredient: 5 mg of an amlodipin (in the form of an amlodipin of a besilat).

Anti-hypertensive drug.

Pharmacological properties:

Pharmacodynamics. Has anti-anginal and hypotensive effect. Anti-anginal action is caused by expansion of coronary and peripheral arteries and arterioles: at stenocardia reduces expressiveness of ischemia of a myocardium; expanding peripheral arterioles, reduces the general peripheric resistance of vessels, reduces load of heart, reduces the need of a myocardium for oxygen.

Expanding the main coronary arteries and arterioles in not changed and in ischemic zones of a myocardium, increases intake of oxygen in a myocardium (especially at vasospastic stenocardia); prevents development of a konstriktion of coronary arteries (including caused by smoking). At patients with stenocardia the single daily dose increases time of performance of an exercise stress, slows down development of stenocardia and "ischemic" depression of a segment of S-T, reduces the frequency of attacks of stenocardia and consumption of nitroglycerine. Renders long-term dozozavisimy hypotensive effect.

Hypotensive action is caused by direct vasodilating impact on unstriated muscles of vessels. At arterial hypertension the single dose provides clinically significant decrease in the ABP for 24 h (in position of the patient "lying" and "standing"). Does not cause sharp decrease in the ABP, decrease in tolerance to an exercise stress, fraction of emission of a left ventricle. Reduces degree of a hypertrophy of a myocardium of a left ventricle, has anti-atherosclerotic and cardiotyre-tread effect at an ischemic heart disease. Does not increase risk of death at the patients having chronic heart failure (the III-IV class) against the background of therapy by digoxin, diuretics and APF inhibitors.

Does not exert impact on contractility and conductivity of a myocardium, does not cause reflex increase in heart rate, slows down aggregation of thrombocytes, raises a glomerular filtration rate, possesses a weak natriuretic effect. At a diabetic nephropathy does not increase expressiveness of a microalbuminuria. Does not exert adverse impacts on a metabolism and lipids of plasma. Time of approach of effect - 2-4 h; duration - 24 h.

Indications to use:

Arterial hypertension (monotherapy or in a combination with other hypotensive HP), a stable angina of exertion and vasospastic stenocardia (monotherapy or in a combination with other anti-anginal HP).

Route of administration and doses:

Drug is accepted inside. The initial dose makes 5 mg/days at one time with gradual increase within 7-14 days up to 10 mg/days once; at arterial hypertension a maintenance dose - 2.5-5 mg/days. At an angina of exertion and vasospastic stenocardia - 5-10 mg/days once; for prevention of attacks of stenocardia - 10 mg/days.

To thin patients, patients of low growth, elderly patients, the patient with an abnormal liver function as hypotensive medicine амлодипин appoint 2.5 mg in an initial dose; as antiangialny means - 5 mg. At chronic heart failure an initial dose - 2.5 mg of 1 times a day, at good tolerance gradually increase a dose to 10 mg of 1 times a day.

Features of use:

During treatment it is necessary to control body weight and to be observed at the stomatologist (for prevention of morbidity, bleeding and a hyperplasia of gums).

Amlodipin does not influence plasma concentration of K+, glucose, triglycerides, the general cholesterol, LPNP, uric acid, creatinine and an urea nitrogen. Despite the absence of at blockers of slow calcium channels of a syndrome of "cancellation", before the termination of treatment gradual reduction of doses is recommended.

Side effects:

Amlodipin is rather well had, in therapeutic doses does not cause the expressed side effect. The most frequent side effects of an amlodipin are:

from a nervous system: headache, dizziness, excessive fatigue, drowsiness, change of mood, spasm; seldom - a loss of consciousness, a hypesthesia, paresthesias, a tremor, an adynamy, an indisposition, sleeplessness, nervousness, a depression, extraordinary dreams, alarm; very seldom - an ataxy, apathy, agitation, amnesia;

from the alimentary system: nausea, abdominal pain; hyperbilirubinemia, jaundice, increase in activity of "hepatic" transaminases; seldom - dryness in a mouth, anorexia, vomiting, a lock or diarrhea, dyspepsia, a meteorism, a hyperplasia of gums; very seldom - gastritis, increase in appetite, pancreatitis;

from cardiovascular system: heartbeat, hypostases of anklebones and feet, an asthma, "inflows" of blood to the person, is rare - disturbances of a rhythm (bradycardia, ventricular tachycardia, an atrial flutter), thorax pain, decrease in the ABP, orthostatic hypotension; very seldom - development or aggravation SN, premature ventricular contraction, migraine;

from urinogenital system: seldom - a pollakiuria, painful desires on an urination, a nocturia, disturbance of sexual function (including decrease in a potentiality); very seldom - a dysuria, a polyuria;

from a musculoskeletal system: seldom - an arthralgia, arthrosis, a mialgiya (at prolonged use); very seldom – a myasthenia;

from integuments: very seldom - a xerodermia, an alopecia, dermatitis, a purpura; allergic reactions: skin itch, rash (including erythematic, makulopapulezny rash, small tortoiseshell);

others: seldom - a vision disorder, conjunctivitis, a diplopia, eye pain, accommodation disturbance, a xerophthalmia, a ring in ears, a gynecomastia, a dorsodynia, feeling of heat and "inflows" of blood to the person, a fever, increase in body weight, диспноэ, nasal bleeding, the increased sweating, thirst; very seldom - a cold clammy sweat, cough, rhinitis, a parosmiya, a food faddism, a hyperglycemia.

Interaction with other medicines:

Inhibitors of a microsomal oxidation increase concentration of an amlodipin in plasma, strengthening risk of development of side effects, and inductors of microsomal enzymes of a liver reduce.

Hypotensive effect NPVS, especially indometacin, (Na delay + and blockade of synthesis of Pg kidneys), alpha адреностимуляторы weaken, estrogen (Na+ delay), sympathomimetics.

Thiazide and "loopback" diuretics, beta adrenoblockers, verapamil, APF inhibitors and nitrates strengthen anti-anginal and hypotensive effects.

Amiodaronum, quinidine, alfa1-adrenoblockers, antipsychotic medicines (neuroleptics) and blockers of slow calcium channels can strengthen hypotensive action.

Does not exert impact on pharmacokinetic parameters of digoxin and warfarin. Cimetidinum does not influence pharmacokinetics of an amlodipin.

At combined use with the drugs Li + strengthening of manifestations of their neurotoxicity (nausea, vomiting, diarrhea, an ataxy, a tremor, a sonitus) is possible.

The drugs Ca2 + can reduce effect of an amlodipin.

Procaineamide, quinidine, etc. the medicines causing lengthening of an interval of Q-T strengthen a negative inotropic effect and can increase risk of considerable lengthening of an interval of Q-T.

Contraindications:

Hypersensitivity (including to other dihydropyridines), heavy arterial hypotension, pregnancy, the lactation period.

With care: arterial hypotension, an aortal stenosis, chronic heart failure, a liver failure, an acute myocardial infarction (and within 1 month after), a stenosis of the mouth of an aorta, a subaortal stenosis and a mitral stenosis, age up to 18 years (efficiency and safety of use are not established), advanced age.