Amlodipin-Prana

General characteristics. Structure:

Active ingredient: 5 mg or 10 mg of an amlodipin (in the form of a bezilat) in 1 tablet.

Excipients: starch corn, lactose, cellulose microcrystallic, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Action is anti-anginal, hypotensive. Contacting dihydropyridinic receptors, blocks calcium channels, reduces transmembrane transition of calcium ions to a cell (more in smooth muscle cells of vessels, than cardiomyocytes).

Pharmacokinetics. After intake it is slowly absorbed from a GIT. Average absolute bioavailability makes 64%, Tmax is 6-9 h. Equilibrium concentration is reached after 7 days of therapy. Food does not influence absorption of an amlodipin. The average volume of distribution makes 21 l/kg of body weight that indicates that the most part of drug is in fabrics, and rather smaller - in blood.

Communication with proteins of a blood plasma – 95%. Is exposed to slow, but extensive metabolism (90%) in a liver, has effect of "primary passing" through a liver. Metabolites have no significant pharmacological activity. After a single dose in T1/2 varies from 31 to 48 h, and at repeated appointment makes about 45 h. About 60% of the dose accepted inside are excreted with urine preferential in the form of metabolites and 10% in an invariable look, 20 – 25% are removed with a stake, and also with breast milk. The general Cl of an amlodipin makes 0,116 ml / with/kg (7 ml/min., 0,42 l/h/kg).

At elderly patients (65 years) removal of an amlodipin in a slowed-up way (are more senior than T1/2 – 65 h) in comparison with young patients, however the difference has no clinical value. Udleneniye T1/2 at patients with a liver failure to 60 h assumes that at long appointment accumulation of drug in an organism will be higher. The renal failure has no significant effect on kinetics of an amlodipin. Drug gets through GEB. At a hemodialysis is not removed.

Indications to use:

Arterial hypertension (monotherapy or in a combination with other anti-hypertensive HP); stenocardia (including angina of exertion), vasospastic stenocardia (Printsmetall stenocardia); bezbolevy ischemia of a myocardium; dekompensirovanny chronic heart failure (auxiliary therapy).

Route of administration and doses:

Inside. At arterial hypertension and stenocardia: an initial dose - 5 mg of 1 times a day; the maximum dose – 10 mg of 1 times a day; at arterial hypertension a maintenance dose – 2,5÷5 of mg/days.

At an angina of exertion and vasospastic stenocardia - 5÷10 of mg/days, once; for prevention of attacks of stenocardia – 10 mg/days.

At chronic heart failure – 2,5 mg/days. Once, at good tolerance the dose is gradually increased to 10 mg/days.

To thin patients, patients of low growth, elderly patients, at an abnormal liver function as an antihypertensive, амлодипин appoint in an initial dose 2,5 mg, as anti-anginal means – 5 mg.

Does not demand change of a dose at co-administration with thiazide diuretics and APF inhibitors. Does not demand change of a dose from patients with a renal failure.

Features of use:

During treatment control of body weight and consumption of sodium is necessary. It is necessary to maintain hygiene of teeth and to often visit the stomatologist. At increase in a dose careful observation of elderly patients is necessary.

Drug does not influence concentration in K+ plasma, glucose, triglycerides, the general cholesterol, LPNP, uric acid, creatinine and an urea nitrogen.

Precautionary measures. It is necessary to be careful at appointment as the patient with a liver and/or renal failure, chronic heart failure.

In an initiation of treatment dizzinesses and drowsiness are possible, in this case it is necessary to observe special precautionary measures when driving and during the work with mechanisms.

Side effects:

From cardiovascular system: heartbeat, an otdyshka, the expressed lowering of arterial pressure, a faint, a vasculitis, hypostases (anklebones and feet), "inflows" of blood to the person, is rare – disturbances of a rhythm (bradycardia, ventricular tachycardia, an atrial flutter), thorax pain, orthostatic hypotension, is very rare – development or a usuglubleniye of heart failure, premature ventricular contraction, migraine.

From a nervous system: dizziness, a headache, fatigue, drowsiness, change of mood, a spasm, is rare – a loss of consciousness, a hypesthesia, nervousness, paresthesias, a tremor, вертиго, an adynamy, an indisposition, sleeplessness, a depression, unusual dreams, is very rare – an ataxy, apathy, agitation, amnesia.

From an urinary system: seldom – a pollakiuria, painful desires on an urination, a nocturia, disturbance of sexual function (including decrease in a potentiality), it is very rare – a dysuria, a polyuria.

From integuments: very seldom – a xerodermia, an alopecia, dermatitis, a purpura, skin discoloration.

From digestive tract: nausea, vomiting, pains in epigastriums, it is rare – pancreatitis, dryness in a mouth, a meteorism, a hyperplasia of gums, a lock or diarrhea, jaundice, is very rare – gastritis, increase in appetite.

Allergic reactions: skin itch, rash (including erythematic, makulopapulezny small tortoiseshell), Quincke's disease.

Others: a gynecomastia, a hyperuricemia, increase/decrease in body weight, thrombocytopenia, a leukopenia, a hyperglycemia, a vision disorder, a diplopia, conjunctivitis, eye pain, a dorsodynia, диспноэ, nasal bleeding, the increased sweating, thirst, is very rare – a cold clammy sweat, cough, rhinitis, a parosmiya, disturbance of flavoring feelings, accommodation disturbance, a xerophthalmia.

Interaction with other medicines:

Let's combine with the main groups of antihypertensives (diuretics, IAPF, beta адреноблакаторы), nitrates and hypoglycemic drugs.

Means for an inhalation anesthesia (derivatives of hydrocarbons), Amiodaronum, quinidine, etc. antagonists of calcium - can strengthen action.

NPVS (especially indometacin) reduce hypotensive effect, slow down synthesis of prostaglandins in kidneys and a natriuresis.

Contraindications:

Hypersensitivity, including to other derivatives of a digidropiridpn, heavy arterial hypotension, a collapse, cardiogenic shock, an acute myocardial infarction (including in 1 month after it), pregnancy and the period of a lactation, age up to 18 years (efficiency and safety are not established).

With care: an abnormal liver function, a sick sinus syndrome (the expressed bradycardia, tachycardia), dekompensirovanny chronic heart failure, slight or moderate arterial hypotension, an aortal stenosis, a mitral stenosis, a hypertrophic subaortic stenosis, a diabetes mellitus, disturbance of a lipidic profile, advanced age.

Overdose:

Symptoms: the expressed lowering of arterial pressure, tachycardia, an excessive peripheral vazodilatation.

Treatment: a gastric lavage, purpose of absorbent carbon, support of function of cardiovascular system, control of indicators of function of heart and lungs, sublime position of extremities, control of volume of the circulating blood and a diuresis. For recovery of a tone of vessels – use of vasoconstrictive HP (in the absence of contraindications to their use), for elimination of effects of blockade of calcium channels – in/in administration of calcium of a gluconate. The hemodialysis is not effective.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C. To store in the places unavailable to children. A period of validity - 2 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets on 5 and 10 mg. On 10 tablets in a blister strip packaging. 40, 50, etc. to 100 tablets in a polymeric can. Each can, or 1, 2 or 3 blister strip packagings together with the application instruction are placed in a pack from a cardboard.