medicalmeds.eu Medicines The selection antagonists of calcium with preferential action on vessels. Amlodipin, tab. of 5 mg, 10 mg No. 10*3

Amlodipin, tab. of 5 mg, 10 mg No. 10*3

Препарат Амлодипин, табл. 5мг, 10мг №10*3 . ОАО "Красная звезда" Украина

Producer: JSC Krasnaya zvezda Ukraine

Code of automatic telephone exchange: C08C A01

Release form: Firm dosage forms. Tablets.

Indications to use:

General characteristics. Structure:

Active agent: 1 tablet contains - an amlodipina of a bezilat in terms of амлодипин 5 mg or 10 mg;

excipients: microcrystallic cellulose, calcium phosphate disubstituted, sodium krakhmalglikolit, silicon dioxide colloid (anhydrous), magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Amlodipin contacts dihydropyridinic receptors, blocks calcium channels, inhibiting transmembrane transition of calcium ions in a cell (more - in smooth muscle cells of vessels, than in kardiomitsita). Shows the prolonged dozozavisimy antigipertenzivny effect. Hypotensive action is caused by the weakening influence on unstriated muscles of vessels that reduces the general peripheral vascular resistances. As a result of decrease in load of heart the need of a myocardium for oxygen decreases; expansion of large coronary arteries and coronary arterioles, both in not changed, and in ischemic zones of a cardiac muscle increases intake of oxygen in a myocardium. Slows down aggregation of thrombocytes; increases a glomerular filtration rate, a conclusion of sodium and a diuresis. The effect develops in 1-2 h after reception and proceeds about 24 h. Thanks to the gradual prolonged effect causes a smooth lowering of arterial pressure and the minimum reflex stimulation of a sympathetic nervous system. At an idiopathic hypertensia reduces degree of a hypertrophy of a myocardium of a left ventricle; shows anti-sclerous and cardiotyre-tread action at coronary heart disease.

Pharmacokinetics. It is soaked up (irrespective of meal) slowly, but almost completely. Bioavailability – 60-65% (due to effect of "the first passing" through a liver). _Cmax in plasma is reached in 7–8 days. Linkng with proteins of plasma – 97-98%. At constant reception equilibrium concentration is formed in 7–8 days. Distribution volume – 20 l/kg. Gets through a blood-brain barrier. _T1/2 – 35-38 h, level in plasma in 24 h makes 2–12 ng/ml. It Biotransformirutsya in a liver with formation of inactive metabolites; elimination is two-phase: the first phase – short, another lasts 35–50 h. The general clearance – 0,5 l/min. It is excreted with urine (60% in the form of metabolites, 10% - in steady-state condition), with bile (20–25% in the form of metabolites) and with breast milk. _T1/2 at the broken function of a liver and at elderly patients is extended, at a renal failure – does not change.

Indications to use:

Arterial hypertension, coronary heart disease (stenocardia stable and vasospastic).

Route of administration and doses:

Inside. Stenocardia - in an initial dose of 5 mg of 1 times a day, with gradual increase to the maximum 10 mg of 1 times a day; arterial hypertension - 5 mg (at elderly 2,5 mg) 1 time a day, in case of need in 7-14 days increase a dose to 10 mg. The maximum daily dose makes 10 mg.

Features of use:

Restrictions for use are the expressed aortal stenosis, heart failure, an abnormal liver function, children's age (safety and efficiency of use for children are not established). Use at pregnancy is possible if the expected effect of therapy exceeds potential risk for a fruit. For the period of treatment it is necessary to stop feeding by a breast. Drug can cause dizziness which the patients working with potentially dangerous mechanisms, either the managing director of vehicles, or connected with the activity needing attentiveness and coherence of actions need to consider. Patients of old age well transfer drug. The patient with a renal failure drug is appointed in usual doses, changes of concentration of drug in plasma do not correlate with severity of a renal failure. Amlodipin is not brought at dialysis. Does not increase risk of mortality at the patients having heart failure (III-IV a class for NYHA), against the background of therapy by digoxin, diuretics and inhibitors of an angiotensin-converting enzyme.

Side effects:

From cardiovascular system: dermahemia of the person, heartbeat; seldom – disturbance of a rhythm (bradycardia, ventricular tachycardia, an atrial flutter), thorax pain, hypotension (including orthostatic).

From a nervous system and sense bodys: exhaustion, headache, insanity, drowsiness; seldom – fatigue, an adynamy, emotional lability, a vision disorder, paresthesia and extremity pain (at long use).

From storonymochepolovy system: peripheral hypostases (puffiness of anklebones and a foot), increase in frequency of an urination, impotence is rare.

From bodies of digestive tract: nausea, an abdominal pain, it is rare – dyspepsia, increase in level of liver enzymes, change of the mode of defecation, jaundice.

From respiratory system: seldom – an asthma.

From a musculoskeletal system: seldom – an arthralgia, a mialgiya.

From integuments: rash, an itch, it is rare – a poliformny erythema.

Others: seldom – a hyperplasia of gums, a gynecomastia.

Contraindications:

Hypersensitivity (including to others of dihydropyridines), arterial hypotension (it is less than 90 mm hg), shock, an acute myocardial infarction.

Overdose:

Symptoms. An excessive peripheral vazodilatation, the expressed and long lowering of arterial pressure, tachycardia.

Treatment. The gastric lavage, purpose of the absorbent carbon sick put in horizontal position with the raised legs, monitoring of indicators of cardiac performance and lungs, control of volume of the circulating blood and a diuresis, a symptomatic and maintenance therapy, intravenous administration of plasma substitutes, a gluconate of calcium, a dopamine, a phenylephine hydrochloride. The hemodialysis is not effective.