Amlodipine

Chemical name

2-[(2-Аминоэтокси)метил] -4-(2-хлорфенил)-1,4-дигид ро-6-метил-3,5-пиридин dicarbonova acid 3-etil 5-metilovy ether (in the form of bezilata and maleate)

Gross

C20-H25-Cl-N2-O5

Characteristics

Derived digidropiridina-calcium antagonist II generation. The white crystalline powder, malorastvorim water sparingly soluble in ethanol.

Of drugs

The drugs-antianginalnoe, gipotenzivne, sossoudorasshiratee, skin. Associated with digidropiridinovmi receptors, blocking calzieve channels ingibiruet transmembranny transition of calcium ions inside the cells (to a greater extent in cells gladkomyshechne receptacles than cardiomiotita). Provides extended dozozawisimy antigipertenzivny effect. Gipotenzivne effect due to the direct impact of relaxing the smooth muscle receptacles low round. Decreases severity Cerebral infarction by increasing peripheral arteriol and downgrading round in the face of changing little variation. As a result of easing the burden on the heart of a lower demand in the cardiac oxygen; The major coronary arteries and coronary arteriol both unchanged, and ishemizirovannah zones cardiac muscles increases the flow of oxygen in the miocard. Weak affects sinusny and sinusno-predserdny node slightly down AV conduction. Agregatia stops platelets; Increases speed clubockova filtering down sodium and diurez. The effect develops in 1-2 h after administration and lasts for about 24 hours With the gradual emergence of actions and prolongirovannomu effect is a matter of gradual decline and AD minimum fence stimulation sympathetic nervous system. In hypertensive disease reduces the isolationist left heart chamber; Provides антиатеросклеротичес кое and cardioproteguoe up at heart. It increases the risk of death in patients suffering from heart failure (class III-IV in NYHA), in the face of therapy digoxinom, dioretikami and agricultural Apf.vsasavetsa (regardless of mealtimes) slowly, but almost completely. Bioavailability-65% (through economies of the first passage "through the liver). C_max is six hours Linking blood plasma is 97-98%. In permanent employment equilibrium concentration in a 7-8 days. The volume of 20 l / kg Penetrates the GEB. T_1/2 - 35-48 hrs, the plasma within 24 hours of 2-12 ng / J Biotransformiroetsa in the liver with the formation of active metabolites; Dwuhfaznaya off : the first phase is short, the second going 35-50 and The Cl - 0.5 l / min. Excreted in the urine (60% in the form of metabolites, 10% in an unmodified form), from jelchew (20-25% in the form of metabolites), and breast milk. T_1/2 breached in the liver and in older patients longer, if there is a violation of the kidney is not Izmenaetsa.v experiments on rats and rabbits were found teratogenic and embriotoksicskih properties.

Indications

Arterial hypertension (monotherapy or in combination with other hypotensive drugs), a stable stenocardia and vazospastical (Prinzmetala) of which in patients resistant to therapy or nitrates бета-адреноблокатора��и.

Restrictions on the use of

Expressed aortalny stenoses, heart failure, the liver function, the children's age (safety and efficacy of the children are not identified).

Pregnancy and lactation

Perhaps if the effect of therapy outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding.

Contraindications

Гиперчувствительност ь (incl. to digidropiridinam etc.), arterial gipotenzia (less than 90 mm Hg), shock, acute myocardial infarction.

Side-Effects

From the circulatory system and blood (blood, gemostaz) : hyperemia skin, rapid heartbeat; Rarely in rhythm (aetiology, ventricular tachycardia, predserdy fibrillation), the pain in the chest, gipotenzia (incl. ortostatical). From the nervous system and sensory organs : fatigue, headache, dizziness, drowsiness; Rarely arrested, seven, a change in mood, Zrenia.so disorders of the urogenital system : peripheral edema (swollen ankles and feet); rarely increases in the frequency of urination, Impotenzia.so part of the intestine : nausea, pain in the abdomen; rarely neuralgia changes in urinating, Jeltuha.so the respiratory system : rarely Odyshka.so the musculoskeletal system : rarely artralgia, mialgia, paresthesia and pain in the extremities (with the long-term use). For the skin : skin, itching, rarely mnogoformnaya Eritema.prochie : rarely giperplazia gums, ginekomastia, raising liver enzymes.

Patient interaction

Compatible with major groups antigipertenziveh funds (dioretiki, ACE inhibitors, beta-adrenoblokatora), nitrates and gipoglikemicakimi drugs. Funds for inhalation narcosis (hydrocarbon derivatives), amiodaron, quinidine and other calcium antagonists (may exacerbate the effects). NPVS (especially indometacin) reduce antigipertenzivny effect (slow prostaglandines synthesis in the kidneys and natrillurez).

Overdosing

Symptoms : excessive peripheral vazodilatation expressed and prolonged decline in AD Tahikardia.lechenie : washing stomach, the appointment of activated carbon, giving patients the horizontal position with pripodnatami feet, monitoring the performance of the heart and lungs, control and BCC diureza; Symptomatic and supportive therapy, in / with the introduction of liquids glukonata calcium uptake, mezaton. Haemodialysis not effective.

Dosing and Administration

Inside. Angina in the initial dose of 5 mg once a day with a gradual increase to a maximum of 10 mg once a day; Arterial Hypertension - 5 mg (older-2.5 mg) once a day, if necessary, through the 7-14 days dose increased to 10 mg.

Directory → Organotropona funds → Cardiovascular funds → Blockers calcium channel → Amlodipine