Nitrendipine

Chemical name

Ethyl ether 1,4-дигидро-2,6-диметил-4- (3-нитрофенил)-3,5- piridindicarbonova acid

Gross

C18-H20-N2-O6

Characteristics

Derived 1,4-digidropiridina-calcium antagonist II generation.

Of drugs

The drugs-gipotenzivne, sossoudorasshiratee, antianginalnoe, nefroproteguoe. Specifically binds to receptors membrannami governing the potencialzawisimah calcium channel L-tipa, reduces the flow of calcium ions into the cell during membrane depolarization. Mostly affects cells smooth muscles receptacles (coronary less than etc.). And vsokoselektive long sossoudorasshiratm action. The system vazodilatatia, reducing round, and as a consequence, hypotension. AD ought to dose, it is Orthostatic Hypotension and the development of tolerance, does not violate zirkadie rhythm changes AD. Increase pressure kidneys, increases the blood predserdnyi natriyureticski peptide increases down sodium and water, activates simpatoarenalovu (HR usually does not change) and ренин-альдостеронову�� (content angiotenzina plasma renin and substantially increases system). However, in early therapy may experience temporary reflected tachycardia. No impact on sinusovy and AV node. After receiving 20 mg nitrendipina in patients with light and heavy loans has decreased Sad Dad, and by 15 to 20%. Effective in alone, and in combination with gipotiazidom and propranololom. Prolonged therapy helps opposite of the left thyroid heart and show nefroproteguogo action. Gipotenzivny biggest effect is in older patients with low renin plasma. In patients older (60 years and older) with isolated sistolicescoy hypertension (Sad at least 160 mm Hg and Dad less than 95 mm Hg) in the use of a two-year (initial dose, 10 mg / day, and then up to 40 mg / day in 2 admission) prevents cardiovascular complications : reduces the frequency of brain stroke by 42%, the frequency of cardiac complications (heart failure, heart attack, sudden death) by 26%, the frequency of cardiovascular complications by 31%. In sublingwalna software has the opportunity to heavily gipertoniceski kriza. The dose of 10-20 mg / day effectively (especially in the continuous therapy for many years) warns vazospasticescoy attacks and strokes improves remote Prognoz.pri ingestion quickly and almost completely absorbed. Bioavailability 60-70%. C_max plasma achieved in 1-2 hours, the level of plasma, 9-42 ng / ml, has been associated with the protein in the blood of 98%. Almost completely metabolized in the liver by oxidation. Return with the urine (30%) in four polar metabolites, T_1/2 ranges from 8-24 am The Cl - 1.3 l / min. The elderly and patients with liver cirrhosis T_1/2 and concentration in the blood increase (to a daily dose). Provides teratogenic effect.

Indications

Arterial hypertension (monotherapy or in combination with бета-адреноблокатора��и mochegonnami and drugs), diabetic Nephropathy (subject to the availability of contraceptive use or intolerances ACE inhibitors).

Pregnancy and lactation

Contraindicated in pregnancy. At the time of treatment should stop breastfeeding.

Contraindications

Heavy forms of congestive heart failure and weakness syndrome sinusnogo unit stenoses mouth Even expressed gipotenzia arterial, the first weekday after myocardial infarction, pregnancy, breast-feeding.

Side-Effects

From the circulatory system and blood (blood, gemostaz) : hyperemia skin and the upper torso, gipotenzia, tachycardia, anaemia, Trombozitopenia.so the nervous system and sensory organs : headache, drowsiness, parestesia; Rarely impaired vision, mialgia, tremor (at higher doses). From the urogenital system : peripheral edema (swollen ankles, lower limbs); rarely increases in the frequency of urination; worsening renal function (with kidney failure). For part of the intestine : nausea, feeling of fullness stomach, vomiting, constipation; rarely diarrhoea; in a few cases vnutripechenochny Holetaz.so the Skin : erythema, prurit, urticaria, makulopapuleznaya Exantema.prochie : lifting syndrome (5-10%); rarely giperplazia gums, raising transaminaz, ginekomastia (at the elderly patients).

Patient interaction

Antihypertensive, blockers H_2-gistaminovh receptors increase effect estrogena, NPVS-weakened. Could increase plasma concentration of cardiac glycosides developmental toxic effects. Metoprolol, aceboutolol, atenolol and ranitidine may reduce plasma klirens.

Precautions

Be wary of during the drivers of vehicles and people skills relate to the high concentration of attention. During treatment must refrain from receiving alcohol.

Dosing and Administration

Inside, usually on 20 mg morning. Depending on the effect and acceptability daily dose can be gradually increase to a maximum of 40 mg (20 mg twice a day), or reduced to 10 mg.

Literature

Elbl L., V. Chaloupca The effect of the treatment Nitrendipine on the left ventricular function and morphology in hypertensive patients / / Noninvas. Cardiol 1996 .- .- V. 5-N-1 P. 40-54.

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