Spirapril

Chemical name

(8S)-7-[(S)-N-[(S)-1-Карбокси-3- фенилпропил]аланил]-1,4 -дитиа-7-азаспиро [4.4] nonan-8-carbonova 1-etilovy acid ester (and as hydrochloride)

Gross

C22-H30-N2-O5-S2

Of drugs

The drugs-gipotenzivne, sossoudorasshiratee, cardioproteguoe, natriyureticescoe. Biotransformiroetsa in the liver with the formation of the active diazidnyi metabolita (contains carboxialkilnuyu group), enzyme inhibition. It stops making angiotenzina I angiotenzin II, providing sossoudossouerveshchee act expands receptacles reduces round, and the systemic and Sad Dad, the pressure in the lung capillaries. Improves the heart and increases the tolerance for endurance increases renin activity of blood plasma. The effect is a one hour reaches through 4-8 hours and lasts for about 24 hours (round-the-clock to control the AD to the reception once a day). Ingibiruya fabrics ренин-ангиотензинову�� the heart is cardioproteguoe Effects (prevents or contributes to the opposite of hyper and dilatation of the left heart chamber). Increases kidney blood has natriyureticescoe effect. In appointing the dose of 6 mg / day for 4 weeks does not diminish the speed clubockova filtering and Cl creatinine, even in patients with Cl creatinine less than 30 ml / min. Suppress aldosterone synthesis increases activity kallickrein-kininova system of accumulation in the tissues and blood bradikinina (reduces degradation to inactive peptides). This allows the release of biologically active substances (PGE_2 and PGI_2, endotelialny relaxation factor, predserdi natriyureticeski factor), an natriyureticescoe and sossoudorasshiratee effect. Provides education arginin-vazopressina and gli-1, the vazokonstrictoriani properties. Quickly and completely absorbed from the digestive tract. Bioavailability of 28-69%, with the plasma protein-89%. C_max spiraprila achieved through 1h metabolita, 3-4 hours; T_1/2-40 p.m. Return to jelchew and faeces (40-85%), as well as with urine.

Indications

Arterial hypertension, heart failure.

Restrictions on the use of

The ratio of the risk / benefit is needed in the following cases : angioneuroticeski swelling in history, heavy autoimmunity, or aortalny mitralny stenoses, gipertrofica cardiomyopathy (human hemodynamics), or other obstructive changes affecting the outflow of blood from the heart; Stenoses bilateral renal artery stenoses or artery only kidneys, the kidneys perezajenna, chronic obstructive lung diseases, giperuriquemia, giperkaliemia, giponatriemia or restriction of sodium in the diet, a general anesthesia and surgical interventions, dehydration, children's age (safety and efficiency to be determined).

Pregnancy and lactation

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

Contraindications

Hypersensitivity Arterial gipotenzia, severe kidney failure, Cl creatinine less than 10 ml / min expressed giperkaliemia, pregnancy, breast-feeding.

Side-Effects

From the circulatory system and blood (blood, gemostaz) : gipotenzia, incredible, lakopenia, thrombocytopenia, Anemia.so part of the intestine : xerostomia, changes in taste, neuralgia, attacked mindalinah and Azyke.so the nervous system and sensory organs : fatigue, dizziness, headache, сонливость.Аллергиче��кие reactions : angioneuroticeski swelling, skin and skin Zud.prochie : dry cough, muscle bogies lips and limbs, giperkaliemia, giperuriquemia.

Patient interaction

Effects increase gipotenzivee funds (additivoe effect), including beta-adrenoblokatora with significant systemic vsasavanii the eye forms diureticeskie means alcohol weakening - estrogena, NPVS (last at the same time increase the risk of kidney function), sodium chloride, simpatomimetiki. Potenziruet gipoglikemiceski effect protivodiabeticakih oral products; Reduces secondary giperaldosteronizm and gipokaliemia caused dioretikami; Improves concentration and toxic effect of lithium. Kalisberegate dioretiki, ciclosporin, potassium supplements, salt substitutes, milk, low-salt increases the risk of giperkaliemii. Funds depressing the bone marrow, increasing the risk of neutropenia and / or agranulozitoza fatal. Do dampening effect of alcohol on the central nervous system. Antatsida and holestiramin slow induction of the digestive tract.

Overdosing

Symptoms : acute arterial Gipotenzia.lechenie : dose reduction or elimination of the drug; Flush the stomach, giving patients the horizontal position, to introduce measures to increase the volume of circulating blood (a physiological solution, etc. transfusion blood liquids), symptomatic therapy : introduction epinephrine (a / c or / in), hydrocortisone (in / in).

Precautions

Treatment is carried out at regular doctor control. For one week before the start of pre-treatment gipotenzivnuu therapy should be abolished. To reduce the risk of symptomatic hypotension should be lifted for a few days before the start of treatment, or much lower dose adjusted vodno-elektrolitny balance. During a therapy monitoring AD picture control peripheral blood (before treatment, the first six months of treatment and then at periodic intervals for a period of one year, especially in patients with increased risk of neutropenia), the level of protein, potassium in plasma urea nitrogen, creatinine, kidney function, body mass index, diet. With the development of the patient giponatriemii or dehydration is a correction mode (decrease doses). During treatment recommended that the use of alcoholic beverages and use appropriate measures of contraception. Be wary of during the drivers of vehicles and people skills relate to the high concentration of attention. In leading up reception dose double.

Dosing and Administration

Dose picked individually, depending on the development of AD. Inside, with liquid squeezed small amounts of fluid one (morning). Adults initial dose of 3 mg once a day, if necessary, up to 6 mg / day to achieve the desired effect. If any of the kidney mode depends on the Cl creatinine : Cl in 30-60 ml / min designate average therapeutic dose, and Cl 10-30 ml / min to 3 mg.

Literature

1. DV Preobrazhensky, A. Sidorenko, Romanov NE, Shatunov IM Clinical pharmacology major classes of drugs antigipertenziveh / / Consilium Medicum .- 2000 .- T. 2-N 3-A 99-127.2. A. Sidorenko, DV Preobrazhensky Clinical use of inhibitors ангиотензинпревращаю щего Enzyme-Metro : LIA "Presid", 1998-1996 pp.

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