ETAKRYNOVY ACID (Acidum etacrynicum; synonym: Uregitum, Ede-cril, Endecril, Etacrynic acid, Ure-git, etc.; SP B) — diuretic. 2,3-Dikhlor-4-(2-metilenbutit) - phenoxy-acetic to - that; Ci3Hl804C12:
AA. to. badly a rastvorima in water, it is rather good — in solutions of alkalis and organic solvents.
Strengthens allocation by kidneys of ions of chlorine, sodium, potassium, calcium and magnesium, increases release of water. Expressiveness of diuretic effect does not depend on a condition of water-salt balance of an organism. AA. to. works preferential in the ascending part of a nephronic loop where it blocks active transport of ions of chlorine. Therefore it is carried to group of so-called loopback diuretics, to-rye have the expressed natriuretic and chlorine-uretichesky effect. Mechanisms of action E. to. are found out insufficiently. Drug blocks sulphhydryl groups in kidneys, and also Na-, K-dependent ATP-ase. Assume that E. to. increases permeability of intercellular intervals for ions owing to what overall performance of sodium and chloric ionic pumps in renal tubules decreases and umenshav the reabsorption of ions of sodium and chlorine etsyatsya.
It is well soaked up from went. - kish. path. At intake E. to. the diuresis develops in 30 — 601 min., reaches a maximum in 2 hours and proceeds apprx. 6 — 9 hour. At intravenous administration 1/3 from the entered dose it is allocated to cookies, and 2/3 are removed by kidneys. In a kidney E. to. intensively is exposed to canalicular secretion and in a significant amount comes to a gleam of a proximal tubule. In urine find not changed E. to. and two of its metabolites, one of to-rykh represent a conjugate E. to. with cysteine.
AA. to. apply at the hypostases connected with a circulatory unefficiency, hypostases of a renal origin and also at wet brain and a fluid lungs. AA. to. has moderate hypotensive effect and it can be used in combination with other antihypertensives for treatment of an idiopathic hypertensia.
Appoint inside the adult, since 0,05 g and if necessary raising a daily dose to 0,1 — 0,2 g. The daily dose of drug is usually accepted in the morning after food. Drug is more effective if it is used not daily, and with a break in 1 — 2 day. If necessary to cause bystry effect etakridi-new to - that enter intravenously in a dose of 0,05 g.
As side effects E. to. can cause a hypopotassemia, a gipokhloremichesky alkalosis and a hyperuricemia. For prevention of a hypopotassemia appoint a diet rich with potassium or drugs of potassium. The phenomena of a hypopotassemia are weakened at simultaneous use E. to. with antagonists of Aldosteronum, napr, with Spironolactonum. In some cases at administration of drug dizziness, weakness, dyspepsia, diarrhea develops. Decrease in hearing is possible, especially at introduction of high doses E. to. the patient with a renal failure that is explained by change of electrolytic structure of an endolymph of an inner ear. The Ototoksichesky effect of drug amplifies at its simultaneous use with antibiotics from group of aminoglycosides.
AA. to. it is contraindicated at a heavy renal failure and severe damages of a liver. It is not recommended to appoint drug in the first months of pregnancy.
Form of release: tablets on 0,05
ETHANOLAMINES 359 and 0,1 of; the ampoules containing 0,05 g of sodium salt of Acidum etacrynicum to-ruyu before introduction dissolve in isotonic solution of sodium chloride or glucose.
See also Diuretics. Bibliography: Lebedev of A. A. Diure
tics and blood circulation, page 71, M., 1984; The pharmacological basis of therapeutics, ed. by A. G. Gilman and. lake, N. Y., 1980; Nechay B. R. Biochemical basis of diuretic action, J. clin. Pharmacol., v. 17, p. 626, 1977. And. A. Lebedev.