PHEPROMARONUM (Phepromaronum; joint venture. A) — anticoagulant of indirect action. Z-a-Fenil-R-propionil-etil-4-oksikumarin; C20H18O4:
Inodorous crystal powder, white or white with slightly creamy shade. It is almost water-insoluble, a little alcohol-soluble. In water of a rastvorim sodium salt F. (nafarin).
As well as other aitikoagu-lyanta of indirect action, T. is an antimetabolite of phthiocol. Affects coagulability of blood only in an organism. II (prothrombin), VII (proconvertin), IX (Christmas factor), X reduces biosynthesis of blood-coagulation factors (Stewart — Prauer a factor). Before others this action F. II is shown concerning factors of VII and IX, and late and X (see. Coagulant system of blood). In the same sequence there occurs also recovery of their activity. Reduces aggregation ability of thrombocytes only at long appointment. T. increases rate of volume flow of a coronary blood-groove. At patients with coronary heart disease drug has spasmolytic effect on coronary vessels that is followed by weakening of a pain syndrome. At patients with atherosclerosis F. normalizes a ratio in blood and - and R-liioproteidov.
T. it is quickly enough and fully soaked up in went. - kish. a path and in 15 min. after intake. it is found in a blood plasma. In the maximum concentration collects in blood in 60 — 90 min. Decrease in concentration F. in blood occurs within 24 — 48 hour. Kinetic curve of concentration F. in plasma after intake has the three-phase form: initial increase in concentration in blood due to intensive absorption, a cut is replaced by its bystry falling in 8 — 10 hours then there comes the phase of slow equilibrium removal of drug. In blood F. highly contacts albumine of plasma, but practically does not come at the same time to uniform elements of blood. Nek-ry pharmaceuticals, napr, acetilsalicylic to - that and Butadionum, oppress binding F. with proteins of plasma. These preparatm reduce stage of latency of antikoagulyatsn-onny action F. and time of achievement of a maximum of its effect, distribution and removal accelerate. Inductors of microsomal ferkhment of a liver, napr, phenobarbital, accelerate metabolism F., slightly influencing kinetics of its distribution. At the same time they considerably reduce anticoagulating activity F. also reduce duration of its action, but do not influence duration of stage of latency.
Like other anticoagulants of indirect action, T. apply to long decrease in coagulability of blood for the purpose of prevention and treatment of trokhmboembolichesky complications.
T. appoint inside the adult in the 1st day in a daily dose 0,03 — 0,05 g. For the 2nd day the dose is reduced to 0,02 — 0,03 g. In the next days drug is appointed in maintenance doses on 0,01 — 0,005 g a day or every other day depending on indicators of a blood coagulation. Therapeutic level of hypocoagulation consider such, at Krom tromboplastinovy time on Kvika is extended by 2 — 2,5 times that corresponds to a prothrombin ratio of 40 — 50%. It is contraindicated in the same cases, as other anticoagulants (at the lowered coagulability of blood, a peptic ulcer, pregnancy and DR-) -
the Form of release: tablets on 0,01 g. Storage: in the place protected from light.
See also Aitikoagulyanta.
Bibliography: L and to and K. M. Eksperi's N
a mental research of anticoagulants of a monocoumarinic row, Cardiology, t. 9, No. 7, page 80, 1969; L and to and K.M. N and d river. Pharmacokinetics antikoagulyan * t, derivative 4 oxycoumarins, Pharm. and toksikol., t. 44, No. 4, page 484, 1981;
L yu with about in V. A., Belousov Yu. B. and B about to and p e in I. N. Treatment trombo-
call and hemorrhages in clinic of internal diseases, page 191, M., 1976; Mayo
ditch of IO. M. Comparative assessment of anticoagulants of indirect action of Phepromaronum and nitrofarin, Cardiology, t. 11, No. 11, page 100, 1971; Malinov-s to and y H. N and Kozlov V. A. Anticoagulating and thrombolytic therapy in surgery, M., 1976; H and -
z about in E. And. both L and to and K. M N. Anticoagulants and fibrinolitic means, M., 1977. K. M. Lakin.