TsELANYD (Celanidum; synonym: Isolanidum, Cedilanid, Ceglunat, Digila-nid C, Isolanid, Lanatigen C, Lana-tosidum C; GF X, SP. A) — cardiotonic means from group of cardiac glycosides. Molecule C. consists of an aglikon of the digoksigenin and glycane containing two molecules D-digitoxoses and on one molecule of an atsetildigitoksoza and D-glucose; C49H76O20:
Colourless or inodorous white crystal powder. We will dissolve in water very little, we will difficult dissolve in 95% alcohol, we will dissolve in methyl alcohol, it is a little ether-soluble, chloroform and petroleum ether; pier. weight (weight) 985,1. C. is drug of primary gdikozid (lanatosidum C) foxgloves of woolly (Digitalis Lanata Ehrh). At euzymatic hydrolysis after eliminating from it of glucose and acetic to - you are formed a secondary glycoside digoxin (see), Celanidum is very close to Krom on properties and differs in a little bit smaller activity and more bystry development of action.
It is similar to another cordial a glycoside am (see). C. possesses positive inotropic and negative
chronotropic effect, complicates atrioventricular conductivity and increases automatism of heart. Mechanism of kardiotropny action of C., as well as other cardiac glycosides, perhaps, it is connected with blockade of transport Na+, K+-ATF - elements in membranes of cardiomyocytes in this connection C. breaks transport of ions of K+ in cells and ions of Na + from cells (see Transport of ions). Strengthening of ions of Na + in cardiomyocytes leads to the strengthened receipt in cells of ions of Sa2 + in exchange for ions of Na+. Brake influence of ions of Sa2 + on system troponin — tropomyosine promotes interaction of actin and a myosin and strengthening of reductions of myofibrils (see. Muscular contraction). Negative chronotropic effect of C. increase in automatism — decrease in maintenance of ions of K+ in fibers of the carrying-out system of heart is caused by reflex stimulation of vagus nerves (a cardio-cardial reflex), and that leads to acceleration of slow (diastolic) depolarization and respectively — to increase in frequency spontaneous an impulse - a tion (see Heart, physiology).
Biol. activity of Celanidum — 14 000 — 16 000 ICE, or 3200 — 3800 KED in 1 g. Therapeutic index C., as well as all cardiac glycosides, it is low: therapeutic dose of C. makes apprx. 50 — 60% of its toxic dose.
At purpose of C. inside in went. - kish. a path 20 — 40% of the accepted dose are soaked up. Effect of drug begins in 1 — 2 hour and reaches a maximum in the 6th hour. At intravenous administration action of C. begins in 15 — 30 min. and reaches a maximum in 2 hours. An elimination half-life — apprx. the 30th hour. Celanidum contacts proteins of a blood plasma a little and from all glycosides of a foxglove has the smallest ability to cumulation. It is allocated generally with kidneys, considerably in not changed look.
C. apply at acute and hron. to heart failure, takhisis-tolichesky form of a ciliary arrhythmia of auricles, supraventricular Bouveret's disease. In an initiation of treatment of C. appoint inside 0,00025 — 0,0005 g in tablets or on 10 — 25 drops of 0,05% of solution 3 — 4 times a day. After achievement of full therapeutic effect (usually on 3 — the 5th day) C. appoint in maintenance doses 0,00025 — 0,0005 g in tablets or 10 — 40 drops of 0,05% of solution a day. Intravenously C. enter on 1 — 2 ml 0,02% of solution into 20 ml of 20% of solution of glucose (slowly) 1 — 2 time a day. The highest doses for adults inside: one-time 0,0005 g
(0,5 mg), daily 0,001 g (1 mg); intravenously: one-time 0,0004 g (0,4 mg), daily 0,0008 g (0,8 mg).
At overdose of C. premature ventricular contraction, disturbance of atrioventricular conductivity, nausea, vomiting, loss of appetite can be noted. C. it is contraindicated at heart blocks and intoxications other cardiac glycosides. At the coronary insufficiency, active myocarditis expressed to bradycardia drug appoint with care.
Form of release: tablets on
0,00025 g (0,25 mg); bottles on 10 ml of 0,05% of solution (0,5 mg in 1 ml) for intake; ampoules on 1 ml of 0,02% of solution (0,2 mg in 1 ml). Storage: in the place protected from light.
Bibliography: Here B. E. and Sluts chat
M. E cue. Cardiac glycosides, M., 1973. V. V. Maysky.