FOXGLOVE (Digitalis) — sort of perennial herbaceous plants this. a figwort family (Scrophularia-seaye), including up to 36 types, from to-rykh 7 grows in the territory of the USSR. As sources of medicinal raw materials use generally 5 types of N. — purple, large-flowered, woolly, rusty and ciliate.
Foxglove purple (Digitalis purpurea L.) — large biannual herbaceous plant up to 120 cm high, leaves of an oblong and ovoid form, petiolar, up to 30 cm long and up to 15 cm wide. Leaves are fragile, wrinkled, from above dark green, from below grayish from abundance of long hairs. The smell of dry leaves weak, sharply amplifies during the insisting in hot water. The flowers 3 — 4 cm long which are horizontally rejected a cup campaniform, a nimbus sympetalous, purple or, more rare, white, a little wrong (braid), in a form the reminding thimble (fig). A fruit — an ovoid box with two shutters. Seeds very small, numerous, brown, wrinkled. Blossoms in June — July. In the USSR in a wild look it does not meet and cultivated in Ukraine, the North Caucasus and in other areas.
Foxglove large-flowered (D. grandiflora Mill.; synonym of D. ambigua Murr.) — perennial wild herbaceous plant up to 1 m high. Leaves elongated lantsetovid-nye, with an acute top, green color on both sides, up to 20 cm long and 2 — 6 cm wide. Flowers yellow, hung. Unlike purple N. large-flowered in the USSR is a wild-growing look. Meets in forest and forest-steppe zones of the European part of the USSR, in the Urals and in the districts of Western Siberia adjoining to it. Grows in deciduous and mixed forests, on edges of the woods, among bushes. Sometimes meets also on cuttings down in the pine woods. N purple contains 3 main primary glycosides: to a purpura and a glycoside And, purpureaglikozid In and glyuko-gitaleksinony Along with primary glycosides owing to the proceeding euzymatic processes purple and large-flowered N.'s leaves contain the secondary glycosides formed after eliminating of molecules of glucose: digitoxin, Gitoxinum and gitaloksinony
Foxglove woolly (D. lanata Ehrh.) — perennial herbaceous plant. Differs from N. purple in smaller leaves and flowers, a form and color of a nimbus, existence of a dense opushennost of an axis of an inflorescence, bract and share of a cup, brown-yellow with lilac veins. In a wild look grows on the Balkans, in the USSR in a small amount meets in Moldova in this connection it is included in «Red List» of the rare plants which are subject to protection. For receiving medicinal raw materials in the USSR it is entered into culture. N.'s leaves woolly contain more than 40 cardiac glycosides, lanatosidums And yes With, digitali-num verum, glyukolanatoksin, etc., the sum to-rykh makes 0, 48 — 0,56%.
Foxglove rusty (D. ferruginea L.) — a perennial plant with one or several stalks up to 1 m high. Leaves are prodolgovatolantsetovidny, smooth-edged, 7 — 15 cm long, 1 — 2,5 cm wide. On stalks multiflowered brushes 15 — 20 cm long, flowers with stupid calux lobes, a nimbus rusty zhel-ty with brown specks inside. Grows in the Caucasus and in Transcaucasia (except the territory of Armenia). Leaves contain apprx. 0,725% of cardiac glycosides (lanatosidums And, In, C and E, strospezid, verotoxin, etc.).
Foxglove ciliate (D. ciliata Trant.) — a perennial herbaceous plant with several branchy stalks up to 60 cm high. Leaves are lance-linear, 4 — 7 cm long, with rare hairs on veins. Flower brush one-sided, nimbus pale yellow, 1,5 — 2 cm long, flowers naperstkovidny. Grows in the Caucasus. From a grass more than 20 cardiac glycosides are emitted.
As medicinal raw materials from all types of N. (except N. ciliate) prepare leaves, and from N. ciliate — a grass. N.'s leaves prepare in July — August in a dry sunny weather, N.'s grass ciliate — during full blossoming and the beginning of fructification. Collected leaves at once dry up at t ° 60 — 70 °. Leaves of cultivated N.'s types after collecting immediately maintain within 30 min. at t ° 55 — 60 ° and then quickly dry up. Quantitative assessment of activity of the active ingredients which are contained in raw materials is carried out by method biol, by standardization on frogs and cats (see. Standardization of pharmaceuticals ), being guided by the relevant articles GFH. Suitable for the use consider N.'s leaves purple, large-flowered and rusty with activity, equal 50 — 66 ICE and 10,3 — 12,6 KED in 1 g. Viols, activity of leaves of N. woolly shall be not less than 100 ICE, N.'s herbs ciliate — not less than 80 ICE. At storage in unfavorable conditions activity of leaves of N. gradually decreases in this connection raw materials are exposed to annual control check by method biol, standardization.
Active ingredients H. are cardiac glycosides — the difficult connections like ethers containing in the structure genin (aglikon) and a carbohydrate component. The following 5 types of genin are characteristic of cardiac glycosides H.: digitoxigenin, gitoksigenin, gitaloksigenin, digoksigenin and diginatigenin, having a difficult cyclopentanperhydrophenanthrene kernel at the heart of structure.
where R — a carbohydrate part of a molecule, R 1 — H or OH, R 2 — H, OH or oson.
Depending on a structure of a sugar component distinguish primary, or geiuinny, glycosides (purpureaglikozida And yes In; Digilanidums And, In, With, etc.) and secondary, half-learning-mye at enzymatic eliminating of the separate carbohydrate remains. So, during the eliminating of trailer glucose from a purpureaglikozid And digitoxin, is formed of a purpureaglikozid In — gitoksinony Genuinical glycosides of N. woolly — Digilanidums, or lanatosidums — have the acetylated third digitoxose and trailer glucose. During the eliminating from lanatosidum And acetyl group and glucose digitoxin, from lanatosidum In — Gitoxinum is formed, and from lanatosidum With — digoksinony the Structure of the carbohydrate remains at various glycosides of N. is presented in the table.
Table. Options of a structure of the carbohydrate remains at glycosides of a foxglove
The N is long since applied in traditional medicine. In Russia since 1730 N. began to grow up as a medicinal plant. Implementation of drugs H. in scientific medicine is connected with the publication of work of the English doctor of W. Withering in 1775.
Drugs H. have specific cardiotonic effect. N.'s glycosides increase force and slow down heart rate, extend a diastole, lower conductivity on atipichesky fibers of a myocardium that can cause an urezheniye of heart rate and even a total atrioventricular block, and increase excitability of nodes of a myocardium. The last effect is especially accurate at introduction of high doses of drugs H. and is shown by tachycardia and emergence of geterotopny impulses in heart.
Therapeutic effect of drugs H. at a circulatory unefficiency comes down to fuller systolic emptying of ventricles (thanks to the combined impact on a systole and a diastole), to increase in cordial emission, decrease in venous pressure and reduction of compensatory tachycardia. At the same time the sizes of heart decrease, time of a circulation of blood is reduced, venous pressure goes down and the volume of blood decreases, hypostases decrease or liquidated. The ABP raises partially owing to direct vasoconstrictive peripheral effect, partially thanks to the central or reflex effect. The vasoconstrictive effect of N. can be shown in celiac arteries. Rise in systolic pressure is connected with increase in a stroke output of heart. Improvement of a peripheral hemodynamics leads to increase in a diuresis, decrease in volume of the circulating blood and reduction of hypostases.
At intake N.'s glycosides are soaked up rather fully. Effect of drugs H. develops only after stage of latency, duration to-rogo, as well as duration of effect of drugs, is various for separate glycosides. Due to the slow removal from an organism N.'s glycosides have ability to cumulation (see), edges in the sharpest degree it is expressed at digitoxin and least — at digoxin.
Drugs N. apply for treatment of heart failure of various origin, ta of a soars-michesky form of a ciliary arrhythmia, and also for prevention of heart failure at patients with organic lesions of heart. Treatment by drugs H. is carried out usually by appointment in the first 2 — 5 days of the maximum doses (taking into account individual sensitivity and associated diseases), to-rye shall provide optimum therapeutic effect. Further pass to maintenance doses, level to-rykh the hl is defined. obr. extent of elimination of glycosides. Administration of drugs of N. shall be long and is carried out under observation of the doctor. At intravenous administration drugs H. dissolve previously in 10 — 20 ml 5, 20 or 40% of solution of glucose or isotonic solution of sodium chloride.
In the course of treatment toxic action of N. can be shown by various disturbances of a cordial rhythm, frustration from outside went. - kish. path, cardiovascular and c. N of page, from organs of sight, skin, blood, endocrine organs. In medical practice of drugs of individual glycosides of N. precursory symptoms of overdose, characteristic of neogalenical drugs H. (e.g., loss of appetite, nausea, vomiting, a diarrhea) meet with implementation rather seldom, however disturbances of a cordial rhythm and conductivity more often began to be noted (premature ventricular contraction, a sinus arrhythmia, atrial tachycardia against the background of the atrioventricular block, and sometimes fibrillation of ventricles). Bouveret's atrial or ventricular disease is the basis to the immediate termination of administration of drugs of N. Development of intoxications by drugs H. is promoted by disturbances of electrolytic balance (a hypopotassemia and a hypercalcemia), a renal failure, existence of inflammatory and toksiko-allergic processes, a hypoxia, states after elektropmpulsny therapy, etc.
At emergence of symptoms of intoxication drugs H. it is necessary to stop accepting them. For treatment of arrhythmias use drugs of potassium, antiarrhythmic means (see), napr, dipheninum, xycain, ^-adrenoblockers ((((((((((anaprilin, etc.), novokainamid, Ajmalinum, Ethmosinum, Unithiolum (see), antagonists of calcium ions (magnesium sulfate) or the drugs connecting calcium (sodium citrate, sodium salt ethylene diamine tetraacetic to - you). At unsuccessfulness of medicinal therapy carry out electropulse treatment (see. Countershock ), at a cardiac standstill or a bradyarrhythmia artificial pacemakers use (see. Cardiostimulation ) .
Contraindication to use of drugs H. the expressed bradycardia, an atrioventricular block of various degree are.
Drugs of a foxglove
Drugs of a foxglove purple. Purple treat drugs of a foxglove: a leaf of a foxglove purple in powder, water infusion from leaves of a foxglove, extract of a foxglove dry, digitoxin (see), Gitoxinum, Cordigitum.
A leaf of a foxglove purple in powder (Pulvis foliorum Digitalis, SP. B) appoint inside or rektalno (in suppositories) the adult 0,05 — 0,1 g 3 — 4 times a day, to children — from 0,005 to 0,06 g to reception depending on age. The highest doses for adults inside: one-time 0,1 g, daily 0,5 g. Forms of release: the powder, tablets containing 0,05 g of powder from leaves of N.
Water infusion from leaves of a foxglove (Infusum foliorum Digitalis) is prepared at the rate of 0,5 — 1 g of leaves on 180 ml of water. Appoint the adult 1 table. l. 3 — 4 times a day, to children infusion (from 0,1 — 0,4 g of leaves on 100 ml) — on 1 chayn. l. 3 — 4 times a day.
Extract of a foxglove dry (Extractum Digitalis siccum, SP. B) appoint in the same doses, as a leaf of a foxglove purple in powder. Forms of release: the tablets containing 0,05 g of extract.
Gitoxinum (Gitoxinum, SP. A) — the individual glycoside received from a foxglove purple. On properties it is close to digitoxin, but is less active. Appoint inside in the first days of treatment 0,0002 — 0,0004 g a day; in the next days the dose of drug is reduced (to 0,0002 — 0,0001 g a day). Form of release: tablets on 0,0002 g.
Cordigitum (Cordigitum, SP. B) — the purified extract from leaves of a foxglove purple, containing the sum of glycosides. Appoint inside on V2 — 1 tablet 2 — 4 times a day or rektalno on 1 candle of 1 — 2 time a day. Forms of release: the tablets containing 0,0008 g of drug; the candles containing 0,0008 or 0,0012 g of drug.
Drugs of a foxglove woolly. Hl differ from drugs of a foxglove purple. obr. more bystry development of cardiotonic action and smaller ability to cumulation. In medical practice use drugs of individual glycosides of a foxglove woolly — acetyldigitoxin (see), digoxin (see) and Celanidum (see), and also the drugs containing the sum of glycosides, for example: Dilanisidum, lantosidum.
Lantosidum (Lantosidum, SP. B) — the neogalenical drug received from leaves of a foxglove woolly. Appoint inside 15 — 20 drops 2 — 3 times a day, and at the dispeptic phenomena rektalno in the form of microclysters (20 — 30 drops of drug in 20 ml of isotonic solution of sodium chloride). The highest doses for adults inside: one-time 25 drops, daily 75 drops.
Drugs of a foxglove rusty on pharmakol, are close to properties and use to drugs of a foxglove purple. From drugs of a foxglove rusty in modern medical practice apply digalen-neo.
Digalen-neo (Digalen-neo, SP. B) — the neogalenical drug containing the sum of glycosides from leaves of a foxglove rusty. Appoint inside or subcutaneously. Inside appoint 10 — 15 drops 2 — 3 times a day. Subcutaneously enter the adult 0,5 — 1 ml of 1 — 2 time a day, to children till 1 year on 0,05 — 0,1 ml, from 2 to 5 years — on 0,25 — 0,4 ml, from 6 to 12 years — on 0,4 — 0,75 ml. The highest doses for adults inside: one-time 0,65 ml (20 drops), daily 1,95 ml (60 drops); under skin: one-time 1 ml, daily 3 ml. Forms of release: ampoules on 1 ml for injections; the bottles containing 15 ml of drug for intake.
Drugs of a foxglove ciliate. From drugs of a foxglove ciliate in medical practice apply digitsnl.
Digicil (Digicilum, SP. B) — the neogalenical drug containing the sum of glycosides of a foxglove ciliate. Appoint inside on 0,5 — 1 tablet 2 — 3 times a day (1 tablet of digicil on activity corresponds to 0,1 g of leaves of a foxglove). See also Cardiac glycosides , Medicinal plants .
Bibliography: The atlas of areas and resources of medicinal plants of the USSR, under the editorship of P. S. Chikov, page 270, M., 1976, bibliogr; Clinical pharmacology, under the editorship of V. V. Zakusov, page 242, M., 1978, bibliogr.; Mashkovsky M. D. Pharmaceuticals, p.1, page 344, M., 1977; Sycheva I. M. and Vinogradov A. V. Chronic circulatory unefficiency, M., 1977, bibliogr.
Ya. I. Hadzhay.