This section is from the book "A Treatise On Therapeutics, And Pharmacology Or Materia Medica Vol2", by George B. Wood. Also available from Amazon: Part 1 and Part 2.
Black hellebore is the root (rhizome and fibres) of Helleborus niger, a small, herbaceous, perennial plant, sometimes, from its period of inflorescence, and the aspect of its flower, called the Christmas rose. The plant is a native of the hilly regions of southern and middle Europe, from the Archipelago on the one side, to the Bay of Biscay on the other. The root, as used in this country, is imported chiefly from Germany.
it consists of a blackish or brownish knotted head or rhizome, very irregular in shape, half an inch thick or less, and several inches long, showing the remains of the leafstalks on its upper surface, with numerous dark brown, radical fibres, cylindrical, about as thick as a straw, and from four to twelve inches long, which are sometimes attached to the sides and under surface of the rhizome, sometimes separate, and generally more or less broken. The colour of the root is internally whitish; and, when one of the radicles is broken transversely, the pith appears somewhat stellate. By these characters, the root may generally be distinguished from those of other plants, which are said to be now frequently mixed with or substituted for it. The root has a very feeble odour, said to resemble that of seneka, and a taste which, though slight at first, becomes bitterish, acrid, and nauseous. in the fresh root the taste is extremely acrid and burning; but the acrimony is diminished by drying, and very much impaired by time. Water and alcohol extract its virtues; which are much injured by long boiling.
Active Principle. Black hellebore contains a volatile oil, with which its acrimony is probably connected, in some measure at least, and upon the escape of which may possibly depend the diminution of the activity of the drug by drying and by time. There is also said to be an acrid fixed oil among its ingredients; and a peculiar principle has been discovered, called helleborin, which is white, crystallizable, bitter to the taste, with a slight tingling effect on the tongue, and neuter in its relation to acids and alkalies. (See U. S. Dispensatory.) How far this principle is connected with the medicinal activity has not, I believe, been ascertained.*
* Some entirely new views of the properties of black hellebore have been presented by Professor Schroff, of Vienna, based upon experiments on rabbits, and on man both healthy and diseased. I give them in a note, because they are so much in opposition to common opinion, that they cannot be received as quite correct, until confirmed by further research. The root, he says, is inodorous, nearly tasteless, and destitute of any active volatile principle, as it is not more energetic fresh than dried. it has little medicinal activity. Two drachms of the fresh, and a drachm of the dried root are well supported by rabbits, and the same is the case with the watery or ethereal extract in the dose of from 15 grains to a drachm. in man, 23 grains of the watery and half the quantity of ethereal extract produce no remarkable effect. The root collected in May is most active. The physiological effects are ascribable to a narcotic and an acrid principle; the former producing heaviness of the head, vertigo, abnormal sounds, dilatation of the pupil, troubled sleep, the retardation of the pulse, etc.; the second, vomiting, stomachic and intestinal pains, and diarrhoea, which is, however, exceptional. Sometimes the salivary and urinary secretions are increased. Professor Schroff does not admit that black hellebore has, with man, the properties of a drastic cathartic. it even produces more frequently constipation than purgation; though it very often occasions loss of appetite, nausea, and even vomiting. When it causes death, it acts by paralyzing the heart; probably through the ganglionic nerves, which it reaches through the blood. it never produces gastro-intestinal inflammation. The watery extract is less active than the alcoholic; the former containing only the narcotic principle, while the latter contains both (Archives Generates, Aout, 1859, p. 232.) From this summary of the properties of black hellebore, it would appear to belong less to the cathartics than to the nervous sedatives, and would take rank with digitalis, aconite, American hellebore, etc. (Note to the second edition.)
Black hellebore was long thought to be the celebrated hellebore of the ancients; but, at present, it is generally believed that the latter was the root of another species, Helleborus orientalis, which has been found growing in the districts, where in the yet unsettled state of our knowledge of the chemical and physiological properties of the hellebores, I deem it better to keep the reader acquainted with the results of experimental research, as they are presented to us in the journals, than to endeavour to draw precise conclusions, for which there are yet scarcely sufficient grounds. The most recent experiments are those of Messrs. Marine and Husemann, who examined three different species, II viridis, II. niger, and H foetidus, and present us the following results. in the lower leaves and roots of these species there are two active fixed principles, of the nature of glucosides, and in the H. foetidus probably a third principle which is volatile. The two non-volatile principles are named by the authors, respectively, helleborin and helleborein. They are both poisonous to the lower animals, and inferentially also to man. The volatile oil, referred to in the text, freed from these glucosides, may be taken in considerable quantities without dangerous effects.
Helleborein is characteristically indifferent to alkalies or ferments, but is readily soluble and easily absorbed. Though not irritant to the skin when protected by the cuticle, it is strongly so to the mucous membranes; inflaming the conjunctiva, causing sneezing when in contact with the Schneiderian membrane, and exciting the salivary secretion both by its local influence, and through the circulation when absorbed. in very small doses, it produces no observable effect when swallowed, but, if allowed to accumulate, it causes anorexia, nausea, and even vomiting, with pain, augmented secretion, and, if in sufficient quantities, gastro-enteritis. The kidneys and female genitals are also stimulated. While very small doses act on the heart similarly to digitalin, retarding the circulation; large doses greatly accelerate the contractions of that organ, often even fatally; and gradual paralysis and convulsions may coexist with this effect on the heart.
Helleborin is less soluble in water, and less irritant to the mucous membrane, but more poisonous in small doses. The tongue is affected by it as by aconite The nervous system is peculiarly disturbed. in greater or less degree, according to the dose, disordered nervous symptoms are produced in animals, beginning with hurried breathing, restlessness, tension and trembling of the muscles, great depression, uncertain movement, then retardation of the pulse and breathing, irritability of the surface, great dilatation of the pupil, loss of hearing, and finally almost complete anaesthesia, with strong cerebral and spinal congestion, and even apoplexy. in other respects helleborin coincides in its effects with other narcotics.
The decidedly poisonous properties of II. foetidus, which contains less of the helleborin, is probably owing to its volatile principle, together with the helleborein. (Am. Journ. of Pharm , May, 1866, p. 245; from the Druggists' Circular, April,. 1866,. p. 90.) - Note to the third edition.
the plant used by the ancients is known to have been most abundant. in the recent state, the root is said to be violently acrid, producing, when applied to the skin, inflammation and even blistering; but this property is much diminished by drying, and is lost by time. When taken internally, the medicine has been considered as a drastic hydra-gogue cathartic, with a disposition to stimulate the uterus, and was therefore ranked with the emmenagogues. it is, however, uncertain in its operation, sometimes acting harshly in doses, in which, at other times, it produces little or no effect, and in over-doses causing hypercatharsis, with vomiting, abdominal pains, cramps, and convulsions, which have sometimes ended fatally. This inequality of action may arise, in part, from difference of susceptibility in the persons taking it, which seems to be common in relation to the Ranunculaceae, and partly from the great inequality in the strength of the medicine, in consequence of the deterioration it undergoes by keeping. Some suppose that its active matter is absorbed, and has a special disposition, like that of aloes, to act on the pelvic viscera. From the manner in which it acts poisonously on the lower animals, it has been supposed to operate also specially on the brain.
The hellebore of the ancients had great reputation in the treatment of insanity, melancholia, and epilepsy; and was believed to operate usefully in these complaints through its purgative properties; but it is not impossible that the supposed narcotic influence may have had some instrumentality in the favourable results. The ancients used it also in amenorrhoea, dropsy, worms in the bowels, and affections of the skin. in this country, black hellebore is little employed,, except, perhaps, in amenorrhoea, in which it is supposed to be useful by a specific action on the uterus, independently of purgation. At one time I employed the medicine to a considerable extent, but found it so often quite ineffectual, and at all times so uncertain, that I long since abandoned the use of it altogether.* My want of success with it may have been owing to the deteriorated character of the drug, in consequence of its having been long kept in the shops. I can readily understand, however, that, in the countries where it may be obtained fresh, and of unimpaired powers, it may be a useful remedy in the complaints in which its congener was employed by the ancients.
* This want of success is readily explained, if the researches of Professor Schroff are correct. in this case, it would seem that the inactivity referred to in the text is owing, not to the loss of power by time, but in fact to original deficiency. The remarks above made in reference to the acrimony of the fresh root, its drastic cathartic properties when recently dried, and its loss of power by time, were of course based on the authority of European writers; as the plant is not cultivated in this country, and the author has never had the opportunity of using the fresh root. [Note to the second edition.)
The dose of the root, with a view to full effect, is from ten to twenty grains. From three to six grains of it may be given as an alterative and aperient, in skin affections and portal congestion. A decoction, made by boiling two drachms in a pint of water, has been recommended in the dose of a fluidounce every four hours.
The Alcoholic Extract (Extractum Hellebori Alcoholicum, U. S.), prepared as directed in the U. S. Pharmacopoeia, may be administered in the dose of ten or twelve grains.
But the Tincture of Black Hellebore (Tinctura Hellebori, U. S., Lond.), not unfrequently called tinctura melampodii, is the preparation most employed. it is used chiefly in amenorrhoea, in the dose of one or two fluidrachms. Dr. Meade, who especially recommended it in this affection, gave two teaspoonful, in a glass of warm water, twice a clay.