Pilocarpus 1907 PILOCARPUS. U. S. (Br.) PILOCARPUS [Jaborandi]
" The leaflets of Pilocarpus Jaborandi Holmes or of Pilocarpus microphyllus Stapf (Fam. Butacete), yielding, when assayed by the process given, below, not less than 0.5 percent, of alka-loids." U. S. " The dried leaflets of Pilocarpus Jaborandi, Holmes." Br.
Jaborandl Folia, Br.; Jaborandi leaves; Pilocarpi Foliola ; Jaborandi, Folia Jaborandi. Jaborandiblatter. Jaborandi, Jaborandi (Hoja de), Piloearpus was first introduced to the notice of the European profession by Coutinho under the name of Jabo-randi, a name which has adhered to the drug, although the terms Jaborandi, borandi and Jamborandi are used in South America to designate various pungent, sudorific plants, most of which belong to the genus Piper, but some of which have no botanical relation at all with the peppers. Although the leaves of the Piper Jaborandi have been sent into commerce as Jaborandi, none of the true jaborandies of South America have any physiological relations with the official drug, which in South America is known as Arruda do Mato or as Arruda brava and rarely as Jamguarandi or Jaurandi.
The genus Piloearpus consists of woody shrubs belonging to the Rutaceae and inhabits tropical and subtropical America, including Cuba, Guadeloupe, Martinique, and probably other islands. For an elaborate botanical and histological study of the commercial species of Piloearpus by A. Duval, see B. Sc. Pharm., vii., Feb. 1903. The commercially important species of the genus are as follows:
P. Jaborandi, Holmes; P. officinalis, Poehl. This plant inhabits the northern and north-eastern part of Brazil whence its leaves find their way through Sergipe, Allogoa, Sobral and Ceara, etc., to Liverpool and Hamburg, the chief centres of European commerce in the drug. Like those of P. selloanus its leaves are two or three jugate and are especially sepa-rated from those of the P. pennatifolius by the fact that all of the leaflets except the terminal one have their bases cordate, while the bases of all the leaflets of P. pennatifolius are attenuate.
P. pennatifolius, Lemaire; P. simplex, Baillon, inhabits the southern portion of Brazil and Paraguay, whence its leaves were formerly largely exported through Buenos Ayres and Rio Janiero; at present they seem to have almost disappeared from commerce.1 The leaves are oval, elliptical, obtuse, attenuate at the summit, which is feebly emarginate, and also attenuate at their base but not petiolated. The species is recognized in the French Codex.
P. selloanus, Engler, formerly official in the U. S. P., appears to be a variety of P. pennatifolius, Lemaire, from which it differs almost solely in the length of its flower stalk, which is six times as long as the flower bud, while that of P. pennatifolius is but three to four times as long as the bud. P. selloanus seems to be the more southern plant of the two, and is especially abundant in Paraguay.
Properties.—An alkaloid was isolated in 1875 from jaborandi almost simultaneously by A. W. Gerrard and M. Hardy. To this the name of pilocarpine was given. Gerrard at the same time stated that there were at least two alkaloids in the leaves, and this view seemed to be confirmed when jaborine was discovered. He also obtained a volatile oil, tannic acid, a peculiar volatile acid, and potassium chloride. Pilocarpine may be prepared as follows. The leaves are exhausted with 80 per cent, alcohol containing 8 grammes of hydrochloric acid in a liter, the tincture is distilled and evaporated to the consistence of a liquid extract, and this is mixed with a small quantity of water, and filtered. The filtrate is treated with a slight excess of ammonia, and then with a large quantity of chloroform. The chloroform solution is agitated with water, to which hy-drochloric acid is added, drop by drop, in sufficient quantity to neutralize the alkaloid, the hydrochloride of which is obtained in long needles on evaporating the aqueous solution, while foreign principles remain dissolved in the chloroform. By dissolving the crystals in water, treating the solution with ammonia and chloroform, and evaporating the latter solution, pilocarpine is obtained as a soft viscous mass, which is only slightly soluble in water, but is freely soluble in alcohol, ether, and chloroform.
1907 Uses of Pilocarpus
Uses.—When an infusion containing sixty to ninety grains of jaborandi is given to an adult, in about ten minutes the face and neck become deeply flushed, and free perspiration and salivation commence. After a hypodermic injection of the alkaloid, the symptoms may set in in six minutes. The sweating begins on the face; both it and the salivation are excessively profuse, and last from three to five hours. There is frequently nausea, and sometimes vomiting. The pulse is generally more or less quickened, as is also usually the respiration. After the sweating has ceased, the patient is left more or less exhausted. The nasal and lachrymal secretions are very generally increased under the action of the drug, and Gubler has noted diarrhoaa. There is some-times contraction of the pupils, and even disturbance of vision. These effects of the drug are in the adult fairly constant, but subjects have been occasionally found who were not susceptible to the action of the remedy, and, very curiously, in Ringer's experiments children were found to be very insusceptible, although doses of sixty grains were employed. Schwann and subsequent observers have noticed in the lower animals that very violent intestinal peristalsis is produced by the drug. The sweat produced by jaborandi is often enormous in quantity (from nine to fifteen ounces by estimation). It is stated to be at first acid, then neutral, and finally often clearly alkaline, as is also the saliva. Not only the aqueous but also the solid portions are increased, and the elimination of urea is said especially to be affected. Usually, but not always, when the drug acts very moderately upon the skin the salivary glands are but slightly affected, and vice versa. The cause of the excessive secretion is a direct action upon either the gland cells or the peripheral nerve endings, most probably upon the former. In the first stages of sweating the bodily temperature sometimes rises, but it usually falls after the sweating.
When applied to the eye, pilocarpine pro-duces great contraction of the pupil, tension of the accommodative apparatus, and an approximation of the nearest and farthest points of distinct vision, by a peripheral action. It is stated to produce less irritation than Calabar bean.
Jaborandi is the most reliable and powerful of the diaphoretics. In dropsies it has been widely employed, and certainly is a most efficient remedy. Great value has been ascribed to it in facilitating the removal of local aqueous effusions, such as occur in pleurisy and pulmonic tKdema. In urcemia it is the most efficient remedy at our command. In the forming stage of subaeute rheumatism, coryza, influenza, and similar conditions, pilocarpine may be very useful. In acute or chronic Bright's disease it is of great value, sufficing in the one case to bring about convalescence, and in the other greatly to prolong life and make it comfort-able. The sweats may be repeated daily, bi-weekly, or weekly. Recently, the plan of giving very small doses at short intervals as a diuretic has been strongly commended.
Jaborandi is usually given in the form either of the fluidextract or of the alkaloid. The full diaphoretic dose of the fluidextract is from forty to sixty minims (2.5 to 3.75 Ce.), of a salt of piloearpine one-sixth of a grain (0.01 Gm.). When excessive vomiting is produced by the drug, it is better to administer it every ten minutes in fractional doses. After the second or third dose, unless contraindicated, whisky and hot water should be given.
It has been proved by elaborate experimentation that in many of their actions upon the human system pilocarpine and atropine are directly antagonistic, and in poisoning by jaborandi or its alkaloid, atropine has the power to arrest the excessive secretion and save life. The value of pilocarpine in atropine poisoning is not quite so certain, but there is enough evidence to demand further trial of it. Purjesz of BudaPesth, reports (Centralb. fur Prakt. Augenhk., 1880) a case in which two and a half grains of atropine sulphate were said to have been taken, and relief, with final recovery, was secured by hypodermic injections of 0.4 grain of pilocarpine every ten minutes until 6.4 grains had been administered. For other similar but less striking cases, see B. M. J., Jan. 1887; L. L., July, 1890.
Dose, of jaborandi, from twenty to sixty grains (1.3 to 3.9 Gm.).
Off. Prep.—Fluidextractmn Pilocarpi, U. 8. (Br.) ; Tinotura Jaborandi, Br.
The Dispensatory Of The United States Of America
By Dr. Geo. B.Wood And Dr. Franklin Bache.
Thoroughly Revised, Largely Rewritten, And Based Upon The Eighth Decennial Revision Of The United States Pharmacopoeia Issued June 1, 1907.
Philadelphia And London
J.B. Lippincott Company