Cocaina Cocaine, U.S.P.

Erythroxylon Coca, Lamarck, and other species. An alkaloid obtained from the leaves.

Habitat. Peru, Bolivia, Ecuador--eastern slopes of the Andes (Colombia, Brazil, India, Ceylon, Javal); cultivated.

Syn. Erythroxylon, Spadic, Coca leaves, Cuca, Hayo, Ipado, Coca Folia; Fr. Feuilles de Coca; Ger. Kokablatter; Cocain, Methyl-benzoyl-ecgonine; Br. Cocaina; Fr. Cocaine; Ger. Cocainum, Kokaina.

Er-y-throx'y-lon. L. See Etymology, above, of Erythroxylaceae.

Co'ca. Sp. From native name, meaning tree or plant, par excellence.

Plant

Shrub 1-2 M. (3-6 degrees) high, with many spreading, purplieh, brown branches, wrinkled bark, smooth twigs; flowers small, yellow petals 5, stamens 10; fruit reddish drupe, oval, 12 Mm. (1/2') long, sarcocarp scanty. Leaves oval-elliptical, 2.5-7.5 Cm. (1-3') long, 2-4 Cm. (4/5-1 3/5') broad, greenish-brown or clear brown, smooth, slightly glossy and coriaceous, shortly petioled, base short and abruptly narrowed, entire, midrib prominent underneath, with conspicuous line of collenchyma tissue running longitudinally on either side, one-third the distance between it and the margin, the enclosed areola of slightly different color; odor characteristic; taste bitterish, faintly aromatic, followed by numbness of tongue, lips, and fauces; powder yellowish-green. Dose, gr. 15-60 (1-4 Gm.).

Adulterations

Leaves that are smudgy brown or with dull surface, also small jaborandi leaves, sometimes 40-50 p.c.; Inga and Pacay flowers by accident.

Commercial

Coca, although not introduced into England until 1870, was used in S. America prior to the Spanish conquest, 1569, by the aborigines, who extolled it as a God-given plant ("The Divine Plant of the Incas") that satisfied hunger, strengthened the weak, and banished man's misfortunes; but the invaders, intolerant of such homage, forbade its use and cultivation until they observed that it enabled the conquered to perform better work and service. Previous to 1884 the alleged properties were thought legendary and imaginative, when, being considered simply a mild stimulant like tea, Koeler proclaimed its local anesthetic power. Species differ when wild and under cultivation, and escaping this soon degenerate and show marked changes in leaf-characteristics. It is cultivated extensively in the Andes on terraced plantations, cocales, cleared from the forests on the warm declivities, thriving best in a moist atmosphere and amid scattered trees, but not deep shade, which, as well as low elevation, develops bitterness, consequently any variation in this or in the prescribed soil, exposure and curing may affect quality. Propagation is similar to our peach, yielding leaves the second year and continuing for fifty thereafter. Leaves when bright green above and yellow-green below are picked carefully to avoid breaking, or injuring young leaf-buds that form the next crop, removed in baskets, spread on unroofed floors, and dried quickly for a few hours in the sun, if too rapidly losing odor and green color, if too slowly acquiring disagreeable odor and taste; after remaining 2-3 days in the coca-house, in loose piles, they are exposed again for a short time to the sun, to drive off developed sweat, and then compressed into bales (cestos), 25-50 pounds; 11.6-23.3 Kg., or better, tin-lined boxes that prevent likely deterioration in shipping through fermentative decomposition. Irrespective of the care in drying and keeping impairment begins at once, cocaine decreasing materially, especially in dampness, owing to which they should be discarded after a few months. Although in some localities collection is almost continuous there are at least 2-3 yearly harvests, the September being best, the April next, each yielding when dried 60-80 pounds (27-37 Kg.) per acre; the annual production is about 80,000,000 pounds (37,383,177 Kg.), exported largely from Huanuco, Lima, Truxillo, etc. There are two varieties: 1, Huanuco (Cuzco--E. Coca, short-styled), after cities of S. Peru, has best aroma, most cocaine, and less isatrophyl-cocaine; grown mostly in Bolivia, S. Peru, thriving and yielding maximum product at 1,050-1,800 M. (3,500-6,000 degrees), in 18 degrees south, and inferior grades at lower elevations; the true Bolivian (E. Bolivia'num, long-styled) is prized most highly, has larger fruit, smaller leaves, and owing to home demand seldom is exported; 2, Truxillo (Trujillo--E. Truxillense, short-styled), leaves ovate-oblanceolate, 1.6-5 Cm. (2/3-2') long, one-half as broad, pale green, thin, brittle, usually much broken, smooth, shining, petiole short and stout, slight point at apex, entire, the two collenchyma lines underneath frequently incomplete or obsure; odor more tea-like than preceding; taste and numbing effect similar; powder pale green; grown more northward, thriving well at lower elevations and preferred by natives for chewing. Java and India coca (E. Coca, var. Sprucea'num, long-styled, styles exceeding stamens) seems identical with this variety but owing to inferiority is not exported.

Constituents

Cocaine (1860) .5-1 p.c., cinnamyl-cocaine, truxilline (truxil-cocaine, isatrophyl-cocaine, cocamine), CHON -- all three upon hydrolysis yielding ecgonine and methyl alcohol; pseudotropine, ecgonine, coca-tannic acid, wax, volatile oil, ash 8-10 p.c.; hygrine (volatile aromatic liquid) is doubted by some, while cocainidine, probably isomeric with cocaine, but weaker, has not yet been studied thoroughly.

Cocaina. Cocaine, CHON. -- This alkaloid, composed of methyl alcohol, benzoic acid, and ecgonine, into which it separates by heating with strong sulphuric acid, is obtained by moistening leaves with sodium hydroxide solution, treating with benzin (kerosene), from which the alkaloids and cocaine are precipitated (hygrine, etc., remaining in solution); cocaine may now be separated by filtering and expressing, and purified by crystallizing from alcohol.  It is in colorless crystals, white crystalline powder, odorless, permanent, soluble in water (600), hot water (270), alcohol 6.5), chloroform (.7), ether (3.5), olive oil (12), liquid petrolatum (30-50), very soluble in warm alcohol, melts at 97 degrees C. (207 degrees F.); forms salts (hydrochloride, nitrate, sulphate, etc.).  Dose, gr. 1/8-2 (.008-.13 Gm.).

Preparations

1.  Cocainae Hydrochloridum.  Cocaine Hydrochloride, CHONHCl.  (Syn., Cocain.  Hydrochl., Cocainum hydrochloricum, Cocaine Chloride, Cocainae Hydrochloras, Cocaine Hydrochlorate; Fr. Chlorhydrate de Cocaine; Ger. Cocainum hydrochloricum, Kokainhydrochlorid.)

Manufacture

Dissolve pure alkaloid, cocaine, in alcoholic solution of hydrochloric acid, and allow anhydrous salt to crystallize.  It is in colorless, transparent crystals, lustrous leaflets, white, crystalline powder, permanent, odorless, soluble in water (.4), alcohol (3.2), warm alcohol (2), chloroform (12.5), glycerin, insoluble in ether; aqueous solution (1 in 20) neutral, levorotatory; melts at 183-191 degrees C. (362-376 degrees F.), the higher point indicating greater purity.  Tests: 1.  Aqueous solution (1 in 20) + silver nitrate T.S. -- white precipitate, insoluble in nitric acid.  2.  Aqueous solution (1 in 50) 5 cc. + 5 drops of chromium trioxide solution (1 in 20) -- yellow precipitate, redissolved on shaking; now add hydrochloric acid 1 cc. -- permanent orange crystalline precipitate.  3. Dissolve .5 Gm. in sulphuric acid 1 cc. -- not more than slight yellow tint (abs. of readily caronizable substances) -- add cautiously distilled water 2 cc. -- aromatic odor of methyl benzoate, on cooling -- crystals of benzoic acid separate; incinerate .5 Gm. -- ash negligible.  4. Aqueous solution (1 in 50) 5 cc. + N/1 sulphuric acid .3 cc. + N/10 potassium permanganate .1 cc. -- violet color does not disappear entirely in half hour (abs. of cinnymyl-cocaine).  Impurities: Cinnamyl-cocaine, isatropyl-cocaine, readily carbonizable substances.  This salt is dispensed generally under the name of cocaine in (hypodermic) solutions, 2-4-5-10 p.c.  Dose, gr. 1/8-2 (.008-.13 Gm.).

Unoff. Preps.: I. LEAVES: Fluidextract (diluted alcohol), 3ss-2 (2-8 cc.).  Infusion, 5 p.c., 3j-2 (30-60 cc.).  Tincture, 20 pc. (diluted alcohol), 3j-4 (4-15 cc.).  Wine, 6.5 p.c., 3ij-4 (8-15 cc.).  II. COCAINE: Oleate, 5-10 p.c.  Unguentum Cocainae (Br.), 4 p.c.  III.  COCAINE HYDROCHLORIDE: Injectio Cocainae Hypodermica (Br.), 5 p.c., mv-10 (.3-.6 c.).  Lamellae Cocainae, Discs (Br.), 1/50 gr. (.0013 Gm.).

Properties

Cerebral stimulant, bitter tonic, diuretic, mydriatic, diaphoretic, anaphrodisiac, narcotic.  Locally, has little action upon the unbroken skin, but acts upon mucous membranes and subcutaneous tissue as anesthetic and analgesic, producing also its constitutional effects.  It increases digestion, respiration, heart action, temperature, arterial tension, and the irritability of the sensory nerves, followed by mental, moral, and muscular depression.  It anesthetizes the gastric mucous membrane, thereby temporarily deadening the sensations of hunger and thirst, which, however, seem all the greater as the effects wear off; the brain is stimulated by increasing the blood supply, producing wakefulness, a sense of hilarity and well-being (similar to cannabis), increased muscular strength and endurance.  Acts as a diuretic by checking waste processes, lessening the quantity of urea, but increases that of urine; dilates the pupil by stimulating the ends of sympathetic nerve in the iris.  When full amount (leaves) chewed one works cheerfully as long as the effect lasts, irrespective of meal hour, which may continue 3-4 days from repeated doses -- usually, however, food is taken at night, and only the meal of mid-day bridged over.  Natives drink its tea like Chinese tea elsewhere, and carry a bag of leaves and one of ashes or lime; after forming a quid of the leaves deprived of ribs (3j-4 Gm.), a little ash or lime is added to give pungency and to aid the secretion of saliva; each chew lasts an hour, when a new one follows.  Cocaine, in general action, resembles atropine; causes little injury to native, but strangers soon become haggard-looking and idiotic.

Uses

In melancholia, hysteria, epilepsy, spinal paralysis, insanity, diabetes, headache typhoid state, opium-habit, uterine inertia, vomiting of pregnancy, gastric irritability, cholera morbus, spermatorrhea, debiity, poisoning by chloral hydrate, opium, or bromides.  Locally, to burns, painful ulcers, fissures of anus, hay fever, sore throat, laryngitis, hemorrhoids, bronchitis, coryza, and in surgical operations; hypodermically in fingers, toes, small tumors--for amputation; for spinal anesthesia not as safe as novocaine, stovaine, eucaine; no more than gr. 3/4 (.045 Gm.) should be applied at once.

Poisoning

Have nervous excitement, oppression, and fullness of head, sometimes nausea and vomiting, pulse and respiration at first rapid, then slow, breathing labored, face cyanotic, pupils dilated, extremities cold, convulsions, coma, death; may have delirium and unconsciousness early, or only asphyxia.  Place in horizontal position and fresh air, empty stomach, stimulants -- strong coffee, etc., and if circulation fails -- strychnine, ether, alcohol, amyl nitrite, caffeine, atropine, oxygen and ammonia inhalations; chloral hydrate (gr. 30-60 (2-4 Gm.), paraldehyde, sulphonal, chloroform, ether or morphine injections; artificial respiration; nitroglycerin (hypodermically) for convulsions.  Chronic poisoning (cocainism or habit), marked by loss of flesh, disordered circulation, insane delusions and hallucinations, collapse, is more rapid and nearly as degenerative and serious as that of opium, and may be treated similarly, but usage does not create nerve irritation to the same extent, consequently one with strong will power may desist abruptly its use without suffering other than the denial of mental satisfaction and pleasures, the craving for which it tends to establish.

Incompatibles

Alkalies, alkaline carbonates and bicarbonates, mercuric chloride, iodine, iodides, ammonia, zonc chloride, borax.

Synergists

Cerebral effects -- alcohol, cannabis, belladonna; analgesic--atropine, phenol, conium, opium; mydriatic--atropine.