Constituents. - Cocaine (1860) .5-1 p. c., cinnamyl-cocaine, trux-illine (truxil-cocaine, isatropyl-cocaine, cocamine), C19H23NO4 - all three upon hydrolysis yielding ecgonine and methyl alcohol; 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, C17H21NO4. - This alkaloid, consisting 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, as salts, can be transferred to diluted sulphuric acid by agitation; upon adding excess of sodium hydroxide solution the lesser 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 large, colorless, 4-6-sided monoclinic prisms, white crystalline powder, odorless, soluble in water (600), hot water (270), alcohol (6.5), chloroform (.7), ether (3.5), olive oil (12), very soluble in warm alcohol, slightly in liquid petrolatum, melts at 97° C. (207° F.); forms salts (hydrochloride, nitrate, sulphate, etc.). Should be kept dark, in well-closed containers. Dose, gr. 1/8-2 (.008-.13 Gm.).
Preparations. - 1. Cocainae Hydrochloridum. Cocaine Hydrochloride, C17H21NO4.HCl. (Syn., Cocain. Hydrochl., Cocaine Chloride,
Cocainae Hydrochloras, Cocaine Hydrochlorate; Fr. Chlorhydrate de Cocaine; Ger. Cocainum hydrochloridum, Kokainhydrochlorid.)
Manufacture: Dissolve pure alkaloid, cocaine, in alcoholic solution of hydrochloric acid, and allow anhydrous salt to crystallize. It is in colorless, transparent, monoclinic prisms, flaky, 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, laevorotatory; melts at 183-191° C. (362-376° F.), the higher point indicating greater purity. Tests: 1. Aqueous solution (1 in 100) + silver nitrate T. S. - white precipitate, insoluble in nitric acid. 2. Aqueous solution (1 in 50) 5 Ml. (Cc.) + 5 drops of chromium trioxide solution (1 in 20) - yellow precipitate, redissolved on shaking; now add hydrochloric acid 1 Ml. (Cc.) - permanent orange crystalline precipitate. 3. Dissolve .1 Gm. in sulphuric acid 1 Ml. (Cc.) - not more than slight yellow tint (abs. of readily carbonizable substances) - add cautiously distilled water 2 Ml. (Cc.) - aromatic odor of methyl benzoate, on cooling - crystals of benzoic acid, dissolved on adding alcohol; incinerate .5 Gm. - ash non-weighable. 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), dose, 5ss-2 (2-8 Ml. (Cc.)). Infusion, 5 p. c., dose, ℥ j-2 (30-60 Ml. (Cc.)). Tincture, 20 p. c. (diluted alcohol), dose, 3j-4 (4-15 Ml. (Cc.)). Wine, 6.5 p. c, dose, 3ij~4 (8-15 Ml. (Cc.)). II. Cocaine: Oleate, 5-10 p. c. Unguentum Cocainae (Br.), 4 p. c. III. Cocaine Hydrochloride: Injectio Cocainae Hypodermica (Br.), 5 p. c., dose, v-10 (.3-.6 Ml. (Cc.)). Lamellae Cocaina, 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 anaesthetic 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 anaesthetizes 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 natives, 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, spermatorrhoea, debility, poisoning by hydrated chloral, opium, or bromides. Locally, to burns, painful ulcers, fissures of anus, hay fever, sore throat, laryngitis, hemorrhoids, bronchitis, coryza, and in surgical operations. No more than gr. 3/4 (.045 Gm.) should be applied at once.
Poisoning: Have nervous excitement, oppression, and fulness 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; hydrated chloral (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 a 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.
Synergists: Cerebral effects - alcohol, cannabis, belladonna; analgesic - atropine, phenol, conium, opium; mydriatic - atropine.