Preparation And Routes Of Administration

Cocaine is the most potent stimulant of natural origin. It is a benzoyl-methylecgonine, an ester of benzoic acid and a nitrogen-containing base. Cocaine occurs naturally in the leaves of Erythroxylon coca and other species of Erythroxylon indigenous to Peru, Bolivia, Java, and Columbia. There are several basic routes to cocaine administration: chewing the leaves, cocaine sulfate (paste), cocaine hydrochloride, freebase cocaine, and crack cocaine. South American natives who chew coca leaves experience diminished hunger and fatigue, and an improved sense of well-being without evidence of chronic toxic-ity and dependence. However, other preparations and routes of administration of cocaine have a more rapid onset of action and are more problematic.

Cocaine sulfate (paste) is the intermediate form between the coca leaf and the finished cocaine hydrochloride crystal. The smoking of coca paste, popularly known as "pasta" or "bazooka," is prevalent in South America and also occurs in some parts of the United States. This results in a gray to white or dull brown powder, with a slightly sweet smell, that is 40-85% cocaine sulfate.

Cocaine hydrochloride is a stable, hydrophilic salt. Thus, it is frequently snorted (insufflation) or "tooted" in "lines" or "rails" about one-half to 2 inches long and one-eighth of an inch thick. Users pour the powdered cocaine onto a hard surface such as a mirror, glass, or slab of marble, and arrange it into lines with a razor blade, knife, or credit card. One line is snorted into each nostril via a rolled bill, straw, miniature coke spoon, or a specially grown fingernail. A single gram of cocaine produces about 30 lines averaging 10-35 mg of powder. The actual amount of cocaine hydrochloride present in each line depends on the purity of the drug. Absorption through the nasal mucosa is relatively modest due to a small surface area and the fact that cocaine is vasoconstrictive.

The bioavailability of intranasal cocaine is about 60%. Peak plasma levels occur over a range of 30-120 minutes (Barnett, Hawks, & Resnick, 1981). Cocaine is a topical anesthetic and causes numbness of the nose during snorting. Nasal congestion, with stuffiness and sneezing, may occur after snorting cocaine due to both vasoconstrictive properties and contaminants in the preparation. Users may flush out the inside of the nose with a saltwater mixture after a round of snorting, and they commonly employ decongestants and antihista-mines to relieve symptoms.

Cocaine can also be injected intravenously: "shooting" or "mainlining." The cocaine hydrochloride is mixed with water in a spoon or bottle cap to form a solution. Unlike heroin, cocaine hydrochloride may not need to be heated to enter solution. "Kicking" or "booting" refers to drawing blood from the vein back into the syringe and reinjecting it with each cocaine mixture. Injection drug users feel that this produces a heightened drug sensation or "rush," despite the lack of a pharmokinetic basis. Following intravenous administration, users achieve peak plasma levels almost instantaneously.

Freebase cocaine is obtained by extracting cocaine hydrochloride with an alkali, such as buffered ammonia, then mixing it with a solvent, which is usually ether. The solvent fraction is separated and volatilized, leaving very small amounts of residual freebase material. Cocaine freebase is most often smoked in a special freebase glass pipe with a small bowl, into which the freebase cocaine is placed, or in a water pipe with a fine stainless steel screen on which the cocaine is vaporized. Cigarettes are rarely used, because only a small amount of cigarette smoke actually enters the lungs, wasting valuable cocaine. Cocaine hydrochloride is soluble in water and has a melting point of 195°C. In contrast, cocaine freebase is lipid-soluble and has a vaporizing point of 98°C. Thus, cocaine freebase vapors can be smoked, readily crossing the blood-lung barrier

(DePetrillo, 1985), resulting in nearly immediate peak plasma levels that are achieved at a rate similar to that of injecting cocaine hydrochloride.

"Crack" or "rock" is cocaine that has been processed from cocaine hydrochloride to a freebase for smoking. To prepare crack cocaine for injection, the crack cocaine is dissolved in water or alcohol, either by heating the solution or by acidifying it. The resultant viscous solution, which is too thick for use in standard insulin syringes, requires a larger bore needle. Because these needles are considerably harder to obtain, the incidence of needle sharing, along with the risk of HIV infection, is greater.

In the United States, popular street names for cocaine include toot, snow, blow, flake, white lady, snowbirds, paradise, and white. Adulterants commonly found in illicitly purchased cocaine include inert substances such as talc, flour, cornstarch, and various sugars (lactose, inositol, sucrose, maltose, and man-nitol). Local anesthetics such as procaine, lidocaine, tetracaine, and benzocaine may be added to replace or enhance the local anesthetic effect of cocaine. Cheaper stimulants, including amphetamines, caffeine, methylphenidate, er-gotamine, aminophylline, and strychnine ("death hit"), may also be added to the preparation. Quinine may be added for taste, and other compounds such as thiamin, tyramine, sodium carbonate, magnesium silicate, magnesium sulfate, salicylamide, and arsenic (Lombard, Levin, & Weiner, 1989) may be found. Crack and cocaine are also used frequently in conjunction with tobacco cigarettes and cigars (bananas, coolies, geek joints), 3,4-methylenedioxymeth-amphetamine (MDMA; "bumping up"), heroin (snow balls, speed balls, smoking gun, dynamite), marijuana (woolas, lace, Sherman stick, champagne, caviar), and amphetamines (snow seals).

Contaminants may include bacteria, fungi, and viruses. Users frequently take cocaine in combination with other drugs, citing the need to take the edge off the abrupt effects and "crash" from cocaine. Intravenous injection of heroin and cocaine mixed together is called "speedballing," and ingesting alcohol in conjunction with cocaine may be referred to as "liquid lady." Any drug combination is possible, and other opioids and depressants, as well as hallucinogens, phencyclidine (PCP), and marijuana, are all frequently used in conjunction with cocaine.

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