Plasma Cocaine Metabolite Levels and Liver CYP450 3A4 Isoenzyme Activity as Indicators of Cocaine Metabolism in Rats Treated With Salako Supplements

Introduction

Cocaine (C₁₇H₂₁NO₄), classified as a stimulant, is described as being the most potent, powerfully addictive stimulant of natural origin. The leaves of the Coca plant (Erythroxylum coca) can be harvested several times a year. The alkaloid, cocaine, is extracted from the leaves of the Coca plant, which originates in South America, and to a lesser extent, in Africa, Indonesia and India (UNODC, 2010). Cocaine is one of the oldest known psychoactive substances. Coca use has been traced as far back as around 5000 B.C. wherein the leaves of the plant were continually chewed in the mouth. Pure cocaine was isolated in the 1880’s (National Institute on Drug Abuse, 2008). In the early 1900s, pure cocaine was the main active ingredient in numerous pharmaceutical and recreational formulations due to their properties that enhanced general activity and decreased fatigue.

Illicit cocaine from South America is produced normally as relatively pure hydrochloride salt (ranging from 80 – 95 percent) for export to the United States. Illicit cocaine is distributed ranging from a white crystalline powder (cocaine hydrochloride), to that of an off-white chunky material (“crack” or “rock” cocaine) (Drug Enforcement Agency, 2005). Street cocaine is usually adulterated with various substances such as mannitol, lactose and glucose, talc and flour. Due to the heat labile property of cocaine hydrochloride, the preferred method of introduction is usually via snorting or by dissolving in water and injected. Crack cocaine on the other hand is smoked (Drug Enforcement Agency 2005). Crack is the term given to the product formed with the processing of cocaine with ammonia or sodium bicarbonate and water.

Cocaine use varies widely with drug users and can range from occasional to repeated or compulsive use. The primary routes of cocaine administration are intranasal, intravenous (injection), inhalation and oral. Injecting the drug releases the drug directly into the bloodstream which increases the drug intensity. The duration of the euphoric effects produced by cocaine is dependent on the route of administration. The faster the absorption of cocaine, the more rapid and intense the high produced, but the shorter the duration of action. Toxic amounts of cocaine can be absorbed by any route of administration, which can have a wide range of effects which can include sudden death (Williams & Wasserberger 2006).