Smoked administration route cocaine

The high-dose transition is defined as a transition phase in which the individual suddenly increases the doses of stimulants or switches to smoking (e.g., cocaine crack ) or IV route of administration (Gawin and Ellinwood 1988). This change leads to a rapid escalation of plasma levels and intense euphoria (i.e.. rush) often with subsequent increase in dosing frequency. In its most severe form, the high-dose pattern is characterized by binges of... 

A two-compartment open linear model has been described for the pharmacokinetic profile of cocaine after intravenous administration.14 The distribution phase after cocaine administration is rapid and the elimination half-life estimated as 31 to 82 min.14 Cone9 fitted data to a two-compartment model with bolus input and first-order elimination for the intravenous and smoked routes. For the intranasal route, data were fitted to a two-compartment model with first-order absorption and first-order elimination. The average elimination half-life (tx 2 3) was 244 min after intravenous administration, 272 min after smoked administration, and 299 min after intranasal administration. 

Adverse effects of cocaine include constricted peripheral blood vessels, dilated pupils, and increased body temperature, heart rate, and blood pressure. Cocaine induces several immediate euphoric effects, such as hyperstimulation, reduced fatigue, and mental clarity, all of which depend on the administration route. The faster the absorption of cocaine, the more severe the effects. In contrast, faster absorption limits the duration of action. For example, the effect from snorting cocaine may last 15 to 30 minutes, whereas effects from smoking may last 5 to 10 minutes. Increased use can reduce the period of stimulation, as addicted humans may develop tolerance. In rare instances, sudden death may occur on the first use of cocaine or unexpectedly thereafter. 

Perez-Reyes et al.8 estimated that only 32% of a dose of cocaine base placed in a pipe is actually inhaled by the smoker. Cone9 compared the pharmacokinetics and pharmacodynamics of cocaine by the intravenous, intranasal, and smoked routes of administration in the same subjects. Venous plasma cocaine concentrations peaked within 5 min by the intravenous and smoked routes. Estimated peak cocaine concentrations ranged from 98 to 349 ng/ml and 154 to 345 ng/ml after intravenous administration of 25-mg cocaine hydrochloride and 42-mg cocaine base by the smoked route, respectively. After dosing by the intranasal route (32 mg cocaine hydrochloride) estimated peak plasma cocaine concentrations ranged from 40 to 88 ng/ml after 0.39 to 0.85 h.9 In this study, the average bioavailability of cocaine was 70.1% by the smoked route and 93.7% by the intranasal route. Jenkins et al.10 described the correlation between pharmacological effects and plasma cocaine concentrations in seven volunteers after they had smoked 10 to 40 mg cocaine. The mean plasma... 

For recreational use, cocaine (hydrochloride salt) is often administered by nasal insufflation ( snorting ) or less frequently, intravenously. Cocaine is more volatile when converted from the salt to the freebase therefore freebase cocaine may be inhaled by smoking. This latter route of administration results in a rapid onset of action. It has gained increased popularity owing to the ready availabihty of the freebase cocaine form known as crack. Consequently the number of emergency room admissions related to cocaine toxicity has increased. 

Smoking is another fast route of administration. Its quick delivery may be why smoking can be such a seductive prospect for many users, whether the drug of choice is nicotine or crack cocaine. It is obvious that the potential for addiction is much greater when a highly addictive drug can be taken in convenient fashion. Many professionals consider the immediate reinforcement of intravenous injection and oral filtration a major contribut-... 

A number of reports in the mid to late 1980 s described patients who developed rhabdomyolysis while using cocaine [118-120]. Some of these patients experienced acute renal failure [121-125]. While the exact incidence of acute renal failure secondary to cocaine rhabdomyolysis is unknown, in one reported series it occurred in only three of 211 admissions for cocaine related complications [114]. On the other hand, in another series of nearly 40 patients the incidence of cocaine related acute rhabdomyolysis increased over the period of enrollment from 2 patients in 1985 to 22 patients in 1987 [126]. Several reports of patients with cocaine-induced rhabdomyolysis have clearly defined both the clinical syndrome and the risk factors for the development of acute renal failure and an adverse outcome [123, 126, 127]. Most patients have been previously healthy young males (mean age 30-35 years old and 80-85% male). The cocaine has been smoked, used intravenously, snorted, or taken orally implying that route of administration was not relevant [122,123,126, 127]. In contrast to narcotic related rhabdomyolysis, a history of prolonged coma or stupor is absent. On presentation, the majority of patients are combative and... 

Cocaine is active via nearly every possible route of administration however, insufflation of snow or coke represents one of the most popular routes. Administered in this manner, peak effects and plasma levels are achieved within 30 minutes (48). Smoking the freebase form of cocaine ( crack ) results in an even more rapid effect. The freebase form rather than the hydrochloride salt is used for smoking, because the temperatures required for vaporization of the salt result in considerable decomposition (48). Intravenously administered cocaine can achieve peak blood levels within a few minutes. Cocaine is metabolized to benzoylecgonine, the methyl ester of eegonine, and to a lesser extent, to eegonine, norcocaine, and hydroxylated derivatives. 

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