Cocaine: So Tantalizing, Why Resist?
by Sarah Kim


Where does Coca-Cola get its name? Why was it created? In 1886, the Georgia pharmacist, John Pemberton, designed Coca-Cola as a headache remedy and a stimulant. The original beverage contained cocaine and was used both as an intoxicating beverage and a medically useful tonic. The effects of the drink helped make it popular. Only in the early twentieth century was the drug eliminated from the Coca-Cola recipe and replaced with increased amounts of caffeine.[1] 


Cocaine has a long history which also involves the once condoned use for medicinal purposes in the 1890's to being one of the most widespread abused drug today. Cocaine was the first effective local anesthetic for use in minor surgery. Before being used in medicine, the Inca civilization of Peru confined the use of coca to the royal classes and priesthood because the leaves were considered a symbol of divinity, a gift bestowed by the sun god. They clearly appreciated its pharmacological effects: deflecting fatigue and hunger, enhancing endurance, and promoting a sense of happiness.[1] Other civilizations gave cocaine to their slaves and workers instead of food and rest. "There is ample evidence that Indians under the influence of coca can withstand exceptional hardships and perform heavy labor, without requiring proper nourishment during that time....[By] using coca the Indians are able to travel on foot for hundreds of hours and run faster than horses without showing signs of fatigue."[11] What is cocaine? How does cocaine increase alertness and decrease one's appetite? It is all in the head, more accurately, in the brain. 


Cocaine is derived from the coca plant Erythroxylon coca in a white crystalline alkaloid powder. Cocaine affects the person by retarding the reuptake, or the reentry, of the neurotransmitter dopamine, a chemical that helps keep our thoughts and perceptions in accord with reality, into the Central Nervous System. Cocaine use results in both physiological and behavioral effects. The principal mental effects are alertness and euphoria, the suppression of appetite, and the alarming and dangerous psychosis. Cocaine enhances sensory power and increases energy when taken in small doses. Therefore, it makes the user energetic, talkative, contemplative, and sensitive to the sensations of sight, sound, smell, and touch. However, the affects are all temporary. Sigmund Freud, best known as the father of psychoanalysis, gives a first hand account of the effects of cocaine on him. "A few minutes after taking cocaine, one experiences a sudden exhilaration and feeling of lightness. One feels a certain furriness on the lips and palate, followed by a feeling of warmth in the same areas; if one now drinks cold water, it feels warm on the lips and cold in the throat. On other occasions the predominant feeling is a rather pleasant coolness in the mouth and throat."[11] If cocaine is taken in large doses, it may produce negative physical symptoms such as chest pain, nausea, blurred vision, fever, muscle spasms, convulsions, coma, and death. Death can occur from convulsions, heart failure, or the loss of vital brain centers which control respiration. Cocaine is an extremely strong reinforcer, an appetitive stimulus, thus, the potential for abuse is very high. Therefore, it is clearly not a drug that is to be taken for casual use. 


The basic mechanism that cocaine uses to produce its effects is by disrupting the neurotransmitters, or chemicals, in the brain. Cocaine blocks the reuptake of released chemicals such as dopamine, norepinephrine, and serotonin. Therefore, they accumulate in the synaptic cleft, a space between the presynaptic membrane and the postsynaptic membrane(synapse=junction between the terminal buttons of an axon and a membrane of another neuron), which multiplies the effect of the neurotransmitter. Cocaine is able to have such a drastic effect because it is able to permeate water and the human body is made mostly of water. 


Research has indicated that the chemical balance of chronic cocaine abusers is altered in such a way that decreases in dopamine result in physical cravings for more cocaine. Studies performed by Jay B. Justice of Emory University illustrate a "delayed effect of long-term cocaine administration."[2] The research involved 10 rats that were administered cocaine daily for 10 days. Upon termination of cocaine injections, the rats displayed no change. After 10 days however, Justice observed a 50 percent decrease in dopamine levels which shows the physical craving for the drug, proving cocaine addiction. 


Chronic cocaine users who have not used cocaine in one week or less showed approximately 30 percent fewer dopamine receptors relative to non-users. After one month off cocaine, however, research has showed that cocaine users had almost the same number of dopamine receptors as healthy individuals. Consequently, Nora D. Volkow along with the State University of New York at Stony Brook states that "the decrease in the number of dopamine receptors reflects the body's attempt to balance a system gone out of control." As dopamine floods synapses, postsynaptic receptors decrease in number to avoid "excess" stimulation. Therefore, the addiction to cocaine involves the craving for stimulation. When chronic users are deprived of cocaine, postsynaptic receptors are "temporarily starved" which explains why most relapses of abuse occur in the initial weeks of withdrawal. [3] When Freud went through withdrawal, he wrote, "During this first trial I experienced a short period of toxic effects, which did not recur in subsequent experiments. Breathing became slower and deeper and I felt tired and sleepy; I yawned frequently and felt somewhat dull." [11] 


Other researches at the Detroit Medical Center made other observations. The doctors observed that cocaine users may risk brain hemorrhages during the mid-fifties, which is approximately 20 years earlier than non-abusers of cocaine. Cocaine increases the heart rate which causes a rapid increase in blood pressure. This causes exhilaration and a feeling of lightness. However, the increase in pressure is so rapid that it may cause aneurysms which could further result in death. Of the cocaine abusers studied, patients were found to have either brain hemorrhages, ruptured aneurysms affecting the base of the brain, or a stroke. Of the 27 cocaine users Dr. Richard Fessler studied, nine were unable to move their arms, could not speak, could not comprehend speech, or had a facial droop on one side. Nevertheless, doctors are still unable to determine whether the subjects had previous brain abnormalities that may have emerged in later years or not at all, or whether the cocaine produced such a condition. [4] 


In addition, researchers in Hennepin County Medical Center in Minnesota have observed cerebral atrophy in chronic cocaine users. Researchers compared the brain scan of habitual users with moderated users and subsequently, observed a significantly greater rate of atrophy in the brain in heavy cocaine users. [5] 


Another effect of cocaine on the Central Nervous System (CNS) is that it stimulates the sympathetic nervous system, a part of the nervous system that acts upon many glands and involuntary muscles, and thus, accelerates heart rate. However, Stephen S. Hull of the University of Oklahoma discovered that cocaine appears to inhibit the parasympathetic nervous system, which is vital in the heart's ability to fluctuate in rate. Therefore, the heart cannot slow down and regulate the heart rate. By administering cocaine to 10 dogs, he observed that all subjects suffered from severe arrhythmia because of the effect of cocaine on blood pressure and heart rate. The rise of blood pressure signals the brain to stimulate the parasympathetic nervous system and subsequently lower the heart rate. Thus, Hull has proposed treatment for cocaine overdoses. He suggests electrical stimulation of the vagus nerve, the major nerve regulating heart function, to reach parasympathetic nerve fibers or heart-stabilizing drugs "just as if [cocaine overdosers] were heart attack patients. [6] 


Another detrimental effect of chronic cocaine abuse is abnormality in reproduction function. This includes impotence, gynecomastia, and high risk of abnormal pregnancies. Dr. Jack H. Mendelson, et al. measured the anterior pituitary, part of the pituitary gland which secretes hormones, in plasma samples from female patients recently hospitalized for cocaine abuse. In addition, Mendelson evaluated specific hormone (basal) levels for the duration of the hospitalization. Studies show an initial suppression of plasma prolactin levels, a hormone necessary for the production of milk, after "acute cocaine self-administration." However, plasma prolactin levels increased after continued withdrawal from cocaine. [7] 


The fundamental reason that there is such a widespread abuse of cocaine is because it is physically addictive. Furthermore, it has been experimentally concluded that in conditions of unlimited availability, self administration of cocaine will continue to escalate until physical exhaustion or overdose overcomes the subjects. Consequently, Dr. Nora D. Volkow has investigated changes in brain function associated with cocaine dependence and withdrawal to gain insight on the processes that lead to uncontrollable self administration of cocaine. [8] 


The neurological effects of prolonged cocaine abuse have been addressed. Therefore, the effect of cocaine abstinence must be addressed as well. Cocaine withdrawal involves three steps: the crash, withdrawal, and extinction. Studies by Dr. Sally L. Satel and associates illustrate the changes in dopaminergic function appearing after abrupt withdrawal from cocaine. Reports on cocaine withdrawal state that during detoxification, cocaine abusers feel fatigue, depression, agitation, diaphoresis, nausea, sleep disturbance, paranoia, and drug craving. In past studies, dysphoria and craving decreased linearly during the 28 days involved in the study. A "classic withdrawal pattern" was not observed in a Weddington et al study performed earlier. [9] 


The effects of cocaine are magnification of normal pleasures. The environment is intensified, but not distorted. This is one factor in cocaine addiction. The appetite for food is not enhanced. The National Institute of Drug Abuse estimates 10 to 15 percent of those who try cocaine become abusers. [10] As an individual's addiction to cocaine increases, dosage and duration increases. Consequently, there is an increase in binge frequency and duration. This phenomenon has been repeatedly illustrated in animal experiments involving self-administration of cocaine. Tests show that monkeys will continually self-administer cocaine until death and consistently choose cocaine over food regardless of any other stimulus. The mechanism of abuse of cocaine involves the electrical self-stimulation of neurotransmission in specific parts of the brain, therefore producing a reward-seeking behavior. 


The neurobiological effects of cocaine on the brain and nervous system have been studied in great depth. Researchers have concluded that the mechanism of cocaine is inhibition of dopamine reuptake resulting in continuous postsynaptic stimulation. Treatment for cocaine use and overdose have been addressed in many aspects as well. Some researchers believe cocaine overdosers should be treated as if they were heart attack victims. Furthermore, some researcher suggest cocaine antagonists that will decrease dopamine transport and thus reduce the effects of cocaine. Nevertheless, the effects of cocaine are both physical and psychological and detrimental in every aspect. The danger of cocaine is its addictive and abusive potential. Research has illustrated that cocaine produces an insatiable appetite for more cocaine. Consequently, cocaine has become one of the most widespread abused drug in the United States.