Cocaethylene toxicity

Information processing was tested with an infant-controlled habituation procedure. At 8 months, cocaine-exposed infants and controls had no differences in cognitive functioning. Their abilities to process information indexed by habituation and response to novelty were comparable.

In case of the 13-year-old girl, CE increased from an average baseline of 0.6ng/mg to 1.8ng/mg 12 months before death, a small peak of 2.6ng/mg 6 months before death, and to 8.4ng/mg in the weeks immediately before death. The high CE/COC ratio of 0.53 in the last 1.5 months before death suggests extensive alcohol intake coupled with frequent coca chewing. On the other hand, CE/COC in the lower range should show that alcohol was present only occasionally or in low concentrations during cocaine use. Cocaine also is a local anesthetic agent, slowing nerve impulses from neuronal pain fibers by blocking the inward movement of sodium across cell membranes . Sodium channel blockade across myocardial cells, similar to the class IA antidysrhythmics, is responsible for the occasional conduction abnormality that is noted in patients with acute cocaine toxicity. Predicting violence among cocaine, cannabis, and alcohol treatment clients.Addictive behaviors,33, 201–205.

  • The chief degradation of cocaine occurs via the catalytic properties of human carboxylesterase 1 which hydrolyzes the methyl ester linkage on cocaine to form benzoylecgonine and methanol.
  • It is thought to be more harmful than cocaine because it stays in the body longer.
  • Also the onset and intensity of the “rush” were indistinguishable by the subjects for cocaine and CE.
  • The half-life of cocaethylene in plasma, or the liquid portion of blood, is abouttwo hours.

According to the Journal of Medical Toxicology, this unique substance is created as alcohol and cocaine are metabolized in the liver. Alcohol disrupts the metabolism of cocaine so instead of being filtered out of the body, about 20 percent of the drug remains. After about two hours, the remaining alcohol and cocaine will cause a chemical reaction in the liver. This creates the toxin known as cocaethylene which has a myriad of negative effects on the body. Purification and characterization of a human liver cocaine carboxylesterase that catalyzes the production of benzoylecgonine and the formation of cocaethylene from alcohol and cocaine.

Nowadays, additive/synergistic activities of parent/metabolites at hERG/QT/TdP can be assessed using in vitro/in vivo assays. The spectrophotometric competitive inhibition assay used here represents an effective method to identify drug or environmental esters metabolized by carboxylesterases like hCE-1. Google AnalyticsGoogle Analytics helps us analyze and improve the user behavior of our website to provide you with the best possible user experience. By submitting this form you agree to the terms of use and privacy policy of the website. Cocaine also causes changes to other brain chemicals like norepinephrine and serotonin. Cocaethylene can raise the risk of stroke even more because it can stay around in the body for days to weeks.

Catalytic activities of cocaine hydrolases against the most toxic cocaine metabolite norcocaethylene.

In 1885, cocaethylene was first synthesized , and in 1979, cocaethylene’s side effects were discovered. We publish material that is researched, cited, edited and reviewed by licensed medical professionals. The information we provide is not intended to be a substitute for professional medical advice, diagnosis or treatment. It should not be used in place of the advice of your physician or other qualified healthcare provider.

The adult brain contains a small population of neural stem cells that help to repair and maintain cerebral tissue . Adult mammals experience neurogenesis to a limited extent over the course of their lifetime . In a study of mice, the long-term exposure of animals to ethanol and cocaine induced pathological changes in the brain and neurodegeneration . Ethanol decreased the amount of benzoylecgonine excreted in the urine by 48%. In this study, subjects reported that the combination of cocaine plus ethanol was more intoxicating and pleasurable than either agent alone . The cocaine and cocaethylene molecules are structurally and chemically similar.

The plasma elimination half-life of CE is ~2 h compared with ~1 h for cocaine. The concentrations of CE in blood after drinking alcohol and taking cocaine are difficult to predict and will depend on the timing of administration and the amounts of the two precursor drugs ingested. After an acute single dose of cocaine and ethanol, the concentration–time profile of CE runs on a lower level to that of cocaine, although CE is detectable in blood for several hours longer.

It is essentially a high that the body produces as ethyl alcohol interferes with the body’s efforts to stop cocaine from circulating in the bloodstream. Euphoric feelings are even more powerful than cocaine and will last longer. There hasn’t been enough studies to back up the theory but some researchers do believe there is a correlation between alcohol and cocaine use for the sake of producing cocaethylene effects.

Alyssa who is the National Director of Digital Marketing, joined the Banyan team in 2016, bringing her five-plus years of experience. She has produced a multitude of integrated campaigns and events in the behavioral health and addictions field. Through strategic marketing campaign concepts, Alyssa has established Banyan as an industry leader and a national household eco sober house boston name. Depending on how the drug is tested can determine the duration of the substance’s stay in the system. For example, cocaethylene can be tested in the hair for up to ninety days after the last use. Additionally, urine tests can detect the chemical a week after use and, if tested in the blood, this can be seen for up to ten hours after the last use.

Why Do People Combine Alcohol and Cocaine?

Like its parent drug, cocaethylene blocks the reuptake of dopamine and increases post-synaptic neuronal activity; the parent drug may also block reuptake of serotonin as well. Cocaethylene has been studied in animal models in terms of its pharmacology and its potential neurological effects. Most cardiac-related risk assessment tools do not ask about cocaine use, which can prevent clinicians from making optimal therapeutic choices. Greater awareness of cocaethylene is needed for clinicians, and those who use cocaine should also be aware of the potential for polysubstance use of cocaine and ethanol to produce a potentially potent and long-lasting psychoactive metabolite. Using alcohol and cocaine simultaneously causes a third drug to form.

Cocaine users may feel that alcohol prolongs or enhances their “high” without knowing exactly why. In fact, greater education is needed for patients, their families, and illicit drug users. Patients should be informed about the risks of using cocaine and ethanol at the same time. The longer half-life of cocaethylene may allow some to overdose on cocaine, not realizing that the cocaethylene metabolite was still active. When cocaethylene is produced in the liver, it’s important to understand that it’s actually more toxic than cocaine. Studies have found that cocaethylene toxicity is 30% more than cocaine.

These include withdrawal symptoms, the possibility of relapsing, and persistent feelings of shame and guilt. The liver is responsible for eliminating waste chemicals from the bloodstream. This organ processes them before they are excreted from the body through sweat or urine. It can get worn out by an unhealthy lifestyle or by an overwhelming presence of toxic chemicals. If the metabolic process is disrupted, the toxins fester and eventually spread throughout the body. Data from this study have shown for the first time that COC and its metabolites BZE and EME are evenly distributed between plasma and whole blood following controlled single dose intranasal cocaine administration.


When controlled for the effects of marijuana, alcohol, and tobacco use, the use of cocaine in the third trimester was negatively related to state regulation, attention, and responsiveness among the exposed infants. Twice as many cocaine-exposed infants as controls failed to come to and maintain the quiet alert state required for orientation testing. Whenever a person consumes any substance, there are a number of waste products, and some substances can build up in the system and be harmful. When certain harmful substances and/or waste products accrue in the bloodstream, they are processed through the liver where the natural process of metabolism breaks them down so they can be eliminated from the body, typically through urine. Cocaethylene, as well as the substances involved in its production, is very addictive. This can result in dependency and other psychological issues that require extensive treatment and intervention methods.

Cocaine and alcohol effects that cause cocaethylene to be produced will cause you to be more impulsive. This can include violence, unprotected sex, or taking whatever drugs are available around you. Cocaethylene toxicity can lead to liver damage more than if cocaine and alcohol abused separately. When someone uses these substances at the same time, they are more likely to drink too much alcohol or use too much cocaine. The typical pattern is of someone who starts drinking, and then gets a craving for cocaine.

Cognitive effects

Taking cocaine on its own causes a rush of energy, a high or feelings of euphoria. Although alcohol usuallyslows the body down, taking cocaine and alcohol together can make the effects and risks of cocaine more severe. The risk of dying when you combine alcohol and coke is 20 times higher than it if you just use cocaine alone. Not only can cocaethylene be produced when you use alcohol and coke only once together, but it also has the potential to build up in the body over time. Medically Reviewed By Dr. Sarah Dash, PHDA licensed behavioral health or medical professional on The Recovery Village Editorial Team has analyzed and confirmed every statistic, study and medical claim on this page.

  • However, the oxygen demands of the body remain the same and the body has to compensate with a reflex mechanism that elevates the heart rate and maintains adequate blood flow to all the tissues.
  • Even if a patient is forthcoming about the quantity and timing of taking cocaine, the effects of the drug may be significantly prolonged when alcohol is involved.
  • The amount of cocaine converted to CE depended on the route of administration, being 34 ± 20% , 24 ± 11% (i.v.) and 18 ± 11% .
  • The two main carboxylesterase enzymes in humans are carboxylesterase 1 and 2 mostly localized in the liver.
  • Extensive treatment will be required in more serious life-threatening situations.

Often, it is only when someone attempts to quit that they realize they have a problem. Users take these substances together as it intensifies the effects of both substances, meaning that they get a greater high. Unfortunately, this also causes them to experience a greater comedown following use. When users take both of these substances consistently over a period of time, the dependence can be greater than if a user only uses cocaine or only drinks alcohol.

Greater Effects of Alcohol and Cocaine

Good rehabs will provide you with MAT , which is medication that means that you will be as safe and comfortable as possible while you are going through the withdrawal process. Cocaethylene is the name for the chemical compound that forms when cocaine is combined with alcohol. It is thought to be more harmful than cocaine because it stays in the body longer. Cocaethylene also has a stronger effect on the heart and nervous system, which leads to an increased risk of heart attack, stroke, and seizure.

When people mix cocaine and alcohol, cocaethylene can stay around for days to even weeks in the body. How your liver, pancreas, and kidney are working also play into duration time. First, alcohol promotes the vasodilation of peripheral blood vessels which is the primary cause of the warm flushing feeling a person experiences when they have ingested ethanol. A dilation of blood vessels causes an increase in blood delivery whilst decreasing the resistance the blood has to encounter when being pumped across a vessel wall. This decrease in resistance essentially lowers the force by which the heart has to pump and thus decreases the blood pressure.

Cocaethylene, also known as ethylbenzoylecgonine, is an active metabolite of cocaine formed in the liver when the illicit drug cocaine is consumed along with alcohol. The rise of cocaethylene and cocaine increases heart and liver toxicity. The biggest danger of using both are sudden heart-related problems, such as a heart attack or change in heart rhythms. Cocaine, on the other hand, can be metabolized by any one of three esterase enzymes into water soluble metabolites. Intestinal carboxylesterase and serum butyrylcholinesterase hydrolyze the benzoyl ester linkage of cocaine, but these two metabolic pathways are relatively insignificant.


Further research should be implemented to know if abusers of both substances are doing so in order to obtain the cocaethylene production in the body. Cocaine withdrawal can be quite intense and alcohol withdrawal can cause dangerous side effects. As detox becomes more complex when you have two substance to quit, it’s suggested that you do inpatient alcohol rehabilitation for a successful recovery. While many cocaine users take ethanol together with cocaine, few understand that it produces a new potent metabolite in the body that has a longer half-life and potentially more dangerous cardiotoxic effects.

Clinicians may be unaware that the concurrent consumption of ethanol and cocaine may result in prolonged cocaine-like effects and may be more cardiotoxic than if the drugs are not taken at the same time. Greater study is needed about the effects and metabolic pathways of cocaethylene in the body. Cocaethylene is the byproduct of concurrent consumption of alcohol and cocaine as metabolized by the liver. Normally, metabolism of cocaine produces two primarily biologically inactive metabolites—benzoylecgonine and ecgonine methyl ester. The hepatic enzyme carboxylesterase is an important part of cocaine’s metabolism because it acts as a catalyst for the hydrolysis of cocaine in the liver, which produces these inactive metabolites.

Human liver carboxylesterase hCE-1: binding specificity for cocaine, heroin, and their metabolites and analogs.

Other medications to treat cocaine dependence are being used off-label with limited success. A recent study of cocaine use data from 2011 to 2015 found people who reported heavy alcohol use in the past month had higher rates of weekly cocaine use. One reason people use alcohol and cocaine together might be because they believe alcohol can curb the withdrawal and anxiety when cocaine’s effects start to wear off. The ability of hCE1 to catalyze the trans-esterification reaction of ethanol and the methyl ester on cocaine seems like a difficult case to make.

The presence of cocaethylene in the body carries an 18- to 25-fold increase over cocaine alone for immediate death. Thecocaethylene half lifeis three to five times longer than cocaine alone. In a brain analysis, it showed that cocaethylene and cocaine produce the same euphoric effects. This would indicate that the dependency on cocaine occurs just as much with a drug our body creates. Cocaethylene effects are actually more intense and also more dangerous than cocaine as they are enhanced and last longer. When you arrive for cocaethylene treatment, you will be detoxed from both cocaine and alcohol.

However, a mechanism has been proposed that would explain ethanol’s ability to still attack the acyl-enzyme intermediate based on the presence of what is known as a of residues kitty-corner to the bottom of the active site. Second, alcohol also inhibits the secretion of vasopressin from the anterior pituitary gland. Vasopressin is responsible for preventing water loss by promoting re-absorption in the collecting duct of the nephron in the kidneys. Thus, alcohol’s inhibition of vasopressin causes a loss of water, which in turn causes a drop in blood pressure because the heart has to do less work to move less volume in the cardiovascular system. However, the oxygen demands of the body remain the same and the body has to compensate with a reflex mechanism that elevates the heart rate and maintains adequate blood flow to all the tissues.

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