Last reviewed by Dr. Manish Goyal on September 4th, 2018.
What is Cocaine?
Cocaine is a powerful stimulant of the central nervous system and often used as a recreational drug. It is also associated with addictive and psychoactive effects.
Cocaine occurs naturally as a chemical in the leaves of Erythroxylum coca or coca plant, native to South America. Cocaine is implicated as a local anesthetic in the form of topical preparations before surgical procedures involving the oral, laryngeal, or nasal cavities.
Presently, Cocaine is considered to be a Schedule II drug with high potential for abuse. The risk for abuse and severe local vasoconstriction associated with Cocaine prevents its widespread clinical uses but however, can be administered by a doctor under certain conditions. The drug acts as a stimulant by increasing levels of the neurotransmitter dopamine in brain that regulates pleasure and movement.
The drug is available under generic name Cocaine hydrochloride. It produces short-term effects such as intense feeling of well being and excitement, and energy besides its negative effects like raising heart rate and blood pressure.
History of Cocaine:
Coca leaves (Erythroxylon coca) have been used and abused for thousands of years for their stimulant effects. Cocaine was first isolated (extracted from coca leaves) by German chemist Albert Niemann in 1859. However, it became popular in the medicine only after 1880s.
Purified Cocaine was the main component in many tonics and elixirs in early 1900s that was used to treat a wide array of illnesses and was also used in the early formulations of Coca-Cola®.
Cocaine availability, forms and effects:
Cocaine is available in the form of white crystalline powder as a street drug and also known as Coke, Snow, Powder, or Blow. It is often diluted with non-psychoactive substances and other drugs like procaine or amphetamine and even combined with heroin (Speedball). The two main forms of Cocaine include the water-soluble hydrochloride salt and the water-insoluble Cocaine base (or freebase/Crack Cocaine).
The powdered form is either injected or snorted (inhaled through the nose) while the base form (with street name “crack” created by processing of the drug with ammonia or sodium bicarbonate (baking soda) and water, and then heating it to remove the hydrochloride to produce a smokable substance) is smoked.
The way of administration of Cocaine determines the intensity and duration of Cocaine’s pleasurable effects. Injecting or smoking the drug delivers it rapidly into the bloodstream and brain, producing a quicker and stronger effect than is the case with snorting.
Cocaine can affect the body in a wide variety including constriction of blood vessels, dilation of pupils, and increasing body temperature, heart rate, and blood pressure. It also results in headaches and gastrointestinal complications.
Besides, use of Cocaine also causes heart attacks or strokes, resulting in sudden death. Cocaine can also pose risk for contracting HIV in users due to impaired judgement and risky sexual behaviour due to Cocaine intoxication.
The administration mode also determines the type of undesirable effects. Regular inhalation of Cocaine can cause nosebleeds, loss of the sense of smell, problems with swallowing, and a chronically runny nose.
Cocaine ingestion results in severe bowel gangrene whereas injecting Cocaine may cause severe allergic reactions and increased risk for contracting HIV, hepatitis C, and other blood-borne diseases. Binge-patterned cocaine often results in irritability, restlessness, and anxiety. Users can also experience severe paranoia (characterized by auditory hallucinations).
Mechanism of action of Cocaine:
Cocaine hydrochloride is associated with central nervous systems (CNS) stimulating and local anesthetic activity. The mechanism of action through which Cocaine put forth local anesthetic effects is by inhibition of the excitation of nerve endings or blockage in peripheral nerves conduction.
This is achieved by reversible binding and inactivation of voltage gated sodium channels present in the neuronal cell membrane. Sodium influx through these channels plays important role in the depolarization of nerve cell membranes and subsequent propagation of nerve impulses.
Cocaine disrupts the initiation and conduction of nerve impulses and results in a reversible loss of sensation by stabilizing neuronal membranes. Cocaine is the only local anesthetic associated with vasoconstrictive properties owing to its ability to block norepinephrine reuptake in the autonomic nervous system.
Cocaine can bind differentially to the dopamine, serotonin, and norepinephrine neurotransmitters and directly prevents their re-uptake into pre-synaptic neurons.
This results in an accumulation of the respective neurotransmitters in the synaptic cleft and thereby increases postsynaptic receptor activation. Its effect on dopamine levels causes CNS stimulation and euphoria, and ultimately dependence.
Physico-Chemical properties of Cocaine:
- Cocaine is available as hydrochloride salt and the compound belongs to the class of organic compounds known as benzoic acid esters.
- Cocaine is an ester derivative of benzoic acid and an aromatic heteropolycyclic compound.
- It is a semi-synthetic drug and has a molecular formula C17H21NO4
- The molecular weight of Cocaine is 81388 g/mol.
- Chemically, Cocaine is known as methyl (1R,2R,3S,5S)-3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate.
- The melting point of Cocaine is 98 °C.
- It has a water solubility of 1800 mg/L (at 22 °C).
- The pKa of Cocaine is 8.61 (at 15 °C).
- Cocaine is solid, white, opaque, odourless, crystalline, bitter, powder (Cocaine powder).
- Pure Cocaine is slightly soluble in water; freely soluble in alcohol, in chloroform, and in ether. However, the salt of Cocaine i.e., Cocaine Hydrochloride is very soluble in water; freely soluble in alcohol; soluble in chloroform and in glycerin; insoluble in ether.
Biological properties of Cocaine:
- Cocaine is rapidly absorbed following smoking, snorting and intravenous administration.
- The bioavailability of Cocaine varies depending upon the way of administration and is 57% following snorting and ~70% following smoking.
- Peak concentrations are achieved within five to ten minutes after intravenous injection or smoking and within 60 minutes after snorting.
- Cocaine is 91% bound in plasma.
- A small amount of Cocaine is excreted unchanged in the urine, but the majority is extensively metabolized in liver to a variety of compounds including benzoylecgonine, ecgonine, norcocaine, and ecgonine methyl ester.
- The half-life for Cocaine is short, approximately 0.8 hours, while the half-life of benzoylecgonine is 6 hours.
Cocaine: tolerance and dependence
Cocaine is psychologically habit forming or addictive agent with prolonged and frequent use. Regular users of Cocaine can develop dependence and tolerance to it, i.e., they require larger amounts of Cocaine to get the same feeling or effect.
Dependence on cocaine can be psychological, physical, or both. People who are dependent on Cocaine feel the top priority of using the drug than to perform any other activity in their life. They feel strong desire for the drug and can’t stop using it.
It is characterized by an urge in people to use the drug in a particular surrounding and during gathering with friends. The symptoms of psychological dependence include a major change in a person’s personality, Cocaine being the top priority and other activities become neglected. The users become obsessed to always have enough Cocaine.
Physical dependence occurs when a person begins to rely on the use of drug to function properly. It is characterized by an intense desire for Cocaine, fatigue and an increased appetite.
Drug tolerance is described as a reduced drug’s effects, owing to its repeated or prolonged exposure. Higher amount of drug is required for experiencing the original drug effect in case of drug tolerance.
People develop initial tolerance to Cocaine with continuous heavy use of the drug and further become resistant for increasing amounts. However, regular users may encounter a ‘reverse tolerance’, characterized by more intense effects of the drug.
This is also known as Cocaine sensitization which can lead to life-threatening events including cardiac arrest, Cocaine overdose at very low dosages, respiratory failure.
Cocaine tolerance manifests itself as the increased need for more Cocaine for achieving euphoric effect. Pattern of Cocaine tolerance varies with individuals and also with time.
Individuals affected by a Cocaine tolerance may need to increase the drug dosage, as well as frequency of use, in order to attain the perceived desired effect which may ultimately lead to serious health consequences, and even sudden death.
Absorption and distribution of Cocaine:
Cocaine is absorbed by various routes with varying proportions depending upon the way of drug administration. After oral administration, Cocaine appears in blood after about 30 minutes, and reaches its maximum concentration in 50 to 90 minutes.
In acid medium, Cocaine gets ionised, and can’t reach cells. However, in alkaline medium, there is an increase in absorption due to less ionisation. In case of nasal administration, clinical effects manifest 3 minutes after drug administration that can last for 30 to 60 minutes with peak plasma concentration around 15 minutes.
Oral or intra-nasal routes result in 60 to 80% absorption of Cocaine. Inhalation can result in 20% to 60% absorption depending upon secondary vasoconstriction.
However, freebase does not undergo first-pass hepatic metabolism resulting in immediate rise in plasma concentrations to 1 to 2 mg per litre. The effects on the brain are very violent occurring very rapidly and lasting only 5 to 10 minutes. By the intravenous route, blood concentrations of Cocaine rise to a peak within a few minutes.
After being absorbed, Cocaine gets distributed within all body tissues, and crosses the blood brain barrier. Due to its lipid solubility, it gets accumulated in the central nervous system and in adipose tissue after large, repeated doses.
The volume of distribution of the drug varies between 1 to 3 litres per kilogram. Cocaine can also cross the placental membrane and accumulates in the fetus after repeated use.
Metabolism of Cocaine:
Cocaine is metabolized primarily by the hepatic system metabolism within 2 hours of drug administration. The rate of metabolism depends upon the concentration of the drug in the plasma. The metabolism of Cocaine can occur by various routes.
Basically, there are 3 different routes by which Cocaine gets bio-transformed. The major route involves Cocaine hydrolysis by hepatic and plasma esterases, resulting in loss of a benzoyl group and production of ecgonine methyl ester.
Esterase activity differs substantially from one individual to another. The secondary route is characterized by spontaneous hydrolysis of Cocaine non-enzymatically by demethylation, leading to production of benzoylecgonine.
The final degradation of Cocaine takes place after the principle and secondary routes of metabolism, and results in the production of ecgonine. A minor route of metabolism of Cocaine leads to norcocaine.
The principle metabolites of Cocaine metabolism thus includes benzoylecgonine, ecgonine methyl ester, and ecgonine which are inactive and norcocaine which is active and play an important role after acute intoxication.
Concomitant use of Cocaine with alcohol further produces another active metabolite, known as cocaethylene which is more toxic than Cocaine. The metabolism of Cocaine is also influenced and decreased by various factors including pregnancy, age, and diseased state like liver disease, and congenital choline esterase deficiency.
Elimination and excretion of Cocaine:
Upto 10% of administered Cocaine is eliminated unchanged in the urine. The metabolites of Cocaine namely ecgonine methyl ester, benzoylecgonine, and ecgonine are recovered in differing proportions depending on the route of administration.
Most of the drug is eliminated from plasma after 4 hours,, whereas metabolites can be present up to 144 hours after administration. Unchanged Cocaine is excreted in the stool and in also in saliva.
Withdrawal of Cocaine:
Withdrawal symptoms often appear whenever a person addicted to Cocaine abruptly ceases its use. The withdrawal symptoms include severe cravings for the drug, anxiety, lack of energy, and angry outbursts.
The symptoms can be physical or psychological. The physical withdrawal symptoms vary from individual to individual and last for relatively short length of time according to the severity of drug addiction.
However, the duration of psychological withdrawal symptoms occurs for a longer duration due to the person’s brain being trained to rely on the use of drug to get the feelings of pleasure.
The drug addicts to Cocaine also have to deal with social cues that encourage them to start the drug again and include the people and places where they have been taking the drug previously. People can get rid of the drug addiction by taking the help of professionals that comprise a doctor, hospital or rehabilitation center.
How long does Cocaine stay in your system?
Discontinuation of Cocaine is necessary for its clearance from the system. After its use is ceased, it remains in the system between 3.3 and 5.5 hours. However, the primary active metabolite of Cocaine known as “benzoylecgonine” remains for a considerably longer (between 1 and 2 days) time to get fully eliminated from the body.
This is attributed to the fact that upon Cocaine administration, approximately 40% is hydrolyzed to form “benzoylecgonine,” whereas remaining 40% is metabolized in liver to form “ecgonine methyl ester.”
Cocaine has a half life of 1 hour that causes its rapid elimination in comparison to benzoylecgonine, with a half life of 6 hours. There are many factors that contribute to the duration of Cocaine stay in the system and are outlined below:
The dosage of Cocaine determine the time of Cocaine stay in your system. People who consume a greater amount of Cocaine take longer time to get rid of Cocaine (and its active metabolite benzoylecgonine) from the body fully in comparison to the users who ingest an extremely low level of Cocaine and take lesser time for its removal.
Mode of administration:
The mode of Cocaine administration influence how long the Cocaine stays in your system. This is because certain modalities of uptake are associated with rapid absorption and a rapid shorter lasting high effect in comparison to others with a slower absorption and a longer-lasting high. The diverse modes of administration are associated with quicker elimination half-lives than others and are summarized as follows:
Intravenous injection (50 mg>): The elimination half life associated with intravenous injections of Cocaine is approximately 5 minutes and would be cleared from the body within 30 minutes.
Snorting cocaine (50 mg to 150 mg): Snorting cocaine leads to elimination half life of approximately 30 minutes.
Smoking “freebase” cocaine: The elimination half life of Cocaine in case of smoking is approximately 45 minutes and over 4 hours for the body to eliminate the drug.
Oral ingestion: The elimination half life associated with oral ingestion of Cocaine is 1 hour and would take approximately 5.5 hours to eliminate it from your body.
- Time Span: Long term users of Cocaine are associated with longer duration of Cocaine stay in the body in comparison to those who have used the drug for a shorter-time. This is due to the fact that the drug is stored within fatty tissues such as the liver and keeps on accumulating there with each successive usage. The long term users take considerably longer time for the body to fully detoxify from Cocaine due to slow release of the drug within the blood stream. However, short- term users can efficiently process Cocaine and clear it from their system due to consumption of smaller dosages of drug compared to long-term users and lesser amounts of Cocaine within their liver tissues.
- Frequency: Frequency of drug usage also plays a major role in determining clearance from the system. For a person who has used Cocaine many a times per year shows longer duration of Cocaine stay in the body in comparison to the one who has used Cocaine less frequently per year. Greater frequency of usage results in lesser efficiency of the body to clear the drug due to neurophysiological adaptations that slow the process of drug clearance. Besides, frequent, long-term users tend to accumulate and retain greater concentrations of Cocaine within various body tissues including the liver and often build up a tolerance to lower doses of the drug and end up administering larger doses resulting in extension of time of Cocaine stay.
- Cocaine purity: The greater purity of the drug is associated with the greater potency of its effect. The highly purified Cocaine would have larger amount of the active ingredient, and thus would stay or be retained within the body for a longer duration. However, the impure “diluted” Cocaine with lesser active ingredient would be quickly cleared from the body.
- Individual Factors: Drug elimination from the body may vary from person to person due to the individual’s variation. Person who have fast metabolism, take detoxification supplements, or who ingest a small amount of Cocaine per pound of bodyweight have a quicker rate of drug elimination. On the other hand, users with a slow metabolic process and taking a large amount of Cocaine per pound of bodyweight are associated with a slower rate of drug clearance. Besides these, other individuals factors that contribute to differential drug stay in the system include genetics, body size (weight and height), exercise, supplements, other drugs (especially alcohol), water intake, dietary intake, etc
- Concomitant use with alcohol: Co-administration of Cocaine with alcohol extends the clearance rate of metabolites from the body. Cocaine and alcohol together results in the formation of “cocaethylene,” which can take some extra time to eliminate from the body.
What is the average time for benzoylecgonine (active metabolite of Cocaine) stay in your system?
Most of the drug tests are based on the duration of “benzoylecgonine,” (active metabolite of Cocaine) stay in the system due to longer existence in comparison to Cocaine. Users who take a small amount of Cocaine show benzoylecgonine clearance from the body within 2 days.
However, in case of frequent Cocaine users (or those ingesting large dosages), benzoylecgonine clearance would take between 5 and 10 days. Besides, other factors like alcohol or drug consumption, healthy diet, and exercise may also result in quicker clearance of benzoylecgonine. Furthermore, staying hydrated by consuming plenty of water also help in the removal of benzoylecgonine.
Different types of drug tests to detect Cocaine
There are many different types of drug tests (or screenings) that can be used for the detection of recent Cocaine consumption by an individual. These tests include: saliva tests, urine tests, blood tests, and hair tests.
These tests find implication in detection of Cocaine metabolites within saliva within just 5-10 minutes of taking the drug. Saliva samples are capable of detecting Cocaine in your system till 2-4 days following complete cessation of Cocaine. This test is often employed by companies and is not often as accurate as urine tests or blood tests.
Urine tests can detect the administration of Cocaine within just several hours of ingestion (after 2 to 5 hours of use) till a period of 3 to 4 days. They can also determine whether an individual had used Cocaine within a 2-day span period. Urine testing is most popular for detecting Cocaine as it is painless, simple, easy and inexpensive.
The blood tests are among the most accurate ways to screen the body for Cocaine consumption or its active metabolite. They are also more specific. Blood tests are capable of detecting the presence of Cocaine within 5-6 hours of ingestion till around 5 to 7 days or even more.
Hair tests are considered best in determining whether someone has used Cocaine within the past several months. The drug shows its presence in hair after 5 to 7 days till around 80 to 90 days. However, new Cocaine users are not likely to be caught through a hair test as it often takes up to 7 days (a full week) for drug detection
A combination of saliva, urine, blood, and/or hair tests can be performed to arrive at a final conclusion regarding Cocaine uptake. A combination of these types of tests prevents inaccuracies.
An individual is considered positive for Cocaine test only with a presence of the active metabolite (benzoylecgonine) at level of 300 ng/mL (or greater).
How to detoxify Cocaine from your body?
Detoxification is the act of cleaning out those undesirable toxins from the body that can be detrimental as well as harmful to the health. Various methods can be utilized to get Cocaine out of your body and these involve the following:
- Rehydrate your body by drinking lots of water as water is a natural detox and can flush out the drug, toxins or unwanted items from the body in the form of sweat and urine.
- Use of detox drinks or pills can help to get rid of Cocaine from the body.
- Consumption of salads and fruits should be encouraged and avoid foods that are rich in caffeine, fat and sugar.
- Detoxification process can be enhanced by consuming foods that are rich in vitamin B.
- Steam bath can be taken to increase the rate of perspiration and hence rate of Cocaine removal from the body.
- Protein rich food or amino acid supplements should be encouraged.
- Lessening your stress can help in getting rid of the stress hormones such as cortisol (which can be detrimental to the health) and also leads to detoxification. Stress can be reduced by taking a massage that causes toxin release from the body, getting more sleep to keep body in peak health, medication or yoga.
- Eat green leafy vegetables such as kale, romaine, wheatgrass, seaweed, etc. These vegetables are rich in fiber and help to flush out your body and also provide anti-oxidants that boost your immune system.
- Consumption of rich sources of omega 3 fat including wild caught fish, avocados, and almonds help to suppress your cravings and also help with depression.
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