What is cocaine?

Cocaine is a powerfully addictive stimulant drug made from the leaves of the coca plant native to South America. It is an alkaloid with a tropane ester chemical structure and belongs of the family of drugs that stimulate the activity of brain and sympathetic peripheral nervous systems by enhancing neurotransmitter activity at catecholaminergic synapses.

Cocaine is produced mainly in Bolivia, Colombia, and Peru and smuggled primarily to North America and Europe. Cocaine was first isolated and synthesized in 1859 in Germany. Merck pharmaceutical produced only 0.75 pounds of cocaine in 1983 and this number was increased to 158,352 within in a year, in 1984. The number of cocaine users in the world in 2005 was estimated at 14.3 million which represents 0.3% of the 15- to 64-year-old population. Of these, 44% were in North America which can be translated to 6.4 million people with a prevalence of 2.2%.

Cocaine is legally available in the United States only as a 4% or 10% injectable solution (or powder for reconstitution) or viscous liquid for use as a local or topical anesthetic.

An estimated 530 to 710 metric tons of cocaine entered the United States in 2006 (USONDCP 2007). The average purity of cocaine was found to be 50% to 60% in the United States in 2007 (USDEA 2008).

Diluents (also called “cut”) such as dextrose, lactose, mannitol, starch, benzocaine, lidocaine, procaine, ephedrine, amphetamine, caffeine, benzene, acetone, allergy pills, or sodium bicarbonate or PCP are commonly added to cocaine in retail stage to increase the margin of profit (Shesser 1991). Stimulants also have been used to augment the response to standard antidepressants. (DeBattista 2006)

Cocaine along with caffeine and ephedra are naturally occurring plant alkaloids. It is believed that one out of every 5 person who uses cocaine regularly gets addicted to it.

Cocaine is taken by mouth, inhaled, injected into the veins, and smoked. In recent years, the number of cocaine users who smoke crack cocaine has increased. Cocaine stimulates the central nervous system (CNS) to produce an increase in energy and psychomotor activity; a heightened sense of sensory arousal, pleasure, and euphoria; and a decrease in appetite and the need for sleep. It affects judgment and behavior, as well.

How common is cocaine dependence?

Cocaine abuse and addiction represent a significant health problem in the United States (NIDA 1994). In recent years, this problem has increased, inflicting much harm on addicted individuals, their families, and society. Many individuals with cocaine problems have other substance use disorders, medical problems, psychiatric disorders, and psychosocial problems.

According to SAMHSA 2014 report:

  • 1.5 million (0.6%) people used cocaine (including crack).
  • People aged 18 to 25 were more than twice as likely to use cocaine compared with other adults.
  • Men (0.8%) were twice as likely to use cocaine compared with women (0.4%).


Potential benefits of cocaine

Why do people use cocaine?

Cocaine has two main pharmacological actions. It is both a local anesthetic and a central nervous system stimulant—the only drug known to possess both of these properties. The effects experienced in the early stages of cocaine use include a generalized state of euphoria in combination with feelings of increased energy, confidence, low appetite, mental alertness, and sexual arousal.

Stimulants have been used in medicine in the treatment of the following clinical conditions:

  1. Cocaine
    1. Local or topical anesthetic (Harper 2006).
    2. Brompton’s cocktail: a combination of cocaine, alcohol and opiate has been used in the treatment of cancer pain.
  2. Methamphetamine
    1. ADHD,
    2. Weight control
  3. Amphetamine (as d-isomer or racemic mixture)
    1. Amphetamines have been used to improve recovery after stroke, but their efficacy is questionable (Martinsson 2007)
    2. to counteract opiate-induced sedation and respiratory suppression, thus allowing larger doses of opiates to be used (Homsi 2000)
    3. ADHD,
    4. Narcolepsy
    5. weight control
    6. depression
  4. Methylphenidate (as d-isomer or racemic mixture)
    1. ADHD,
    2. Narcolepsy (Banerjee 2004; Morgenthaler 2007)
  5. Lisdexamfetamine (l-lysine-d-amphetamine
    1. For treatment of ADHD
  6. Benzphetamine
    1. Used for weight control
  7. Phenmetrazine
    1. Used for weight control
  8. Phenmetrazine
    1. Used for weight control


Nonmedical Use, Abuse, and Dependence

Stimulants, both prescription and OTC, have been widely used in workplace, school, military, truck drivers, and sports settings for their alerting, sleep-suppressing, and performance-enhancing properties (Svetlov 2007; Wilens 2008)

Both animal and human studies has demonstrated stimulants do increase aggressive and violent behavior to stimulant-induced irritability, paranoia, or frank psychosis (Licata 1993; Fukushima 1994)

Cocaine is commonly used with heroin (speedballing) to get a better high and enhance the acute psychological effects of cocaine (Foltin 1996) Cocaine users commonly use alcohol, benzodiazepines, opiates, and marijuana after cocaine to reduce anxiety, paranoia and restlessness effects of cocaine and/or to relieve symptoms of cocaine withdrawal. This is called “Up and Down”.

How is cocaine metabolized in body?

Absorption and Distribution

  1. Smoked:
    1. Stimulants are rapidly absorbed through the lungs and can reach the brain within 6 to 8 seconds.
    2. The onset of peak effects after smoking occurs within minutes of administration.
    3. Positron emission tomography (PET) studies with radiolabeled cocaine showed that intravenous administration produces peak brain uptake in 4 to 7 minutes (Telang 1999)
  2. Intranasal and oral use:
    1. Stimulants have a slower absorption and onset of effect (30 to 45 minutes), a longer peak effect, and a more gradual decline from peak.
    2. The peak intensity of effect is weaker than with smoked or intravenous administration because less active drug reaches its site of action in the brain.


Stimulants and their metabolites are largely eliminated in the urine. (Jenkins 1998) Benzoylecgonine is the cocaine metabolite found in highest concentration in urine for several days after cocaine use which is measured in Urine Drug Screening tests.

What are the potential risks related to regular cocaine use?

Physical, behavioral, and social problems are common among cocaine addicts and may include any of the following specific consequences:

Cocaine intoxication can present with a combination of some of the following symptoms:

  1. Increased energy, alertness, and sociability;
  2. Elation or euphoria; and
  3. decreased fatigue, need for sleep, and appetite (Romanelli 2006)
  4. Anxiety
  5. Irritability
  6. Panic attacks
  7. Interpersonal sensitivity
  8. Hypervigilance
  9. Suspiciousness
  10. Paranoia
  11. Grandiosity
  12. Impaired judgment
  13. Delusions and hallucinations
  14. Psychosis
  15. Hallucinations
  16. Tactile hallucinations (formication)
  17. Restlessnes
  18. Agitation
  19. Tremor
  20. Dyskinesia, and repetitive or stereotyped behaviors such as picking at the skin or foraging for drug
  21. Tachycardia
  22. Pupil dilation
  23. Diaphoresis
  24. Nausea

 Some of the chronic Effects of cocaine use:

  1. Cognitive impairment (Rogers 2001) such as visuomotor performance, attention, inhibitory control, and verbal memory.
  2. Reduced gray and white matter volumes in the frontal cortex of the brain
  3. Enlarged basal ganglia (Magalhaes 2005)
  4. Psychotic flashbacks have been reported in methamphetamine abusers up to 2 years after their last drug use and often are precipitated by threatening experiences (Yui 1998)
  5. Hemorrhagic stroke
  6. movement disorders as the result of increased dopamine activity in the basal ganglia and other brain areas that control movement (Warner 1993):
    1. Acute dystonic reactions,
    2. Choreoathetosis
    3. Akathisia (crack dancers)
    4. Buccolingual dyskinesias
    5. Exacerbation of Tourette’s syndrome and tardive dyskinesia.

 Withdrawal symptoms of the cocaine dependence can be:

  1. Depressed mood,
  2. Anhedonia
  3. Fatigue
  4. Difficulty concentrating,
  5. Increased total sleep and rapid eye movement sleep duration

 Cardiovascular System

  1. Increase heart rate, blood pressure, and systemic vascular resistance
  2. Myocardial infarction
  3. Cardiac arrhythmias
  4. Blockade of myocyte sodium channels
  5. Cardiomyopath
  6. Myocarditis

 Pulmonary effect of cocaine use:

  1. Acute and chronic pulmonary toxicity
  2. Cough
  3. Shortness of breath,
  4. Wheezing
  5. Chest pain
  6. Hemoptysis
  7. Exacerbation of asthma

 Effect of cocaine use in kidneys:

  1. Acute renal failure

 Gastrointestinal effects of cocaine use:

  1. Cocaine reduces gastric motility and delays gastric emptying
  2. Gastroduodenal ulceration and perforation,
  3. Intestinal infarction and perforation, and
  4. Ischemic colitis (Glauser 2007)
  5. Concealing cocaine by swallowing large packets (“body packing”) may result in severe acute toxicity if the wrapping deteriorates and allows cocaine into the gastrointestinal tract

 Effect of cocaine in Liver:

  1. Cocaine is hepatotoxic in rodents, but is no direct evidence that cocaine is hepatotoxic in humans.
  2. Liver abnormalities reported in case series of cocaine users can be accounted for by viral hepatitis from injection drug use, alcoholic liver disease, or other consequences of a drug-using lifestyle.

 Endocrine effects of cocaine use:

  1. Acute cocaine use activates the hypothalamic-pituitary-adrenal (HPA) axis, stimulating secretion of epinephrine, corticotropin-releasing hormone (CRH), ACTH, and cortisol (Mello 1997; Warner 1998)
  2. Decreases plasma prolactin concentrations in cocaine-naive individual

 Musculoskeletal effects of cocaine use:

  1. Rhabdomyolysis

 Head and Neck symptoms can be:

  1. Chronic rhinitis, perforated nasal septum and nasal collapse, oropharyngeal ulcers, and osteolytic sinusitis
  2. Gingival ulceration
  3. Dental enamel erosion
  4. Crack cocaine may cause corneal ulcers (Ghosheh 2007)

 Effect of cocaine use in immune system:

  1. Variety of vasculitic syndromes primarily affecting skin and muscle
  2. Henoch Schönlein purpura,
  3. Steven-Johnson syndrome, or
  4. Raynaud phenomenon.
  5. Wegener’s granulomatosis (Peikert 2008)

 Effect of cocaine use on sexual function:

  1. Stimulants are commonly thought of as an aphrodisiac, but chronic use usually impairs sexual function (Palha 2008)
  2. Men may experience erectile dysfunction or delayed or inhibited ejaculation.
  3. Priapism is rare.
  4. Women may develop irregular menses.

 Reproductive, Fetal, and Neonatal Health

  1. Prescription stimulants, including cocaine and amphetamines, are classified by the FDA in pregnancy category C, meaning that risk cannot be ruled out because human studies are lacking.
  2. vaginal bleeding,
  3. abruptio placenta,
  4. placenta previa,
  5. premature rupture of membranes,
  6. decreased head circumference,
  7. low birth weight, tremulousness,
  8. irritability
  9. poor feeding, and
  10. autonomic instability

What are the health risks related to using cocaine with other medications or substances?

Stimulant medications: Such interactions with medications that enhance catecholamine activity risk overstimulation of the sympathetic nervous system, with possible cardiac arrhythmia, hypertension, seizure, cardiovascular collapse, and death.

MAOIs: Prescription stimulants, such as amphetamine and methamphetamine, should not be used within 2 weeks of MAOI use.

TCAs: Stimulants should be used cautiously in conjunction with tricyclic antidepressants, many of which block presynaptic reuptake of catecholamines.

Alcohol: When cocaine is used in combination with alcohol, a new compound, cocaethylene is formed (Penningers 2002) which may contribute to more severe or longer-lasting toxic effects of cocaine.

What are the symptoms of cocaine addiction?

Although each client may evidence a unique pattern of cocaine addiction, he or she will manifest three or more of the symptoms listed below. These are based on the following criteria for substance dependency from DSM-IV of the American Psychiatric Association’s Diagnostic and Statistical Manual of Mental Disorders (American Psychiatric Association 1994, pp. 175-272).

  • Excessive or inappropriate use of cocaine (or other substances): For example, getting high on cocaine or other drugs or getting drunk on alcohol and not being able to fulfill obligations at home, at work, or with others; feeling as if cocaine or other substances are needed to fit in with others or function at work or at home; or driving under the influence of substances.
  • Preoccupation with getting or using chemicals: For example, living mainly to get high on cocaine, other drugs, and/or alcohol; making substance use too important in life; or being obsessed with using cocaine or other substances.
  • Change in one’s tolerance for addictive substances: For example, needing more cocaine or other substances to get high or getting high much more easily and by using less of the substance than was used in the past.
  • Having trouble reducing or abstaining from cocaine or other substance use: For example, not being able to control how much or how often one uses cocaine or other substances or using more cocaine or other substances than planned.
  • Withdrawal symptoms: For example, getting sick physically, including having the shakes, feeling nauseous, having gooseflesh, having a runny nose, etc., once one cuts down or stops using cocaine or other substances; or experiencing mental symptoms such as depression, anxiety, or agitation.
  • Using cocaine and other substances to avoid or stop withdrawal symptoms: For example, using cocaine or other substances to prevent withdrawal sickness or drinking or using drugs to stop withdrawal symptoms once they’ve started.
  • Using cocaine or other substances even though they cause problems in one’s life: For example, not taking a doctor’s, therapist’s, or other professional’s advice to stop using because of problems substances have caused in one’s life.
  • Giving up important activities or losing friendships because of cocaine or other substance use: For example, discontinuing participation in activities that once were important, giving up friends who don’t get high, losing friends because of how cocaine or other substance use affects relationships with others.
  • Stopping cocaine or other substance use for a period of time (days, weeks, or months), only to begin again: For example, promising to quit using cocaine or other substances only to begin getting high again or being unable to remain abstinent from cocaine or other drugs.
  • Getting into trouble because of cocaine or other substance use: For example, losing jobs or being unable to find a job, getting arrested or having other legal problems; sabotaging relationships or having trouble with family or friends, or having money problems
    because of cocaine or other substance use.

Is there any treatment currently available for cocaine dependence?


  • A review of 18 double-blind clinical trials found only three of studies with significant differences between the study regimen and placebo. Overall the review did not support the clinical use of antidepressants in the treatment of cocaine dependence.

Dopamine Agonists:

  • Three most studied dopamine agonists (Amantadine, bromocriptine and pergolide) from 17 randomized double-blind, placebo controlled studies found inconsistent results. (Soares et al 2010)

Dopamine Antagonists:

  • Antipsychotics such as Olanzapine, Risperidone, and Ecopipam have been tried in several studies. Their results suffer from poor compliance, high side effects and high subjective attrition. (Amato et al 2007; Grabowski 2004)


  • Disulfiram has been found promising in reducing quantity and frequency of use and reducing number of cocaine positive UDS. (Pani et al 2010; Sofuoglu 2006)


  • Is a GABAergic antiepileptic drug
  • Reduces the number of cocaine positive urines, so it might be an effective treatment but further studies are needed. (Sofuoglu 2006)


  • have been found to be superior to placebo in reducing cocaine use and its use in treatment of cocaine dependence has been supported. (Kenna 2007)


  • Propranolol is an Alpha Adrenergic Antagonist (alpha blocker)
  • When administered in dose of 100 mg/day have been found to reduce withdrawal symptoms and increase treatment retention among heavy cocaine users. (Kampman 2001; Kampman 2006)


  • Modafinil is an stimulant drug used in treatment of narcolepsy and excessive daytime sleepiness.
  • It may block cocaine-induced euphoria, enhance periods of abstinence and reduce total cocaine use. (Dackis 2003; Dackis 2005; Martinez-Raga 2008)

Cocaine recovery program

Because cocaine addiction is a disease that involves losing control of cocaine and other substance use, addicted individuals often enter treatment feeling demoralized and out of control. They enter a treatment program to help them regain control of their lives. Thus, treatment must provide a safe, structured environment through regular, frequent contact with the treatment staff.

Abstinence from all drugs is the primary goal of treatment in the treatment protocol. Changing one’s lifestyle, solving problems, and improving coping skills are additional goals that help support the overall goal of abstaining from cocaine or other substances.

Detoxification and Stabilization: 

The first step in treating cocaine addiction is detoxifying the client from cocaine and other addictive drugs. Immediately upon entering treatment, the client participates in a brief stabilization phase designed to detoxify him or her from addictive drugs, to assess psychosocial
stability, and/or to begin to establish basic recovery supports. The group counselor works with the client throughout the stabilization period. The goals of the stabilization phase of treatment are to:

  • Help the client establish abstinence from cocaine and other drugs.
  • Help the client become motivated to participate in ongoing treatment sessions.
  • Assess the client’s psychosocial stability, i.e., whether he or she lacks a stable, drug-free living environment or has significant psychopathology that may interfere with his or her benefiting from the cocaine recovery program.
  • Provide education and support to help the client increase his or her knowledge of cocaine addiction and recovery and encourage him or her to engage in treatment and the recovery processes.

This phase of treatment lasts up to 2 weeks. Some clients complete detoxification from cocaine use before they start group treatment. Others continue to use cocaine or other substances even though they have started treatment. In such cases, treatment aims to help them focus on strategies to initiate abstinence. Not all clients begin the treatment program with the same level of motivation or become substance free before attending actual treatment sessions.

Brief, frequent contact with a counselor is helpful for the cocaine addict attempting to detoxify and stabilize on an outpatient basis. Of course, some clients with severe addiction problems are best detoxified in a hospital or addiction rehabilitation program and may enter outpatient treatment following an inpatient stay. Others enter outpatient treatment after completing a brief residential addiction program.

During the detoxification and stabilization phase, the group counselor sees the client 2 to 5 days each week. Clients typically attend treatment sessions two to three times a week. Clients may attend as many as five sessions of treatment a week if they are detoxifying from alcohol or another substance in addition to cocaine, or if they express a need for additional support. Each stabilization visit lasts 10 to 30 minutes.

What is the purpose of counseling and psychotherapy?

Group treatment sessions are a vital aspect of recovery from cocaine addiction. Groups give clients the opportunity to learn the facts about cocaine addiction and recovery so that they can better understand their drug use problems. Clients also gain strength and hope from each other, learn to use and benefit from social support, and begin to feel valued because they are helping others who are trying to recover from cocaine addiction. Although specific group sessions vary in content and focus during Phase I (weeks 1-12) and II (weeks 13- 24), the general purpose of group treatment is to provide members with an opportunity to:

1) Acquire information about important concepts and aspects of recovery from addiction to cocaine or other substances. This includes but is not limited to information on—

  • Symptoms of addiction dependence and withdrawal
  • Factors contributing to addiction
  • The recovery process
  • Biopsychosocial issues in recovery
  • Phases of recovery and common problems experienced in
    each phase
  • Cocaine and other drug cravings
  • Social pressures to use substances
  • People, places, events, and things that trigger substance use
  • Effects of cocaine addiction on family and other relationships
  • Self-help groups
  • Support systems
  • How to cope with feelings
  • Guilt and shame
  • Relapse risk factors
  • Relapse warning signs
  • Tools for use in ongoing recovery

2) Learn recovery coping skills to deal with problems that contribute to or result from the addiction, to reduce the chances of a relapse to cocaine addiction and to improve functioning. These coping skills include cognitive, behavioral, and interpersonal skills that can be used to manage the various challenges of recovery.

Important note

This document is prepared by Dr Siavash Jafari, MD, MHSc, FRCPC, ABAM. This document is provided for information purposes only and does not necessarily represent endorsement by or an official position of the Essentials of Medicine. Advice on the treatment or care of an individual patient should be obtained through consultation with a physician who has examined that patient or is familiar with that patient’s medical history.


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