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Cocaine’s Mechanism of Action

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With cocaine remaining one of the most widely used addictive substances in America, there is still fairly limited information on exactly what it is that gives this substance such highly addictive qualities. Throughout this article, you will learn just how potent this powdery plant extract can be, why it has such an addictive grip on so many, and what happens to your brain and body when you use it.

As cocaine addiction takes over a person, the effects can be detrimental. The good news is, there is hope. At Guardian Recovery, we understand just how powerful addiction can be, but also how recovery is possible. We are dedicated to providing the highest quality of substance use treatment for you or a loved one that may be struggling. If this is you, call today to start your journey to freedom.

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Cocaine’s Properties & How It Works Chemically in the Body

The rapid onset and powerful feeling of euphoria are hallmarks of the experience many feel when ingesting cocaine. There are a few factors that play into why this experience is so powerful and addictive.


Depending on how cocaine is ingested (1) will determine how it is introduced into the bloodstream and the effects that are felt by the person using.  When ingested nasally, cocaine is absorbed through the mucous membranes located in the nasal and sinus cavities. It is quickly dispersed throughout the body and the effects are felt rapidly. Similarly, when smoked, cocaine is absorbed into the lungs and sent directly to the heart which quickly disburses the substance as well.


Metabolism is the body’s breaking down of substances into usable material when they enter the body. The rate at which you metabolize substances varies greatly due to a multitude of factors including age, weight, diet, and exercise. When speaking specifically of substances like cocaine, how quickly you are able to metabolize (2) a substance will determine how long this substance stays in your body and therefore, how long you experience its effects.


Half life (3) is the measure of the time it takes for half of a substance to be metabolized in the body. Cocaine has an extremely quick half life, usually somewhere between 30 and 90 minutes. The rapid nature at which the substance is used and filtered out of the body is one of the key factors in its powerful onset.


Cocaine toxicity (4) is a condition frequently treated in emergency rooms for those who have extreme negative effects when ingesting cocaine. Factors that can be at play include potency of the cocaine, length of use, chronic use, and preexisting conditions. Cocaine affects virtually every major organ in the body, but has the greatest impact on the cardiovascular system. This system is often most damaged when cocaine toxicity occurs. Similar to an overdose, the body becomes unable to function due to the stress placed on it by the substance ingested resulting in short or long term health issues.

Mechanism of Action in the Body

In a normally functioning brain (5), two neurons will send signals to each other by sending and absorbing various chemicals. Different chemicals send different signals and chemicals like dopamine play a key role in the body’s reward system. As cocaine is ingested, it interacts with this system by releasing extremely high amounts of this and other “feel good” chemicals to produce a euphoric sensation that the person using will want to seek out again.

Cocaine Blocks Monoamine Reuptake Transporters

In a naturally functioning brain, neurotransmitters like dopamine (5) are used for communicating from one neuron to another and then recycled into the body for later use. This process is called reuptake and limits the amount of dopamine and other chemicals at work in the body at one time. Along with releasing large amounts of these chemicals, cocaine is also responsible for blocking the mechanism responsible for reuptake. This causes unnatural levels of dopamine to be introduced into the brain as less of it is being reabsorbed.

Blockage of Sodium Ion Channels

Another effect that cocaine can have is anesthetic properties (6) when blocking Sodium Ion channels. When these channels are blocked it limits the brain’s ability to respond to pain in specific areas. It is for this reason that cocaine continues to remain a Schedule II substance with some potential medical benefits.

Pharmacodynamics of Cocaine

Cocaine has pharmacodynamic properties (3) of interacting with the brain and body to stimulate the central nervous system. Due to its chemical makeup, cocaine is classified as a stimulant. It possesses a multitude of complex mechanisms leading it to have anesthetic properties when used topically in contact with mucus membranes. This is due to its constriction of blood vessels and the blockage of sodium channels.

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Cocaine in Therapeutic Nasal Procedures

Due to its topical anesthetic properties (7) for nasal and sinus cavities, it is often preferred by surgeons while performing procedures on these areas. Though it is preferred, it is rarely used due to the potential danger in toxic reactions for patients. Safer alternatives that are more widely utilized include lidocaine (lignocaine) and tetracaine (pantocain) in combination with epinephrine (adrenaline), naphazoline or oxymetazoline.

The Effects of Cocaine on Myocardial Oxygen Demand

As cocaine is ingested, it directly affects the cardiovascular system, (8) specifically the amount of oxygen that allows for blood to circulate and flow properly. As oxygen availability is limited blood is not able to flow at proper levels resulting in potential fatal side effects.

Cocaine’s Mechanism of Action Creates Health Risks & Addiction

Among many of the intended effects that people using cocaine seek, a multitude of unwanted side effects come as an unintended consequence of use.

Dopamine & Reward System

One of dopamine’s primary roles (6) is communicating to your brain and body that a behavior needs to be repeated. This naturally is intended to occur during sex, after exercise, when smelling high calorie foods, etc. When cocaine is introduced and the brain is flooded with this potent neurotransmitter, it communicates a strong signal to the brain that this behavior needs to be replicated. This is the beginning of the addictive cycle that many find themselves in.

Vasoconstriction in Heart Attacks & Strokes

Aside from the mental side effects, cocaine is notorious for causing potentially deadly effects (4) on the body’s cardiovascular system. As blood vessels are constricted, blood flow and oxygen do not travel throughout the body as well. This causes the heart to have to overwork as well as important organs like the brain not having the necessary oxygen to function.

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Seeking Treatment for a Cocaine Use Disorder

As with any illegal drug, the potential for addiction is a reality that comes with its use. Many begin using occasionally but find that this casual use has turned into a life controlling struggle that they feel powerless to break free from. If this is your or someone you love, Guardian Recovery understands. Thousands have come through our doors with the very same feelings of hopelessness and discovered that they are not alone and true recovery is possible. Start your journey to freedom today by contacting Guardian Recovery.


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Reviewed professionally for accuracy by:

Ryan Soave


Ryan Soave brings deep experience as a Licensed Mental Health Counselor, certified trauma therapist, program developer, and research consultant for Huberman Lab at Stanford University Department of Neurobiology. Post-graduation from Wake Forest University, Ryan quickly discovered his acumen for the business world. After almost a decade of successful entrepreneurship and world traveling, he encountered a wave of personal and spiritual challenges; he felt a calling for something more. Ryan returned to school and completed his Master’s Degree in Mental Health Counseling. When he started working with those suffering from addiction and PTSD, he found his passion. He has never looked back.

Written by:

Cayla Clark

Cayla Clark

Cayla Clark grew up in Santa Barbara, CA and graduated from UCLA with a degree in playwriting. Since then she has been writing on addiction recovery and psychology full-time, and has found a home as part of the Guardian Recovery team.

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