Cocaine’s Mechanism of Action

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.

Absorption

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

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

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.

Toxicity

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.