Cocaine

Cocaine

Cocaine 3D balls

Cocaine
INN
Drug class	Stimulant, Local anesthetic
Routes of administration	Topical, Oral, Insufflation, Intravenous, Smoking
Pregnancy category
Bioavailability	Oral: 33% Insufflated: 60–80% Nasal Spray: 25–43%
Metabolism	Liver (CYP3A4)
Elimination half-life
Excretion	Kidney
Legal status	Varies globally
CAS Number
PubChem
DrugBank
ChemSpider
KEGG

Cocaine is a powerful stimulant and local anesthetic derived from the coca plant. It is widely known for its illicit use due to its euphoric effects, but also has limited medical applications in anesthesia. Cocaine can be snorted, injected, smoked, or applied topically, each method affecting the onset and intensity of its effects.

History and Origin

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Leaves of the Coca plant, the source of Cocaine

Cocaine is derived from the leaves of the Erythroxylum coca plant, which is native to South America. Indigenous Andean cultures have chewed coca leaves for centuries to combat fatigue, hunger, and altitude sickness.

During the 19th century, cocaine was isolated and became widely used in medicine, beverages, and tonics. It was an active ingredient in the original formula of Coca-Cola, contributing to the brand's name.

Medical use of cocaine peaked in the early 20th century, but its addictive properties led to global regulation. Today, it remains a Schedule II controlled substance in the United States, allowing limited medical use as a local anesthetic.

Effects and Mechanism of Action

Lines of Cocaine prepared for snorting

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Cocaine hydrochloride for medicinal use

Cocaine works by blocking the reuptake of dopamine, serotonin, and norepinephrine in the central nervous system. This leads to an increase in these neurotransmitters, creating euphoria, increased energy, and alertness.

Short-term Effects

• Euphoria – Intense pleasure and confidence
• Increased energy – Reduced fatigue
• Alertness – Heightened sensory perception
• Reduced appetite – Temporary suppression of hunger
• Numbness – When applied topically

Negative Effects

• Paranoia – Irrational fears or suspicions
• Increased heart rate – Risk of cardiac arrest
• Anxiety and restlessness
• Hallucinations – In some users
• Aggressive behavior
• Increased blood pressure – May lead to stroke or heart attack

Forms and Routes of Administration

Powdered Cocaine ("Coke") 

• Method: Snorted, injected, or rubbed on gums
• Effects: Lasts 15–60 minutes
• Risks: Damage to nasal tissues, infections

Crack Cocaine ("Crack") 

• Method: Smoked
• Effects: Intense but short-lived high
• Risks: Highly addictive, lung damage

Injectable Cocaine 

• Method: Mixed with water and injected
• Effects: Immediate, intense high
• Risks: Overdose, HIV and Hepatitis C transmission from shared needles

Oral (Chewing Coca Leaves) 

• Method: Chewed with alkaline substance
• Effects: Mild stimulation, prolonged effect
• Risks: Minimal compared to other forms

Medical Uses

Despite its recreational abuse, cocaine is still used medically, particularly in otolaryngology (ENT) and dentistry.

• Topical anesthesia – Used for nasal and throat surgeries
• Vasoconstriction – Reduces bleeding in minor procedures
• Pain relief – Historically used for toothaches (before being replaced by safer alternatives)

Dangers and Addiction

Cocaine hydrochloride powder, commonly abused in illicit drug use

Cocaine is highly addictive, particularly when smoked or injected. Repeated use leads to tolerance, requiring higher doses for the same effect, increasing the risk of overdose.

Health Risks 

• Heart complications – Increased risk of heart attack, arrhythmias
• Brain damage – Can cause strokes, seizures
• Respiratory issues – Crack cocaine users often develop lung disease
• Mental health disorders – Increases risk of depression, anxiety, psychosis

Cocaine Overdose Symptoms 

• Extreme agitation
• Severe chest pain
• Hallucinations
• Hyperthermia (high fever)
• Seizures
• Loss of consciousness

In extreme cases, cocaine overdose can result in sudden death due to cardiac arrest or respiratory failure.

Legality and Global Regulation

Cocaine is illegal in most countries, except for limited medical use. It is classified as:

• Schedule II in the United States (restricted medical use)
• Class A in the United Kingdom
• Schedule 8 in Australia
• Class A in New Zealand

In many South American countries, chewing coca leaves remains legal due to cultural significance, but processed cocaine is strictly prohibited.

See Also

• Crack Cocaine
• Stimulants
• Local anesthetics
• Addiction
• Neurotransmitters
• Coca-Cola (History of Cocaine use)