Cocaine Types and Forms

Cocaine Types and Administration

• Coca leaves, the natural form of cocaine, can be taken orally (chewed).
• Coca paste is made by smashing coca leaves into water, resulting in a concentrated paste.
• Cocaine hydrochloride, a salt version in powder form, is extracted from coca leaves, can be snorted or injected intravenously, but it cannot be smoked.
• Freebase cocaine is made by freeing the cocaine base from the salt with ether, which allows it to be smoked, but it is dangerous to produce.
• Crack cocaine is made by mixing cocaine with baking soda to remove the hydrochloride, which allows it to be smoked, snorted, or injected.

Cocaine Origin and Synthesis

• Cocaine is naturally derived from the coca plant through extraction.

Crack vs. Freebase Cocaine

• Freebase cocaine was the first smokable form, created by freeing the cocaine base from the salt using ether, a dangerous process.
• Crack cocaine is a safer alternative to freebase, created by treating cocaine with baking soda, which frees the base.

Historical Use of Cocaine

• In the 1860s, cocaine was used medically as a local anesthetic.
• In 1884, Freud promoted cocaine as a psychological treatment but later discovered its addictive properties.
• In 1886, cocaine was an ingredient in soft drinks like Coca-Cola, but it was later replaced by caffeine after the Harrison Narcotic Act.
• In 1914, cocaine was controlled and regulated as a Schedule 2 drug under the Harrison Narcotic Act.

Cocaine Metabolism

• Cocaine is metabolized quickly by enzymes in the liver and blood.
• Benzoylecgonine is an inactive metabolite.
• Cocaethylene, is formed when cocaine and alcohol are metabolized together and is more toxic, has higher rates of dependency, and causes worse withdrawal symptoms.

Neurotransmitter Effects of Cocaine

• Cocaine blocks the reuptake of dopamine, norepinephrine, and serotonin, which enhances their effects in the brain.

Primary Actions of Cocaine

• Cocaine acts as a local anesthetic, numbing the gums, nose, and throat.
• It is a vasoconstrictor, narrowing veins, which can lead to cardiovascular problems.
• It is a psychostimulant leading to reinforcement and addiction.

Speedball

• A speedball is a combination of cocaine (stimulant) and heroin (depressant), typically injected, and can lead to overdose.

Cocaine Dependence Treatment

• Ritalin is a safer anti-withdrawal agent.
• Zofran is an anti-craving agent used to combat nausea.

Cocaine "Crash"

• A cocaine "crash" occurs after high doses, resulting in dopamine pathway exhaustion and depression, leading to more drug use.

Amphetamine History and Creation

• Amphetamine is a family of psychostimulants used for 90 years.
• Isolated from the Ma Huang herb (ephedrine), Gordon Alles created amphetamine as a synthetic version of ephedrine.

Amphetamine Timeline

• 1930s: Benzedrine was used as an OTC sinus decongestant and to treat various conditions.
• 1940s: Methedrine, the first version of methamphetamine, was used for ADHD.
• 1970s: Amphetamines were scheduled and regulated under the US Drug Regulation Control Act.

Amphetamine Forms

• Amphetamine (pill version): Used to treat ADHD.
  • Dextroamphetamine treats ADHD, fatigue, and weight loss.
  • Levoamphetamine is weaker and less prone to abuse.
• Methamphetamine hydrochloride (pill or powder form): A methyl group helps it cross the blood-brain barrier faster.

Amphetamine Administration Routes

• Oral ingestion leads to slower effects with a longer duration.
• Smoking delivers the drug rapidly, leading to a quick, intense high.
• Injection leads to intense effects and increases the risk of addiction and blood clotting.

Crossing the Blood-Brain Barrier

• The methyl group on methamphetamine allows it to cross the blood-brain barrier faster than amphetamine because it is more effective at getting across, and has a faster onset of effects than amphetamine.

Amphetamine Metabolism

• Amphetamines are not significantly affected by metabolism.
• About 10% become metabolites and are excreted in urine.
• It takes 48 hours for amphetamine to show up in urine analysis
• Can be detected in urine for 1-4 days.
• Can test positive if you take something with ephedrine (false positive).

Neurotransmitter Effects of Amphetamine

• Amphetamine is an agonist of dopamine and norepinephrine, leading to more of these neurotransmitters in the synapse.
• It stimulates the release and blocks the reuptake of these neurotransmitters.

Effects on the Autonomic Nervous System

• Amphetamine activates the sympathetic nervous system, increasing respiratory rate, heart rate, blood pressure, and causing pupil dilation, euphoria, increased energy, and decreased appetite.

Amphetamine Psychosis

• High doses and long-term use can cause psychosis, including paranoia, delusion, hallucination, and violent behavior.

ADHD Treatment Drugs

• Ritalin (Methylphenidate): Blocks reuptake of DA and NE and slightly increases releases.
• Adderall: A mixture of dextroamphetamine and amphetamine.
• Concerta: Methylphenidate SR, similar to Ritalin but longer lasting.

Side Effects of ADHD Drugs

• Ritalin can cause stunted growth, sleep problems, and appetite suppression.
• Adderall may increase blood pressure, heart rate, psychomotor activity, and weight loss.
• In people without ADHD, these drugs can overstimulate the brain, reducing learning and memory, and can lead to cognitive impairment, dependence, and withdrawal symptoms.

Caffeine Content in Products

• Over-the-counter stimulants like No Doz and Vivarin have high caffeine content.
• Decaf coffee and caffeine-free coke have low caffeine content.

Xanthines

• Theophylline in tea and theobromine in milk chocolate
• Caffeine is the only legal over the counter stimulant.

Caffeine and Adenosine Receptors

• Caffeine blocks the action of adenosine receptors, leading to behavioral changes and physiological effects.

Caffeine Metabolism

• CYP1A2 breaks down 98-99% of caffeine.
• Caffeine Metabolites include theophylline, theobromine, and paraxanthine.

Physiological Effects of Caffeine

• Caffeine dilates coronary arteries, increases blood pressure and respiration, induces diuresis, activates the sympathetic nervous system, and constricts cerebral blood vessels.

Adverse Effects of Caffeine

• Individuals with anxiety, sleep disorders, heart conditions, and older adults (65+) may experience adverse effects from caffeine.
• Those taking medications like EFFEXOR may also have increased sensitivity.

Alleviating Headaches with Caffeine

• Caffeine alleviates headaches by constricting cerebral blood vessels, reducing pressure on nerves.

Dangers of Energy Drinks

• Energy drinks may contain taurine, vitamin B3 (niacin), vitamin B9, and Gautama seed extract, which can cause adverse effects.

Caffeinism

• Drinking excessive caffeine (1000-2000 mg) can lead to restlessness, nervousness, insomnia, tachycardia, and GI upset.

Diseases Associated with Smoking

• Heart problems: Premature death is common among smokers.
• Mouth cancer: Risk increases with pipe smoking and chewing tobacco.
• Lung problems: COPD, lung cancer, and larynx cancer are common.

Nicotine Receptors

• Nicotine binds to nicotinic ACh receptors in the brain and throughout the body.

Autonomic Nervous System Effects of Nicotine

• Nicotine increases heart rate and blood pressure and stimulates the release of HCL in the stomach.

Nicotine Withdrawal Symptoms

• Withdrawal includes anxiety, problems concentrating, cravings, restlessness, weight gain, and insomnia, lasting a week or two.

Benzopyrene

• Benzopyrene is a carcinogen found in cigarettes that causes lung cancer.

Atherosclerosis vs. Arteriosclerosis

• Atherosclerosis: A buildup of products that decreases the diameter of blood vessels, leading to reduced blood flow and potential blood clots.
• Arteriosclerosis: The hardening of arteries, causing them to rupture.

Nicotine Dependence Treatment

• Nicotine replacement therapy: Patches and gum are used temporarily.
• Prescription drugs: Zyban (DA and NE reuptake inhibitor) and Chantix (partial nicotinic receptor agonist).
• Add behavioral interventions, therapeutic, psychotherapy, etc.

Area Postrema

• The area postrema, located in the brain stem behind the medulla, triggers vomiting from smoking and can cause puffy hands and faces.

Hookah vs. Cigarettes

• Hookah smoking is not safer than cigarettes; one hour of exposure equals 100-200 times the smoke from a cigarette.