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Questions and Answers
Cocaine is a direct agonist for serotonin with low affinity.
Cocaine is a direct agonist for serotonin with low affinity.
False
Cocaethylene is formed when cocaine and alcohol react chemically.
Cocaethylene is formed when cocaine and alcohol react chemically.
True
Cocaine has a longer half-life compared to amphetamines.
Cocaine has a longer half-life compared to amphetamines.
False
The use of beta-blockers is recommended during cocaine intoxication to mitigate sympathetic effects.
The use of beta-blockers is recommended during cocaine intoxication to mitigate sympathetic effects.
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Amphetamines can penetrate the blood-brain barrier easily.
Amphetamines can penetrate the blood-brain barrier easily.
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Hyperthermia caused by cocaine can lead to fatal outcomes in hot weather.
Hyperthermia caused by cocaine can lead to fatal outcomes in hot weather.
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Cocaine autometabolizes in the liver, which is a common feature among all drugs.
Cocaine autometabolizes in the liver, which is a common feature among all drugs.
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Cocaine can cause dysrhythmias due to sodium and potassium blockade.
Cocaine can cause dysrhythmias due to sodium and potassium blockade.
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Cocaine is synthesized from the Erythroxylon coca plant.
Cocaine is synthesized from the Erythroxylon coca plant.
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Amphetamines are primarily used for treating anxiety disorders.
Amphetamines are primarily used for treating anxiety disorders.
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Methylphenidate is commonly used to treat ADHD.
Methylphenidate is commonly used to treat ADHD.
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Crack cocaine is a form that can be smoked.
Crack cocaine is a form that can be smoked.
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Caffeine is considered a psychostimulant.
Caffeine is considered a psychostimulant.
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Cocaine and amphetamines both inhibit the reuptake of serotonin in the brain.
Cocaine and amphetamines both inhibit the reuptake of serotonin in the brain.
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The main effect of psychostimulants is to induce a state of calmness and sedation.
The main effect of psychostimulants is to induce a state of calmness and sedation.
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Vasoconstriction is a potential side effect of cocaine use.
Vasoconstriction is a potential side effect of cocaine use.
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Study Notes
Psychostimulants: Cocaine, Amphetamines
- Cocaine and amphetamines are psychostimulants.
- Learning objectives include: familiarizing with examples, understanding mechanisms of action, and describing side effects of abuse.
- Central Nervous System (CNS) Stimulants
- Cocaine: Crack (freebase or hydrochloride), powder form. -Amphetamine: Methamphetamine, methylphenidate (Ritalin), D-amphetamine,phenmetrazine (Preludin).
- Hallucinogens: MDA, MDMA, DOM, methylenedioxymethamphetamine ("ecstasy")
- Khat: Cathinone, methcathinone -Methylxanthines: Caffeine (coffee), theophylline (treating asthma), theobromine (chocolate)
Cocaine Overview
- Alkaloid from Erythroxylon coca plant (native to South America).
- Coca leaves have religious, mystical, social, stimulant, and medicinal uses.
- Main stimulant uses: enhance endurance, feeling of well-being (euphoria), appetite suppression.
- Medical uses: local anesthetic & vasoconstrictor (nasal congestion).
Cocaine Production
- Cocaine paste extracted from soaked and mashed coca leaves (60-80% cocaine).
- Cocaine powder made by mixing paste with hydrochloric acid.
- Freebase/crack cocaine extracted from powder with baking soda (smokable).
Amphetamine Overview
- Synthetic analog of ephedrine, active in mahuang.
- Mahuang is used in China for asthma.
- Equivalent to "poor man's cocaine" (crystal meth, ice, glass, speed)
- Methamphetamine and methylphenidate (Ritalin) are similar.
- Medical uses: obesity, ADHD, narcolepsy.
Chemical Structure of Stimulants
- Chemical structures of cocaine, amphetamine, methamphetamine, and methylphenidate.
- Images provide visual representation of molecular structures.
Neurophysiology of Cocaine
- Cocaine blocks the reuptake of norepinephrine, causing it to remain in the synaptic cleft.
Cocaine Pharmacology by Route of Administration
- Inhalation ("Crack"): Onset 8 seconds, peak 2-5 minutes, duration 10-20 minutes.
- Intranasal (snorting): 2-5 minutes, 5-10 minutes, 30 minutes
- Intravenous (IV): Seconds, peak 10-20 minutes, duration 60-90 minutes
- Oral: 30-60 minutes, unknown
- Skin popping: Unknown, unknown, unknown
Effects on Mind, Brain, Behavior
- Increase: alertness/vigilance, concentration, mental acuity, sensory awareness, euphoria/elevated mood, brain electrical activity, self-confidence, grandiosity, sleep need (insomnia)
- Decrease: appetite, brain blood flow, glucose metabolism.
Effects on Mind, Brain, Behavior (Continued)
- Increase: anxiety, suspiciousness, paranoia, convulsions, tremor, seizure, psychosis, delirium, locomotion (at low/moderate doses), reinforcement/addiction.
- Decrease: judgment, complex multi-tasking.
Peripheral Effects (Sympathomimetic)
- Sympathomimetic effects: Fight-flight-fright response.
- Increased: blood pressure, blood sugar, heart rate, irregular heart beat, vasoconstriction, body temperature rise, bronchodilation, impaired breathing.
Clinical Effects of Sympathomimetics
- Symptoms may include hypertension, hyperthermia, tachycardia, mydriasis, diaphoresis, and central nervous system excitation.
Cocaine Cardiac Features
- Cocaine dysrhythmias: sodium and potassium blockade.
- Supraventricular tachycardia (SVT)
- Wide or prolonged QRS may be dangerous leading to V-tach. Treatment includes sodium bicarbonate.
- Atrial fibrillation/flutter
- Wide complex tachycardia.
Body Packers/Stuffers
- Body packers smuggle drugs by packing them in their bodies.
- Body stuffers swallow contraband to evade detection.
Cocaine Pharmacokinetics: Absorption
- Routes of administration: insufflated (snorted), intravenous (IV), inhaled (freebased), oral.
Pharmacokinetics: Distribution and Metabolism
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Cocaine and amphetamines readily cross the blood-brain barrier.
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Cocaine half-life: 50-90 minutes.
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Amphetamine half-life: 5-10 hours.
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Methamphetamine half-life: 12 hours.
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Metabolites are active and inactive compounds.
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Cocaine is unusual as it "autometabolizes" in the blood system in addition to normal liver metabolism
Cocaethylene
- Alcohol inhibits the metabolism of cocaine (making it accumulate and last longer).
- Alcohol and cocaine react chemically to form cocaethylene.
- Cocaethylene is an active compound with similar effects to cocaine but greater cardiac toxicity.
Cocaine Pharmacodynamics
- Indirect agonist (high affinity) of dopamine and norepinephrine.
- Modest affinity for serotonin (5-HT).
- Mechanism: Blocks monoamine reuptake.
Amphetamine Pharmacodynamics
- Indirect agonist (high affinity) for dopamine and norepinephrine.
- Modest affinity for serotonin.
- Mechanisms: Blocks monoamine reuptake, inhibits vesicular storage, inhibits MAO metabolism, and reverses reuptake.
Withdrawal and Addiction
- Withdrawal symptoms: physically mild to moderate (hunger, fatigue, anxiety, irritability, depression, panic attacks).
- Dysphoric syndrome (1-5 days after crash), characterized by decreased activity, amotivation, intense boredom, anhedonia, intense craving for cocaine. Withdrawal can last from 1-10 weeks.
- Intense cravings are common.
- Route of administration can affect risk of addiction.
Khat
- Ingesting large amounts of Khat ( Catha edulis) causes sympathomimetic effects (seizures, cardiac arrhythmias).
- Khat addiction tends to be somewhat physiological
Treatment for Sympathomimetic Toxicity
- Benzodiazepines are first-line treatment.
- Beta-blockers are contraindicated, as unopposed alpha-receptor stimulation needs to be addressed.
- Cocaine-induced wide complex tachycardia can be treated with sodium bicarbonate and Alprazolam (Xanax).
- Hypertension unresponsive to benzodiazepines, Phentolamine can be used.
- Decontamination with bowel irrigation or opening bowel for removal of large amounts of drug. Activated charcoal for pills.
Causes of Stimulant-Induced Chest Pain
- Can be non-cardiac or cardiac-related causes, including pneumothorax, pneumomediastinum, aoriti dissection, pulmonary infarction, infection (foreign body aspiration, pericarditis), ischemia/infarction, and more.
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Description
This quiz explores psychostimulants, focusing on cocaine and amphetamines. It covers examples, mechanisms of action, and the side effects of abuse. Additionally, it will touch on related substances like hallucinogens and methylxanthines.
