Cocaine, Amphetamines, and Related Stimulants

Approach to Drug Discussion

  • History and prevalence

  • Pharmacology

  • Effects

Controlled Stimulants

  • Key examples:

    • Cocaine: Angel powder, mama coca

    • Dextroamphetamine: Adderall, Vyvanse

    • Methamphetamine: Desoxyn

    • Methylphenidate: Ritalin, Concerta

    • Methcathinone: cat

    • Mephedrone: Bath salts

Coca Leaf

  • Indigenous use by Bolivians, Ecuadorians, and Peruvians for thousands of years.

  • First isolated cocaine in 1850.

Early Cocaine Use

  • Sigmund Freud advocated using cocaine for ailments.

  • Local anesthetic implications led to its popularity, followed by backlash by the late 19th century.

Amphetamines

  • Synthesized late 19th century; first medical use in 1920s.

  • Usage in WWII and subsequent epidemics in Japan and Europe.

Cocaine Epidemic

  • 1970s: Cocaine glamorized and revitalized.

  • Emergence of freebasing and widespread crack use in the 1980s.

Cocaine Drug Wars

  • Colombian cartels dominated distribution in the 1980s.

  • Anti-Drug Abuse Acts led to severe penalties and racial disparities in prosecutions.

Methamphetamine

  • First prominence in 1970s; resurged in early 1990s in the U.S.

  • Declining use rates, but significant social impact remains.

Bath Salts

  • Synthetic stimulants that emerged post-2009; linked to acute psychosis and health crises.

  • Schedule 1 substances with ongoing synthesis.

Stimulant Action Mechanism

  • Affects brain via monoamine neurotransmitters (dopamine, norepinephrine, serotonin).

  • Cocaine and amphetamines inhibit reuptake; synthetic cathinones vary.

Pharmacokinetics of Stimulants

  • Effects vary based on route: IV is fastest; oral slowest.

  • Cocaine effects last 20-80 minutes; amphetamines 4-12 hours.

Acute Effects at Low/Moderate Doses

  • Enhance mood, increase alertness, suppress appetite.

  • Risks include state-dependent learning, impaired complex learning tasks.

Risks of High Stimulant Doses

  • Possible stimulant psychosis and overdose risks.

  • Associated with acute deaths from cardiovascular issues.

Effects of Chronic Use

  • Tolerance develops, particularly for cocaine.

  • Withdrawal symptoms include depression and anxiety, with identifiable phases of craving and response.

Origin, Source, and Production

  • Coca Leaf: Indigenous use by Bolivians, Ecuadorians, and Peruvians for thousands of years; cocaine was first isolated in 1850.

  • Amphetamines: Synthesized late 19th century, with first medical use in the 1920s.

  • Methamphetamine: Gained prominence in the 1970s and resurged in the early 1990s in the U.S.

  • Bath Salts: Synthetic stimulants that emerged post-2009; ongoing synthesis of Schedule I substances.

Uses

  • Indigenous Use: Coca leaf used for thousands of years (e.g., for energy, altitude sickness).

  • Early Medical Use: Sigmund Freud advocated cocaine for various ailments; widely used for local anesthetic implications.

  • Prescription Stimulants: Dextroamphetamine (Adderall, Vyvanse) and Methylphenidate (Ritalin, Concerta) are used medically.

  • Historical Use: Amphetamines used in WWII for soldiers to combat fatigue.

Benefits (Perceived or Clinical)

  • Acute Effects (Low/Moderate Doses): Enhance mood, increase alertness, and suppress appetite.

  • Medical: Cocaine was important for its local anesthetic properties.

Administration

  • Routes of administration impact onset and duration of effects: intravenous (IV) is fastest, oral is slowest.

  • Historical and common routes include insufflation, smoking (freebasing, crack), and oral ingestion.

Mechanism of Action and Pharmacokinetics

  • Mechanism of Action: Stimulants affect the brain by influencing monoamine neurotransmitters, primarily dopamine, norepinephrine, and serotonin.

    • Cocaine and amphetamines inhibit the reuptake of these neurotransmitters.

    • Synthetic cathinones (bath salts) have varied mechanisms of action, some also affecting reuptake or increasing release.

  • Pharmacokinetics: Duration of effects varies significantly by substance and route of administration.

    • Cocaine effects typically last 20-80 minutes.

    • Amphetamines generally last 4-12 hours.

Acute Effects

  • Low/Moderate Doses: Enhance mood, increase alertness, suppress appetite.

  • Risks: State-dependent learning and impaired performance on complex learning tasks.

  • High Doses: Can lead to stimulant psychosis and overdose, with acute deaths often resulting from cardiovascular issues.

Chronic Effects

  • Withdrawal symptoms include depression and anxiety.

  • Chronic use can lead to identifiable phases of craving and response.

  • Stimulant psychosis may persist with chronic high-dose use.

Tolerance

  • Tolerance develops with chronic use, particularly noted for cocaine.

Dependence

  • Chronic use leads to psychological dependence, evidenced by withdrawal symptoms such as depression, anxiety, and intense craving.

Trends

  • Cocaine: Glamorized in the 1970s; emergence of freebasing and widespread crack use in the 1980s during the

Approach to Drug Discussion - History and prevalence - Pharmacology - Effects
Controlled Stimulants

  • Key examples:

    • Cocaine: Angel powder, mama coca

    • Dextroamphetamine: Adderall, Vyvanse

    • Methamphetamine: Desoxyn

    • Methylphenidate: Ritalin, Concerta

    • Methcathinone: cat

    • Mephedrone: Bath salts

Coca Leaf

  • Indigenous use by Bolivians, Ecuadorians, and Peruvians for thousands of years.

  • First isolated cocaine in 1850.

Early Cocaine Use

  • Sigmund Freud advocated using cocaine for ailments.

  • Local anesthetic implications led to its popularity, followed by backlash by the late 19th century.

Amphetamines

  • Synthesized late 19th century; first medical use in 1920s.

  • Usage in WWII and subsequent epidemics in Japan and Europe.

Cocaine Epidemic

  • 1970s: Cocaine glamorized and revitalized.

  • Emergence of freebasing and widespread crack use in the 1980s.

Cocaine Drug Wars

  • Colombian cartels dominated distribution in the 1980s.

  • Anti-Drug Abuse Acts led to severe penalties and racial disparities in prosecutions.

Methamphetamine

  • First prominence in 1970s; resurged in early 1990s in the U.S.

  • Declining use rates, but significant social impact remains.

Bath Salts

  • Synthetic stimulants that emerged post-2009; linked to acute psychosis and health crises.

  • Schedule 1 substances with ongoing synthesis.

Stimulant Action Mechanism

  • Affects brain via monoamine neurotransmitters (dopamine, norepinephrine, serotonin).

  • Cocaine and amphetamines inhibit reuptake; synthetic cathinones vary.

Pharmacokinetics of Stimulants

  • Effects vary based on route: IV is fastest; oral slowest.

  • Cocaine effects last 20-80 minutes; amphetamines 4-12 hours.

Acute Effects at Low/Moderate Doses

  • Enhance mood, increase alertness, suppress appetite.

  • Risks include state-dependent learning, impaired complex learning tasks.

Risks of High Stimulant Doses

  • Possible stimulant psychosis and overdose risks.

  • Associated with acute deaths from cardiovascular issues.

Effects of Chronic Use

  • Tolerance develops, particularly for cocaine.

  • Withdrawal symptoms include depression and anxiety, with identifiable phases of craving and response.

Origin, Source, and Production

  • Coca Leaf: Indigenous use by Bolivians, Ecuadorians, and Peruvians for thousands of years; cocaine was first isolated in 1850.

  • Amphetamines: Synthesized late 19th century, with first medical use in the 1920s.

  • Methamphetamine: Gained prominence in the 1970s and resurged in the early 1990s in the U.S.

  • Bath Salts: Synthetic stimulants that emerged post-2009; ongoing synthesis of Schedule I substances.

Uses

  • Indigenous Use: Coca leaf used for thousands of years (e.g., for energy, altitude sickness).

  • Early Medical Use: Sigmund Freud advocated cocaine for various ailments; widely used for local anesthetic implications.

  • Prescription Stimulants: Dextroamphetamine (Adderall, Vyvanse) and Methylphenidate (Ritalin, Concerta) are used medically.

  • Historical Use: Amphetamines used in WWII for soldiers to combat fatigue.

Benefits (Perceived or Clinical)

  • Acute Effects (Low/Moderate Doses): Enhance mood, increase alertness, and suppress appetite.

  • Medical: Cocaine was important for its local anesthetic properties.

Administration

  • Routes of administration impact onset and duration of effects: intravenous (IV) is fastest, oral is slowest.

  • Historical and common routes include insufflation, smoking (freebasing, crack), and oral ingestion.

Mechanism of Action and Pharmacokinetics

  • Mechanism of Action: Stimulants affect the brain by influencing monoamine neurotransmitters, primarily dopamine, norepinephrine, and serotonin.

    • Cocaine and amphetamines inhibit the reuptake of these neurotransmitters.

    • Synthetic cathinones (bath salts) have varied mechanisms of action, some also affecting reuptake or increasing release.

  • Pharmacokinetics: Duration of effects varies significantly by substance and route of administration.

    • Cocaine effects typically last 20-80 minutes.

    • Amphetamines generally last 4-12 hours.

Acute Effects

  • Low/Moderate Doses: Enhance mood, increase alertness, suppress appetite.

  • Risks: State-dependent learning and impaired performance on complex learning tasks.

  • High Doses: Can lead to stimulant psychosis and overdose, with acute deaths often resulting from cardiovascular issues.

Chronic Effects

  • Withdrawal symptoms include depression and anxiety.

  • Chronic use can lead to identifiable phases of craving and response.

  • Stimulant psychosis may persist with chronic high-dose use.

Tolerance

  • Tolerance develops with chronic use, particularly noted for cocaine.

Dependence

  • Chronic use leads to psychological dependence, evidenced by withdrawal symptoms such as depression, anxiety, and intense craving.

Trends

  • Cocaine: Glamorized in the 1970s; emergence of freebasing and widespread crack use in the 1980s during the Cocaine Drug Wars, leading to severe penalties and racial disparities in prosecutions.

  • Methamphetamine: First prominence in the 1970s; resurged in the early 1990s in the U.S., significantly impacting society despite declining use rates.

  • Bath Salts: Synthetic stimulants that emerged post-2009; linked to acute psychosis and health crises, considered Schedule 1 substances with ongoing synthesis.

Variables Impacting Use

  • Social/Environmental Factors: Peer pressure, availability, cultural acceptance, and local drug policies.

  • Psychological Factors: Mental health conditions (e.g., depression, anxiety), stress, trauma, and individual coping mechanisms.

  • Biological Factors: Genetic predispositions, individual differences in brain chemistry, and variations in drug metabolism.

  • Economic Factors: Socioeconomic status, educational attainment, and cost/accessibility of substances.

  • Legal/Regulatory Factors: Severity of penalties, enforcement practices, and access