M2 Sec02: Amphetamines and Cocaine

Amphetamines

Drugs of widespread misuse; controlled substances in Canada

Amphetamines drug class

Includes amphetamines, dextroamphetamine, and methamphetamine

Amphetamine-related compounds

Includes methylphenidate and MDMA

Methylphenidate (Ritalin)

used to treat ADHD

MDMA (Ecstasy)

An often-misused derivative of methamphetamine; fosters feelings of intimacy and empathy, improves intellectual capacities

Neurotoxicity of MDMA

Causes neuronal damage and death; long-lasting if not permanent

Chemistry of amphetamines

Synthetic organic compounds similar in structure to norepinphrine and dopamine ; easily synthesized, resulting in illicit manufacturing (especially methamphetamine)

Illicitly manufactured amphetamine purity

Varies - may contain side products of the chemical reaction, unreacted chemicals, and dangerous filler agents

Pharmacological effect of amphetamines

Increase excitation by increasing the amount of dopamine or norepinephrine in the synaptic cleft

Amphetamine duration of action

Long (up to 12 hours)

Amphetamine mechanism of action

Blocks vesicular monoamine transporters, increase dopamine/norepinephrine at synapse

Amphetamine CNS effects (4)

1. Decreased threshold for transmitting sensory input to the cerebral cortex (leads to CNS excitation)

2. Feelings of euphoria and reward

3. Temperature-regulation and hunger/satiation centre modifications (results in appetite suppression)

4. Increased aggressive behaviour and mood swings

CNS excitation

• Increased alertness, feeling of power, reduced fatigue, increased responsiveness

• Increased heart rate and BP

Amphetamine short-term use effects

• Angina (chest pain) or heart pain

• Cardiovascular collapse (from high doses)

• Increased respiratory rate

• OD may result in seizure, high fever, or stroke

Amphetamine long-term use effects

• Chronic sleeping problems

• Poor appetite

• Anxiety, repetitive behaviour, psychoses, aggressive behaviour

• Elevated BP and abnormal cardiac rhythm

Concurrent drug use with amphetamines

• May be sought to antagonize various toxic effects of amphetamines (or vice versa)

• Additional issues include: drug-drug interactions, misusing additional drugs, potential SUD

Therapeutic uses of amphetamines

1. Narcolepsy

2. ADHD

Methylphenidate will be used rather than amphetamine.

Amphetamine potential for misuse

Extremely high
(powerful euphoria, readily injectable causing rapid response, inherent harmfulness toxicities are long-term and non deterring)

Amphetamine tolerance

Develops to: euphoria, appetite suppression, cardiovascular and respiratory stimulatory effects, lethal effects
Does NOT develop to: therapeutic effects, psychosis

Amphetamine withdrawal symptoms

Mood depression

Prolonged sleep

Huge appetite

Lack of energy, fatigue

Amphetamine addiction

Due to reward effect; users experience intense craving for drug and panic if not available

Cocaine pharmacological classification

Local anesthetic and CNS stimulant

Cocaine legal classification

Narcotic

Cocaine duration of action

Short (less than an hour)

Cocaine routes of administration

Commonly sniffed or smoked

Cocaine pharmacological effect

Cause generalized CNS stimulation in a dose-dependent manner

Cocaine mechanism of action

Inhibition of dopamine and serotonin

Increased activation of postsynaptic neuronal receptors

Therapeutic use of cocaine

Local anesthetic for mouth/throat (rarely used)

Long-term cocaine use effects

Toxic psychosis (including paranoia)

Hallucinations

Impaired sexual function

Permanent brain damage

High BP, irregular heart rhythm

Changes to nasal mucosa

Concurrent consumption of alcohol and cocaine

Very dangerous — reaction of the 2 drugs forms cocaethylene

Cocaethylene

Metabolite produced by the reaction of alcohol and cocaine; dangerously increases BP, aggression, violent thoughts, poor judgement

Cocaine potential misuse

Extremely high

Due to powerful euphoria (rapid effect, non deterrent inherent harmfulness)

Cocaine tolerance

Develops to: mood-elevating effect
Does NOT develop to: psychotic effect

Cocaine withdrawal

Similar symptoms to amphetamine withdrawal

Cocaine addiction

Occurs due to rewarding and pleasurable effects, reinforcing repeated drug use