Download Chapter 16 Cholinesterase Inhibitors

Chapter 40
Drug Abuse IV: Major Drugs of
Abuse Other Than Alcohol and
Nicotine
Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc.
Drug Abuse IV:
Major Drugs of Abuse
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Heroin and other opioids
General CNS depressants
Psychostimulants
Marijuana and related preparations
Psychedelics
3,4-Methylenedioxymethamphetamine (MDMA,
Ecstasy)
Phencyclidine
Inhalants
Anabolic steroids
Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc.
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Heroin, Oxycodone, and
Other Opioids
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Major drugs of abuse
Most opioids are Schedule II
Patterns of abuse
Subjective and behavioral effects
Preferred drugs and routes of administration
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Heroin
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Patterns of use
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Greatest use among 18- to 25-year-olds
All segments of society
First exposure usually social or for pain management
Subjective and behavioral effects
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Moments after IV injection, lower abdominal sensation that is
similar to sexual orgasm and lasts about 45 seconds
 Followed by euphoria
 Initial use causes nausea and vomiting
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Preferred drugs and routes of administration
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Opioid of choice for street use
High lipid solubility
IV route preferred, but also smoking, nasal inhalation
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Meperidine
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Nurses and physicians who abuse opioids
often select meperidine
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Highly effective in oral route (unlike injections,
leaves no sign)
Minimal effect on smooth muscle: fewer problems
with constipation and urinary retention
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Oxycodone
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Opioid similar to morphine
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Intended as controlled-release drug (OxyContin)
Abusers crush tablet
Snort powder or dissolve in water for IV
Entire dose absorbed immediately with high risk of
death
Tolerance and physical dependence
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Oxycodone
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Treatment of acute toxicity
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Classic triad
• Respiratory depression, coma, pinpoint pupils
Naloxone (Narcan)
Nalmefene (Revex)
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Tolerance and Physical
Dependence
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Tolerance
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Prolonged use
Effects for which tolerance develops
Effects for which tolerance does not develop
Cross-tolerance
Physical dependence
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Long-term use
 Abstinence syndrome
 Acute phase and second phase
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Opioid Detoxification
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Detoxification
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Methadone substitution
• Long-acting oral opioid
• Most commonly used agent
• Approximately 10 days
 Clonidine-assisted withdrawal
 Rapid and ultrarapid withdrawal
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Drugs for Long-Term Opioid
Addiction Management
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Three groups of medications
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Methadone
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Maintenance and suppressive therapy
Buprenorphine
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Opioid agonists, opioid agonist-antagonists, and
opioid antagonists
Maintenance therapy and detox facilitation
Naltrexone
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Discourages renewed opioid abuse
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Sequelae of Compulsive
Opioid Use
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Few direct detrimental effects
Treatment programs vs. street drugs and
subculture
Accidental overdose
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General CNS Depressants
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Barbiturates, benzodiazepines, alcohol, and
other agents
Benzodiazepines have unique properties
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Barbiturates
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Depressant effects are dose-dependent
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Mild sedation to sleep to coma and death
Subjective effects similar to those of alcohol
Agents with short to intermediate duration of
action have highest abuse incidence and are
Schedule II
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Amobarbital, pentobarbital, and secobarbital
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Benzodiazepines
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Tolerance
Physical dependence and withdrawal
techniques
Acute toxicity
Flumazenil (Romazicon)
Benzodiazepines (Schedule IV)
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Much safer than barbiturates
Overdose rare when taken alone and orally
Risk increased with IV or with other depressants
Alcohol and miscellaneous CNS depressants
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Methaqualone (Quaalude)
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Psychostimulants
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CNS stimulants (Schedule II) that have a high
potential for abuse
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Amphetamines
Cocaine
Related substances
Can stimulate the heart, blood vessels, and
other structures under sympathetic control
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Cocaine
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Extracted from leaves of coca plant
CNS effect similar to that of amphetamines
Two forms used by abusers
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Cocaine
“Crack”
Can produce local anesthesia,
vasoconstriction, and cardiac stimulation
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Cocaine
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Cocaine
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Cocaine hydrochloride
• White powder
• Diluted for sale
• Taken intranasally
 Cocaine base: commonly called “crack”
• Also called “crystals” or “rocks”
• Heated for use
• Taken by IV injection
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Methamphetamines
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In abuse, usually taken orally, snorted,
smoked, or IV
Also called “ice” or “crystal meth”
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Form of dextroamphetamine
Smoked, snorted, or inserted into rectum
Effects
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Arousal, euphoria, sense of increased physical
strength and mental capacity
Hallucinations, psychotic state, sympathomimetic
actions
Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc.
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Methamphetamines
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Other adverse effects
Tolerance, dependence, and withdrawal
Treatment
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Bupropion (Wellbutrin, Zyban)
Modafinil (Provigil, Alertec)
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Marijuana
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Cannabis sativa (hemp)
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Marijuana and hashish are derivatives
Common names: “grass,” “weed,” “pot”
Most commonly used illicit drug in the United
States
95 million Americans have tried marijuana at
least once
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Marijuana
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Psychoactive substance
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Delta-9-tetrahydrocannabinol (THC)
Routes
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Smoking
• 60% of THC content absorbed, effects begin in minutes
and peak within 20–30 minutes
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Oral
• Majority of THC is inactivated by first-pass effect
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Marijuana
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Increased production of prostaglandin E2
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Behaviors
• Euphoria
• Sedation
• Hallucinations
 Therapeutic uses
• Antiemetic
• Appetite stimulant
• Neuropathic pain
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Marijuana
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Effects
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Low to moderate dose
High dose
Long-term use
Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc.
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Marijuana
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Effects
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Cardiovascular
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Low to moderate dose
High-dose
Long-term use
Schizophrenia
Dose-related increase in heart rate
Respiratory
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Acute: bronchodilation
Chronic: airway constriction
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Marijuana
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Reproduction
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Altered brain structure
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Males and females affected
Hippocampal volume left hemisphere
Tolerance and dependence
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Therapeutic Use Marijuana
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Approved uses for cannabinoids
Unapproved uses for cannabinoids
Medical research on marijuana
Legal status of medical marijuana
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Therapeutic Use Marijuana
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Comparison of marijuana with alcohol
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Aggressive behavior is rare with marijuana use
Loss of judgment is less with marijuana
Increased appetite with marijuana: fewer problems
with nutritional deficiencies
Marijuana produces increased toxic psychosis,
dissociative phenomena, and paranoia, more so
than with alcohol
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Psychedelics
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Lysergic acid diethylamide (LSD)
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Acts on serotonin receptors of brain
Routes: oral, IV, smoked
Alters the following (as otherwise occurs only in
dreams):
• Thinking
• Feelings
• Perception
• Relationship to environment
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Other Psychedelic Drugs
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Subjective and behavioral effects are similar
to those of LSD
None approved for medical use
Salvia
Mescaline
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From peyote cactus
Psilocybin
Psilocin
Dimethyltryptamine
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Dissociative Drugs
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Phencyclidine (PCP) and ketamine
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Original use: surgical anesthetics
Recreational use: distort sight and sound and
produce dissociation
Act in the cerebral cortex and limbic system
PCP synthesized/manufactured easily by
amateurs
Routes: oral, intranasal, IV, smoking
Ketamine
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Dissociative Drugs
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Phencyclidine (PCP)
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Effects
• Low to moderate doses, high doses
Toxicity
Ketamine
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Similar to PCP in structure, mechanism, and
effects
Shorter duration of effects
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Dextromethorphan
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OTC cough suppressant
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Low dose for antitussive: no psychologic effects
At doses 5–10 times higher, produces euphoria,
disorientation, paranoia, altered sense of time,
and hallucinations
Also used in combination cold products
Highly abused by adolescents and teenagers
OTC = over-the-counter.
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3,4Methylenedioxymethamphetamine
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Common names: MDMA, Ecstasy
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Complex drug with stimulant and psychedelic
properties
Structurally related to methamphetamine
(stimulant) and mescaline (hallucinogen)
• Low doses: mild LSD-like psychologic effects
• Higher doses: amphetamine-like effects
Promotes release of neurotransmitters
Usually taken orally; also snorted, injected, or
taken by rectal suppository
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MDMA, Ecstasy
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Adverse effects
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Can injure serotonergic neurons, stimulate the
heart, and dangerously raise body temperature
Neurologic effects
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Seizures, spasmodic jerking, jaw clenching, teeth
grinding
Confusion, anxiety, paranoia, panic
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Inhalants
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Term can refer to many drugs; common
characteristic is administration by inhalation
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Anesthetics
Volatile nitrites
Organic solvents
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Anabolic Steroids
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Androgens
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Taken to enhance athletic performance
Increase muscle mass and strength
Massive doses that are often used have high risk
for adverse effects
Most are classified as Schedule III drugs
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