Drugs of Abuse

v
def. drugs or chemicals which are
taken repeatedly in a pattern &
amount that interferes with one’s
health or normal function
v
used for a variety of reasons; they
have multiple effects, usually
producing a feeling of well-being in
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Classification of Drugs of
Abuse
v
Opiates & Opioids: morphine,
codeine, heroin, meperidine
(Demerol), hydromorphone
v
Sympathomimetic stimulants:
cocaine, amphetamines,
metamphetamines, MDMA
v
Depressants: barbiturates,
benzodiazepines, ethyl alcohol
v
Hallucinogens: LSD, mescaline,
MDMA,
v
Others: PCP, marijuana, nicotine
v
Classification of drugs of
abuse

CNS actions
v
Stimulants: amphetamine, caffeine,
nicotine, cocaine -
v
Depressants : barbiturates,
benzodiazepines, ETOH
v
Analgesics: narcotics (opiates &
opioids)
v
Sedative–Hypnotics: relaxants, induce
sleep: alcohol; anti-anxiety agents-
tranquilizers; nonbarbiturates-
Halcion, Quaalude; long-acting
barbiturates – Phenobarbital; short-
acting barbiturates - Seconal
Legal classification
v
Schedule 1: high abuse, no
recognized medical use, lack of
safety
v
Schedule 2: high abuse, medical
utility, high dependency risk
v
Schedule 3: lower abuse, medical
utility, moderate dependency
risk
v
Schedule 4: limited abuse, high
medical utility, limited
dependency risk
v
Schedule 5: minor problems
Drugs of abuse
v
Schedule 1:
§
Heroin
§
LSD
§ MDMA
§
Marijuana
§
Methaqualone
v
Schedule 2:
§
Opium
§
Morphine
§ Coca
§
Cocaine
§
Methadone
§
Methampethami
ne
v
Schedule 3:
§
Amphetamine
§
Barbiturates
§ Valium
§
Xanax
§
Anabolic steroids
§
Codeine
v
Schedule 4:
§
Chloral hydrate
§ Meprobamate
§
Paraldehyde
§
phenobarbital
v
Schedule 5:
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DEFINITIONS
v
Positive reinforcement: release of
positive reinforcement
neurotransmitters e.g. dopamine,
endorphins
v
Tolerance: reduced effect with
repeated use of the drugn
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o n urotr nsm tt rs ·
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v
Cross-tolerance: for drugs of the
same class
DEFINITIONS
v
Dependence- compulsion to take the
drug repeatedly
v
Psychological dependence – positive
reinforcement causes a compulsion
to take the drug
v
Physical dependence – negative
reinforcement – distress upon
stopping the drug (withdrawal) is
the main reason for continuing to
take it
v
Cross-dependence – different drugs
within a pharmacological class can
generally maintain physical
dependence produced by another
member
DEFINITIONS
v
Sensitization – craving for the
drug
v
Withdrawal – symptoms are
opposite to the acute effects of
a drug
v
Detoxification – used to treat
physical dependence
§
“cold turkey” – abrupt stoppage of
the drug
§
“warm turkey” – gradual reduction in
drug dosage
Psychomotor stimulants
v
Drugs:
§
Cocaine
§
Amphetamine(
s)
§
Methylpenidat
e
§
Ephedrine
§
Cathinone
v
Effects
§
Mood
elevation
§
Wakefulness;
increased
alertness,
restlessness
§
Heightened
energy
§
Mild to
moderate
anorexia
§
Sleep
disturbance
§
Psychomotor stimulants
v
mechanism of action: indirect
agonists – increase synaptic activity
of the monoamines
v
withdrawal syndrome: lethargy.
Depression, hypersomnia, craving
v
Cocaine –
§
available as leaves, paste, salt, smokeable
base –
§
can be chewed, inhaled, snorted, rubbed on
mucosa (e.g. gums)
§ metabolized in plasma, Liver
§ “crack baby”
Amphetamines: shabu &
ecstasy
v
metabolized by Liver or excreted
unchanged
v
effects:
§
increased wakefulness,
§
anorexia,
§
Sympathomimetic: mydriasis,
vasoconstriction, tachycardia,
hypertension, hyperthermia,
hyperventilation,
§
Vivid hallucinations & paranoid
ideation
§
Euphoria, sense of well-being, self-
confidence
v
opiates
v
Opium – papaver (poppy plant)
v
Opiate alkaloids – morphine &
Codeine
v
Semi-synthetic opioids –
Heroin (diacetylmorphine)
v
Synthetic opioids –
§
phenylheptamines (Methadone),
§
phenylpiperidines (Fentanyl,
Meperidine),
§
morphinans (Levorphanol),
§
benzomorphans ( Pentazocine)
Opiates
v
opioid receptors:
§
mu,
§
delta,
§
kappa
v
Endogenous opioids:
§
endorphins,
§
enkephalins,
§
dynorphins,
§
endomorphins
Opiates
v
Opioid antagonists:
§
naloxone,
§
naltrexone
v
physiologic effects –
§
analgesia,
§
miosis,
§
constipation,
§
cough suppression

Opiates
v
Chronic use:
§
Tolerance
§
Sensitizations
v
Physical dependence
v
Pharmacological Tx of Opioid
abuse:
§
Substitution: Methadone,
Buprenorphine
§
Opioid antagonist: Naltrexone
marijuana
v
delta-9-tetrahydrocannabinol
(THC)

in the resin of Cannabis sativa
v
Cannabinoid receptors
v
Endogenous cannabinoids
v
Acute effects: euphoria &
exhiliration; relief of anxiety,
disinhibition, time distortion,
hunger/thirst, bloodshot eyes,
attention & memory
impairment, motor impairment
v
marijuana

Therapeutic uses: Dronabinol (Marinol)
v
Antiemetic/antinausea – esp. in CA
chemoTx
v
Appetite stimulant
v
Antispasmodic
v
Reduction of intraocular Pressure - in
Glaucoma
v
Analgesia – in tic doloreaux
v
Bronchodilation – in asthma
v
Neuroprotective – in seizures
Psychedelics / hallucinogens
v
Serotonin-like: LSD
v
Catecholamine-like:
§
Mescaline
§
Methoxyamphetamines: MDMA
v
Anticholinergic
§
Atropa belladona
§
Datura stramonium
§
Mandragora officinarum
§
Scopolamine, Hyoscyamine,
Atropine
v
Dissociatives
§
Phencyclidine (PCP, angel dust)
§
Ketamine
v
CAFFEINE & XANTHINES
v
Coffee : Coffea
arabica & C.
robusta
v
Tea: Camellia
(Thea)
sinensis
v
Chocolate:
Theobroma
cacao
v
Cola: Cola
acuminata

v
v
Effects:
§
Bronchodilatio
n
§
Increased HR,
BP
§
Arousal
v
High dose:
caffeinism,
panic
attacks;
tremors
nicotine
v
Nicotiana tabacum (Tobacco)
v
Receptors: nicotonic ACh
receptors
v
Effects
§
Psycomotor activity
§
Alertness attention
§
Cognitive function
§
Sensorimotor performance
§
Fluid retention
§
Tremors
§
Increased respiration
nicotine
v
Withdrawal: craving, dysphoria,
anxiety, irritability,
restlessness, impatience,
anger, increased appetite,
insomnia
v
Toxicity: cigarette smoke
v
Cancer: mouth, throat, larynx,
lungs, bladder, pancreas,
uterus,
Cns depressants &
alcohol
v
Ethyl Alcohol: Acetaldehyde
§
10 gm in 12 oz beer, 4 oz unfortified wine,
or 1.5 oz 80-proof liquor
§ rapidly absorbed in the stomach & small
intestines
§
Metabolized by the liver at the rate of
10gm/hr
• Acute intoxication: mainly affects the CNS &
Stomach
• 20-30mg/dL= powerful depressant effect on cortical
inhibitory centers= loss of inhibitions= “party”
syndrome; Euphoria; disordered cognitive & motor
functions
• 100mg/dL= legal level of intoxication= Ataxia
• 200-250mg/dL= narcosis= drowsiness

300-400mg/dL= coma; profound anesthesia; death
§ Chronic Alcoholism: induces injuries in all
tissues
§
Liver - most commonly & severely affected=
fatty change, acute hepatitis--- Cirrhosis
§ CNS – Wernicke’s encephalopathy- ataxia,
global confusion, ophthalmoplegia, loss of
neuropil & demyelination (vit B1 def) &
Korsakoff syndrome- profound memory
deficit both recent & remote; cerebellar
degeneration; cerebral atrophy
§
Fetal Alcohol Syndrome: microcephaly,
cardiac defects, mental deficiency, facial
malformations
§
Misc.: neuropathies; congestive
cardiomyopathy; ↑frequency of cancer in
the larynx, oropharynx, esophagus,
rectum, lung
CNS depressants
v
Drugs:
§
Bromide, Chloral hydrate
§
Barbiturates
§
Methaqualone
§
Benzodiazepines
v
sedative effect
v
toxicity: respiratory depression

v
Controlled Substances act 1990(1970)

Adverse drug reactions
v BLOOD (DYSCRACIAS)
§ Granulocytopenia
§ Aplastic anemia
§ Pancytopenia
§ Hemolytic anemia
§ thrombocytopenia
v CNS
§ Tinnitus, dizziness
§ Acute dystonic
reactions
§ Parkinson’s
syndrome
v CUTANEOUS
§ Urticaria
§ Petechia
§ Exfoliative
dermatitis
v
v BLOOD DYSCRACIAS
§ Anti-neoplastics
§ Immunosuppressant
s
§ Chloramphenicol
§ Quinidine
§ Methyldopa
v
CNS
§ Salicylates
§ Phenothiazine
antipsychotics
§ Sedatives
vCUTANEOUS
§ Sulfonamides
§ Hydantoin
§ Anti-neoplastics

Adverse drug reactions
vCARDIAC
§ Arrhythmias
§ Cardiomyopathy
§
v
HEPATIC
§ Fatty change
§ Cholestasis
§ Hepatocellular
damage
v
PULMONARY
§ Acute
Pneumonitis
§ Interstitial
fibrosis
§ Asthma
v
vCARDIAC
§ Theophylline
§ Hydantoin
§ Doxorubicin,
Daunorubicin
v
HEPATIC
§ Tetracycline
§ Chlorpromazine,
Estrogens
§ Halothane,
Acetaminophen,
INH
v
PULMONARY
§ Salicylates
§ Nitrofurantoin
§ Busulfan, Bleomycin
v
Adverse drug reactions
v
RENAL
§
Glomerulonephri
tis
§
Tubulointerstitial
nephritis
§
Acute tubular
nephritis
§

v
SYSTEMIC
§
Anaphylaxis
§ Lupus
erythematosus
syndrome
v
RENAL
§
Penicillamine
§ Phenacetin
§
Salicylates
§
Aminoglycosides,
Cyclosporine,
Amphotericin B
v
SYSTEMIC
§ Penicillin, Aspirin
§
Hydralazine,
Procainamide

Fatal drug reactions
v
Tricyclic anti-
depressants
§ Alprazolam
§
Ipramine,
Desipramine
§
Nortriptyline

v
Acetaminophen
v
Halothane
v
Aspirin
v
CNS depression
v
Hepatic necrosis
v
Hepatic necrosis
v
Metabolic
acidosis; Fluid
& Electrolyte
imbalance