Jenny B.

Jimenez, BSMT
3A

Drugs of Abuse
 def. drugs or chemicals which are taken
repeatedly in a pattern & amount that interferes
with one’s health or normal function
 used for a variety of reasons; they have multiple
effects, usually producing a feeling of well-being in
the user repeated use higher & higher dose
needed to replicate the feeling  emotional
dependence, & in some, true physical dependence
 Classification of Drugs of Abuse
Opiates & Opioids: morphine, codeine,
heroin, meperidine (Demerol),
hydromorphone
Sympathomimetic stimulants: cocaine,
amphetamines, metamphetamines, MDMA
Depressants: barbiturates, benzodiazepines,
ethyl alcohol
Hallucinogens: LSD, mescaline, MDMA,
Others: PCP, marijuana, nicotine
 Classification of drugs of abuse
CNS actions
 Stimulants: amphetamine, caffeine, nicotine,
cocaine -
 Depressants : barbiturates, benzodiazepines,
ETOH
 Analgesics: narcotics (opiates & opioids)
 Sedative–Hypnotics: relaxants, induce sleep:
alcohol; anti-anxiety agents-tranquilizers;
nonbarbiturates- Halcion, Quaalude; long-acting
barbiturates – Phenobarbital; short-acting
barbiturates - Seconal
 Legal classification
Schedule 1: high abuse, no recognized
medical use, lack of safety
Schedule 2: high abuse, medical utility, high
dependency risk
Schedule 3: lower abuse, medical utility,
moderate dependency risk
Schedule 4: limited abuse, high medical
utility, limited dependency risk
Schedule 5: minor problems
 Drugs of abuse
Schedule 3:
1:
 Amphetamine
Heroin
 Barbiturates
LSD
 Valium
MDMA
 Xanax
Marijuana
 Anabolic
Methaqualone
steroids
Schedule
 Codeine 2:
Schedule
 Opium 4:
 Chloral
Morphinehydrate
 Meprobamate
Coca
 Paraldehyde
Cocaine
 phenobarbital
Methadone
Schedule
 Methampethamine
5: limited amts
 DEFINITIONS
 Positive reinforcement: release of positive
reinforcement neurotransmitters e.g. dopamine,
endorphins
 Tolerance: reduced effect with repeated use of the
drugneed for progressively higher doses to
produce the same effect; due to downregulation of
receptors, changes in receptors, exhaustion of
neurotransmitters, increased metabolic
degradation, physiological adaptation
 Cross-tolerance: for drugs of the same class
 DEFINITIONS
 Dependence- compulsion to take the drug
repeatedly
 Psychological dependence – positive reinforcement
causes a compulsion to take the drug
 Physical dependence – negative reinforcement –
distress upon stopping the drug (withdrawal) is
the main reason for continuing to take it
 Cross-dependence – different drugs within a
pharmacological class can generally maintain
physical dependence produced by another
member
 DEFINITIONS
Sensitization – craving for the drug
Withdrawal – symptoms are opposite to the
acute effects of a drug
Detoxification – used to treat physical
dependence
 “cold turkey” – abrupt stoppage of the drug
 “warm turkey” – gradual reduction in drug dosage
 Psychomotor stimulants
Effects
Drugs:
 Mood elevation
Cocaine
 Amphetamine(s)
Wakefulness; increased alertness, restlessness
 Methylpenidate
Heightened energy
 Ephedrine
Mild to moderate anorexia
 Cathinone
Sleep disturbance
 Psychomotor stimulants
 mechanism of action: indirect agonists – increase
synaptic activity of the monoamines
 withdrawal syndrome: lethargy. Depression,
hypersomnia, craving
 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
 metabolized by Liver or excreted
unchanged
 effects:
 increased wakefulness,
 anorexia,
 Sympathomimetic: mydriasis, vasoconstriction,
tachycardia, hypertension, hyperthermia,
hyperventilation,
 Vivid hallucinations & paranoid ideation
 Euphoria, sense of well-being, self-confidence
 opiates
Opium – papaver (poppy plant)
Opiate alkaloids – morphine & Codeine
Semi-synthetic opioids – Heroin
(diacetylmorphine)
Synthetic opioids –
 phenylheptamines (Methadone),
 phenylpiperidines (Fentanyl, Meperidine),
 morphinans (Levorphanol),
 benzomorphans ( Pentazocine)
 Opiates
 opioid receptors:
 mu,
 delta,
 kappa
Endogenous opioids:
 endorphins,
 enkephalins,
 dynorphins,
 endomorphins
 Opiates
Opioid antagonists:
 naloxone,
 naltrexone
 physiologic effects –
 analgesia,
 miosis,
 constipation,
 cough suppression
 Opiates
Chronic use:
 Tolerance
 Sensitizations
Physical dependence
Pharmacological Tx of Opioid abuse:
 Substitution: Methadone, Buprenorphine
 Opioid antagonist: Naltrexone
 marijuana
delta-9-tetrahydrocannabinol (THC)
in the resin of Cannabis sativa
Cannabinoid receptors
Endogenous cannabinoids
Acute effects: euphoria & exhiliration;
relief of anxiety, disinhibition, time
distortion, hunger/thirst, bloodshot eyes,
attention & memory impairment, motor
impairment
 marijuana
Therapeutic uses: Dronabinol (Marinol)
 Antiemetic/antinausea – esp. in CA chemoTx
 Appetite stimulant
 Antispasmodic
 Reduction of intraocular Pressure - in Glaucoma
 Analgesia – in tic doloreaux
 Bronchodilation – in asthma
 Neuroprotective – in seizures
Psychedelics / hallucinogens
 Serotonin-like: LSD
 Catecholamine-like:
 Mescaline
 Methoxyamphetamines: MDMA
 Anticholinergic
 Atropa belladona
 Datura stramonium
 Mandragora officinarum
 Scopolamine, Hyoscyamine, Atropine
 Dissociatives
 Phencyclidine (PCP, angel dust)
 Ketamine
 CAFFEINE & XANTHINES
Effects:
Coffee : Coffea arabica & C. robusta
 Bronchodilation
Tea: Camellia (Thea) sinensis
 Increased HR,
Chocolate: BP
Theobroma cacao
 Arousal
Cola: Cola acuminata
High dose: caffeinism, panic attacks;
tremors
 nicotine
Nicotiana tabacum (Tobacco)
Receptors: nicotonic ACh receptors
Effects
 Psycomotor activity
 Alertness attention
 Cognitive function
 Sensorimotor performance
 Fluid retention
 Tremors
 Increased respiration
 nicotine
Withdrawal: craving, dysphoria, anxiety,
irritability, restlessness, impatience, anger,
increased appetite, insomnia
Toxicity: cigarette smoke
Cancer: mouth, throat, larynx, lungs,
bladder, pancreas, uterus,
Cns depressants & alcohol
 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
 Drugs:
 Bromide, Chloral hydrate
 Barbiturates
 Methaqualone
 Benzodiazepines
 sedative effect
 toxicity: respiratory depression

 Controlled Substances act 1990(1970)

 Adverse drug reactions
 BLOOD DYSCRACIAS(DYSCRACIAS)
 Anti-neoplastics
Granulocytopenia
 Immunosuppressants
Aplastic anemia
 Chloramphenicol
Pancytopenia
 Quinidine
Hemolytic anemia
 Methyldopa
thrombocytopenia

 CNS
CNS
 Tinnitus, dizziness
Salicylates
 Acute dystonic antipsychotics
Phenothiazine reactions
 Parkinson’s
Sedatives syndrome

 CUTANEOUS
CUTANEOUS
 Urticaria
Sulfonamides
 Petechia
Hydantoin
 Exfoliative dermatitis
Anti-neoplastics
 Adverse drug reactions
 CARDIAC
 CARDIAC
 Theophylline
 Arrhythmias
 Hydantoin
 Cardiomyopathy
 Doxorubicin, Daunorubicin
 HEPATIC
 HEPATIC
 Tetracycline
 Fatty change
 Chlorpromazine, Estrogens
 Cholestasis
 Halothane, Acetaminophen, INH
 Hepatocellular damage
 PULMONARY
 PULMONARY
 Salicylates
 Acute Pneumonitis
 Nitrofurantoin
 Interstitial fibrosis
 Busulfan, Bleomycin
 Asthma
 Adverse drug reactions
RENAL RENAL
 Glomerulonephritis  Penicillamine
 Tubulointerstitial  Phenacetin
nephritis  Salicylates
 Acute tubular nephritis  Aminoglycosides,
Cyclosporine, Amphotericin
B

SYSTEMIC SYSTEMIC
 Penicillin, Aspirin
 Anaphylaxis
 Hydralazine, Procainamide
 Lupus erythematosus
 Fatal drug reactions
Tricyclic anti-depressants
CNS depression
 Alprazolam Hepatic necrosis
 Ipramine, Desipramine Hepatic necrosis
 Nortriptyline
Metabolic acidosis;
Fluid & Electrolyte
Acetaminophen imbalance
Halothane
Aspirin