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Flashcards in Drugs with abuse potential Deck (26):
1

THC/Cannabis: Epidemiology

Most common abuse in high schoolers
Surpass tobacco usage
M > F

2

THC: Formulations

Traditional Marijuana – 10% THC
Hashish > 10%
Hash Oil – 50%

3

THC: Metabolism

Rapidly metabolized by liver to 11-OH-∆9 -THC, which is highly active in man.
Metabolized to 9-nor-COOH-THC which is inactive.
Metabolites excreted in urine and feces. They are detectable in urine for many days. 

4

THC: Pharmacokinetics

Smoked it reaches brain in 15 to 30 seconds.

3-5 times more potent smoked than when ingested
Oral onset of action is about 30 min.

Metabolized and redistributed in fat
Slowly leaves body.
Duration of action 1 to 6 hours

Plasma half-life - 20-50 hours; 20% remains in body after 5 days and is not detectable at 30 days

5

THC: MoA

CB1 receptor: High in cerebellum hippocampus and basal ganglia, low in hypothalamus
CB2 receptor: Peripheral tissue
Negatively coupled to adenylyl cyclase via Gi – Inhibits transmitter release
Affinity for receptor correlates with psychoactive potency of cannabinoid agonists

6

THC: Effects

Euphoria, memory impairment, perceptual/motor alterations

CV (Tachycardia, orthostatic hypotension, angina)

Pulm (Bronchodilation, lung irritant, decrease alveolar macrophage activity, decrease in ciliary function)

Reproductive (Lowers testosterone/sperm, LHRH release decreased (low FSH and LH), prolactin release decreased in females (abnormal menstrual), hazard to marginally fertile)

Psychopathologic (Acute anxiety reaction, transient paranoia, exacerbation of schizophrenia, diffuse acute brain syndrome – clouding of consciousness and memory, perceptual and sleep disorders, amotivational syndrome) 

7

THC: Withdrawal

Restlessness, irritability and mild agitation, sleep difficulties, decreased appetite and nausea, craving

8

THC: Medical Indications

Nausea, AIDS wasting syndrome – Dronabinol
MS pain tx. and cancer pain – THC/Cannabidiol mixture in Canada
Weight loss drug – CB1 antagonist, now removed from market

9

K2 or Spice

MoA
Legality/Scheduling

THC-like CB1 agonist activity
Not DEA scheduled

10

PCP/Ketamine: Pharmacokinetics

Rapid/complete absorption
Plamsa T1/2 12 to 24 hours (overdose up to 72 hours)
Hydroxylation and conjugation in liver
Excretion in urine, primarily as biotransformation products

11

PCP/Ketamine: Cardiovascular Effects

Tachycardia
HTN
Potentiation of catecholamines

12

PCP/Ketamine: CNS effects

Ketamine less potent, shorter duration
Small doses – Drunken state with numbness of extremities
Moderate doses – Analgesia and anesthesia
Psychic state – Resembles sensory isolation except sensory impulses reach neocortex
Catalepoid motor phenomenon
Large doses may produce convulsions

13

PCP/Ketamine: MoA

NMDA Antagonist

14

PCP: Overdose

CNS Manifestations: Anxiety, aggression, halucinations, dysphoria, convulsions, delirium
Sympathomimetic: Tachycardia, HTN crisis

15

PCP/Ketamine: Treatment

Vital sign support
Gastric suction
Acidify urine
Diazepam/Anti-HTN agent
Haloperidol

16

LSD - Indoleamine: Pharmacokinetics

Less than 1 % crosses Blood-Brain barrier
Onset -15 to 20 minutes, duration - 12 hours 

17

LSD - Indoleamine: Effects

Sympathomimetic - Tachycardia, increased BP, psychomotor stimulation

Sensory and subjective effects
Altered perception - particularly visual
Lability of mood
Impaired judgment

Tolerance and cross tolerance

18

LSD-Indoleamine: Toxicity

Acute reactions
Hallucinations, anxiety, panic and depersonalization.
< than 24 hours
Quiet environment, BDZs for sedation

Flashbacks - days to years later, can be associated with drug use.

Neurotoxicity - 5-HT damage may be associated with phenethylamine type drugs such as MDMA

19

MDMA: Effects

Induces feelings of “well-being and connection”
Altered time perception
Pyschomotor stimulation, restlessness, bruxisim, anorexia, sweating, tremor

20

MDMA: Pharmacokinetics

Typical oral dose 100-150 mg
Onset of action 20 - 40 minutes; duration 3-4 hours 

21

MDMA: 
Hangover effect
Neurotoxic against which neurons

Hangover - anhedonia
Neurotoxicity - serotonin neurons

22

GHB: Endogenous pharmacology

Found in brain, precursor and metabolite of GABA
May have own receptor
Can be made in body from GBL

23

GHB: Pharmacokinetics

Typical dose about 1 - 1.5 g
Effects last about 3 hours 

24

GHB: Effects

Primarily a depressant - induces a state of relaxation and tranquility
Interacts with ethanol
Overdose characterized by drowsiness, ataxia, nausea and vomiting
Higher doses - loss of bladder control, temporary amnesia, clonus and seizures.

25

Salvia Divinorum
Pharmacology
MoA
Pharmacokinetics

Pharmacology: Oral psychedelic
MoA: Kappa opiod agonist
Pharmacokinetics: Short duration of action – 20 to 45

26

Examples of "legal" drugs

Prescription Drugs
OTC drugs containing dextromethorphan

 “Bath Salts”
Mephedrone
Stimulants found in Khat
Now scheduled