Drugs of Abuse Flashcards
What is recreational drug use?
use of a pharmacologically active agent for purposes other than its intended medicinal or other purpose
what is tolerance?
a state at which there is no longer the desired response to the drug; to achieve the desired response, more drug is required
how long does it take before tolerance is typically lost?
10-14 days
what is reverse tolerance?
sensitization; requires less drug to achieve the desired response
what is functional tolerance?
aka pharmacodynamic tolerance
change in the post synapses of the CNS
desensitization of receptors is short; down regulation of receptors/signalling pathways is long
what is metabolic tolerance?
aka pharmacokinetic tolerance
adaptation of the metabolic machinery to repeated exposure to a drug (similar to drug resistance mechs)
what is withdrawal?
a maladaptive behavioural change, with physiological and cognitive concomitants, that occurs when blood or tissue concentrations of a substance decline in an individual who had maintained prolonged heavy use of the substance
what are some drug classes that are known to cause withdrawal?
alcohol opioids hypnotics anxiolytics sedatives amphetamines nicotine cocaine cannabis
what is dependence?
the state at which the user functions normally only when taking the medication
reinforced by withdrawal symptoms
what is an example of physiological dependence?
withdrawal of alcohol from an alcoholic can be life threatening
what is an example of psychological dependence?
repeated crack cocaine use; drug seeking habits in spite of risks; repeated dosing related need to keep the high
implies addiction
what are 5 characteristics of addiction?
1) Inability to consistently abstain
2) Impaired in behavioural control
3) craving: or increased “hunger” for drugs or rewarding experiences
4) diminished recognition of significant problems with one’s behaviours and interpersonal relationships
5) a dysfunctional emotional response
what is the difference between opioids and opiates?
opioids - fully synthetic; umbrella term
opiates - synthetic derivatives from opium poppy
what are some other effects opioids have on the body besides euphoria?
respiratory depression
dependence
prominent effect on GI tract
miosis (excessive constriction of eye pupil)
which receptor are opioids selective for? what is the one exception?
mu receptor
pentaocine (kappa receptor)
what are some desirable effects of opioid use?
analgesia euphoria sedation relief of anxiety depress cough reflex
what are some undesirable effects of opioid use?
dysphoria (dizziness, nausea) vomiting constipation biliary tract spasm urinary retention withdrawal respiratory depression
what are the available routes of administration for opioids
oral IV IM smoked intranasal transdermal
briefly describe the PK of opioids
readily absorbed orally lipid solubility affects distribution and CNS levels First pass metabolism: glucoronidation renal elimination enterohepatic recycling
what are some effects of opioid toxicity?
CNS: convulsions
Resp: rate/volume/exchange depression, decreased resp responsiveness
CV: orthostatic hypotension, stroke, ECG abnormalities
GI: decreased motility, intestinal obstruction, increased biliary tract pressure
what symptoms will be experienced in the first 8-12h of opioid abstinence syndrome? (4pts)
lacrimation
perspiration
yawning
rhinorrhea
what symptoms will be experienced in the first 12-14h of opioid abstinence syndrome? (7pts)
irritability piloerection restlessness weaknesses mydriasis tremor anorexia
what symptoms will be experienced in the first 48-72h of opioid abstinence syndrome? (13 pts)
increased irritability increased HR insomnia marked anorexia hypertension sneezing hyperthermia hyperpnea aching muscles hot and cold flashes nausea/vomiting piloerection abdominal cramps
how long does opioid abstinence syndrome typically last?
7-10 days
what is acetyl fentanyl?
designer drug that is 5-15x more potent than heroin
what is some effects of acetyl fentanyl?
euphoria
altered mood
drowsiness
resp depression
what is the problem with acetyl fentanyl?
responsible for multiple deaths
what are some effects of cannabis that cause it to be used recreationally
dysphoria and hallucinations
what is the major psychoactive constituent in cannabis?
THC
what is the MoA of cannabis?
bind to cannabinoid receptors CB1 and CB2
CB1 associated with MAP kinase/adenylyl cyclase/K-channel
what is the approx % of THC in leaves, hashish, and oil extract?
leaves: 2-5%
hashish: 5-25%
oil extract: >20%
what are some CNS effects of cannabis?
euphoria
lack of concentration
motor function impairment (reaction time)
impaired attention, memory, learning
users at heightened anxious state (CB1 in amygdala)
paranoia
what are some CV effects of cannabis?
increased HR decreased BP (vasodilation)
what are some resp effects of cannabis?
deceased resp rate
bronchodilation
lung damage (smoking)
What are two drug interactions that can occur with cannabis?
cocaine/amphetamines - increased hypertension, tachycardia, possible cardiotoxicity
CNS depressants - additive effect
briefly describe the PK of cannabis
smoking: rapid onset and 18-50% bioavailability
oral: slower onset, 6-18% bioavailability, first pass effect
THC is lipophilic; enterohepatic circulation; t1/2 = 3 days in chronic users
what are the desirable effects of cocaine?
locomotor stimulation euphoria elevation of mood increased energy alertness, sociability confidence sexual arousal decreased need for food
what are some undesirable effects of cocaine?
dysphoria (state of unease/dissatisfaction) irritability drug craving paranoia assaultive behaviour hallucinations hyperthermia psychosis death
what is cocaine?
a stimulant that inhibits the reuptake of NE, DA, and 5-HT
how do DA, NE, and 5-HT contribute to the side effects of cocaine?
DA - localized in the striatum; reward and control of motivation; hyperthermia
NE - adrenergic (tachycardia)
5-HT - dysphoria, depression and craving
what is the difference between crack cocaine and cocaine?
cocaine - hydrochloride salt
crack cocaine - free base
when is the peak effect of cocaine seen in the following forms: IV, smoking, intranasal
IV = 5min smoking = 7min intranasal = 20min
what is the time to decrease effect to 1/2 max of cocaine in the following forms: IV, smoking, intranasal
IV = 15min Smoking = 17min Intranasal = 27min
what is the duration of action for cocaine?
10-30min
what are some of the withdrawal symptoms for cocaine?
fatigue
irritability
loss of sexual desire
muscle pain
what are some symptoms of cocaine toxicity? (9pts)
1) increased muscular activity and vasoconstriction (hyperthermia)
2) psychosis
3) grand-mal convulsions
4) coma
5) vasoconstriction
6) ventricular arrhythmia
7) MI
8) chenyn-stoke breathing
9) respiratory paralysis
what are some of the combination drugs that include cocaine?
speedball: cocaine and heroin and alcohol
tick: cocaine and phencyclidine
turbo: cocaine and marijuana
what are some of the symptoms that can occur with chronic cocaine use? (9pts)
1) malnutrition
2) violent protective behaviour
3) hyperkinetic behaviour
4) distorted perception
5) rhinitis (nasal septum performation)
6) SoB
7) cold sweats
8) tachycardia
9) MI; stroke (vessel rupture)
how does ecstasy cause its effects on the body?
increases 5-HT, DA, and NE release and inhibits serotonin receptors
what are the positive effects of ecstasy?
empathy
well-being
reduced anxiety
what are the adverse effects of ecstasy?
hyperthermia dehydration increased BP depression risk of serotonin syndrome
what is the difference between the S and R enantiomers of ecstasy in regards to effects on the body?
S is far more neurotoxic than R
what are the effects of bath salts on the body? (15pts)
1) paranoia, violent behaviour
2) hallucinations
3) delusions
4) suicidal thoughts
5) seizures
6) panic attacks
7) chest pain
8) N/V
9) Increased HR
10) increased BP
11) increased body temp
12) rhabdomyolysis
13) multiple organ failure
14) coma
15) death
give an example of a bath salt
mephedrone
