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Pharmacology > Drugs of Abuse > Flashcards

Drugs of Abuse Flashcards

1
Q

What is drug tolerance?

A
  • a state at which there is no longer the desired response to the drug
    Progressive model: to achieve the desired response, more drug is required
  • development of tolerance is not necessarily an addiction
  • tolerance is typically lost in 10-14 days
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2
Q

What is reverse tolerance?

A

Sensitization

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3
Q

What is functional tolerance?

A
  • aka pharmacodynamic tolerance
  • change in the post synapses of the CNS
  • stimulatory and inhibitory pathways
  • exposure to psychoactive drugs (could also mean hormone)
  • desensitization of receptors (short term)
  • down regulation of receptors/signalling pathways (long term)
  • cross tolerance
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4
Q

What are examples of post synapse receptors?

A

G protein, ionotropic, extrasynaptic proteins

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5
Q

What is metabolic tolerance?

A
  • aka pharmacokinetic tolerance
  • adaptation of the metabolic machinery to repeated exposure to a drug
  • similar to drug resistance mechanism
  • enzyme induction
  • drug metabolism:
    • CYP P450, glucuronidation
  • cross tolerance: drug metabolized similarly
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6
Q

What is drug withdrawal?

A
  • 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
  • after developing unpleasant withdrawal symptoms, the person is likely to take the substance to relive or to avoid these symptoms
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7
Q

What are some common drug classes and bring physiological sx of withdrawal?

A
  • alcohol
  • hypnotics
  • anxiolytics
  • opioids
  • sedatives
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8
Q

What is the definition of dependence?

A
  • a state at which the user functional normally only when taking the drug
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9
Q

Withdrawal symptoms ____ dependence and are a response of the body to less drug

A

re-inforce

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10
Q

What kind of dependence implied addition?

A

psychological dependence

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11
Q

What is addition characterized by? (the ABCDE’s of addiction)

A
  • Inability to ABSTAIN
  • impairment in BEHAVIOURAL control
  • CRAVING or increased hinger for drugs or rewarding experiences
  • DIMINISHED recognition of significant problems with one’s behaviours and interpersonal relationships
  • a dysfunctional EMOTIONAL response
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12
Q

Opiates can be what? (synthetic, plant extracts or semi-synthetic) What are opioids? What is heroin? Morphine? Fentanyl?

A
  • opiates: plant extracts and semi-synthetic
  • opioids: semi-synthetic
  • heroin: semi-synthetic
  • morphine: plant extract
  • fentanyl: synthetic
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13
Q

What are the 3 types of endogenous opioids?

A
  • enkephalins, endorphins and dynorphins
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14
Q

When is there a euphoric effect associated with opioids?

A
  • when there is recreational use of them
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15
Q

What are the other effects that opioids produce?

A
  • respiratory depression
  • variable euphoric effect (the high)
  • dependence
  • prominent affect on the GI tract
  • miosis
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16
Q

Opioids are all similar in pharmacology but differ in what regard?

A
  • duration of action
  • oral availability
  • relative potency
  • adverse effect profile
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17
Q

What are the different opioid receptors?

A

mu, kappa and delta

most opioids are selective for the Mu receptor

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18
Q

What are the desirable effects of opioids?

A
  • analgesia
  • euphoria
  • sedation
  • relief on anxiety
  • cough suppression
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19
Q

What are the undesirable effects of opioids?

A
  • dysphoria
    • dizziness
    • nausea
  • vomiting
  • constipation
  • biliary tract spasm
  • urinary retention
  • withdrawal
  • respiratory depression
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20
Q

What are the most common findings associated with opioid overdose on an autopsy?

A
  • pulmonary congestion and frothing of the mouth
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21
Q

____ affects distribution of opioids and CNS levels

A

lipid solubility

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22
Q

What are the stages of first pass metabolism in opioids?

A

glucuronidation (liver) and active metabolites

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23
Q

_____ recirculation happens with opioids?

A

enterohepatic

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24
Q

What are the CNS effects of opioid tonicity?

A
  • convulsions (delta receptor dependent and targets to hippocampal pyramidal cells)
  • meperidine metabolism to normeperidine
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25
Q

What are the respiratory effects of opioid toxicity

A
  • depression of rate, volume and exchange

- decreased respiratory responsiveness

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26
Q

What are the cardiovascular effects of opioid toxicity?

A
  • orthostatic hypotension
  • stroke
  • ECG abnormalities
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27
Q

What are the GI effects of opioids toxicity?

A
  • decreased motility
  • intestinal obstruction
  • increased biliary tract pressure
28
Q

What happens in the first 8-12 h of opioid abstinence syndrome?

A
  • lacrimation, perspiration, yawning and rhinorrhea
29
Q

What happens in the first 12-14 h of opioid abstinence syndrome?

A
  • irritability, piloerection, restlessness, weakness, mydriasis, tremor, anorexia
30
Q

What happens in the first 48-72 hours of opioid abstinence syndrome?

A
  • irritability, insomnia, marked anorexia, sneezing, hyperthermia, hyperpnea, aching muscles, increased heart rate, hypertension, hot and cold flashes, nausea/vomiting, piloerection, abdominal cramps
31
Q

How many days does opioid abstinence syndrome last for?

A

7-10 days

32
Q

What percentage of marijuana users become addicted?

A

9% (this number increases in those that start young and also in those that use it daily)

33
Q

What is the long term risk associated with marijuana use?

A
  • overall decrease in cognitive performance

- higher chance of lifetime addiction

34
Q

What is the major psychoactive component of cannabis?

A

THC (delta-9-tetrahydrocannabinol)

35
Q

What is the mechanism of action of cannabis?

A

cannabinoid receptors: CB1, CB2

  • endogenous cannabinoids: anadamide and 2-arachidonyl glycerol
  • CB1: MAP kinase/adenylyl cyclase/K channel-linked
36
Q

What is the THC % of leaves? Hashish? High potency oil?

A
  • leaves: 2-5%
  • Hashish: 5-15 % TH
  • high potency oil: up to 98%
37
Q

What are the CNS effects of cannabis?

A
  • euphoria
  • lack of concentration
  • motor function impairment (reaction time): driving under the influence
  • impaired attention, memory and learning
  • users at a heightened anxious state
  • paranoria
38
Q

What are the coronary effects of cannabis?

A
  • increased HR

- decreased BP (vasodilation)

39
Q

What are the respiratory effects of cannabis?

A
  • decreased respiratory effects
  • bronchodilation
  • lung damage
40
Q

What are the drug interactions that can be observed with cannabis?

A
  • cocaine and amphetamines: increased hypertension, tachycardia and possible cardiotoxicity
  • CNS depressants: impaired driving enhanced with alcohol
41
Q

What is the onset bioavailability of cannabis in smoking? When you take it orally?

A
  • smoking: rapid onset-minutes
    18-50% bioavailability
  • oral: slower onset (1-5h)
    6-18% bioavailability
42
Q

When dosing cannabis orally, the liver makes it hard to make bioavailable due to the ____

A

first pass effect

43
Q

THC is lipophilic and undergoes ______ circulation

A

enterohepatic

44
Q

What is the urinary t1/2 of the 11-carboxy-THC (as glucuronide)

A

3 days in chronic users

45
Q

What are the desirable effects of cocaine?

A
  • locomotor stimulation
  • euphoria
  • elevation of mood
  • increased energy
  • alertness, sociability
  • confidence
  • sexual arousal
  • decreased need for food
46
Q

What are the undesirable effects of cocaine?

A
  • dysphoria
  • irritability
  • drug craving
  • paranoia
  • assaultive behaviour
  • hallucinations
  • hyperthermia
  • psychosis
  • death
47
Q

What is the effect of cocaine?

A

works as a stimulant (inhibits reuptake of NE, DA and serotonin)

  • DA - localized in the striatum (reward and control of motivation) some side effects, hyperthermia
  • NE - adrenergic (tachycardia)
  • 5HT - dysphoria; depression and craving seen in withdrawal
48
Q

What is the route of administration of cocaine?

A

hydrochloride salt vs free base (crack)

49
Q

What is the purity of cocaine HCl vs crack cocaine?

A

cocaine HCl: 20-95%

crack cocaine: 20-80%

50
Q

What is the peak effect in cocaine blood level after IV? After smoking? After intranasal use?

A
  • 5 min after IV
  • 7 min after smoking
  • 20 minutes after intranasal use (dose dependent)
51
Q

What is the duration of action of cocaine? What does this lead to?

A
  • short t1/2 of 10-30 minutes and this leads to a binge use for hours or days
52
Q

What causes the crash in cocaine?

A

depletion of NE, DA

53
Q

What are the most common signs of cocaine withdrawal?

A

fatigue, irritability, loss of sexual desire, muscle pain, etc

54
Q

What are the toxic symptoms that high doses and chronic use of cocaine can lead to?

A
  • anxiety, insomnia, irritability, paranoia, suspiciousness (toxic paranoid psychosis)
55
Q

What are the symptoms of acute cocaine toxicity

A
  • increased muscular activity and vasoconstriction (hyperthermia), pronounced CNS stimulation (psychosis, grand-map convulsions, coma), cardiovascular overstimulation (vasoconstriction, ventricular arrhythmia, MI), respiratory dysfunction (paralysis)
56
Q

What are the toxicity symptoms associated with chronic cocaine use?

A
  • malnutrition
  • psychiatric disturbance
    (violent behaviour, hyperkinetic behaviour)
  • rhinitis
  • shortness of breath
  • cold sweats
  • cardiovascular toxicity
    (tachycardia, vessel rupture, MI, stroke, tolerance to cardiovascular affects does not occur during a cocaine run)
57
Q

What is the action of amphetamines and methamphetamine?

A

stimulants- promotes synthesis and release of DA, serotonin and NE

58
Q

What are some examples of toxicity induced by methamphetamines and amphetamines?

A
  • parasitosis
  • meth mouth
  • cardiac toxicity, endocarditis, aortic dissection, dilated cardiomyopathy, aneurisms
59
Q

What are the respective half life of amphetamine and methamphetamine?

A

Amphetamine: 7-34 hours
Methamphetamine: 12-34 hours

60
Q

What are the 3 other drugs that get metabolized to amphetamine and methamphetamine?

A
  • selegeline
  • faprofazone
  • benphetamine
61
Q

What effect does ecstasy have on the NT in the brain?

A
  • increases 5HT, DA and NA release

- inhibits serotonin transporters, neurotoxic to serotonin neurons

62
Q

What are the positive effects of

ecstasy?

A

empathy, well being, reduced anxiety

63
Q

What are the adverse effects of ecstasy?

A

hyperthermia, dehydration, increased blood pressure, depression, risk of serotonin syndrome

64
Q

MDMA is considered to be _____ because it causes damage to the serotonin nerve terminals

A

neurotoxic

65
Q

What are the common effects of bathsalts?

A
  • paranoia and violent behaviour
  • hallucinations
  • delusions
  • suicidal thoughts
  • seizures
  • panic attacks
  • chest pain
  • nausea and committing
  • increased heart rate
  • increased bp
  • increased body temperature
  • rhabdomyolysis (skeletal muscle tissue breakdown)
  • multiple organ failure
  • coma
  • death

Pharmacology (23 decks)

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