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PHAR 230 > M6 L1 Narcotics > Flashcards

M6 L1 Narcotics Flashcards

1
Q

2 classifications of analgesics

A
  1. narcotic (opioids)
  2. non-narcotic (antipyretics)
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2
Q

4 types of opioids

A
  1. endogenous
  2. plant alkaloids
  3. semisynthetic
  4. synthetic
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3
Q

3 ex of endogenous opioids (less important to remember)

A

endorphins, enkephalins, dynorphins

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4
Q

2 ex of plant alkaloids opioids

A

morphine, codeine

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5
Q

3 ex of semisynthetic opioids

A

heroin, hydromorphone (common pain killer), buprenorphine

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6
Q

what are classified as natural opioids

A
  1. endogenous
  2. plant alkaloids
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7
Q

2 ex of synthetic opioids

A

methadone, pentazocine

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8
Q

how do opioids work?

A
  • bind to specific receptors in the CNS and other tissues
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9
Q

what are opioid receptors

A
  • G-protein coupled receptors
    Types:
    1. delta (δ) (1 and 2)
    2. kappa (κ) (1, 2, 3)
    3. mu (μ) (1, 2, 3)
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10
Q

mu receptors (μ)

A
  • analgesia
  • respiratory depression **(can kill pt w overdose)
  • sedation
  • euphoria
  • meiosis
  • reduced GI motility
  • physical dependence
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11
Q

delta receptors (δ)

A
  • analgesia
  • respiratory depression **(can kill pt w overdose)
  • affective behaviour
  • reinforcing actions
  • reduced GI motility
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12
Q

kappa receptors (κ)

A
  • analgesia
  • respiratory depression **(can kill pt w overdose)
  • sedation
  • dysphoria (pt won’t enjoy this) and hallucinations
  • meiosis
  • physical dependence
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13
Q

desirable effects of opioids

A
  • analgesia (can help w severe pain)
  • sedation
  • antitussive (especially of codeine, suppresses dry cough)
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14
Q

sometimes desirable effects of opioids

A
  • constipation (w diarrhea it would b good)
  • hypotension
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15
Q

undesirable effects of opioids

A
  • nausea/vomiting
  • respiratory depression
  • mental clouding, confusion -> coma
  • tolerance
  • addiction
  • physical dependence
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16
Q

when would you use opioids?

A
  • treatment of pain (analgesic effect)
  • anxiety
  • dry cough (codeine)
  • diarrhea (opium only)
  • opioid dependence (methadone and buprenorphine)
17
Q

why are opioids good as analgesics

A
  • strongest known
  • act on mu and kappa receptors mainly
  • variable dose w no upper limit

only use in: SEVERE pain
- acute (post-operative)
- chronic (palliative care, when dependence is not the main concern)

most annoying adverse effect: constipation*

gradual stoppage of drug to avoid withdrawal manifestations

18
Q

how do opioids work as pain killers?

A

2 main ways of attacks:

  1. Local Attacks
    - sensory nerves, they attack presynaptic neurons of the neurotransmitters involved in the pain process
    - block effect of any released transmitter in the postsynaptic neurons
  2. Central Attacks on CNS
    - inhibit pathways to block pain input, bc they are activated by opioids
    - if still pain happening if works on how it will receive pain by acting on the limbic system of the brain (emotions, memory, behaviour, etc)
19
Q

opioid tolerance

A

body will adapt to opioids -> decreased drug potency -> higher dose is needed to obtain same analgesic effect

20
Q

cross tolerance

A

tolerance to an opioid (ex: morphine) -> you’d also develop tolerance to other opioids (meperidine)

21
Q

addiction to opioids

A

physiological attachment to certain effects of opioids -> compulsive repeated use

22
Q

opioid physical dependence

A

develop opioid withdrawal syndrome after:
- stopping of drug
- administration of opioid antagonist

23
Q

what are some opioid withdrawal syndrome

A
  • CNS stim
  • tachypnea
  • tachycardia & hypertension
  • severe flulike illness
  • yawning, lacrimation, diarrhea
  • abdominal cramping, leg cramping
  • tremors and muscle twitching
  • piloerection
  • dilated pupils
24
Q

opioid antagonist

A

antagonist: naloxone

mixed agonists/antagonists: pentazocine

25
Q

what is naloxone

A
  • competitive opioid inhibitor
  • has no analgesic effect
  • causes withdrawal symptoms (so use in combo w other drugs)
  • antidote for opioid drug overdose
    diagnosis and treatment of opioid dependence
  • should always be available when opioids are being used thru IV
26
Q

what is pentazocine

A
  • has agonist action (analgesia)
  • has weak antagonist action
  • if used w opioid agonists (morphine) -> can induce withdrawal sympt
  • activates kappa but blocks mu receptors
27
Q

drug therapy of dependence for:
methadone or buprenorphine

A
  • same opioid effect -> prevent withdrawal manifestations
  • much less dependence
    (now pt is dependent, but better to b dependent on this than a stronger opioid (ex: heroin) then you let the amount of this decrease to cause pt to not be dependent)
28
Q

drug therapy of dependence: naloxone

A
  • opioid antagonistic effect
  • blocks drug-seeking behaviour
29
Q

how does buprenorphine work to stop opioid dependence?

A
  • act on mu not kappa receptors
  • buprenorphine will take the place the morphine, like musical chairs (competitive inhibition)
  • buprenorphine blocks opioids as it dissipates
30
Q

what is heroin (agonist or antagonist)

A

full agonist

31
Q

what is buprenorphine (agonist or antagonist)

A

partial agonist

32
Q

what is naloxone? (agonist or antagonist)

A

antagonist

33
Q

how does acute opioid toxicity appear (mild/early)

A
  • pinpoint pupils
  • hypothermia
  • hypoflexia (flaccid muscles)
  • hypotension and bradycardia
  • respiratory depression
34
Q

how does acute opioid toxicity appear (severe/late)

A
  • severe respiratory depression -> respiratory arrest
  • severe cardiovascular depression
  • seizures
  • coma
35
Q

Acute Opioid Toxicity (CPR-3H)

A

Coma
Pin point pupil
Respiratory depression
Hypotension
Hypothermia
Hyporeflexia

36
Q

treatment for acute opioid toxicity

A

naloxone (antidote)
- reverses toxic manifestations
- shorter half-life, repeat dose
- general supportive measures

PHAR 230 (31 decks)

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