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Pharmacology > pain and opioid analgesics > Flashcards

pain and opioid analgesics Flashcards

1
Q

drugs that relieve pain without major impairment of other senses

A

analgesics

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2
Q

block all sensation

A

anesthetics

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3
Q

the path of the ‘pain signal’

A

nociceptor detects painful stimuli–>synapse at dorsal horn in spinal cord–>ascending pathway to brain

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4
Q

how can pain signaling be decreased by descending inhibition?

A

decending pathways from medulla cause release of enkephalins (endogenous opioids)

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5
Q

how is pain signaling increased by peripheral and central sensitization?

A

something not normally painful becomes painful (showering after sunburn–>allodynia)

a normally painful stimulus is more painful that usual (pricked with a pin–>hyperalgesia)

causes are both peripheral AND central–>tissue damage, inflammation, nerve damage, enhanced ascending pathway activity (central sensitization)

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6
Q

what are the NTs involved in pain transmission w/in the spinal cord?

A
  1. glutamate–> directly acts on AMPA and NMDA receptors, and directly depolarizes post-synaptic neuron
  2. substance P–> peptide that allows channels to open more readily
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7
Q

what are the major mechanisms for pain control?

A
  1. activate opioid receptors (body’s natural pain control mechanism)
  2. decrease production of inflammatory mediators that sensitize pain fibers: NSAIDs
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8
Q

opioids

A

cmpds that activate the body’s endogenous opioid receptors to produce analgesia (morphine and codeine)

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9
Q

opioid receptors and endogenous ligands

A

mu: responsible for most analgesic effects
kappa: dysphoria and hallucination at high doses
delta: not well understood, maybe role in analgesia?
endogenous peptide ligands: endorphins, enkephalins, dynorphins

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10
Q

what type of receptors are the opioid receptors?

their cellular and physiological effects?

A

GPCR coupled to Gi

cellular: inhibit adenylyl cyclase–>decrease cAMP–>open K+ and close Ca2+ channels
physiological: inhibition of NT release at prononiceptive synapses; release of inhibition on descending pathways (‘release th brakes’)

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11
Q

acts of opioids on brain, spinal cord, and peripheral nociceptors, brainstem

A

brain: decreased emotional suffering
spinal cord: decreased activation of ascending pathways
peripheral nociceptors: decreased activation
brainstem: increased activity of descending inhibitory pathways

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12
Q

opioid adverse effects

A
  • respiratory depression
  • abuse/addiction
  • pruritis
  • N/V, constipation
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13
Q

morphine

A
  • opioid natural/semisynthetic

- prototype drug

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14
Q

hydromorphone (dilauded)

  • efficacy to morphine?
  • potency compared to morphine?
  • water solubility characteristic?
A
  • opioid natural/semisynthetic
  • simillar efficacy to morphine
  • approx. 10x potency
  • better water solubility allows lower IV volume
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15
Q

oxycodone

  • efficacy?
  • good ___ ____
A
  • opioid natural/semisynthetic
  • somewhat lower efficacy
  • good oral bioavailability
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16
Q

codeine

  • efficacy?
  • prodrug issue?
A
  • opioid natural/semisynthetic
  • low efficacy
  • prodrug susceptible to CYP2D6 pharmacogenetics
17
Q

fentanyl

  • fast or slow acting?
  • potent vs. not?
  • short or long duration of action?
  • what is it used for? transdermal patch vs. lollipops?
A
  • synthetic opioids
  • fast acting
  • very potent
  • SHORT duration of action (vs. methadone)

-used in pain control during procedures, transdermal patch for pain management, lollipops for peds patients

18
Q

methadone

  • used to treat?
  • long or short duration of action?
A
  • synthetic opioid
  • used to treat addiction but also for pain
  • very LONG duration of action (vs. fentanyl)
19
Q

loperamide

-describe effect at normal vs. high dose

A
  • antidiarrheal
  • effect at normal dose restricted to GI tract
  • activation of mu receptors in GI tract reduces contraction and decreases secretions
  • potential for abuse!
20
Q

tramadol

  • parent cmpd MOA?
  • cytochrome issue?
  • adverse effects?
A

parent cmpd MOA: inhibits serotonin and NE reuptake (SNRI)

  • weak mu agonist
  • CYP2D6 converts tramadol into a mu agonist 300x more potent than parent cmpd

adverse effects: dependence potential; a lesser known drug of abuse, lowers seizure threshold

21
Q

naloxone

  • treats?
  • adverse effects?
A
  • opioid antagonist
  • tx overdose
  • cause precipitated withdrawal in ppl who are physically dependent
22
Q

buprenorphine

  • tx?
  • (+) naloxone effects?
A
  • partial mu agonist with high potency
  • helps wean patients off opioids by preventing severe withdrawal sxs
  • can precipitate withdrawal if full agonist in patient’s system
    • naloxone to deter IV and intranasal abuse; sublingual film, if injected/snorted, naloxone blocks opioid receptors–>withdrawal
23
Q

Understand the relationship between tolerance, physical dependence, and addiction

A

tolerance: dose may need to increase over time to continue relieving pain, or may need to switch to a different drug
physical dependence: body has adapted to drug and can get opioid withdrawal
addiction: lack of impulse control over taking drug, and person seeks it despite negative consequences (family, job, etc.)

24
Q

morphine

A

prototype drug

25
Q

hydromorphone (dilaudid)

A
  • similar efficacy to morphine
  • 10x potency
  • better water solubility–> lower IV volume
26
Q

oxycodone

A
  • lower efficacy

- good oral bioavialability

27
Q

codeine

A
  • low efficacy

- prodrug susceptible to CYP2D6 pharmacogenetics (cannot convert codeine to morphine)

28
Q

fentanyl

A
  • fast acting and very potent (100x more than morphine)
  • SHORT duration of action
  • uses: pain control during procedures, transdermal patch for pain management, lollipops for peds pts
29
Q

methadone

A
  • treats addiction and pain

- LONG duration of action

30
Q

loperamide

A
  • antidiarheal
  • effect at normal dose mainly restricted to GI tract
  • activation of mu receptors of GI tract–>reduces contraction and decreases secretions
  • potential for abuse
31
Q

tramadol

A

-

Pharmacology (7 decks)

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