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Pharmacology > Opioid Analgesics > Flashcards

Opioid Analgesics Flashcards

1
Q

what are the major classes of opioid receptors and where do most opioid analgesics work

A
  • μ, δ and κ.

- most work at the μ receptor

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2
Q

what are opioids action on neurons

A
  • close voltage gated Ca channels on presynaptic nerve terminals –> reduced neurotransmitter release
  • open K channels –> hyperpolarizing and inhibiting postsynaptic neurons
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3
Q

opioids reduce the release of large numbers of neurotransmitters. what are the neurotransmitters?

A

NAGSS

  • norepinephrine
  • acetylcholine
  • glutamate
  • serotonin
  • substance P
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4
Q

where does the analgesic effects of opioids come from (aka what is the mechanism that leads to analgesia)

A
  • directly inhibits ascending transmission of nociceptive info from spinal cord dorsal horn
  • indirectly activates pain inhibitory circuits
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5
Q

receptors that opioids work on in spinal analgesia and the mechanism

A
  • μ, δ and κ.
  • inhibits the release of excitatory neurotransmitters substance P and glutamate from these primary afferents
  • also inhibits the dorsal horn pain transmission neuron directly
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6
Q

receptors that opioids work on in supraspinal analgesia and mechanism

A
  • μ, δ and κ.

- activation of pain inhibitory descending neurons

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7
Q

mechanism of peripheral analgesia

A

-stimulation of peripheral μ receptors by opioids decrease sensory neuron activity and release

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8
Q

what are the mixed agonists-antagonists of opioids (what do they agonize and antagonize)

A

Pentazocine
Butorphanol
Nalbuphine
Buprenorphine - partial μ agonist and κ antagonist

partial agonist/antagonist of μ receptors and are agonists of κ receptors

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9
Q

what are the opioid antagonist and what receptors do they antagonize

A

antagonize all - μ, δ and κ

naloxone and naltrexone

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10
Q

what are the opioid agonist

A 
Morphine
Fentanyl
Meperidine
Methadone
Codeine
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11
Q

might need this box later

A

thanks

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12
Q

what are the CNS effects of opioids

A
  • analgesia
  • euphoria
  • sedation and drowsiness
  • respiratory depression
  • cough suppression
  • miosis
  • truncal rigidity
  • nausea and vomiting
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13
Q

peripheral effects of opioids

A
  • hypotension
  • GI effects: constipation
  • Biliary Colic
  • Decreased renal flow
  • Uterus: prolongs labor
  • Release of ADH, PRL, Somatotropin and inhibit LH
  • Pruritis
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14
Q

how are opioids excreted

A

turned to metabolites mostly glucuronides then excreted by the kidney

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15
Q

what types of patients should be monitored when given opioids like morphine

A

those with renal impairment since it is conjugated to a glucuronide then excreted by the kidney

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16
Q

how are opioids like heroin and remifentanil metabolized

A

they are hydrolyzed by tissue esterases

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17
Q

which opioids causes seizures if in high concentration and what type of patients experience these seizures

A

normeperidine

patients with decreased renal function since it cannot be excreted hence –> seizures

18
Q

clinical uses of opioid analgesics

A

5 As

  • Analgesia: pain
  • Acute pulmonary edema: relieves dyspnea by reducing cardiac preload and afterload
  • Antitussives: relieve cough
  • Antidiarrheals
  • Anesthesia: sedative, anxiolytic, and analgesic properties
19
Q

adverse effects of opioids

A 
MAIN ONES:
nausea
vomiting
sedation
itching
constipation

IN ADDITION:
urinary retention
hypotension
respiratory depression

20
Q

contraindications/cautions in opioid therapy

A
  • using pure agonists with partial: diminishes effect
  • head injury: CO2 retention caused by respiratory depression –> cerebral vasodilation
  • pregnancy: fetus becomes dependent and experiences withdrawal postpartum
  • impaired pulmonary function: opioids respiratory depressive properties –> acute respiratory failure
  • decreased renal function: can’t excrete it so leads to problems associated with high conc
  • endocrine disease: adrenal insufficiency or hypothyroidism can have prolong and exacerbated response
21
Q

drug interactions of opioids

A
  • with sedative hypnotics –> resp depression
  • antipsychotics –> increases sedation
  • MAOI: meperidine and tramadol –> excitement, muscle rigidity, hyperthermia, unconsciousness
22
Q

strong opioid agonists

A 
Morphine, Hydromorphine, Oxymorphine
Heroin
Meperidine
Fentanyl
Methadone
Levorphanol
23
Q

affinity of morphine towards opioid receptors

A

high affinity towards μ receptors

lower affinity towards δ and κ

24
Q

how is heroin hydrolyzed and explain which is more liposoluble and its importance

A

heroin –> 6-monoacetylmorphine (6-MAM) –> morphine

heroin and 6-MAM are more liposoluble hence enter the brain more readily

25
Q

what are primarily μ receptor agonists

A

Fentanyl, Meperidine, Methadone

26
Q

who is meperidine contraindicated in and why

A
  • people with tachycardia because it has antimuscarinic effets
  • those on MAOI/serotonergic agents because it can cause serotonin syndrome due to it blocking neuronal reuptake of serotonin
27
Q

what happens with large doses of meperidine given in short intervals

A

produce tremors, muscle twitches, DILATED PUPILS, hyperactive reflexes, convulsion

28
Q

mechanism of methadone (and its difference from morphine)

A

μ receptor agonist
NMDA receptor antagonist
serotonin and norepinephrine reuptake inhibitor

29
Q

drug used for opioid abstinence syndrome or treatment of heroin users in those with withdrawal symptoms and why?

A

methadone

  • less euphoria
  • longer half life and though it prolongs the abstinence syndrome, it is less severe than short acting opiates like heroin
30
Q

what are the mild to moderate opioid agonist

A

Codeine, oxycodone, hydrocodone

Tramadol

31
Q

mechanism of codeine’s analgesic effect

A

it is converted to morphine by CYP2D6

32
Q

mechanism of tramadol and use

A

weak μ agonist
norepinephrine and serotonin reuptake inhibitor

used for neuropathic pain (pain from injury to nervous system)

33
Q

contraindication of tramadol

A

taken it with serotonergic agents like MAOIs because of its inhibition of serotonin reuptake and hence can lead to serotonin syndrome

34
Q

adverse effects of mixed agonist-antagonist opioid analgesics(name them)

A

pentazocine, butorphanol, and nalbuphine are associated with psychotomimetic effects (not as common in buprenorphine)

35
Q

uses of opioid antagonists analgesics (name them)

A

naloxone and naltrexone

naloxone - acute opioid overdose

naltrexone - decrease craving for alcohol in chronic alcoholics (longer duration than naloxone)

36
Q

what are the antitussives

A

dextromethorphan

codeine

37
Q

contraindication of antitussives

adverse effects/differences in the antitussives

A

do not give to those on MAOIs

dextromethorphan has no analgesic effect so it is preferred and less likely to have constipation

38
Q

opioid anti motility agents/ antidiarrheals and are they agonists or antagonists

A

they are opioid agonists

diphenoxylate and loperamide

39
Q

what does commercial use of diphenoxylate contain that discourages overdosage

A

atropine (antimuscarinic - might contribute to antidiarrheal action)

40
Q

adverse effects of diphenoxylate

A

higher doses can cause CNS effects

Pharmacology (79 decks)

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