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IC Part II > Opioids > Flashcards

Opioids Flashcards

1
Q

-any drug, natural or synthetic, that acts at opioid receptors

A

opioids

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2
Q

-derived from opium poppy, contains many opiate compounds including morphine and codeine

A

opiates

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3
Q
  • at least 3 receptor types (mu, kappa, delta)
  • all are Gprotein coupled
  • close calcium channels, reducing evoked transmitter release (presynaptic)
  • open potassium channels, hyperpolarizing membranes (postsynaptic)
A

morphine

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4
Q

_____ receptors produce analgesic, sedative, and euphoric effects of opiates, as well as most of untoward side effects

A

mu

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5
Q

_____ receptors appear to contribute to analgesia at spinal levels

A

delta

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6
Q

____ receptors may also contribute to analgesia, but primarily results in dysphoria

A

kappa

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7
Q
  • opioid receptors in peripheral tissues
  • dorsal horn of spinal cord (IPSPs, inhibition of NT release)
  • ventral caudal thalamus
A

afferent pain transmission from periphery to CNS

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8
Q
  • periaqueductal grey matter
  • rostral ventral medulla
  • dorsal horn of the spinal cord
A

pain modulating descending paths from the CNS

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9
Q
  • analgesia
  • euphoria/dysphoria
  • sedation
  • respiratory depression
  • cough suppression
  • miosis (parasympathetic, cholinergic)
  • truncal rigidity
  • nausea and vomiting
A

CNS effects of opioids

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10
Q
  • arterial and venous dilation
  • constipation
  • biliary colic
  • decreased RBF
  • decreased uterine tone
  • endocrine alterations: increase ADH, prolactin, somatotropin, decreased LH
  • histamine: flushing, sweating, rashes and itching
A

peripheral effects of opioids

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11
Q
  • acute or chronic pain (analgesic, no apparent max dose, less effective for neuropathy)
  • acute pulm edema or MI, decreases sensation of crisis
  • cough, antitussive
  • diarrhea
  • anesthesia, preop meds
A

uses of opioids

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12
Q
  • respiratory depression (primary cause of death)
  • dysphoria
  • nausea, vomiting
  • constipation
  • seizures at high doses, delta mediated
A

opioid toxicity

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13
Q
  • clinically apparent in 2 weeks
  • develops to euphoria, resp depression, analgesia, sedation, nausea, cough suppression, antidiuresis
  • minimal or none to constipation, seizures, miosis
A

tolerance

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14
Q

dysphoria, rinorrhea, lacrimation, yawning, chills, vomiting, diarrhea, anorexia, insomnia, anxiety, hostility
-no tolerance but craving can persist

A

opioid withdrawal

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15
Q

equal to 10mg morphine

A

equianalgesic dose

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16
Q

morphine, methadone, meperidine, hydromorphone, oxymorphone, fentanyl, alfentanil

A

high efficacy analgesics (severe pain, trauma, post surgical)

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17
Q
  • poor oral bioavailability

- duration 4-5 hours

A

morphine

18
Q
  • longer acting, 6 hours, plasma half life 24 hours
  • good oral bioavailability
  • used as maintenance in opioid addicts
A

methadone

19
Q
  • medium acting 2-4 hours
  • antimuscarinic, may cause tachycardia
  • metabolized to active metabolite
  • psychoactive, can cause seizures
A

meperidine

20
Q
  • short acting, 1hr
  • 100X more potent than morphine
  • acts at mu receptors
  • poor oral bioavailability
  • transdermal available
A

fentanyl

21
Q
  • very short acting, 15-45min
  • very potent, parenteral only
  • for brief, painful procedures
A

alfentanil

22
Q

codeine, hydrocodone, oxycodone, propoxyphene, tramadol

A

low to medium efficacy analgesics

23
Q

low efficacy, metabolized into morphine by CYP2D6

A

codeine

24
Q

full agonist, moderate/high efficacy

A

oxycodone

25
Q
  • propoxyphene like metabolites, inhibits NE and 5HT reuptake
  • may have efficacy for neuropathic pain
A

tramadol

26
Q
  • believed to have less addictive potential and risk of respiratory depression
  • used for moderate to severe pain
  • also used for opioid addiction
A

partial or mixed agonist-antagonist analgesics

27
Q
  • mu partial agonist

- maintenance of opioid dependance as depot or in combo with naloxone

A

buprenorphine

28
Q

buprenorphine, butorphanol, nalbuphine, pentacozine

A

partial or mixed agonist-antagonist analgesics

29
Q

-antidiarrheals, poor permeation of BBB

A

diphenoxylate, loperamide

30
Q

codeine and dextromethorphan

A

antitussives

31
Q
  • opioid antagonist used for acute overdose
  • 1-2 hr duration
  • high affinity for mu receptors
  • used in combo with buprenorphine for maintenance of opioid dependance, and in combo with oxycodone for chronic pain
A

naloxone, for acute opioid overdose

32
Q

used to prevent relapse in recovering addicts, or buproprion for weight loss

A

naltrexone

33
Q

methylnaltrexone or naloxegol, poor BBB penetration

A

opioid antagonist, used for constipation

34
Q

many opioids have low bioavailability due to 1st pass metabolism, except which two?

A

methadone and codeine

35
Q

______ is more potent than morphine but has poor BBB permeability, glucoronidated

A

M-6G

36
Q

______ and ______ are metabolized into morphine

A

codeine and heroin

37
Q
  • head injuries
  • pregnancy
  • impaired pulm function
  • hepato or renal compromised patients
  • endocrine disorders
A

contraindications of opioids

38
Q

pure agonists and mixed-agonist/antagonist _______ analgesia, can precipitate withdrawal symptoms

A

decrease

39
Q

opioids + other sedative hypnotics ______ sedation and respiratory depression

A

increase

40
Q

opioids + antipsychotics _____ sedation and respiratory depression, _____ risk of seizures

A

increase, increase

41
Q

opioids + MAOIs ______ risk of hyperpyrexic coma and hypertension

A

increase

IC Part II (29 decks)

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