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MSK 2 > Opiods > Flashcards

Opiods Flashcards

1
Q

Full agonist analgesics

A

Methadone
Heroin
Fentanyl
Morphine
Codeine

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2
Q

Partial and “mixed” agonists

A

Buprenorphine
Nalbuphine

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3
Q

Antagonists

A

Naloxone
Naltrexone
Methylnaltrexone

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4
Q

What is an analgesic

A

drug that relieves pain

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5
Q

Endorphins

A

“endogenous morphines”
begin with an enkephalin motif (Tyr-Gly-Gly-Phe-) (required for activity at the opioid receptors)

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6
Q

enkephalins

A

Derived from preproenkephalin and proopiomelanocortin
Act at delta and mu receptors
Actions similar to morphine, both analgesia and addiction
Short-lived, having mainly the minimal required structure
Found in brain, adrenal medulla, gut, immune system
Regulate pain pathways, emotions (particularly anxiety), GI tract, immune system

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7
Q

dynorphins

A

Dynorphin A and B and neoendorphins α and β, larger peptides
Derived from prodynorphin
Act at mu, kappa, and NOP receptors
CNS localization and released in response to pain
Longer-acting analgesia than the enkephalins

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8
Q

endorphins

A

Mainly β-endorphin
Larger peptide, 31 amino acids
Derived from proopiomelanocortin (POMC)
Acts at kappa, mu, delta receptors
Found in brain, pituitary, adrenal medulla
The longest-acting of the endogenous peptides

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9
Q

Endomorphins and Nociceptin/Orphanin FQ

A

The other members of this peptide family Physiological roles not yet clear

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10
Q

The spectrum of opioid effects

A

All mediated by morphine

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11
Q

CNS effects

A

a. Analgesia, spinal or supra-spinal
b. Euphoria
c. Sedation
d. Respiratory depression (a limiting side effect)
e. Cough suppression (another use)
f. Miosis (very useful for diagnosis of overdose)
g. Truncal rigidity (chest and abdominal muscles)
h. Nausea and vomiting
i. Body temperature changes
j. Sleep effects

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12
Q

Peripheral organ effects

A

a. CV system – some bradycardia
b. GI system – constipation
c. Biliary tract – constriction, biliary colic
d. Renal – decreased function, multiple components
e. Uterus – may prolong labor
f. Endocrine
- increased ADH (decreased urine output)
- increased prolactin, somatostatin
- decreased LH (low T in males, dysmenorrhea or amenorrhea in females)
g. Skin – pruritis; flushing, itching; in part due to histamine release
h. Immune system – one source of opioids endogenously; very complex effects

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13
Q

Opiate

A

a compound purified from the juice or resin of the opium poppy

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14
Q

Opioid

A

any compound with actions similar to the opiates and act at opioid receptors

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15
Q

Narcotic

A

from the word for sleep; often used in connection with opioids; but now generally refers to illegal use and/or addiction; of opioids or most any other addictive and/or illegal drugs

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16
Q

Opioid receptors, mechanisms, effects

A

All are agonists at specific G protein-coupled receptors, termed the opiate receptors

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17
Q

Mu receptors

A

Mediate morphine-like actions
- analgesia, sedation, anti-anxiety, euphoria, dependence
- respiratory depression, slowed GI transit
Expressed in CNS, spinal cord, periphery
.

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18
Q

Kappa receptors

A

Mediate pentazocine-like actions
- analgesia, sedation, dependence
- dysphoria, hallucinations, miosis
Expressed in CNS, spinal cord

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19
Q

Delta receptors

A

Mediate dynorphin-like actions
- analgesia, euphoria, dependence, tolerance
Expressed in CNS, periphery

20
Q

NOP receptors

A

Nociceptin/orphanin FQ receptors, the “newest” set of receptors
Respond to the endogenous peptide nociceptin, aka orphanin FQ
But only weakly to most opioid analgesics
Not currently a clinical target, but much research

21
Q

Morphine mainly acts at

A

mu and kappa receptors

22
Q

All full agonist opioid analgesics act at

A

mu receptors

23
Q

Mechanisms for opioid analgesia

A
  1. Inhibition of pain signaling
    • Acts at both peripheral and spinal levels to block pain transmission
  2. Pro-analgesic effects
    - Acts at higher brain levels to block response to pain
  3. Multiple specific neuronal pathways and brain regions involved
    • Beyond the scope of this course
24
Q

Tolerance

A

“desensitization” of opioid receptors
need increasingly larger amounts of drug for some effect

25
Q

Dependence

A

need drug to feel normal

26
Q

Withdrawal

A

the unpleasant responses that a drug-dependent person experiences if the
drug is NOT continuously available and used

27
Q

Addiction and abuse

A

“psychological dependence” in addition to “pharmacological” dependence

28
Q

“Opioid Abuse Epidemic”

A

“physician-driven” epidemic; opioids over-prescribed

29
Q

Morphine

A

gold standard drug
oral administration
pain relief in 5-15 min (primarily for acute pain)
max effect in 60-90 min
4-5 hour duration
contin= continued release
IR=immediate release
ER= extended release
blocks pain transmission at spinal levels
acts at higher levels to block response to pain
raises pain threshold
Overdose, nausea, vomiting, constipation (little or no tolerance), miosis (no tolerance), pruritus,
cannot be used in patients with decreased respiratory reserve, head injuries, CNS tumors, pregnancy
Drug interactions: CNS depressants

30
Q

Codeine

A

only given orally for mild to moderate pain (often given with acetaminophen)
also used for cough impression
less potent than morphine
metabolized by CYP2D6
analgesia
Converted to morphine
More likely to cause constipation than morphine
Less addicting than morphine (schedule II drug, mixed into soda)
some patients are ultra-rapid metabolizers (concerning in children)

31
Q

Fentanyl

A

synthetic opioid
extremely potent analgesic (chronic pain, anesthesia, CV surgery)
Schedule II drug
more rapid onset than morphine and longer duration
multiple routes of administration
no histamine release
truncal rigidity
high addiction/abuse potential

32
Q

Heroin

A

more potent than morphine
more rapid CNS entry
shorter acting
extremely high abuse and addiction potential
schedule I drug (no approved uses

33
Q

Methadone

A

synthetic opioid (long-lasting analgesic)
unrelated to morphine or codeine
oral or IM at low dose
slow metabolism by CYP2B6 and CYP3A4
Schedule II
CV effects (QT prolongation)
major use for opioid abuse
methadone maintenance therapy (slow onset, high oral potency, long duration

34
Q

Partial agonist opioids

A

agonists when given alone
act as antagonists when on board with full agonists

35
Q

Mixed agonist-antagonist

A

Agonists at one receptor type
antagonists at another receptor type
drug class unique to opioids

36
Q

Nalbuphine

A

kappa receptor agonist (analgesic component)
mu receptor antagonist (avoid respiratory depression)
no oral admin due to rapid first-pass metabolism
similar potency to morphine
15 minute onset with 4-5 hour duration

37
Q

Buprenorphine

A

partial agonist at mu receptors (celing on respiratory depression)
antagonist at kappa receptor
mu receptor analgesia without kappa receptor side effects
opposite of nalbuphine
Schedule III drug
no oral admin due to rapid first-pass metabolism
used to treat opioid dependence and cocaine abuse
precipitates withdrawal symptoms in people using full agonists

38
Q

Loperamide

A

anti-diarrheal
full agonist
orally admin
NO CNS action (not an analgesic)
not a scheduled drug

39
Q

Diphenoxylate

A

ainti-diarrheal
Schedule V
prescription-only (high doses may cause opioid effects)

40
Q

Dextromethorphan

A

used for cough (antitussive effects like codeine)
not an analgesic
acts on opioid receptors

41
Q

Naloxone

A

prototype opioid antagonist counteracts opioid effects such as respiratory depression (only due to opioids)
treatment of acute opioid overdose (respiratory depression, miosis, coma)
binds partial agonist agents
given IV (not potent orally)
rapid-acting but short duration
will cause withdrawal

42
Q

Naloxone

A

prototype opioid antagonist counteracts opioid effects such as respiratory depression (only due to opioids)
treatment of acute opioid overdose (respiratory depression, miosis, coma)
binds partial agonist agents
given IV (not potent orally)
rapid-acting but short duration
will cause withdrawal

43
Q

Naltrexone

A

more orally effective and longer duration of action than naloxone
used to treat opioid dependence
used to prevent effects of opioids so they won’t be used
used to treat alcohol dependence

44
Q

Methylnaltrexone

A

treatment of opioid-induced constipation

45
Q

drugs given with naloxone

A

morphine
oxycodone
buprenorphine

MSK 2 (6 decks)

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