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MSK 2 > Opiods > Flashcards

Opiods Flashcards

(45 cards)

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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

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A

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

20
Q

NOP receptors

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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

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A

mu and kappa receptors

22
Q

All full agonist opioid analgesics act at

23
Q

Mechanisms for opioid analgesia

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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

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A

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

25
Dependence
need drug to feel normal
26
Withdrawal
the unpleasant responses that a drug-dependent person experiences if the drug is NOT continuously available and used
27
Addiction and abuse
"psychological dependence" in addition to "pharmacological" dependence
28
"Opioid Abuse Epidemic"
"physician-driven" epidemic; opioids over-prescribed
29
Morphine
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
Codeine
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
Fentanyl
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
Heroin
more potent than morphine more rapid CNS entry shorter acting extremely high abuse and addiction potential schedule I drug (no approved uses
33
Methadone
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
Partial agonist opioids
agonists when given alone act as antagonists when on board with full agonists
35
Mixed agonist-antagonist
Agonists at one receptor type antagonists at another receptor type drug class unique to opioids
36
Nalbuphine
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
Buprenorphine
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
Loperamide
anti-diarrheal full agonist orally admin NO CNS action (not an analgesic) not a scheduled drug
39
Diphenoxylate
ainti-diarrheal Schedule V prescription-only (high doses may cause opioid effects)
40
Dextromethorphan
used for cough (antitussive effects like codeine) not an analgesic acts on opioid receptors
41
Naloxone
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
Naloxone
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
Naltrexone
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
Methylnaltrexone
treatment of opioid-induced constipation
45
drugs given with naloxone
morphine oxycodone buprenorphine

MSK 2 (6 decks)

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