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Pharmacology Exam 4 > Exam 4 - Opioids > Flashcards

Exam 4 - Opioids Flashcards

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1
Q

Endogenous Opioids

3 families and Receptors

A

BED

1) Beta
2) enkephalins
3) dynorphins

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2
Q

Endogenous Opioids

Beta Receptor, Gene

A
  • mu and delta receptor
  • POMC gene
  • pituitary
  • gene related to ACTH, MSH
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3
Q

Endogenous Opioids

Enkephalin Receptor, Gene

A
  • delta and mu receptor
  • pro-enkephalin gene
  • brain, spine
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4
Q

Endogenous Opioids

Dynorphine Rceptor, Gene

A
  • kappa receptor
  • pro-dynorphin gene
  • brain, spinal cord
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5
Q

Endogenous Opioids

Mu receptor effects

A

-analgesia, resp depression,

euphoria, dependence

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6
Q

Endogenous Opioids

Delta receptor effects

A

-analgesia, otherwise unclear

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7
Q

Endogenous Opioids

Kappa receptor effects

A

-spinal analgesia, sedation, endocrine,

dysphoria, psychotomimetic

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8
Q

Endogenous Opioids

Non-opioid receptor

A

-DM: antitussive effects

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9
Q

Opioids

Therapeutic effects

A
  • analgeisa (not neuropathic)
  • antitussive (not SOPD, emphysema)
  • antidiarrheal (but constipation :( )
  • acute Pulm Edema relief (but resp depress)
  • good mood! (but don’t abuse it)
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10
Q

Opioids

Analgesia

A
  • not neuropathic (shingles)
  • best for slow pain (C fiber)
  • increase threshold/tolerance
  • selective for pain
  • inhibit ascending pathway (C fiber)
  • activate supra-spinal descending inhibitory pathway (PAG
  • pre-med anasthesia
  • spinal anasthesis (local + fentanyl)
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11
Q

Opioids

Antitussive

A
  • not opioid receptor mediated
  • DM receptors /(not stereoselective)
  • dextro isomers only have antituss effects
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12
Q

Opioids

Ant-diarrheal

A
  • mu enteric receptors
  • decrease peristalsis, secretions
  • no long-term tolerance
  • delays other drug absorption
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13
Q

Opioids

Adverse effects

A

-constipation (use stool softeners)
-nausea/vomit (tx w/ ondansetron)
-sedation (dimishes w/ time)
-miosis (tx w/ atropine)
-pruritus from mast cell stim
LESS COMMON
-urinary retention
-resp depression
-CV effects, truncal rigidity, dysphoria, addiction

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14
Q

Opioids

OD triad

A

1) pinpoint pupils
2) resp depression
3) coma

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15
Q

Opioids

Tolerance

A
  • after 2 weeks of use
  • w/ high/fx dosing
  • cross-tolerance between opioids
  • therapeutic index unchanged
  • constipation and miosis unchanged
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16
Q

Opioids

equi-analgesia

A

-same potency across class

17
Q

Opioids

Contraindications

A
  • head injury, preg,
  • pulm/renal/hepatic dysfx’n
  • Addison’s/hypothyroidism
  • abuse hx
  • drug interactions
18
Q

Opioids

Drg Interactions

A

-MAOIs w/ meperidine, propoxyphene
(causinbg serotonin syndrome)
-sedative hypnotics and antipsychotics
(causing resp depression)

19
Q

Opioids

Routes

A

oral, buccal, sublingual, transdermal,

nasal, suppository, parenteral

20
Q

Opioids

ADME

A
  • liver 1st pass (morphine high, methadone low)

- higher oral dose than IV

21
Q

Opioids

High efficacy

A

1) morphine, methadone, fentanyl

2) meperidine, (heroin)

22
Q

Opioids

Morphine

A
  • high 1st pass (25% avail)
  • IV more potent
  • don’t crush ‘em!
  • glucuronidation to M6G (full) and M3G (partial)
  • crosses BBB
  • M3G no analgesia, causes seizures
23
Q

Opioids

Fentanyl

A

-1st line high efficacy class
-compared to morphine: more potent, lipophilic,
short-acting
-chronic pain patch, breakthrough pain lozenge
-epidural for preggos
-primary anesthesia for CV surg

24
Q

Opioids

Methadone

A

-1st line high efficacy class
-lower first pass, high bioavailability,
long half-life
-tx heroin addiction
-analgesia
-no histamine release
-blocks K channel -> long QT syn

25
Q

Opioids

Meperidine

A
  • 2nd line high efficacy class
  • less potent, faster acting than morph
  • demethylation to normeperdine
  • normeperidine can have fatal CNS effects, seizure
  • tachycardia, mydriasis; no miosis
26
Q

Opioids

Heroin

A
  • 2nd line high efficacy class

- pro-drug w/ rapid conversion

27
Q

Opioids

low/med efficacy

A

-usuall combo’d w/ aspirin/ibu
Codeine
Oxycodone

28
Q

Opioids

Codeine

A
  • demethylation by CYP2D6
  • poor and ultra metabolizers
  • higher antitussive effects
  • high histamine effects
29
Q

Opioids

Oxycodone

A
  • highest low/med efficacy
  • CYP2D6
  • slow release preparations available
  • hilbilly heroin (crush to abuse)
30
Q

Opioids

mixed/other

A

-agonism at kappa (analgesia); anatagonism at mu
-side effects: dysphora, hallucinations
pentazocine, tramadol, buprenorphine

31
Q

Opioids

Pentazocine

A
  • high kappa agonism, low mu antagonism
  • parenteral site necrosis; use orally
  • combo w/ acetominophen
32
Q

Opioids

Tramadol

A
  • Weak mu agonist
  • inhibits NE and 5HT reuptake, blocks NMDA receptors
  • mod pain tx
  • risk seizures
  • avoid MAOIs
33
Q

Opioids

Buprenorphine

A
  • partial mu agonism, kappa antagonism
  • sublingual to avoid 1st pass
  • opioid dependence tx
  • combo with naxolone to prevent IV abuse
34
Q

Opioids

Anatagonist

A
  • naxolone
  • competes w/ all opioid receptors (not DM)
  • tx for opioid overdose
35
Q

Opioids

non-analgesics

A

dextromethorphan, loperamide

36
Q

Opioids

dextromethorphan

A
  • antitussive

- only active at DM receptors

37
Q

Opioids

loperamide

A
  • no BBB pen

- Imodium AD antidiarrheal

38
Q

Pain Mgmt

3 steps

A

MILD: ASA/APAP/NSAIDs
MOD: combo ASA/APAP/NSAID w/ low/med efficacy
SEVERE: high eff opioid w/ or w/o adjuncts

Pharmacology Exam 4 (10 decks)

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