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Pharm Test 2 > Opioids > Flashcards

Opioids Flashcards

1
Q

High efficacy agonist

Rx

A

Morphine
Meperidine
Methadone
Fentanyl

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2
Q

Low/Medium efficacy ags

A

Codeine
Oxycodone
Hydrocodone

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3
Q

Mixed Ags/Antags

A

Pentazocine

Buprenorphine

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4
Q

Antags

A

Naloxone

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5
Q

Non-analgesic opioid

A

Dextromethorphan

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6
Q

Opiate

Term

A

Includes non-analgesics

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7
Q

Opioids

Name

A

Include synth drugs, endogenous (enkephlins)

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8
Q

Analgesic

Name

A

Pain-relieving

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9
Q

Endogenous Opioid

Mu receptor

A

Binds

  • B-endorphin
  • Enkephalins

MOST OPIOID EFFECTS
*analgesia, Respiratory, euphoria, dependence

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10
Q

Endogenous Opioids

Delta receptor

A

Binds

  • B-endorphins
  • enkephalins

Analgesia

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11
Q

Endogenous Opioids

Kappa receptors

A

Binds
*dynorphins

Analgesia, sedation, endocrine

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12
Q

Opioid Txs

A
  • Analgesia (NO neuropathy)
  • Antitussive (BUT NO COPD/ASTHMA (mucus)
  • Antidiarrheal (CONSTIPATION)
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13
Q

Opioid

Analgesia effects

A

*threshold (discriminative)

ONLY IN OPIOIDS = *Tolerance (affective /emotion) = care less about pain
*ONLY PAIN = not temp, touch, proprioception (like LOCAL ANALGESICS)

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14
Q

Opioid Analgesia

Sites

A

Peripheral = C fiber

Spinal = stop ASCENDING PAIN pathway

Supraspinal = activate DESCENDING PAIN INHIBITORY PATHWAY

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15
Q

Major receptor for analgesic opioid fact

A

Mu

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16
Q

Opioids

Uses

A

Premedication for general anesthesia

  • OR*
  • general anesthetic adjunct
  • primary general anesthetic (no CV risk) - fentanyl
  • Spine anesthesia*
  • fentanyl+anesthetic (epidural)
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17
Q

Antitussive effects

Mediated by (receptor)

A

DM receptor

NOT OPIATE RECEPTOR

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18
Q

L stereoisomer activates

A

Mu (opioid)
+
DM (Anti-tussive)

  • Natural opioids
  • Opiates
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19
Q

D stereoisomer activates

A

UNNATURAL STEREOISOMER

DM (antitussive ) ONLY
NO MU S.E.

*dextromethorphan

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20
Q

Opioid Anti-diarrheal effects

A

*Mu receptor

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21
Q

Opioid antidiarrheal

S.E

A

Delayed gastric emptying - other oral Rx slowed

If no cross BBB, no CNS effects

No tolerance

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22
Q

Opioid

General S.E.

A

Mostly MU RECEPTOR

  • Constipation (no tolerance)
  • N/V (Mu in CTZ + vestibular apparatus). = tx ondansetron
  • Sedation = additive w/ other Rx
  • miosis = (no tolerance, atropine)
  • Pruritis = (NOT MU, from mast cell histamine)
  • Respiratory depression - additive w/ other Rxs, delayed up to 12 hrs)
  • urinary retention
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23
Q
  • pinpoint pupils
  • respiratory Depression
  • decreased consciousness
A

Opioid OD

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24
Q

Opioid less common SE

Cardio

A

Meperidine - TAC (anti-musc)

Most - bradycardia

25
Opioid tolerance SE change?
SE move with tolerance (except constipation + miosis) = T.I. DOESN'T change
26
Opioid dosing * Cut back when pt shows... * Switch when...
Lower dose = Higher respiratory effect Switch = SE untenable, equi-analgesia across Rxs
27
Pt needs analgesia, but is Opioid abuser
Give larger dose than Naive patient
28
Opioid drug interactions
SSRI + Meperidine = serotonin syndrome + Benzos/Barbituates/alcohol = Respiratory depression
29
Tx Acute severe pain
IV - morphine/fentanyl
30
Tx Chronic pain (cancer)
* Underlying pain = extended-release morphine * breakthrough pain = fast/short-acting (fentanyl lolipop, hydromorphone oral, Percocet (oxycodone), vicoden (hydrocodone)
31
Tx Nociceptive/inflammatory
Opioids
32
Tx Neuropathic pain
Opioids ADD Anticonvulsants
33
Change dose if patient :
* opioid dependent * Impaired GI motility * Hepatic/renal impairment * Oral rx ability
34
High first pass effect
Morphine | only 25% bioavailable
35
Low first pass effect
Methadone | Almost 100% available
36
Opioid Analgesia Use against this pain
GOOD **2nd (C fiber - slow) pain = dull/achy LESS**1st (Abeta - fast) pain = sharp, intense WORST **Neuropathic pain (ex. post-herpetic neuralgia)
37
Non-opioid receptors w/ opioid effects DM receptor
*antitussive effects
38
Descending pain inhibitory pathway
MOR activated in PAG --> Raphe nucleus --> enkephalin-containing neuron in spinal cord releases enkephalins -->inhibit substance P releasing C-fiber + Hyperpolarize ascending spinothalamic tracts
39
Morphine * absorption * duration * addiction-resistance * Metab? * SE
*High 1st pass *4-5 hours *slow-release = chronic pain *MS-Contin = crush resistant *metab = glucuronidation *SE= seizure (M3G metabolyte) =renal fail pt (M3G)= lower dose =histamine release = bronchoconstriction, HypoTN,
40
Hydromorphone *SE
* dilauded * no Histamine = NO bronchoconstriction/hypoTN/pruritis * M3G, NO M6G - So NO dose change w/ renal fail
41
Fentanyls * onset * forms * SE
* more lipophilic * Fast acting * Can't tolerate oral opioids? --> many forms * Poor cardio function but need surgery antalgesic? - IV fentanyl * No Histamine releases = NO pruritis, bronchoconstriction, hypoTN
42
Methadone * Uses * absorb * SE
* treat heroin addicts, analgesic * well absorbed in GI * long t 1/2 * non opoid receptor effects --> analgesia * no histamine * PROLONGED QT
43
Low-medium efficacy opiods * combos * contraindications
All oral NO WITH LIVER DZ Combine with aspirin (=dan) Combine w/ acetaminophen (=cet) *liver toxicity
44
Ultrametabolizer (CYP2D6) of codeine?
Use alternative: * buprenporphine * hydromorphine
45
Codeine * uses * SE
* converted by CYP 2D6 to moprhine * antitussive (bind direct to DM - no CYP conversion needed) * histamine release
46
Oxycodone * efficacy * Metab * slow release
* highest efficacy * CYP2D6 = metab to oxymorphone (NOT AFFECTED BY RECESSIVE CYP FORMS) * slow-release = Oxycontin
47
Hydrocodone * efficacy * metab * SE
* moderate efficacy * CYP2D6 to hydromorphone = NOT AFFECTED by RECESSIVE CYP FORMS * antitussive, pruritis * most prescribed
48
Kappa agonists Effects
* kappa agonist = analgesia | * partial/full mu agonist = anagonizes other mus
49
Misc Opioid Analgesics Buprenorphine * receptors * use * combo
*partial mu ag Kappa antag *sublingual * 1st line - opioid dependence (opioid receptor full-ag blockers) * combo = +naxolone (Suboxone)
50
Opioid antags Naloxone
*parenteral * Use - Opioid OD * short duration = give multiple doses to OD
51
Opioid Antags Naltrexone * Duration * use
Long-acting | *use - alcohol addiction + other addiction
52
Neuropathic pain Fibers
A-beta NOT C + A-delta
53
Amitriptyline Imipramine Desipiramine * mech * use
NE reuptake inhibitor *neuropathic pain ADDs
54
Diabetic neuropathy Tx
Carbamazepine | Pregabalin
55
Postherpetic neuralgia Tx?
Gabapentin | Pregabalin
56
TX pain 1) Mild pain
Aspirin NSAIDS Acetaminophen
57
TX Pain 2) Moderate pain
+ low/medium efficacy opioids NEW GUIDELINES CDC = start w/ atypical opioids + lifestyle change
58
TX pain 3). Severe pain
High efficiacy opioids
59
Dextromethrophan * receptor * SE
* DM receptor * less addiction = no MU effects Antitussives

Pharm Test 2 (13 decks)

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