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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
Q

Opioid tolerance

SE change?

A

SE move with tolerance (except constipation + miosis) = T.I. DOESN’T change

26
Q

Opioid dosing

  • Cut back when pt shows…
  • Switch when…
A

Lower dose = Higher respiratory effect

Switch = SE untenable, equi-analgesia across Rxs

27
Q

Pt needs analgesia, but is Opioid abuser

A

Give larger dose than Naive patient

28
Q

Opioid drug interactions

A

SSRI + Meperidine = serotonin syndrome

+ Benzos/Barbituates/alcohol = Respiratory depression

29
Q

Tx

Acute severe pain

A

IV - morphine/fentanyl

30
Q

Tx

Chronic pain (cancer)

A
  • Underlying pain = extended-release morphine
  • breakthrough pain = fast/short-acting (fentanyl lolipop, hydromorphone oral, Percocet (oxycodone), vicoden (hydrocodone)
31
Q

Tx

Nociceptive/inflammatory

A

Opioids

32
Q

Tx

Neuropathic pain

A

Opioids
ADD
Anticonvulsants

33
Q

Change dose if patient :

A
  • opioid dependent
  • Impaired GI motility
  • Hepatic/renal impairment
  • Oral rx ability
34
Q

High first pass effect

A

Morphine

only 25% bioavailable

35
Q

Low first pass effect

A

Methadone

Almost 100% available

36
Q

Opioid Analgesia

Use against this pain

A

GOOD **2nd (C fiber - slow) pain = dull/achy

LESS**1st (Abeta - fast) pain = sharp, intense

WORST **Neuropathic pain (ex. post-herpetic neuralgia)

37
Q

Non-opioid receptors w/ opioid effects

DM receptor

A

*antitussive effects

38
Q

Descending pain inhibitory pathway

A

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
Q

Morphine

  • absorption
  • duration
  • addiction-resistance
  • Metab?
  • SE
A

*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
Q

Hydromorphone

*SE

A
  • dilauded
  • no Histamine = NO bronchoconstriction/hypoTN/pruritis
  • M3G, NO M6G
  • So NO dose change w/ renal fail
41
Q

Fentanyls

  • onset
  • forms
  • SE
A
  • 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
Q

Methadone

  • Uses
  • absorb
  • SE
A
  • treat heroin addicts, analgesic
  • well absorbed in GI
  • long t 1/2
  • non opoid receptor effects –> analgesia
  • no histamine
  • PROLONGED QT
43
Q

Low-medium efficacy opiods

  • combos
  • contraindications
A

All oral
NO WITH LIVER DZ

Combine with aspirin (=dan)

Combine w/ acetaminophen (=cet)
*liver toxicity

44
Q

Ultrametabolizer (CYP2D6) of codeine?

A

Use alternative:

  • buprenporphine
  • hydromorphine
45
Q

Codeine

  • uses
  • SE
A
  • converted by CYP 2D6 to moprhine
  • antitussive (bind direct to DM - no CYP conversion needed)
  • histamine release
46
Q

Oxycodone

  • efficacy
  • Metab
  • slow release
A
  • highest efficacy
  • CYP2D6 = metab to oxymorphone (NOT AFFECTED BY RECESSIVE CYP FORMS)
  • slow-release = Oxycontin
47
Q

Hydrocodone

  • efficacy
  • metab
  • SE
A
  • moderate efficacy
  • CYP2D6 to hydromorphone = NOT AFFECTED by RECESSIVE CYP FORMS
  • antitussive, pruritis
  • most prescribed
48
Q

Kappa agonists

Effects

A
  • kappa agonist = analgesia

* partial/full mu agonist = anagonizes other mus

49
Q

Misc Opioid Analgesics

Buprenorphine

  • receptors
  • use
  • combo
A

*partial mu ag
Kappa antag
*sublingual

  • 1st line - opioid dependence (opioid receptor full-ag blockers)
  • combo = +naxolone (Suboxone)
50
Q

Opioid antags

Naloxone

A

*parenteral

  • Use - Opioid OD
  • short duration = give multiple doses to OD
51
Q

Opioid Antags

Naltrexone

  • Duration
  • use
A

Long-acting

*use - alcohol addiction + other addiction

52
Q

Neuropathic pain

Fibers

A

A-beta

NOT C + A-delta

53
Q

Amitriptyline
Imipramine
Desipiramine

  • mech
  • use
A

NE reuptake inhibitor
*neuropathic pain

ADDs

54
Q

Diabetic neuropathy

Tx

A

Carbamazepine

Pregabalin

55
Q

Postherpetic neuralgia

Tx?

A

Gabapentin

Pregabalin

56
Q

TX pain

1) Mild pain

A

Aspirin
NSAIDS
Acetaminophen

57
Q

TX Pain

2) Moderate pain

A

+ low/medium efficacy opioids

NEW GUIDELINES CDC = start w/ atypical opioids + lifestyle change

58
Q

TX pain

3). Severe pain

A

High efficiacy opioids

59
Q

Dextromethrophan

  • receptor
  • SE
A
  • DM receptor
  • less addiction = no MU effects

Antitussives

Pharm Test 2 (13 decks)

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