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FTCM Pharm > Opioid Analgesics > Flashcards

Opioid Analgesics Flashcards

1
Q

What do opioid agonists do?

A

produce analgesia by activating receptors located in brain and spinal cord

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2
Q

Opioid receptor types:

A

3 main classes (mu, delta, and kappa) and are G protein linked couple to Gi

majority of opioid act on the mu receptor

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3
Q

2 actions on neurons

A
  1. close voltage gated Ca2+ channels on presynaptic terminals
  2. open K+ channels on postsynaptic neurons

both reduce NT release

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4
Q

Analgesic effects of opioids are due to ability to

A
  1. inhibit ascending pain transmission

2. activate descending pain-inhibitory circuits

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5
Q

Spinal analgesia

A

inhibit ascending pain transmission

all 3 receptor types

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6
Q

Supraspinal analgesia

A

inhibitory descending neurons inhibit pain transmission

all 3 receptor types

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7
Q

Descending pain inhibitory neurons are inhibited by

A

GABA**

meaning theres a transmission of pain

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8
Q

Opioids and supraspinal analgesia

A

Opioids inhibit GABA neurons –> activate pain inhibitory descending neurons –> inhibition of pain transmission

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9
Q

Opioid analgesics are classified into

A
  1. Pure agonists- high affinity for mu receptors
  2. Mixed agonists and antagonists
  3. Antagonists
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10
Q

Agonists and receptors

A

My Father & My Mothers Children (MFMMC)

Morphine (mu, weak delta/Kappa)
Fentanyl (mu)
Meperidine (mu)
Methadone (mu)
Codeine (weak at mu/delta)
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11
Q

Mixed A/As and receptors

A

Peanut Butter, No Butter (PBNB)

Pentazocine (mu ant, k ago)
Butorphanol (mu ant, k ago)
Nalbuphine (mu ant, k ago)
Buprenorphine (mu ago, k ant)

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12
Q

Antagonists and receptors

A

Naloxone
Naltrexone

Ant at all receptors

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13
Q

CNS effects

A
  • euphoria
  • analgesia
  • sedation
  • miosis
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14
Q

Peripheral effects

A
  • hypotension
  • constipation
  • contraction of biliary SM
  • pruritus
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15
Q

Opioids are converted to?

A

glucuronides

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16
Q

Morphine is conjugated to?

A

M3G

M6G

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17
Q

Heroin is hydrolyzed to?

A

Monoacetylmorphine and morphine

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18
Q

Codeine is converted to?

A

Morphine

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19
Q

What is metabolized by CYP2D?

A

Codeine, oxycodone, and hydrocodone

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20
Q

Merperidine is converted to?

A

Normeperidine

increase in normeperidine can occur in pt with decreased renal function and high conc can cause seizures

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21
Q

Fentanyl is metabolized by ___ to inactivate ___

A

CYP3A4, metabolites

22
Q

Methadone is metabolized by ____

A

P450

23
Q

OA use:

A
  • analgesia
  • acute pulmonary edema
  • cough
  • diarrhea
  • anesthesia
24
Q

OA AE:

A
  • nausea
  • vomiting
  • sedation
  • itching
  • constipation
25
Q

Contraindications

A
  • use of pure agonist with weak partial agonists
  • pt with head injuries
  • pt with impaired pulmonary function
  • impaired hepatic funtion
  • impaired renal function
  • pregnancy
  • children and breastfeeding moms (codeine and tramadol –> CYP2D6)
26
Q

Drug interactions

A
  1. Sedative hypnotics- increase CNS depression

2. MAO inhibitors –> serotonin syndrome

27
Q

Which opioids inhibit serotonin reuptake?

A
  • methadone
  • meperidine
  • tramadol
  • fentanyl
28
Q

What is serotonin syndrome?

A

when opioids are taken with MAO inhibitor

  • delirium
  • hyperthermia
  • headache
  • coma
  • death
29
Q

Properties of specific agents

A 
Agonists 
Mixed agonist-antagonists
Antagonists
Antitussives
Antimotility
30
Q

Agonists

A
  • Morphine, hydromorphone, oxymorphone
  • Heroin
  • Meperidine
  • Fentanyl
  • Methadone
  • Levophanol
  • Codeine, oxycodone, hydrocodone
31
Q

Morphine, hydromorphone, oxymorphone

A

severe pain treatment DOC
mu high affinity
d/k low affinity

32
Q

Heroin

A

rapid hydrolization to 6-MAM –> morphine

heroin and 6-MAM enter brain quick

33
Q

Meperidine

A

mu agonist

  • short term treatment of acute pain
  • half life 3 hrs
  • normeperidine has longgg half life so be careful of use of meperidine cause it can accumulate normeperidine leading to tremors, twitches, and seizures
34
Q

Fentanyl

A

mu agonist

  • severe pain
  • rapid and potent
35
Q

Methadone

A
  • long duration
  • severe pain
  • mu agonist
  • NMDA antagonist
  • serotonin and NE reuptake inhibitor
36
Q

Methadone use and AE

A

managing opioid withdrawal for addicted pt bc long half life and less euphoria

AE- long QT, torsades de pointes and death

37
Q

Levorphanol

A

all receptor agonist
serotonin and NE reuptake inhibitor
NMDA antagonist
severe pain

38
Q

Oxycodone and Hydrocodone

A

Oxy- moderate and severe pain, alone or used with nonopioid

Hydro- moderate and severe pain, only with NSAID and Acetaminophen

39
Q

Codeine

A

mild to moderate pain
low affinity for opioid receptors

effect due to conversion to morphine by CYP2D6

40
Q

Mixed A/As

A 
Peanut butter no butter (PBNB)
PENTAZOCINE
BUTORPHANOL
NALBUPHINE
BUPRENORPHINE
41
Q

PENTAZOCINE
BUTORPHANOL
NALBUPHINE

cause?

A

psychotomimetic effects

42
Q

BUPRENORPHINE

A

approved for management of opioid addiction

43
Q

Mixed A/As are not recommended bc?

A

ceiling effect

44
Q

Tramadol

A

metabolized by CYP2D and CYP3A4
mu agonist
NE and 5HT reuptake inhibitor
mild to moderate pain treatment

45
Q

Naloxone

A

acute opioid overdose

46
Q

Naltrexone

A

opioid and alcohol addiction

47
Q

High efficacy opioids

A

Everything except oxycodone, hydrocodone, pentazocine, and codeine (lowest)

48
Q

Antitussives

A
  • Dextrometorphan and codeine

- suppression of cough

49
Q

Antimotility

A

Diphenoxylate and Loperamide

  • treatment of diarrhea
  • usual doses lack analgesic effects
50
Q

Diphenoxylate

A

contain atropine to discourage overdose

- high doses have CNS effects

FTCM Pharm (4 decks)

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