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Pharmacology- Test 2 Material > 10- Opioids > Flashcards

10- Opioids Flashcards

1
Q

codeine

A

Opioid agonist (morphine derivative)

  • prodrug in which 10% of administered dose converted to morphine via demethylation by CYP2D6 to cause analgesia
  • people who are rapid metabolizers via CYP2D6 can have inc. active drug levels (can have dangerous effects)
  • less 1st pass metabolism when taken orally
  • commonly mixed with acetaminophen (Tylenol #3)
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2
Q

fentanyl (Duragesic)

A

Opioid mu receptor agonist

  • 50-100x more potent then morphine (100mcg fentanyl = 10mg morphine)
  • onset 3-5 min, with variable T1/2 depending on length of administration
  • 100% hepatic extraction (inactive metabolites)
  • –clearance directly correlated to liver blood flow
  • –decreased with P450 inhibitors (cimetidine, erythromycin)
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3
Q

heroin

A

Opioid agonist (morphine derivative)

  • acetylated morphine
  • 2-4x more potent then morphine with faster onset
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4
Q

hydrocodone (Vicodin)

A

Opioid agonist (morphine derivative)

  • metabolized to hydromorphone by CYP2D
  • commonly mixed with acetaminophen
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5
Q

hydromorphone (Dilaudid)

A

Opioid agonist (morphine derivative)

  • about 5x more potent then morphine and more lipid soluble so faster onset
  • onset in 5min; peak 10-20min
  • can be given IV or PO
  • 1-2mg IV Dilaudid = 10-20mg IV morphine
  • glucuronide metabolism forms hydromorphone-6G (less efficacy then morphine-6G) and hydromorphone-3G (inactive metabolite)
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6
Q

meperidine (Demerol)

A

Opioid agonist

  • 1/10th the potency of morphine but more lipid soluble so has faster onset
  • less bradycardia and resp. dep. than with equianalgesic dose of morphine
  • dysphoric and psychotomimetic effects- kappa receptor
  • metabolized in the liver which produces an active metabolite normeperidine that has T1/2 of 14-21 hrs (can cause seizures and death)
  • useful for post-op shivering
  • inhibits serotonin reuptake and can cause Serotonin Syndrome in ppl taking MAOIs or SSRIs
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7
Q

morphine

A
  • classic mu opioid receptor (mu 1 and 2) and influences motivational-effective aspect of pain
  • only 23% non-ionized and able to cross BBB and also has low lipid solubility (1.4) so slow onset of action
  • T1/2 of 2-3 hours and DOA of 4-6 hrs
  • decreases ventilatory responses to inc. CO2 AND dec. O2
  • metabolized (70%) in liver via glucuronidation
  • liver disease has minimal effect on metabolism
  • –reduced blood flow will slow metabolism
  • metabolites excreted by the kidney
  • –M-3-glucuronide 75-85% inactive metabolite
  • –M-6-glucuronide 5-10% active metabolite (10x more potent then parent morphine)
  • excretion of active metabolite can be impaired in renal disease leading to dangerous build-up
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8
Q

Alfentanil

A

μ receptor agonist

  • roughly 10x more potent than MSO4 and 1/10th to 1/4th the potency of fenatnyl (1000mcg Alfent=100mcg Fent=10mg MSO4).
  • Rapid onset of action (1-2”)
  • Approximately 90% in the unionized form at physiological pH
  • lower lipid solubility than fentanyl, so less accumulation in tissues.
  • metabolized in liver, no active metabolites.
  • Give in small increments to decrease onset of respiratory depression.
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9
Q

Remifentanil

A

μ receptor agonist
-“equipotent to Fentanyl”
-Very rapid onset (1”) and offset
-Offset not determined by length of infusion.
+metabolized by nonspecific esterases
-Not great for continued, ongoing pain post-op.
-Dose long acting narcotic and allow MEC to be reached before stopping Remi gtt to prevent hyperalgesia.

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10
Q

buprenorphine (Buprenex)

A

μ receptor Agonist-antagonist

  • partial μ receptor agonist and K receptor agonist
  • high affinity for μ (hard to reverse)
  • good for opioid addiction at higher doses.
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11
Q

nalbuphine (Nubain)

A

μ receptor Agonist-antagonist

  • K receptor agonist, partial μ receptor agonist, and μ receptor antagonist.
  • good for acute moderate to severe pain (not for chronic pain).
  • lower S/E profile.
  • butorphanol is similar, but nubain is 10x more potent than butorphanol.
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12
Q

pentazocine (Talwin)

A

Opioid receptor Agonist-antagonist

  • 2 isomers, but only + has affinity for K receptors.
  • has ceiling effect.
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13
Q

tramadol

A

μ receptor partial agonist

  • also inhibits MAO reuptake.
  • metabolized by CYP2D6 to active metabolite
  • combined with acetaminophen (Ultracet)
  • for mild to moderate acute and chronic pain.
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14
Q

tapentadol

A

μ receptor partial agonist

  • also inhibits MAO reuptake.
  • less pharmacological variability than tramadol.
  • greater μ receptor efficacy
  • metabolized by CYP2C9, 2C19, and 2D6.
  • for mild to moderate acute and chronic pain.
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15
Q

opioids

A

mu, kappa, delta receptor agonist
analgesic effects and other unwanted side effects
inhibit NT- block Ca2+ influx and increase K+ efflux

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16
Q

nocieptors

A

specialized nerve endings

gate control theory- input from afferent and nociceptors are gated in the spinal cord (T cell and substantia gelatinosa)

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17
Q

opioid intoxication

A

overdose
sedation, stupor, coma, death
-unresponsive, respiratory depression, pupil constriction

18
Q

serotonin syndrome

A

Delirium
Fever
Convulsion
Meperidine inhibits the re-uptake of serotonin

19
Q

dynorphins

A

endogenous opioid for the KAPPA receptor

20
Q

endomorphins

A

endogenous opioid for the MU receptors

21
Q

endorphins

A

endogenous opioid for the MU and DELTA receptor

22
Q

enkephalins

A

endogenous opioid for the DELTA receptor

23
Q

delta receptor

A

Location: BRAIN
Action: analgesia, antidepressant effects, CONVULSANT EFFECTS, physical dependence

24
Q

kappa receptor

A

Location: brain, spinal cord, peripheral sensory neurons
Actions: analgesia, anticonvulsant effects, dissociative & delirium, diuresis, dysphoria, miosis, sedation, REDUCED SHIVERING

25
Q

mu receptor

A

Location: brain, spinal cord, peripheral sensory neuron, intestinal tract
Actions: sedation, analgesia, physical dependence, respiratory depression, miosis, euphoria, reduced GI motility, vasodilation

26
Q

motivational-affective

A

unpleasantness and bother to the patient (nauseating, sickening)
- opioids are most effective against this dimension of pain

27
Q

sensory-discriminative

A

sensation, location, quality of pain

28
Q

CYP2D6

A

metabolizes codeine to morphine
metabolizes oxycodone to oxymorphone
metabolizes tramadol and tapentadol

29
Q

CYP3A

A

metabolize tramadol

30
Q

morphine glucuronides

A

M3-glucuronides– 75-85% inactive metabolite, no analgesia, maybe hyper analgesic
M6-glucuronides– 5-10% ACTIVE metabolite, 10x more potent that parent morphine
(excreted by organic ion transporters in the kidney)

31
Q

addiction

A
  • primary, chronic, neurobiological disease with genetic, psychosocial and environmental factors influencing its development and manisfestations
  • characterized by: impaired control over drug use/psychological dependence, compulsive use, continued use despite physiologic, psychosocial and/or econonmic harm, craving
  • uncommon with appropriate medical treatment of acute pain
32
Q

physical dependence

A
  • withdrawl symptoms that are precipitated when an opioid agonist is stopped or an antagonist is given
  • develops concurrently with tolerance
  • common with prolonged use
33
Q

psychological dependence

A
  • impaired control over drug use
  • taking it for the reinforcement
  • related to the mesolimbic dopamine system
34
Q

tolerance

A

decreased response to a drug with repeated use

develops to most opioids, but not to ocular/GI effects

35
Q

withdrawl

A

s/sx: restlessness, insomina, perspiration, abdominal cramps, nausea, vomiting, diarrhea, tachycardia, tachypnea, HTN, hypotension, hot/cold flashes
-gradual reduction of the opioid dose may reduce or eliminate s/sx

36
Q

side effects of opioids

A 
bradycardia
constipation
dysphoria
euphoria
itching
miosis
othrostatic hypotension
respiratory depression
sedation
stupor/coma
vasodilation
vomiting
37
Q

Sufentanil

A

highly selective for μ receptors (synthetic derivative).
-Roughly 500-1000x more potent than eqivalent dosing of MSO4.
+5-10mcg Sufent=5-10mg MSO4.
-more lipid soluble than fentanyl, remifentail, and alfentanil.
+slower onset and offset than remifentanil and alfentanil.
+plan to discontinue infusion about an hour or so before conclusion of case to allow for offset.
-we do not have sufentanil on formulary at UIHC

38
Q

oxycodone

A
  • less first pass metabolism. CYP2D6 active metabolite oxymorphone
  • sustained release when taken whole, bolus dose when crushed
39
Q

methadone

A
  • ultra long acting, half-life 15-60 hours

- useful for chronic pain management, addicted patients maintenance

40
Q

naloxone

A
  • competitive antagonist at mu, kappa, and delta receptors
  • IV or IM effective in 1-2 minutes
  • half-life 60 min (3hrs in infants), may need to redose for opioid reversal
  • metabolized via glucuronidation
41
Q

naltrexone

A
  • oral opioid antagonist, much slower than naloxone, not for acute reversal
42
Q

oxymorphone

A
  • mu receptor and partial delta receptor agonist. 6-8 times more potent than morphine
  • oral medication, NOT metabolized by CYP2D6

Pharmacology- Test 2 Material (10 decks)

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