Opioids Flashcards
What is a classical analgesic receptor?
mu receptor
What are opioids a mix of?
Agonist-antagonist agents
What is an opiate? What are some examples?
Natural agents from opium
Codeine, morphine
What are opioids?
Modifications of natural opiates (synthetics)
What are some examples of mixed opioid agonists?
Buprenorphine
Butorphanol
Pentazocine
Nalbuphine
Are mixed agents frequently or infrequently used?
Little used
What is an exception to the little use of mixed opioid agonist-antagoinsts?
Nalbuphine
Describe nalbuphine
More effective in females
Ceiling effect on respiratory depression
Used in L&D
What are endorphins derived from?
Small endogenous peptide hormones
What do endorphins account for?
Variability of response to pain
List the SEs to opiates/opioids
Nausea Itching Sedation & cognitive impairments Respiratory depression (possibly life-threatening) Meiosis (pinpoint pupils) Decreased GI peristalsis -> constipation
How do we deal with the effects of opioids on the GI tract?
Anticipate and prophylax
Can we expect tolerance to opioid constipation?
No
Review slide 42
Bowel regimens for opioid constipation
What opioids do we use for mild-moderate pain?
Tramadol
Codeine
Hydrocodone
What kind of opioid is tramadol? What is it useful for?
Weak opioid analgesic
Useful for chronic pain
What are the 3 forms of tramadol?
Immediate release
Tramadol 37.5mg/acetaminophen 325 mg
ER tabs
What happens as we increase dosage of tramadol over weeks? What does this mean?
High incidence of NV
Limits use for acute pain
Does tramadol have a single or dual MOA
Dual
What is tramadol useful for?
Neuropathic pain
Is tramadol a controlled substance? If so, why? When did this happen if it did?
Yes
Less abuse potential
2014
What kind of opiate is codeine?
Weak analgesic and antitussive
Relate codeine to ASA
60 mg less effective than 650 mg aspirin
What is codeine metabolized by? What does this metabolize codeine to?
CYP2D6
Morphine
What does CYP2D6 inhibitors do to codeine? Give some examples
Decrease its effect Antiemetic phenothiazines (thorazine, compazine, phenergan) Haloperidol Fluoxetine Paroxetine
What % of the population lack the CYP2D6 enzyme?
10%
What forms does codeine come in?
Codeine (C-II)
Tylenol w/ codeine (C-III)
Guaifenesin w/ codeine (C-V)
How is hydrocodone available PO?
Only available w/ acetaminophen PO
How many mg does hydocodone exist w/in Norco?
325 mg
Give two more examples of hydrocodone PO meds
Lortab
Vicoden
How does hydrocodone relate to codeine?
Better pain relief
Longer duration
What is hydrocodone metabolized by and to what?
CYP2D6
Hydromorphone
What % of unintentional overdoses involve combination products? What is the MC opioid in these combination products?
63%
Hydrocodone
What opioids do we give for moderate to severe pain?
Morphine Hydromorphone Oxycodone Meperidine Methadone Fentanyl
What type of drug is morphine?
Prototype pure mu receptor agonist
How many active metabolites does morphine have? How are they eliminated?
What are they?
2
Renally
A neurotoxin and an analgesic 2-4xs that of morphine
What does morphine induce? What happens because of that?
Histamine release
Hypotension, pruritus
What kind of first-pass effect does morphine have?
Significant
What is the parenteral to oral dose ratio of morphine?
1:3
What is the concentration of injectable morphine?
2 mg/mL
Give the examples of oral morphine
Immediate release tabs SR capsules (Kadian) CR tabs (MS Contin) Oral solution (roxanol)
How much more potent is hydromorphone than morphine? What is an issue w/ that?
5-7
Often forgotten by prescribers -> results in iatrogenic overdoses
What are two benefits of hydromorphone?
Less histamine release
No active opioid metabolites
In what doses do the sustained release products of hydromorphone come in?
8
12
16
32 mg
Why was SR palladone recalled by the FDA?
Alcohol destroyed time-release mechanism, which led to overdoses
What is a common concentration of hydromorphone injections?
2 mg/mL
How does oxycodone relate to morphine?
More potent Less SEs (histamine release, pruritus, N)
What is oxycodone metabolized to and by what?
Oxymorphone
CYP2D6
What pt populations is oxycodone helpful with?
PTs w/ CYP2D6 deficiency or on inhibitors (phenothiazine antiemetics, fluoxetine, paroxetine)
Useful in non-responders to codeine and hydrocodone
Give some examples of oxycodone dosage forms
Oxycodone IR
Roxicodone
Oxycodone CR
How do you administer oxycodone CR and how often?
Q12 hours PO
Is meperidine a 1st line agent?
No
Describe the qualities of meperidine
Lipophilic
Rapid onset
Shorter duration (2-3 hours)
What is meperidine metabolized to? Whys is that a bad thing?
Normeperidine
Its neurotoxic
Does normeperidine have a long or short half life?
Long
What are the indications of noremperidine toxicity?
Euphoria
Irritability
Seizures
Is normeperidine toxicity reversible by opiate antagonists?
No
How is normeperidine eliminated?
Renally
When is meperidine contraindicated? What does it cause?
Pts on MAOIs
Serotonin syndrome
When can meperidine be used?
In pts w/ opiate allergies
What is meperidine useful in controlling?
Post anesthesia shivering
What makes methadone unique? What is one of its uses?
Racemic mix of L and D isomers
Neuropathic pain
What does the L isomer do for methadone?
Opioid activity
What does the D isomer do for methadone?
NMDA antagoinst and NE/5HT reuptake inhbitor
Describe the half-life of methadone
Very long and variable
12-190 hours
Usually about 24
How long do methadone’s analgesic effects last?
4-8 hours
How often do you dose methadone for analgesia?
Q6-8 hours
How much more potent than morphine is fentanyl?
In what units is it dosed because of this?
100 times
Mcg
Describe the qualities of fentanyl
Extremely lipophilic
Rapid onset
SHORT duration (30-60 mins)
Does fentanyl have any metabolites? What does this mean for use?
No
One of the safest options in renal failure
How do the AEs of fentanyl compare to morphine/dilaudid? Describe them
Fewer
Minimal histamine release, little hypotensive effect
How do we give fentanyl?
Injection
Lozenge
Transdermal (duragesic)
Review slide 55
Duragesic calculator
With what pt population do we not use duragesic cautions?
Opiate niave pts
How long do we monitor the respiratory rate for pts recieving the duragesic patch?
First 24 hours
When do we replace the duragesic patches?
Q 72 hours
Do you just add additional patches of duragesic?
No
What do you need to look for when admitting out patient pts on the duragesic patch?
Multiple patches
What are the fentanyl lozenges used for?
Long-standing chronic pain
cancer
What are two fentanyl lozenge products?
Fentora
Actiq
What kind of drug is naloxone?
Pure mu receptor antagonist
What is naloxone used for?
To reverse sedation/respiratory depression
How do you administer naloxone?
1) Dilute 0.4 mg to > 10 mL saline (0.9% NaCl)
2) administer via slow IVP (1 mL/1-2 min)
3) Monitor respiratory rate
4) Stop when RR increases
Review slide 60 and 62
Equianalgesic dosing and chart
Review slide 65
Common PCA settings
What is oxycodone w/ acetaminophen?
Percocet
What is oxycodone w/ aspirin?
Percodan