Opioids and Non Opioids Flashcards
What do opioids bind to?
Mu and Kappa receptors in the CNS
What are 3 receptors in CNS and which do opioids work on?
MU, KAPPA, delta
Which receptor is responsible for analgesia, rep. depression, sedation, physical dependence, and euphoria?
MU
Which receptor is responsible for analgesia, sedation, and psychotomimetic effects (hallucination/thought disturbance)
KAPPA
how does an AGONIST fxn?
drug that OCCUPIES receptors and ACTIVATES them
How does an ANTAGONIST work?
drug that OCCUPIES a receptor but does NOT ACTIVATE
–BLOCKS receptor activation by AGONISTS
Which gives you full activation? agonist, antagonist, or combo?
agonist
ex: morphine
With a combo of agonist/ antagonist what is happening with Mu and Kappa
overall less activation
- AGONIST effect @ KAPPA
- ANTAGONIST effect @ MU
What does a full antagonist do? example?
- no analgesia
- will precipitate withdrawal
- Narcan, Naloxone
Which drug is the gold standard opioid that all other opioids are compared to?
Morphine
Opioids have no analgesic _____
ceiling!
- can increase dosing as high as needed to manage pain
All of the opioid sxs are limited to person developing a tolerance except
- miosis
- constipation
What is the main cause of opioid death with overdose?
respiratory depression
Common opioid side effects
- resp depression
- sedation
- constipation
- nausea
- itching
- postural hypotension
- urinary retention
Less common opioid side effects
- neurotoxicity
- miosis
- euphoria/dysphoria
- anxiety/unease
- increase ICP
- biliary colic
- immune depression w/ long term use
2 beneficial uses of opioid side effects
- anti-tussive
- anti-diarrheal
2 patiennt conditions when should not use opioids
- head injury –> increase ICP
- cholecystitis –> biliary colic
When do you see respiratory depression with IV, IM, SubQ opioids?
- IV: within 7 min
- IM: within 30 min
- SubQ: within 90 minutes
How long can respiratory depression with opioids last?
4-5 hours
if < 12 RR/minute with opioids
- elevate HOB
- arouse
- treat with naloxone
What can make respiratory depression worse with opioid usage?
if using with other CNS drugs, elderly, or other resp problems
*less likely to happen with chronic use
How do you prevent constipation with opioids?
increase fluid/fiber, prune juice, activity
Meds for opioid constipation use for prevention and treatment
- softener - ducosate/colace
2. stimulant laxative- senna/senokot
What position helps with nausea from opioids?
recumbent
-ambulation makes it worse
what causes nausea with opioids?
stimulation of chemoreceptors in medulla
Nausea is common in the opioid _____ but gets better with____
naive, more doses
How do you deal with itching caused by opioids?
- premedicate with antipruretic
- change to different opioid
If BP is low ____
do not give opioid
How to deal with hypotension from opioids?
- change position slowly
- only up with assistance
- do not give if BP is too low
How to manage urinary retention from opioids
- monitor
- encourage fluids
- may need I&O
- avoid anticholinergic drugs
List the 5 strong opioids
- Morphine Sulfate
- Hydromorphone (Dilaudid)
- Fentanyl
- Methadone (Dolophine)
- Meperidine (Demerol)
(many horny females mate madly)
Fentanyl is ____ times stronger then morphine and is dosed in ____.
80X, micrograms
When is fentanyl used? chronic or acute?
chronic
Fentanyl also comes in which 2 unique routes
patch an nasal spray
What is methodone used for?
low dose to treat opioid addiction
Why is methadone difficult to dose?
long half life
Methadone can’t be used with which population?
elderly
Methadone has which unique risk/adverse affect?
Toursad de Pointe
How long should Meperidine (Demerol) be used for?
2 days max!
Why can you only use Meperidine for a short time?
-makes a toxic metabolite called “normaperidine” which can cause seizures
Half life of Meperidine?
Half life of normaperidine?
2-4 –> frequent dosing
24-48 hours with normal renal fx
How would normaperidine toxicity manifest?
nervousness, temors, seizure
Meperidine is a ____opioid and gives patients a sense of ____
synthetic, euphoria
List 4 moderate to strong opioids
- Codeine and Tylenol (Tylenol #3)
- Hydrocodone and Tylenol (Vicodin or Loratab)
- Oxycodone and Tylenol (Percocet, Tylox)
- Oxycontin Extended Release
Why give tylenol with moderate to strong opioids?
-potentiates giving synergistic effect
Which of the moderate to strong opioids is the most widely used RX in the USA?
Hydrocodone + Tylenol (vicodin, loratab)
Which of the moderate to strong opioids has a high abuse potential and is thus being used less?
oxycontin extended release
What class does Tramadol (ultram) fall under?
Non-opioid centrally acting Analgesic
How does Tramadol (ultram) work?
- analog of codeine
- weak action at MU receptors
- BLOCKS Norepinephrine and Serotonin
How long until Tramadol (Ultram) takes effect? How long last?
- onset within 1 hour
- work for 6 hours
Side effects of Tramadol (Ultram)
(non-opioid centrally acting analgesic)
-sedation, dizziness, headache, dry mouth, constipation, serious risk of suicide
How do opioid agonist- anatgonists work?
bind as AGONIST on KAPPA
weak ANATAGONIST on MU
What are the benefits of Agonist- antagonist opioids?
-decrease analgesia and respiratory depression –> decrease abuse potential
Side effects of opioid agonist-anatagonist?
-psychomimetic effects due to Kappa binding
What happens if give agonist-antagonist to patient who is physically dependent on an opioid?
withdrawal
Examples of opioid agonist- anatagonist?
Butophanol (stadol)
Pentazocine (Talwin)
Which class of drugs is frequently used in Labor and Delivery and why?
Agonist/antagonist due to decrease risk of respiratory depression in neonate
What is the fxn of opioid antagonist?
- BIND to MU and KAPPA but no analgesia
- used to reverse overdose/sedation
Examples of opioid antagonist
Naloxone (narcan)
-
Duration of opioid agonist Naloxone
1 hour
Route for opioid agonist Naloxone
IV, IM, SubQ , Nasal
Naloxone is only effective on opioid ____ or _____
agonist or agonist/antagonist
What fxn of is Alvimopan (Entereg)?
- opioid ANTagonist
- works on selective Mu receptors in bowel
- blocks adverse effects on bowel action- no effect on analgesia
Why would you used Alvimopan (Entereg)?
-short term use to prevent ileus in bowel resection surgery and accelerate bowel recovery
Alvimopan (Entereg) can only be used in ____ patients due to increase risk of ____
hospitalized, heart attack
2 types of non-opioids for pain?
- NSAID (nonsteroidal anti inflammatory drug)
2. Acetaminophen
Acetaminophen and NSAIDS both work on what enzyme?
cyclooxygenase
Where is cyclooxygenase found?
in all tissues
Cyclooxygenase is divided into what 2 categories?
Cox 1 and Cox 2
What is the function of Cox2 ?
-mediates pain, inflammation, fever
What is the function of Cox 1?
GI mucosal protection, renal flow, platelet thomboxane (clotting)
What do prostaglandins do?
mediate pain, inflammation, fever, GI mucosal protection
Whose good, cox 1 or cox 2? and why?
Cox 1
- protects stomach
- protects renal fxn
- protects against bleeding
Whose bad, Cox 1 or 2? and why?
Cox 2
-promotion of Mi, stroke
How do 1st generation NASIDS work?
- nonselective blockage of Cox 1 and Cox 2
- decrease pain, inflammation, fever
- increase ulceration, bleeding risk, renal impairment
What generation of NSAID is Aspirin?
1st generation
How does Aspirin Fxn?
-irreversible inhibition of COX resulting in long acting effect
What chemical family does aspirin belong to?
Salicylate
Benefits of aspirin
- analgesic for moderate/mild musculoskeletal pain
- antipyretic
- anti inflammatory in high doses
- antiplatelet effect
- colon cancer prevention in high dose
A high dose of aspirin can cause what 2 BENEFICIAL things?
- colon cancer prevention
- anti inflammatory
Aspirin and antiplatelet effect, dosing?
81 mg
one dose lasts a week for preventing platelet aggregation to prevent stroke/ TIA
When not to use aspirin
- Visceral organ pain
- Kids with previous viral illness (Reyes Syndrome)
- 1 week prior to surgery
- Bleeding disorders
- Alcoholic use disorder (GI bleed risk)
- Renal impairment
- Allergic rxn (hx asthma, rhinitis, nasal polyps)
Long term side effect from Aspirin?
gastric ulceration, perforation, bleeding
High dose Aspirin has what toxicity
salicylate toxicity
–headache, dizziness, tinnitus, sweating
Patient education for Aspirin?
- take with milk/food
- prophylaxsis proton pump inhibitor for high risk population like elderly
Examples of non-aspirin 1st gen NSAIDs?
IBUPROFEN, naproxen, dilofenac
Indication for using ibuprofen?
- analgesic
- anti-inflammatory
- antipyretic
Side effects of ibuprofen
- gastric ulceration
- bleeding
- renal impairment
- RISK OF MI/STROKE (lower then COX2 though)
Who should not take ibuprofen?
cardiac history
How does ibuprofen work?
nonselective blockage of cox 1 and cox 2
What is Ketorolac (Toradol)? Duration of use?
- IV formulation of 1st gen non aspirin NSAID
- only use for 5 days
Whats up with NSAIDS and Kidneys?
If give NSAID it will block prostaglandin making afferent arteriole constrict causing decrease blood flow to the kidney
-prostaglandins keep the afferent arteriole vasodilated
How doe 2nd generation NSAIDs fxn?
selectively inhibit Cox 2, still effects Cox 1 a little bit
Which is more dangerous 2nd or 1st gen NSAID?
2nd because of increase risk of MI/ stroke
What are the indications of use for 2nd generation NSAID?
- analgesic
- anti-inflammatory
Side effects of 2nd generation nsaid?
- gastric erosion/ulcers
- MI/stroke
- renal impairment
example of 2nd generation NSAID?
Celecoxib (Celebrex)
What is acetaminophen not?
NSAID or Opioid
Anti-inflammatory
How does Acetaminophen fxn?
- selective inhibition of COX (enzyme that makes prostaglandins)
- only works in CNS
Indications for using Acetaminophen?
- analgesic
- antipyretic
1 side effect of acetamiophen?
Liver injury!
Max dose of acetaminophen for regular and chronic alcohol abuse
regular = 4 g alcohol = 2 gram
What is treatment for toxicity from acetamiophen?
Acetlycystine (Mucomyst)
-minimized liver damage
If acetylcystine is given with _____hours there is ___% chance of full recover
8-10 hours of overdose, 100%
Which medication smells like rotten eggs?
acetylcystine
Preferred route for acetylcystine is _____ but also comes in ____
preferred = oral
comes in - IV
Chronic use of NSAIDs can lead to what?
hypertension
Multimodal pain order
- using adjuvants (gabapentin, antidepressant, flexoril)
- around the clock order for tylenol and ibuprofen
- ice therapy
- heating pad
- abd binder
- tens unit
- local anasethetic
