opioids

Question 1

what are the three opioid receptors?

Answer 1

mu, kappa, delta

Question 2

agonizing mu leads to what body responses?

Answer 2

analgesia, respiratory depression, sedation (plus bradycardia, euphoria, and physical dependence)

Question 3

agonizing kappa leads to what body responses?

Answer 3

analgesia and respiratory depression

Question 4

agonizing delta leads to what body responses?

Answer 4

analgesia, respiratory depression, and sedation

Question 5

what three places are the mu receptors? what does binding cause?

Answer 5

CNS, GI, urinary bladder

causes inhibition of ascending pain pathway (alters perception and response to pain)

Question 6

where are kappa receptors? what does binding cause?

Answer 6

dorsal horn of spinal cord

decrease release of substance P

Question 7

binding of opioid receptors cause what two things?

Answer 7

inhibit release of excitatory NT from nerve terminal (dec Ca influx) AND increases amount of K leaving post synaptic cell

Question 8

7 forms of opioid preparations

Answer 8

oral, injectable, rectal suppository, transdermal patch, intranasal spray, buccal transmucosal, PCA

Question 9

need to remove transdermal patch before what procedure and why?

Answer 9

before MRI because can get burns

Question 10

compare use of MSContin and MSIR oral preps

Answer 10

MSContin- slow release which gives longer and more stable pain control but doesnt work fast
MSIR- quick release which gives faster relief for breakthrough pain

Question 11

intranasal spray is used for what type of relief? what are two advantages?

Answer 11

QUICK relief

avoids first pass metabolism and don’t need to give as high of a dose

Question 12

what are the three types of opioid action on receptors?

Answer 12

full agonist, partial agonist, mixed agonist/antagonist

Question 13

a full agonist binds to what receptor? produces what kind of response?

Answer 13

binds to mu receptor and produces a maximal response

Question 14

describe analgesia effect with full agonist

Answer 14

NO ceiling effect- can keep increasing dose to increase pain relief
stop when analgesia is reached or dose limiting side effects are reached

Question 15

a partial agonist binds to what receptor? and produces what type of response?

Answer 15

binds to opioid receptor and produces a less-than-full response when fully occupying the receptors

Question 16

how do mixed agonist/antagonists work?

Answer 16

drug acts as full agonist but antagonist binds to receptors as well (without activation) to prevent agonist from binding = LESS THAN FULL EFFECT

Question 17

full agonist medications (12)

Answer 17

Codeine
Morphine
Hydrocodone
Hydromorphone
Oxycodone
Oxymorphone
Methadone
Meperidine/Demerol
Fentanyl
Sufentanyl, alfentanyl, remifentanyl (RAS-nyls)

Question 18

what is our partial agonist drug?

Answer 18

buprenorphine

Question 19

tramadol is a synthetic analog of what drug? it is a weak morphine receptor agonist with ______ and ______. what level of controlled substance?

Answer 19

codeine; NET and SERT; 4

Question 20

what can tramadol cause in some patients?

Answer 20

cause or exacerbate seizures (esp people who are already taking meds that lower seizure threshold- TCAs, SSRI, MAOI

Question 21

Nucynta is what type of receptor agonist and what type of inhibitor?

Answer 21

opioid agonist and NE reuptake inhibitor

Question 22

what significant ADR can you get while using Nucynta with an MAOI?

Answer 22

serotonin syndrome (too much serotonin in body)- don’t use within 14 days of taking MAOI

Question 23

what can having no ceiling effect cause?

Answer 23

respiratory depression

Question 24

how do you calculate total daily dose of opioids? 3 steps

Answer 24

1) . determine total amount of EACH opioid taken per day
2) . multiply each dose by conversion factor to get MME
3) . add MMEs together

Question 25

above 50 on MME score means patient is at an increased risk of what?

Answer 25

respiratory depression

Question 26

how to dose opioids when stopping use?

Answer 26

TAPER- avoid ADRs and seizures this way

Question 27

oral opioids are metabolized how? how does this impact dose?

Answer 27

significant first pass effect for oral opioids (this VARIES per person)- important because oral dose might be a lot higher than parenteral

Question 28

describe distribution for oral opioids

Answer 28

rapidly leave blood compartment and localize in highly perfused tissues (LARGE volume of distribution)

Question 29

what three forms of opioids are absorbed well?

Answer 29

IM, SQ, PO

Question 30

morphine is metabolized to what 2 things?

Answer 30

M3G and M6G

Question 31

Hydromorphone is metabolized to what?

Answer 31

H3G

Question 32

what two metabolites have neuroexcitatory properties and can cause seizures? what pt pop do you need to watch these in?

Answer 32

M3G and H3G; watch in renal failure (CNS side effects) pts or pts on morphine/hydromorphone for a LONG time

Question 33

what does M6G accumulation cause?

Answer 33

over-sedation and respiratory depression

Question 34

Meperidine becomes what metabolite?

Answer 34

normeperidine

Question 35

what does normeperidine cause?

Answer 35

TOXIC metabolite- seizures in patients with renal failure, elderly, or on a high dose for a long time

Question 36

oxymorphone goes through what type of metabolism?

Answer 36

phase 2- converts drug into more water soluble INACTIVE metabolites

Question 37

CNS effects that occur when stimulating opioid receptors (6)

Answer 37

1) . euphoria 2) . sedation without amnesia 3) . dose related resp depression with inc PCO2 (inc cerebral pressure) 4) . cough suppression with codeine 5) . Miosis (pupil constriction)- no tolerance 6) . nausea/vomiting activation of chemoreceptor zone

Question 38

how does cough suppression with codeine use lead to airway obstruction?

Answer 38

other opioids may allow accumulation of secretions so by decreasing cough, secretions could block airway

Question 39

what do you always want to make sure of in a pt who is taking codeine?

Answer 39

that they can metabolize it into morphine

Question 40

in what two cases can opioids affect BP?

Answer 40

if pt has CV disease or in a hypovolemic state, opioids can cause blood vessel dilation and hypotension

Question 41

what effect does meperidine have on CV system?

Answer 41

binds to M2 receptor as an antagonist and increase HR

Question 42

what opioid receptor causes constipation when activated?

Answer 42

MU

Question 43

opioid receptor activation causes what in pts with gallbladder dz?

Answer 43

contraction of biliary smooth muscle, increasing pain

Question 44

opioids have what effect on the bladder?

Answer 44

increase bladder tone and can lead to urinary retention

Question 45

opioids can have what effect on the uterus?

Answer 45

it can decrease uterine tone and potentially prolong labor (still used tho)

Question 46

opioids in what form can cause pruritis?

Answer 46

parenteral- due to histamine release

Question 47

tolerance of opioids develops how fast?

Answer 47

in 2-3 weeks if chronically exposed

Question 48

what three ADRs of opioids do you never develop tolerance to?

Answer 48

miosis, seizures, and constipation | -tolerance to analgesia and other effects

Question 49

what are four opioid constipation treatments?

Answer 49

relistor, movantik, symproic, entereg

Question 50

how does opioid rotation work for tolerance?

Answer 50

switch pt off current opioid to different one AND at a lower dose

Question 51

what two things will make opioid withdrawal worse?

Answer 51

higher the dose and longer the pt has been taking it

Question 52

which class of opioids are more addictive?

Answer 52

full agonists

Question 53

pregnant women dependent on opioids should switch to what two specific types?

Answer 53

buprenorphine or methadone

Question 54

what are four pt populations who opioids are contraindicated in?

Answer 54

1) . Head injuries- opioids inc PCO2 by inc cerebral blood flow 2) . Pregnancy 3) . COPD/lung dz- opioids dec resp drive 4) . hepatic/renal impairment (accumulation of metabolites)

Question 55

always prescribe what with a benzo prescription?

Answer 55

narcam (or other antagonist)

Question 56

5 drugs classes that increase respiratory depression when used with opioids

Answer 56

alcohol, general anesthetics, phenothiazines, benzos (Ativan/valium), TCAs

Question 57

avoid what type of drugs with opioid use so that you don't get urinary retention or constipation

Answer 57

anticholinergics

Question 58

which drugs increase risk for serotonin syndrome?

Answer 58

MAO inhibitors, methadone, meperidine, fentanyl, nucynta

Question 59

WHO ladder- Mild pain moderate pain severe pain

Answer 59

mild- non opioid (Tylenol, aspirin, NSAID), +/- adjuvant moderate- opioid (codeine/tramadol), +/- non opioid, +/- adjuvant severe- opioid (morphine/fentanyl), +/- non opioid, +/- adjuvant

Question 60

Acute pain management: what to use for mild-moderate pain localized pain severe pain

Answer 60

mild-moderate: nonopioids- asp, Tylenol, NSAIDs localized: topical (diclofenac gel or lidocaine) severe: immediate release opioids ONLY ( lowest effective dose and no more than 7 days)

Question 61

how to treat chronic non cancer pain

Answer 61

use non pharm tx first (PT, acupuncture, chiropractor, CBT) and then agents for acute pain until pain is relieved

Question 62

what do you give pts with chronic cancer pain?

Answer 62

FULL AGONISTS- not worried about addiction in these people; inc dose if tolerance is developed; give immediate release products for breakthrough pain

Question 63

how to tx neuropathic pain (4)

Answer 63

1) . antidepressants- TCAs, SNRIs 2) . antiepileptics- gabapentin, pregabalin, zepines 3) . topicals- lidocaine, diclofenac 4) . opioids if nothing else works

Question 64

what opioid might you use with acute pulmonary edema?

Answer 64

morphine (MONA-B)- decreases SOB (usually Lasix is 1st line)

Question 65

what opioid should you use if pt is having acute pain from an MI?

Answer 65

morphine

Question 66

should Plavix be taken with morphine?

Answer 66

no, decreases Plavix levels so patient would clot faster

Question 67

how do you use opioids for cough/diarrhea? what two agents should be used?

Answer 67

at much lower doses (not like pain doses); dextromethorphan (OTC cough suppressant) or diphenoxylate paired with atropine for diarrhea

Question 68

how long do opioid antagonists take to work? what are our two agents?

Answer 68

1-3 minutes; naloxone and naltrexone (revia/vivitrol)

Question 69

naltrexone blocks what opioid and its effects?

Answer 69

heroin effects for up to 48 hours

Question 70

opioids are not prescribed to people younger than....

Answer 70

18 years old