Pharm Block C Opioids

Front 1

Main endogenous ligand for mu receptors

Back 1

endomorphin (main) and beta-endorphin

Front 2

main endogenous ligand for kappa receptors

Back 2

dynorphin

Front 3

main endogenous ligand for delta receptor

Back 3

enkephalin

Front 4

What are 2 G protein types intermediate cell signaling pathways that are used by opioid receptors?

Back 4

Gi/o and GIRK; GIRK is a grotein linked inward rectifying potassium channel (both cause hyperpolarization)

Front 5

What are four ways in which opioids have analgesic properties?

Back 5

thermal, tactile, inflammatory, and neuropathic

Front 6

What are 3 good properties of morphine as an analgesic?

Back 6

no analgesic ceiling, lifts mood, and causes sedation

Front 7

What are 2 side effects of morphine that you never become tolerant to?

Back 7

miosis (pinpoint) and constipation

Front 8

Side effects of morphine

Back 8

"MORPHINE DiD iT"-Miosis and biliary spasM, Ortho. hypoTN, Respiratory depression, Pruritus -DIRECT HISTAMINE RELEASE, Intestinal immobility, Nephritic supression and urinary retention, Dysphoria, Dependence, and Tolerance

Front 9

What is the active form of morphine?

Back 9

morphine-6B-glucuronide

Front 10

In what pt should you watch for accumulation of morphine?

Back 10

renal failure pt

Front 11

heroin and distinguishing feature from morphine

Back 11

diacetyl morphine which crosses BBB faster; once in brain it is converted to morphine

Front 12

hydromorphone duration and potency

Back 12

available as a supository; shorter duration but 8-10x more potent

Front 13

oxymorphone

Back 13

similar to hydromorphone

Front 14

codeine potency and requirement for activation

Back 14

1/10th as potent as morphine; converted to morphine via CYP2D6

Front 15

Why do some pts not get relief from codeine?

Back 15

they may lack CYP2D6 to convert codeine to morphine

Front 16

oxycodon

Back 16

10x potency of codeine so about the equivalent of morphine once oxycodone gets converted; activated by CYP2D6 to morphine

Front 17

hydrocodone

Back 17

same as oxycodone

Front 18

dihydrocodeine

Back 18

same as oxycodone

Front 19

Which form of codeine is often combined with APAP to act synergistically? Why is the combo done?

Back 19

oxycodone, hydrocodone, and dihydrocodeine; this combo increases the analgesia without increasing the negative S/E

Front 20

meperidine S/E

Back 20

"all the M's"-no Miosis, no smooth Muscle spasm, gila Monster venom synergy, toxic Metabolite that can lead to seizures

Front 21

fentanyl potency; onset, duration

Back 21

80-100x as potent as morphine; fast onset with short duration

Front 22

-fentanil and 3 types with relative potencies

Back 22

fentanyl ddx, very fast onset and short duration; al- < su- < remi- (10,000x); "remi has the most letters so it has the most numbers"

Front 23

What are 3 types of opium alkaloids?

Back 23

morphine, codeine and its ddx, and heroin

Front 24

methadone use; feature about route of administration; tolerance?; half life

Back 24

used to tx heroin W/D; oral admin has low 1st pass effect so oral has 4x potency as opposed to 1x if given IV; no tolerance as seen by increased duration of action by repeated use; 24 half life as opposed to 6 hrs for morphine

Front 25

levomethadyl use and distinguishing feature from methadone

Back 25

used for opiate W/D; has 72 hr half life so pt doesn't have to come back for treatment as often as with methadone which wears off in a day (not given in US)

Front 26

propoxyphene use, potency, and S/E

Back 26

synthetic opioid; used when refractory to codeine and often combined with APAP; only as potent as a placebo; cardiotoxic, pulmonary edema, and convulsions (due to the active metabolite)

Front 27

What are 2 opioids that can cause seizures/convulsions?

Back 27

meperidine and propoxyphene

Front 28

naloxone and route of administration

Back 28

Mu receptor antagonist; used for short term opiate O/D but wears off quickly; 95% first pass effect if taken orally, so has to be given IV

Front 29

naltrexone and one hesitancy for its use

Back 29

Mu receptor antagonist; used for longer control of opiate O/D because half life is close to 24 hrs; hepatotoxicity

Front 30

nalmefene and 2 distinguishing features from naltrexone

Back 30

Mu receptor antagonist; no hepatotoxicity but same effects as naltrexone but shorter half life (naltrexone 24 hrs vs nalmefene 6 hrs)

Front 31

What happens to body temp when O/D on opiates?

Back 31

temp drops

Front 32

What happens to skeletal muscles when O/D on opiates?

Back 32

relaxation

Front 33

pentazocine class and route of admin

Back 33

mixed agonist/antagonist; kappa/DELTA agonist but mu antagonist (weak); admin. orally; the kappa and delta effects were analgesic and were reasons people abused it via IV; mu antagonism wasn't strong enough to prevent the analgesia

Front 34

What drug is now combined with pentazocine to prevent its use IV?

Back 34

Pentazocine and naloxone is combined because orally, naloxone has no mu antagonism but when injected IV it prevents any analgesia

Front 35

butorphanol and route of admin

Back 35

mixed agonist/antagonist opioid; kappa agonist and mu antagonist; admin nasally

Front 36

What class of opioids is 5x more potent in women than men?

Back 36

mixed agonists: nalbuphine, butorphanol, pentazocine (note they are also more efficacious in women)

Front 37

nalbuphine: setting in which it is often given, difference from nalorphine; effects of combo with morphine

Back 37

mixed opioid; kappa agonist, mu antagonist; given in an ambulance for analgesia (bu is better than or); ambulances have this because less risk of abuse; less dysphoria than nalorphine which was pulled off the market; morphine will not be able to work due to mu antagonism so morphine + nalbuphine --> W/D

Front 38

What are 3 mixed agonist/antagonist opioids?

Back 38

pentazocine, butorphanol, nalbuphine

Front 39

What are the 3 ways in which Tramadol helps cause analgesia?

Back 39

decreased re-uptake of NE and 5HT in the descending fibers of the spinal cord; weak activation of mu receptors; activation of alpha 2 receptors on pre-synaptic pain fibers to prevent NT release from sensory pain fibers; all of these inhibit the sensation of pain

Front 40

buprenorphine and use

Back 40

partial opioid; partial mu/kappa 3 agonist but kappa 1 antagonist; used for addict analgesic; virtually no abuse potential

Front 41

salvinorin A MOA and S/E and hwo to tx if O/D

Back 41

kappa 1 agonist; hallucinogen; naloxone

Front 42

Which opioid can be used as an analgesic for an addict? Why?

Back 42

buprenorphin because it has partial mu/kappa agonism with kappa 1 antagonism; it has virtually no abuse potential; note that buprenorphin is the only opioid that antagonizes kappa

Front 43

What is the only opioid that has antagonistic properties against a kappa receptor?

Back 43

buprenorphine

Front 44

Is W/D from an opioid life-threatening?

Back 44

no

Front 45

What is the one opioid that doesn't cause miosis?

Back 45

meperidine

Front 46

What is one opioid that is converted to a toxic metabolite that can cause seizures? Convulsions?

Back 46

meperidine and propoxyphene respectively

Front 47

Cardiotoxic opioid

Back 47

propoxyphene

Front 48

opioid that can cause pulmonary edema

Back 48

propoxyphene