Pain Non-COX (2)

Question 1

Acetaminophen how works and 4 effects

Answer 1

Inhibs prostaglandins in CNS but min effect on COX in periphery

analgesic
antipyretic
weak anti-inflam
no anti-platelet effects

Question 2

Acetaminophen is rapidly absorbed in the GI subject to _________ and can attack the ________. It’s excreted in ______

Answer 2

1st pass metabolism
attack of the liver
urine

Question 3

N-acetylcystine

Answer 3

Tx for acetaminophen OD

don’t exceed 3G acetaminophen/24hrs

Question 4

schedule __ drugs are a high risk for abuse, you need a new prescription every month…(4 ex)

Answer 4

II

morphine, oxycodone, methadone, meperidine

Question 5

Mu receptor agonists cause.. (7)

Answer 5

resp depression, phys depression, tolerance, constipation, euphoria, miosis; primary analgesic response

Question 6

Kappa receptor agonists cause… (4)

Answer 6

spinal-level analgesia and sedation, w/o respiratory depression, miosis

Question 7

Sigma receptor agonist cause… (4)

Answer 7

vasomotor stimulation, psychotomimetic effects, miosis,

BINDS NON-OPIOID AGENTS

Question 8

Delta receptor agonists cause…

Answer 8

Enkephalins (natural opioids) more selective w/the delta receptors in the periphery

Question 9

Pure agonists bind __ receptors to produce analgesia that inc with dose w/o ceiling effect
Name the 3 groups

Answer 9

mu

Phenanthrenes
Phenylpiperidine
Diphenylheptane

Question 10

Partial agonists/antagonists partially stimulate the mu receptor and antagonize the ___ receptor

Answer 10

kappa

reduced sfx at mu receptor, psychomimetric effects d/t kappa antagonism

possible w/drawl sx in pt dependent on pure agonists

Question 11

Name the 2 strong phenanthrenes

Answer 11

morphine

hydromorphone (dilaudid)

Question 12

what is the strong phenylheptylamine

Answer 12

methadone

Question 13

Most widely used phenylpiperdines are strong agonists, but _________ and _________ specifically

Answer 13

meperidine and fentanyl

Question 14

Morphine action

Answer 14

Mu receptor

works in CNS and GI, inhibs pain by inhib NT release

extensive 1st pass effect

Question 15

Morphine effects (3)

Answer 15

suppress cough
relieves diarrhea (eventual constipation)
histamine release

Question 16

PT on morphine needs to be monitored for

Answer 16

respiratory or CV depression

Question 17

Meperidine action

Answer 17

Binds to opioid receptors and kappa

antimusc activity, can precipitate tremors or sz.

causes mydriasis rather than miosis seen in morphine b/c kappa effect

Question 18

Meperidine is usually given__________, it is excreted in _________; caution 1/2 life longer in ______and _____ pts

Answer 18

post surgery
excreted in urine
inc in liver and kidney

Question 19

Meperidine contraindicated in pts taking _________ in past 2-3 wks
3 other meds also interact

Answer 19

MAOI (metabolize NE=bp changes, excitatory and rigidity)
barbiturates
chlorpromazine
phenytoin

Question 20

Meperidine NOT to be used in pts with_______

Answer 20

chronic pain (build up of metabolite)

Question 21

with meperidine moniter pt for________

Answer 21

sx of jerking/twitching (indicates normeperidine accumulation)

Question 22

Methadone action

Answer 22

greatest action at mu receptor

equal potency to morphine with less euphoria

analgesic substituted for morphine/heroin to control w/drawl

Question 23

methadone is a good addiction tx because

Answer 23

less euphoric

1/2 life is loooonnng (therefore inc risk for toxicity)

Question 24

2 cautions with Methadone

Answer 24

variable kinetics

wide range of dose equivalents

Question 25

7 signs of methadone withdrawal

Answer 25

``` lacrimation rhinorrhea diaphoresis yawning restlessness insomnia dilated pupils ```

Question 26

Fentanyl is more/less potent

Answer 26

more potent than morphine

Question 27

Fentanyl is used for ___________ combined with droperidol.

Answer 27

anesthesia | esp patches in post-operative pain

Question 28

Fentanyl cautions..(3)

Answer 28

abuse lack of titration variable absorption

Question 29

Fentanyl has more/less allergy risk

Answer 29

LESS allergy risk b/c no histamine release | prefered in pts with CV issues

Question 30

Fentanyl causes _____ depression and when taken with P450 inhib effect of fentanyl is _____

Answer 30

CNS depression | increased

Question 31

what are the three mild-moderate phenanthrenes

Answer 31

codeine oxycodone hydrocodone

Question 32

what are the 3 mild-moderate phenypiperidines

Answer 32

diphenoxylate diphenoxylate loperamide

Question 33

2 partial agonist/antagonist phenanthrenes

Answer 33

nalbuphine | buprenorphine

Question 34

what is the partial agonist/antagonist morphinans

Answer 34

butorphanol

Question 35

what is the partial agonist/antagonist benzomorphans

Answer 35

pentazocine

Question 36

buprenorphine action

Answer 36

20x more potent than morphine (long acting) partial mu agonist can antagonize resp dep caused by morphine

Question 37

butorphanol and nalbuphine action

Answer 37

analgesic, also 20x more potent than morphine kappa agonist~ spinal analgesia

Question 38

Pentazoxine action

Answer 38

mild mu and kappa agonist sigma activity may account for dysphoria made in an attempt to have little or no abuse potential

Question 39

Naloxone binding

Answer 39

Pure antagonist | high affinity for mu receptor and competitive antagonist of kappa and delta..

Question 40

naloxone use

Answer 40

no effect in normal individuals but in pts taking opiates it can reverse OD, respiratory depression and coma DOA up to 48 hours

Question 41

Tramadol

Answer 41

weak mu agonist inhibit NE/SE CNS reuptake

Question 42

what are the 4 centrally acting skeletal musc relaxants and why are they used

Answer 42

cyclobenzaprine baclofen tizanidine carisoprodol releif from musc spasm and hyper-reflexia

Question 43

centrally acting skeletal musc relaxants are metabolized by ________, and the 3 side effects are

Answer 43

hepatic metabolism drowziness and xerostomia N/V seen in Baclofen

Question 44

Peripherally acting skeletal musc relaxants are aka ________________ agents

Answer 44

neuromuscular blocking agents

Question 45

what are the 2 peripheral neuromuscular blocking agents

Answer 45

succinylcholine | Vecuronium

Question 46

how do neuromusc blocking agents work?

Answer 46

block the transmission of cholinergics between somatic motor neuron and skeletal fibers at neuromuscular jxn