Pcol Sem 2 Test 3 Analgesics

Front 1

what do you use to treat inflammatory pain

Back 1

NSAID
Steroids

Front 2

what do you use to treat post surgical

Back 2

opiods, NSAIDS

Front 3

what do you use to treat neuropathic

Back 3

anticonvulsants

Front 4

what do you use to treat cancer

Back 4

opiods

Front 5

what do you use to treat headache

Back 5

5-HT agonist

Front 6

what is unique about endogenous opioid peptides

Back 6

opioid alkaloids produces analgesia through actions at regions in the brain containing endogenois opioid peptides which diminish the sensation of noxious stimuli/pain

endogenous peptides normally exist as precursor proteins and need to be activated via trypsin enzyme degredation

Front 7

what are the endogenous opioid peptides

Back 7

endorphins : POMC
enkaphalins
dynorphins

Front 8

where are all 3 receptors precent

Back 8

cerebral cortex
spinal dorsal horn
hippocampus

Front 9

where are the mu, kappa, and delta Rc found

Back 9

mu/kappa = mid brain
delta = amygdala

Front 10

what are the functions of mu, kappa, delta Rc at high []

Back 10

mu = CV, respiratory depression and physical dependency
kappa = micturition (urination)
delta = seizures

Front 11

what are the predominant endogenous ligands for mu, kappa, delta

Back 11

mu: end > enk > dyn
kappa: dyn > end/enk
delta: enk > dyn/end

Front 12

what peripheral tissue are all 3 receptors mainly found

Back 12

GI and Urinary tract

Front 13

what is Opiate Rc coupled function (therapeutic MOA)

Back 13

Adenylate Cyclase inhibition
voltage gated Ca channel inhibition resulting in decrease in neuronal pathway excitability
elevated K current causing hyperpolarization and stabilizing the membrane
PKC/PLC activation

Front 14

what is the gold standard

Back 14

morphine

Front 15

what are the natural opiods

Back 15

morphine
codeine

Front 16

what are the semisynthetic opiods

Back 16

heroin
oxymorphone
hydromorphone

Front 17

what are the synthetic opiods

Back 17

phenylpiperidines: meperidine fentanyl
methadone and cogeners (propoxyphene)
morphinans: levorphanol

Front 18

where does morphine primarily act

Back 18

Mu

Front 19

what is the ADME of opiods

Back 19

well absorbed when given IM, SQ, oral
reach high [] in well perfused organs: brain, liver, kidney, spleen, lungs

most are converted to h2o sol metabolites and excreted via kidney except for phenylpiperidines (meperidine/fentanyl) which undergo hepatic oxidation

Front 20

acute toxicity of opiods causes what and how do you treat

Back 20

miosis, coma, depressed respiration

treat via naloxone, and establish airway and ventilation

Front 21

how does tolerance occur

Back 21

persistance activation of Mu Rc resulting in its downregulation/uncoppling

Front 22

what symptom does tolerance not develop for

Back 22

miosis and constipation

Front 23

what happens to pain when you become tolerant to opiods

Back 23

increase pain sensation
decreased pain threshold

Front 24

what are some symptoms seen w/ opioid abstinence

Back 24

hyperthermia
hyperventilation
mydriasis
diarrhea
chills/gooseflesh
muscle aches

Front 25

what are the contraindications of opiods

Back 25

never combine full agonist w/ partial agonist
elevated intracranial pressure
pregnancy
pt w/ impaired pulmonary, renal, hepatic endocrine functions
w/ other sedative/hypnotics/antipsychotics

Front 26

why are opiods contraindicated in head injury

Back 26

opiods cause respiratory sedation which increase PCO2 and also cause cerebral vasodilation which increases intracranial pressure

Front 27

why are opiods not given during pregnancy

Back 27

fetus may develop a physical dependency

Front 28

what are the properties of meperidine

Back 28

Mu agonist
no antitussive effect (morphine has it)
less constipation (morphine has it)
mydriasis @ toxic levels
cross tolerance w/ morphine
high levels cause seizures

Front 29

what are the properties of Fentanyl

Back 29

Mu agonist
MORE POTENT THAN MORPHINE
short duration of action
used as post operative analgesia

Front 30

what can fentanyl be given w/ as IV anesthetic

Back 30

droperidol

Front 31

what are the properties of methadone

Back 31

Mu agonist
treatment of opioid abstinence syndrome and heroin users
long duration

Front 32

what are the properties of propoxyphene

Back 32

structurally related to methadone
less potent and selective Mu agonist than morphine/codeine
used for mild/moderate pain

Front 33

what is given w/ propoxyphene for higher analgesic activity

Back 33

aspirin
acetaminophen

Front 34

what are the opioid antagonist

Back 34

naloxone
naltrexone
nalmefene

Front 35

what are the properties of naloxone

Back 35

highest affinity for Mu Rc (also antagonises K/D Rc)
used to treat acute opioid OD, withdrawl syndrome in pt w/ physical dependence, reverse opioid effects

Front 36

what are the mixed agonist/antagonist (partial agonist)

Back 36

Buprenorphine
Pentazocine
Nalbuphine
Butorphanol

Front 37

what are the properties of Buprenorphine

Back 37

agonist for Mu Rc
alternative to methadone for managment of opioid withdrawl
ANTAGONIST AT K AND DELTA RC

Front 38

what are the properties of pentazocine, nalbuphine, butorphanol

Back 38

partial agonist

K agonist, Mu antagonist

Front 39

what are the antitussive agents

Back 39

codeine, hydrocodone, dextromethorphan

Front 40

what are the antidiarrheal agents

Back 40

diphenoxylate
loperamide (OTC)

Front 41

what endogenous and selective agonist work @ Mu

Back 41

endorphin
enkephalins
morphine
methadone
fentanyl

Front 42

what endogenous and selective agonist work @ K

Back 42

pentazocine
dynorphin A

Front 43

what endogenous and selective agonist work @ Delta

Back 43

Enkephalins

Front 44

,what is the rank in analgesic effects

Back 44

fentanyl > morphine > NSAIDS