Opioids

Question 1

agonists MOA

Answer 1

bind to/activate Mu/Kappa/Delta receptor in the brain. elicit endorphin response

Question 2

pharm characteristics of agonists

Answer 2

tolerance, dependence, no ceiling to pain effect, no antipyretic or anti inflam

Question 3

agonist side effects

Answer 3

constipation, vasodilation, urinary retention, seizure, res depression, mood, mitosis, N/V

Question 4

agonist drug examples

Answer 4

codeine, morphine, oxycodone (oxycontin)

Question 5

traditional agonists and allergy

Answer 5

cross react! codeine/morphine/oxy

Question 6

alternative agonists- why use?

Answer 6

no allergy cross reaction, Dif side effects/costs/route

Question 7

alternative agonist examples

Answer 7

fentanyl, methadone, meperidine

Question 8

fentanyl

Answer 8

80-100x more potent than morphine- never use first. long acting dermal, slow parenteral.

Question 9

methadone MOA

Answer 9

long acting mu receptor

Question 10

methadone half life

Answer 10

pain is shorter half-life than withdrawal. concern- cardiotoxic QT

Question 11

meperidine

Answer 11

anti diarrheal! active metabolite&raquo_space; SEIZURE

Question 12

what is the seizure drug

Answer 12

meperidine

Question 13

antagonist mOA

Answer 13

competitive inhibition, block binding/activation of receptor

Question 14

antagonist example drug

Answer 14

naloxone

Question 15

naloxone

Answer 15

high mu affinity, displace opioid. quick onset, short duration, no oral bioavailability

Question 16

mixed drug

Answer 16

buprenophine

Question 17

buprenophine MOA

Answer 17

kind Kappa and Mu, agonist and antagonist

Question 18

mixed adverse

Answer 18

sedation, dizzy, nausea, acute withdrawal from other opioids

Question 19

opioid like drug

Answer 19

tramadol

Question 20

tramadol MOA

Answer 20

weak mu agonist, inhibit serotonin and norepinephrine reuptake

Question 21

tramadol pharm

Answer 21

less tolerance/dependance than opioids, prodrug, CYP450

Question 22

CYP450 drugs

Answer 22

codeine, tramadol