Pharm 10 Opioids Flashcards Preview

Test 7 > Pharm 10 Opioids > Flashcards

Flashcards in Pharm 10 Opioids Deck (36):
1

Main analgesic receptor

Mu Opioid Receptor (G-protein)

2

Opioid Receptor MOA

1. Decrease Ca current (decrease NT release)
2. Increase K current (Hyperpolarize)

3

Nociceptive afferent synapse

Dorsal Horn

4

Descending pathway synapse

Modulate dorsal horn via interneuron

5

Main Opioid effect

Block Glutamate and Substance P release at Dorsal Horn synapse

6

Opioid effect on Rostral Ventral Medulla

Block inhibition, let RVM inhibit Dorsal Horn

7

Opioid effect on interneuron

Hyperpolarize, block excitatory drive to Dorsal Horn

8

Only Opioid effect not mediated by Mu receptor

Psychotomimesis

9

Morphine problem

Poor lipid solubility

10

-Morphine-
MOA

MOR

11

-Morphine-
Metabolism
Major SE

CYP450

Respiratory depression

12

-Morphine-
CI

MAOI
Alcohol

13

-Fentanyl-
Indication
MOA

Severe pain

Very potent MOR (100x morphine)
Very lipophilic

14

-Fentanyl-
Useful application

Transdermal patches

15

-Fentanyl-
SE

Less nausea
More muscle rigidity

16

-Methadone-
Indication
MOA

Analgesia and Heroin withdrawal
Potent MOR agonist

17

-Meperidine-

MOR agonist
Less potent and quicker than morphine

18

-Meperidine-
Unusual effects

Doesn't prolong labor
Not antitussive
Less constipation

19

-Meperidine-
SE

Toxic metabolites
Tachycardia
Dysphoria

20

-Codeine-
Indication
MOA

Moderate pain
Cough suppressant

MOR, unless you have CYP2D6 mutation (10%)

21

-Codeine-
Metabolism

CYP450
Need to metabolize to morphine with CYP2D6

22

-Propoxyphene-

Toxic Psychosis
Heart Toxicity

23

-Oxycodone-
Indication
MOA

Moderate pain
+acetaminophen = percocet

MOR

24

-Hydrocodone-

Moderate pain
+acetaminophen = vicodin

25

-Tramadol-
Indication
MOA

Use with Naloxone to get analgesic w/o respiratory depression

5HT & NE reuptake blocker
Very weak MOR until metabolized by CYP2D6

26

-Tramadol-
SE
CI

Seizures

SSRIs, MAOIs

27

-Pentazocine-
Indication
MOA

Moderate pain, but has ceiling effects
Formulated with naloxone to prevent euphoria (IV only)

KOR agonist
Partial MOR antagonist

28

-Pentazocine-
SE

Increase HR/BP
Psychotomimesis
Anxiety

29

-Buprenorphine-
Indication
MOA

Strong analgesic
Decrease addiction cravings

KOR antagonist
Partial MOR agonist

30

-Buprenorphine-
SE

Less respiratory depression
More sedation

31

Opioid antagonists:
Need higher doses for 2 drugs

Buprenorphine
Pentazocine

32

-Naloxone-

Fast onset, fast offset (complete first-pass metabolism)
Need multiple injections

33

-Naltrexone-

More potent, longer half life
Helpful for addiction
Don't give for people with pain or dependence

34

Tx strategy for moderate pain

Moderate opioid in combination with acetaminophen or aspirin

35

Effect of giving a partial agonist to a patient already taking a full agonist

Precipitate withdrawal, pain

36

Opioid interaction with MAOIs

HTN