Pharm 10 Opioids Flashcards Preview

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Flashcards in Pharm 10 Opioids Deck (36)
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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