EXAM #3: OPOID ANALGESICS Flashcards Preview

Pharmacology > EXAM #3: OPOID ANALGESICS > Flashcards

Flashcards in EXAM #3: OPOID ANALGESICS Deck (41):
1

What types of disease are opioid analgesics in to delay or arrest the disease process?

Autoimmune disease e.g. RA

2

Where do opioid analgesics exert their MOA?

Ascending:
1) At the damaged/inflammed peripheral nerve
2) Dorsal horn/ spinal cord
3) Thalamus

Descending pathways

3

What are the effects of opoids?

- Euphoria
- Analgesia
- Sedation
- Anti-diarrheal
- Cough suppression

4

What is opium?

Exudate from poppy seeds

5

What is an opiate?

Drug extracted from the exudate of a poppy seed

6

What is an opoid?

Natural or synthetic drug that binds to opoid receptors w/ agonist effects

7

What is a narcotic?

General term to categorize drugs that treat moderate to severe pain

8

What are the endogenous opoids?

Endorphins
Enkephalins
Dynorphins

9

Agonism of what subtype of opoid receptor produces the MOST analgesia?

Mu

****Kappa and delta do produce some analgesia****

10

What is the difference between Mu1 and Mu2?

Mu1= outside the CNS
Mu2= inside the CNS

11

What is morphine metabolized to? What is unique about the metabolites?

Morphine undergoes glucuronidation to two products:
1) Morphine-3-glucuronide (90%)
2) Morphine-6-glucuronide (10%)

*****Morphine 6-glucuronide is MORE potent than morphine*****

12

What are heroin and codeine metabolized to?

Morphine

13

What happens upon Mu opoid receptor activation to produce analgesia?

- Mu opoid receptors are GPRCs coupled to Gi subunits
- Decreased adenylyl cyclase
- Decreased cAMP

-->Less intracellular Ca++ and increased K+ opening i.e. INHIBITION or neurotransmission

14

How do opoid analgesics inhibit the ascending pain pathways?

1) Inhibition of afferent pain transmission
2) Blocked peripheral effects
3) Blocked dorsal horn of the spinal cord

15

How do opioid analgesics affect the descending pain pathways?

Block inhibitory GABAergic interneurons

****This leads to ENHANCED INHIBITION of nociceptive processing*****

16

What is unique about the analgeisa produced by opioid analgesics?

Reduce BOTH the sensory and affective components of pain

17

What is an important adverse effect of opoid analgesics?

Respiratory depression

18

What should you keep in mind about opoid analgesics and head trauma?

1) Respiratory depression leads to increased Co2 tension
2) Increased Co2= reflexive cerebral vasodilation

****This can be dangerous with head trauma****

19

What is the effect of opioids on histamine?

Opioids can induce histamine release leading to urticaria

20

List the theraputic indications for opioids.

1) Analgesia
2) Anesthetic
3) Anti-tussive
4) Anti-diarrheal
5) Acute pulmonary edema

21

What class of drugs are contraindicated with opioids?

MAOIs

22

What specific opioid should be avoided if a patient is taking a MAOI?

Meperidine

23

What is the adverse reaction that happens with co-administration of Meperidine and MAOIs?

Hyperpyrexia

24

What is the prototype strong opioid agonist used for severe pain?

Morphine

25

What is the prototype moderate agonist used for moderate pain?

Codeine

26

What is the prototype opioid antagnoist?

Naloxone

27

What receptors do strong opioid agonists interact with?

Mu

28

What is the only opioid agonist used as an anti-tussive agent?

Codeine

29

What drug is related to the opioids that is used as an OTC anti-tussive?

Dextromethorphan

30

What is loperamide?

Antidiarrheal

31

What is the MOA of Tramadol?

Mu agonist PLUS:
- 5-HT/NE uptake inhibitors

32

How does the potency of Hydromorphone compare to morphine?

7-10x more potent (Dilaudid)

33

What is the only opioid that is available in a transdermal preparation?

Fentanyl

34

Why is Codeine used as an anti-tussive when all the other opioids have anti-tussive properties too?

1) Less euphoria= less abuse
2) Rarely produces dependence

****Note that it can still produce significant sedation*****

35

How long does it take for Naloxone to take effect?

30 seconds

36

What is the clinical use for Naltrexone?

Maintenance drug for addicts in treatment programs

37

List the strong opioid agonists.

Morphine
Hydromorphone
Oxymorphone
Methadone
Fentanyl
Sufentanil
Meperidine
Heroin

38

List the moderate opioid agonists.

Codeine
Hydrocodone
Oxycodone

39

List the mixed opioid agonist-antagonists.

Bupreneorphine
Butorphanol
Nalbuphine
Pentazocine

40

List the "other" opioid agonists.

Dextromethorphan
Diphenoxylate
Loperamide
Tramadol

41

List the opioid antagonists.

Naloxone
Naltrexone
Nalmefene

Decks in Pharmacology Class (64):