Opioids/Narcotics Flashcards Preview

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Flashcards in Opioids/Narcotics Deck (20):
1

What mu agonists have the best oral bioavailability?

Methadone and Levophanol

2

What mu agonists are much more potent then morphine?

Hydromorphone, Oxymorphone, Levorphanol (all -orph)

3

What mu agonist has a low potency?

Meperidine

4

What is the inactive metabolite of morphine? What forms it?

Nomorphine
Formed by CYP3A4

5

What are the active metabolites of morphine? What forms them?

UGT 1A1/2B7 form M-3 and M-6-glucuronide
Dehydrogenase converts morphine-> hydromorphone

6

How does the half life and oral bioavailability of Methadone different from Morphine? This makes it useful for what?

Methadone- longer half life (27hrs vs 2 for morphine)
Better oral bioavailability (90% vs 20% for morphine)
Useful for withdrawal/maintenance and Detox

7

What is the Methadone MOA?

Independent of Opioid receptors
Direct effect on IRK channels

8

What distinguishes Meperidine from the other mu agonists?

Causes mydriasis instead of miosis
Has toxic metabolite normeperidine-> seizures

9

What is the shortest acting High Potency Full mu Agonist, often used in childbirth?

Remifentanil

10

What mu agonist acts on kappa, delta, and mu receptors?

Sufentanil

11

Suffix for high potency full mu receptor agonists?

-entanil (anyl)

12

What anti-tussive agent receives cough independently of opioid receptors?

Dextromethophan

13

What kind of agonists are codeine, hydrocodone, and oxycodone? How does it dictate strength of response?

Codeine/Hydrocodone= partial agonists
Oxycodone= full agonists-> higher efficacy

14

What breaks down codeine to morphine?

CYP2D6

15

What gene duplication will an ultrafast codeine metabolizer have?

CYP2D6 gene duplicaiton-> more morphine then expected

16

What OTC opioids are used as antidiarrheals?

Loperamide and Diphenoxylate

17

What opioid acts as both a moderate mu agonist and inhibits catecholamine repute?

Tramadol

18

What does a partial mu agonist do when taken with morphine? Clinical use?

Displaces morphine-> causes withdraw
Used for office-based detox/maintenance
Classic example-> Buprenorphine

19

What is the MOA for mu receptor antagonists? What are they called?

Occupy/competitively inhibit other mu agonists from receptors
Antidote for opioid overdose
Naloxone IV and Naltrexone po

20

What drug can be used as a peripheral acting opioid antagonist to decrease opioid-induced constipation?

Methylnaltrexone