S65(2) - Opiate Cessation

Question 1

What is the time of onset for the therapeutic actions of naloxone given nasally?

Answer 1

8-10 minutes…

Question 2

What are hepatic CYP enzyme mainly associated with methadone metabolism?

Answer 2

CYP3A4 and CYP2B6

Question 3

Which opiate receptors does buprenorphine effect?

Answer 3

Partial µ receptor agonist and kappa receptor antagonist

Question 4

Strategies to prevent opioid-related deaths

Answer 4

Pharmacologic
- Antidote: naloxone
- Multimodal pain control
Non-pharmacologic
- Regulatory policies

Question 5

Naloxone pharmacokinetics

Mu opioid receptor antagonist

Answer 5

Onset of action
2 minutes (IV)
8-10 minutes (nasal)
2-5 minutes (IM)

Question 6

Methadone maintenance therapy is the cornerstone for opiate addiction.
Specific methadone clinics established in health systems.

Answer 6

true

Question 7

Methadone – Basic Pharmacokinetics (cont.).

Answer 7

Commercial formulation has racemic R and S isomers.
R methadone binds to the mu opiate receptor.
S methadone binds to the NMDA receptor.

Question 8

Highest concentration in 11 alleles for methadone

Answer 8

true

Question 9

Buprenorphine (BUP) – partial mu opiate receptor agonist and antagonist at the kappa opiate receptor.
Used alone – alternative to methadone for opiate addiction.

Answer 9

true

Question 10

Incorporation of naloxone (NLX) with BUP for a sublingual (SL) preparation (Suboxone®).

Answer 10

true

Question 11

suboxone: FDA approved fixed dose combinations of 4:1 ( 2mg BUP / 0.5 mg NLX; 8 mg BUP / 2 mg NLX).

Answer 11

true

Question 12

Methadone: Metabolism primarily by CYP3A4 and CYP2B6; other reported includes CYP2C9 and CYP2C19.

Answer 12

true