Opioids

Question 1

How has the opioid epidemic progressed?

Answer 1

Rising since 1990s

Heroin and opioid deaths steadily have risen
Heroin in particular has increased in the past few years
Abuse resistant formulations of opioids were created

In response: Needle exchanges, oral methadone clinics, buprenorphine

Question 2

What is the epidemiology of opioids?
How does it present in clinic?
What is the mortality rate and what are the causes of death?

Answer 2

Onset late teens/twenties, male:female = 1.5:1
Genetic predisposition: Impulsivity and novelty-seeking, peer selection
Decreasing prevalence with age
White middle-class female increasing use
Present as depression, sexual problems, cellulitis, poverty
Mortality rate 2%: OD, hepatitis, HIV, endocarditis, suicide

Question 3

What interactions are important for codeine?
For demerol?

Answer 3

Codeine to morphine by CYP2D6
Inhibited by Paxil, Prozac, Quinidine

Demerol toxic with MAOI
Normeperidine causes seizures

Question 4

What is special about demerol’s side effects?

Answer 4

Demerol has atropine symptoms (large pupils)

Question 5

How long does withdrawal last?
How can you treat it?
Is it fatal?

Answer 5

Two to three months
Can be somewhat treated by clonidine
Not fatal but horrible

Question 6

What is special about tolerance for opioids?

Answer 6

Cross tolerance across all opioids

Question 7

How quickly does fentanyl reach the brain?
How quickly does morphine reach the brain?
What is the implication for ODs?

Answer 7

Fentanyl – 15 seconds to brain
Morphine – 10-20 minutes to brain

High OD death rate for lipid solubility
Due to respiratory alkalosis, depression
In lipid soluble drugs this occurs much more quickly, do not respond to the hypoxia quickly enough

Question 8

Buprenorphine

MoA
Pharmacokinetics
Effect on cravings
Termination of use

Answer 8

Partial agonist with a long ceiling

Stays in blood for several days, keeps effect over the course of the entire day

Brain changes tolerance, desire to use opioids disappear

Taking patients off buprenorphine often results in death, counseling is not effective

Question 9

Buprenorphine pain relief considerations

Answer 9

Mild-moderate pain: Continue using buprenorphine, use non-opioid
Moderate-severe: Need to discontinue buprenorphine (partial agonist acts as a partial antagonist) and transition to a true opioid

Question 10

What is suboxone?

Answer 10

Buprenorphine and naloxone (full antagonist) combination

Question 11

Methadone

MoA
Special Dispensing Consideration

Answer 11

Full agonist
Special federal license and affiliated program