Opioids & Antagonists

Question 0

Hydromorphone

Answer 0

Strong opioid - more potent (not stronger) than morphone

moderate-severe pain, met don’t accumulate (ok in renal dysf), less histamine release

Question 1

Morphine

Answer 1

Strong opioid - Severe pain- 10mg SC or IM (standard dose)
high first pass (better IV), short t1/2-fast onset
CYP2D6 (fluoxetine/paroxetine interactions)
metabolites:M6G potent , M3G adverse effects
itching, vomiting, crosses placenta

Question 2

Heroin

Answer 2

Strong opioid - Schedule 1

Question 3

Methadone

Answer 3

Strong opioid- long term/hard to tx pain, maintenance tx of addicts
Long action, little euphoria, long withdrawal
blocks Ne/5HT reuptake- serotonin synd w/ MAOIs

Question 4

Meperidine

Answer 4

Strong opioid - used post-op to reduce shivering
Anticholinergic - tachy, mydriasis
Euphoria, no cough supp, less: N/V/C,resp depression (obstetrics), urinary ret (BPH)
Met: normeperidine - causes seizures
DI: Serotonin syn w/ MAOIs (blocks reuptake of 5HT/NE as well)

Question 5

Fentanyl

Answer 5

Strong opioid - very potent, very lipid soluble
Short duration, anesthesia for short sx procedures (+midazolam)
High abuse, truncal rigidity (rapidly IV)
CYP3A4 met, transdermal (slow long control needed), lollipops

Question 6

Alfentanil
Sulfentanyl
Remifantanyl

Answer 6

Strong opioid- very lipid soluble similar to Fentanyl

Shorter action-T1/2

Question 7

Hydrocodone

Answer 7

Strong-moderate opioid, moderate/severe pain
CYP2D6 met (int w/ SSRIs-fluoxetine, paroxetine)
Schedule II (or III if +acetaminophen=vicodin), abuse potential

Question 8

Oxycodone

Answer 8

Strong-moderate opioid
For: moderate/severe pain, Tourette’s, restless leg
Met by CYP2D6 to oxymorphone (can use w/ SSRIs)
+acetaminophen (Percocet) +aspirin (Percodan)

Question 9

Oxymorphone

Answer 9

Strong-moderate opioid

Active metabolite of Oxycodone after CYP2D6 met: can use w/ SSRIs

Question 10

Oxycontin

Answer 10

Extended release form of oxycodone

Question 11

Codeine

Answer 11

Moderate opioid- mild/moderate pain, Antitussive (low dose)
CYP2D6 met to morphine, some abuse, not for children, oral.
Sch II alone, III +aspirin or acetaminophen, V cough suppressant

Question 12

Buprenorphine

Answer 12

Mixed opioid - Partial agonist on mu
less euphoria (ceiling), low abuse
used to tx opioid addicts- dec cravings
If combined w/ naloxone sublingual, not IV.

Question 13

Pentazocine

Answer 13

Mixed opioid - Kappa agonist, Mu partial agonist - moderate pain tx
less sedation, resp depression and GI
Dysphoria (k), withdrawal in pt dependent, low abuse- Sch IV

Question 14

Naloxone

Answer 14

Opioid antagonist - DOC for opioid OD

Short duration- repeat dose, IV (give til pupils dilate)

Question 15

Nalmefene

Answer 15

Opioid antagonist

similar to naltrexone, longer duration of action and less liver toxicity

Question 16

Naltrexone

Answer 16

Opioid antagonist
Long duration, oral
Hepatotoxicity, will precipitate withdrawal in opiod addicts

Question 17

Dextromethorphan

Answer 17

Opioid- antitussive, no analgesia
blocks NMDA (abuse) dec 5HT reuptake (serotonin syn w/ MAOIs)
abuse/death in adolescents

Question 18

Diphenoxylate + atropine

Answer 18

Anti-diarrheal - Lomotil

Opioid that doesn’t cross BBB

Question 19

Loperamide

Answer 19

Antidiarrheal - Imodium

Opioid that doesn’t cross BBB

Question 20

Tramadol

Answer 20

Moderate opioid- mild/moderate pain
Weak mu agonist, blocks NE/5HT reuptake
DI: +antidepressants=seizures, serotonin syn +MAOIs, TCAs, SSRIs
Low abuse, Sch IV