atypical opioids and triptans Flashcards Preview

MOHD IV > atypical opioids and triptans > Flashcards

Flashcards in atypical opioids and triptans Deck (16):
1

buprenophine

partial agonist
MOR high affinity, partial efficacy
KOR antagonist
ceiling effect of analgesia and respiratory depression
long 1/2 life
tx with naloxone to treat addiction
may precipitate withdrawal symptoms with full agonists

2

pentazocine, nalbuphine

agonist-antagonists
MOR high affinity but poor MOR agonist
KOR agonist
ceiling effect for analgesia
may precipitate withdrawal
may be used to offset pruritis in opioid tx
nalbuphrine used in labor due to no resp depression
pentazocine-> dysphoria

3

naloxone

antagonist
MOR high affinity but no efficacy
no oral absorption, GI lumen to tx constipation
IV or IM effects both CNS and PNS
short 1/2 life
pared with burenorphine for addiction

4

natrexone

antagonist
MOR high affinity, no efficacy
well absorbed with longer 1/2 life
added to opioids to discourage addiction

5

methylnalfrexone

PAMORA
subQ
quarery structure so no BBB crossing

6

alvimopan

PAMORA
oral
high affinity for peripheral MOR
associated with MI

7

naloxegel

PAMORA
pegylated naloxone

8

triptan AE and drug interactions

AE
-serotonin syndrome
-chest px
-dizziness or vertigo
-tingling
-nausea
-dizziness/lightheaded
-increased BP
Drug interaction
-antidepressants (except buproprion)
-opioids
-anipsychosis
-ergoalkoloids
-CYP3A4

9

sumatriptan

1/2L 1-2 hours
onset
SubQ-15 min
oral- 30 min
IN- 15 min

10

zolmitriptan

1/2L 2-3 hrs
onset
oral- 1-3 hours
IN-10-15 minutes

11

naratriptan

1/2L 5.5 hours
onset oral 1-3 hours

12

Rizatriptan

1/2L 2 hours
onset oral 30-60 minutes

13

Eletriptan

1/2L 4-5 hours
onset oral 30-60 minutes
18 hour duration somehow

14

almotriptan

1/2L 3-4 hours
onset oral 30 min to 2 hours

15

froratriptan

1/2L 25 hours
onset oral 2 hours

16

tramadol

atypical opioid
decreases re-uptake of serotonin and NE
partial agonist
prodrug
CYP2D6 and CYP3A4