atypical opioids and triptans

Question 1

buprenophine

Answer 1

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

Question 2

pentazocine, nalbuphine

Answer 2

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

Question 3

naloxone

Answer 3

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

Question 4

natrexone

Answer 4

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

Question 5

methylnalfrexone

Answer 5

PAMORA
subQ
quarery structure so no BBB crossing

Question 6

alvimopan

Answer 6

PAMORA
oral
high affinity for peripheral MOR
associated with MI

Question 7

naloxegel

Answer 7

PAMORA

pegylated naloxone

Question 8

triptan AE and drug interactions

Answer 8

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

Question 9

sumatriptan

Answer 9

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

Question 10

zolmitriptan

Answer 10

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

Question 11

naratriptan

Answer 11

1/2L 5.5 hours

onset oral 1-3 hours

Question 12

Rizatriptan

Answer 12

1/2L 2 hours

onset oral 30-60 minutes

Question 13

Eletriptan

Answer 13

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

Question 14

almotriptan

Answer 14

1/2L 3-4 hours

onset oral 30 min to 2 hours

Question 15

froratriptan

Answer 15

1/2L 25 hours

onset oral 2 hours

Question 16

tramadol

Answer 16

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