MOA, pKa, Vd, onset

Question 1

thiopental

Answer 1

potentiates GABA receptors (agonist)

Question 2

methohexital

Answer 2

potentiate GABA receptors,

Question 3

midazolam

Answer 3

facilitate GABA receptors (do not directly activate), pKa 6.15, Vd increases in elderly and obese, onset 30-60 seconds, peak effect 5min, duration 1.9

Question 4

diazepam

Answer 4

facilitate actions of GABA (ionophores a1, a2, a5). larger Vd in women, crosses placenta. extensively protein bound. >40h half life.

Question 5

lorazepam

Answer 5

slower onset than midazolam/diazepam. max plasma concentration 2-4h after PO admin. onset 1-2min, increased Vd in obese. peak effect 20-30min IV, duration of sedative effect 6-10hours. half life 14 hours (longer in obese)

Question 6

flumazenil

Answer 6

competitive benzodiazepine antagonist. reverses in 2 min.

Question 7

Propofol

Answer 7

selective modulator of GABA (A) receptor. pKa 11. Vd 3.5-4.5L/kg, .5-1.5h half life. metabolism via CYP450. active metabolite 4-hydroxypropofol. clearance 30-60ml/kg/min

Question 8

Etomidate

Answer 8

selective modulator of GABA(A) receptors. pKa 4.3. large Vd 2.2-4.5L/kg. T1/2 2-5h, lasts 8h (corticosteroid effects). metabolized by hydrolysis (phase 1)

Question 9

Ketamine

Answer 9

NMDA antagonist, Vd 2.5-3L/kg, T1/2 2-3h, demethylation by CYP450 micro enzymes (phase 1), metabolism depends on hepatic BF. pKa 7.5.

Question 10

dextromorphan

Answer 10

low affinity NMDA antagonist

Question 11

dexmedetomidine

Answer 11

alpha 2 adrenergic agonist, 2-3h half life

Question 12

scolpalamine

Answer 12

decreases activity of reticular activating system, anticholinergic

Question 13

morphine

Answer 13

pKa 7.9, onset 15-30min, only small amount of morphine reaches CNS.

Question 14

codeine

Answer 14

half life 3-3.5h

Question 15

meperidine

Answer 15

selective kappa and mu receptor agonist, crosses placenta, 2-4h half life

Question 16

fentanyl

Answer 16

blocks sympathetic stimulation to surgical response, analgesia. pKa 8.4. large Vd, >80% leaves plasma in <5min. context sensitive half time increases with infusion >2h, longer t1/2 than morphine

Question 17

sufentanil

Answer 17

extensive protein binding compared to fentanyl. rapid distribution terminates effect

Question 18

alfentanil

Answer 18

small Vd, 90% of drug exists in nonionized form at physiologic pH

Question 19

remifentanil

Answer 19

selective Mu agonist. VERY small Vd .05L/kg. context sensitive half time 4min

Question 20

methadone

Answer 20

long but unpredictable half life (12h)

Question 21

tramadol

Answer 21

weak/moderate Mu agonist

Question 22

butorphanol

Answer 22

agonist antagonist opioid. low affinity for mu receptors, moderate affinity for kappa receptors. half life 2.5-3 hours.

Question 23

nalbuphine

Answer 23

agonist antagonist. Mu antagonist, 3-6 hour half life.

Question 24

naloxone

Answer 24

pure Mu antagonist. half life 30-45minutes.

Question 25

nalmefene

Answer 25

pure opioid antagonist

Question 26

methylnaltrexone

Answer 26

quaternary opioid receptor agonist

Question 27

aspirin

Answer 27

NSAID, smaller Vd

Question 28

acetaminophen

Answer 28

NMDA antagonist

Question 29

gabapentin

Answer 29

acts on VgCa channels inhibiting glutamate

Question 30

toradol

Answer 30

nonselective

Question 31

celebrex

Answer 31

only COX 2, small Vd

Question 32

lidocaine

Answer 32

uncertain MOA, may involve Na channels or block priming of polymorphonuclear granuloctyles

Question 33

magnesium sulfate

Answer 33

NMDA antagonism in CNS, regulation of calcium influx into cells

Question 34

capsaicin

Answer 34

TRPV1 (transient receptor potential vanilloid) channel agonist, activation releases high intensity impulses and substance P

Question 35

succinylcholine

Answer 35

depolarizing, onset 60 seconds, recovery to 90% muscle strength 9-13min

Question 36

steroidal NMB’s

Answer 36

pancuronium, vecuronium, rocuronium

Question 37

benzylisoquinolinium NMB’s

Answer 37

atiacurium, cisatricurium, mivacurium

Question 38

pancuronium

Answer 38

onset time to maximum block 2.9min

Question 39

vecuronium

Answer 39

onset time to max block 2.4min

Question 40

rocuronium

Answer 40

onset time to max block 1.7min

Question 41

AchE inhibitors

Answer 41

neostigmine, edrophonium, pyridostigmine

Question 42

sugammadex

Answer 42

attach in plasma to circulating NMB, encapsulates it so it cannot work.