Dr. Proteau Nicotinic Ag/Antag

Question 1

what are key characteristics of S-+-nicotine?

Answer 1

lipophilic
readily crosses membranes
accesses CNS

Question 2

structurally, what two groups does succinylcholine have?

Answer 2

two cholines combined into one structure

Question 3

succinylcholine is rapidly hydrolyzed by?

Answer 3

butyrylcholinesterase (aka plasma cholinesterase)

Question 4

nicotinic muscular blockers all have what structural features?

Answer 4

they are symmetrical or dimer-like and have 2 charged Ns

Question 5

cisatracurium besylate is used only as which isomer?

what is the original product?

Answer 5

1R cis-1R cis

atracurium

Question 6

how many isomers are possible for atracurium?

Answer 6

10

Question 7

how does a quaternary ammonium effect duration of action?

Answer 7

increases duration of action of the drug

Question 8

what is the name of the metabolite formed by both pancuronium bromide and vecuronium bromide?

Answer 8

3-desacetyl metabolite`

Question 9

what is the only difference in structure between pancuronium bromide and vecuronium bromide?

Answer 9

pancuronium has two quaternary ammoniums, vecuronium has one quaternary ammonium and one tertiary amine

Question 10

how does Rocuronium bromide differ from pancuronium bromide and vecuronium bromide?

Answer 10

it has no 3-desacetyl group, so it has no active metabolite and will be less potent

Question 11

what’s the name of the big structure that’s circular with several sulfur linkages and sodium atoms?

Answer 11

sugameddex

Question 12

what is sugameddex used for? (drug class)

Answer 12

selective relaxant binding agent (SRBA)
agent for reversal of neuromuscular blockade
-> reverses effects of rocuronium and vecuronium, but not very effective at reversing effects of pancuronium

Question 13

what is the order of affinity towards the “ium” drugs of sugameddex?

Answer 13

rocuronium > vecuronium > pancuronium