Exam 1 Structures

Question 1

Answer 1

nicotine s enantiomer

effects ganglia and skeletal muscle, metabolized to cotinine and nicotine n-oxide

Question 2

Answer 2

Bethanechol

relieves urinary retention, stimulates GI, systemic

Question 3

Answer 3

carbachol

constricts pupil in glaucoma, alternative to pilocarpine for ocular surgery

Question 4

Answer 4

carbaryl

insecticide, indirect reversible cholinergic

Question 5

Answer 5

cevimeline

direct agoinst; selective M1, M3

-treatment of dry mouth

Question 6

Answer 6

cotinine

-metabolite of nicotine

Question 7

Answer 7

methacholine

• direct agonist
• diagnostic for asthma

Question 8

Answer 8

muscarine

• postganglionic parasympathetic effects
• insensitive to AchE
• no clinical use

Question 9

Answer 9

neostigmine

• methyl on carbamate increases stability
• quaternary ammounium makes polar: does not cross BBB
• topical applicaiton
• myasthenia gravis 150mg/day

Question 10

Answer 10

nicotine n oxide

-metabolite of nicotine

Question 11

Answer 11

nicotine s enantiomer

-effects ganglia and skeletal muscle

Question 12

Answer 12

ach alpha

• nicotinic activity
• no muscarinic activity

Question 13

Answer 13

physostigmine

• reversible indirect agonist
• glaucoma treatment

Question 14

Answer 14

pilocarpine

• direct agonist, muscarinic
• glaucoma, pupil constriction, reduce ciliary muscle spasm

Question 15

Answer 15

propoxur

• reversible indirect agonist
• insecticide

Question 16

Answer 16

tacrine

• reversible agonist, Alzheimers
• Inhibits K1
• Liver toxicity

Question 17

Answer 17

donepezil

• reversible indirect agonist, Alzheimers
• free base crosses BBB
• occupies active site of enzyme
• no hepatoxicity

Question 18

Answer 18

rivastigmine

• reversible indirect agonist, Alzheimers
• cross BBB, carbamate limits regeneration of AchE

BID, 10 hr duration

-diarrhea

Question 19

Answer 19

galantamine

-treats dementia

limits formation of complex w/ enzyme

Question 20

Answer 20

isofluorophate

• irreversible inhibitor
• glaucoma
• discontinued: absroption into the skin and persistant miosis

Question 21

Answer 21

echothiophate

• irreversible inhibitor
• does not cross BBB or skin
• treatment of glaucoma
• discontinued

Question 22

Answer 22

parathion

• irreversible inh ACHE
• insecticide
• humans may convert to paraoxon, banned in US

Question 23

Answer 23

malathion

• irreversible, organophosphate
• replaced parathion as insecticide
• can be eliminated through carboxyesterases
• converted to the very powerful malaoxon

Question 24

Answer 24

pralidoxime

2-PAM

• reverses phosphorylation by an organophosphate
• must be used quickly

Question 25

Answer 25

sarin -nerve gas (phosphonate) no regeneration by 2-PAM

Question 26

Answer 26

soman - nerve gas (phosphonate) - more stable and toxic than sarin - AchE cannot be regenerated by 2-PAM