Drug List 3: Moa [Pharmacology I]

Front 1

Mechanism of Action for Edrophonium (ed’ roe foe’’ nee um)

Back 1

Edrophonium non-covalently inhibits AChE by reversibly binding to the choline subsite of the active center.

Front 2

Mechanism of Action for Neostigmine (nee oh stig’ meen)

Back 2

Neostigmine, like Pyridostigmine, is a quaternary amine sporting a carbamoyl ester linkage that serves as a substrate for AChE. It reacts to produce a dimethylcarbamoyl moiety, which reversibly sequesters the enzyme in a more stable form, precluding it from hydrolyzing ACh.

Front 3

Mechanism of Action for Pyridostigmine (peer id oh stig’ meen)

Back 3

Pyridostigmine, like Neostigmine, is a quaternary amine sporting a carbamoyl ester linkage that serves as a substrate for AChE. It too reacts to produce a dimethylcarbamoyl moiety, which reversibly sequesters the enzyme in a more stable form, precluding it from hydrolyzing ACh.

Front 4

Mechanism of Action for Ambenonium (am be noe’ nee um)

Back 4

Ambenonium is a reversible inhibitor of AChE.

Front 5

Mechanism of Action for Physostigmine (fye zoe stig’ meen)

Back 5

Physostigmine is a tertiary amine sporting a carbamoyl ester linkage that serves as a substrate for AChE. It reacts to produce a methylcarbamoyl moiety, which reversibly sequesters the enzyme in a more stable form, thus precluding it from hydrolyzing ACh.

Front 6

Mechanism of Action for organophosphates, such as diisopropyl fluorophosphate (DFP)

Back 6

Organophosphates like DFP inhibit AChE in a relatively irreversible manner by phosphorylating the active center serine to form an extremely stable conjugate.

Front 7

Mechanism of Action for Tacrine (tak’ reen)

Back 7

Inhibits AChE by reversibly binding to the active center. It does so with a higher affinity than does edrophonium and, having primary structure rather than a quaternary one, it is more lipophilic and more readily crosses the BBB.

Front 8

Mechanism of Action for Donepezil (doe nep’ e zil)

Back 8

Inhibits AChE by reversibly binding to the active center. It does so with a higher affinity than does edrophonium and, being a tertiary structure rather than a quaternary one, it is more lipophilic and more readily crosses the BBB.

Front 9

Mechanism of Action for Rivastigmine (ri va stig’ meen)

Back 9

Rivastigmine is a tertiary amine sporting a carbamoyl ester linkage that serves as a substrate for AChE. It reacts to produce an alkylcarbamoyl moiety, reversibly sequestering the enzyme in a more stable form, precluding it from hydrolyzing ACh. It also inhibits butylcholinesterase.

Front 10

Mechanism of Action for Galantamine (ga lan’ ta meen)

Back 10

Galantamine is a reversible inhibitor of cholinesterase activity and it also has nicotinic receptor agonist properties.

Front 11

Mechanism of Action for Echothiophate (eck oh thigh’ oh fate)

Back 11

Echothiophate is a long-lasting cholinesterase inhibitor, the only quaternary ammonium organophosphorus compound used clinically.

Front 12

Mechanism of Action for Demecarium (deh meh kare’ ee um)

Back 12

Demecarium is essentially two neostigmine entities connected by ten methylene spacers. It contains carbamoyl ester linkages that serve as substrates for AChE and, upon reacting with it, reversibly sequesters the enzyme, precluding it from hydrolysizing ACh.

Front 13

Mechanism of Action for Pralidoxime (2-PAM) (pral’ i dox’’ eem)

Back 13

Reactivates the phosphorylated esteratic site of AChE, but only if the phosphorylated enzyme has not “aged” to the point of irreversible inhibition.