Drugs for Alzheimer's

Question 1

Describe the molecular action of donepezil. What kind of Alzheimer’s is it used to treat?

Answer 1

Inhibits AChE; treats mild, moderate, and severe Alzheimer’s

Question 2

Describe the molecular action of galantamine. What kind of Alzheimer’s is it used to treat?

Answer 2

Inhibits AChE; treats mild to moderate Alzheimer’s

Question 3

Describe the molecular action of rivastigmine. What kind of Alzheimer’s is it used to treat?

Answer 3

Inhibits AChE and BuChE; treats mild to moderate Alzheimer’s

Question 4

Describe the molecular action of tacrine. What kind of Alzheimer’s is it used to treat?

Answer 4

Inhibits AChE and BuChE; previously used for mild to moderate Alzheimer’s, but is now used very rarely

Question 5

Describe the molecular action of memantine. What kind of Alzheimer’s is it used to treat?

Answer 5

NMDA receptor antagonist; treats mild, moderate, and severe Alzheimer’s

Question 6

Besides treating Alzheimer’s, donepezil and rivastigmine could also be used to treat what 3 CNS diseases?

Answer 6

Parkinson’s, dementia with Lewy bodies, and vascular dementia

Question 7

Besides treating Alzheimer’s, galantamine and memantine could also be used to treat what CNS disease?

Answer 7

Vascular dementia

Question 8

Describe the metabolism and excretion of donepezil.

Answer 8

Metabolized by P450, excreted in urine

Question 9

Describe the metabolism and excretion of galantamine.

Answer 9

Metabolized by P450, excreted in urine

Question 10

Describe the metabolism and excretion of rivastigmine.

Answer 10

Hydrolyzed by cholinesterases, excreted in urine

Question 11

Describe the metabolism and excretion of memantine.

Answer 11

Not metabolized, excreted unchanged in urine

Question 12

Give 2 reasons why tacrine is now rarely used to treat Alzheimer’s.

Answer 12

Hepatotoxicity and has to be taken 4x/day

Question 13

Which Alzheimer’s drug can be given as a transdermal patch? List 2 advantages of the patch compared to a pill.

Answer 13

Rivastigmine; better compliance and fewer side effects (ex. nausea, vomiting, diarrhea)