Chelator pharmacology FINAL test Flashcards
How do chelators work on heavy metals?
-Render heavy metal ions unavailable for covalent interactions
How does the half life of the heavy metal affect the ability of a chelator to remove it from a target organ?
-The longer the 1/2 life the less effective is the chelator
Is it better to treat with chelators quickly or take a wait and see approach when exposure has occurred?
-Usually most effective when treated ASAP
What are four chelators?
- Dimercaprol
- Unithiol
- Succimer
- Edetate calcium disodium
Dimercaprol is FDA approved for which heavy metal poisonings as a monotherapy?
- Acute arsenic
- Acute Mercury
Dimercaprol can be administered with edetate calcium disodium to treat chronic poisoning with what heavy metal?
-Severe lead poisoning
Why should dimercaprol no be given as a monotherapy after chronic exposure to lead?
-It pulls Pb from bone and it goes to brain and causes toxicity?
Is dimercaprol water soluble?
-No
What is the only route of administration of dimercaprol?
-IM route only
How does the therapeutic index of dimercaprol compare to succimer or unithiol?
-It can be very toxic, especially on kidneys
T/F Succimer has for the most part eplaced dimercaprol
True
Unithiol is a water soluble derivative of what other chelator?
-Dimercaprol
What are the routes of administration of unithiol?
- Orally
- IV
How does the half life of unithiol’s compare to the other chelators?
-20 hours, which is much longer than other chelators
What heavy metal poisonings is unithiol FDA approved to treat?
-None
What heavy metal poisoning is unithiol effective against?
- Mercury
- Arsenic
- Lead
- it is effective against these, just not FDA approved to treat