PEBC: Theme of the Week: Reversal Agents

Medications can be great when they work the way they intend to. However, sometimes you want to stop its action due to excessive adverse effects or overdose. That is why we have specific antidotes designed for reversing the effects of a medication. How many of these do you recognize?

--------------- Antagonistic Mechanism


1) Vitamin K: reverses warfarin action, which is a blood thinner. This allows for clotting factors to be synthesized again to manage uncontrolled bleeding risk.


2) Acetylcysteine: reverses acetaminophen action, which is a pain/fever reliever. Accetaminophen is detoxified in the liver by glutathione. Acetylcysteine restores glutathione storage sites, allowing for effective neutralization of toxic metabolites from acetaminophen metabolism.


3) Glucagon: reverses insulin action, used for diabetes. If glucose levels go too low into hypoglycemia, glucagon can stimulate glycogen breakdown from liver storages to raise levels.

--------------- Binders


1) Digifab/Digibind: an immune fab fragment which binds to digoxin, a cardiac glycoside for atrial fibrillation or heart failure.


2) Praxbind: an antibody for dabigatran (Pradaxa), a blood thinner.


3) Andexanet alfa: an antibody for factor Xa inhibitors (i.e. blood thinners such as apixaban, rivaroxaban, edoxaban)


4) Protamine: a peptide which binds to heparin, also a blood thinner.

--------------- Blockage of Receptor Site


1) Naloxone: Opioid overdoses are commonly reversed by naloxone which compete at opioid receptors.


2) Flumazenil: reverses benzodiazepines, used for anxiety, by competing at the GABA receptor.





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