A Prodrug is sorta like a trojan horse with a good purpose – a compound that our body absorbs and then metabolizes (in the liver for example) into it’s active drug form within the body. Some of these are created of purpose for better absorption, needing lower doses and lesser side effects. Here are some common drugs used in medical practice – can you guess which of these are prodrugs ? It can be useful to know how they are metabolized into the active form since dose or med adjustments maybe needed in some diseased states.
Results
#1. Codeine
Codeine converts to Morphine and Norcodon and to a small extent – hydrocodone, in the Liver. Effects of codeine are largely due to these metabolites. Not recommended in Cirrhotics / Liver Failure
#2. Prednisone
Prednisone is converted into Prednisolone in the Liver , which is the active melabolite.
So in cirrhotics, rather use Prednisolone !
#3. Ibuprofen
Confused you didn’t I 😉
Ibuprofen is a active drug by itself …
#4. Clopidogrel (Plavix)
Cytochrome system in the Liver converts Plavix to it’s active metabolite. Plavix may not be effective in slow cytochrome metabolizers (gene testing is available for this)
#5. Tamiflu (Oseltamivir)
Oseltamivir is hydrolyzed in our body hepatic esterases and converted to the active metabolite oseltamivir carboxylate.
#6. Lisinopril
Not a prodrug, lisinopril is an active compound by itself
#7. Enalapril
Unlike Lisinopril, body converts Enalapril to active compound Enalaprilat in the liver and intestinal wall
#8. Simvastatin
Simvastatin is converted in the body to an active beta-hydroxy acid form that exerts action on HMG-CoA reductase
#9. Rosuvastatin (Crestor)
Simvastatin and Lovastatin are the only prodrugs amongst commonly used statins
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