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About Joshua Cappuccilli
Expertise
I can answer most questions involving medication use, side effects, adverse effects, interactions and how drugs relate to specific disease states. Noone can answer all questions; I will respond as such if I cannot provide an answer. I will provide resources / references for the information that I use to formulate the answer given.

Experience
I am a PharmD with my degree from the University of FLorida - currently I am preparing to take the state boards in Florida.

Organizations
California Phamacist Association American Pharmacy Assocaition

Education/Credentials
BA University of South Florida PharmD University of Florida

 
   

You are here:  Experts > Health/Fitness > Pharmacology > Pharmacology > drugs

Pharmacology - drugs


Expert: Joshua Cappuccilli - 10/24/2007

Question
What steps are involved in sulphadimidine metabolism?

Answer
Sulfadimidine is well absorbed orally, and distributed widely to various tissues and fluids. T½ = 1.5-5 hours. The rate and extent of metabolism in the liver depend on individual acetylator status. Up to 85% is excreted in the urine with variable amounts (15-70%) unchanged.

http://web.uct.ac.za/depts/mmi/jmoodie/j01part6.html

Sulfadimidine is acetylated and hydroxylated in humans. The hydroxylation pathways account for 10-20% of the dose, leaving the acetylation as the major metabolic pathway. The hydroxylation pathways are independent of the acetylator phenotype. The plasma concentration-time curve of sulfadimidine in fast acetylators is biphasic, with half-lives of 1.7 and 5.4 h, whereas that in slow acetylators is monophasic, with a half-life of 7.6 h. Hydroxylation of a methyl group in sulfadimidine lowers the protein binding from 90 to 60%, while acetylation does not affect the protein binding. Methyl hydroxylation markedly increases the renal clearance.

This second quote is absolutely the BEST reference that I was able to find for these three questions.

http://www.ncbi.nlm.nih.gov/sites/entrez?Db=pubmed&Cmd=ShowDetailView&TermToSear...
Ther Drug Monit. 1986;8(4):434-9

Pharmacokinetics, metabolism, and renal excretion of sulfadimidine and its N4-acetyl and hydroxy metabolites in humans.
Vree TB, Hekster YA, Nouws JF, Baakman M.

I could not access a digital copy of this article because it was far too old for the system that I have however, the abstract was very helpfull.

Check this pubmed search for the best articles - note most are old.  
http://www.ncbi.nlm.nih.gov/sites/entrez?Db=pubmed&DbFrom=pubmed&Cmd=Link&LinkNa...

Please also note that the alternate spelling of SULFADIMIDINE instead of SULPHADIMIDINE (as you spelled it) brings a great deal more results - it is in the literature both ways but this spelling seems to be more common.

Hope that helps!  

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