COTRIMOXAZOLE

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Namaste Folks!!
Hope you all doing well.
So, today i am gonna tell you something interesting about a drug which is used in common infections like urinary tract infections, respiratory tract infections, bacterial diarrhoeas and dysentery, Pneumocystis jiroveci, chancroid, etc.


COTRIMOXAAZOLE


The fixed dose combination of trimethoprim and sulfamethoxazole is called cotrimoxazole. Cotrimoxazole introduced in 1969 causes sequential blog of folate metabolism.
Trimethoprim is >50,000 times is more active against bacterial DHFRase than against the mammalian enzyme. Thus, human folate metabolism is not interfered at antibacterial concentrations of trimethoprim.
Individually, both sulfonamide and trimethoprim are bacteriostatic, but the combination becomes cidal against many organisms. 
Sulfamethoxazole was selected for combining with trimethoprim because both have nearly the same half life (~10 hr). Optimal synergy in case of most organism is exhibited at concentration ratio of sulfamethoxazole 20 : trimethoprim 1. The two are given in a dose ratio of 5:1 because trimethopriom enters many tissues and has a larger volume of distribution than sulfamethoxazole and attains lower plasma concentration.
Moreover, trimethoprim is more rapidly absorbed than sulfamethoxazole -concentration ratios may vary with time. Trimethoprim is 40% plasma protein bound, while sulfamethoxazole is 65% bound. Trimethoprim is partly metabolized in liver and excreted in urine.

So, guys this was general overview on COTRIMOXAZOLE still many things are being left to tell in further updates.
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