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Codrug
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<h2 id="elements-of-codrug-design">Elements of codrug design</h2> <p>An effective codrug should be pharmacologically inactive in its own right but should release the constituent drugs upon biochemical breakage of the chemical linkage at the target tissue where their therapeutic effects are needed. As such, the chemical linkage (usually a <a href="/facts/Covalent_bond/EzMLf3Pz">covalent bond</a>) should be subjectable to biodegradation, such as hydrolysis, by an enzymatic or non-enzymatic mechanism. The differential distribution of enzymes capable of catalyzing the breakage of the chemical linkage in different tissues may be exploited to achieve tissue-specific metabolism of the codrug to release the constituent drugs. </p> <h2 id="common-codrugs">Common codrugs</h2> <ul><li><a href="/facts/Sulfasalazine/Dzw9KpKJ">Sulfasalazine</a>: <a href="/facts/Sulfapyridine/LPj4It5m">Sulfapyridine</a> linked via an azo group to <a href="/facts/5-aminosalicylic_acid/p9svfBpg">5-aminosalicylic acid</a>.</li> <li><a href="/facts/Alpha-GPC/8p3dHl28">Alpha-GPC</a>: <a href="/facts/Choline/wf9EVzfx">Choline</a> linked to <a href="/facts/Glycerophosphate/3upX66wU">glycerophosphate</a>.</li> <li><a href="/facts/Benorylate/ljS0jkg7">Benorylate</a>: <a href="/facts/Paracetamol/SNDfQWcf">Paracetamol</a> linked via <a href="/facts/Ester/FoUAIIw4">esterification</a> to <a href="/facts/Acetylsalicylic_acid/opMK4qLk">acetylsalicylic acid</a>.</li> <li><a href="/facts/Cod-THC/fVYLat3t">Cod-THC</a>: <a href="/facts/THC/ljryfDfg">THC</a> linked via a <a href="/facts/Carbonate_ester/4L0jLRBo">carbonate</a> group to <a href="/facts/Codeine/lr7WHXmX">codeine</a>.</li> <li><a href="/facts/Fenethylline/0LbNzb8c">Fenethylline</a>: <a href="/facts/Amphetamine/yKIpLJ9E">Amphetamine</a> linked to <a href="/facts/Theophylline/qJzjQVB2">theophylline</a>.</li> <li><a href="/facts/Sultamicillin/j9a0NKKx">Sultamicillin</a>: <a href="/facts/Ampicillin/oIodNyBw">ampicillin</a> linked via esterification to <a href="/facts/Sulbactam/PrUQYFBa">sulbactam</a>.</li> <li>Cefilavancin: a <a href="/facts/Vancomycin/enHvz4uP">vancomycin</a> derived antibiotic linked to a <a href="/facts/Cephalosporin/WeB7I75T">cephalosporin</a> antibiotic.</li> <li>Rifaquizinone: a <a href="/facts/Rifamycin/PB079hum">rifamycin</a> derived antibiotic linked to a <a href="/facts/Quinolone_antibiotic/1jRTHzYW">quinolone antibiotic</a>.</li></ul> <h2 id="see-also">See also</h2> <ul><li><a href="/facts/Combination_drug/pVS5UD72">Combination drug</a></li> <li><a href="/facts/Small_molecule_drug_conjugate/Lkc2PRKa">Small molecule drug conjugate</a></li> <li><a href="/facts/Synergy/lfcwWuAc">Drug synergy</a></li> <li><a href="/facts/Ampicillin/sulbactam/6lWkY2Ao">Ampicillin/sulbactam</a></li></ul> <h2 id="references">References</h2> <ol> <li id="fn:1"><p>Lau WM, White AW, Gallagher SJ, Donaldson M, McNaughton G, Heard CM (2008). "Scope and limitations of the co-drug approach to topical drug delivery". Current Pharmaceutical Design. 14 (8): 794–802. doi:10.2174/138161208784007653. PMID 18393881. <a href="/wiki/Doi_(identifier)" target="_blank">/wiki/Doi_(identifier)</a> <a href="#fnref:1" class="footnote-back-ref">↩</a></p></li> <li id="fn:2"><p>Das N, Dhanawat M, Dash B, Nagarwal RC, Shrivastava SK (December 2010). "Codrug: an efficient approach for drug optimization". European Journal of Pharmaceutical Sciences. 41 (5): 571–588. doi:10.1016/j.ejps.2010.09.014. PMID 20888411. <a href="/wiki/Doi_(identifier)" target="_blank">/wiki/Doi_(identifier)</a> <a href="#fnref:2" class="footnote-back-ref">↩</a></p></li> <li id="fn:3"><p>Lau WM, White AW, Gallagher SJ, Donaldson M, McNaughton G, Heard CM (2008). "Scope and limitations of the co-drug approach to topical drug delivery". Current Pharmaceutical Design. 14 (8): 794–802. doi:10.2174/138161208784007653. PMID 18393881. <a href="/wiki/Doi_(identifier)" target="_blank">/wiki/Doi_(identifier)</a> <a href="#fnref:3" class="footnote-back-ref">↩</a></p></li> <li id="fn:4"><p>Das N, Dhanawat M, Dash B, Nagarwal RC, Shrivastava SK (December 2010). "Codrug: an efficient approach for drug optimization". European Journal of Pharmaceutical Sciences. 41 (5): 571–588. doi:10.1016/j.ejps.2010.09.014. PMID 20888411. <a href="/wiki/Doi_(identifier)" target="_blank">/wiki/Doi_(identifier)</a> <a href="#fnref:4" class="footnote-back-ref">↩</a></p></li> </ol>