Potentnost (farmakologija)

Semi-log graf dva agonista sa različitim Kd vrednostima.

U polju farmakologije, potentnost je mera aktivnosti leka izražena u vidu količine supstance neophodne da se proizvede efekat datog intenziteta.[1] Veoma potentni lek (npr., morfin, alprazolam, hlorpromazin) izaziva veliki respons na niskim koncentracijama, dok nisko potentni lek (ibuprofen, acetilsalicilna kiselina) izaziva mali respons na nikim koncentracijama. Potentnost je proporcionalna afinitetu i efikasnosti.[2]

Afinitet je sposobnost leka da se veže za receptor. Efikasnost je odnos između zauzetosti receptora i sposobnosti iniciranja responsa na molekularnom, ćelijskom, tkivnom ili sistemskom nivou. Respons je jednak efektu (E), koji je zavistan od vezivanja leka, kao i sposobnosti receptora sa vezanim lekom da proizvede respons; tako da je potentnost zavisna od afiniteta i efikasnosti. Agonist (ligand, lek ili hormon) koji se veže za receptor i proizvede respons se obično obeležava sa A ili D. Ispod određene koncentracije agonista ([A]), E je suviše nizak da bi se merio, ali na višim koncentracijama on postaje uočljiv i povišava se sa porastom koncentracije agonista [A], dok na dovoljno visokim koncentracijama on se više ne povećava sa porastom [A] (Emax).

Emax je maksimalni mogući efekat agonista. Koncentracija A na kojoj je E vrednost na 50% od Emax se naziva polu-maksimalna efektivna koncentracija i obeležava se sa [A]50, ili EC50. Termin potentnost se odnosi na [A]50 vrednost. Što je niža EC50 vrednost, to je manja koncentracija leka potrebna da bi se proizvelo 50% maksimalnog efekta, i to je veća potentnost.

Reference

  1. ↑ Hardman JG, Limbird LE, Gilman AG. (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10 izd.). New York: McGraw-Hill. DOI:10.1036/0071422803. ISBN 0-07-135469-7. 
  2. ↑ Thomas L. Lemke, David A. Williams, ur. (2007). Foye's Principles of Medicinal Chemistry (6 izd.). Baltimore: Lippincott Willams & Wilkins. ISBN 0-7817-6879-9. 

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