Quantification of drug action

FDA) for use in humans to treat malaria because this drug is considered a safe drug with few side effects.These features prompted various scientists around the world to evaluate the potential of artemisinin (1) and derivatives to control cancer cells proliferation. This chapter reviews the recent advances on analytical methods for extraction and quantification of artemisinin (1) from A. annua. Examples of artemisinin-derivatives with antiproliferative activities are listed, describing the structure-activity relationships of 96 compounds. This knowledge is essential for future development and use of artemisinin derivatives in cancer therapy. The mechanism of action of artemisinin and derivatives on cancer cells have been well reviewed in literature and therefore is not discussed in this chapter. 

PK/PD models are obtained by combining a PK model (Section 13.2.4) and a PD model (Section 13.2.5), allowing the quantification of the relationship between drug administration and drug action. The principles of PK/PD modelling will be dealt with briefly. For a more detailed treatise, some excellent reviews can be found in the literature [21]. 

No less revolutionary in the quantification of pharmacodynamics was the insistance on size relationships which Alfred Joseph Clark (London) introduced in his book, The Mode of Action of Drugs on Cells (Clark, 1933). The mnemonic diagram that forms the frontispiece of the present book will serve to introduce this aspect. In it we see a typical mammal (dog) followed by a typical insect (flea) which is a thousand times smaller, and this is followed by a typical microbe (streptococcus) which is yet a thousand times smaller, and finally a typical bioactive molecule (p-aminobenzoic acid) which is one thousand times smaller still. Thus we have familiar reference objects staked out over a size-range of 10 (a million-millionfold). 

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