Metabolism

Active drug

Active metabolite

amitriptylme

nortriptyline

codeine

inorphine

chloroquine

hyd roxychloroquine

diazepam

oxazepam

spironolactone

can renone

3. Conversion of a pharmacologically inactive to an active substance, i.e. prodrugs; the effect may confer advantage or disadvantage. (The process then follows 1, above.)

/noetic subs ion cc benorilate cholecalcifcrol cyclophosphamide penndopril levodopa sulindac sulfasalazine terfenadine zidovudine

AcliVe meiaboKtefsj Comment salicylic acid and possibly reduced paracetamol gastric toxicity

I -cf-hydroxy-cholecakiferol 4-keto-cyclophosphamtde less risk of first dose hypotension perindoprilat dopamine sulindac sulphide 5-arninosalicylic acid fexofenadine levodapa, but not dopamine, can cross the blood-brain barrier possibly reduced gastric toxicity life-threatening tachycardia if metabolism is inhibited (see p. 555)

zidovudine triphosphate

Most drugs are treated by the body as foreign substances (xenobiotics) and become subject to its various mechanisms for ridding itself of chemical intruders.

Metabolism is a general term for chemical transformations that occur within the body and its processes change drugs in two major ways:

• by reducing lipid solubility

• by altering biological activity.

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