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ORGMEDS: BIOTRANSFORMATION, DRUG METABOLISM - Coggle Diagram
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DRUG METABOLISM
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Xenobiotic
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Goal: to make polar, para di making toxic sa liver or sa katawan, conversion of the drug to a more water soluble compound, active to inactive
Anything that enters our body, anything foreign chemicals
Some are toxic, we rely on detoxification biotransformation
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Sites
Liver
- has a lot of enzymes
- has a lot of supply of blood
Intestinal mucosa
- orally administered drug
-Cyp 3a4 isozyme
-p glycoprotein
- n most not beneficial because of first pass effect
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4 possible effects:
-deactivation (active to inactive)
-activation (some are converted to active metabolite, like prodrugs) e.g.levodopa ( ttx Parkinson’s) upon conversion, converted to L dopa - active neurotransmitter, tataas ulit ang dopamine levels. Active form converted to another active form.
- e.g. Minoxidil (tx HTN) upon metabolism converted to minoxidil sulfate
-Cytotoxicity (upon metabolism some can increase toxicity)
- altered pharmacological activity( either increase or decrease)