Converts a drug into a metabolite (becomes for polar/easier to excrete)
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Why is it important to understand the Phase I reactions a potential therapeutic drug undergoes?
Able to work out the toxicity of metabolites (location of toxicity e.g. liver)
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Which family of enzymes are responsible for the majority of Phase I metabolism?
Cytochrome P450 (CYP)
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Describe features of C-oxidation
Can be either aliphatic c-oxidation or aromatic c-oxidation (aromatic- double bonds in rings). Oxidation results in the addition of an OH group (P450 used)
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Describe features of C-epoxidation
Intermediates. Very reactive (bond angle), C-O-C bond (P450 used)
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Describe features of N and S oxidations
FMO mechanism used. Only tertiary amines produce N oxide. S oxidised to form sulphoxide
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Primary aromatic/aliphatic amines under which type of reaction
N-oxidation (e.g. 2-napthylamine to N-hydroxyl napthylamine). N in rings don't undergo N-oxidation
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Describe C-oxidations and N/S/O dealkylations
OH added to alkyl group. Alkyl group is removed (OH on original compound and form formaldehyde as another product)
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Give examples of reduction reactions
Aromatic nitro group reduction and azo group reduction
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Describe features of hydrolysis
Esterase activity. Using a water molecule to break down a compound e.g. procaine, procainamide - esters are very reactive/toxic (lots of esterase in the body)
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Why are esters toxic?
COO (electronegative oxygens interact, lead to delta + and delta -, prone to nucleophilic attack)
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Other cards in this set
Card 2
Front
Why is it important to understand the Phase I reactions a potential therapeutic drug undergoes?
Back
Able to work out the toxicity of metabolites (location of toxicity e.g. liver)
Card 3
Front
Which family of enzymes are responsible for the majority of Phase I metabolism?
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