Drug Metabolism Flashcards
(12 cards)
Herceptin (trastuzumab)
treatment of breast cancer with HER2 overexpression
Gleevec (imatinib)
treatment of Philadelphia chromosome + CML
Erbitux (cetuximab)
treatment of EGFR-expressing metastatic colorectal cancer
p-glycoprotein
drug efflux transporter found in intestine, liver, kidney, BBBdrives drug back into lumenlimit absorption to limit plasma concentrationinhibited (increase amt of drug) or induced (decrease amt of drug) by certain drugs
Types of P450 Reactions (Phase 1)
Aliphatic HydroxylationAromatic HydroxylationEpoxidationN-dealkylationO-dealkylation** (codeine to morphine)N-oxidationS-OxidationDehalogenationMicrosomal ethanol-oxidizing system
CYP2D6
O-dealkylationcodeine to morphine* different people metabolize this at different rates, can have fatal side effects (hyper/hypometabolism)NOT induciblePMs of CYP2D6 = Thioridazine contraindicated for use as antipsychotic
Oxidation Phase 1 Reactions
Alcohol DehydrationAldehyde DehydrationPurine OxidationMAO Oxidation
Phase 2 Reactions (Conjugations)
GlucuronidationAcetylationGlutathione ConjugationSulfationMethylation** happens in cytosol, except UDP-glucuronyl transferase
Tizanidine-Fluvoxamine Interaction
Fluvoxamine = CYP1A2 inhibitor, increases amt of Tizanidine
Tizanidine-Fluvoxamine Interaction
Fluvoxamine = CYP1A2 inhibitor, increases amt of Tizanidine
St. John’s Wort-Indinavir Interaction
St. John’s Wort = CYP3A inducer, decreases amt of Indinavir
St. John’s Wort-Indinavir Interaction
St. John’s Wort = CYP3A inducer, decreases amt of Indinavir
