Term
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Definition
- Network of enzymes mostly in the liver (some are located in the GI tract)
- Metabolizes endogenous (ie hormones, steroid, lipids, etc) & exogenous substances (ie medications)
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Term
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Definition
÷Subgroups responsible for the metabolism of many drugs
¢3A4
¢2D6
¢2C9, 10, 19
¢1A2
¢2E1 |
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Term
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Definition
| utilizes the CYP450 system for metabolism |
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Term
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Definition
¡Tricyclic Antidepressants (TCAs)
¡Warfarin (Coumadin®)
¡Theophylline
÷Chemically similar to caffeine
¡Caffeine |
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Term
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Definition
¡Non-Steroidal Anti-inflammatories (NSAIDs)
¡Oral hypoglycemics
¡Warfarin (Coumadin®) |
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Term
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Definition
¡Proton Pump Inhibitors (PPIs)
÷Used for GERD
¡Antiepileptic drugs |
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Term
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Definition
Beta Blockers
Antipsychotics
Antidepressants
÷TCAs
÷Selective Serotonin Reuptake Inhibitors (SSRIs)
Codeine
÷Problem for patients with genetic enzyme problem
÷Must be transformed before it is active; therefore, patient cannot feel relief from codeine |
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Term
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Definition
¡Anesthetics
¡Acetaminophen (Tylenol®)
¡Ethanol |
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Term
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Definition
¡Antibiotics-Macrolides
¡Benzodiazepines (BZDs)
÷Used for anxiety
¡Immunosuppressants
÷Patients could become very ill, if other 3A is being used, therefore, immunosuppressants gro up
÷If given medication that induces 3A, then body will reject organ
¡HIV antivirals
¡Calcium Channel Blockers (CCBs)
¡Statins
¡Hormones (estrogen, progesterone)
Many other miscellaneous |
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Term
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Definition
Some medications have the capacity to increase the activity of CYP 450 enzymes
÷More activity of CYP 450 enzymesàIncreased metabolism àLower plasma concentration |
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Term
Consequences of CPY 450 induction |
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Definition
÷Decreased plasma drug concentrations
÷If inactive metabolite: decreased drug activity (¯therapeutic effects)
÷If the drug has an active metabolite, induction may increase the activity of the medication (but in general it is assumed that induction will decrease the activity)
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Term
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Definition
1A2: foods (broccoli, brussel sprouts, other), tobacco smoke
2C9: Rifampin
2C19: Rifampin, Carbamazepine
2D6: Rifampin
2E1: Ethanol
3A (4,5,7): HIV antivirals, Barbiturates (phenobarbital), Carbamazepine, Phenytoin (Dilantin®), Rifampin
Overall Common CYP 450 Inducers
¡Phenobarbital, Phenytoin, Rifampin, Carbamazepine (Tegretol®) |
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Term
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Definition
Some medications have the capacity to decrease the activity of CYP450 enzymes
÷Less activity of CYP 450àdecreased metabolism àhigher concentration of plasma drug levelsàpossible side effects or toxicity |
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Term
| Common CYP 450 Inhibitors |
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Definition
¡1A2: Fluroquinolones (FQs)
¡2C9: Azole Antifungals
¡2C19: PPIs, Some Antidepressants (SSRIs, TCAs)
¡3A (4,5,7): HIV antivirals, macrolide antibiotics, azole antifungals, grapefruit juice, CCBs
Overall common inhibitors
¡Cimetadine (Tagamet®), Grapefruit juice, Amiodarone |
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