Term
| Drug Metabolism 3 Families |
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Definition
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Term
| # of Cytochrome P450 Families |
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Definition
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Term
# of CYP's that are mitochondrial
Function? |
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Definition
7
Steroid hormone synthesis |
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Term
CYP2E1 Action
Name of system
Location
Oxidizing Agent |
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Definition
Oxidizes Ethanol to acetaldehyde
Microsomal Ethanol Oxidizing System
ER
NADPH |
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Term
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Definition
| Hydroxylation of drug using NADPH and Oxygen |
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Term
| Main drug metabolism organ |
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Definition
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Term
|
Definition
CYP2A1 metabolizes it to compound producing liver cancer
Wet grain and peanuts |
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Term
Vinyl Chloride
Effect of product |
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Definition
CYP2E1 Oxidizes Vinyl Chloride to an epoxide
DNA damage |
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Term
Benzypyrene
Effect of product
Location (2) |
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Definition
Metabolized by Cytp450's into an epoxide.
Reacts with guanines, disrupts GC base pairs and leads to cancer
Cigarette Smoke and Charcoal-Broiled meats |
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Term
| Risk of lung cancer from smoking |
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Definition
| Increases with inducing CYP2A6 |
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Term
|
Definition
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Term
Alcoholic CYP2E1 problems
Result |
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Definition
Increased ability to metabolize certain drugs due to chronic increased levels of CYP2E1
Need higher dose of drug |
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Term
Alcoholic CYP2E1 and Drug Simultaneous
Result |
|
Definition
Competition occurs for the enzyme
Drug will be more effective at lower dose. |
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Term
|
Definition
Very broad
Easy for two drugs to compete |
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Term
CYP3A4 inhibition (2)
Result |
|
Definition
Grapefruit juice
CYP3A4 inhibited by many drugs
Taking a drug that is an inhibitor with one that is metabolized by CYP3A4 can be very severe. |
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Term
St. John's Wort
Result (3) |
|
Definition
Induces CYP3A and CYP1A2
Accelerated metabolism of 1. theophylline for asthma
2. Warfarin for blodo clotting
3. oral contraceptives |
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Term
Multi-Drug Transporter
Result of long term activation |
|
Definition
Removes drugs from cells by active transport and is induced with CYP3A4
Acquired resistance to certain drugs |
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Term
|
Definition
CYP3A4 metabolizes this
Blood levels down
Decreased efficacy |
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Term
|
Definition
CYP3A4 metabolizes this
Increased or decreased when administered
Increased metabolism due to CYP3A4 induction
Decreased metabolism due to CYP1A2 inhibition |
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Term
Oral Contraceptives
Result? (2) |
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Definition
CYP3A4 metabolizes this
Reduce blood levels decreased
Efficacy decreased |
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Term
CYP2D6
Special Feature
Deficiency
Special Title |
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Definition
Converts codeine to morphine
Is NOT inducible
7% of Whites and Blacks are missing this and can't get codeine to work
Metabolize 25% of drugs currently marketed |
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Term
|
Definition
CYP1A2 Metabolizes Caffeine
Neonates lack this |
|
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Term
|
Definition
CYP2C9, CYP3A4, CYP1A2 metabolize this
Deficiency in CYP2C9 results in someone being unable to coagulate on very small warfarin doses |
|
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Term
|
Definition
| Used in determining a person's sensitivity to Warfarin's action |
|
|
Term
# of polymorphic CYP's
Result |
|
Definition
20 CYP genes
40% of CYP action by polymorphic enzymes |
|
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Term
|
Definition
Poor metabolizers
Intermediate metabolizer
Extensive (normal) metabolizer
Ultra-rapid metabolizer |
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Term
|
Definition
| Normal dosage of a drug results in elevated drug levels and severe side effects |
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Term
|
Definition
| Requires higher than normal drug levels for therapeutic effect |
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Term
|
Definition
| Analyzes DNA for isoforms of CYP2D6 and CYP2C19 |
|
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Term
|
Definition
1. PCR amplification
2. Fragmentation through RE's
3. DNA hybridization
4. Staining on microarray chip
5. Scan results |
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Term
| CYP2E1 Painkiller function |
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Definition
| Metabolizes Tylenol to a toxic product |
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Term
|
Definition
1. Glucuronidation
2. Sulfation
3. Glycine Conjugation
4. Glutamine Conjugation
5. Mercapturic acid formation |
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Term
|
Definition
Oxidized Drug is reacted with UDP Glururonic Acid
Produces Drug-Glucuronic Acid conjugate |
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Term
|
Definition
| Oxidized drug + PAPS yields Drug-Sulfate Ester |
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Term
|
Definition
| Carboxylated drug + Glycine yields Drug-Glycine conjugate |
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Term
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Definition
| Carboxylated drug + Glutamine yields Drug-Mercaptic Acid |
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Term
|
Definition
| Drug-X Plus Glutahione-SH yields Drug-Mercaptic Acid conjugate |
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Term
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Definition
| Excreted as Glycine Conjugates |
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Term
| Acetaminophen Normal Metabolism? (2) |
|
Definition
Excreted after glucuronidation
Sulfation |
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Term
| Acetaminophen Metabolism with Alcohol (4) |
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Definition
Ethanol induces CYP2E1
CYP2E1 converts acetaminophen to NAPQI
NAPQI accumulates due to depleted Glutathione
NAPQI leads to liver failure |
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Term
|
Definition
| Glutathione reactions dispose of it |
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Term
| Most CYP characteristics (4) |
|
Definition
Inducible
Broad specificity
Phase I reactions
Add hydroxyl or epoxide |
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