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Factors affecting drug action
Pharm Assessment 14
22
Pharmacology
Graduate
02/26/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
What Pharmocogenomic Information is required on drug labeling?
Definition
Impact/lack of impact of genotype on phenotype

If genomic test is available - Recommended or necessary

Pharmoacogenomic info subsection

Changes in dose based on genotype
Term
What 3 factors can cause variations in drug response?
Definition
Environmental factors
Drug Interactions
Genetic Factors
Term
What 6 factors affect absorption of drugs?
Definition
IV compatibility & dilution problems
Chelators
Changes in Gastric pH
Alterations in gastric emptying time
Alterations in GI transit time
P-gp substrate
Term
How do changes in gastric pH affect absorption of drugs?
Definition
Increase pH (Antacids, H2 blockers)
-decrease weak acid absorption
-increase weak base absorption

Decrease pH (Infections)
-increase weak acid absorption
-decrease weak base absorption
Term
Over expression of what protein in intestinal epithelium can decrease absorption and overall plasma levels of the drug?
Definition
P-gp

**Mutated or decreased expression will cause Increased plasma levels**
Term
What SNP has been associated with increased plasma levels of simvastatin, rosuvastatin, pravastatin, and atorvastatin?
Definition
SLCO1b1 c. 521T>C
Term
What CYP enzymes are the most commonly involved in Drug Metabolism?
Definition
46% CYP3A

16% CYP2C9
12% CYP2C19

12% CYP2D6

9% CYP1A

2% CYP2B6

2% CYP2E1
Term
How does induction and inhibition of CYPs affect drug metabolism?
Definition
Induction - decreases substrate T1/2

Inhibition - Increases substrate T1/2
Term
How are Basic drugs effect by urine pH? (antihistamines, amohetamines, meperidine, etc)
Definition
Decreased Reabsorption by Decreased pH (NH4Cl)

Increased reabsorption by Increased pH (NaHCO3)
Term
How are Acidic drugs effected by Urine pH? (aspirin, phenobarbital, streptomycin, etc)
Definition
Decreased reabsorption by Increased pH (NaHCO3)
Increased reabsorption by Decreased pH
Term
What CYP isoenzyme is needed for greatest efficacy of Tamoxifen?
Definition
CYP2D6
Term
What CYP isoenzyme do Ultra-rapid metabolizers of Codeine -> Morphine have? What does this result in?
Definition
CYP2D6*2x2

Higher than expected serum morphine levels.
Term
Polymorphism of CYP2C19
Definition
Clopidogrel
reduced metabolism -> decreased active metabolite -> higher CV risk

Voriconazole
reduced metabolism -> Increased drug exposure
Term
Polymorphism of CYP2C9
Definition
Warfarin
Reduced metabolism -> Higher bleeding time
Term
polymorphism of CYP2D6
Definition
Codeine
Ultra rapid metabolism

Tamoxifen
Poor metabolism -> higher plasma conc.
Term
polymorphism of G6PD
Definition
Rasburicase
Severe haemolysis with several drugs
Term
Polymorphism of HLA-B*1502
Definition
Carbamazepine and Abacavir
Hypersensitivity Reaction
Term
LDLR polymorphism
Definition
Atorvastatin
LDL receptor deficiency -> familial hypercholesterolaemia
Term
NAT polymorphism
Definition
Rifampicin
Increased drug exposure
Term
TPMT polymorphism
Definition
Azathioprine
Slow metabolism -> increased risk of myelotoxicity
Term
UGT1A1 polymorphism
Definition
Irinotecan
increased neutropenia risk

Nilotinib
Increased Jaundice
Term
VKORC1 polymorphism
Definition
Warfarin
SNPs associated with lower dose requirements
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