Term
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Definition
| In ______, individuals show differing drug responses |
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Term
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Definition
this term refers to how the drug gets moved about in the body and relates to Rate of
Absorption
Transport
Metabolism
Excretion |
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Term
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Definition
this term refers to the variation in therapeutic response to the drug
Variation in the drug’s targets
Receptors
Enzymes
Pathways |
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Term
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Definition
Phase I metabolism of xenobiotics
56 different enzymes 56 separate genes
Heme proteins
Located in liver
Catalyze redox reactions using NADPH
Add O to C,N or S
Most common reaction is hydroxylation
Hydroxylation is common in Phase I metabolism
Introduction of polar (O) group
Permits Phase II (addition of Glc, AcOH etc.) |
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Term
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Definition
| what are the three most important cytochrome families that act against the widest variety of drugs? |
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Term
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Definition
| Which specific cytochrome family detoxifies the largest percentage of drugs? |
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Term
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Definition
| this type of chromosome response leads to a risk of toxicity with standard dose |
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Term
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Definition
| this type of chromosome response leads to a risk of sub-therapeutic levels at standard dose |
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Term
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Definition
| codeine is hydroxylated to? |
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Term
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Definition
is a topioisomerase inhibitor used in cancer chemotherapy
High levels can lead to bone marrow and GI toxicity
Product of gene UGT1A1 conjugates this drug and permits its excretion with bile |
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Term
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Definition
| ____ in TATA box results in variation in gene transcription |
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Term
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Definition
UGT1A1*1 has _ repeats (normal)
UGT1A1*28 has _ repeats (reduced transcription) |
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Term
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Definition
| has 5 times the normal risk of complications with camptothecin therapy |
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Term
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Definition
is used to treat Tuberculosis
Impaired metabolism can lead to peripheral neuropathy and bone marrow suppression
Elevated metabolism results in poor curative value for TB (this is an example of N-Acetyltransferase Polymorphism)Allelic differences in the NAT2 gene
3 slow alleles are common
Also many rare ones
Also “rapid” metabolizers |
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Term
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Definition
| Fast acetylators need higher doses of (2)? |
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Term
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Definition
Slow Acetylators at risk of
___ ____ like syndrome |
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Term
| thiopurine methyltransferase |
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Definition
6-mercaptopurine and 6-thioguanine
Treatment for childhood leukemias
Immunosuppression
Metabolized by ? |
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Term
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Definition
| this drug has prolonged postoperative paralysis |
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Term
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Definition
this drug is paralytic and
Hydrolyzed by Butyrylcholinesterase |
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Term
| G-6-PD deficiency and Hemolytic Anemia |
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Definition
X-linked
10% african males affected
Drug-induced hemolysis
400 variant alleles
Mostly point mutations
Oxidative drugs stress glutathione system
Primaquine
Sulfonamides
Sulfones
Naphthalene
Favism |
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Term
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Definition
AD common reaction to inhaled anasthetics (halothane)
High fever
Elevated Ca2+ in sarcoplasm
Muscle rigidity and temperature elevation
1 in 50000 adults, 1 in 5000 children
RYR1 and CACNL2 genes (calcuim channels)
Exact mechanism not known |
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Term
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Definition
combined effect of pharmacokinetics and dynamics
Anticoagulant – thromboembolism
Blocks Vitamin K epoxide reductase complex 1 |
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Term
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Definition
Involved in carboxylation of factors II, VII, IX and X; A/A needs half as much as B/B (3X variation in mRNA)
20M patients in US p.a.
0.1 – 1% fatal bleeds p.a., 0.5 – 6.5% serious bleeds |
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Term
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Definition
| this cytochrome family is polymorphic (kinetics) Heterozygotes need 20% lower dose |
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Term
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Definition
this term refers to the assesment of common genetic variants for impact on drug therapy
Mechanism, gene-function need not be known
Demonstrate positive predictive value
Ehnicity and race
Complex factors
Environmental factors |
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