PGx of Drug Metabolism pt. 1

What are the three main PGx approaches that are commonly used?

:aims to optimize medication use by have genetic information at the point of prescribing for all patients regardless of demographic or risk parameters.

:uses the same principle except for a specifically defined "at-rirsk" population

: occurs after the patient has already been diagnosed or after a patient is non-responder or toxic responder resulting in a patient needing a treatment that may have a PGx implication

______ is not clinically benefit to 50% of _________ and many suffer frequent adverse drug-related events.

The lipid & cholesterol-lowering drug _________ leads to _________ in about 25% of patients.

- objective, quantifiable characteristics of biological processes.

Interaction of a drug with its biological target is a __________ effect related to ________

Metabolism affects drug _________ (amount of drug levels in body). This is measured with ________

-the fraction of drug reaching the blood circulation after absorption from GI tract and a first-pass through the liver (portal vein).

Are NRTIs active or prodrugs?

What are Phase I (functionalization) reactions?

What are Phase II (conjugation) reactions?

Phase II metabolism typically results in ____________ of the drug.

-these individuals are deficient in ALDH2 enzyme

-clinical manifestations include: characteristic facial flushing, headaches, nausea, dizziness, and cardiac palpitations

What type of mutation is the ALDH2*2 mutation?

Most common ethnic group affected by ALDH2*2 ?

-ALDH2 inhibitor

-used to support treatment of alcoholism

-produces acute sensitivity to ethanol by preventing acetaldehyde oxidation to acetate

What kind of reaction is this? And what phase does this occur?

What kind of reaction is this? What phase does this occur?

What kind of reaction is this? What phase does this occur?

What kind of reaction is this? What phase does this occur?

Phase I Metabolism generally results in metabolite having _________.

Where are CYP450 enzymes found in humans?

Blue represents -

Green represents-

Yellow represents-

Number represents

______ and _______ families do most drug metabolisms.

The anticonvulsant drug ________, is first-pass metabolized by _______

_________ non-nucleoside HIV reverse transcriptase inhibitor (NNRTI). It is a(n) ______ drug. Metabolized by _______

__________ is a prodrug metabolized by _______ into the active analgesic ______.

Which fruit juice inhibits CYP3A4 enzyme, therefore resulting in higher levels of drug concentration?

: substrate drugs directly affected by drug-drug or drug-food interactions

:drugs that interfere with victim drug metabolism

- drugs that inhibit enzymes

-results in increased drug concentration

-drugs that increase enzyme function

-results in decrease drug concentration

LYNPARZA (Olaparib) is a

a. perpetrator inhibitor

b. perpetrator inducer

c. victim drug

Itraconazole is a

a. perpetrator inhibitor

b. perpetrator inducer

c. victim drug

Rifampcin is a

a. perpetrator inhibitor

b. perpetrator inducer

c. victim drug

-one functional and more than two copies of functional alleles as a result of gene duplication

-two functional alleles

or

-one functional and a decreased function allele

-one LOF allele and a decreased-function alleles

-two decreased function alleles

-two LOF alleles

-one LOF and gene deletion