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Fundamentals 1 > Pharm Week 2 > Flashcards

Pharm Week 2 Flashcards

1
Q

agonist

A

substance that binds to and activates certain receptors on cells

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1
Q

positive allosteric modulator

A

enhances binding affinity of the endogenous ligan with the primary site

increase activity

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2
Q

negative allosteric modulator

A

slows or inhibits binding of ligands to the primary site

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3
Q

competitive antagonist

A

compete for same binding site

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4
Q

Can you overcome a competitive antagonist?

A

yes you can

increase dose and you can reach Emax

this lowers potency

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5
Q

non-competitive antagonist

A

binds to distinct site on a receptor

efficacy decreases but potency (EC50) remains the same

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6
Q

CYP3A

A

most active in drug metabolism

heme-containing oxidase

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7
Q

CYP450

A

active in drug metabolism

heme-containing oxidase

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8
Q

Natural CYP3A4 inhibitor

A

grapefruit juice

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9
Q

4 inhibitors of CYP3A4

A

cimetidine
fluconazole
amiodarone
erythromycin

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10
Q

EC50 vs ED50

A

EC50 is half maximal effective concentration, measure of potency

ED50 is dose that produces a specific effect in 50% of studied population

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11
Q

First order elimination

A

constant proportion of drug is eliminated

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12
Q

GABA

A

major inhibitory neurotransmitter

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13
Q

Phase I reactions

A

oxidation, reduction or hydrolytic reactions

most take place in ER

doesn’t make inactive

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14
Q

Phase II reactions

A

faster than phase I, often uses products from phase I

inactivates drug

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15
Q

Prodrug

A

typically metabolized by phase I reactions to turn into active form

16
Q

UGT1A1

A

clinically relevant UGT

has role in metabolism and elimination of bilirubin

17
Q

xenobiotic

A

refers to any substance that is foreign to the body

18
Q

What form should a drug be in for elimination?

A

hydrophilic

19
Q

Zero order elimination

A

constant amount of drug is eliminated per unit time

Fundamentals 1 (29 decks)

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