Week 2 Flashcards by Ethan Wong

pharmacology

how drug affects body & body’s response to drug

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pharmadynamics

what drugs does to body

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pharmacokinetics

what body does to drug

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pharmacogenetics

how genetics influence drug response

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pharmacotherapeutics

drug choices for treatment / prevention

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toxicology

body’s response to harmful effects of drugs

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binding types

agonists, competitive & non-competitive antagonists, allosteric activator

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agonists

activates receptor for effect

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competitive antagonist

competes with agonists to bind to receptor binding site

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non-competitive antagonist

binds to other receptor site that affects main binding site

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allosteric activator

binds to other receptor site that enhances main receptor binding site

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principles of pharmacokinetics

MADE = metabolism, absorption, distribution, excretion

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metabolism

drug transformation of drug into hydrophilic form for kidney elimination

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where does metabolism mainly occur

liver

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enzymatic phases of metabolism

phase 1 = functionalization / catabolism
phase 2 = conjugation / anabolism

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what does functionalization mainly involve

cytochrome P450 group of enzymes

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CYP enzymes are ___ - containing enzymes

heme

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most common CYP

CYP 3A4

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alcohol is metabolized by __

CYP 2E1

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CYP inducer example

rifampicin

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CYP inhibitor example

fluconazole

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CYP substrate example

warfarin

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what does conjugation involve

adds molecule to increase hydrophilicity via
- methylation
- acetylation
- glucuronidation
- sulphation

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absorption

% of drug that remains unchanged entering systemic circulation via plasma administration

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why is oral administration not 100%

incomplete absorption across gutwall / first-pass elimination by liver

oral administration is mainly absorbed in __

ileum

absorption modes

- facilitated passive diffusion - active transport - passive diffusion

distribution

amount of drug in relation to concentration in plasma/body

Vd formula

amount of drug in body / plasma concentration

high Vd =

exceeds bodyweight

low Vd =

value close to blood volume (5L)

Can Vd exceed physical volume of body

yes

major compartments of distribution

- plasma (5%) - interstitial fluid (16%) - intracellular fluid (35%) - transcellular fluid (2%) - fat (20%)

lipid insoluble drugs mainly confined to __

plasma & interstitial fluid

excretion

drug eliminated from kidneys into urine

if patient have defective kidneys, how should you change your drugs

reduce dose / switch to alternative agents

main excretory routes are __

kidneys, hepatobillary, lungs

clearance is fundamental ___ parameter for drug elimination

pharmacokinetic

what factors are involved in dose planning

concentration, intervals, route of administration

what does dose planning determine

therapeutic index for safe drug testing

when is monitoring needed

for narrow therapeutic index drugs

half-life

time for drug concentration reduced by 1/2

decreased T1/2 = increased ___

drug clearance & dosing intervals

an ideal therapeutic dose has __ efficacy, ___ toxicity

high; low

where is the therapeutic index

between ED50 & TD50

ED50

median effective dose

TD50

median toxic dose

what causes drug response variations

- different drug concentration reaching receptor site - different endogenous receptor ligand concentration - altered receptor function - changes in downstream response to receptor binding

tachyphylaxis

sudden desensitization to drug

adverse drug effects

hypersensitivity, idiosyncratic, iatrogenic, teratogenic

hypersensitivity

allergies

idiosyncratic

unusual response to drug

iatrogenic

negative effect of drug

teratogenic

harmful to fetus

drug interactions

ASAP additive, synergistic, antagonist, potentiation

drug administration methods

instillation inhaler sublingual transdermal suppository topical subcutaneous intravenous intramuscular

instillation occurs at

ophthalmic (eyes), ears, intranasal

where does intramuscular injection occur at

deltoid, vastus lateralis, gluteus maximus

most rapid onset of drug administration

intravenous

parenteral

any drug administration which involves using a needle

parenteral examples

intravenous, intramuscular, subcutaneous, intraosseous, epidural, intradermal

what CYP is important for clopidogrel

CYP2C19

variants of CYP 2C19

*1 = normal *2 - *8 = no / reduced enzyme *17 = increased activity

why are some medications taken after food

increases bioavailability & pH adjusted when digesting food

a drug with a low Vd tends to remain in ___

plasma

a drug with high Vd means __

more distribution to other tissues

Week 2 Flashcards

(66 cards)