Intro Flashcards
A response to a drug which is noxious and unintended, and which at doses normally used in man
Adverse drug reaction
1 out of ____ elderly patients admitted to hospital with ADR or had one during stay.
10
What are factors that predispose patients to develop ADRS?
- unlicensed/off label Rx
- Pharmacokinetics/pharmacodynamics
- OD
- underreporting (not identified
What are medications involved with ADR ED visit?
insulin/anticoagulant/antibiotics/OD/ibuprofen
allergic reactions
What are the demographic variables for adherence
age
literacy
language
education level.
Medical variables for adherence?
severity/duration of illness
impairment
stress
What is pre-clinical development process of drugs?
target audience identified
Chemist make compounds
Testing occurs
What are phases of drug development process?
Saftey
Safe + effective
Safe and EFFECTIVE
SAFE
drug names based on
source
chemistry
effect
regulation
What are the pharmacokinetics
Absorption
Distribution
Metabolism
Elimination
What is absorption influenced by?
Physiochemical properties Lipid/water coefficient (lipid better) Blood flow to side of administration Dosage form (liquid) Temp(high)
What are the physiochemical properties?
non-ionized absorb better
acids better in low pH base at high.
Distribution of drug depends of what?
where blood flows and presence of plasma proteins (albumin)
hypothetical concept to describe where drug exists in body?
Volume of distribution
dose/ plasma concentration
a small Vd is?
large?
drug confined to plasma
drug passes easily and distributed.
modifies drug to facilitate excretion
Metabolism
Phase 1 of metabolism?
reactions make drug more water soluble
done by p450 enzymes
Phase 2 of metabolism?
conjugation reaction.
adding endogenous polar molecule to drug.
What happens in elimination of pharmacokinetics?
drugs undergo glomerular filtration to enter tubular fluids.
reabsorbed if not water soluble.
% of given dose that reaches systemic circulation?>
Bioavailability
IV=100%
Bioavailability is reduced by:
- incomplete absorbtion
- first pass metabolism.
Drug increases activity of enzymes responsible for its metabolism?
decreased?
enzyme induction
inhibition
rate of elimination proportionate to concentration
first order elimination
time is takes for concentration of drug to decrease to half the value it had at start of dosing interval?
half-life elimination.
A constant amount of drug is lost per unit time?
zero-order elimination
What are the enteral routes of administration?
oral/sublingual/rectal
Parenteral: injection/inhale/topical/transdermal/IV
What is the goal of dosing?
to maintain a plasma concentration with a specified range over long periods of time
What does dosing take into consideration?
clearance
desired plasma concentration
bioavailability
Sites of drug action?
-receptor/ion channels
-transport molecules
enzymes
direct bind to nucleic acids
non-human targets
What is drug-receptor interaction?
drug combines with molecule on cell to produce biologic effect
transmits conformational change to generate signal.
Transmembrane spanning proteins that allow selective passage of specific ions
ion channels
a compound that binds to a receptor and produces the biological response?
agonist
partial agonist cant produce 100% response.
Blocks or reverse effect of agonist?
antagonists.
competitive make less potent
non-competitive bind to dif site.
dose at 1/2 Emax?
Kd/ EC50
small kd= more potent
What is equation for therapeutic index?
do you want it big or small?
TD50/ED50
big so that more causes harm.
what changes in pharmacokinetics with age?
liver fx declines
renal clearance declines
maintenance dose decreases
expect a _____ increase in plasma drug levels at temps higher than 30 deg C
1.5-2.5 fold
Why is there delay in absorbtion of oral drugs with exercise?
slow gastric emptying. and slow bowel transit time.
What is reduced with exercise meaning more rapid elimination?
Vd
Low hepatic extraction drugs are generally not affected by change in blood flow due to exercise but may be affected by ____
level of fitness.
For high extraction ratio drugs, there is _______ during exercise
less metabolism
Regular exercise caused greater _____ and shortened ____
metabolism
t1/2
GFR decreases______ with exercise.
meaning
30%..
decreased elimination
What are some assumptions with exercise and drugs?
- decreased GI absorbtion
- increased subQ/IM/transdermal absorption
- reduced Vd/metabolism/elimination
