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30 Cards in this Set

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what the drug does to the body.
Drug properties
3-D in shape, solubilities (water,oil/fat), elect charges(acid/base)
***these encourage or inhib drug from going thru body and also it's effect
what's it look like and move thru?
Drug effects: actions
act thru receptors; rely on lock-key fit; Must reach receptor at concentration to trigger effect; specific enough to limit other effects (SE), grouped into 2 processes
Therapeutic vs adverse effect:
Therapeutic: what trying to achieve
Adverse: (SE) what trying to avoid 1.toxic (OD,interactions) vs Idiosyncratic/allergic effects (surprise)
Risk:Benefit Ratio
balance btwn probability of Tx & Adv Effects
Drug Receptors
1.macromolecular components of an organ that drug binds
2.result in change of physiologic function
3.Most are proteins on surface of cell
4.for endogenous molecules
Mimics signaling of endogenous compound
drug receptor interaction
Blocks normal signalling
Partial agonist
Yields an attenduated signaling (lock/key); close to fitting, but only partially; can start compound reaction
Ie. block hr getting too high, but won't go too low that you pass out
What constitutes if there is a hypo- or hyper-reactivity with an interaction?
1. concentration of the drug at the receptor
2. concentration of receptor
3. function of receptors (genetically- will mafunct if not enough receptors)
4. components of resonse distal to receptor
5. Genetic variants (can now test for enzyme before giving- a drug that could kill the person if they didn't have the enzyme)
think receptors
what the body does to the drug
Therapeutic range
range of drug tissue concentration w/in where pahrm response is produced and adverse effects are prevented
faction of administered dose that reaches circulation
f=.5 or 50%
First pass effect
absorbed through the GI tract and then gets processed by the liver; the dose that will never reach its systemic circulation due to breakdown
f=100% iv route: doesn't go through gi tract then liver.
-definition and what inhibited by
pumps the drug back into GI lumen, opposing their absorption
Inhibited By: durgs
Inhibition by: grapefruit juice component
True or False:

Protein binding changes are RARELY a cause of significant interactions
Transporter Protein: Effects
1. @ intestine will alter drug absorption
2. @kidneys or lier will alter drug metabolism
3. @ BBB will decrease CNS toxicity
4. @ tumor cells will decrease drug efficacy
where are they at and what happens there?
Volume of Distribution (Vd)
definition and what it's associated with...
A proportianlity constant relating the amt of drug in the body to the serum concentration;
Apparent volume
Assoc with:
1.increasing lipophilicity (moves into fat)
2.decreasing hydrophilicity (moves into water
Drug Metabolism primarily at what organ?
Drug excretion primarily through:
what organ?
What happens to the drug when metabolized?
changes/altered to make it more water soluble (polar or electrically charged) for easier elimination from the body
Phase I-Metabolism
Change in structure; by the liver
1. Oxidation:
Hydroxylation- Phenytoin, APAP
Dealkylation- diazepam
Deamination- Amphetamine
Sulfaxidaton- Chlorpromazine
2. Reduction- Sulfasalazine, Chloramphenicol
3. Hydrolysis- ASA
3 changes- O R H
Phase II Metabolism
conjugation by liver; adds mol to drug

1. Glucuronidation- apap,chloramphenicol
2. Methylation- Norepi
3. Acetylation- Procainamide, Isoniazid
True or False:
You can have phase II without undergoing phase I of metabolism.
Cytocyhrome P450 enzyme
aid in oxiding reactions
Name cytochrome p450 enzyme abbrev:
1. cytochrome Superfamily
2. cytochrome family
3. cytochrome Subfamily
4. cytochrome Isoenzyme
1. CYP
2. CYP 2
3. CYP 2C
4. CYP 2C19
Where are the CYP?
1. the cell-endoplasmic reticulum
2. Tissue- skin, kidneys, lungs, brain, liver, intestine
name 2
Drug Elimination
fremoving drug from the body
describes function of the kidney; estimated by creatinine clearance (CLcr)
m=(ml/min)=(140-age)x wt(kg)/ 72 x Scr
f= est CLcr male x 0.85

** use IBW if obese