Essentials to Pharmacology
Terms
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- Pharmacodynamics
- 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 - 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 - Agonist
- Mimics signaling of endogenous compound
- Antagonist
- 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) - Pharmacokinetics
-
what the body does to the drug
Absorption
Distribution
Metabolism
Excretion - Therapeutic range
- range of drug tissue concentration w/in where pahrm response is produced and adverse effects are prevented
- Bioavailability
- faction of administered dose that reaches circulation
- 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. -
PgP
-definition and what inhibited by -
P-glyco-protein-
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 - True
-
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?
- Liver
- Drug excretion primarily through:
- kidney
- 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 - 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. - True
- 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 - Drug Elimination
- fremoving drug from the body
- GFR
- describes function of the kidney; estimated by creatinine clearance (CLcr)
- CLcr
-
m=(ml/min)=(140-age)x wt(kg)/ 72 x Scr
f= est CLcr male x 0.85
** use IBW if obese