Pharm exam 1 FINAL REVIEW Flashcards
Chiral
something that has chiral center that can rotate around center, has mirror image of itself.
Enantiomer
2 mirror images
e.g. racemic mixtures, may have both compounds present
Isomer
Same chemical formula but different structure
Kd
Drug concentration at which 1/2 of receptors are bound
Low k/d = ?
High drug/receptor affinity
k/d does not equal?
EC50, two different concepts
Receptors can spontaneously
shift into active configuration
Tachyphylaxis
quick tolerance
Conventional hybridoma technology antibodies
Takes cancer protein, inject to mouse, mouse makes antibodies, isolate splenic antibodies, combine with tumor cells, makes the antibodies proliferate.
Purple denotes
human
IND, NDA
Investigational new drug, new drug application
Receptors can be ___ or _____ the cell
inside or outside
Receptors that we dont know what they do
orphan receptors
Inert receptors
Drug carriers, albumin, don’t transmit signal but they hold drug.
What does Albumin, alpha-1 acid glycoprotein, and lipoproteins bind to
Albumin: Acidic
a1-acid: basic
Lipoproteins: neutral drugs
Cell surface receptors
Catalytic, ion, GPCRs
Intracellular receptors are
lipid soluble drugs
GPCRs have ______ desensitization and a _______ response.
rapid; fast
Catalytic cell surface receptor example
Tyrosine kinase (TKR)
TKRs
Two monomers, dimerize, dimer then activates, using 6 ATPs, tyrosines become phosphorylated, interacts with relay proteins to make a response
Hydrophobic molecules binding inside the cell membrane
NO and steroids
Permeation
Aqueous diffusion, lipid diffusion, special carriers, endo/exocytosis.
Whole blood/plasma volume
5.6L/2.8L per 70kg person.
Most important factor of therapeutic monitoring is
clearance
Drugs that do not penetrate fat well, you use
IBW
Phase 1 reactions
take off groups
Oxidation, reduction, hydrolysis, hydrogenation
Types of CYP450 (oxidation)
3a4 50%, 2D6 20%, 2B6 8%
CYP450 pathway
-drug binds to p450
- Series of oxidation reduction reactions
-NADPH oxidizes to NADP+
-flavoprotein is reduced/oxidized,
-p450 is reduced, FE3+ to FE2+
-Oxygen binds to CYP450
-oxygen reduced to water
-Drug has hydroxyl group on it
-Drug becomes more water soluble, from lipophilic to hydrophilic+
Phase 2 reactions
attach larger molecules to drug
e.g. glucuronidation, sulfation, glutathione conjugation, glycine
Acetaminophen pathway
Glucuronidation, then sulfation if more of it.
if toxic dose ingested, phase 1 reactions come in. Glutathione conjugation can occur to deactive. Toxic reagent nucleophilic binds to proteins in cell and destroys liver cells, leading to liver cell death.
how many DNA codes for proteins
1-2%
Examples of drugs that need adjustments for genetics
6-MP: TPMT mutations
Warfarin: CYP2C9, poor or rapid metabolizer
Herceptin: tumor overexpressing HER2, target for herceptin therapy.
What % of membrane proteins are carrier proteins
15-30%
ABC uses
ATP
SLC21 uses ______ transport
passive
