316 Complexation and Drug Protein Binding Quiz

ndifranco94's version from 2015-09-24 19:47


Question Answer
Transition metals in biomed applicationsImaging agents (MRI, PET), therapeutic (Cancer)
MRI imaging agentsMn, Fe, Gd
PET imaging agentsCu
Cancer therapeuticsCisplatin (platinum)
Can we use free metal ions in the body? NO, interact with proteins, toxicity
Coordination bond in transition metal complexesmore partially filled d orbitals = high electron spin, more magnetic props
Ligandcompound or ion that donates electron pairs to metal ions for forming complexes
Coordination number# of coordination bonds formed b/n center ion w/ ligand or several ligands
If the ligand is a strong electron donor?weaker magnetic props b/c less coordination bonds; will fill up d orbital first
Stability constantKd = [MLm] / [M][L]^m
Dissociation constant1/Kd
SPECTSingle-photon emission computed tomography
Polydentate ligandscontain multiple electron donor atoms
Chelationcomplexation b/n polydentate ligands and metal ions
Chelation vs. linear transition metal complexesChelation is STRONGER b/c more bonds from chelating groups
Why are more chelation bonds more stable?less chance of transition metal being replaced
Organic molecular complexeshydrogen bonding, electron donor-acceptor complexes, inclusion complexes
Hydrogen bondingDrugs interact w/ organic molecules through H-bonding, improves OR impairs absorption, bioavailability, pharm activity
Ex. of H-bonding altering pharmacological fxnCaffeine (base) + Aspirin (acid) --> Acid-Base Complex
Electron donor-acceptor complexesIodine forms 1:1 charge transfer complexes w/ some drugs, alter pharm fxn
Polymer-Drug complexesNon-covalent interactions b/n drug and excipient (e.g. PEG, PVP) affect absorption, biodistribution, and pharamacological props
Inclusion complexentrapment of a guest molecule in the cavity of a host molecule (e.g. cyclodextrins); solubilize and stabilize hydrophobic drugs
Cyclodextrinshydrophobic cavity, hydrophilic exterior
How to modify release rate in inclusion complexchange affinity b/n drug and pocket
Drug-Protein Bindingfacilitate DISTRIBUTION, INACTIVATE drug by lowering conc at receptor, retard EXCRETION, dislpace hormones/other agent, configurational change in protein, form drug-protein complex that is biologically active
Charge-Charge Protein-Drug interactionscharged protein side chains complex w/ oppositely charged hydrophobic drugs
Hydrophobic Protein-Drug Interactionshydrophobic side chains complex w/ hydrophobic drug
H-bonding Protein-Drug Interactionspolar side chains form bonds w/ polar drug
Protein binding and clearanceprotein binding controls volume of distribution and affects hepatic and renal clearance
Free drugusually what is correlated to pharmacological effect (bound drug can't do anything)
Drug displacementcan occur by direct competition of two drugs at same binding site