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BMS Chapter 2

Terms in this set (27)

What is a core structure (scaffold or pharmacophore) on which different functional groups can be added to enhance binding to the biological target on which it works, to change the physical properties of the drug for better absorption or distribution, or to block (or enhance) metabolism for the body to eliminate the drug?
Structure Activity Relationship (SAR)
All of these play unto the SAR of a drug class
what can differences in drug effectiveness be traced to?
functional groups that are placed on a scaffold that looks very similar from one drug to the next.
The strength of the interaction between the drug and the target determines what?
how long the drug will have an effect on that target (on/off aspect of drug binding)
The strength of the drug binding in dependent upon interactions of what?
Functional groups between the drug and the target
The more interactions, the tighter and longer the fit, which also means what?
A stronger effect
How many target molecules need to be affected?
It varies - you may need a lot or only a small percentage depending on the effectiveness amount
What is the point at which one sees the effect (and lower levels will cause nothing)?
Threshold for action
What does it mean when the threshold for action has been reached?
The appropriate number of target being affected (bound to) by the drug
Why do we see different doses of drugs?
The concentration of drug for an effect can vary from person to person
What is the importance of drug therapy and dosing?
dose can make it a drug or poison
Why are old drugs sometimes no longer made?
profit margins are low, so manufactured in China or India
What is a concern during manufacturing?
Sometimes companies take short cuts and lower concentrations or add toxic compounds
What is the study of design, development, and ultimately pharmacology of compounds that have therapeutic value or purpose, and can be developed into drugs to treat disease or other physiological issues? It seeks to learn how to best affect an interaction with a target by manipulation of structures that have a common motif, and thus are identifiable for a specific purpose?
Medicinal Chemistry
Modern drug discovery and development is based on what?
ADMET
How was drug development originally done?
Discovered at random, tested on animals, called a drug, then tested on humans. So, side effects sometimes took a long time to find or be noticed.
What drug taken by pregnant women for morning sickness caused children to be born with flippers for limbs?
Thalidomide
What is important to look at for deciding if a drug is safe overall?
Risk VS benefit
What does A in ADMET mean?
Absorption (how much gets into the body)
What does D in ADMET mean?
Distribution (Where does the drug end up)
What does the M in ADMET mean?
Metabolism (how does the body alter this med)
What does the E in ADMET mean?
Excretion (Where is it eliminated)
What does the T in ADMET mean?
Toxicity (Risk vs Benefit, will this harm the patient)
Absorption is intimately affected by the ________ of the drug.
Polarity (non-polar=better absorption; polar=poor absorption)
What part of ADMET is determined first?
Toxicity - listed last because this can be determines at any time, not just clinical trials (however, if it appears here, likely wont be able to continue)
How do they determine risk vs benefit?
No number associated with risk. It is dependent on the type of drug (antibiotic vs cancer drug)
When did the FDA regulate more?
When formation of the Consumer Product Safety Commission and consolidation of previous laws and amendments passed.
What happens if there are red flags?
additional studies are required if drug has certain properties
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