Answers
When were the first recordings of drug actions China in 2000 BC, also Egyptians (Ebers Papyrus)
Pharmacology the science of drug action on biological systems
Pharmacy clinical practice devoted to the formulation, proper and safe distribution and use of
drugs
Pharmaceutical Drug chemical substance for medical diagnosis, treatment, or prevention of disease
Who is the father of western medicine? the ancient Greek physician Hippocrate
What did Hippocrates believe that was different than Separation of medicine from religion/superstition, involvement of ethics in medicine
previous medicine?
What did Galen introduce? introduced the study of anatomy and described the actions of agonists and
antagonists
What did scientist develop during Islamic Golden Age? an understanding of drug quantities and formulations
What was the Swiss-German physician/scholar Paracelsus the father of toxicology: "The dose makes the poison.
refered to as?
What did William Withering, English botanist in the 1700's digitalis
discover and what is its relationship to Tucson? Used to treat heart conditions
nerium oleander here in tucson
What did the Lewis and Clark expedition discover? willow bark tea to treat fever and pains (salicilin is metabolized to aspirin -
also known by Hippocrates)
What did Friedrich Serturner do? isolated an alkaloid from opium, then tried it himself with 3 friends, all overdosed for
3 days with wild dreams
Decided to call it Morphine
Why is it called morphine? caused weird dreams, morpheus is the greek god of dreams
Who founded modern pharmacology? Friedrich Wohler and Claude Bernard
What did Friedrich Wohler do? started synthetic organic chemistry
, What did French physiologist Claude Bernard found? Founded the concept of homeostasis (maintain the internal environment despite
external inputs).
Pharmacodynamics the mechanism of drug action
Drugs act on ______ resulting in a change in the system receptors (usually proteins)
_ _____ are molecules that translate the receptor drug effectors
interaction into a change in cellular activity
Why is the lock and key model wrong? receptors are not completely inactive until an agonist comes along
no perfect key just only ratios between how well your drug binds to your prefered
target vs others
Receptors fluctuate between ________ and ________ favored, disfavored energy states
R= favored energy states
R*= disfavored, active, high energy state
Agonists do what to free energy states lower free energy of the activated states, making it more favorable than the baseline
state
Binding of a ligand can cause _________ induced fit--> conformational shift of the receptor that can cause effector signaling
Receptors are never completely "on" or "off". True or False True
some imperfect agonists can still stimulate the receptor given enough
concentration
Saturation Radioligand Binding a known amount fo radiolabeled established drug is competed off of a receptor by
a non-radiolabeled drug with unknown affinity
Bmax total number of binding sites
Kd binding constant (affinity) of the drug (usually in nM)
IC50 concentration at 50% inhibition
Ki binding constant (affinity) of our experimental, unlabeled drug (nM)
Assumptions -bound concentraion is negligible compared to free
-no binding coopertivity
-at equilibrium
-binding is reversible and follows Law of Mass Action
What is the problem with competiton binding Allosteric sites
experiments? -other sites on the protein
Most drug binding to receptors involve ______ interactions non-covalent
with key amino acids.