Lecture 1 - Introduction and Case Study Flashcards
a scientist that researches new drugs
pharmacologist
a licensed health professional who prepares, dispenses, and advises on medical drugs
pharmacist
what is pharmacology?
the science of drugs and their effects on living things
what are the two main divisions of pharmacology?
pharmacodynamics and pharmacokinetics
how do drugs exert their effects on the body?
by binding to targets and triggering a change in physiology
drugs exert their effects on the body by binding to _____
receptors
what is pharmacodynamics?
what drugs do to the body
includes duration and magnitude of response, and dose-response considerations
pharmacodynamics
what is pharmacokinetics?
what the body does to drugs
includes measures of drug absorption, distribution, metabolism, and elimination
pharmacokinetics
a drug which was marketed as an anti-histamine that did not cause drowsiness
terfenadine (seldane)
terfenadine is metabolized by the liver into its active antihistamine form:
fexofenadine
the molecular target of a drug
receptors
a compound which is not intrinsically active, and is activated by some metabolic step after administration
prodrug
if metabolism of terfenadine to fexofenadine is inhibited somehow, the inactive form can circulate in the body and ____
block certain potassium ion channels in the heart
what does it mean for a drug to have an off-target effect?
drugs are usually not perfectly specific for one receptor type and will sometimes influence closely related or completely unrelated receptors
in the context of pharmcology, what is an adverse event?
an undesirable drug effect which can vary in severity; some are mild/benign and some are lethal
the genetic background of a pateint which can affect how they respond to a drug
pharmacogenomics
one drug/substance can adversely affect the reponse to another. for instance, ingesting multiple drugs at once can have unexpected consequences
drug interations
all of our physiological functions are a result of _____ interacting with _____ in our body
chemicals, proteins
target proteins must possess a high _____ for its endogenous _____
affinity, ligand
what happends when a ligand binds to a receptor?
some early, recognizable chemical event must occur
receptors must possess structural and steric _____ for ligands
specificity
receptors are _____ and _____
saturable, finite
what is a ligand?
any molecule that binds to a receptor
drugs interact with target proteins to produce a change in:
the state of the protein, which is translated into a physiological effect
how do drugs bind to receptors?
the vast majority of drugs bind reversibly to proteins
true or false: an equilibrium between bound and unbound proteins exists
true
what type of interactions allow drugs to bind to proteins?
electrostatic interactions (common, reversible), or covalent bonds (rare, generally irreversible)
a drug that binds very tightly to its receptor requires a ______ to achieve the desired therapeutic effect
lower dose
drug binding induces a _____ in the receptor, which causes a physiological effect
conformational change
are receptors selective or specific?
selective
what does it mean for a drug to be selective?
they can bind many different drugs with different affinities