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Selectivity
elicits only responses for which it is given
pharmacodynamics
study of a drug at the site of action and effect it has on the body
pharmacokinetics
study of drug absorption, distribution, metabolism, and excretion
toxicology
study of harmful effects of chemicals (drugs, environmental toxins, and poisons)
absorption
dependent on route of administration, product formulation, gastric emptying, disease states, drug interactions, and pH, and first-pass effect
first-pass effect
after absorption, drug is transported to the liver where a significant amount may be metabolized before it reaches the site of action
bioavailability
extent to which the drug reaches systemic circulation
distribution
dependent on drug characteristics (lipid solubility, molecular size, ionized vs unionized) & binding to plasma proteins (albumin; only free drugs can be transported, disease states or drug interactions can displace drugs from binding and increase drug amount and effect)
volume of distribution (Vd)
body space into which a drug can diffuse
metabolism
phase 1: to make drug hydrophilic, phase 2: conjugate to make more polar for elimination so body cannot reabsorb
elimination
filtration-protein binding and molecular size & charge. Passive transport is dependent on pH and lipid solubility
clearance (Cl)
amount of blood from which all drug is removed per unit of time
half-life
predicts how long it takes dosing regimen to achieve steady state concentration
graded dose response curve
dose vs effect, effective concentration: the dose in a patient that will result in half the maximal effect
potency
related to the dosage that produces a given response in a specific amplitude
Emax
maximum effect produced, potency ≠ maximal efficacy
efficacy
refers to the ability of a drug to bind to the receptors, activate it, and lead to some physiological response
quantal dose response curve
represents dose-response relationships in populations, ex. hyperactive vs hypoactive of % people responding to drug
idiosyncratic drug response
infrequently observed drug effect
hypo-, hyper-reactive
on quantal dose curve
hypersensitivity
allergic reaction to a drug
tolerance
time-related loss of response to a drug (weeks > months)
tachyphylaxis
tolerance that happens very quickly (mins > hours)
therapeutic index
indicator of drug's safety, greater the value of TI, the safer the drug is considered to be
receptors
proteins with unique binding sites that can be located free inside the cell and on the cell surface
affinity
refers to the attraction between a receptor and a ligand (drug)
agonist
a drug that binds to the receptor and causes some type of response, has both affinity and efficacy
antagonist
a drug that binds to the receptor without resulting in any response, has only affinity
second messengers
allow the cell to take an external stimulus and turn it into an internal stimulus (cellular response), allow for quick movement of a signal
signal transduction
a drug binds to the receptor and that receptor becomes activated and propagates a signal. proteins are turned on (phosphorylated) and mobilize second messenger molecules
over the counter (OTC)
drugs that do not require a doctor's prescription can be bought off-the-shelf in stores regulated by the FDA through OTC drug monographs