Intro to Pharm Flashcards
Agonist
binds to same site as ligand and makes same signal
Allosteric Agonist
binds to diff site than ligand
no signal
greater response than agonist
Partial Agonist
binds to same site
same signal
weaker response
Antagonist
same site
no signal
weaker response- inhibits agonist
Competitive Antagonist
reversibly bind
same site
receptor can reach max effect with enough agonist concentration
Non-competitive Antagonist
irreversibly bind
diff site
receptor cannot reach max effect
Therapeutic Index
TI
TD/ED
higher numbers = safer drug
Potency
concentration to produce 50% of max effect (EC50)
Efficacy
Emax
peak of dose-response relationship
Pharmacologic Antagonism
one receptor
responds to one drug while is inhibited by another
Chemical Antagonism
no receptor
2 drugs bind to each other and antagonize each other
Physiologic Antagonism
D1 affects R1, D2 affects R2
receptors oppose each other
Absorption
movement of drug from administration site to blood
Distribution
drug mvmt through blood throughout the body
Biotransformation
metabolism
drug converted to form where it is more easily eliminated
Elimination
excretion of drug from body
Oral Route
convenient but slow
subject to first pass effect
First Pass Effect
most of drug metabolized in liver before it reaches blood stream
Sublingual and Buccal
direct absorption into bloodstream
Intramuscular
fast absorption
can be given higher dose
Subcutaneous
slower absorption
can be given higher doses
Intravenous
NO ABSORPTION
Inhalation
Fastest absorption
Topical
for local effect
Transdermal
for systemic effect
Passive Diffusion
driven by concentration gradient- no E
no carrier- not saturable
Facilitated Diffusion
driven by concentration gradient- no E
carrier- saturable
Active Transport
against gradient- E needed
carrier- saturable
Charged or uncharged pass best through membranes?
uncharged
- pKa
acidic
+ pKa
basic
pKa
pH where 50% is ionized and 50% is nonionized
Lipid Soluble
nonionized
Water Soluble
ionized
Basic pH will do what to weak acids?
get rid of it
Basic pH will do what to weak bases?
keep it