Pharmacology Flashcards
Who is Paracelsus?
father of pharmacology; worked on mercury; said every drug is a poison, the dosage determined its toxicity
what is coumadin?
aka warfarin; it’s a blood thinner.
what is the name of the first experiments in humans?
phase I clinical trials; not intended for effectiveness of drug
phase II clinical trials?
have to show that drug is actually beneficial
phase III clinical trials?
crucial phase; very expensive; multi-center trials; double blind studies
phase IV clinical trials?
NOT part of the drug approval process; after drug is approved, clinical data continues to be collected by FDA in the “real world”; able to see rare side effects due to larger # of people taking the drug
what source of drug info does our prof use the most?
The physicians desk reference
CLASS I:
a. abuse potential
b. examples
c. physical/psychological effects
d. handling
a. abuse potential: highest
b. examples: heroin, LSD, marijuana, mescaline
c. physical/psychological effects: no accepted medical use
d. handling: experimental or research only
CLASS II:
a. abuse potential
b. examples
c. physical/psychological effects
d. handling
a. abuse potential: high
b. examples: morphine, meperidine, amphetamine, methylphenidate, secobarbital, phencylcidine (PCP)
c. physical/psychological effects: may produce dependence, accepted medical uses
d. handling: prescriber’s signature required; NO refills
CLASS III:
a. abuse potential
b. examples
c. physical/psychological effects
d. handling
a. abuse potential: moderate
b. examples: codeine mixes, weaker stimulants and sedatives
c. physical/psychological effects: may produce moderate-low dependence; accepted medical uses
d. handling: prescriptions may be called in; <5 refills/6 mo; container w/ warning labels
CLASS IV:
a. abuse potential
b. examples
c. physical/psychological effects
d. handling
a. abuse potential: less
b. examples: benzodiazepines, pentazocine; phenobarbital; d-propoxyphene
c. physical/psychological effects: none
d. handling: same as C-III
CLASS V:
a. abuse potential
b. examples
c. physical/psychological effects
d. handling
a. abuse potential: least
b. examples: some codeine containing cough syrup, d-propoxyphene
c. physical/psychological effects: none
d. handling: OTC in some states
Does class II drugs have medical use? how can it be acquired?
yes; get it w/ prescriber’s signature
Does class IV drugs have medical use? how can it be acquired?
yes; prescriptions may be called in
who coined the term receptor?
Langley
occupancy theory?
higher number of receptors binding drugs means greater effect
spare receptors?
full effect of drug w/ less than 100% of receptors binding drug
What are the 4 processes of pharmacokinetics?
Absorption, distribution, metabolism, excretion
what drug is an exception to being metabolized/absorbed before being excreted?
NO
oral dose stays in therapeutic range longer than an IV dose bc ut us absorbed slower. t/f?
true!
inhalation as a method of drug administration is useful for what?
peptides (i.e. insulin)
what are some prolonged release preps for drugs?
drug coatings, drug salts, ion-exchange resin complex, drug polymer
matrix storage and reservoir storage?
matrix - drug imbedded in solid
reservoir - drug dissolved in liquid
what are specific molecular carriers?
viral envelopes, erythrocyte ghosts, liposomes (very good!)
- first 2 methods = not good
liposomes are coated in what?
coated w/ polyethylene glycol (PEG) to stabilize liposomes & evade body defenses
examples of liposomes drugs?
doxil and myocet - for delivery of doxorubicin to solid tumors
what is the lipid/water partition coefficient?
how much drug has gone in each partition (Lipid or water)
statin’s work really well bc…?
they have transporters in the liver that bring them directly to the site of action
what is the fastest method to cross membranes for drugs?
transporters
hexanoic acid?
type of alipoic acid; easy to cross memb; hydrophilic or lipid soluble; need transporter for glc
if you have a weak acid w/ ____ pH, more of the weak acids will be in charged form.
low pH
if you have low pH, more weak bases will be in ______ form.
uncharged
when is pH = pKa?
when there is an equal amt of charged/uncharged form
An acid drug in an acid compartment is going to be transferred _____ and will be present in its ____ form.
rapidly; uncharged
a basic drug in an ____ environment won’t be absorbed bc it will remain in its charged form.
acidic
What are anion drug transporters?
P-glycoprotein (MDR or MDRP–multidrug resistance proteins) & organic anion transport protein (OATP)
tl;dr: MDR/MDRP & OATP
What are cation drug transporters?
Organic cation transport proteins (OCT)
Multidrug & toxin extrusion (MATE)
Organic Cation/Carnitine Transporters (OCTN)
what promotes diffusion? (fick’s law)
larger SA, thinner memb, larger conc gradients
*Fick’s law only covers uncharged form of a drug.