General Principles of Pharacology Flashcards
name 3 physiochemical properties of drugs
molecular size
fat/water solubility
ionic charge
what determines the degree of fat and water solubility of drug
polarity of drug
what determines ionic charge of drug
acidic basic neutral nature of drug
how is molecular size determined
number and type of atoms in molecule
arrangement of molecules (sterochemistry)
Why is molecular size important for drug
determine whether it passes through pores or between cells
Adding what type of element makes molecules bigger
halogens
why is solubility important for a drug
determines if drug stays in plasma or penetrates tissue
what type of molecule makes a drug polar
ionizing
how is solubility measured
partition coefficient (P.C.)
formula for partition coefficient (P.C.)
[drug]fat/[drug]water
what does P.C. >1 mean
lipophilic
hydrophobic
P.C. Less than 1
hydrophillic
define acids ( weak/strong)
proton donor
for weakly acidic drugs, what are characteristics of its conjugate base
polar hydrophilic in plasma
characteristics of weakly acid drug
lipophillic in tissue
define base
proton acceptor
characteristics of weakly basic drugs
lipophillic in tissue
many amines
for weakly basic drugs, what are characteristics of its conjugate acid
stay in plasma
define neutral compounds
neither donates or accepts protons
what are two categories of neutral durgs
charged and uncharged
neuromuscular blocking drugs are what type of drugs
neutral charged
neuromuscular blocking drugs characteristics and how is it usually adminstered
IV
quaternary ammonium is what type of drug
neutral charge
carboxylic acid contributes to becoming what type of drug
acidic groups
amines contributes to becoming what type of durg
basic groups
what is so special about categorizing amino acids
they have both amine and carboxylic acid
alcohols, aldehydes, amides, esters are in what group
neutral uncharged
Henderson-Hasselbach equation determines what in drug
if drug is going to be ionized or unionized in its form
-whether it not it crosses barrier
equation for Henderson-Hasselback for weak acid
pH = pKa + log (base)/(acid)
A-
base form of weakly acidic drug
HA
acid form of weakly acidic drug
equation Henderson-Hasselback for weak base
pH = pKb + log (acid)/(base)
B
base form of weakly base drug
BH+
acid form of weakly basic drug
Name 4 ways drugs cross biological membranes
filtration through pores
passive diffusion
active transport
endocystosis
name 2 types of passive difusion
simple
carrier
how do most uncharged drugs cross the membrane
passive diffusion
how do most charged drugs cross the membrane
active transport
driving force for filtration through pores
pressure gradient
what is the rate of filtration through pores dependent on
pressure gradient
size of particle
what provides the pressure gradient for filtration through pores
heart contraction
active transport requires what
cellular energy
active transport can transport across what gradient
low to high
against [] gradient
what determines the rate of drug transport by active transportation? what does this cause?
- binding capacity of drug species with carrier
- limited availability of drug
- causes competition
drug molecule must have what characteristic in order to move by active transport
full positive or full negative charge
passive (non-ionic) diffusion occurs in what direction?
high to low
proportion to physical force provided
when drugs cross membrane with passive (non-ionic) diffusion what characteristics must the drug have
dissolve in aq. solution
dissolve in lipid membrane
how do neutral uncharged drugs go though membrane
maybe pores
no active transport
maybe passively diffuse
how do neutral charged drugs go though membrane
maybe pores
maybe active transport ( permanent cations)
no passive difusion
how do acid form of weakly acid drugs pass
maybe pores
no active transport
maybe passive diffusion