pharmaceutics concept exam 2

what does Tf = 0.52 mean

will be isoosmotic with blood

colligative property of nonelectrolyte

all have identical colligative properties

colligative properties of electrolytes

equimolal solution of electrolytes will have higher osmotic pressures than equimolal solution of nonelectrolytes

is weak serum osmolality leads to

weakness or worse - seizure/coma

is strong serum osmolality leads to

weakness, CNS changes

body osmotic pressure identical to what

0.9% solution of NaCl

hypertonic

-water leaves, shrinks

isotonic

perfect 50/50

hypotonic

-water adds in, bursts

class I method

calculate amount of NaCL need to be added

class II method

calculate volume of 0.9% NaCL that need to be added

examples of class I equation

sodium chloride equivalent, freezing point depression, Liso method

examples of class II equation

white vincent method

white vincent method calculate what

correct volume of water needed to dissolve drug to produce isotonic solution

in metal complex primary valence is

normally ionisable

in metal complexes secondary valence is

non ionisable

metal complex made to

contain ligant that occupy two or more coordination positions

another word for chelating agent

claw hand

calcium chelate of Na2EDTA

used instead of NA2EDTA

what is MOA used for

removes metal by exchange with Ca++, help treat lead poisoning

iron complex

alpha and beta chain (both have heme in middle)

ferrous sulfate

treat anemia, give iron to hemoglobin to treat

platinum complex,c isplatin DNA binding

3D structure that cross DNA and kills cancer, Cl replaced with other groups

copper ion

protein use Ca instead of Fe as center, hemocyanin proteni similar to hemoglobin

ex of copper iron in blood

crab has blue blood instead of red

cobalt

interact with 6 diff bond (covalent bonds formed)

zinc complex, insulin relation

stored as hexamer in drugs for patient, how fast insulin affects the body modulated Zinc in complex

zinc as insulin monomer

active form

cyclodextrin

help transport nonsoluble drugs, increase solubility, biocompatible, dont elicit immune response, low toxic in animal, improve bioavailability of drugs

cyclodextrin serve to increase

aqueous solubility of hydrophobic compounds

cyclodextrin enhance

absorption and bioavailability of hydrophobi drugs

cyclodextrin stabilize

compound that degrade by heat, moisture, oxidation, light

cyclodextrin decrease

toxicity of drug in gastrointestinal tract

cyclodextrin overal decrease

toxicity and degradation

cyclodextrin overall increase

stabilization

Q10

estimate shelf life at a new temp

Q10 storage temp decrease

-2.5

Q10 storage temp increase

2.5

on graph where is pH represented to be most stable

at the lowest point of graph

first order kinetics include

reversible, parallel, consecutive

bigger Km

weaker enzyme

smaller Km

better enzyme

what is michaelis menten constant

Km

as S increase further

rate is independent of S and approach constant

as S increase

initial velocity decreases

do the enzyme and substrate react linearly or reversibly to form a complex

reversibly

catalyst

increase rate of reaction without being used up

zero order drug

decrease linear with time

zero order rate of elimination

constant

zero order half life

no true one

first order drug

decrease exponentially with time

first order rate of elimination

proportional to drug

first order half life

constant regardless of drug

example of pseudo zero order

milk of magnesium

how to get linear zero order graph

conc, time

how to get linear first order graph

ln of concen, time

how to get linear second order graph

1/conc, time

drug stability

limit shelf life, extent which preparation retain properties it had at formulation

drug stability unchanged in

physial, chemical property, theraputic activity, microbiological sterility

aggregation of protein

caused by heat, freeze, stress, chemical degradation of amino acids (ex. push drug in needle quick)

protect against photodegradation

color glass, store in dark, coat tablet with UV absorbers

photodegradation

sodium nitroprusside, inorganic, stable for year away from light, shelf life 4 hours if seen with light

how to tell if reaction went through photodegradation exposed to light

hv present, H removed cause loss in drug activity

which wavelength most damaging

300-400nm

specific protein ligand interaction

drug -receptor, enzyme-substrate, antibody-antigen

non specific protein ligand interaction

protein-drug interaction

are protein ligand interactions reversible or not

reversible

most abundant plasma protei, multifunctional

human serum albumin

HSA has

2 binding sites, if 2 go to same site they compete

parameter of protein binding

affinity (association constant) and capacity (bind site on protein)

the higher the Ka the

stronger the binding

if phenyl has higher Ka than warfarin, what to expect

increse in free warfarin bc all phenyl binded due to strong Ka - lead to strong binding

where is the association constant in a graph

the intercept value

where is the number of binding sites

the n value on the intercept (n x 10^6)

class I drugs

most protein not occupied, given in low dose

class II drugs

all protein occupied, given in high dose

both class I and II

drug from class II bind to all protein, warfarin free number increase

vitamin E+C best way to

remove free radicals

vitamin C

become free radical and catches free radicals and remove them while moving as well

antioxidant

oxygen scavengers, terminate free radical reactions

what does EDTA do

catch heavy metals and prevent them acting as catalyst in oxidation reactions

how to determine oxidation reaction

look for OH bonds present

how to determine hydrolysis reaction

look for ester/amide

hydrolysis

ester form carboxylic acid and alcohol

amide form carboxylic acid and amine

-water breakdown

-attract electrons

low temp water

slows down degradation

old to new drug changes

longer half life → more stable

how to prevent hydrolysis

momdify active compound strucutre, dry powder by reconstitution in water, store at low temp

oxidation

increase in C-O bond, reduced C-H bonds

-loss of electrons

-can form disulfide bond

autoxidation

in ambient temp, involve molecular oxygen and free radicals

free radical oxidation phases

initiation, propagation, termination

initiation

RH → .R + .H

propagation

.R + O2 → .RO2

termination

.R + .R

superoxide

free radical

peroxide

suepr free radical