INTRODUCTION Flashcards
branch of science which deals with the study of the effect of drugs on biologic systems
pharmacology
path by which a drug, fluid, poison, or other substance is taken into the body
routes of drug administration
through mouth
oral
underneath the tongue; usually for heart ailment patients; the capillaries there immediately absorbs the drug
sublingual
through the anus
rectal
injections into veins
intravenous
injections into muscles
intramuscular
under the skin
subcutaneous
drugs are atomized into smaller droplets so that the drugs can pass through the windpipe (trachea) and into the lungs
inhalation
directly applied on the skin
topical
penetrates through the skin
transdermal
refers to the fate of an administered drug (what will happen once the drug is administered?)
pharmacokinetics
movement of a drug into our bloodstream after being administered
it affects the bioavailability
drug absorption
how quick and how much drug will reach their intended target site
bioavailability
movement of a drug to and from bodily tissues
drug distribution
biotransformation of drugs intro our body
drug metabolism
makes drug easy to be eliminated in our body
biotransformation
elimination of biproducts of pharmaceutical substances
drug excretion
rate at which an active drug is removed from our body
drug input = drug output, then the rate is at steady state
drug clearance
drug response depends on both the affinity of a drug for its receptors and the drug’s efficacy
receptor theory
strength of binding
between a drug and its receptor
affinity
the degree to which a drug is able to induce maximal effects
efficacy
a drug interaction where 2 or more drugs are taken together, and the effects of each drug will add up
addition
a drug interaction where 2 or more drugs are taken work together against one target
synergism
a drug interaction where drug a will have to boost the effect of drug b
potentiation
a drug interaction where drug a will reduce/block the effect of drug b
antagonism
amount of drug which induces a specified clinical effect in 50% of subjects given the drug
Effective Concentration/Dose
50% (EC/ED 50)
measure of the safety of a
drug
therapeutic index
50% of the subject will die if a drug is given in a certain dose
LD50 or lethal dose 50
50% of the subject will have a positive effect if a drug is given in a certain dose
ED50 or effective dose 50
margin between therapeutic
and lethal doses of a drug
margin of safety
study of exogenous clinical compounds that profoundly influence bodily functions, either in a deleterious way or for therapeutic benefits
toxicology
enables physicians to adjust and optimize the dosage on an individual basis
therapeutic drug monitoring
TDM
- identify the offending drug/s
- establish diagnosis, assess level of intoxication, suggest course of therapy
identification of drugs in
acute intoxication
for pre-employment and medicolegal cases
urine testing for drugs of abuse
four areas of toxicology
- drugs of abuse
- therapeutic drugs
- environmental carcinogens
- toxins
ppm – Parts per million
ppb – Parts per billion
ppt – Parts per trillion
units used to measure toxins
In 1 m3 block 1cc
1ppm
In 1 m3 block 0.001cm3
0.001cc or 1ppb
In 1 m3 block .000,000,001m3
0.000,001cc or 1ppt
1 cc = 1ml = 1g 1 liter of water = 1 kg 1 mg / kg = 1 ppm 1mm3 / liter = 1 ppm 1 mg / liter = 1 pp
relationships
normal procedure in order to determine the toxicity of chemicals the laboratory
expose test animals
By ingestion, application to the skin, by inhalation, gavage, or some other method which introduces the material into the body, or placing the test material in the water or air of the test animals’ environment
methods in testing animals
toxicity is measured in how deadly it is
mortality
toxicity is measured in their ability to cause birth
defects
•teratogenicity
toxicity is measured in their ability to cause cancer
carcinogenicity
toxicity is measured in their ability to cause changes in the DNA
mutagenicity
technique that notes the antibody and antigen reactions
immunologic
separation technique for drug analysis
chromatography
technique that uses spectrophotometer by measuring light spectrum of examples
spectrophotometry
serum (contains the analyte) + antibody + enzyme labelled drug + substrate
measured enzyme activity is proportional to the drug concentration
more rapid than RIA
enzyme multiplied immunoassay technique (EMIT)
MDH & G-6-PD or malate dehydrogenase and glucose-6-phhosphatedehydrogenase
main substrates in enzyme multiplied immunoassay technique (EMIT)
it is a protein that catalyzes enzymatic reaction
enzyme
it is the reaction between enzyme and substrate
enzymatic reaction
drug to be measured is the hapten (-small molecules; they have to bind to larger molecules like protein so it could be measured and elicit response like production of antibodies)
specific antibodies bound to a solid state carrier
patient antigen is sandwiched between the solid-phase antibody and enzyme-labelled antibody
enzyme-linked immunosorbent assay (ELISA)
sandwich immunoassay
in enzyme-linked immunosorbent assay (ELISA), the enzyme activity can be manifested through __?
color
a fluorogenic
substrate/reagent of fluorescence immunoassay
umbelliferyl-β- galactoside
Fluorogenic reagent + antibody + beta-galactosidase — incubated w/ serum sample in 37 degrees C
drug of interest and reagent will compete for binding sites
fluorescence immunoassay
no analyte of interest, no competition
fluorescence immunoassay
Incubation of serum + antibody + radiolabeled drug
serum and radiolabeled drug compete for antibody binding sites
we count for radioactivity
radioimmunoassay
most common technique for testing of drug abuse
adsorption of drug to a solid support and elution by means of a mobile , liquid phase
chromatography
screening for drug identification
thin layer chromatography (TLC)
primarily for quantitating serum drug levels in TDM and also for confirming drug identification
HPLC or high-performance liquid chromatography
GLC or gas liquid chromatography
spectral scan, used for tentative identification of drugs
no longer used because chromatography is more specific in results
spectrophotometry
visible spectrum measures
salicylate
ultraviolet spectrum measures
barbiturates
fluorescence measures
quinidine