What is pharmacology? - Answers the study of medicine/drugs
what is a drug? - Answers any substance received by a biological system that is not for nutritional
purposes
What is pharmacokinetics? - Answers what the body does to the drug
What is pharmacodynamics? - Answers what the drug does to the body
what is pharmacogenomics? - Answers the study of genetic factors that underlie variations in drug
responses
why do we use drugs? - Answers 1. To achieve a beneficial effect on an individual
2. To exert a toxic effect on an invading organism
what is the most common mechanisms of action? - Answers mediated by receptors
what is a receptor - Answers a proteins that is the target of drug actions, can be extracellular or
intracellular
what type of drugs attach to extracellular receptors? - Answers water-soluble drugs
what type of drugs attach to intracellular receptors? - Answers fat-soluble drugs
what are the forms of drug receptors? - Answers R-regulatory proteins, E-enzymes, S-structural
proteins, T-transporters
which site of a receptor can drugs bind to? - Answers the active site or the allosteric site
what are the drugs that act on the active site called? - Answers full agonists
partial agonists
antagonists
inverse agonists
drugs are coupled with... - Answers intracellular receptors
ion channel receptors
g-protein coupled receptors
enzyme-linked receptors
dose - Answers the measured quantity of a therapeutic agent to be taken at one time
drug response - Answers the response on the body from a drug
dose-response relationship - Answers the more drug given, the greater the response, to a certain
point
potency - Answers the dose or concentration of a drug required to produce a response of a certain
magnitude
efficacy - Answers the maximal response that a drug can produce as we increase the dose in that
system
which is clinically favoured: potency or efficacy? - Answers efficacy
therapeutic index - Answers Quantitative measurement of the relative safety of a drug, compares the
amount of drug that causes therapeutic effect to the amount that causes toxicity
how do you calculate TI? - Answers TI = TD50/ED50 (toxic dose to 50% of people to effective dose in
50% of subjects)
therapeutic range - Answers the range of drug levels in the blood of a pt in which the drug has the
desired effects upon the body
do drugs with small therapeutic ranges need to be more closely monitored or are they relatively safe?
- Answers need to be very closely monitored
ADME - Answers absorption, distribution, metabolism, excretion
absorption - Answers movement of the drug from site of administration into the bloodstream
distribution - Answers movement of drug from blood to tissues
metabolism - Answers conversion of a drug into a different compound
excretion - Answers Removal of a drug and its metabolites from the body
bioavailability - Answers the percentage of a drug that reaches the systemic circulation
what method of administration has a bioavailability of 100%? - Answers intravenous
lipid soluble drugs can or cannot cross the cell membrane - Answers CAN cross it
most drugs are.. - Answers weak acids or weak bases
ionized forms of drugs are soluble in... - Answers water
unionized forms of drugs are... - Answers soluble in lipids
which organ does absorption mainly occur in and why? - Answers the SI, it has a large surface area,
lots of blood flow, high permeability
, distribution determines the drug's... - Answers onset, duration, and intensity
volume of distribution - Answers measure of the apparent space in the body available to contain the
drug
How is Vd calculated? - Answers (total amount of drug in body/drug concentration in the plasma) x
70kg
what is the purpose of metabolism of drugs? - Answers to increase the drug's water solubility to help
elimination from the body
where is the primary site of metabolism? - Answers the LIVER since it has a high concentration of
enzymes, high blood flow, and receives blood from the GI
what happens in Phase 1 reactions? - Answers usually oxidation via cytochrome P450 enzyme in the
liver, more specifically, CYP 3A4 which metabolizes 50% of the drugs, can also be hydrolysis or
reduction but less likely
what happens in the Phase 2 reaction? - Answers Conjugation: addition of a water-soluble moiety to
the product from phase 1 to make it easier for the kidneys to excrete (main ones are sulfation,
acetylation, glutathione conjugation, glucuronidation)
first pass metabolism - Answers inactivation of orally administered drugs before reaching the systemic
circulation, results in barely any drug reaching the blood
how can you avoid first pass metabolism? - Answers change the route of administration
what is the primary organ in excretion? - Answers the kidneys
what are the main processes that occur before excretion? - Answers filtration, reabsorption of
important things like water back into the blood, and secretion of waste products into the urine
other routes of excretion - Answers lungs, skin, GI tract, body fluids
excretion via bile - Answers excreted by hepatocytes into bile and eliminated as feces
drug half-life - Answers the amount of time it take to eliminate 50% of the drug from the body
t1/2 = - Answers 0.7 x Vd / CL
drug clearance - Answers the process of removing the drug from the body, includes metabolism and
excretion
CL = - Answers rate of elimination of the drug / drug concentration in the blood
first order kinetics - Answers body eliminates a fixed percentage of a drug every time period,
elimination is directly proportionate to the concentration of the drug, not saturable, relies on the
KIDNEYS
zero order kinetics - Answers relies on the liver, body eliminates a fixed amount of the drug per unit of
time, saturable, rate is independent of the drug conc.
Plateau principle - Answers repeated administration of a drug increases the plasma concentration
until the rate of administration (input) = the rate of elimination (output), which takes 5 t1/2 to reach
it
does the plateau principle apply to all drugs? - Answers No, only those that are eliminated via first-
order kinetics
dosage intervals - Answers the amount you take every interval
how to calculate child's dose? - Answers dose = (BSA/1.73) x adult dose
latrogenic - Answers error in prescribing/dispensing/administering the drug
adverse drug reactions - Answers any harmful or unintended reponses produced by the drug
2 types of ADR - Answers pharmacodynamic and non-pharmacodynamic
pharmacodynamic ADRs - Answers extension of the therapeutic effect, could be caused by drug
receptors found in organs other than the target one
non-pharmacodynamic ADRs - Answers unrelated to main action of the drug
drug idiosyncrasy - Answers rare genetic drug reaction
teratogenisis - Answers Process by which agent or drug induces physical defects in unborn child. Can
be over the counter, viruses, environmental pollutants.
idiopathic - Answers unknown cause
drug-drug interactions - Answers modification of the effect of one drug by the presence of another,
can be beneficial or harmful
types of DDI - Answers additive, antagonistic, synergistic, potentiation, altered physiology
additive - Answers drugs are given together to double the effectiveness, they both bind to the same
receptors (1+1=2)
synergistic effect - Answers interaction of two or more medicines that results in a greater effect than
when the medicines are taken alone, exaggerates the effect, bind to different receptors (1+1=3)