Fundamental techniques and knowledge Flashcards
types of drug names (4)
(1) chemical, (2) generic (nonproprietary), (3) trade and (4) street
what does the stem (last part of name) of a generic drug name indicate?
class or function
stem that indicates an antidepressant
-oxetine
what is the trade name for diazepam?
Valium
stem for local anaesthetics
-caine (eg.dibucaine)
stem for antianxiety agents
-azepam (eg. lorazepam)
which type of drug name is capitalized?
trade names
excipients
fillers, coloring agents, binding agents, and coatings
what is the common street name for MDMA?
ecstasy
drug dosages are in ____
milligrams (mg)
a milligram is 1/____ of a gram
1000
behavioural and physiological effects of a drug are related to its _______ rather than the absolute amount of drug administered
concentration in the body
dose-response curve (DRC)
a graph with the dose on the x-axis and effect on the y-axis
the horizontal axis of a DRC curve is usually plotted ____
logarithmically
ED50
median effective dose
LD50
median lethal dose
median effective dose
the does that is effective in 50% of the individuals tested
median lethal dose
the does that is lethal in 50% of tested individuals
therapeutic index (TI)
the ratio of the LD50 to the ED50 (higher is safer)
TI = LD50/ED50
potency
differences in the ED50 of two drugs with the same effect (lower is more potent)
effectiveness
differences in the maximum effect that drugs will produce at any dose
antagonism
when one drug diminishes the effect of another
what shift would you see in a DRC if antagonism was occuring?
a shift to the right
additive effect
when one drug increases the effect of another
what shift would you see in a DRC if a drug was having an additive effect?
shift to the left
superadditive effect or potentiation
drugs have an effect together that is greater than might be expected simply by combing their effects
pharmacokinetics
the study of how drugs move into, get around in, and are eliminated from the body
processes of pharmacokinetics (3)
(1) absorption, (2) distribution and (3) elimination
sites of action
the area of the body where a drug has an effect
parenteral routes of administration
injection through the skin into various parts of the body using a hollow needle and syringe
divisions of parenteral routes of administration (4)
(1) subcutaneous, (2) intramuscular, (3) intraperitoneal, (4) intravenous +other
vehicle
the liquid in which a powder drug is dissolved or suspended (usually a weak salt solution)
common vehicle
normal or physiological saline (0.9% sodium chloride)
example of a non-water based vehicle and why it might be used
vegetable oil; if drug is not water soluble it may be lipid-soluble (slows rate of absorption and prolongs drug’s effect over several days)
bolus
the small bubble of drug and vehicle that is injected into the body
subcutaneous (s.c. or sub-q)
drug is injected to form a bolus just under the skin or cutaneous tissue (eg. arm, thigh)
intramuscular (i.m.)
needle is inserted into a muscle and a bolus is left there (eg. deltoid, gluteus maximus); usually absorbed through the muscle’s capillaries within about an hour
intraperitoneal (i.p.)
needle inserted directly into the peritoneal cavity
peritoneum
sack containing the visceral organs (eg. intestines, liver and spleen)
intravenous (i.v.)
needle is inserted into a vein and the drug is injected directly into the bloodstream (very quick distribution)
other parenteral routes (3)
(1) intrathecal (nervous system via space between the base of skull and first vertebra), (2) intracerebroventricular (brain’s ventricles) and (3) intracerebral (brain tissue)
cannula
like a catheter, except a rigid tube that is often attached to the animal’s skull using dental cement and can remain permanently implanted
absorption is NOT necessary in what type of parenteral route?
intravenous (i.v.)
which parenteral site absorbs the fastest?
intraperitoneal (i.p.)
which parenteral site absorbs the slowest?
subcutaneous (s.c)
which factors can speed up absorption from i.m. and s.c. sites?
heat and exercise (increases blood flow to skin and muscle)
which substances CANNOT move in and out of capillaries?
RBCs and large protein molecules
diffusion
the process by which a substance tends to move from an area of high concentration to an area of low concentration until the concentrations are equal in both areas
why is absorption faster from i.m. sites than s.c. sites?
muscles need oxygen so there is a richer capillary supply than the skin
how many litres of blood are in the body and how fast does the heart pump them?
about 6L; all 6 are pumped in about a minute
depot injections
the drug is dissolved in a high concentration in a viscous oil (often sesame) which is then injected into a muscle (usually the buttock); slowly diffuses over a long period of time (up to 4 weeks)
intranasal administration (insufflation)
sniffing/ snorting drugs
per oral/ per os (p.o.)
drugs absorbed into the body through the digestive system by swallowing
intrarectal administration
suppositories inserted into the rectum
olive oil partition coefficient
equal amounts olive oil and water are placed in a beaker and a fixed amount of drug is mixed in; later the oil and water are separated and the amount of drug dissolved in each is measured
when a molecule of a drug carries an electric charge (ion) it ____ it’s ability to dissolve in lipids
loses
percentage of ionized molecules in a solution is determined by what? (3)
(1) whether the drugs is a weak acid or a weak base, (2) whether it’s an acid or a base and (3) its pKa
pKa
pH at which half of the molecules are ionized
transdermal administration
absorbed through the skin
drugs must be _____ soluble for transdermal administration
lipid
highly lipid-soluble drugs tend to concentrate in ____ ___ outside the ___
body fat; CNS
when a drug is dissolved in fat it is, in effect, ____
inactive
because of ion trapping, drugs that are weak bases will be concentrated in the fluid on the side of a membrane that is more ___
acidic
difference is pH is logarithmically related to ______ difference
concentration
a pH difference of 3.0 across a membrane will create what size difference in concentration?
1000
blood-brain barrier
a special barrier of cells wrapped around capillaries and blocking pores separates blood and the brain (CNS); a solid lipid barrier
what are two examples of brain areas with weak/incomplete blood-brain barriers?
area postrema of the medulla oblongata (vomit response to toxins in the blood); subfornical organ (hormone level detecting)
passive transport mechanism
large protein molecules create channels that allow non-lipid-soluble molecules to pass through in response to diffusion; or carrier protein
active transport mechanism
works against normal diffusion by concentrating a substance on one side of a membrane; requires energy and only takes place in living membranes (eg. ion pump)
protein binding
drugs may attach to a protein that is too large to diffuse out of the capillary pores; remains attached until metabolized or never get to action site; may act like depot injections
placental barrier
similar to the blood-brain barrier
drug concentration in the blood of a fetus usually reaches ___-___% of that of the mother within ____ of administration
75-100%; 5 minutes
what is the dynamic duo of excretion?
(1) kidneys and (2) liver
liver function
comparable to that of a chemical factory; molecules are modified to form useful substances and toxic molecules are made less harmful and ready to be filtered out by kidneys
enzymes
catalyst; substance that controls a certain chemical reaction
metabolism
process of restructuring molecules
products of metabolism are ____
metabolites
in terms of drugs, metabolic processes are sometimes called _____
detoxification
does detoxification always lead to less harmful metabolites?
no; example is THC (causes prolonged action)
are metabolites usually more likely or less likely to ionize?
more likely
why is it important that metabolites often ionize?
ionized molecules cannot be reabsorbed by through the nephron wall, meaning it is easier to excrete them
first-pass metabolism
when drugs are absorbed from the digestive system and pass through the liver before going anywhere in the body; subject to a certain amount of metabolism by liver enzymes before reaching target site; can also experience some metabolism in the stomach and intestines before absorption (eg. alcohol)
primary function of kidneys
maintain correct water/salt balance in body fluids
the kidney acts as a ____
filter
what is the functional unit of the kidney?
nephron
Bowman’s capsule
one end of the nephron; contains a clump of capillaries called the glomerulus
glomerulus
clump of capillaries inside Bowman’s capsule
collecting tube
back end of the nephron which empties into the ureters/ urinary bladder
what passes through the pores in the capillaries of the glomerulus?
most things except RBCs, WBCs and large proteins
what passes through the pores in the capillaries of the glomerulus (out of the blood and into the nephron)?
most things except RBCs, WBCs and large proteins
the kidney does not filter out impurities, it _____
filters everything out and then selective reabsorbs what is required
mechanisms of kidney reabsorption (3)
(1) diffusion, (2) lipid solubility and (3) active/passive transport
pH of urine
6.0
pH of blood
7.5
at low concentrations, the rate of metabolism will be ___
lower
half-life of a drug
rate of excretion; time taken for the body to eliminate half of a given blood level of a drug
first order kinetics
when the elimination of a drug changes with concentration
what is an important example of a drug that CANOOT be described in terms of a half-life (has zero order kinetics)?
alcohol
the excretion curve for alcohol is a ____ line
straight
what is the general rate of alcohol excretion?
15mg of alcohol/ 100 ml blood/ hour
zero order kinetics
when the rate of elimination of a drug is a straight line