Pharmacology and Pharmakinetics Flashcards
define neuropharmacology
study of actions of drugs on the CNS and their following effects on human behavior
match the definition to the term
widespread alternations in physiology resulting from drug actions
drug effects
match the definition to the term
molecular changes resulting from the drug binding to a receptor
drug actions
if someone takes aspirin for a heart attack, and it also relieves a headache -> which is the therapeutic and which is the side effect
therapeutic -> get rid of heart attack symptoms
side effects -> relief of headache
if someone takes an antidepressant to decrease depression symptoms but gets nausea everytime, what kind effect is nausea
adverse effect
what is the abbreviated chemical name for benadryl
diphenhydramine
what are the 3 functions of benadryl
antihistamine, decongestant and mild sedative
what is the therapeutic effect of benadryl as an antihistamine/decongestant
it drys out the mucous membranes
define specific effects
a result from biochemical interactions between drug and target receptor
define nonspecific effects
a byproduct result -> may happen as a result of an individual’s state
placebo effect is influenced by what two things
expectancy and conditioning
match the definition with the term
drug effect without any drug action
placebo effect
explain the experiment on ulcer patients given a placebo
group A -> given placebo by physician who said medication would give relief -> 70% efficacy
group B -> given placebo by a nurse who said medication would give relief -> only 25% efficacy
define pharmacokinetics
factors that influence the bioavailability and efficacy of drugs in the body
what is the acronym learned in class for the principal components of the drug
ADME -> absorption, distribution, metabolism, excretion
provide 3 examples of routes of administration
oral, inhalation and intravenous
what is the number 1 fastest route of administration of a drug
intravenous
what is the second fastest route of administration of a drug
inhalation
how is inhalation fast
it does not need metabolism so it does not have to go through the liver -> straight from lungs to brain
what is a disadvantage of intravenous administration
overdose danger and cannot be readily reversed
what is the most convenient form of administration
oral
what are the most direct ways of administration to access the CNS
epidural, intercranial, intracerebroventricular or intracisternal
what is the first pass effect in oral administration
blood flow from stomach goes directly to the liver for detox
define drug absorption
movement of drug from the site of administration to the circulatory system
what is drug absorption affected by
drug concentration, breakdown, solubility and ionization
true or false - drug absorption is dependent on active transport
false - passive diffusion
What are the three intrinsic properties of the drug when it comes to factors affecting absorption?
polarity, solubility and pKa
True or False: the intestines are the site of most (oral) drug absorption, have a larger surface area and are faster at absorption than the stomach.
true
Where is the drug concentration highest in and of which 4 organs?
tissues with the greatest blood flow
heart, liver, brain, and kidneys
what capillaries are highly porous allowing ready distribution of drugs (lipophilic or hydrophilic) into tissues?
peripheral
which drugs does the BBB permit for passive diffusion?
lipophilic drugs
passage of solutes through the BBB often occurs at?
specific transporters (e.g. glucose and amino acids)
True or False: some drugs are actively removed from the ICF (intracellular fluids) by efflux transporters.
false, they are actively removed from the ECF (extracellular fluids)
What 2 sites have direct access to the circulatory system and what are their functions?
- chemoreceptor trigger zone (CTZ) of the medulla, allows direct detection of toxins in the blood
- hypothalamus, allows direct access to capillaries for secretion of neurohormones and hormone-releasing factors
what is the similar barrier to the BBB that is unique to pregnant mammals?
placental barrier
What is the definition of depot binding and what are the 3 sites?
drug depots are inactive drug-binding sites with no measurable biological effects
the 3 sites are: adipose tissue, muscle tissue, albumin
What are the advantages of depot binding?
decreases circulating drug concentration and prolongs drug action-> can act as a reservoir for drug release and protects stored drug from metabolism
Short answer: give 2 examples of the effect of depot binding on therapuetic outcome
- Bound drug is not metabolized -> drugs remains in the body for prolonged action
- Rapid binding to depots before reaching target tissue-> slower onsets and reduced effects
which organ is primarily responsible for metabolism?
liver
what does the cytochrome P450 family do?
oxidize majority of psychoactive drugs (opioids, antidepressents, amphetamines, nicotine)
True or False: metabolism is a non-specific detoxification process that occurs in two distinct types or phases.
true
What are the two non-specific types?
type I- non synthetic modification, oxidation, reduction, hydrolysis
type II- synthetic modification, conjugation with glucronide, sulfate, or methyl groups
what organ does most excretion occur in?
kidneys
Fill in the blank: Type 1 metabolism during first pass can produce___ metabolites of the pharmaceutical preparation of drugs.
active
True or false: metabolic products are returned to circulation from the liver and can reach target sites of action or sites for excretion.
true
What are the four influencing factors of metabolism?
enzyme induction, enzyme inhibition, drug competition, individual differences
which one of the four factors influencing metabolism is responsible for a decrease in enzyme activity?
a. Individual differences
b. Drug competition
c. Enzyme inhibition
d. Enzyme induction
C: enzyme inhibition
what is the primary means of excretion?
filtration
what are most drugs excreted by?
first-order kinetics
what is exponential elimination?
constant fraction removed in a given time
True or false: most drugs are removed by zero-order kinetics
false, only a few drugs are because it is at a constant rate
by what hour will you see 98% of the drug removed from your body?
hour 6
describe the effectiveness of each of these routes of administration
IV, IM, SC and oral
IV -> maximum effectiveness but leaves the body the quickest
IM -> once it reaches the blood, it is quick to leave
SC -> takes longer to enter the blood but lasts longer
oral -> less of the drug concentration in the blood
true or false - blood is more like water than oil
true
what happens when the drug is injected into oil
drug will last longer because our body is not able to metabolize it as fast
true or false - oral administration is highly invasive
false - delivery to CSF is more
what are the 3 traits of polar molecules
water soluble, hydrophilic, lipophobic
what are the 3 traits of non polar molecules
lipid soluble, hydrophobic and lipophilic
non polar molecules freely diffuse across ….
semi permeable membranes
what are examples of semi permeable membranes
intestinal wall and BBB
true or false - many orally administered drugs are strong acids or bases
false - weak acids or bases
why do drugs alternate between ionized and non ionized forms
-> causes them to cross the BBB more slowly and makes the drug last longer -> prolonged effects and maximum concentration
what happens to aspirin in the stomach with a pH of 2
it is uncharged and readily diffuses across cell membranes
