Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
139 Cards in this Set
- Front
- Back
multiple |
every drug has _____ effects |
|
amount taken (dose-response effect) |
the effects of a drug depend on_____ |
|
individuals history and expectation |
the effects of a drug depends on an individual's _______ and _______ of the drug taking experience |
|
site of action |
the place in the body where the drug acts to produce its effect |
|
1. route of admin 2. amount admin 3. extent and rate of absorbtion 4. distribution in the body 5. binding or deposition in tissues 6. biotransformation rate 7. excretion rate |
relevant factors for achieving an adequate conc in the SOA |
|
1. molecular size and shape 2. solubility at site of absorbtion 3. degree of ionization 4. relative lipid solub of ionized and non-ionized forms |
drug characteristics that influence absorption at the site of admin |
|
enteral |
route of drug admin that includes oral, rectal, sublingual |
|
liver |
drugs administered by the enteral route reach the ______ before going into general circulation |
|
rectal route |
route is useful when oral ingestion is precluded by vomiting or when patient is unconscious -absorption is irregular and incomplete however |
|
microbes |
affects how your brain will get drugs to the SOA, contribute more genes to human survival than human genes |
|
gut microbiota |
bidirectional communication between ______ and components of the gut brain axis influence normal homeostasis and contribute to the risk of disease -depressed people more at risk for health issues |
|
siblingual |
this route does not go through the liver first -drain out of mucus and go right intoc the vena cava into the heart and then to the brain quickly |
|
acidic, basic |
in the stomach ____ drugs are absorbed and _____ drugs accumulate |
|
basic, acidic |
in the intestine which is only slightly acidic, ____ drugs are better absorbed than acidic drugs |
|
nonioniozed |
______ drug are better at getting through the membranes |
|
fats |
dietary _____ can increase the absorption of fat soluble vitamins and drugs |
|
empty |
drugs are absorbed fastest and most completely when the stomach is ______ |
|
small intestine |
orally administered drugs are primarily absorbed through the _______ -anything that slows emptying of the stomach thus slows absorption of the drug |
|
temp, size of food particle and pH in stomach |
passage of drugs from the stomach is influenced by ______, ______and ________ |
|
parenteral |
route that are given other than via intestines -injection, inhalation (intravenous, subcutaneous, and intramuscular routes) |
|
safe, self-admin, economical, no needle related complications |
oral (PO) advantages |
|
slow, and highly variable absorption, subject to first-pass metabolism, less predictable blood levels |
oral (PO) disadvantages |
|
most rapid, most accurate blood conc |
intravenous (IV) pros |
|
overdose danger, cannot readily be reversed, requires sterile needles and medical technique |
intravenous (IV) cons |
|
slow and even absorption |
intramuscular (IM) pros |
|
localized at site of injection, needs sterile equip |
intramuscular (IM) cons |
|
slow and prolonged absorption |
subcutaneous injection (SC) pros |
|
variable absorption depending on blood flow |
subcutaneous injection (SC) cons |
|
large absorption surface, very rapid onset, no injection equipment needed |
inhalation pros |
|
irritation of nasal passages, small particles inhaled may damage lungs |
inhalation cons |
|
localized action and effects, easy to self-administer |
topical pros |
|
may be absorbed into general circulation |
topical cons |
|
controlled and prolonged absorption |
transdermal pros |
|
local irritation, useful only for lipid soluble drugs |
transdermal cons |
|
bypasses blood-brain barrier, very rapid effect on CNS |
epidural pros |
|
not reversible, needs trained anesthesiologist, possible nerve damage |
epidural cons |
|
increases blood flow |
if a drug _______into its own region, it enhances its own rate of absorption -vasodilation of blood vessels and enhanced absorption |
|
cocaine |
example of a drug that contricts blood vessels and reduces its own absorption into the body -blocks Na+ channels -> causes less blood flow to the nose and he cartilage becomes necropsic and breaks down |
|
mucous and skin surfaces, inunction |
two types of topical applications and name given for application |
|
mucous membranes |
type of topical application with fast absorption |
|
skin |
few drugs can readily penetrate intact ______ -absorption usually proportional to the surface area over which they are applied and to their lipid solubility |
|
dermis |
skin layer that is freely permeable to many drugs |
|
abraded, burned, denuded |
systemic absorption occurs more readily through __________ skin |
|
inflammation |
also causes enhanced absorption |
|
hydrated |
______ skin is more permeable than dry skin |
|
oily vehicle |
suspending the drug in _______ and rubbing into skin can help (in inner forearm and thigh) |
|
lymph nodes |
these on inner surfaces can develop large lumps sometimes when suntan lotion is rubbed in |
|
brain, bone, fat |
anything that collects in _________ has to go through the blood and metabolizes most of the time and doesn't go to the site of action |
|
highest |
well vascularized areas will have the ________ concentration of the drug (brain receives 20% of blood flow to the heart) |
|
partition coefficient |
the relative affinity of a drug for either lipid or water environments -determines how fast a drug with pass out of the barriers to get to the site of action -statement of how soluble a drug is in oil v water |
|
euphoric effect |
speed of entry into the brain is the basis of its __________ |
|
size and degree of ionization |
______ and _________ of a molecule effects its entry rate into the brain |
|
ionization factor |
how easily ionized a drug is by the solution it is in (depends on the pH of the solution) |
|
pKa |
the extent of ionization of a drug is expressed as the ____ of a drug |
|
pH |
pKa is equal to the _____ of the aqueous solution in which the drug is 50% ionized |
|
acids, bases |
weak ______ ionize more readily in alkaline solutions, and weak _____ ionize more readily in acidic solutions |
|
ionized drugs |
ionized/nonionized drugs do not move around easily and cannot get to their SOA |
|
ion trapping |
when drugs and metabolites can become trapped inside or outside of membranes and cannot move across |
|
excreted with the urine |
once a drug is 'caught' outside of the blood, inside of the kidneys, it is NOT reabsorbed and will be___________ |
|
urine |
ionized drugs carry a charge and attracts water molecules which makes it bigger and prevents it from getting out of the _________ |
|
kidney compartment |
ionized drugs are transported out of the blood into the ______ where the pH can vary due to what you've eaten recently (eg orange juice) |
|
plasma membrane and blood-brain barrier |
before getting to the brain a drug must pass these two barriers -they prevent drugs from diffusing out of the bloodstream |
|
subarachnoid space |
the BBB is in this part of the brain |
|
blood brain barrier |
made up of many parts, most important may be the peculiar type of capillaries that are in the brain |
|
tight junctions, no fenestra, no pinocytosis, presence of a thick basement membrane |
characteristics of capillaries in the brain |
|
astrocytes |
these buffer pH changes in the brain, electrolyte changes etc -conduct nutrients and drugs from the blood to the neurons and transport waste away from the blood and CSF -take nutrients out of vascular system and take nutrient/drug into the neuron and is much closer to SOA |
|
astrocytic process |
this covers the basement membrane in brain capillaries |
|
carrier |
transport is ________ mediated |
|
lipophylic elements |
the BBB is composed of ________ elements |
|
lipids |
drugs solubles in ____ will enter the brain easier |
|
BBB |
selectively permeable to what it thinks you need, reduces flow of water soluble or ionized molecules -does not impede on lipid soluble or un-ionized molecules |
|
area potreme |
-place in the brain where the BBB is not intact -vomiting center/projectile vomiting -samples the presence of molecules that are toxic, metabolites of a drug that you take and to induce vomiting -small network of neurons that initiate small motor program that makes you vomit |
|
feeding centers |
no BBB on feeding centers |
|
neurotransmitters |
the BBB is not permeable to _______ -this conserves them within the nervous systems so they don't leak out -isolates brain from exogenously produces ______ systems |
|
plasma proteins |
drugs bind to __________ to help them circulate in the blood -prevents the drug from diffusing out of the blood stream -produced in healthy livers |
|
distribution |
the ______ of many drugs is slowed because they combine readily with proteins within the blood plasma |
|
synapse |
the site of action in the brain for a drug |
|
law of mass action |
the cells response to a drub is proportional to the total number of receptors occupied -more receptors stimulate/bind=more effect |
|
receptor protein |
within the synpase, the SOA is often a _______ |
|
receptors |
these live on the surface of the neuron |
|
neurotransmitters |
old_____ are discarded very quickly and only the newest and freshest _____ released first -make a lot of _____ but do not release it, it will just become desensitized |
|
agonist |
binds to receptors and produces a pharmacological action |
|
antagonist |
binds to receptors but produces no pharmacological action |
|
intracellular action |
-after drug binds to a receptor promotes synthesis or release of an intracellular regulatory molecule (second messenger)
|
|
desensitization |
following continued stimulation of receptors aka down regulation
|
|
agonist |
-this causes desensitization -to much stimulation so # receptors go down |
|
super sensitivity |
following continued blockade of receptors -upregulation |
|
antagonist |
this causes increased # receptors -not enough stim, so increase # receptors to increase stimulation |
|
maximum response |
achieved when all receptors are fully occupied |
|
dose |
amount of pharmocological effects for a given concentration |
|
potency |
determined by the affinity of drug for the receptor, as well as accessibility of drug to receptor site -only determines drug dose, does not alter maximum effectiveness |
|
maximal efficacy |
the maximal effects produced by a drug, determined by drugs inherent properties, reflected as a plateau in doe response curve |
|
undesired side effects |
efficacy can be limited by ________ that limit the amount or use of the drug, regardless of its efficacy |
|
TD(LD)50/ED50 |
therapeutic index |
|
redistribution away from the SOA |
a mechanism by which drug action is terminated |
|
metabolized in the liver and excreted by the kidneys |
most drugs are metabolized in ________ as a way to terminate drug action |
|
metabolism |
______ may take place in the plasma, kidneys, and other tissues, but most occur within the liver |
|
convert fat soluble substances into water soluble substances |
primary effect of metabolic process is to convert ____________ substances which are more easily excreted by the kidneys |
|
oxidation |
most common type of transformation in metabolism of drugs |
|
conjugation |
when drugs are are converted into a larger molecule which is water soluble |
|
cytochrome p450 |
-concentrated in the liver -oxidizes drugs -levels depend on the need for this enzyme which can be up or down regulated |
|
active |
some drugs are metabolized into more ______ substances (must be taken into account) |
|
chemical transformations |
only a few types of _________ are actually involved in spite of the enormous diversity of drug types that exist |
|
stimulating or inhibiting the oxidation system |
some drugs influence the metabolism of other drugs by _______ |
|
rapidly |
in general the more _______ a drug is metabolized, the lower the blood levels, the smaller the drug effect |
|
carcinogenic compound |
occasionally, a non-toxic drug may be metabolized by the liver into a ______ (eg hot dogs with sodium nitrite) |
|
urine, feces, expired air, sweat, and breastmilk kidney |
drugs can be excreted in ______ primary excretory pathway is the _____ |
|
rate |
the _____ at which a substances is excreted is pH dependent |
|
basic, acidic |
drugs that are _____ are excreted more rapidly when urine is acidic, where ____ drugs are excreted faster when urine is alkaline |
|
alkaline |
nicotine is excreted more slowly when the urine is _____ (bc nicotine is basic) they wil smoke less |
|
eating |
______affects urine pH ( the urine becomes more acidic 30 minutes after _____ |
|
increases |
-heavy breathing also blows of CO2 and _______ blood pH -accelerates the removal of nicotine from the brain |
|
plasma proteins, hemoglobin, and carbonic acid |
three blood pH buffers |
|
excretion rate |
given as the half life of the drug in the body the time to reduce plasma concentration by half -because if its in the blood then it can do something |
|
rebound effects |
the withdrawal of drugs that modify physiological or behavioral systems is often accompanied by changes in the opposite direction of the original compound (eg alcohol and barbiturates suppress dreaming and REM sleep and also reduce the vividness of dreams, during withdrawal, dream time and vividness of the dreams are increased |
|
age, weight, biological rhythms and personality |
4 important factors that influence responsiveness to drugs |
|
children |
often are hyperactive to drugs because of incomplete development of metabolic enzyme systems |
|
older people |
may be hyperactive to drugs because of impaired metabolic excretory mechanisms |
|
BBB |
in some young species drug responsiveness changes due to an underdeveloped __________ |
|
drugs |
at least 200,000 elderly are hospitalized every year because of _______ accidents |
|
dose |
______ must b adjusted to the weight of the drug recipient |
|
9:30 and 11:30pm |
people are more responsive to drugs during the hours of ___________ due to rhythmic variations and activity of physiological systems |
|
law of initial value |
describes the personality variables that effect responsiveness to drugs -says degree of response depends on the beginning level of excitation
|
|
law of initial action |
describes why a dose of morphine given to a patient in pain causes euphoria, but similar dose in a happy pain-free pt causes mild anxiety and fear |
|
physiological state |
this alters a drugs actions in an individual -ex, aspirin lowers temp in patients with fever but not in patients with normal temp -ex caffeine more toxic in dehydrated mice |
|
examples of genetic causes to different responsiveness to drugs |
-different strains of mice metabolize drugs at different rates -ibuprofen more effective in men than women -women metabolize morphine and anti-rejection drugs faster |
|
tolerance |
progressive requirement with chronic use for higher drug doses to produce a given effect
|
|
cross tolerance |
develops among related drugs -become tolerant of a drug we didn't take bc similar in structure to a drug we did take |
|
characteristics of tolerance |
-reversible when drug use stops -dependent on dose and frequency of drug use and drug-taking environment -may occur rapidly or never (after long use) -not all effects of a drug show the same amount of tolerance -several different mechanisms explain multiple forms of tolerance |
|
sensitization |
when responsiveness to a drug increases with repeated administrations eg marijuana, amphetamine, cocaine, barbiturates, and morphine |
|
withdrawal |
-the abstinence syndrome -set of behaviors and physiologic symptoms that occur when drug treatment is withdrawn from a person who has developed a tolerance to the drug |
|
physical dependence |
an adaptive state that manifests itself by intense physical disturbances when the administration of the drug is suspendeD |
|
pharmacodynamic tolerance |
cause for the craving of certain substances (neurochemical adjustment of brain to presence of the drug) |
|
psychological dependence |
condition in which a drug produces a feeling of satisfaction and a psychic drive that requires periodic or continuous administration of the drug to reduce pleasure or to avoid discomfort |
|
bioavailability |
refers to the efectiveness with which a drug is absorbed -all preparations that contain identical amounts of active ingredients are not equally utlized |
|
dosage regimen |
the uniform administration of drugs to maintain a steady state level of a drug that should be given at uniform intervals equal to the drug's half life |
|
placebo effect |
may have greater implications for psychotherapy than any other form of treatment because psychotherapy and _________ function primarily through psychological mechanisms -influence both SELECTIVE and OBJECTIVE measures |
|
diabetes, blood sugar levels |
what does the placebo effect NOT influence |
|
virgin mary |
devout catholics reported feeling peaceful and secure when viewing the ________ and felt less pain |