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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