Chapter 3 Flashcards by Julissa Andazola

Defining “Dose”

the effect of a drug is related to its CONCENTRATION in the body not just the total AMOUNT of the drug taken
small vs large person, weight matters

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Metric system

administer milligrams per kilogram (mg/kg)

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5mg/kg of morphine doesn’t have the same effect in mice and humans

mice metabolize drug at a different rate (faster) than humans

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Dose Response Curves

Info about a range of drug doses
x-axis = dose
y-axis = affected

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Effective Dose

min dose necessary to produce the intended drug effect in a given percentage of the population

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ED50

effective dose for 50% of the population

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Lethal Dose

min dose necessary to produce death in a given percentage of the population

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LD10

does is lethal for 10% of the population

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Therapeutic index

safety ratio

LD50/ED50 = 100/10 = 10, index is 10, thus they would have to take 10x’s the ED50 dose to have a 50% chance of dying

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Potency

absolute number of molecule of drug required to cause a response, dose required

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Efficacy

max effect obtainable, additional doses produce no more effect

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Slope

individual diff in drug response, measure of variability

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Factors that influence drug effect

route of admin, metabolism, tolerance

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Route of Admin

injection, inhalation of gases/smoke/solids, oral, rectal, and trasndermal

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Injection

under skin, subcutaneous (s.c.)
slow acting
*intramuscular (i.m.) in muscle
*intraperitoneal (i.p.) in abdominal space
*intravenous (i.v.)

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Inhalation of Gases

whippets

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Inhalation of Smoke

nicotine, cocaine (crack), methamphetamine (ice)

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Inhalation of Solids

cocaine, meth, ketamine

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Oral

aspirin, edibles, mushrooms, LSK

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Rectal

for unconscious, vomiting or unable to swallow
-alc, meth, coffee
you get drunk faster, can’t smell it, trying to finess police

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Distribution of Drugs

lipid solubility, pass through more easily, stay in lipid outside of CNS
-drugs are distributed throughout the body by blood

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Absorption

the movement of a drug from the site of admin to the blood

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Parental

veins -> heart -> lungs -> heart -> brain/body

Oral

Stomach -> liver (metabolize) -> intestines

first pass metabolism

oral admin

Tolerance

process by which repeated exposure to a drug produces a decrease in sensitivity to the drug

Dose-response curve - tolerance

when tolerance is present it is shifted to the right

3 types of tolerance

Dispositional, functional, behavioral | can be either or, or both, or all

Dispositional (Pharmacokinetic)

decrease the amount of the drug reaching the target site due to an increase in metabolism

Functional (Pharmacodynamic)

decrease in reactivity in the target site acute v protracted short v long term

Behavioral (Learned)

tolerance occurs in same environment the drug was administered, must take drug in exact same location * much lower tolerance in a new environ. * also called context specific tolerance - due to homeostasis

Characteristics of Tolerance

Tolerance is reversible; cross tolerance, selective tolerance

Reversible tolerance

decreases as you decrease use of drug

cross tolerance

exposure to one drug can produce tolerance to another drug

selective tolerance

tolerance develops to some drug effects but not to others

Reverse Tolerance

sensitization: some effects can actually increase in sensitivity -low dose is required to obtain effect shift to left in dose response curve

location of curve along the dose axis

potency

greatest attainable response

efficacy

change in response per unit dose

slope

Bioavailability

to describe the portion of the original drug dose that reaches its intended site of action

inhalation

when a drug is a gas or in small liquid droplets, an individual can breathe in the drug through the mouth

intranasal

a drug is breathed in via the nose, the drug can be absorbed through the thin mucous membranes that line the inside of the nose and the sinus cavities

sublingual

drug is placed under the tongue and dissolved in saliva,

transdermal

drug is absorbed by placing it on the skin using a patch

Drug metabolism

biochemical modification of a drug, typically via enzyme systems, into another form

Drug excretion

chemical can leave via the kidneys, lungs, bile, or skin

half-life

time that passes for the dose of drug in the body to be reduced by half

A drug that is taken sublingually is?

placed under the tongue

Which of the following drugs can be detected in urine for up to one month following chronic use?

marijuana

The faster the drug reaches the brain, ______.

the more rewarding the drug effect

Fred is applying for a job that requires preemployment drug testing. He has used one illicit drug in the past but his last use was more than a month ago. Which drug is most likely to still be detectable in a urine drug screen?

marijuana

A typical dose-effect, the ______ is plotted on the vertical axis and the ______ is plotted on the horizontal axis.

effect size, range of doses

The safety of drug is sometimes described using a thera- peutic index, which is calculated by the ratio of:

LD50/ED50

Sarah has developed an addiction to prescription pain medication and takes it all the time. When she is at work, her coworkers report to Sarah’s boss that she is slurring her speech and acting high. When Sarah is questioned by her boss, Sarah manages to pull herself together and talk clearly by talking more slowly than normal. This is an example of:

behavioral tolerance

Brandon has noticed that he really wants to smoke marijuana and he thinks about this all the time. He has not felt any illness symptoms since he stopped smoking. It is likely that Brandon exhibits ______, but not ______.

psychological dependence, physical dependence