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64 Cards in this Set

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  • Back
What is a dose response curve?
it is a curve that depicts the relationship between the dose of the drug administered (X axis) and the resulting pharmacologic effect (Y axis.)
List four descriptive characteristics of the dose response curve, by which dose response curves are characterized differently:
potency.

slope.

efficacy.

individual variability.
Describe how potency of the drug is depicted on the dose response curve?
potency is depicted by its location along the dose axis (usually the x axis.)
What effect does increased affinity of the drug for its receptor site shift the dose axis on the dose response curve?
to left.

decreased affinity shift the curve to the right.
What is the relationship seen between drug potency and receptor affinity?
they are directly related. The more potent the drug, a greater the affinity for its receptor.
What does the slope of a dose response curve revealed about the drug?
it indicates the number of receptors that must be occupied before the drug effect occurs.
What does steep dose response curve indicate about the drug?
it means that a majority of the receptors must be found before a relevant effect occurs.
How steep is the dose response curve with neuromuscular blocking drugs?

what does this indicate?
it is steep.

this indicates that a majority of receptors must be occupied before there is an effect.
Define drug efficacy:
it is a measure of the intrinsic ability of the drug to produce a given physiologic or clinical affect.

the maximal effect of the drug reflects intrinsic activity or efficacy.
Where on the dose response curve is efficacy depicted?
on the plateau.

a higher plateau correlates with greater efficacy.
Describe how the presence of competitive antagonists would alter the dose response curve:
it would shift the curve to the right, with no change in the efficacy (plateau) or slope.

the rightward shift is caused by competition for the same number of receptors.
Describe how the presence of a noncompetitive antagonists would alter the dose response curve of the drug:
it would shift the curve rightward and downward, with a decrease in the slope of the curve.

this is because the maximal effect cannot be achieved in the presence of the noncompetitive block. In other words, a noncompetitive block cannot be reversed by excess agonist.
What is LD50/ED 50?
it is the therapeutic index.

it is LD50 divided by ED 50.

TI equals LD50/ED 50.
What is LD50?
the median lethal dose of a drug.
what is ED 50?
the median effective dose of a drug.
A patient who is allergic to one drug is also allergic to another related drug. What is this phenomenon called?
cross sensitivity or cross reactivity.

patient may be cross sensitive to structurally similar drugs.
The patient is known to be allergic to penicillin. This patient is likely to have cross sensitivity to what other group of antibiotics?

why?
cephalosporins.

this is because penicillins and cephalosporins both have a beta lactam ring.
Is there cross sensitivity among ester local anesthetics?

why?
yes.

this is because they have a common metabolite, para amino benzoic acid (paba.)
Is there cross sensitivity between ester and amide local anesthetics?
no.
Can a patient with analogy to an ester local anesthetic receive an amide local anesthetic?
yes.

can a patient with an allergy to an amide local anesthetic receive an ester local anesthetic?
write an equation that shows how the volume of distribution is calculated:
Vd = Q/Cp

Vd is volume of distribution.

Q is the quantity of drug injected.

Cp is the plasma concentration of the drug that will be achieved if the drug distributed instantaneously within is volume of distribution after its injection.
What is the elimination half time of the drug?
the time it takes for the plasma concentration to decreased by one half.
What two factors determine elimination half time?
volume of distribution (directly related to halftime.)

clearance (Cl, is inversely related to halftime.
Mathematically, what does T 1/2 equal?
Vd/Cl.
A substance with what clearance (large or small) and what volume of distribution (large or small) will have the longest halftime elimination?
half time elimination is greater if volume of distribution is large and/or clearance is small.
A drug is eliminated by first order kinetics. Four grams. Five hours later, 2 g have been metabolized.

after 10 more hours, how much more is metabolized?
1.5 g.

the half life is five hours because the amount of drug decreased from 4 g to 2 g in five hours.

in the next five hours, 1 g is lost in five hours later another 0.5 g is lost.
In first order kinetics, how much of the drug is gone after one half life?
one half.
If the drug is excreted by first order kinetics, how long will it take for the plasma concentration to fall 50 mg if the half life is 20 hours and 200 mg was administered?
40 hours.

in first order kinetics, a plasma concentration decreases by one half during each half life. The concentration dropped from 200 mg to 100 mg in the first 20 hours (one half life) and from 100 mg to 50 mg in the next 20 hours.
If 60 mg of the drug is given and 15 mg remained after 12 hours, how much drug is eliminated in the next 12 hours?
11.25 mg.

the half life is six hours (decreased from 60 to 30 in six hours and from 30 to 15 in the next six hours.)

half the remaining 15 mg (7.5 mg) will be excreted in the next six hours, and then one half of 7.5 mg (3.75 mg) will be excreted in the following six hours.

thus, 7.5 mg +3.75 mg equals 11.25 mg to be excreted in the next 12 hours.
Diffusion of the drug across a membrane is proportional to the concentration gradient. Diffusion is also dependent on what three factors?
solubility of the drug in lipid.

thickness of the membrane.

molecular weight of the drug (the larger the molecular weight, the slower the rate of diffusion.)
The degree of protein binding of a drug in the blood is dependent upon what primary factor?
the total amount of protein in the blood.

the amount of drug bound to protein will change when plasma protein levels change.
What is the most important plasma protein providing of drugs ?
albumin.
Rank the following routes of administration, from greatest to least, with regards to peak plasma concentration:

subcutaneous, intravenous, caudal epidural, intrathecal:
intravenous> intrathecal> caudal epidural> subcutaneous.
Identify the most important determinant of the buildup of intravenous agent in a given tissue:
blood flow to the tissue.
Besides blood flow, what two other factors determine the amount of intravenous anesthetic going into and out of a tissue compartment?
lipid solubility and degree of ionization in plasma.
Drugs that are absorbed from the gastrointestinal tract must first pass through which organ before reaching general circulation?
the liver, via the portal circulation.
Drugs that are absorbed from the gastrointestinal tract may be metabolized to some extent by the liver before reaching the general circulation. What does this affect called?
first pass effect.
What is an acid?
a hydrogen ions or proton donor.
Why is a substance called a weak acid?
because it does not ionized 100% in solution.
Why is a substance called the strong acid?
because it ionizes 100% in solution.

example: HCl.
Why is carbonic acid considered a weak acid?
because carbonic acid ionizes only 0.2% in physiologic solution.

an acid that does not dissociate 100% to its ionized form is a weak acid.
What agents used in anesthesia are weak acids?
barbiturates.
What happens to the amount of weak acid in not ionized form as pH falls?

what is the amount ionized?
as pH decreases, the amount of weak acid in non ionized form increases.
What is the rule with weak acids in solutions when pH either increases or decreases?
plus acid equals more nonionized.

as pH decreases, or is nonionized.

if pH increases, more of the weak acid in ionized form increases.
A weak acid with a 7.8 will be more than 50% or less than 50% nonionized at pH 7.4?
more than 50%.
What happens when a weak acid is injected into an acidotic patient?
more drug is nonionized.

as pH decreases, the nonionized fraction increases.

acid plus acid equals nonionized.
How much barbiturate crosses the blood brain barrier when you give it to a patient with low pH, more or less?

explain:
more. Barbiturate is nonionized at lower pH, so greater amounts cross the blood brain barrier.
Propofol, a weak acid, has pKa of 11. His propofol mostly ionized or mostly unionized that normal physiologic pH of 7.4?

explain:
since the normal physiologic pH of 7.4 is less than the PKa 11 of propofol, the body environment is an acidic environment for the weak acid propofol.

acid plus acid equals more nonionized. Therefore, propofol but mostly nonionized at 7.4.
What agents used in anesthesia are weak basis?
all local anesthetics.

all opioids.

etomidate.

ketamine.
What happens to the amount of a weak base in ionized form as pH decreases?
it increases. Rule: base plus acid equals more ionized.
What happens to the amount of a weak base in ionized form as pH increases?
it decreases.

rule: base plus base equals more nonionized.
A weak base with a PK of 7.8 will become more than 50% or less than 50% nonionized at pH 7.4?
less than 50% nonionized.
During resuscitation, intravenous access is not or cannot be established, what route of administration can result in high peak plasma drug levels?
endotracheal.

it is almost identical to intravenous.
What happens when a weak base is administered to an acidotic patient?
less drug is nonionized.

rule, base plus acid equals more ionized.
Do drugs that are weak acids form salts with positive ions such as sodium or negative ions such as sulfate or chloride?
drugs that are weak acids form salts with positive ions (sodium, potassium, calcium, magnesium.)

sodium pentobarbital is an example of a weak acid. A drug is a weak acid if it forms a salt with a positive ion.
Do drugs that are weak bases form salts with positive ions such as sodium or negative ions such as sulfate or chloride?
drugs that are weak bases form salts with negatively charged ions (chloride, sulfate, phosphate.)
Give two examples of commonly used drugs that are weak bases:
lidocaine and morphine sulfate.
?
more than 50% ionized.

sulfate equals weak base.

the key to solving this problem is determining if you are dealing with a weak acid or a weak base.
A new drug, sodium X., has a pKa of nine. Will this drug to be more than 50% ionized, 50% ionized, or less than 50% ionized abnormal body pH of 7.4?
less than 50% ionized.

sodium x is a weak acid.
Our morphine, meperidine, fentanyl, and sufentanil more than 50% nonionized or less than 50% nonionized at pH 7.4?

explain:
they will be less than 50% nonionized.

opioids are weak bases.
are alfentanil and remifentalil more than 50% nonionized or less than 50% nonionized at pH 7.4?

explain:
there will be more than 50% nonionized at pH 7.4. Their pH's are 6.5 and 7.26, respectively.
?
more than 50% ionized.

sulfate equals weak base.

the key to solving this problem is determining if you are dealing with a weak acid or a weak base.
?
more than 50% ionized.

sulfate equals weak base.

the key to solving this problem is determining if you are dealing with a weak acid or a weak base.
A new drug, sodium X., has a pKa of nine. Will this drug to be more than 50% ionized, 50% ionized, or less than 50% ionized abnormal body pH of 7.4?
less than 50% ionized. -- sodium x is a weak acid.