PharmacoTherapeutics. Exam 1 Flashcards

1
Q

What are three factors that influence drug effects?

A
  1. Pharmacokinetic differences
  2. Pharmacodynamic differences
  3. Secondary Factors
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2
Q

A _______ difference exists if a drug is given at a specific dose but reaches a difference concentration in different people.

A

pharmacokinetic

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3
Q

A ________ difference exists if a drug present at a given concentration produces difference responses in different people.

A

pharmacodynamic

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4
Q

________ is a very important concept in pharmacokinetics that determines dosage differences within a specific drug that will produce either a therapeutic effect or a toxic side effect.

A

Therapeutic Index

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5
Q

What is more dangerous, a low TI or a high TI?

A

a low TI is dangerous (there is only a slight difference between the dosage that has effect and the dosage that is deadly)

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6
Q

True or False: Both pharmacokinetic and pharmacodynamic differences exist in children.

A

True.

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7
Q

In general, dosing in children is based on ______ because complexities and uncertainties make prediction difficult.

A

clinical data

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8
Q

True or False: Geriatric patients tend to be hyporeactive to drugs.

A

False. More often they are hyper-reactive

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9
Q

Dosage for women tends to be _____, but much data is missing to base dose on sex alone.

A

lower

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10
Q

What is a drug induced arrhythemia?

A

an alteration in cardiac rhythm due to influence on the conduction system or physiological changes

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11
Q

True or False: In lactating women, drugs may be excreted through breast milk.

A

True

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12
Q

What are four environmental factors that can have influences on drug effects?

A
  1. Temperature
  2. Sunlight
  3. Altitude
  4. Diet
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13
Q

Nitrous oxide is _____ effective at high altitude.

A

less

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14
Q

True or False: Eating cheese or drinking red wine with antidepressant medications could cause a hypertensive crisis.

A

True

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15
Q

How could cheese or red wine cause hypertensive crisis?

A

If taking antidepressants, the MAO enzymes are blocked from breaking down norepinephrine and serotonin. Tyramines in cheese/wine release norepinephrine which is not metabolized as it should be.

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16
Q

_______ is responsible for metabolism of 60% of all drugs.

A

CYP3A4

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17
Q

How does grapefruit juice effect drug metabolism?

A

Grapefruit juice reduces the expression of CYP3A4

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18
Q

The ________ has a significant effect on metabolism of drugs and changes the pharmacokinetics of a drug when the patient is taking antibiotics.

A

bacteria in the gut

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19
Q

_______ is a decreased responsiveness to drug upon repeated or continuous administration.

A

Tolerance

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20
Q

What effect does pharmacokinetic tolerance have on the drug?

A

the effective drug concentration is diminished

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21
Q

In pharmacodynamic tolerance, the _____ is diminished.

A

response

kinetic = concentration, dynamic = response

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22
Q

Tachyphylaxis is a _____ loss of response after repeated drug administration in short intervals. For example, it may occur with ______ because norepi. stores are depleted.

A

rapid

tyramine

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23
Q

What are two mechanisms of pharmacodynamic tolerance?

A
  1. Down regulation of receptors

2. impairment in signal transduction

24
Q

Drugs can induce changes in ________ such as the over-expression of proteins that pump drugs out of cells.

A

cellular distribution

25
Q

What are extension effects?

A

adverse drug effects in which the drug does too much of what you expected it to do. For example, Warfarin = inhibits clotting…extension = hemorrhaging

26
Q

When you see side effects from an overdose, the drug is acting at _______ targets.

A

Unintended

27
Q

What are idiosyncratic reactions?

A

effects that occur rarely and unpredictably among the population; unusual metabolism, distribution, binding affinity for receptor

28
Q

What drug interaction account for 10% of all adverse effects?

A
drug allergies
(IgE = immediate reaction, IgG = cytotoxic)
29
Q

Drugs taken orally are ____ allergenic; Drugs taken topically are _____ allergenic.

A

less

more

30
Q

What is a pseudo-allergy?

A

a reaction produced by the direct release of mediators from mast cells and basophils that shows a downstream effect that mimics that of an allergy

31
Q

True or False: Drugs can cause cancer.

A

True

32
Q

How many categories exist for the labeling of drugs based on fetal risk?

A

five: A, B, C, D, X

33
Q

Sodium Fluoride is labeled as drug class ____.

A

A

34
Q

If the potential risk of a drug to a fetus clearly outweighs the potential benefit, the drug is labeled as class ____.

A

X (ex. warfarin, estradiol)

35
Q

What is pharmacogenetics?

A

field of study that attempts to understand the genetic basis for differences in how patients respond to drugs

36
Q

By using pharmacogenomics, patients can be _______ for a drug in order to identify who will benefit and who will suffer adverse effects.

A

pre-screened

37
Q

What is a monogenic phenotype?

A

variation in a single gene

38
Q

What is a polygenic phenotype?

A

variation in multiple genes that complicates its predictive value

39
Q

Pharmacokinetic (concentration) variations usually result from differences in ________ and are ________ understood.

A
metabolism
better understood (many examples)
40
Q

Pharmacodynamic (response) variations usually result from differences in _______ or ______ and are not well understood (few examples).

A

targets

downstream elements

41
Q

Polymorphisms of drug-metabolizing enzymes can effect ______.

A
plasma concentration
(homozygote wild type vs homozygote variant)
42
Q

Phase II conjugation by N-acetyltransferase effects drug metabolism by acting on drugs that contain aromatic _____, _______, and hydroxylamines. Slow acetylator phenotype is most common in which population?

A

amines
alcohols
Egyptian (85%)

43
Q

True or False: Some consequences of slow acetylation include neurophathy, systemic lupus, and cancer predisposition.

A

True

44
Q

Oxidation of many drugs occurs through which enzyme?

A

Cytochrome P450 enzymes (many alleles)

45
Q

Which four alleles of Cytochrome P450 are most important?

A

CYP3A4
CYP2D6
CYP2C9
CYP2C19

46
Q

What does CYP2D6 do?

A

about 25% of drugs are metabolized by this particular allele of CYP.
it removes methyl groups from oxygen*

47
Q

_______ is a muscarinic agonist that is used to treat dry mouth and is metabolized by CYP2D6. Poor metabolizers of CYP2D6 could experience nausea and vomiting because of _____poisoning.

A

Cevimeline

muscarinic

48
Q

Why would poor metabolizers have generally poorer outcomes when treated for breast cancer with tamoxifen?

A

Tamoxifen is the prodrug for the active form (Endoxifen). CYP2D6 is required to create the functional antagonist to estrogen.

49
Q

Codeine is an _______ that is converted to morphine by CYP2D6.

A

Opioid Agonist

50
Q

For 10% of the population, codeine is ineffective as an analgesic. Why?

A

poor metabolizers cannot convert codeine to morphine

51
Q

Ultra metabolizers of CYP2D6 experience ______ in response to codeine.

A

severe abdominal pain

52
Q

CYP2C9 poor metabolizers may have serious _______ complications with drugs such as Warfarin.

A

bleeding

53
Q

Succinylcholine is a muscle relaxant that can induce prolonged _____ in poor metabolizers.

A

apnea

54
Q

The ________ receptor mediates calcium-mediated calcium release from the sarcoplasmic reticulum in muscle and a mutant allele for this receptor could cause _________.

A

Ryanodine

malignant hyperthermia

55
Q

Malignant Hyperthermia (ryanodine receptor) is an example of a ________ polymorphism in drug targets.

A

pharmacodynamic (response from target is different not the metabolism)