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NURS 572 Advanced Pharmacotherapeutics UofA Nursing > Foundations of Pharmacology > Flashcards

Foundations of Pharmacology Flashcards

1
Q

Which main transport protein helps with preventing passage to the blood-brain barrier

A

P-glycoprotein (Pgp) - efflux pump facilitating removal of drugs and toxins out of the cell.

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2
Q

What does a low partition coefficient signify about a drug’s properties?

A

The drug is hydrophilic and primarily resides in water.

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3
Q

What is the partition coefficient of a drug?

A

Concentration of unionized drug in n-octanol phase (organic phase)
DIVIDED BY
Concentration of unionized drug in water phase.

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4
Q

What term describes drugs that are soluble in water?

A

hydrophilic

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5
Q

What is the difference between pharmacokinetics and pharmacodynamics?

A

Pharmacokinetics = what the body does to the drug
Pharmacodynamics = what the drug does to the body

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6
Q

What does MTC stand for? (plasma concentration)

A

Maximum tolerated concentration

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7
Q

What does MEC stand for? (plasma concentration)

A

Minimum effective concentration

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8
Q

How is a drug’s onset of action determined?

A

measuring the time it takes for plasma drug concentrations to reach the minimum effective concentration (MEC).

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9
Q

What does the therapeutic range or window refer to?

A

The therapeutic window is the range of drug plasma concentrations that provide a therapeutic effect while limiting adverse effects and toxicity.

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10
Q

Which of the following is the formula for calculating the therapeutic index (TI)?

A

TI = TD50/ED50.
The therapeutic index (TI) is calculated by dividing the dose that produced toxicity in 50% of patients (TD50) by the dose that produced a favorable or effective response in 50% of patients (ED50).

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11
Q

How is oral systemic bioavailability calculated?

A

F = Fa X Fg X Fh

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12
Q

Fa stands for?

A

Intestinal absorption (a=absorption)

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13
Q

Fg stands for?

A

Intestinal metabolism (g=gut metabolism)

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14
Q

Fh stands for?

A

Hepatic metabolism

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15
Q

What does first-pass effect mean?

A

Hepatic enzymes metabolize a fraction of the drug before it enters systemic circulation.

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16
Q

Why do drugs absorb better in the small intestine than the stomach?

A

Drugs absorb better in the small intestine than the stomach due to its higher surface area, blood flow, and permeability.

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17
Q

Why are acidic drugs more likely to be absorbed in the stomach than basic drugs?

A

The low pH of the stomach means acids mostly exist in their unionized form. This allows them to permeate cell membranes and be absorbed.

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18
Q

What role does gastric emptying play in drug absorption?

A

Gastric emptying influences how quickly a drug is moved from the stomach to the small intestine. Slow gastric emptying, caused by factors such as high-fat food or certain medications, can delay drug absorption.

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19
Q

How do efflux transporters like P-glycoprotein (Pgp) impact systemic drug absorption?

A

Efflux transporters like Pgp can limit systemic absorption by pumping drug molecules back into the intestinal lumen, reducing the amount of drug available for absorption into the systemic circulation.

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20
Q

Which kinds of agonists bind to and activate receptors but do not elicit the same magnitude of response as endogenous agonists?

A

Partial agonists

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21
Q

Which group of enzymes is the most common for polarizing a drug for renal excretion?

A

CYP450

22
Q

How can genetic polymorphism affect CYP450 enzyme function?

A

Polymorphism, attributed to genetic variations between individuals, can increase or decrease the efficiency of CYP450 enzymes.

23
Q

What are the top three CYP450 enzymes responsible for most drug metabolism?

A
  1. CYP3A4 = 36%
  2. CYP2D6 = 19%
  3. CYP2C9 = 16%
24
Q

Which type of CYP450 enzyme activity can lead to increased serum concentration of a drug?
A. Inhibitors
B. Reducers
C. Enhancers
D. Inducers

A

A. Inhibitors.

Inhibitors of CYP450 enzymes may decrease their metabolic activity. This can lead to increased serum drug concentrations.

25
Q

What effect does grapefruit have on CYP450 enzymes?

A

Inhibitors of CYP450 enzymes.

26
Q

Which medication will increase digoxin levels because of P-gp inhibition?

A

Amiodarone

27
Q

Which medication would cause toxicity of methotrexate because of efflux transporter inhibition?

A

Naproxen

28
Q

What over-the-counter medications can reduce iron absorption and HIV medication effectiveness?

A

Antacids

29
Q

What causes Nitroglycerine to become lethal?

A

PDE5 medications for erectile dysfunction.

30
Q

Which medications can induce serotonin syndrome when taking SSRIs?
1. antibiotic
2. analgesic.

A

Antibiotics = linezolid & tedizolid
Analgesic - Tramadol

31
Q

Which medication would interact with Tamoxifen (estrogen-receptor sensitive breast cancer tx)?

A

Paroxetine or fluoxetine (SSRIs)

32
Q

Which 3 common medications inhibit CYP2C9 and increase bleeding risk with Warfarin?

A

Amiodarone, Fluconazole, Metronidazole

33
Q

Which class of medication inhibits activation of clopidogrel?

A

PPIs like Prilosec

34
Q

Which class of medications interferes with statin medication metabolism thru CYP3A4?

A

HIV meds (protease inhibitors) Saquinavir

35
Q

What type of drug elimination is INDEPENDENT of the drug concentration? i.e. Aspirin

A

Zero-order Kinetics (the same amount of drug is eliminated per hour no matter how much drug is in the body)

36
Q

Which type of drug elimination is DEPENDENT on the drug concentration? i.e. Vancomycin

A

First-order Kinetics (the more drug in the body, the more is eliminated per hour)

37
Q

Which statement about drug absorption through the stomach is true?
A. Nutrients can induce metabolic processes but not inhibit these processes and therefore rarely affect the bioavailability of a drug.
B. Changes in pH from antacids can reduce absorption of folic acid, iron, and vitamin B12, which can cause different types of metabolic symptoms and diseases.
C. Foods and nutrients cannot create adverse reactions to a drug. This can happen only with drug interactions and allergies to the drug.
D. Vitamins are not nutrients and therefore are not considered when discussing nutrient intake.

A

B. When the stomach becomes less acidic due to foods or antacids, the absorption of folic acid, iron, and vitamin B12 can be reduced.

38
Q

Which statement is true about the CYP 450 enzymes?

A. They are highly homogenous genetically and work in roughly the same way to metabolize drugs in the body.
B. They have a high genetic variability and are the most important of the phase I metabolizing enzymes.
C. They are found only in the liver and therefore the liver is solely responsible for drug biotransformation.
D. They are responsible for the amount of drug that is bioavailable at any given time and are regulated by the bone marrow and adrenal glands.

A

B. There are differences in metabolism based on genetic variations and therefore genetics can affect the ability of the phase I metabolism.

39
Q

The patient is taking warfarin, a drug that is highly protein-bound. The patient is involved in an accident that results in loss of blood and a low albumin level. Which consideration would be appropriate regarding the patient’s warfarin?

A. Consider increasing the warfarin dose to maintain effective concentration.
correct
B. Consider decreasing the warfarin to balance the expected increase in free drugs.
C. Consider adding a diuretic to increase excretion of free drugs.
D. Consider adding a drug that will decrease the half-life of the warfarin.

A

B. Once the warfarin has less protein to bind to based on low albumin levels, it will be more bioavailable; therefore, the warfarin dose should be decreased.

40
Q

How do antagonist drugs work on the cell?
A. Antagonists produce no direct response. They occupy a receptor site to prevent other molecules from occupying the site, which thereby produces a response.
B. Antagonists cause the cell to create an irritant on the cell membrane that allows the drug to get into the cell and cause a response.
C. An antagonist binds with a drug molecule to guide it away from the cellular receptor.
D. Antagonist drugs reduce the enzyme activity of the agonist drug so that it is less potent.

A

A. Antagonists produce no direct response. They simply stop the receptor site from being occupied by other molecules. This means that the antagonists have affinity but no efficacy.

41
Q

The APN prescribes a drug that has a high protein-binding affinity. Which statement about this drug is true?
A. The drug will have a large volume of distribution.
B. Protein binding is an irreversible process.
C. Only the unbound portion of the drug will be therapeutically active.
D. Gastric pH determines protein binding.

A

C. The amount of drug bound to protein in the bloodstream is not bioavailable and cannot be used by the body.

42
Q

Which foods can inhibit drug metabolism due to the CYP3A4 enzyme that decreases first-pass metabolism in drugs?

A

Grapefruit. These juices cause the CYP3A4 enzyme to inhibit metabolism of the drugs mentioned and therefore could increase the amount of drug in the body, which could create an ADR or toxic situation.

43
Q

Why do bisphosphonates (osteoporosis drug) need to be taken on an empty stomach with a full glass of water?

A

Calcium in any form is difficult for the body to absorb, and putting the bisphosphonate in an acidic environment further decreases its ability to be absorbed.

44
Q

What are the elements of the Mneumonic, “I Can PresCribE A Drug?

A

I-Indication
C-Contraindications
P-Precautions
C-Cost/Compliance
E-Efficacy
A-Adverse effects
D-Dose/Duration/Direction

45
Q

Why does a polymorphism in the CYP2D6 enzyme cause lack of efficacy of Percocet.

A

Because codeine is a prodrug, if the polymorphism in the CYP2D6 enzyme is unable to convert this drug to morphine, it will not be beneficial in pain reduction in this patient.

46
Q

What does Phase 1 of a drug trial look at?

A

Phase I looks at how the drug is tolerated at different doses.

47
Q

What does Phase 2 of a drug trial look at?

A

Phase II looks at how effective the drug is in those people who have the disease the drug is intended for.

48
Q

What does Phase 3 of a drug trial look at?

A

Phase III looks at safety of the drug in patients.

49
Q

Is there a Phase 4 of drug trials?

A

No

50
Q

What are the most common ADEs for Cannabis use?

A

vertigo (52%), drowsiness (52%), dry mouth (36%), ataxia (14%), euphoria (11%), sleep disturbance (11%), dysphoria (9%), and headache (6%).

51
Q
A

NURS 572 Advanced Pharmacotherapeutics UofA Nursing (19 decks)

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