Prodigy Pharmacokinetics Flashcards

1
Q

Which is the single most important enzyme, accounting for 40-45 percent of all mediated drug metabolism?

A

CYP3A4

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2
Q

After intravenous administration of fentanyl, there is an initial rapid increase in plasma concentration of the drug followed by a rapid decline in plasma administration. This initial, rapid decline is due primarily to

A

redistribution to highly-perfused organs

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3
Q

Once injected, the plasma concentration of an opioid such as fentanyl _______

A

rises rapidly.

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4
Q

Shortly after this initial rise, the plasma concentration rapidly

A

decreases as the drug is distributed into the highly perfused organs such as the brain, liver, and kidneys. A second, slower decrease in the plasma concentration occurs as the drug distributes into the less well-perfused tissues such as the muscles and adipose tissue.

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5
Q

A protein binds to a cell membrane receptor, causing it to open and allow the passage of substances into the cell. This is an example of a

A

ligand-gated receptor

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6
Q

A ligand-gated receptor is triggered by the

A

binding of a chemical to the receptor. When this occurs, the receptor’s shape alters causing the channel to open. This allows the passage of specific substances through the channel.

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7
Q

Which drug exhibits the classic drug-drug interaction associated with serotonin syndrome when combined with MAOIs?

A

Meperidine

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8
Q

The classic drug interaction associated with serotonin syndrome is the combination of meperidine with.

A

MAOIs

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9
Q

Phenylpiperidines including (4) associated with interactions with MAOI and serotonin

A

fentanyl, methadone, and tramadol and methylene blue have also been associated.

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10
Q

The term that describes the amount of drug within the body as a whole compared to the amount of the drug in the bloodstream is the

A

The volume of distribution is a number that describes the amount of drug in the body compared to how much is actually in the bloodstream.

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11
Q

Vd: It is calculated as

A

Vd = Amount of drug in body/Plasma concentation of the drug. It actually describes an apparent volume.

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12
Q

If a large amount of a drug has been administered and only a small amount of the drug appears in the plasma, the drug is said to have a ____Vd

A

have a large volume of distribution.

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13
Q

What term refers to the dose of a drug required to produce a given effect in 50 percent of subjects

A

Potency (ED 50)

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14
Q

The only process that does not involve the cytochrome P450 pathway is

A

Hydrolysis

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15
Q

Cytochrome P450 enzymes are involved in

A

oxidation, reduction, and conjugation reactions.

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16
Q

The only metabolic pathway in which CYP 450 they are not present is

A

hydrolysis, which typically occurs outside of the liver.

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17
Q

Drugs such as(4) undergo hydrolysis.

A

remifentanil, esmolol, succinylcholine, and ester local anesthetics

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18
Q

Which of the following measurements predicts the time it takes for 50% of a drug to be eliminated from the central compartment when a continuous infusion is discontinued?

A

Context sensitive half time

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19
Q

The steady-state plasma concentration corresponds to the

A

steady concentration at the site of action and is determined by a concentration-response curve

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20
Q

Which term refers to the theoretical volume of blood from which a drug is completely and irreversibly removed in a unit of time?

A

Elimination clearance

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21
Q

The most important factor determining the rate of diffusion of a drug across a membrane is

A

Concentration gradient accross the membrane

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22
Q

What is hepatic enzyme induction?

A

If liver enzymes are exposed to particular compounds or drugs over a period of time, they will increase their activity, resulting in an increased ability to metabolize the drugs.

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23
Q

A chemical that can bind with a protein to form a new complex is a

A

Ligand

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24
Q

The primary function of phase II conjugation reactions are to make the molecule more

A

Water-soluble

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25
Q

Remifentanil exhibits a _____ volume of distribution than fentanyl due to a(n) _____ clearance.

A

smaller, increased

26
Q

Drugs such as fentanyl that are

A

highly lipophilic and exhibit low protein-binding exhibit a high volume of distribution.

27
Q

Opioids such as remifentanil and alfentanil exhibit a

A

smaller volume of distribution due to increased protein binding and a faster clearance

28
Q

Most drug metabolism is performed by microsomal enzymes in the smooth endoplasmic reticulum of the

A

Liver cells

29
Q

The vessel-poor group is comprised of bone, ligament, and cartilage, accounts for

A

20% of the body mass, and receives a negligible amount (0%) of the cardiac output.

30
Q

The vessel-poor group is comprised of

A

bone, ligament, and cartilage, accounts for

31
Q

The muscle group is comprised of muscle and skin. It accounts for______% body mass and receives ___% of the Cardiac output

A

50% of the body mass and receives 19% of the cardiac output.

32
Q

Vessel RICH GROUP It comprises ____%of the body mass but receives 75% of the cardiac output.

A

10%

33
Q

The maximum duration that a single transdermal medication patch would be effective is about____days? Why?

A

7 days; Because the skin sloughs and regenerates about every 7 days, the maximum duration for a single transdermal application is about 7 days.

34
Q

A drug is being administered by continuous infusion, and its plasma concentration is now constant. The drug is said to be in

A

Steady state

35
Q

Ideally, a medication used for a transdermal application has (weigh)

A

a molecular weight less than 1000 daltons

36
Q

Ideally, a medication used for a transdermal application has (ph and lipid solubility)

A

pH between 5-9 in an aqueous solution

37
Q

Ideally, a medication used for a transdermal application has (daily requirements)

A

less than 10 mg

38
Q

Hepatic clearance is the product of the hepatic blood flow and the drug’s

A

hepatic extraction ratio

39
Q

Which of the following is a Phase II reaction?

A

conjugation and synthesis reactions.

40
Q

Which anesthetic intervention is typically avoided in patients undergoing a large hepatic resection?

A

Epidural catheter placement

41
Q

Even if the preoperative coagulation studies were normal, patients undergoing liver resection can exhibit an

A

abnormal INR and platelet count postoperatively.The effect peaks on postop day 1 or 2 and typically resolves by about 5 days postop. Because of the alteration in coagulation studies, many practitioners avoid epidural catheter placement.

42
Q

The diffusion of a drug across a membrane from an area of higher concentration to an area of lower concentration without the expenditure of energy is

A

Passive transport

43
Q

Erythromycin administration in patients taking theophylline can lead to

A

theophylline toxicity. erythromycin can inhibit the metabolism of theophylline and potentially lead to theophylline toxicity.

44
Q

What is pharmacokinetics?

A

Pharmacokinetics, or what the body does to the drug can be remembered with the ADME mnemonic, which stands for absorption, distribution, metabolism, and excretion of the drug.

45
Q

In opioids with a small volume of distribution, the termination of the analgesic effect is primarily due to

A

Clearance of the drug

46
Q

Determining the safety margin of a drug requires that you know data about the effective dose of the drug and

A

the Lethal dose

47
Q

Select two inducers of hepatic drug metabolism.

A

Rifampin

Phenytoin

48
Q

Name some inducers of CYP450

A

carbamazepine, ethanol, glucocorticoids, phenobarbital, phenytoin, rifampin, St. John’s Wort, and tamoxifen.

49
Q

What determines the duration of action of an irreversible antagonist?

A

Receptor regeneration

50
Q

When you administer a bolus dose of a drug intravenously, which tissue would have an increase in the tissue concentration of the drug first?

A

Liver

51
Q

The plasma half-life of a drug is inversely proportional to its

A

rate of clearance

52
Q

The percent of a drug that the liver can clear as it passes through it is referred to as the

A

hepatic extraction ratio

53
Q

Which of the following terms refers to compounds that bind to receptors without producing any changes in cellular function?

A

Antagonists

54
Q

Which drug or drug class is an inhibitor of hepatic drug metabolism?

A

azole antifungal drugs, cimetidine, disulfiram, grapefruit juice, macrolide antibiotics, protease inhibitors, quinidine, SSRIs.

55
Q

One of the advantages of transdermal medication over other routes is that it

A

provides a more consistent plasma concentratio

56
Q

transdermal site A common side effect

A

can be rash or erythema at the application site.

57
Q

Hepatic enzyme induction will result in a reduction in the ____ of a drug.

A

half-life

58
Q

Which of the following medication administration routes can undergo first-pass hepatic metabolism?

A

oral / rectal

59
Q

In opioids with a high volume of distribution, the decrease in plasma concentration and termination of the analgesic effect is due primarily to

A

Redistribution

60
Q

Which Phase 1 reaction is characterized by reactions that remove electrons from a molecule?

A

Oxidation

61
Q

Select two common treatments for moderate to severe serotonin syndrome.

A

Chlorpromazine

Cyproheptadine