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Pharmacokinetics Flashcards

1
Q

What are the 3 major routes of drug administration?

A

Enteral
Parenteral
Topical

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2
Q

What are the 3 delivery methods of Enteral administration?

A
  • Oral
  • Sublingual
  • Buccal
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3
Q

What is a chemical envelope that protects the drug from stomach acid, delivering it instead to the less acidic intestine, where the coating dissolves and releases the drug?

A

Enteric-coated preparations

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4
Q

What kind of drugs is enteric-coating useful for?

A

Acid-unstable drugs

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5
Q

What medications have special coatings or ingredients that control the drug release, thereby allowing for slower absorption and a prolonged duration of action?

A

Extended-release medications

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6
Q

What kind of drugs is parenteral administration used for?

A

poorly absorbed drugs
drugs that are unstable in the GI tract
unable to take oral medications

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7
Q

True or False: Parenteral administration has the highest bioavailability

A

True

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8
Q

What are the three major Parenteral routes?

A
  • Intravascular
  • Intramuscular
  • Subcutaneous
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9
Q

What kind of route is effective for respiratory disorders (such as asthma and COPD), because the drug is delivered directly to the site of action, thereby minimizing systemic side effects?

A

Oral inhalation

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10
Q

How is intrathecal/intraventricular route administered?

A

directly into the CSF

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11
Q

How is transdermal route administered?

A

application of drugs to the skin

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12
Q

What advantage does the rectal route have on other routes?

A

preventing destruction of the drug in the GI environment.

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13
Q

What is the term known as the transfer of a drug from the site of administration to the bloodstream?

A

Absorption

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14
Q

What does the rate and extent of absorption depend on?

A
  • environment where the drug is absorbed
  • chemical characteristics of the drug
  • route of administration
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15
Q

Which type of mechanism of absorption do drugs mostly use?

A

Passive diffusion

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16
Q

Which mechanism of absorption is used to transport drugs of exceptionally large size across the cell membrane?

A

Endo/Exocytosis

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17
Q

Which mechanism of absorption is Vitamin B12 used with?

Neurotransmitters such as NE?

A

Vitamin B12: Endocytosis

Norepinephrine: Exocytosis

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18
Q

True or False: A drug passes through membranes more readily if it is uncharged.

A

True

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19
Q

True or False: the lower the pKa, the more acidic the drug is.

A

True

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20
Q

What is the transmembrane transporter protein responsible for transporting various molecules, including drugs, across cell membranes

A

P-Glycoprotein

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21
Q

What is known as the rate and extent to which an administered drug reaches the systemic circulation?

A

Bioavailability

22
Q

How do you determine the bioavailability of a drug?

A

By comparing plasma levels of a drug after a particular route of administration

23
Q

What is known as the extent of absorption of the drug?

A

area under the curve (AUC)

24
Q

True or False: oral administered drugs undergo first-pass metabolism.

25
Q

What is the process called if a drug is rapidly metabolized in the liver or gut wall during its initial passage, and the amount of unchanged drug entering the systemic circulation is decreased

A

First-Pass metabolism

26
Q

What is it called when 2 drugs show comparable bioavailability and similar times to achieve peak blood concentrations?

A

Bioequivalence

27
Q

What is it called when 2 drugs have the same dosage form, contain the same active ingredient, and use the same route of administration) with similar clinical and safety profiles?

A

Therapeutic equivalence

28
Q

What is it when a drug reversibly leaves the bloodstream and enters the interstitium (extracellular fluid) and the tissues?

A

Drug distribution

29
Q

What do hydrophilic drugs need to pass through in order to penetrate cell membranes?

A

slit junctions

30
Q

True or False: Volume distribution is a useful pharmacokinetic parameter for calculating the loading dose of a drug

31
Q

True or False: an increased volume distribution, increases half-life and extends the duration of action of the drug

32
Q

What system does Phase I reactions utilize?

A

Cytochrome P450 system

33
Q

What is it called when the rate of elimination is proportional to the concentration of free drug?

A

First Order Kinetics

34
Q

What is it called when rate of elimination remains constant and is independent of the drug concentration?

A

Zero Order Kinetics (can lead to toxicity)

35
Q

Is the Half-Life constant or dependent on drug concentration with First-Order Kinetics? Zero-Order Kinetics?

A

First Order Half-Life: Constant

Zero Order Half-Life: Dependent

36
Q

Which CYP has been shown to exhibit genetic polymorphism?

37
Q

What results in increased biotransformation of drugs and can lead to significant decreases in plasma concentrations of drugs metabolized by these CYP isozymes, with concurrent loss of pharmacologic effect

38
Q

Which CYP is the inducer St. John’s wort?

39
Q

What is the most common form of inhibition?

A

competition of the same isoenzyme

40
Q

What is the most common and the most important conjugation reaction?

A

Glucurinidation

41
Q

True or False: Drugs must be sufficiently polar to be eliminated from the body

42
Q

What are the 3 processes in which drugs can be eliminated from the kidney?

A

1) Glomerular filtration
2) Proximal Tubular secretion
3) Distal Tubular reabsorption

43
Q

What is the process called that takes place with Distal Tubular reabsorption when weak acids can be eliminated by alkalinization of the urine, whereas elimination of weak bases may be increased by acidification of the urine?

A

Ion trapping

44
Q

What is the major organ of elimination?

45
Q

True or False: The steady-state plasma concentration (Css) is directly proportional to the infusion rate.

46
Q

True or False: the steady state plasma concentration (Css) is inversely proportional to the clearance of the drug

47
Q

How long does it take for a drug to reach steady-state?

A

4-5 half-lives

48
Q

What is the sole determinant of the rate that a drug achieves steady state?

A

The half-life

49
Q

What is it called when you want to maintain the Css of a drug within the therapeutic window?

A

Maintenance Dose

50
Q

What 3 factors determine the Maintenance Dose?

A

Target plasma concentration
Clearance
Bioavailability

51
Q

What is it called when you need to achieve the desired plasma level rapidly, followed by a maintenance dose to maintain the steady state?

A

Loading Dose

52
Q

Is a loading dose most useful for drugs that have a relatively long or short half-life?

A

Long Half-life

Pharmacology (21 decks)

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