Pharmacokinetics Flashcards

1
Q

Difference between PK and PD?

A

PK: what the body does to a drug
PD: what the drug does to the body

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2
Q

Components of PK

A

Absorption
Distribution
Metabolism
Excretion

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3
Q

What happens in passive distribution?

A

Movement of drugs from area of high concentration to low concentration

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4
Q

What happens in active transport?

A

Drugs are moved across the gut wall via transporter proteins - requires energy

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5
Q

Drug absorption pathway when given orally vs IV

A

Oral –> stomach –> small intestine –> hepatic portal vein –> liver –> systemic circulation

IV –> systemic circulation

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6
Q

Disintegration vs dissolution

During which is the active ingredient released?

A

Disintegration - when a drug is broken into smaller pieces

Dissolution - when a drug dissolves; this is when active ingredient is released

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7
Q

Dosage forms fastest to slowest rate of absorption

A
IV
SL
ODT
IR tablet
ER tablet
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8
Q

What is a “micronized” medication? What is the benefit?

A

Drug with very small particle diameters

Increased dissolution rates over other oral formulations of the same drug

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9
Q

What is bioavailability?

A

The extent to which a drug is absorbed into the systemic circulation

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10
Q

What is considered a high bioavailability?

A

70% or higher

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11
Q

What is considered a low bioavailability?

A

10% or lower

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12
Q

Bioavailability calculation

A

100 x (AUC extravascular/AUC intravenous) x (Dose intravenous/Dosse extravascular)

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13
Q

What is drug distribution?

A

The process by which drug molecules move from systemic circulation to the various tissues and organs of the body

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14
Q

What factors favor greater drug distribution?

A

High lipophilicity
Low molecular weight
Unionized status
Low protein binding

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15
Q

If a medication is highly protein bound, what will make it’s distribution higher?

A

Low albumin (higher percentage of drug will be unbound from albumin and able to move extravascularly)

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16
Q

Corrected calcium formula and when not to use it

A

Reported calcium + [(4-albumin) x 0.8]

Do not use if measuring free calcium

17
Q

Corrected phenytoin formula and when not to use it

A

Total phenytoin measured

(0. 2 x albumin) + 0.1

Do not use if measuring free phenytoin

18
Q

Volume of distribution equation

A

concentration of drug in plasma

19
Q

What is Volume of distribution (Vd)?

A

how large an area in the patient’s body the drug has distributed into
***theoretical value

20
Q

What does metabolism do?

A

Converts original drug form into a form that can be eliminated
Facilitates elimination

21
Q

Primary sites for drug metabolism

A

Gut and liver

High levels of enzymes

22
Q

What is first-pass metabolism - what effect does it have on drug concentration in the body?

A

Hepatic metabolism of a drug before it reaches the systemic circulation
Reduces bioavailability

23
Q

What are phase 1 and phase 2 reactions involved in in enzyme metabolism?

A

Phase 1: oxidation, reduction, hydrolysis; makes molecule more reactive and hydrophilic
Phase 2: conjugation

24
Q

What is excretion

A

irreversible removal of drugs from the body

25
Q

How to increase excretion of a weak base through the urine? Weak acid?

A

Weak base - make urine more acidic

Weak acid - make urine more basic

26
Q

Clearance equation

A

Concentration

27
Q

What is first order pharmacokinetics?

A

Where a constant PERCENTAGE of drug is removed per unit of time
Graph is a curved line

28
Q

What is zero order pharmacokinetics?

A

constant AMOUNT of drug is removed per unit of time, no matter how much drug is in the body
Graph is a straight line

29
Q

What is Michaelis-Menten Kinetics?

A

saturable, non-linear Kinetics
Max rate of metabolism is Vmax
Increase in dose leads to disproportionate increase in drug concentration at steady state
Doubling the dose may lead to more than double the serum concentration

30
Q

Elimination rate constant (ke) definition and equation

A

Fraction of drug eliminated (cleared) per unit of time
Cl
—–
Vd

31
Q

Half-life (t1/2) equation

A

ke

32
Q

How many half-lives does it take to reach steady state?

A

~5

33
Q

How to calculate loading dose

A

F