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Pharm > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

Define Pharmacokinetics

A

It is what the body does to the drug

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2
Q

Define Absorption

A

The movement of a drug from its site of administration into the central compartment

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3
Q

Define Distribution

A

The movement of a drug from the systemic circulation into tissues and body fluids

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4
Q

Define Metabolism

A

The transformation of a drug into a usable form

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5
Q

Define Elimination

A

The excretion of a drug from the body

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6
Q

Name the 4 Enteral routes of administration

A
  1. Oral (PO)
  2. Rectal (PR)
  3. Sublingual (SL) (under the tongue)
  4. Buccal (between the gums/inner lining of the mouth)
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7
Q

Name the 8 Parenteral routes of administration

A
  1. Intravenous (IV)
  2. Intramuscular (IM)
  3. Subcutaneous (SC)
  4. Intrathecal
  5. Intraarterial
  6. Topical
  7. Transdermal
  8. Respiratory/Pulmonary
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8
Q

What are the 8 factors that affect absorption?

A
  1. Dosage form
  2. Size
  3. pH
  4. Blood flow to site
  5. GI motility/contact time
  6. Water solubility
  7. Gut transporters
  8. Other drugs
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9
Q

What is the First-pass Effect?

A

The metabolism of a drug before it reaches the systemic circulation

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10
Q

What does the First-pass Effect change about the drug?

A

Decreases the amount of bioavailable drug

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11
Q

What does the First-pass effect apply to, and how is it measured?

A
  1. Applies to oral and rectal administration
  2. Measured by Extraction Ration (ER)
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12
Q

Define Bioavailability

A

It’s the fraction of unchanged drug that reaches the systemic circulation, after it is administered.
*IV administration is 100% bioavailable

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13
Q

What are the 4 factors that affect drug Distribution?

A
  1. Membrane permeability
  2. Tissue perfusion
  3. Protein binding
  4. Volume of Distribution
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14
Q

What are the 3 scenarios of membrane permeability?

A
  1. Drug is confined to circulation (very large drug molecules)
  2. Drug excluded by cell membranes (very polar drug molecules)
  3. Drug enriched in fat (lipophilic drugs)
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15
Q

What is Tissue Perfusion?

A

The rate of blood flow through tissues

*Certain diseases states (liver, heart, and renal failure) change cardiac output therefore changing perfusion of blood through tissues

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16
Q

What is important about protein binding?

A

Drugs bound to proteins cannot diffuse out of the plasma, they need to be free and unbound

17
Q

What is important about metabolism?

A

Drugs require biotransformation to be active
(Phase 1 and 2 rxns)

18
Q

What is Volume of Distribution?

A

An indicator of the extent of drug distribution into body fluids and tissues
*only extent and not location
VD= Dose/Concentration in Plasma

19
Q

Name 5 organs involved in drug metabolism

A
  1. Liver
  2. Gut
  3. Lungs
  4. Kidneys
    5 Brain
20
Q

Name 5 factors that affect Metabolism

A
  1. Disease States
  2. Age
  3. Biological Sex
  4. Organ function
  5. Genetic polymorphisms
  6. Other drugs
21
Q

What are the main organs involved in Elimination and how is it measured?

A
  1. Liver and Kidney
  2. Measured by Half-life
22
Q

Describe what Half-life is

A

Time required to change the amount of a drug in the body by one-half during elimination

23
Q

Is half-life constant or inconsistent for drugs that follow first-order kinetics?

A

Constant

24
Q

Define steady state

A

When the amount of drug administered per unit time equals the drug eliminated per unit time

25
Q

How many half-lives are required for steady state?

A

After approximately four half-lives

26
Q

What causes fluctuations in half-life?

A
  1. Proportional to dose interval/half-time
  2. Slow absorption
27
Q

Define clearance

A

Measure of the ability of the body to eliminate a drug
*Clearance=Rate of elimination/plasma concentration

28
Q

Describe first-order elimination

A
  1. Elimination is directly proportional to concentration
  2. Constant proportion or rate of drug is eliminated
  3. Most drugs exhibit this type of elimination
29
Q

Describe zero-order elimination

A
  1. Constant amount of drug is eliminated independent of concentration
  2. Examples: EtOH, ASA, phenytoin
  3. Also known as saturable metabolism
  4. If dosing rate exceeds elimination, steady state cannot be achieved
30
Q

Name 5 factors that affect elimination

A
  1. Disease states
  2. Biological sex
  3. Organ function
  4. Age
  5. Other drugs

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