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Pharm (Cholley) > Basic Principles > Flashcards

Basic Principles Flashcards

1
Q

Define: pharmacology

A
  • Study of substances that interact w/ living system
  • Beneficial therapeutic effect
  • Toxic effects
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2
Q

Define: toxicology

A
  • Undesirable effects of chemicals on systems
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3
Q

Define: pharmacotherapeutics

A

Study of therapeutic uses & effects

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4
Q

Define: pharmacokinetics

A

“What the body does to the drug”
- Absorption, distribution, metabolism, elimination =
“ADME”

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5
Q

Define pharmacodynamics, & what is potency?

A

“What the drug does to the body”

  • Study of the relationship btwn drug [ ] & response of pt
  • Potency = Amt of drug needed to produce effect
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6
Q

Define: Bioavailability, & what type of administration is equal to 100%?

A
  • Fraction of dose administered that reaches circulation

- 100% for IV administration

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7
Q

How is bioavailability reduced?

A
  • Incomplete absorption

- 1st pass metabolism

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8
Q

Oral bioavailability (What is the percentage?)

A

5 - < 100%

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9
Q

Geriatric population (How are drugs & nutrients absorbed?)

A
  • Most drugs absorbed via passive diffusion
  • Nutrients absorbed by active transport
  • Evidence of decreased 1st-pass effect on hepatic or gut wall metabolism –> increased bioavailability
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10
Q

Define: 1st-pass effect

A
  • [ ] of drug is reduced before reaching circulation

- Fraction lost during absorption

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11
Q

Effect of protein binding

A
  • Fraction unbound can be altered by variables
  • Higher drug [ ] & decreased plasma protein can lead to higher fraction unbound
  • Clearance increases
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12
Q

Protein-bound molecules are not available to do what?

A

Exert pharmacologic effects

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13
Q

Define: Volume of distribution (Vd)

A

Relates amt of drug in body to serum [ ]

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14
Q

What is Vd used to calculate?

A

The loading dose of a drug that will immediately achieve a steady-state [ ]

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15
Q

PK: Distribution in peds

A
  • ↑ Total body water
  • ↑ Extracellular fluid volume
  • ↓ Binding of drugs to plasma proteins
  • ↓ Amt of body fat
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16
Q

PK: Distribution in pregnancy

A
  • ↑ Body fat

- ↓ Plasma albumin [ ]

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17
Q

PK: Distribution in geriatrics

A
  • ↓ Total body water
  • ↓ Lean body mass
  • ↑ Body fat
  • ↔ or ↓ Serum albumin
  • ↑ α1-Acid glycoprotein
  • ↓ CO
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18
Q

Define: receptors

A

Molecules in which drugs interact to produce changes in fxn of the system

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19
Q

Define: agonist

A

Drugs bind to & activate the receptor, which directly or indirectly brings about the effect

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20
Q

Define: partial agonist

A

Binds to its receptor but produces a smaller effect at full dosage than a full agonist

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21
Q

Define: antagonist

A

Drugs, by binding to a receptor, compete w/ & prevent binding by other molecules

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22
Q

Define: allosteric

A

Drugs bind to the same receptor molecule but do not prevent binding of the agonist

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23
Q

Define Irreversible antagonist

A

Antagonist that cannot be overcome by increasing the agonist

24
Q

What are sites of drug metabolism?

A
  • Liver = most important organ for metabolism
  • Kidney plays a role
  • A few drugs are metabolized in many tissues bc of their enzymes
25
Q

Describe Phase I Reactions

A

Convert parent drug to a more polar or more reactive product by unmasking or inserting a polar functional group s/a —OH, —SH, or —NH2
- Usually changed to inactive

26
Q

Describe Phase II Reactions

A
  • Increase H2O solubility by conjugation of the drug molecule w/ a polar moiety s/a glucuronate, acetate, or sulfate
  • Forms a highly polar conjugate
27
Q

Define: Cytochrome P450 (What phase? Responsible for what?)

A
  • Part of Phase I reactions

- Enzyme species, responsible for much of drug metabolism

28
Q

Define: substrate

A

Drug metabolized by 1 of the CYP450 enzymes

29
Q

Define: inducer

A

Drug that increases activity of a CYP450 enzyme

30
Q

Define: inhibitor

A

Drug that decreases activity of a CYP450 enzyme

31
Q

What are some inhibitors of P-gp?

A
  • Verapamil

- Furanocoumarin components of grapefruit juice

32
Q

What drugs are normally expelled by P-gp?

A
  • Digoxin
  • Cyclosporine
  • Saquinavir
  • More toxic when given w/ a P-gp inhibitor
33
Q

Metabolism in peds

A
  • Slower in infants than in older children & adults
  • Sulfation pathway is well developed in infants
  • Glucoronidation pathway is undeveloped in infants
34
Q

Metabolism in pregnancy

A

Hepatic perfusion increases

35
Q

Metabolism in geriatrics

A
  • ↓ Hepatic size
  • ↓ Hepatic blood flow
  • ↓ Phase I metabolism
36
Q

Define: Steady state

A

Avg total amt of drug in the body does not change over multiple dosing cycles

37
Q

What do most drugs follow?

A

Linear pharmacokinetics

- steady-state serum drug [ ]s change proportionally w/ long-term daily dosing

38
Q

What kind of drugs follow nonlinear pharmacokinetics?

A

Those w/ serum [ ]s that change more or less than expected

39
Q

What is the most important pharmacokinetic parameter?

A

Clearance

40
Q

What does clearance determine?

A
  • Steady-state [ ] for a given dosage rate
  • Efficiency of the organ extracting the drug from the bloodstream
  • Determined by blood flow to the organ that metabolizes/eliminates the drug
41
Q

What can reduce the clearance of drugs that depend on renal fxn?

A
  • Renal disease
  • Reduced CO
  • Liver disease (less common)
42
Q

How does impairment of hepatic clearance occur?

A

When liver blood flow is reduced

- Ex. HF, severe cirrhosis

43
Q

Define: GFR

A
  • Total filtration rates of functioning nephrons of kidney
  • Cannot be measured directly
  • Used for detection, severity, & tx of kidney disease
44
Q

What are variables of GFR?

A
  • Gender
  • Age
  • Weight
  • Race
45
Q

Efficiency of renal excretion in pediatric pts is determined by what?

A
  • Glomerular filtration
  • Tubular secretion
  • Tubular reabsorption
  • Processes may not develop fully for several weeks to 1 yr after birth
46
Q

Excretion in pregnancy

A
  • Maternal plasma volume, CO, & glomerular filtration increase by 30% to 50% or higher
  • Higher levels of estrogen & progesterone alter liver enzyme activity
47
Q

Excretion in geriatrics

A 
↓ GFR
↓ Filtration fraction
↓ Tubular secretory function
↓ Renal mass
↓ Renal blood flow
48
Q

Describe the MDRD equation

A
  • Estimates GFR adjusted for BSA
  • More accurate than Cockroft-Gault
  • Used by most laboratories as eGFR
49
Q

Cockroft-Gault equation

A
  • Uses body weight

- Standard for drug dosing

50
Q

When is ABW (actual body weight) used?

A

If ABW is less IBW

51
Q

Define: efficacy

A

Greatest effect an agonist can produce if the dose is taken to the highest tolerated level
*Partial agonists have lower efficacy than full agonists

52
Q

Define: P-glycoprotein (Where is it found? What is its fxn?)

A

ATP-dependent transport molecule

  • Found in epithelial & cancer cells
  • Expels drug molecules from the cytoplasm into the extracellular space
  • In epithelial cells, expulsion is via the external or luminal face
53
Q

Define: Half life (t1/2)

A

Time required for serum [ ] to decrease by 1/2 after absorption & distribution are complete

54
Q

What does half life determine?

A

Time required to reach steady state & dosage interval

55
Q

What variables usually alter the clearance of a drug?

A

Disease, age

56
Q

What is half life dependent upon?

A

Clearance & Vd

57
Q

What is the MAP equation?

A

(SBP x 1/3) + (DBP x 2/3)

Pharm (Cholley) (9 decks)

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