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Pharmacology > pharmacokinetics - ADME > Flashcards

pharmacokinetics - ADME Flashcards

1
Q

pharmacokinetics

A

what the body does to the drug

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2
Q

pharmacodynamics

A

what the drug does to the body (mechanism of action)

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3
Q

3 purposes of drugs

A
  1. preventive
  2. diagnostic
  3. therapeutic
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4
Q

what oral conditions results from most commonly prescribed drugs

A

xerostomia and salivary gland dysfunction

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5
Q

3 different ways to classify drugs

A
  1. mechanism of action
  2. organ or system target
  3. therapeutic use
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6
Q

absorption is defined as

A

presence of drug in plasma

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7
Q

metabolism of drugs occurs mainly in the

A

liver

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8
Q

elimination of the drug occurs mainly by

A

kidney and eliminated usually via urine

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9
Q

what is the goal for drug administration

A

adjust drug delivery to optimize drug availability at the therapeutic target

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10
Q

topical administration

A

local application of drug to body surface (intended for effect that that site)

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11
Q

systemic administration

A

drug enters circulatory system and moves throughout the whole body. it is not directed to site of action

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12
Q

enteral drug administration

A

through the GI system

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13
Q

parenteral drug administration

A

not through the GI system

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14
Q

drug formulation

A

form of the drug (cream, patch, pill, etc.); relates to route of admin.

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15
Q

types of drug routes where absorption is through mucosa

A

oral, rectal, inhalation

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16
Q

types of drug routes where absorption is on or through skin

A
  • subcutaneous, intramuscular, intraperitoneal
  • topical and transdermal
  • intravenous, intraarterial
  • intrathecal
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17
Q

what is an exception to topical route

A

patches: the drug is absorbed through the skin and intended to have an effect in areas of the body away from the site of application

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18
Q

3 types of enteral routes

A
  • oral
  • sublingual
  • rectal
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19
Q

oral administration (PO) advantages

A
  • convenient
  • high compliance
  • variety of release forms
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20
Q

first-pass effect

A

drug gets metabolized in liver first, causing reduced concentration of the active drug upon reaching its site of action

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21
Q

oral administration (PO) disadvantages

A
  • MAX FIRST PASS EFFECT

- variable absorption

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22
Q

sublingual (SL) advantages

A
  • rapid absorption

- NO FIRST PASS EFFECT

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23
Q

sublingual (SL) disadvantages

A

-limited to non-irritant drugs

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24
Q

rectal (PR) indications

A

pts with nausea or unable to swallow

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25
Q

rectal (PR) disadvantages

A
  • limited to non-irritant drugs
  • variable absorption
  • LIMITED/VARIABLE FIRST PASS EFFECT
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26
Q

route for lower 1/3 rectum

A

vena cava *NO FIRST PASS EFFECT

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27
Q

route for middle 1/3 rectum

A

both vena cava and portal vein *SOME FIRST PASS EFFECT

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28
Q

route for upper 1/3 rectum

A

portal vein then liver (FIRST PASS EFFECT)

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29
Q

intra-articular injection is a type of ____ route

A

topical, because the injection is directly into site

30
Q

advantages of parenteral drug delivery

A
  1. rapid and predictable administration
  2. accurate dosage
  3. IV bypasses absorption
  4. IV bypasses first pass effect
31
Q

disadvantages of parenteral drug delivery

A
  1. need for asepsis
  2. discomfort/pain
  3. difficult self-administration
  4. risk of tissue damage
  5. risk of medical complications
  6. cost
32
Q

what are 3 routes of admin that are fast

A
  • parenteral
  • intranasal
  • inhalation
33
Q

is oral (PO) fast or slow

A

slow

34
Q

is IV injection slow or fast when first administered

A

fast, because it bypasses GI and liver and doesn’t require time for absorption

35
Q

intervals between doses where concentration is zero is bad for which groups of pts

A
  • pts in chronic pain

- pts on Abx

36
Q

Css (concentration steady state)

A

mean concentration of drug at plateau level where rate of drug input = rate of drug elimination

37
Q

bolus

A

discrete amount of drug over a discrete/short time period

38
Q

example of type of continuous drug administration

A

IV infusion (using drip line)

39
Q

compare the graphs for repeated vs continuous

A

same but continuous is smoother

40
Q

drug absorption

A

transfer of drug from site of admin to bloodstream

41
Q

6 factors affecting drug absorption

A
  1. tissue barriers
  2. mechanism of drug absorption
  3. molecular size of drug
  4. drug protonation/charge
  5. drug solubility (P o/w coeff)
  6. drug binding to plasma protein
42
Q

examples of tissue barriers

A

cell membranes, tight junctions, and capillary permeability

43
Q

systemic capillaries

A
  • unrestricted movement
  • lots of space (fenestrations) to allow passive diffusion
  • pinocytosis
44
Q

renal capillaries

A
  • restricted movement
  • cannot pass through fenestrations
  • could pass through in damaged kidney
45
Q

brain capillaries (BBB)

A
  • restricted movement
  • no fenestrations
  • solutes must diffuse through 2 membranes
46
Q

3 things that make the BBB impermeable

A
  1. glial cells
  2. continuous basement membrane
  3. continuous endothelial cells
47
Q

2 methods for passive diffusion of water-soluble solutes

A
  • gap junctions (connexins)

- aquaporins

48
Q

non-ionized drugs (neutral drugs) cross membranes ___ (more/less) efficiently

A

more efficiently

49
Q

why should basic drugs not be absorbed orally

A

bc they get protonated in the stomach and have an overall + charge, which is harder to be absorbed

50
Q

acids have a __absorption at low pH and a ___absorption at high pH

A

high absorption at low pH

low absorption at high pH

51
Q

the gradual pH increase from stomach -> plasma-> urine allows for

A

ion trapping (neutral in stomach=> charged in urine)

52
Q

drugs with high lipid solubility will have a ___ (high/low) accumulation in cell membranes

A

high

53
Q

drugs with low lipid solubility will have a ___(high/low) accumulation in cell membranes

A

low

54
Q

the bond between drugs and plasma proteins is __ (weak/strong)

A

weak

55
Q

drug binding to proteins is

A

dynamic and reversible

56
Q

what happens when drug is bound by protein

A

nothing! it is not active, metabolized, and eliminated

57
Q

is the protein-bound drug fraction dependent on drug concentration

A

no. it is only drug specific

58
Q

high protein-drug = ___ drug distribution

A

low. only free drug moves in/out bloodstream

59
Q

drugs that bind to proteins may have competition from

A

other protein-binding drugs, causing the drug to remain active

60
Q

what do acidic and neutral drugs bind to

A

albumin or lipoproteins

61
Q

what do basic drugs bind to

A

alpha-1 acid glycoprotein

62
Q

why might it be hard for drugs to bind to proteins in a sick person

A
  • plasma protein levels are altered in disease

- less protein = more free drug = gets active, metabolized, eliminated

63
Q

distribution of water in the body

A
  • 40-44% intracellular

- 16-20% extracellular (intersticial 12-16%, plamsa 4%)

64
Q

volume of distribution

A

amount of drug in body / plasma conc of drug

65
Q

high Vd = ____ (stay/leave) plasma

A

leave

66
Q

low Vd = ____ (stay/leave) plasma

A

stay

67
Q

high Vd will require ___ (high/low) dose to reach a certain conc

A

high

68
Q

apparent Vd uses concentration of drug in

A

plasma (NOT BODY)

69
Q

assumptions of using apparent Vd

A
  • drug is distributed uniformly and in a single compartment

- concentration of plasma is representative

70
Q

describe the order of drug distribution over time (VRG, MG, VPG)

A

VRG=>MG=>VPG

71
Q

biological response modifiers

A
  • antibodies, cell signal mediators, blood products, vaccines, and gene therapy
  • produced by biological organisms
72
Q

radiopharmaceuticals

A

drugs that are intentionally made radioactive (radionuclides) and used for research, diagnostic, and therapeutic purposes

Pharmacology (17 decks)

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