Lecture 54 - Pharmacokinetics Flashcards

1
Q

pharmacodynamics

A

describes the action of the drug in the patient

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2
Q

pharmacokinetics

A

describes the disposition of drugs in the body

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3
Q

what influences drug dose to plasma concentrations

A

pharmacokinetic factors

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4
Q

what influences plasma concentrations to pharmacologic response

A

pharmacodynamic factors

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5
Q

systemic availability

A

F = fraction of drug absorbed
determined from peak concentration (Cmax) and AUC

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6
Q

clearance

A

ability of the body or clearance organ to eliminate a drug

CL, CLs = systemic clearance

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7
Q

Elimination

A

concentration over time

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8
Q

volume of distribution

A

the volume of body fluid into which a drug distributes

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9
Q

summarize the 5 steps in studying pharmacokinetics

A
  1. get subject
  2. administer drug
  3. collect serial blood samples
  4. measure drug concentrations
  5. plot results
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10
Q

absorption rate

A

time taken to reach peak concentration (Cmax)

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11
Q

a short half-life drug needs ____ administration

A

frequent

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12
Q

a long half-life drug needs ____ administration

A

spaced

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13
Q

what 4 factors affect the volume of distribution

A
  1. lipid solubility
  2. drug pKa and pH of tissues (ionization)
  3. drug size
  4. protein binding
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14
Q

T/F: drug diffusion across a plasma membrane depends on its lipophilicity

A

TRUE

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15
Q

high lipophilicity creates ____ diffusion

A

more

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16
Q

drug eliminated/dose rate =

A

drug concentration x clearance

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17
Q

what equation is the rate of delivery

A

Ca x Q

18
Q

what equation is the rate of leaving

A

Cv x Q

19
Q

what equation is the rate of extraction

A

Q (Ca - Cv)

20
Q

what are examples of high-clearance drugs

A

opiates
fentanyl
beta-blockers
cannabinoids
dexmed

21
Q

what is the first-pass effect

A

drugs administered orally will go through detoxification in the liver first and not have the intended effect in target organs

22
Q

describe hepatic flow limited clearance

A

dependent on blood flow
CLh = Qh x ERh

23
Q

describe hepatic clearance when not flow limited

A

dependent on metabolism
CLh = Cli x fu
*protein free drug

24
Q

what is a determinant of drug clearance

A

drug metabolism

25
Q

describe the metabolic pathways of drugs

A
  1. phase I reactions (cytochrome, P450)
  2. phase II reactions (conjugation)
  3. elimination via bile/urine
26
Q

drug undergoes metabolic pathways to be

A

inactive or toxic metabolite

27
Q

prodrug (inactive) undergoes metabolic pathways to be

A

active drug

28
Q

prodrug codeine becomes

A

morphine

29
Q

prodrug oxycodone becomes

A

oxymorphone

30
Q

prodrug hydrocodone becomes

A

hydromorphone

31
Q

prodrug tramadol becomes

A

desmethyl-tramadol

32
Q

what enzyme are cats deficient in for phase II metabolism

A

UDP-glucuronosyltransferase

33
Q

what enzyme are dogs deficient in for phase II metabolism

A

N-acetyltransferase

34
Q

what drugs are not used in cats

A
  • aspirin
  • benzoic acid
  • acetaminophen
  • morphine
  • chloramphenicol
  • desmethyl tramadol
35
Q

Bioavailability

A

rate and extent of drug absorption

36
Q

AUC

A

area under the curve

37
Q

how is systemic availability calculated

A

AUC(non-iv) / AUC(iv)

38
Q

what are the 7 routes of administration

A
  1. IV
  2. IM
  3. SQ
  4. oral
  5. topical
  6. nasal
  7. rectal
39
Q

low systemic availability can be caused by

A
  • poor dissolution
  • poor stability or solubility
  • low permeability
  • drug/food interactions
  • poor intestinal blood flow
40
Q

solubility of an oral medication contributes to

A

dissolution

41
Q

permeability of an oral medication contributes to

A

absorption

42
Q

what are the 3 transdermal medications for cats? what are their jobs?

A
  1. methimazole (hyperthyroidism)
  2. mirtazapine (appetite stimulant)
  3. buprenorphine (pain)