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TxWes Spring '25: Anesthesia Pharm > Pharmacokinetics/dynamics Exam 1 > Flashcards

Pharmacokinetics/dynamics Exam 1 Flashcards

1
Q

Tachyphylaxis definition

A

Tolerance

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2
Q

Agonist vs Antagonist vs partial agonist vs inverse agonist

A

Agonist: Activates receptor by binding to receptor
Antagonist: binds but does not activate the receptor
partial agonist: binds but has lower response than full agonist
inverse agonist: competes for receptor, produces opposite effect

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3
Q

competitive vs non-competitive antagonism

A

competitive: Increasing amounts progressively inhibit the agonist
non-competitive: Even high concentrations of agonist cannot cause the agonist effect

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4
Q

what bonds do agonists and antagonists make with receptors?

A
  1. ion/electrocovalent
  2. hydrogen bond
  3. van der waals
  4. covalent (irreversible)
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5
Q

Inverse agonists previously known as antagonists (6)

A
  1. propranolol
  2. metoprolol
  3. cetrizine
  4. loratidine
  5. prazosin
  6. naloxone
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6
Q

are # of receptors static?

A

No, they can increase or decrease in number

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7
Q

Albuterol effect on receptors

A

Down regulation with repeated doses (less effect)

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8
Q

Pheochromocytoma effect on receptors

A

Decreased b-receptors due to abdormally high amounts of catecholamines

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9
Q

Pharmacokinetics definition

A

What the body does to the drug (ADME)

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10
Q

Pharmacodynamics definition

A

What the drug does to the body

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11
Q

Pharmacogenetics impact

A

Specific genes or genomes can influence responses to drugs and help predict effects

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12
Q

classification of receptors are based on (3)

A

Location:
1. lipid bilayer
2. intracellular
3. circulating (warfarin)

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13
Q

Which drugs work best when all receptors are bound?

A

Paralytics

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14
Q

Common anesthesic solubility

A

Lipid soluble

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15
Q

Vessel rich groups (5)

A

High cardiac output organs: heart, lungs, liver, kidney, brain

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16
Q

Vessel rich group CO% and BM%

A

75% of CO
10% BM

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17
Q

Muscle CO% and BM%

A

19% CO
50% BM

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18
Q

Fat CO% and BM%

A

6% CO
20% BM

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19
Q

Vessel poor CO% and BM%

A

0% CO
20% BM

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20
Q

What is volume of distribution?

A

degree to which a drug is distributed throughout the body after absorption

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21
Q

What does a high Vd imply? Low Vd?

A

High Vd: highly distributed to tissues
low Vd: stays in plasma

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22
Q

what dilutes the drug upon injection?

A

Central compartment:
* venous blood
* IVC
* Right heart
* pulmonary circulation
* lungs
* left heart
* aorta
* then goes to vessel rich groups

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23
Q

What drugs will leave the central compartment?

A

Fat soluble drugs have a high Vd

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24
Q

Protein binding effect on Vd

A

Higher Vd = low protein binding
only free drug can cross cell membranes

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25
Q

Acidic drugs bind to what protein? Alkalotic drugs?

A

Acidic = albumin
alkalotic = A1-acid glycoprotein

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26
Q

Common causes of decreased plasma proteins (5)

A
  • Age
  • Hepatic disease
  • Renal failure
  • Pregnancy
  • Malnutrition
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27
Q

FF of a drug is 2%. if 50% of plasma proteins are lost, what is the new FF?

A

4% (doubles)

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28
Q

High volume of distribution

A

Highly distributed to tissues
Poor protein binding and lipophilic
Thiopental, diazepam

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29
Q

Small volume of distribution

A

Drug remains in plasma, poor distribution
Highly protein bound
warfarin

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30
Q

Metabolism process

A

Conversion from lipid soluble to water soluble for excretion

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31
Q

Drugs that have active metabolites (4)

A
  1. diazepam
  2. propranolol
  3. morphine
  4. codeine
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32
Q

Prodrug definition

A

Drug administered in inactive form and converted to active form

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33
Q

plasma metabolic pathway

A
  1. hoffman eliminiation
  2. ester hydrolysis
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34
Q

Most common metabolism pathway

A

Hepatic Microsomal enzymes

35
Q

which organs metabolize through tissue esterase

A
  1. GI tract
  2. placenta
36
Q

Most common hepatic Microsomal enzyme

A

CYP3A4: metabolizes more than 50% of drugs

37
Q

CYP2 percent homologous?
CYP2A?

A

CYP2 = 40%
CYP2A = 55%

38
Q

Phase I reactions

A
  1. Oxidation CYP450, lose electrons
  2. Reduction removes O2 or adds H+
  3. Hydrolysis use water to break bonds
39
Q

Phase II reaction

A

Conjugation
Conversion to water soluble compound for elimination

40
Q

Cause of dark red liver color

A

Hepatic Microsomal enzymes containing heme cofactor (iron)

41
Q

Enzyme inducer

A

Increases enzyme effect = less drug
Phenobarbital

42
Q

Enzyme inhibitor

A

Decreases enzyme effect = less drug
grapefruit juice

43
Q

Flow limited hepatic clearance definition

A

Flow to the liver limits the metabolic rate
rate is proportional to concentration
more drug = more clearance

44
Q

for most anesthetic drugs, clearance is

45
Q

Capacity limited hepatic clearance definition

A

Liver’s ability to metabolize limits metabolic rate

46
Q

rate of drug metabolsim formula

A

rate = R = Q (C inflow - C outflow)

47
Q

renal clearance involves (3)

A
  1. filtration
  2. secretion (PCN)
  3. reabsorption (thiopental)
48
Q

Elimination half-TIME definition

A

Time to eliminate 50% of drug from PLASMA

49
Q

Elimination half-LIFE definition

A

Time to eliminate 50% of drug from TISSUE

50
Q

Context sensitive half-time definition

A

Time for 50% decrease of drug after INFUSION discontinued

51
Q

context sensitive half-time of fentanyl

A

significantly increases the longer the infusion is given

52
Q

Acids are ionized in ____ pH

53
Q

Bases are ionized in ____ pH

54
Q

Non-ionized vs ionized drug barrier crossing

A

Non-ionized cross lipid barriers

55
Q

drugs that are weak acids example

A

barbiturates

56
Q

drugs that are weak bases example

A
  1. local anesthetics
  2. opioids
57
Q

Non-ionized solubility

A

Lipid soluble

58
Q

Ionized solubility

A

Water soluble

59
Q

What is ionization?

A

When the Pk and pH are identical
50% of drug ionized, 50% of drug non-ionized

60
Q

non-ionized drugs profile

A

Activity: active form
Solubility: lipid soluble
crosses BBB: yes
renal excretion: no
hepatic metabolism: yes

61
Q

ionized drugs profile

A

Activity: inactive form
Solubility: water soluble
crosses BBB: no
renal excretion: yes
hepatic metabolism: no

62
Q

How do we figure out drug ionization?

A

Weak acid = pK AFTER pH
Weak base = pk BEFORE pH

63
Q

Non-ionized pharmacologic effect

A

Active drug

64
Q

Ionized pharmacologic effect

A

Inactive drug

65
Q

Ionization calculations negative numbers

A

Non-ionized

66
Q

Ion trapping explanation

A

Ionized drugs can be “trapped” such as in a fetus
cannot cross barriers if it is ionized (e.g. fentanyl may be OK for mom but will kill baby because of different pH)

67
Q

Ionization effects

A

Ionized drugs lose effectiveness

68
Q

Elderly effects on ADME

A
  1. Decreased CO = decreased blood flow to brain and liver
  2. decreased protein binding = more free drug
  3. increased body fat = more absorption of lipid soluble
69
Q

Potency definition

A

Less drug needed to produce more effect = higher potency

70
Q

Efficacy definition

A

Drug produces higher effect = higher efficacy

71
Q

What is the relative potency of fentanyl vs alfentanyl?

A

Fentanyl equilibrates with brain slow = delay in onset, lasts long
alfentanyl equilibrates with brain fast = rapid onset, wears off fast

72
Q

Effective dose definition

A

ED50: dose to produce effect in 50% population

73
Q

Lethal dose definition

A

LD50: dose to produce death in 50% population

74
Q

Therapeutic index definition

A

TD = LD50/ED50
(wider TI = safer)

75
Q

Enantiomer definition

A
  • Chemically identical
  • mirror image
  • un-superimposable
76
Q

Racemic mixture

A

Mixture of different isomers likely producing different effects

77
Q

R-isomer vs L-isomer

A

R-isomer = molecule sequence to the right
L-isomer = molecule sequence to the left

78
Q

how much of drugs are racemic?

A

1/3 of available drugs

79
Q

Chiral compounds

A

molecules with assymetric centers
related to carbon bonding

80
Q

more potent isomer of ketamine

A

S-ketamine more potent with less delerium

81
Q

bupivicane preferred isomer

A

L-bupivicane less CV toxicity

82
Q

atracurium preffered isomer

A

cisatracurium (nimbex) less histamine effects

83
Q

albuterol vs levalbuterol (xopenex)

A

albuterol = R-albuterol + S-albuterol
levalbuterol = R-albuterol (less S/E)

TxWes Spring '25: Anesthesia Pharm (12 decks)

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