Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

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

Pharmacokinetics/dynamics Exam 1 Flashcards

1
Q

Tachyphylaxis definition

A

Tolerance

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Inverse agonists previously known as antagonists (6)

A
  1. propranolol
  2. metoprolol
  3. cetrizine
  4. loratidine
  5. prazosin
  6. naloxone
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

are # of receptors static?

A

No, they can increase or decrease in number

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Albuterol effect on receptors

A

Down regulation with repeated doses (less effect)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Pheochromocytoma effect on receptors

A

Decreased b-receptors due to abdormally high amounts of catecholamines

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Pharmacokinetics definition

A

What the body does to the drug (ADME)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Pharmacodynamics definition

A

What the drug does to the body

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Pharmacogenetics impact

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

classification of receptors are based on (3)

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Which drugs work best when all receptors are bound?

A

Paralytics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Common anesthesic solubility

A

Lipid soluble

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Vessel rich groups (5)

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Vessel rich group CO% and BM%

A

75% of CO
10% BM

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Muscle CO% and BM%

A

19% CO
50% BM

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Fat CO% and BM%

A

6% CO
20% BM

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Vessel poor CO% and BM%

A

0% CO
20% BM

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What is volume of distribution?

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What does a high Vd imply? Low Vd?

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What drugs will leave the central compartment?

A

Fat soluble drugs have a high Vd

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Protein binding effect on Vd

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
**Acidic** drugs bind to what protein? **Alkalotic** drugs?
Acidic = **albumin** alkalotic = **A1-acid glycoprotein**
26
Common causes of decreased plasma proteins (5)
* Age * Hepatic disease * Renal failure * Pregnancy * Malnutrition
27
FF of a drug is 2%. if 50% of plasma proteins are lost, what is the new FF?
4% (doubles)
28
High volume of distribution
Highly distributed to tissues **Poor protein binding** and **lipophilic** **Thiopental, diazepam**
29
Small volume of distribution
Drug remains in plasma, poor distribution **Highly protein bound** **warfarin**
30
Metabolism process
Conversion from lipid soluble to water soluble for excretion
31
Drugs that have active metabolites (4)
1. diazepam 2. propranolol 3. morphine 4. codeine
32
Prodrug definition
Drug administered in inactive form and converted to active form
33
**plasma** metabolic pathway
1. hoffman eliminiation 2. ester hydrolysis
34
**Most common** metabolism pathway
Hepatic Microsomal enzymes
35
which organs metabolize through tissue esterase
1. GI tract 2. placenta
36
Most common hepatic Microsomal enzyme
**CYP3A4**: metabolizes more than **50% of drugs**
37
CYP2 percent homologous? CYP2A?
CYP2 = **40%** CYP2A = **55%**
38
Phase I reactions
1. **Oxidation** CYP450, lose electrons 2. **Reduction** removes O2 or adds H+ 3. **Hydrolysis** use water to break bonds
39
Phase II reaction
**Conjugation** **Conversion to water soluble** compound for elimination
40
Cause of dark red liver color
Hepatic Microsomal enzymes containing heme cofactor (iron)
41
Enzyme inducer
**Increases** enzyme effect = **less drug** **Phenobarbital**
42
Enzyme inhibitor
**Decreases** enzyme effect = less drug **grapefruit juice**
43
**Flow limited** hepatic clearance definition
Flow to the liver **limits** the metabolic rate **rate is proportional to concentration** **more drug = more clearance**
44
for most anesthetic drugs, clearance is
Constant
45
**Capacity limited** hepatic clearance definition
Liver's ability to metabolize limits metabolic rate
46
rate of drug metabolsim formula
rate = R = Q (C inflow - C outflow)
47
renal clearance involves (3)
1. filtration 2. secretion (**PCN**) 3. reabsorption (**thiopental**)
48
Elimination half-**TIME** definition
Time to eliminate **50%** of drug from **PLASMA**
49
Elimination half-**LIFE** definition
Time to eliminate **50%** of drug from **TISSUE**
50
**Context sensitive** half-time definition
Time for **50%** decrease of drug after **INFUSION** **discontinued**
51
context sensitive half-time of **fentanyl**
significantly **increases** the **longer** the infusion is given
52
Acids are ionized in ____ pH
Alkaline
53
Bases are ionized in ____ pH
Acidic
54
*Non-ionized* vs *ionized drug* **barrier crossing**
**Non-ionized** cross lipid barriers
55
drugs that are **weak acids** example
barbiturates
56
drugs that are **weak bases** example
1. local anesthetics 2. opioids
57
**Non-ionized** solubility
**Lipid** soluble
58
**Ionized** solubility
**Water** soluble
59
What is ionization?
When the Pk and pH are **identical** 50% of drug ionized, 50% of drug non-ionized
60
**non-ionized** drugs profile
Activity: **active form** Solubility: **lipid soluble** crosses BBB: **yes** renal excretion: **no** hepatic metabolism: **yes**
61
**ionized** drugs profile
Activity: **inactive form** Solubility: **water soluble** crosses BBB: **no** renal excretion: **yes** hepatic metabolism: **no**
62
How do we figure out drug ionization?
**Weak acid** = pK **A**FTER pH **Weak base** = pk **B**EFORE pH
63
Non-ionized pharmacologic effect
Active drug
64
Ionized pharmacologic effect
Inactive drug
65
Ionization calculations negative numbers
Non-ionized
66
Ion trapping explanation
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
Ionization effects
Ionized drugs lose effectiveness
68
Elderly effects on ADME
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
Potency definition
**Less drug** needed to produce **more effect** = higher potency
70
Efficacy definition
Drug produces **higher effect** = higher efficacy
71
What is the relative potency of **fentanyl** vs **alfentanyl**?
**Fentanyl** equilibrates with brain **slow** = **delay** in onset, **lasts long** **alfentanyl** equilibrates with brain **fast** = **rapid onset**, **wears off fast**
72
Effective dose definition
ED50: dose to produce effect in 50% population
73
Lethal dose definition
LD50: dose to produce death in 50% population
74
Therapeutic index definition
TD = LD50/ED50 (wider TI = safer)
75
Enantiomer definition
* Chemically **identical** * **mirror image** * **un-superimposable**
76
Racemic mixture
Mixture of different isomers likely producing different effects
77
R-isomer vs L-isomer
R-isomer = molecule sequence to the right L-isomer = molecule sequence to the left
78
how much of drugs are racemic?
**1/3** of available drugs
79
Chiral compounds
molecules with assymetric centers related to carbon bonding
80
more potent isomer of ketamine
**S-ketamine** more potent with less delerium
81
bupivicane preferred isomer
**L-bupivicane** less CV toxicity
82
atracurium preffered isomer
**cisatracurium (nimbex)** less histamine effects
83
albuterol vs levalbuterol (xopenex)
albuterol = R-albuterol + S-albuterol levalbuterol = R-albuterol (less S/E)

TxWes Spring '25: Anesthesia Pharm (13 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions