Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Adv Anes. Pharm Spring 2024 > Exam1/ Lecture 2: Pharmacodynamics and Pharmacokinetics > Flashcards

Exam1/ Lecture 2: Pharmacodynamics and Pharmacokinetics Flashcards

1
Q

Lecture 1/22/23

What are the 5 reason why we need to know about pharmacodynamics and pharmacokinetics ?

A
  • Produce onset of drug effect quickly
  • Produce offset of drug effect quickly
  • Severe consequences to “under” or “over” dosing
  • Need to frequently adjust levels
  • Low therapeutic index

Slide 2

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

Lecture 1/22/24

What is a receptor made of?

A
  • Usually a protein

Slide 3

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

Lecture 1/22/24

What is a agonist

A

Activates receptor by binding to receptor

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

Lecture 1/22/24

What are the 3 bonds in agonist that is reversable

A
  • Ion (or electrocovalent…oppositely charged ions)
  • Hydrogen (to a very electronegative atom)
  • Van der Waals interaction (the sum of attractive or repulsive forces; creates orbital shift)

Slide 4

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

Lecture 1/22/24

What are the 2 things that happen to the receptors once it is activated?

A

Conformational shape changes (Bound vs unbound)
Thermodynamically more/less active

Slide 3

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Lecture 1/22/24

True or False: Drug effects is not effected by the number of bounds receptors.

A

False: Drug effect relates to number of bound receptors
Greatest effect….all receptors bound
Example: paralytics

Slide 3

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

Lecture 1/22/24

What is a antagonist

A

binds to a receptor but does not activate the receptor

Slide 5

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

Lecture 1/22/24

What are the reversible bond forces for an antagonist ?

3 reversible bond

A
  • Ion
  • Hydrogen
  • Van der waals

Slide 5

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

Lecture 1/22/24

What type of antagonism, in large amounts progressively inhibits the agonist and shifts dose respone curve to the right?

A

Competitive antagonism

Slide 6

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

Lecture 1/22/24

What type of antagonism does not allow the agonist effects to happen regardless of how much agonist is given?

A

Non-competitive antagonism

Slide 6

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

Lectue 1/22/24

What type of agonist binds to a receptor casusing less response than the agoinst even at supramaximal dose?

A

Partial agonist

Slide 7

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

Lecture 1/22/24

What type of agonist compete for the same site as the agonist but produce the oppose effects?

A

Inverse agonist

Slide 7

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

Lecture 1/22/24

True or False: The number of receptors cannot increase or decrease depending on the comorbidity and drug therapy?

A

False, can increase or decrease depending on comorbidity, and drug therapy

Slide 10

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

Lecture 1/22/24

What are the 3 types of receptors?

A
  • Lipid bilayer
  • Intracellular proteins
  • Circulating proteins

Slide 11

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

Lecture 1/ 22/24

What are 7 examples of lipid bilaryer receptors?

A
  • Common for anesthesia drugs
  • Membrane bound
  • Opioids
  • bzd
  • b-blockers
  • catecholamines
  • nMbd

Slide 11

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

Lecture 1/22/24

What are 3 examples of Intracellular proteins receptors?

A
  • Insulin
  • steroids
  • milrinone

slide 11

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

Lecture 1/22/24

What is an example of a circuating protein receptor?

A

anticoagulants

Slide 11

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

Lecture 1/22/24

Please label the graph:
* partial agonist
* inverse agonist
* full agoinist
* weak partial agonist

A

partial agonist - B.
inverse agonist - D.
full agoinist - A.
weak partial agonist- C.

Slide 8

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

Lecture 1/22/24

What does Renal Clearance involve?

A

Glomerular Filtration - GFR and amount of protein bound drug controls amount of drug entering tubule
Active Tubular Secretion - from peritubular capillaries, active transport process, penicillins
Passive Tubular Reabsorption - increased if drug is lipid soluble, ie thiopental, almost zero for water soluble drugs… excreted in urine

slide 24

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

1/22/24

What is Elimination 1/2 Time

A

time necessary to eliminate 50% of drug from PLASMA after bolus dose

slide 25

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

1/22/24

Time to a 50% decrease after infusion discontinued
(assumes a constant concentration, roughly relates to 1/2 life, increases the longer the infusion increases - accumulation in peripheral tissues)

A

Context Sensitive Half-Time

slide 27

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

1/22/24

what is Ionization

A

When the pk (dissociation constant) and ph are identical,
-50% of drug ionized, 50% of drug non-ionized

Most drugs are weak acids (Barbs) or weak bases (La and opioids)
-Acids are ionized in an alkaline ph/bases are ionized in an acid ph

slide 28

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

1/22/24

Characteristics of drug molecules

A

slide 29

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

1/22/24

how to figure out ionization vs non-ionization

A

Weak acids (barbiturates)
Pk after ph
Weak bases. (LA or opioids)
Pk before ph

So if a weak acid (pk 7.6) is put in a basic ph (blood 7.8)
7.8 – 7.6 = +0.2 acid drugs are ionized at basic ph

If weak base (pk 8.0) is put in an acid ph (Blood 7.2)
8.0 – 7.2= +0.8 weak bases are ionized at acid ph

“nicely negative numbers are nonionized”

slide 30

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

1/22/24

what is an Ion Trapping example

A

A pregnant lady gets a spinal anesthetic with LA and opioid (weak base, pk 7.3)
But fetal ph is lower than maternal ph (baby is in distress)

7.3 – 7.4 = -0.1 a bit non- ionized for mom
7.3 – 6.8 = +0.5 ionized for fetus and is trapped…. ”ion trapping”

In addition, the concentration gradient of non ionized drug to ionized drug for opioid is still higher in mom….

slide 31

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

1/22/24

what is:

“The sensitivity of the body to the drug”

“what the drug does to the body”

How do we figure this out?
Measure plasma concentrations at different pharmacologic responses….
Dopamine

Ie. Clinically, what are the drugs effects…

A

Pharmacodynamics

slide 33

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

1/22/24

What are causes for Individual Variability?

A

Elderly
-Decreased cardiac output…. To brain and liver….
-Decreased protein binding
-Increased body fat

Enzyme activity
-Acute vs chronic alcohol ingestion

Genetic disorders
-Atypical cholinesterase activity
-Malignant hyperthermia

slide 34

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

1/22/24

what is the difference between Potency vs Efficacy

A

Potency: concentration vs response….less drug with more effect = more potent

Efficacy: the ability of a drug to produce a clinical effect

slide 35

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

What is Relative Potency?

A
  • Time to drug effect
  • Plasma not the site of effect for anesthetic drugs
  • Lag time between administration (plasma concentration) and effect

slide 36

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

What is Effective Dose (ED50) ?

A

Dose required to produce effect in 50% of patients

slide 37

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

What is Lethal Dose (LD50) ?

A

Dose required to produce death in 50% of patients

slide 37

32
Q

What is Therapeutic Index?

A
  • ratio between (LD50/ED50 )
  • the wider/bigger it is, the safer the drug is and the the narrower it is, the more dangerous the drug is

slide 37

33
Q

What is a Stereochemistry?

A

How drug molecules are structured In 3 dimensions

slide 38

34
Q

What are Chiral Compounds?

A
  • Molecules with asymmetric centers
    usually related to way Carbon molecules are bonded.
  • the structure of an anti tumors and several of our popular drugs

slide 38

35
Q

What are structural basis of Enantiomers?

A
  • Chemically identical
  • Mirror images
  • Can’t be superimposed - not overlapping but like having but when my thumbs and my pinkies are on same sides.

slide 38

36
Q

What is Dextrorotatory of an Enantiomer?

A

RIGHT rotation of light in a solution

slide 39

37
Q

What is Levorotatory of an Enantiomer?

A

LEFT rotation of light in a solution

slide 39

38
Q

What are the 2 drug sequences of Enantiomers?

A
  • R: Rectus
  • S: Sinister

slide 39

39
Q

What is a Racemic?

A
  • 50/50 mixture
  • Optical activity equal
  • Can exhibit different ADME
  • One enantiomer is active; other inactive or side effects
  • 1/3 of drugs

slide 39

40
Q

What are examples of different Enantiomers?

A
  • S-Ketamine = more potent with less delirium vs. R-Ketamine = like head injury effects of delirium
  • L-Bupivicaine = less cardiac toxicity
  • Cisatracurium = isomer of Atracurium that lacks Histamine effects
  • Albuterol and Xopenex

slide 40

41
Q

What is Pharmacogenetics/Pharmacogenomics?

A

How a single gene or all genes (genome) influences responses to drugs

slide 41

42
Q

What is Pharmacogenetic Testing?

A

Look for variants in genes that code for:
* Drug-metabolizing enzymes
* Drug targets
* Immune proteins

slide 41

43
Q

What does the acronym ADME stand for?

A

Absorption, Distribution, Metabolism, Excretion

44
Q

Pharmacokinetics is the ________ study that details what the _______ does to the _____

A

Quantitative; Body; Drug

45
Q

Pharmacokinetics determines the measurable concentration of the drug in the ______

A

Plasma

46
Q

In a ONE compartment model, if a patient is hemorrhaging and a drug is administered, does the Volume of Distribution Increase or Decrease?

A

DEACREASE

47
Q

What organs are considered part of a “Vessel Rich Group?”

A

Brain, Liver, Kidney

48
Q

Is a one compartment volume distribution model accurate?

A

No

49
Q

What are 4 common drugs that are taken up in 1st pass metabolism?

A
  • Lidocaine
  • Propranolol
  • Meperidine
  • Fentanyl (Includes SUfentanil and ALfentanil)
50
Q

A HIGH Volume of Distribution of 5,000L indicates that a drug is ____ Soluble

A

Fat/Lipid

51
Q

How does LOW plasma protein affect drug distribution?

A

Allows for more free, unbound drug to be available to cross cell membranes (Distribute through the body)

52
Q

Acidic drugs primarily bind to what protein?

A

Albumin

53
Q

Alkalotic drugs primarily bind to what protein?

A

A1- Acid Glycoprotein

54
Q

Low plasma protein is commonly found in what patient demographics?

A
  • ICU Patients
  • Geriatrics
  • Patients with Extended NPO time
  • patients with Liver Cirrhosis Alcoholics
  • Patients in Renal Failure
  • Burn Patients
55
Q

If a drug has a normal free fraction of 2%, what percentage is bound?

A

98%
(2% is available to go off and elicit desired clinical/physiological response

56
Q

What drug (include its classification) is used as the gold standard to measure other drugs against?

A

Thiopental

It is a Barbiturate

57
Q

If a drug is HIGHLY bound to plasma proteins, does it have a Large or Small volume of distribution? Give an example of one medication

A

Small Vd

Rx: Warfarin

58
Q

The process of metabolism converts active, lipid soluble drugs to ____ soluble

A

Water

59
Q

Why are many anesthetics lipid soluble?

A

The effector sites of the anesthetics are not in the plasma, they are in other parts of the body

60
Q

Active Metabolites can have as high as ___% effect of the parent drug

A

50%

61
Q

What process do Prodrugs require to become active?

A

PO Drugs must first be ingested but all Prodrugs require some form of early Metabolism

62
Q

How are most drugs metabolized?

A

Hepatic Microsomal Enzymes ( the greatest)

Hoffman Elimination

Ester Hydrolysis

Kidneys

Tissue Esterase’s (GI Tract and Placenta)

63
Q

Hofmann Elimination depends on what two physiological properties being within normal limits?

A

Temperature and pH

64
Q

Hofmann Elimination is important in what types of drugs?

A

Neuromuscular Drugs

65
Q

What 2 phases occur in Metabolism?

A

Phase 1: Increase polarity and prepare for Phase 2 reactions

Phase 2: Covalently link with highly polar molecule to become water soluble

66
Q

What processes take place in Phase 1 metabolism?

A

Oxidation, Reduction, Hydrolysis

67
Q

What process takes place in Phase 2 metabolism?

A

Conjugation

68
Q

What gives the liver its red color?

A

A Heme cofactor

69
Q

Where are the P450 enzymes located?

A

Attached to the Smooth Endoplasmic Reticulum of the hepatocytes

70
Q

CYP450 absorbs what wavelength of UV light when exposed to Carbon Monoxide?

A

Wavelength 450nm

71
Q

What is the most common enzyme in the CYP 450 family

A

CYP3a4, responsible for up to 60% of the CYP450 activity

72
Q

Enzymatic INDUCTION leads to a(n) _______ in the amount of enzymes.

A

Increase

73
Q

An induction of enzymes, _______ metabolism of a drug and requires _______ frequent dosing of a drug to reach desired clinical effect.

A

Increase; more

74
Q

Enzymatic INHIBITION leads to a(n) _______ in the amount of enzymes

A

Decrease

75
Q

Inhibition of enzymes, _______ metabolism of a drug and _______ the effects of the drug

A

Decreases; Prolongs

76
Q

For most anesthetic drugs is constant so the Rate of clearance is proportional to ______

A

Concentration

77
Q

What effects can be caused by the limited capacity of the liver to metabolize a drug

A
  • Can lead to a buildup of a drug in the body, if the drug amount given exceeds the liver’s ability to metabolize

Adv Anes. Pharm Spring 2024 (7 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions