Brainscape's Knowledge GenomeTM

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


See full index

Pharmacology I Exam #1 > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

What is pharmacokinetic tolerance?

A

Response is decreased due to drug being broken down before it gets to the target sites - Drug levels change

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

What is pharmacodynamic tolerance?

A

Response is decreased due to changes in receptor number or function
- Drug levels do NOT change

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

What is physiological tolerance? Provide an example.

A

When two agents with opposing physiological effects are administered together
- Histamines cause vasodilation while epinephrine causes vasoconstriction

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

What are the four factors that influence the variability in drug response?

A
  • Differences in drug absorption
  • Differences in ligand concentrations
  • Differences in number/function of receptors
  • Differences in post receptor effects
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What is summation?

A

Two drugs elicit a similar response through different mechanisms; effect equals the sum of the two individual effects

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

What is synergism?

A

Two drugs elicit a similar response through different mechanisms; effect is greater than the sum of the two individual effects

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

Compare additive effect to summation effect

A
  • Summation: two drugs work through different mechanisms

- Additive: two drugs work through the same mechanism

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

What is organ-directed toxicity? Provide two examples.

A

Drugs are toxic to organs/tissue that have no involvement in therapeutic effect

  • Tylenol and liver issues
  • Tetracyclines and teeth discoloration, less bone growth
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What is tachyphylaxis? Provide an example.

A

Rapid development of tolerance following repeated doses over a short period of time
- Meth (aka stimulants)

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

What does the administration of antagonists do?

A

Causes up-regulation (more receptors due to prolonged presence of antagonist)

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

What is an example of metabolic enzyme deficiency?

A

Succinylcholine in patient’s with low serum cholinesterase
- Cholinesterase degrades succinylcholine but if it is deficient, the succinylcholine will remain in the plasma longer - 4 minutes of sedation turns into 4 hours

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

What is an example of competition for plasma binding sites?

A

Warfarin and Phenytoin
- When both are present, they compete for the same binding sites so Phenytoin can displace Warfarin and it will remain free (active) for longer → Warfarin dose must be reduced to avoid toxicity

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

What are six examples of “acceptable” adverse effects?

A
  • Headache
  • Fatigue
  • Dizziness
  • Upset GI
  • Nausea
  • Vomiting
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is overextension-type toxicity? Provide an example

A

Basically overdosing…

- Example is Warfarin causing hemorrhage

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

Provide three examples of organ-directed toxicity.

A
  • Aminoglycoside antibiotics and ototoxicity
  • Acetaminophen and hepatotoxicity
  • Metabolite toxicity: Acetaminophen and Isoniazid hepatotoxicity
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What is often the cause of an idiosyncratic drug response?

A

Mutation (polymorphism)

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

With drug allergies, what type of response is activated?

A

Immunologic response

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

What type of a response is Type I? How is this mediated? Provide an example.

A

Anaphylactic

  • IgE antibody-mediated
  • Ex. Penicillin-induced anaphylaxis
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What type of a response is Type II? How is this mediated? What does this result in?

A

Cytotoxic

  • IgM or IgG antibody-mediated
  • Results in RBC lysis
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What type of a response is Type III? How is this mediated? Provide an example.

A

Immune Complex (Arthus)

  • Antigen antibody-mediated
  • Ex. serum sickness
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What type of a response is Type IV? How is this mediated? Provide an example.

A

Delayed Hypersensitivity

  • Cell-mediated
  • Ex. SJS or Erythema Multiforme
22
Q

Differentiate between up regulation and down regulation.

A

Up-regulation: increase in number of receptors in order to increase response

Down-regulation: decrease in number of receptors in order to decrease response

23
Q

What is covalent binding? Provide an example.

A

Strong, IRREVERSIBLE bonding

- Ex. Aspirin

24
Q

Differentiate between the efficacy of full agonists, partial agonists and antagonists.

Also consider affinity…

A
  • Full agonists have affinity and efficacy (a = 1)
  • Partial agonists have affinity but lower efficacy (0 < a < 1)
  • Antagonists have affinity but no efficacy (a = 0)
25
Q

What does a low therapeutic ratio indicate about a drug? What if the TR is high? Provide an example of each.

A
  • Lower the TR, riskier the drug (Warfarin)

- Higher the TR, the safer the drug (Penicillin)

26
Q

What does a narrow margin of safety indicate about a drug? What if the margin of safety is wide?

A
  • Narrower the margin of safety, the riskier the drug

- Wider the margin of safety, the safer the drug

27
Q

Under what condition to spare receptors exist? How does this effect ED50, and Kd?

A

Spare receptors exist when it’s possible to elicit Emax without occupying all of the available receptors

  • ED50 will decrease
  • Kd will remain the same

Aka if ED50 does not equal Kd, spare receptors are present

28
Q

What do partial agonists act like in the presence of full agonists?

A

Competitive antagonists

29
Q

How will Emax be affected if competitive antagonists are present?

A

Emax will not change

30
Q

How will Emax be affected if non-competitive antagonists are present?

A

Emax will decrease

- Even if more agonist is added, the receptor’s shape has been changed so there are fewer available receptors

31
Q

How will ED50 be affected if competitive antagonists are present?

A

ED50 will increase (takes more medication to achieve 50% maximal effect)

32
Q

How will ED50 be affected if non-competitive antagonists are present?

A

ED50 may change, but may not

33
Q

How is agonist affinity affected if competitive antagonists are present?

A

Agonist affinity for its receptors will decrease

- Kd increases because more drug is needed to get effect

34
Q

How can the affects of a competitive antagonist be overcome?

A

Competitive antagonists bind reversibly so if more agonist is added, the agonists will eventually “win the competition”

35
Q

What is an example of physiological antagonism?

A

Histamines cause a fall in BP, which can be reversed with epinephrine

36
Q

What is an example of chemical antagonism?

A

Neutralizing stomach acid with antacids

37
Q

What is the role of intracellular receptors? How do these effects present?

A

Modify gene transcription and protein synthesis

- Effects are not immediate and tend to be long-lasting

38
Q

What specific receptor type is associated with Transmembrane Receptors? What are two examples of ligands that act on this receptor type?

A

Transmembrane Receptors = Tyrosine kinase receptors

  • Insulin
  • Growth factor
39
Q

What specific protein class is associated with Cytokine Receptors? What are three examples of ligands that act on this receptor type?

A

Cytokine Receptors = JAK

  • Growth hormone
  • Erythropoetin
  • Interferons/Interleukins
40
Q

What are two examples of ion channels?

A
  • Ligand-gated

- Voltage-gated

41
Q

What are two examples of ligand-gated channels?

A
  1. ACh: depolarize cell

2. GABA: hyperpolarize cell

42
Q

What is an example of synergism related to GABA receptors?

A

Benzos and alcohol both act on GABA receptors so when both are present, the effect of each is much greater than the two added alone

43
Q

Give three examples of compounds that use B1 and B2 receptors. Are these stimulating or inhibiting?

A

Stimulate Gs and activate cAMP

  • Epinephrine
  • Norepinephrine
  • Isoproterenol
44
Q

Give three examples of compounds that use a2 receptors. Are these stimulating or inhibiting?

A

Stimulate Gi and inhibit cAMP

  • Epinephrine
  • Norepinephrine
  • Clonidine
45
Q

What are two examples of receptors that involve a secondary signaling mechanism? What signaling pathway does each activate?

A
  • Tyrosine kinase receptors activate the Ras/Raf signaling pathway
  • Cytokine receptors activate the JAK/STAT signaling pathway
46
Q

How do Gs proteins affect cAMP production?

A

Gs proteins increase cAMP production

47
Q

How do Gi proteins affect cAMP production?

A

Gi proteins decrease cAMP production

48
Q

What type of protein are beta receptors associated with?

A

Gs

49
Q

What type of protein are alpha 1 receptors associated with?

A

Gq

50
Q

What type of protein are alpha 2 receptors associated with?

A

Gi

51
Q

What information does a quantal DR curve provide?

A

TR and margin of safety

52
Q

What information does a graded DR curve provide?

A

Potency and Emax

Pharmacology I Exam #1 (5 decks)

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