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BPM1 Exam 2 - Foundations to Medicine 2 > FTM 48-49 - Pharmacodynamics > Flashcards

FTM 48-49 - Pharmacodynamics Flashcards

1
Q

Define Drug

A

Any substance that when administered to a living organism, produces a biological effect.

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2
Q

Define pharmacology

A

The study of how the function of living systems is affected by chemical agents

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3
Q

Define pharmacokinetics and phamacodynamics

A
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4
Q

Define clinical pharmacology and pharmacotherapeutics

A

The both refer to the study of the use of drugs in the prevention and treatment of disease

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5
Q

Define pharmacotherapy

A

The use of drugs to treat disease

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6
Q

Define toxicology

A

The study of adverse effects of drugs

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7
Q

T/F - drugs can add cellular functions

A

False, they can only alter existing functions and processes

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8
Q

What type of molecule are most drug receptors?

A

Proteins

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9
Q

What are the two major examples of drugs that act through GPCRs. What class of drug are they and what are they primarily used for?

A
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10
Q

Describe the IP3 signaling pathway

A
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11
Q

What does the Gi protein do?

A

It inhibits adenylyl cyclase and opens K+ channels

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12
Q

What are the four primary cAMP-Mediated hormonal responses?

A
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13
Q

What are the five primary Ca++ mediated responses?

A
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14
Q

Describe the basic overall structure of ligand-regulated transmembrane enzymes and list what type of encymatic domains they can have.

A
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15
Q

What are the two primay tyrosine kinase receptors?

A

Insulin receptor

Epidermal growth factor receptor (EGFR)

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16
Q

Describe the tyrosine kinase signaling pathway

A
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17
Q

Describe the cytokine receptor signaling pathway

A
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18
Q

What do cytokine receptors mediate the action of?

A

Peptide ligands, such as:

Growth Hormone

Erythropoietin

Interferons

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19
Q

What is a nuclear receptor essentially?

A

A ligand activated txn factor

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20
Q

What are the three well known nuclear receptors?

A

Steroid hormones

Thyroid hormone

Vitamin D

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21
Q

What type of receptor has no intrinsic enzymatic activity?

A

Cytokine receptors, they bind to a JAK to carry out enzymatic activity

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22
Q

T/F - All drugs act by interacting with macromolecular components of an organism.

A

False, antacids do not

23
Q

The relation between drug concentration and effect is described by a __________ curve.

A

Hyperbolic

24
Q

What is the equation that relates drug concentration and effect?

A
25
Q

What is the equation that explains the relationship between the amount of drug bound to a receptor and the concentration of free drug?

A
26
Q

What is Kd a measure of? What does it mean if it is low or high?

A
27
Q

What type of curve is a drug binding curve?

A

Hyperbolic

28
Q

Why are the binding curve and dose response curve of a drug so similar?

A

Because the response to a drug is usually a concsequence of the binding of the drug to the receptor.

29
Q

How is dose-response data usually plotted and why?

A

It is usually plotted against the logarithm of the concentration to transform the hyperbolic curve into a sigmoid curve.

30
Q

Often not all receptors have to be bound to elicit a maximal response. What does this indicate?

A

That there are spare receptors and that signal amplification is taking place

31
Q

What is an EC50?

A

EC50 is the concentration of a drug at which half max response is reached

32
Q

Define efficacy and potency.

A

Efficacy is the magnitude of the response a drug produces. Maximal efficacy is the greatest effect a drug can produce (Emax)

Potency is a measure of the concentration or amount of drug necessary to produce an effect of a given magnitude. The EC50 of a drug is usually a measure of potency.

33
Q

Discuss the efficacies and potencies of these drugs and compare them to one another.

A
34
Q

The clinical effectiveness of a drug depends upon its _______ not its ________.

Whys is this?

A
35
Q

T/F - Competitive antagonism is always reversible

A

False

36
Q

What is noncompetitive antagonism and how would it affect the dose response curve of an agonist?

A

A noncompetitive antagonist is an irreversible antagonist that binds a receptor so that it cannot respond to the binding of an agonist. This type of antagonism lowers Emax and is insurmountable.

Also called allosteric antagonism

37
Q

How does a noncompetitive antagonist work?

A

It binds to the receptor at a site different from the agonist binding site and reduces the action of the agonist (often to zero).

38
Q

What does an indirect antagonistic drug do?

A

It binds to a macromolecule (not the receptor) in the signaling pathway that a agonist triggers to terminate the signal triggered by the agonist, therby decreasing or stopping the response.

39
Q

What does a physiological antagonistic drug do? Give an example?

A

It opposes the action of another drug but via a different receptor pathway.

Epinephrine causes an increase in BP and bronchodilation. Histamin counteracts this through a different signaling pathway.

40
Q

What does a chemical antagonist do?

A

It reacts chemically with an agonist to form an inactive product

41
Q

What is protamine and what does it do?

A

It is a positively charged protein that binds to and inactivates heparin (which is negatively charged)

42
Q

How can an agonist drug interfere with a biological agonist?

A

The drug will compete with the biological agonist for receptor occupancy. If it is a partial agonist then this competition would reduce the response from the biological agonist

43
Q

What does an inverse agonist do?

A

So receptors are always partially active whether they or bound or not, this is called constitutive activity. Inverse agonists reverse the constitutive activity of a receptor.

44
Q

What is another word for drug desensitisation?

A

Tachyphylaxis

45
Q

Define these terms: tolerance, refractoriness, drug resistance

A
46
Q

What are the five major ways drug desensitization & tolerance can occur?

A

Receptor modification (often phosphorylation)

Internalization of receptors

Exhaustion of mediators (there is no more of a molecule to release)

Increased metabolic degradation (the body begins to break the drug down faster)

Physiological adaptation (the body begins to oppose the drug’s effect via a homeostatic response)

47
Q

What is a quantal dose-effect curve?

A

A plot of the fraction of the population that responds to a given dose of a drug as a function of the drug dose.

48
Q

What is the ED50 for a quantal dose-effect curve?

A

The median effective dose (ED50) is the dose at which 50% of individuals exhibit the specified quantal effect.

49
Q

What is a TD50 and LD50?

A

The median toxic dose (TD50) of a drug is the dose of that drug required to produce a particular toxic effect in 50% of animals.

The median lethal dose (LD50) of a drug is the dose of that drug required to cause death in 50% of animals.

50
Q

Compare and contrast graded and quantal dose-response curves.

A
  • Graded curves plot the magnitude of drug response against [drug] or dose
  • Quantal curves plot the fraction of a population that responds to a drug (ie - convulsions did or didn’t stop) against the drug dose given.
  • Only graded curves can provide EC50 and indicate maximum efficacy
  • Only quantal curves can provide ED50, TD50, LD50, and indicate the variability of drug responsiveness among individuals
51
Q

What is the therapeutic index for a drug?

A
52
Q

What is the therapeutic window for a drug?

A

The dosage range between the minimum effective therapeutic concentration and the minimum toxic concentration.

53
Q
A

BPM1 Exam 2 - Foundations to Medicine 2 (29 decks)

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