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Pharmacology Exam 1 > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

Pharmacodynamics

A

The effects of drugs and their mechanism of action within the body.

Basically, what the drug does to the animal.

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2
Q

What types of effects can we see with the drugs?

A
  • Therapeutic effects
  • Side effects
  • Adverse effects
  • Toxic effects
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3
Q

What is the effect of the drug we want?

A

Therapeutic effect

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4
Q

What effect is secondary to the intended effect and may be good OR bad?

A

Side effects

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5
Q

What effect is unintended and unwanted and includes NOT producing the desired clinical effect.

A

Adverse effects

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6
Q

What is the study of studying adverse effects?

A

Pharmacovigilance

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7
Q

What is the response to a drug that is harmful to the health of life or the animal?

A

Toxic effect

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8
Q

What are physical interactions?

A

Non-specific drug effects such as:

Osmotic diuretics
Antacids
Radioactive Iodine

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9
Q

How do osmotic diuretics work in the body? What type of interaction are they?

A

These molecules move through the body dragging water with them by osmosis until they are excreted.

Physical Interaction

Ex. Mannitol

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10
Q

How do antacids work in the body? What type of interaction are they?

A

If given orally they directly interact with acid in the GI tract as a form of physiologic antagonism

Physical interaction

Ex. Calcium carbonate tablets

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11
Q

How does radioactive iodine work in the body? What type of interaction is it?

A

The iodine is actively concentrated in the thyroid and radiation will destroy all tissue within 2-3 mm causing focal, controlled destruction.

Physical interaction

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12
Q

What are types of non-receptor interactions?

A
  • Voltage gated ion channels
  • Enzymes
  • Carrier proteins
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13
Q

How can a drug affect the body using voltage-gated ion channels?

A

Blocking of ion channels can occur by the drug molecule physically obstructing the channel and may also modulate the opening or closing of the channel.

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14
Q

How can a drug affect the body using enzymes?

A
  • Drugs can be analogs that compete with the real substrate for binding to the enzyme (organophsphate compete with Ach for binding sites on acetylcholinesterase)
  • Prodrugs where the drug needs to be metabolized to its active form
  • Act as a false substrate which will lead to the formation of abnormal metabolites (sulfonamides -> dihydropteroate synthase works on the sulfa instead of on PABA and does not produce it’s normal metabolites)
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15
Q

How can a drug affect the body using carrier proteins?

A

Some small, polar molecules cannot cross cell membranes and get carried in and out using a carrier protein

A drug may alter the movement either preventing the uptake of a molecule or preventing output of a molecule

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16
Q

What are the types of Receptor interactions?

A

Specific recognition sites for endogenous chemical messengers

Ionotropic receptors
Metabotropic receptors
Kinase coupled receptors
Nuclear receptors

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17
Q

Ionotropic Receptor

A
  • composed of several proteins embedded in the cell membrane
  • Ligand gated
  • Drugs can bind to these to activate them or prevent them from opening
  • Often involved in fast neurotransmission
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18
Q

Metabotropic Receptor

A
  • Also called 7TM (seven transmembrane)
  • Tranduce an extracellular signal to an intracellular one by activating the G-protein second messenger system
  • Allows signal amplification and specificity
  • Common for secretory and smooth muscle functions (muscarinic ACh and histamine receptors)
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19
Q

Kinase- Linked receptors

A
  • Transmembrane proteins
  • have extracellular receptor portion and inctracellular portion that has enzymatic activity
  • Phosphorylation and activation of proteins which then activate effectors
  • Other enzymatic domains exist besides kinase
  • Insulin receptors, IGF-1, cytokines, and growth promoting hormones and factors
20
Q

Nuclear Receptors

A
  • Transcription factor receptors
  • Located in the cytoplasm, but after the ligand binds they translocate to the nucleus
  • Steroids and thyroid hormones
21
Q

Receptor subtypes

A
  • Endogenous neurotransmitters often bind to more than one type of receptor
  • The same signaling molecular can then cause different effects or have different affinity in different tissues or species
22
Q

What is receptor up-regulation?

A

An increase in the number of receptors (and the drug effect)

23
Q

What is receptor down-regulation?

A

A decrease in the number of receptors and therefore a reduction in effect

  • Can be achieved internalizaing the receptors in lysosomes, recycling them, sequestering, or degrading

_ May play a part of developing TOLERANCE

24
Q

What is the general term for anything that binds to a recognition site?

A

Ligand

25
Q

What are the three types of ligands?

A

Agonist
Antagonist
Mixed agonist-antagonist

26
Q

What mimics the effect of the endogenous ligand?

A

Agonist

27
Q

What are the three types of agonist?

A

Full
Partial
Reverse

28
Q

What type of agonist binds to the receptor and elicits a MAXIMAL response?

A

Full agonist

29
Q

Partial agonist

A

Binds to the receptor but does not cause as much effect as a full agonist but does prevent anything else from binding to the receptor while it is there.

30
Q

What type of agonist binds and produces the opposite effects as the endogenous ligand would?

A

Reverse/Inverse agonist

31
Q

Antagonist

A

Binds to the receptor but does nothing on its own, however it prevents an agonist from binding and blocks the receptor.

32
Q

What is the most common form of antagonism?

A

Competitive

33
Q

What is competitive antagonism?

A

When the antagonist ligand binds and releases as long as it is present and so if the antagonist is present as well as an agonist they will compete for the binding

Reversible or irreversible, concentration- dependent binding

34
Q

Non-competitive antagonsim

A

Refers to a ligand that interacts somewhere other than the receptor but causes a change in the receptor that blocks its ability to bind the normal ligand.

35
Q

What are the type of non-receptor antagonism?

A

Chemical antagonism
Pharmacokinetic antagonism
Physiologic antagonism

36
Q

Mixed agonist-antagonist

A

Acts as an agonist in one type of receptors and as an antagonist on the other type of receptors.

37
Q

Efficacy

A

Maximal effect a drug can have

38
Q

Potency

A

Comparison of the concentration of two drugs needed to induce the same magnitude effect

39
Q

Generally the _____ will account for the potency of the drug.

A

dose

40
Q

Can a partial agonist be more potent than a full agonist?

A

Yes

41
Q

Effective concentration (EC50)

A

concentration at which a drug produces 50% of its maximal effects

in-vitro preparations

42
Q

Effective dose (ED50)

A

Dose that produces a result (usually the desired effect) in 50% of the animals

relates to population

in-vivo

43
Q

Therapeutic index

A

Ratio of LD50 to ED50

44
Q

A high therepeutic index indicates a _____ (safe/unsafe) drug.

A

Safe

45
Q

T/F: A low therepeutic index indicates a safe drug.

A

False

46
Q

Onset of action (latent period)

A

The time required after drug administration for a response to be observed

47
Q

Duration of action

A

The length of time that a drug is effective

Pharmacology Exam 1 (8 decks)

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