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CPR II > (6) DSA | Intro to Pharmacodynamics (Konorev) > Flashcards

(6) DSA | Intro to Pharmacodynamics (Konorev) Flashcards

1
Q

Define:

Pharmacokinetics

A

Effect of the BODY on drugs

ADME

  • Absorption
  • Distribution
  • Metabolism
  • Elimination
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2
Q

Define:

Pharmacodynamics

A

Effects of DRUGS on the body

  • Drug receptors
  • Dose-response curves
  • Mechanisms of drug actions
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3
Q

Define:

A Receptor

A

A specific molecule in a biological system that plays a regulatory role

The receptor interacts with a drug and initiates the biochemical events leading to drug effects

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4
Q

Define:

Inert binding site

A

A compontnet of the biologic system to which a drug binds without changing any function

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5
Q

Define:

Ligand

A

A ligand is a molecule, such as a hormone or a drug, which binds to a receptor

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6
Q

Describe the “lock and key” model of ligand receptor interaction

A
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7
Q

Types of Drug-receptor interactions

Describe: Covalent bonds

A

Irreversible

Drug removal/receptor reactivation requires re-synthesis of the receptor or enzymatic removal of the drug

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8
Q

Types of Drug-receptor interactions

Describe: Non-covalent bonds

A

Reversible

Most drugs bind to receptors via non-covalent bonds

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9
Q

Rank the following types of bonds from WEAKEST to STRONGEST

Hydrophobic interactions

Ionic bonds

Hydrogen bonds

A

Weakest = Hydrophobic interactions

Middlest :) = Hydrogen bonds

Strongest = Ionic bonds

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10
Q

What are the three parameters that describe the interaction of a drug with a receptor?

A
  • Affinity
  • Selectivity
  • Intrinsic activity
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11
Q

What is affinity of a drug?

What does high vs low affinity mean?

A

The affinity of a drug for a receptor describes how readily and tightly that drug binds to its receptor

High affinity= good drug-receptor interaction; LESS drug needed to produce a response

Low affinity= poor drug-receptor interaction; MORE drug needed to produce a response

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12
Q

What is the parameter that describes the affinity?

A

KD

(equilibrium dissociation constant)

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13
Q

Define KD

What are the units?

A

Drug concentration at which 50% of the drug receptor binding sites are occupied by the drug

Molar concentration

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14
Q

What does a LOW KD mean?

A

The lower the KD …

The higher the affinity of a drug for a receptor

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15
Q

What does a high KD mean?

A

The higher the KD …

The LOWER the affinity of a drug for a receptor

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16
Q

What is the equation for calculating KD?

A

[L] = ligand

[R]= receptor

[LR] = ligand-receptor complex

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17
Q

What is drug selectivity?

A

A property of a drug determined by its affinities at various binding sites

*A MORE selective drug would affect fewer targets over a specific concentration range

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18
Q

What is instrinsic activity?

A

The ability of a drug to change a receptor function and produce a physiological response upon its binding to a receptor

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19
Q

What is an agonist?

A

Bind the receptor and stabilize it in a particular conformation (usually the active conformation) producing a physiological response

*HAS intrinsic activity

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20
Q

What is an antagonist?

A

Bind to the receptor but do NOT CHANGE ITS FUNCTION

However, they prevent activation of the receptor in the presence of an agonist

**DO NOT have intrinsic activity

21
Q

What are the three types of agonists?

A

Full agonists

Partial agonists

Inverse agonists

22
Q

What do full agonists do?

A

FULLY activate receptors

Produce max. pharmacological effect when all receptors are occupied

Maximal intrinsic activity

23
Q

What do partial agonists do?

A

PARTIALLY activate the receptor upon binding

Produce a sub-maximal pharmacological effect when all receptors are occupied

24
Q

What do inverse agonists do?

A

Produce an effect OPPOSITE to a full or partial agonist

  • Decrease receptor signaling
  • Intrinsic activity is present and related to the inhibition of receptor function
25
Q

Graphically, depict the response levels of

Full agonist

Partial agonist

Antagonist

Inverse agonist

A
26
Q

What are the three types of antagonism?

A

Pharmacologic

Chemical

Physiologic

27
Q

Describe:

Pharmacologic antagonism

A

aka Receptor antagonism

Action at the same receptor as endogenous ligands or agonist drugs

28
Q

Describe:

Chemical antagonism

A

When chemical antagonist makes the other drug unavailable

29
Q

Describe:

Physiologic antagonism

A

Occurs between endogenous pathways regulated by different receptors

30
Q

Describe a:

Competitive antagonist

A

COMPETES with endogenous chemicals or agonist drugs for binding of the receptor

31
Q

Describe a:

Non-competitive antagonist

What subtypes does this include?

A

Receptor inactivation is not surmountable

Irreversible antagonists= irreversibly bind to and occlude the agonist site on the receptor by forming covalent bonds

Allosteric antagonists = bind to a site other than the agonist site to prevent or reduce agonist binding or activation of the receptor

32
Q

Describe the agonist effect (E) vs agonist concentration (EC) relationships graphically for:

Competitive antagonism

Noncompetitive antagonism

A
33
Q

What is a dose-response curve?

A

Graphic representation of the relationship between a drug and its effects

34
Q

When you plot drug dose arithmetically on the x-axis vs drug effect on the y-axis, you get a ___________

A

Hyperbolic curve

35
Q

When you present the dose-response curve as graphing the logarithm of the drug dose vs the respone, you’ll get a __________

A

Sigmoidal curve

36
Q

What is the:

Emax

ED50

Within a dose-response curve?

A

Emax= the maximal effect thta can be produced by the drug

ED50 = Effective dose, the dose that produces 50% of it’s maximal effect

37
Q

What questions does a graded response answer?

A

“How much?”

38
Q

What questions does a quantal response answer?

A

[All or none; yes-no; “binary” responses]

“Does the response occur or not?”

“In how many?”

39
Q

Describe what a non-cumulative quantal dose response curve looks like:

What information does it include?

A

Number or % of individuals responding at a dose of a drug and ONLY AT THAT DOSE

40
Q

Describe what a cumulative quantal dose response curve would look like:

What information is contained here?

A

Number or % of individuals responding at a dose of a drug AND at all doses loer than that dose

41
Q

Define:

ED50

TD50

LD50

A

ED50= median effective dose

TD50= median toxic dose

LD50 = median lethal dose

42
Q

How do you claculate the therpeutic index?

What does a HIGH TI mean?

A

Therapeutic Index (TI) : TD50/ED50

**The higher the TI, the SAFER the drug

43
Q

Define:

Therapeutic window

A

The range of doses of a drug or of its concentration in a bodily system that provides for the safe and effective therapy

44
Q

Define:

Potency

A

The amout of drug required to produce specific pharmacological effect

45
Q

Define:

Efficacy

A

The maximal pharmacological effect that a drug can produce

46
Q

What are the major classes of drug targets?

A

Membrane receptors

Nuclear receptors

Ion channels

Transport proteins

Enzymes

47
Q

What do protein kinases do?

A

Modify protein by covalently attaching a phosphate group to an amino acid residue

48
Q

What are the effects of the following G protein subclasses?

Gs

Gi

Gq

G12/13

A

Gs = activates all isoforms of adenylyl cyclase

Gi = inhibits adenylyl cyclase

Gq = activates phospholipase C

G12/13 = activates Rho GTPases

49
Q

Note: didn’t include the rest of the DSA info because it’s all biochem review

A

CPR II (30 decks)

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