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POM Final > Introduction to Pharmacodynamics > Flashcards

Introduction to Pharmacodynamics Flashcards

1
Q

Almost all drug targets are…?

A

Proteins

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2
Q

How does an Agonist drug function?

A

Mimics the effects of the endogenous agonists

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3
Q

How does an antaonist drug function?

A

Blocks the effects of endogenous agonists

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4
Q

Drug-receptor interaction equation

A

Reversible reaction

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5
Q

What is the dose-response curve?

A

Shows relationship between ligand/drug concentration and receptor occupancy

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6
Q

What is Kd?

A

The dissociation constant; the concentration of drug at which 50% of receptors are occupied; lower Kd = greater affinity

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7
Q

What is the Hill-Langmuir equation?

A

Describes drug affinity curves; Y = [D] / Kd + [D]

Y = % occupancy

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8
Q

Potency Vs. Efficacy

A

Potency is dependent on receptor affinity; lower Kd = more potent

Efficacy describes the response

Do not always correlate; receptor occupancy does NOT equal effect

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9
Q

Signal amplification

A

affects how we interpret dose response curves; Maximal cellular response at less-then-maximal receptor occupancy

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10
Q

What is the “Receptor reserve”?

A

Receptors that are available for agonist binding, but that are not necessary for maximal effect

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11
Q

Competitive vs. Non-competitive Antagonists

A

Competitive: compete for same site; decrease potency (increse Kd); moves curve to the right

Non-Competitive: bind different sites; can be irreversible; decrease efficacy; moves curve down

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12
Q

Full vs. Partial agonists

A

Full: elicits maximal response from receptor

Partial: elicits sub-maximal response from receptor

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13
Q

What is a neutral antagonist?

A

Reduces the effect of an agonist, but has no effect itself

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14
Q

What is an inverse agonist?

A

They inhibit the basal activity of a receptor in the absence of the normal agonist; they are NOT antagonists because they are not competing with endogenous agonist

Can be competitive antagonists TOO if they bind to same receptor site as endogenous agonist

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15
Q

5 clinically-relevant inverse agonists/antagonists

A
  1. Metoprolol (β1-adrenergic receptor antagonist); Cardio – Hypertension, angina, congestive heart failure
  2. Losartan (angiotensin II receptor antagonist); Cardio - Hypertension
  3. Famotidine (H2-histamine receptor antagonist); GI – GERD, gastric/duodenal ulcers
  4. Risperidone (D2-dopamine receptor antagonist); Neuro – Schizophrenia, bipolar disorder, autism
  5. Naloxone (m-opioid receptor antagonist); Neuro – Emergency treatment for heroin/opioid overdose
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16
Q

Drugs for treating opioid addiction/overdose

A

Not full-agonists at the m-opioid receptor (MOR)

  1. Full agonists: Endorphins, Morphine, Heroin
  2. Partial agonists: Bupenorphine, Nalbuphine
  3. Neutral antagonist: Naltrexone
  4. Inverse agonist: Naloxone
17
Q

Dose-response curves are useful for describing effects that are:

A

Continuous; reduction of pain, BP, anxiety, etc.

18
Q

Dose-response curve for quantal variable

A

The curves shows the % of patients responding; cumulative % of patients exhibiting the therapeutic effect

19
Q

Dose-response curve y-axes (6)

A
  1. Receptor occupancy
  2. Activation of intracellular signaling intermediate
  3. Cell-level physiological effect
  4. Organ-level physiological effect
  5. Organ-system-level physiological effect
  6. Patients responding
20
Q

Drug effects

A

Therapeutic Effect (ED50)

Toxic Effect (TD50)

Lethal Effect (LD50)

21
Q

Therapeutic window and Index

A

The range of drug concentrations between the minimum effective dose and the minimum toxic dose

TI = TD50/ED50 or LD50/ED50; higher is better

22
Q

Why might the shape of the dose-response curve be different for the therapeutic vs. toxic effects?

A

Because different receptors may account for the therapeutic and toxic effects

23
Q

What is the certain safety factor (CSF)?

A

CSF = LD1/ED99

Higher is better

Important for off-target toxicity

24
Q

Synergism, additivity, and antagonism

A

When two drugs have the same therapeutic effect

25
Q

Potentiation

A

When one drug has a therapeutic effect, and a second drug helps it

Probenecid has no antibiotic effect of its own, but potentiates the effect of the antibiotics (Cephalosporins, penicillins in serum) –> causes increased serum [drug] & prolonged therapeutic effect

26
Q

Tolerance/Desensitization

A

Reduced effect with continued use of a drug; Short-term: tachyphylaxis

  1. receptor inactivation
  2. receptor internalization
  3. receptor down-regulation

POM Final (5 decks)

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