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Pharm 2014 Unit 1 > Lecture 1: Basic Principles of Pharmacology I > Flashcards

Lecture 1: Basic Principles of Pharmacology I Flashcards

1
Q

What is pharmacokinetics?

A

Time course of drug absorption, actions, and elimination. (What the body does to the drugs.)

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2
Q

What is pharmacodynamics?

A

Types of drug actions (What the drugs do to the body.)

  1. Physiochemical actions (simple chemical interactions)
  2. Receptor interactions
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3
Q

What do Drug - Receptor interactions cause?

A

Cause molecular events to occur in each cell - enough of the events cause a change in cell function –> ultimately resulting in a change in tissue function.

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4
Q

Name two types of drug - receptor bonds.

A
  1. Reversible: ionic, Van der Waals, Hydrogen

2. Irreversible: covalent

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5
Q

Explain Receptor Theory.

A

The structure of the drug determines how it will fit into the receptor. The better the fit, the better the stimulation. Subtle changes in structure amongst a class of drugs can greatly influence the drugs’ effects.

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6
Q

Explain how agonist drugs work.

A

They bind to the receptor and produce a pharmacologic effect. (Activate receptor after binding.)

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7
Q

Explain how different agonists work on the log dose response graph.

A

All achieve the same Emax (Vmax) at different doses.

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8
Q

What are the two ways of quantifying agonism?

A
  1. Efficacy

2. Potency

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9
Q

What is efficacy?

A
  1. The ability of the drug to activate the effector portion of the receptor once the drug is bound to the receptor.
  2. Depends upon the structure of the drug
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10
Q

(First Aid) What is the significance of efficacy?

A
  1. Equals to Vmax or Emax

2. Non-competitive inhibitors reduce efficacy (change y-axis)

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11
Q

What is potency?

A
  1. Relates to the amount of drug that is needed for an effect
  2. Depends on the
    1) The biologic system
    a. receptor density
    b. efficiency of the stimulus-response mechanisms of the tissue
    2) Interaction of the drug with the receptor
    a. affinity
    b. efficacy
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12
Q

(First Aid) What is the significance of potency?

A
  1. Associated with Km (low Km = high potency)

2. Competitive inhibitors will reduce the potency

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13
Q

(First Aid) Explain efficacy.

A
  1. Maximal effect a drug can produce

2. High-efficacy drug classes are analgesic (pain) medications, antibiotics, antihistamines, and decongestants.

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14
Q

(First Aid) Explain potency.

A
  1. The amount of drug needed for a given effect
  2. Increased potency means increased affinity for receptor.
  3. Highly potent drug classes include chemotherapeutic (cancer) drugs, antihypertensive (blood pressure) drugs, and antilipid (cholesterol) drugs.
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15
Q

How do antagonists work?

A
  1. Antagonists can block the binding of agonists and prevent the pharmacologic response.
  2. Many things are learned about the structure and function of receptors from the use of antagonist
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16
Q

What are some of the agents used as antagonists as therapeutic agents to slow the system down?

A

Paralytic agents

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17
Q

What is the characteristics of competitive antagonists.

A

Antagonist effect can be overcome by increasing the does of the agonist.

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18
Q

What is the characteristics of noncompetitive antagonists?

A
  1. Can’t be overcome by increasing doses of agonist

2. Receptors remain occupied by antagonist and not enough DR interactions occur to achieve Emax.

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19
Q

(FA) Explain Km, Vmax.

A
  1. Km reflects the affinity of the enzyme for its substrate.
  2. Vmax is directly proportional to the enzyme concentration.
  3. Lower the Km higher the affinity
20
Q

(FA) What happens when you add a competitive antagonist on the dose respond curve?

A
  1. Shifts curve to right –> Reduce potency, No change in efficacy
21
Q

(FA) What are some examples of adding competitive antagonists to an agonist?

A

Diazepam + flumazenil on GABA receptor

flumazenil is a competitive antagonist at GABA benzodiazepine receptor

22
Q

(FA) What is the effect of noncompetitive antagonist on the dose respond curve?

A

Shifts curve down –> Reduced efficacy

23
Q

(FA) What is an example of noncompetitive antagonist?

A

Norepinephrine + phenoxybenazmine on alpha receptor (phenoxybenzamine is a nonselective, irreversible alpha blocker)

24
Q

(FA) What is the effect of partial agonist on the does respond curve?

A
  1. Acts at the same site as full agonist, but with reduced maximal effect –> reduced efficacy.
  2. Potency is a different variable and can be increase or decrease
25
Q

(FA) What is an example of a partial agonist?

A

Morphine + buprenorphine at opioid u-receptor

26
Q

(FA) What are the receptors for G-protein-linked 2nd messengers? (G-protein class)

A
  1. alpa1, alpha2, beta1, beta2 (q, i, s, s) –> sympathetic
  2. M1, M2, M3 (q, i, q) –> Para-sympathetic
  3. D1, D2 (s, i) –> Dopamine
  4. H1, H2 (q, s) –> Histamine
  5. V1, V2 (q, s) –> Vasopressin
27
Q

(FA) Mnemonics for G-protein class?

A

Qiss (kiss) and qiq (kick) till you’re siq (sick) of sqs (sex).

28
Q

(FA) H1, alpha 1, V1, M1, M3 (HAVe 1 M&M)

A

Gq –> Phospholipase C –> PIP2 –> DAG (Protein Kinase C) & IP3 (Increased intracellular Ca2+)

29
Q

(FA) B1, B2, D1, H2, V2

A

Gs –> Adenylyl cyclase –> cAMP –> Protein kinase A –> Increased intracellular Ca2+ in the heart

30
Q

(FA) M2, alpha2, D2 (MAD 2’s)

A

Gs –> Adenylyl cyclase –> cAMP –> Protein kinase A –> Increased intracellular Ca2+ in the heart

31
Q

What is drug action?

A

Molecular action - invisible

32
Q

What is selectivity?

A

property of drug to cause a specific effect, few drugs produce a single effect

33
Q

Pharmacokinetic deals with

A

dosing and elimination of drugs

34
Q

Pharmacodynamic deals with

A

effects of the drugs on the body

35
Q

Increased cGMP and cAMP via intracellular signaling leads to muscle ( )

A

relaxation (NO via cGMP, B2 via cAMP)

36
Q

How does Angiotensin II work?

A

Increase IP3 –> increase Ca2+ intracellular conc –> smooth muscle contraction

37
Q

How does NE via adrenergic nerve work via intracellular signaling?

A

Alpha 1 receptor –> increase IP3 –> increase Ca2+ intracellular conc –> smooth muscle contraction

38
Q

Explain how Gs coupled receptor work

A

once ligand is bound, ATP –> cAMP

39
Q

Explain how Gq coupled receptor work

A

Phospholipase C –> PIP2 produces DAG and IP3

40
Q

What is “Intrinsic Activity?”

A
  1. Ability to stimulate the receptor once bound.

2. Relates to structure and influences efficacy and potency.

41
Q

Greater intrinsic activity means

A

greater efficacy

42
Q

(Check with notes) Hypersensitivity can occur

A

with antagonist (example: sudden withdrawal of beta blocker

43
Q

Desensitivity can occur

A

with agonist

44
Q

Efficacy is depend on

A

the structure of the drug

45
Q

Potency is depend on

A
  1. The biologic system
    a. receptor density
    b. efficiency of the stimulus-response mechanisms of the tissue
  2. Interaction of the drug with the receptor
    a. affinity
    b. efficacy

Pharm 2014 Unit 1 (13 decks)

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