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Fall Pharm > Basic Principles of Pharm part 2 > Flashcards

Basic Principles of Pharm part 2 Flashcards

1
Q

Agonist Mimics

A

Has the same effect as the agonist on the receptor, but works somewhere else (see explanation/picture in lecture 2 at 0:04:15)

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2
Q

Irreversible antagonist

A

Covalently bind to receptor and do not come off. The only way to get rid of it is to get rid of that receptor. Can be allosteric or orthosteric.

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3
Q

Partial agonist

A

Will bind to the active site and elicit a partial response. They compete for the same active site as a full agonist. (see lecture 2 @ 0:12:27)

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4
Q

How can a partial agonist act as an antagonist?

A

The full and partial agonists compete for the same site. If the partial agonist takes up the receptor sites, it is not allowing the full agonist to bind therefore, you don’t have the max response you could have.

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5
Q

Partial agonist by itself VERSUS partial agonist in presence of full agonist

A

Partial is an agonist by itself.

Partial is an antagonist in the presence of a full agonist.

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6
Q

Opposite charge antagonist example

A

Heparin (-) binds to Protamine (+) rendering heparin ineffective (has nothing to do with binding to receptors, has everything to do with drug-to-drug interaction in bloodstream)

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7
Q

Physiologic antagonism

A

Drugs acting at different receptors that counter act each other (ex: Epi binding to Beta and acetylcholine binding to muscarinic)

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8
Q

Receptor configuration: unbound

A

Ri (inactive) Ra (active)

can switch on and off spontaneously

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9
Q

Receptor configuration: bound with agonist

A

Ri –>Ra

favors active state

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10
Q

Inverse agonist (and example)

A

Ri

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11
Q

Sympathetic nervous system (SNS)

A

Fight or flight

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12
Q

Parasympathetic nervous system (PSNS)

A

Rest and digest

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13
Q

Factors that determine the duration of a drugs effects:

A
  • As long as the drug stays bound to receptor.
  • If a drug initiates the production of a protein, it will take longer to see effects and longer for response to stop.
  • Receptor is degraded (in covalent bonding)
  • Desensitization
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14
Q

Good receptor properties:

A
  • Selective

- Alteration

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15
Q

Bad receptor properties:

A
  • “Inert binding sites” (non-selective)

- Drug carriers (don’t elicit a response)

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16
Q

Potency

A

A drug is potent when it requires a very low dose to elicit 50% of that drugs maximal effect (Or its EC50).

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17
Q

If a drugs EC50 is low..

A

..the drug is very potent.

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18
Q

Efficacy

A

The maximal response you will see from a particular drug (see lecture 2 at 0:33:05)

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19
Q

ED50

A

Median effective dose

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20
Q

TD50

A

Median toxic dose

21
Q

LD50

A

Median lethal dose

22
Q

EC50 vs ED50

A

EC50: The concentration of drug in blood.
ED50: The actually dose being given.

23
Q

Therapeutic index

A

Establishes the margin of safety of a drug.

TD50/ED50

24
Q

The higher the Therapeutic Index..

A

..the safer the drug.

25
Q

Idiosyncratic

A

means we don’t know why one patient responds differently to a drug than another patient

26
Q

Tolerance

A

Response changes over the course of time

27
Q

Tachyphylaxis

A

Quick tolerance

28
Q

Causes of variation:

A
  • Alteration in concentration of drug that actually reaches the receptor (rate of absorption/distribution/clearance, age, weight, sex, disease state)
  • Concentration of endogenous ligand (maybe affected by health or disease
  • Alteration in function and number of receptors
  • Changes in components of response distal to receptor (largest and most important cause)
29
Q

Toxic effects

A

Some drugs produce both desired and adverse effects at the same receptor. other drugs bind to different classes or receptors

30
Q

Pharmacokinetics: ADME:

A

Absorption
Distribution
Metabolism
Elimination

31
Q

4 main ways a drug will permeate through the body:

A 
Aqueous diffusion
Lipid diffusion
Special carriers
Endocytosis and exocytosis
(*all of these depend if drug is charged/uncharged and size)
32
Q

Aqueous diffusion

A

Larger aqueous compartments in body (ex: blood)
Cells may have aqueous channels
Diffusion by concentration gradient
Molecules can be large

33
Q

Not aqueous diffusion

A

Highly charged molecules

Bound to large proteins (carriers)

34
Q

Lipid diffusion

A

Easiest to cross barriers

example: gases

35
Q

Special carriers

A

Protein that will bind to a drug and move it from one area to another.
Use active transport (energy required) or facilitated diffusion

36
Q

In Fick’s law of diffusion, flux is…

A

..how fast a drug will move from one side of a barrier to another

37
Q

Flux is largely dependent on..

A

..concentration gradient.

38
Q

If the concentration of one side of a barrier is significantly more than on the other side, what will happen to the flux? (Fick’s law)

A

The flux will be very large

39
Q

If the surface area of a barrier is very large, what will happen to the flux? (Fick’s law)

A

The flux will be very large

40
Q

If a barrier is very thick, what will happen to the flux? (Fick’s law)

A

The flux will be very small

41
Q

Endocytosis

Exocytosis

A

Membrane engulfment of molecule
Can be receptor mediated
Slow process
Very large or charged molecules

Merging of vesicle with membrane

42
Q

Henderson Hasselbach Equation

A

pH= pKa + log [A-]/[HA]

43
Q

If pH = pKa..

A

..the ratio of ionized versus unionized is equal

44
Q

If pH < pKa..

A

..favors protonated form

45
Q

If pH > pKa..

A

..favors un-protonated form

46
Q

What part of the kidneys are most drugs filtered at?

A

Glomerulus

47
Q

Concentration of drug in renal tubules is dependent on what?

A

pH

48
Q

“Trapping” drugs in urine:

Weak acids excreted faster in..

A

Alkaline urine

49
Q

“Trapping” drugs in urine:

Weak bases excreted faster in..

A

Acidic urine

Fall Pharm (8 decks)

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