Exam 4 Flashcards

1
Q

What is drug affinity?

A

How well the drug binds to the receptor

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2
Q

What is drug efficacy?

A

How well the drug produces the desired effect

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3
Q

What is drug potency?

A

Compares the relative affinity of a drug to a receptor compared to other drugs
Drug must out compete the native ligand to induce an effect

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4
Q

Where do most drugs fail during development?

A
  • Most drugs fail during the discovery phase
  • ~90% of all drugs fail in clinical testing (1:10,000 success rate)
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5
Q

What is the Lipinski Rule of 5?

A
  • Tool used to measure a new chemical entity (NCE) bioavailability
    Rules:
    1. < 10 hydrogen bond donors (NH, OH) or acceptors (N, O)
    2. < 500 Da molecular weight
    3. < 5 Calculated partition coefficient (cLogP)
    4. Not more than 1 toxicophore
    Violation of more than one rule predicts the NCE non-orally available
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6
Q

What do hydrogen bonds bind to on a receptor?

A

Polar, acidic, and basic groups

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7
Q

Determine the various intermolecular forces for Dibucaine?

A
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8
Q

What are the structural alert drugs and there strucure?

A

Napthelene is the only polycyclic aromatic that is ok
Thiophenes are bad due to sulfur oxidation

NAP AT night

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9
Q

What is the measure of a dalton?
What is considered a “small” drug?

A
  • Da = g/mol
  • 500 da or less
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10
Q

Define an acid and base (Bronsted-Lowry)?

A
  • Acid - proton donor
  • Base - proton acceptor
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11
Q

Determine the acid, base, conjugate acid, and conjugate base of the following reaction?

A
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12
Q

Determine the acid, base, conjugate acid, and conjugate base of the following reaction?

A
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13
Q

Define amphoteric and what compound has this property?

A

Amphoteric means a compound can act as an acid or a base like water

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14
Q

What defines a strong acid? weak acid?
What are the strong acids?

A

Stong acids completely ionize in water
Weak acids partially ionize in water

Bring Clean ClOthes If NOt Swimming

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15
Q

What defines a strong base? weak base?
What are the strong bases?

A

Strong bases completely ionize in water
Weak bases partially ionize in water

LiNK BaCS

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16
Q

What do the equilibrium arrows favor in a reaction?

A

Favors the formation of a weaker acid

17
Q

What is the pH equal to for strong acids and bases?

A

Strong acids: pH = -log[H3O+]
Strong bases: pH= 14 - -log[OH-]

18
Q

Calculate the pH of 1.50 x 10^-3 M HCl?

A

pH = 2.82

19
Q

Calculate the pH of 2.62 x 10^-5 M HCl?

A

pH = 4.58

20
Q

Calculate the pH of 3.51 x 10^-2 M NaOH?

A

pH = 12.55

21
Q

Calculate the pH of 5.25 x 10^-6 M Ca(OH)2?

A

pH = 9.02

22
Q

What should you consider when looking at a change in pH?

A

The pH scale is logarithmic and a change of 1 is actually a change by a factor of 10

23
Q

What ist the true view of the strength of an acid?

A

The ability of the acid to give up its proton
Stong acids readily give up their proton

24
Q

How do we determine how readily an acid will give up its proton?
What does this information mean?

A
  • By its Ka (acid-dissociation constant), = [products]/[reactants]
  • The larger the Ka the easier it is to remove the proton and therefore more acidic
25
Q

What is the range for pH and pKa?
What is the pKa of water?

A
  • pH = 0-14
  • pKa = -20 - 60+
  • pKa H20 = 16
26
Q

How do you calculate the pH of a weak acid?

A

Weak acids do not dissociate completely so we must calculate the pH of the equilibrium concentration
Complete the ICE table and then plug the numbers into the Ka formula ([products]/[reactants]).
This gives you [H30+], then take -log to obtain pH.

27
Q

How do you calculate the pH of a weak base?

A

The same method as weak acid calculations
Remember, this calculation gives you [OH-], so you must take the -log[OH-] to get pOH and subtract that number from 14 to obtain the pH

28
Q

What is the pH of 1.20 M soulution of acetic acid (weak acid, Ka= 1.4 x 10^-5)?

A

pH = 2.39

29
Q

What is the pH of 0.00250 M solution of morphine (weak base, Kb= 1.6x10^-6)?

A

pH = 9.80

30
Q

What is a buffer?

A

Solutions that contain a weak acid and its conjugate base or a weak base and its conjugate acid
Buffers resist change in pH when strong acids or bases are added up until buffering capacity is exceeded.

31
Q

What are the 3 main buffering systems in the body?

A
  1. Bicarbonate
  2. Phosphate
  3. Protein
32
Q

What is Le Chatelier’s Principle?

A

When a system is at equilibrium is disturbed, the system will adjust to reestablish that equilibrium.

33
Q

What is the bicarbonate buffering system equation?

A
34
Q

What anesthetic is a weak base?
What is important about this property?

A
  • Most local anesthetics
  • Drugs with a pKa closer to normal pH are usually lipid soluble and unionized, this allows this to better cross the axonal membrane and initate their effects
35
Q

How do you determine % ionization?

A

(ionized ion/total ions) x 100