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MTP > Exam 2: Prodrugs > Flashcards

Exam 2: Prodrugs Flashcards

1
Q

What is a prodrug?

A

A pharmacologically inactive compound that is converted into an active drug by a metabolic biotransformation

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2
Q

What is the difference between a pro and soft drug?

A

Pro: inactive compounds metabolized to active form

Soft: pharmacologically active metabolized to promote excretion

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3
Q

What is drug latentiation?

A

A prodrug after administration is expected to be appropriately metabolized to the active form

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4
Q

What are the 2 classes of drug latentiation?

A
  1. Carrier-linked prodrug
  2. Bioprecursor prodrug
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5
Q

What are carrier-linked prodrugs?

A

Contains an active drug linked to a carrier group that can be removed enzymatically such as an ester

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6
Q

What are subclasses of carrier-linked prodrugs?

A
  1. Bipartate prodrug
  2. Tripartate prodrug
  3. Mutual prodrug
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7
Q

What is a bipartate prodrug?

A

Comprised of one carrier attached to one drug

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8
Q

What is a tripartate prodrug?

A

Comprised of a carrier attached to a linker that is attached to the drug

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9
Q

What is a mutual prodrug?

A

Consists of two, usually synergistic, drug attached to each other

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10
Q

What is an example of a tripartate-mutual prodrug?

A

Etofibrate

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11
Q

What are bioprecursor prodrugs?

A

Consists of a compound that is metabolized by molecular modification into a new compound which is the active principle drug or is metabolized further to the active drug

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12
Q

What is a hard drug?

A

Nonmetabolizable drug charactered by either high lipid solubility and accumulation in adipose tissues and organelles or high water solubility

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13
Q

Why are hard drug poor substrates for metabolism?

A

Can be sterically hindered or the hydrogen atoms are substituted with halogens that block oxidation

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14
Q

What are soft drugs?

A

Biologically active drugs designed to have predictable and controllable metabolism to nontoxic and inactive products after they have achieved their desired pharmacological effect

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15
Q

What are the advantages of soft drugs?

A
  1. Elimination of toxic metabolites, increases the therapeutic index
  2. Avoidance of pharmacologically active metabolites
  3. Elimination of drug-drug interactions
  4. Simplification of pharmacokinetics problems
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16
Q

What are prodrug utilized for?

A
  1. Aqueous solubility
  2. Absorption and distribution
  3. Site specificity (toxicity)
  4. Instability
  5. Prolonged release
  6. Toxicity
  7. Poor patient acceptibility
  8. Formulation problems
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17
Q

Why is the purpose of aqueous solubility of a drug?

A

Least water soluble is poor bioavailability

18
Q

Why is bioavailability important?

A

For drug’s absorption and distribution

19
Q

In what ways are prodrugs desired depending on the desired site of action?

A
  1. Plasma proteins effect drug binding
  2. Drugs are designed to enhance or reduce plasma protein binding which will determine tissue site and penetration
20
Q

Why is site specificity important for prodrug manufacturing?

A
  1. High concentrations of an enzyme can cleave the prodrug moieties to unmask the active drug
  2. Prodrug functionality can direct the drug to particular target tissue
21
Q

What causes instability of a drug?

A

Rapid metabolism that doesn’t give a the drug enough time to have a pharmacological effect

22
Q

How do prodrugs prevent rapid metabolism?

A

By blocking initial sites of metabolism

23
Q

Why are prodrugs used for prolonged release?

A

Has the ability to convert an active molecule with a short half-life or duration of activity into an extended release prodrug

24
Q

Why is it important for a pro drug to be slowly converted to active form?

A

Enables the desired drug to be released at a steady low concentration over a longer period of time

25
Q

Why do prodrugs need to overcome toxicity?

A

Some active forms have undesirable toxicity

26
Q

What makes drug have a higher therapeutic index?

A

They are administered as nontoxic prodrugs that are converted to their active forms only at the site of action

27
Q

Why is clindamycin given as prodrug?

A

Causes pain on injection and painful

28
Q

What makes the prodrug better?

A

Aqueous solubility (Prednisolone)

29
Q

What makes the prodrug better?

A

Aqueous solubility (methprednisone)

30
Q

What makes the prodrug better?

A

Flucocinolone needs to be more lipophillic to penetrate the skin better

31
Q

What makes the prodrug better?

A

Epinephrine is made to more lipopphillic to penetrate cornea (Dipivefrin)

32
Q

Compare these 2 drugs and their site of action

A

Oxyphenisatin (rectal) not as water soluble than Acetate (Intestine)

33
Q

What makes the prodrug better?

A

Propranalol: increased biovailabilty and stability because of hydrophilicity

34
Q

What makes the prodrug better?

A

Naltrexone: increased biovailabilty and stability because of hydrophilicity

35
Q

What makes the prodrug better?

A

Haloperidol: Increased lipophilicity causing prolonged release

36
Q

What makes the prodrug better?

A

Fluphenazine: Increased lipophilicity causing prolonged release

37
Q

What makes the prodrug better?

A

Epinephrine has adverse side effects, Dipivefrin: limited systemic effect because small dose absorbed in eye due to increase lipophilicity

38
Q

What makes the prodrug better?

A

Aspirin: decreased toxicity by making it hydrophillic and absorbed into gastric environment better, decreasing dose

39
Q

What makes this prodrug better?

A

A tasteless prodrug for pediatrics

40
Q

What makes this prodrug better?

A

Rapid hydrolysis to active form (well-tolerated)

41
Q

What makes this a better drug than formaldehyde?

A

More stable

42
Q

What makes these two drugs different?

A

Left: soft drug

Right: hard drug from EWG Cl-

MTP (15 decks)

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