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[Ther 201] 1st Exam Transes > Bioavailability and Bioequivalence (Leonila Estole-Casanova, MD) > Flashcards

Bioavailability and Bioequivalence (Leonila Estole-Casanova, MD) Flashcards

1
Q

Define: Bioavailability

A

Extent to which an active pharmaceutical agent is absorbed unchanged and becomes available in general circulation

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2
Q

When are two substances bioequivalent?

A
  1. Pharmaceutically equivalent or alternatives
  2. Similar Cmax, Tmax and AUC after administration of same molar dose under same conditions
  3. Essentially same effects
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3
Q

What is an important assumption with bioavailability?

A

Amount of drug reaching plasma is the amount that reaches the target site

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4
Q

What are the two types of bioavailability?

A

Absolute

Relative

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5
Q

How is absolute bioavailability derived?

A

Comparison of AUCs of extravascular and IV administration

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6
Q

T/F: If the drug is administered by IV, the F is 1.

A

True

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7
Q

What is the formula for absolute bioavailability?

A

F = (AUCPo/DosePo)/(AUCIV/DoseIV)

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8
Q

When is relative bioavailability used?

A

When there is no data from IV administration

  1. Expensive IV preparation
  2. Low solubility of drug
  3. Contraindications of IV route
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9
Q

What is the formula for relative bioavailability?

A

Relative Bioavailability = (AUCa)/(AUCb)

where AUCb is the reference standard exposure

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10
Q

What are the factors affecting bioavailability with respect to absorption?

A
  1. Variable absorption from GIT
  2. Drug too hydrophilic (atenolol)
  3. Grapefruit juice (inhibit reverse transporter)
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11
Q

What drugs are degraded extensively by the first pass effect?

A

Lidocaine and propanolol

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12
Q

T/F: Rate of absorption is measured by Tmax.

A

True

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13
Q

What is the range of bioavailability for IM and SC routes?

A

75 - 100%

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14
Q

What is the range of bioavailability for oral and inhalation routes?

A

5 - 100%

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15
Q

Do rectal and transdermal routes provide less first pass effect? What are their bioavailability ranges?

A

Yes.

Rectal - 30 - 100%
Transdermal - 80 - 100%

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16
Q

In bioequivalence, the (1) profiles of two formulations must be equal.

A

(1) plasma concentration vs. time

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17
Q

What is the fundamental reason for performing bioequivalence testing?

A

To ensure the quality of generic drug products

18
Q

What is considered one of the most successful pieces of legislation passed?

A

Hatch-Waxman Amendments to FFD & C Act of 1984

Increased prescription of generics (from 12% - 44% in 16 years)

19
Q

How long are the innovator drug patents in effect?

A

Around 20 years

20
Q

If you are developing a generic or alternative drug, what do you have to prove?

A

Safety
Efficacy
Affordability

21
Q

What are the NDA requirements for branded drugs?

A
  1. Chemistry
  2. Manufacturing
  3. Controls
  4. Labeling
  5. Testing
  6. Animal Studies
  7. Clinical Studies
  8. Bioavailability
22
Q

What are the NDA requirements for generic drugs?

A
  1. Chemistry
  2. Manufacturing
  3. Controls
  4. Labeling
  5. Testing
  6. Bioequivalence
23
Q

What are the requirements for a generic drug?

A
  1. Same active ingredients
  2. Same route of administration
  3. Same dosage form
  4. Same strength
  5. Same condition of use
24
Q

Define: Pharmaceutical Alternative

A

Same molar amount and active pharmaceutical moieties

Different dosage form and chemical form

25
Q

Give examples of pharmaceutical alternatives

A

Tetracycline phosphate and tetracycline hydrochloride

Metformin immediate and extended release tablets

26
Q

Define: Pharmaceutical Equivalence

A

Same molar amount, active pharmaceutical ingredients, dosage form and route

e.g. diazepam 5 mg

27
Q

Can bioequivalent substances be either pharmaceutical alternatives or equivalents?

A

Yes

28
Q

Define: Therapeutic Equivalence

A

Pharmaceutical equivalents or alternatives administered in same molar dose, route and with same effects

29
Q

T/F: Therapeutically equivalent drugs must be bioequivalent.

A

False

30
Q

T/F: Pharmaceutical equivalence = therapeutic equivalence

A

False

31
Q

Pharmaceutical equivalence is acceptable in which dosage forms?

A

Aqueous solutions
Powders for reconstitution
Gases

32
Q

What factors contribute to the differences in drug performance in vivo?

A
  1. Drug particle size
  2. Excipients
  3. Manufacturing equipment or process
  4. Site of manufacture
33
Q

Are bioequivalent drugs therapeutically equivalent?

A

They should be.

34
Q

What is the battle cry of bioequivalence?

A

We want to be the same!

35
Q

What is the standard model of testing in bioequivalence trials?

A

2-treatment cross-over study

There is a wash-out period.

36
Q

What parameter refers to the total amount of active drug that reaches the systemic circulation?

A

AUC 0 - t

37
Q

Cmax and Tmax assess the (1) of absorption, while AUC assesses the (2) of absorption.

A

(1) rate

(2) extent

38
Q

T/F: If Cmax and AUC are the same, CL, Vd, k, and half life won’t be very different.

A

True

39
Q

What is the statistical requirement for bioequivalence?

A

AUC and Cmax must be in between 80 - 125% for a 90% confidence interval.

40
Q

Good manufacturing practices entails that the producers take proactive steps to ensure that their products are?

A

Safe, pure and effective

[Ther 201] 1st Exam Transes (11 decks)

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