Drug Absorption and Oral Route I Flashcards

1
Q

What is the goal of pharmaceutics?

A

Right dose, right time, correct duration, and not to reach other sites in the body where drug toxicities occur

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2
Q

What is the area of study embracing the relationship between the physical, chemical, and biologic sciences as they apply to drugs, dosage forms, and drug action.

A

Biopharmaceutics

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3
Q

Cell membranes mostly bear a _____ charge on surface

A

negative

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4
Q

Cell membrane is _____ permeable

A

selectively

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5
Q

Process by which a compound and its metabolites are transferred from GI tract to circulating system (parent + metabolites) describes what?

A

Absorption

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6
Q

Passive diffusion is governed by the ______ ______

A

concentration gradient

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7
Q

The concentration gradient governs what kind of diffusion?

A

Passive

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8
Q

What is the main difference between active and facilitated transport?

A

Facilitated transportation does not go against a concentration gradient

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9
Q

Active transport:

Concentration ____ to _____
needs _____ and ____

A

Low + High

Carrier + energy

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10
Q

Passive diffusion:

Concentration ____ to ____
no ____

A

High + Low

No carrier/energy

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11
Q

Paracellar transport:

Concentration ____ to ____
no ______

A

High + Low

No Carriers

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12
Q

Facilitated diffusion:

Concentration ____ to ____
Needs ____ but no ____

A

High + Low

Carrier + No energy

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13
Q

What kind of cells do drugs go through when entering to the lymph?

A

M cells

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14
Q

When drugs go through M cells, lipids and particles take what kind of transport rather than intestinal absorption?

A

Transceullular

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15
Q

What is Fick’s first law?

A

Describes passive diffusion; rate of diffusion across a membrane at a steady-state flow

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16
Q

What is the most important physical property of a drug in relation to its ADME?

A

Lipophilicity

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17
Q

_______ is a movement of molecules from one phase to another, e.g. from aqueous to lipid, from liquid to a plastic of container, from outside to inside of a membrane

A

Partitioning

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18
Q

______ : P (or K) is a measure of a molecule’s lipophilic character, indicating its preference for hydrophilic or lipophilic phase.

A

Partition coefficient

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19
Q

What is typically used as the nonaqueous phase in the partition experiment?

A

Octanol

20
Q

What is typically used as the aqueous phase in the partition experiment?

A

Water

21
Q

For partitioning, increase of octanol, will P increase or decrease

A

Increase; molecule is more like the lipid phase

22
Q

pH of the GI fluid could change what?

A
  1. Solubility
  2. pH-partition hypothesis
  3. Chemical stability
23
Q

Degree of a drug’s ionization depends on what?

A

pH of environment + pKa of drug

24
Q

Most drugs are absorbed thru GI tract by _____ diffusion

A

passive

25
Q

Lots of H+ bonds or ionic bonds with water is favorable for diffusion (T/F)

A

False; unfavorable

26
Q

Lipinski’s Rule of 5

Molecular weight should be…

A

<500

27
Q

Lipinski’s Rule of 5

logP should be at….

A

<5

28
Q

Lipinski’s Rule of 5

How many H-bond donors should there be?

A

<5

29
Q

Lipinski’s Rule of 5

How many H-bond acceptors should there be?

A

<10

30
Q

In sink conditions, Fick’s first law changes what?

A

C2 = 0

31
Q

Where is C1 + C2 found?

A
C1 = GI tract
C2 = Blood
32
Q

What is the sink condition equation under Fick’s first law?

A
  • dc/dt = P(C1-C2)

- dc/dt = P(C1) (sink condition)

33
Q

What is the permeability coefficient equation?

A

-dc/dt = DSK/h * C1

34
Q

-dc/dt = DSK/h * C1

What is h?

A

Thickness of absorbing membrane

35
Q

-dc/dt = DSK/h * C1

What is S?

A

Area of absorbing membrane

36
Q

-dc/dt = DSK/h * C1

What is K (or P)?

A

Partition coefficient, measure of permeability of the membrane to the drug

37
Q

-dc/dt = DSK/h * C1

What is D?

A

Diffusion coefficient of drug

38
Q

pH Saliva

A

6.4

39
Q

pH stomach (fasting)

A

1.4 to 2.1

40
Q

pH stomach (fed)

A

3 to 7

41
Q

pH duodenum (fasting)

A

4.4 to 6.6

42
Q

pH duodenum (fed)

A

5.2 to 7.2

43
Q

pH jejunum + ileum

A

6.5 to 8

44
Q

pH colon

A

7 to 7.5

45
Q

pH urine

A

5.5 to 7