Chapter 3: Drug Absorption and Distribution Flashcards

1
Q

The ability of a drug to diffuse across membranes is expressed as:

A

lipid-water partition coefficient

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2
Q

This measures the relative affinity of a drug for the lipid:

A

Partition Coefficient

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3
Q

Increasing the degree of ionization, ______ the lipid water partition coefficient

A

decreases.

inc polarity = dec lipid water partition coefficient

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4
Q

What drug administration route bypasses absorption?

A

Intravenous

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5
Q

The proportion of the total drug concentration that is present in ionized or unionized form is dictated by:

A
  1. ionization constant

2. PH

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6
Q

The most important mechanism of drug transfer?

A

Passive diffusion

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7
Q

Passage through pores:

A

filtration

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8
Q

A drug is said to be absorbed when it enters the:

A

blood or lymph capillaries

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9
Q

Give an example of a drug that uses Active Transport:

A

Iron, Levodopa, PTU, 5-Flurouracil

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10
Q

Oral administration of drug uses what kind of transport?

A

Passive Diffusion

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11
Q

Type of transport that is downhill but does not require energy?

A

Facilitated Diffusion

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12
Q

Botulinum toxin uses what kind of transport?

A

Pinocytosis

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13
Q

What happens when a weak base, such as Diazepam, enters the intestinal lumen?

A

Inc. Unionized thus cross barrier

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14
Q

Ascorbic acid will be able to cross barrier in an acidic or neutral environment?

A

Acidic environment

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15
Q

What is the driving force of Passive Diffusion?

A

The Concentration gradient

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16
Q

Although the surface of the oral cavity is small, absorption can be rapid if the drug has a?

A

High Lipid-Water partition coefficient

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17
Q

Nitrogylcerin trinitrate uses what route of administration?

A

Sublingual

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18
Q

What drugs may be trapped in the stomach?

A

Basic Drugs will be ionized in the acidic environment of the stomach thus unable to cross barrier

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19
Q

Drug accumulation is termed as?

A

ion trapping

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20
Q

Most drug absorption occurs in what part of the GI tract?

A

proximal jejenum

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21
Q

Delay in gastric emptying, will ______ gastric drug absorption and ______ intestinal drug absorption.

A

decrease, increase

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22
Q

Rectal administration of drug is done when:

A

drug causes gi irritation, protracted vomiting, uncooperative and unconscious patients

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23
Q

Rectal administration of drug escapes:

A

hepatic first pass metabolism

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24
Q

What mode of transport is used when traversing the Blood Brain Barrier?

A

Passive Diffusion and Facilitated Diffusion

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25
Q

Enumerate the 4 Factors of Diffusion of Drug:

A

Concentration Gradient, Surface Area, Permeability Coefficient, Thickness

26
Q

What happens to diffusion time if you Increase Concentration Gradient?

A

Increase

27
Q

Increase thickness will _____ Diffusion time?

A

Decrease

28
Q

Ratio of concentration of drug into oil and water phases is called

A

lipid water partition coefficient

29
Q

a lipid water partition coefficient of 5 soluble in what phase?

A

oil

30
Q

Enteric coating dissolves in what environment?

A

alkaline

31
Q

What enzyme play a major role in the extent of drug absorption?

A

Cytochrome p450 enzyme

32
Q

This is responsible for the efflux of drugs back to the gut lumen?

A

P Glycoprotein

33
Q

Insulin and Oxytocin is administered SQ because:

A

It is sensitive to protease (gastric enzyme)

34
Q

Glyceryl trinitrate bypass what phase?

A

pre-systemic metabolism

35
Q

Chlorpromazine is administer IM or IV because:

A

It has an extensive pre-systemic metabolism

36
Q

This is the fraction of a drug which is available in systemic circulation:

A

Bioavailability

37
Q

This compares extent of absorption of 2 drugs:

A

Bioequivalence

38
Q

2 Drugs that are bioequivalent should be pharmaceutically equivalent. T or F?

A

True

39
Q

2 Drugs which are Pharmaceutically equivalent should not be bioequivalent. T or F?

A

True

40
Q

Initially an inactive drug but when taken and metabolized becomes active is called:

A

Prodrug

41
Q

The prodrug Prednisone will be converted to it’s active form namely:

A

Prednisolone

42
Q

What effect does fasting do to drug excretion?

A

Decrease Drug excretion

43
Q

What type of meal can you recommend to a patient taking Griseofulvin?

A

Fatty Meal

44
Q

What is contraindicated to a patient taking Felodipine?

A

Grape Fruit: increases absorption of the drug

45
Q

Divalent ions decreases absorption of what drug?

A

Tetracycline

46
Q

Angulation for IM injection

A

90 degrees

47
Q

Angulation for SQ injection

A

45 degrees

48
Q

Angulation for intradermal

A

10-15 degrees

49
Q

When Protein binding is increase, what happens to Volume of distribution?

A

Decrease

50
Q

The dermis is soluble to both lipid soluble and water soluble compounds. T or F?

A

T due to abundant supply of blood

51
Q

Which parenteral route has a more rapid absorption, SQ or IM?

A

IM

52
Q

IV route is used when:

A
  1. compounds are poorly absorbed
  2. irritating to tissues
  3. rapidly metabolized before or during absorption
53
Q

Delivery of a drug from systemic circulation to tissues is called?

A

Distribution

54
Q

Drug Distribution depends on a variety of factors. List down the 6 factors:

A

Capillary Permeability, Blood Flow Tissue Mass ratio, Extent of Plasma Protein and specific organ binding, pH, transport mechanisms, permeability characteristics of tissue

55
Q

What happens to distribution of the drug, when there is increase blood flow?

A

rapid distribution

56
Q

Only the bound drug can diffuse the capillary wall and produce systemic effects. T or F?

A

False, Unbound drugs can diffuse capillary wall.

57
Q

The binding of drug to plasma protein is specific or non specific?

A

non specific: many drugs may interact with same binding site

58
Q

Chlorpromazine may bind to what specific part of the body?

A

Retina. It has a high affinity to the retinal pigment.

59
Q

Lead and Mercury may accumulate in the kidney because of what protein present in the said organ?

A

Metallothionein which has a high affinity for metals

60
Q

Reason for SQ route of a drug:

A

Fat depots provide a slow sustained released of the active drug

61
Q

What kind of polarity can cross the placental barrier?

A

Low Polar or unionized drugs

62
Q

Reason for inability of chemotherapeutic drugs to reach specific areas of the testis?

A

P glycoprotein, efflux transporter protein, is present in the blood-testis barrier