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Pharmacology > Disposition of Drugs > Flashcards

Disposition of Drugs Flashcards

1
Q

Define disposition of drugs

A

The study of the movement of drugs in the body across biological membranes from the time of absorption until elimination.

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2
Q

Disposition of drugs = _____

A

Pharmacokinetics

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3
Q

What are the 4 stages of drug disposition?

A

1: Absorption
2: Distribution
3: Biotransformation
4: Excretion

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4
Q

What are the factors affecting disposition of drugs?

A

1: Biological cell membranes
2: Concentration gradients
3: Pump mechanisms
4: Site of administration
5: Total body water
6: Plasma protein binding
7: Disease

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5
Q

What are the properties of the biological cell membrane?

A

1: Phospholipid bilayer
2: Membrane proteins and carbohydrates
3: Cell junctions
4: Aqueous pores

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6
Q

What are the 4 mechanisms of drug transport across the cell membrane.

A

1: Passive diffusion
2: Facilitated diffusion
3: Active transport
4: Pinocytosis

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7
Q

Describe passive diffusion

A

1: No energy (ATP) is required for this process
2: Movement down the concentration gradient
3: Hydrostatic pressure differences across membranes
4: Bulk flow of water can carry with it small water soluble substances

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8
Q

What are mechanism types of passive diffusion?

A

1: Transmembrane
2: Paracellular
3: Simple diffusion

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9
Q

Define transmembrane.

A

Movement by passive diffusion through aqueous protein channels in the cell membrane.

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10
Q

Define paracellular.

A

Movement via filtration through intracellular aqueous pores.

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11
Q

Define simple diffusion.

A

Movement through lipid membrane

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12
Q

How do the majority of drugs move through the body?

A

Simple diffusion

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13
Q

Describe facilitated diffusion.

A

1: No energy is required
2: Carrier-mediated transport
3: Movement down the concentration gradient
4: Faster because of the carrier

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14
Q

Describe active transport.

A

1: Needs carrier and energy
2: Carrier mediated transport
3: Movement up the concentration gradient
4: Primary vs. secondary

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15
Q

What is the most abundant active transport pump in the body?

A

Na+/K+ ATPase transport pump

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16
Q

Describe Pinocytosis.

A

1: Cell drinking
2: Specific type of endocytosis where cells engulf the drug molecules dissolved in water.
3: Can interfere with lysosomal function and cause lysosome rupture

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17
Q

What are the properties of passive diffusion?

A

1: Moves down the concentration gradient
2: Requires no energy
3: Substances can be move in or out of cells
4: Most common form of transport

18
Q

What are the properties of facilitated diffusion?

A

1: Moves down concentration gradient
2: Requires a carrier
3: Requires no energy
4: Saturable
5: Substances can be moved in or out of cell
6: May protect cell from harmful substances

19
Q

What are the properties of active transport?

A

1: Moves up the concentration gradient
2: Requires energy
3: Symporters or antiporters
4: Satiability
5: Selectivity
6: Competitive inhibition by co-transported compounds
7: Classified into primary or secondary

20
Q

What are the properties of pinocytosis?

A

1: Special type of endocytosis or cell drinking
2: Drug dissolved in water
3: Can be toxic

21
Q

What are the factors affecting simple diffusion?

A

1: Concentration gradient
2: Lipid solubility
3: Degree of drug ionization

22
Q

Higher lipid solubility of the drug = _____

A

Faster crossing cell membranes

23
Q

Non-lipid soluble drugs are more dependent on _____.

A

Molecular size

24
Q

Non-lipid soluble drugs move via _____.

A

Membrane pores

25
Q

Membranes are more permeable to _____ forms of drugs.

A

Non-ionized

26
Q

Drugs cross biological membranes in the _____ form.

A

Non-ionized

27
Q

What does the rate of diffusion depend on?

A

Degree of ionization

28
Q

What does the degree of ionization depends on?

A

1: pH of the drug
2: pKa of the drug
3: pH of environment in vivo

29
Q

Define pH.

A

Any solution is determined by the number of protons present

30
Q

What does the pH of a drug depend on?

A

Whether it acts as an acid or base in solution

31
Q

True or False: Most drugs act as strong acids or bases.

A

False

32
Q

Weakly acidic drugs are more ionized in _____.

A

Alkaline solutions

33
Q

Weakly basic drugs are more ionized in _____.

A

Acidic solutions

34
Q

Define pKa?

A

Equal to the pH of the medium at which the dissolved drug is 50% ionized and 50% non-ionized.

35
Q

Higher pKa of a weak acid = _____

A

Higher N/I

36
Q

Higher pKa of a weak base = _____

A

Higher I/N

37
Q

Acidic drugs ionize in _____.

A

Basic environment

38
Q

Basic drugs ionize in _____.

A

Acidic environment

39
Q

What can the henderson and hasselbach equation be used for?

A

To determine the degree of ionization

40
Q

pKa of an acid = _____

A

pH of the medium + Log N/I

41
Q

pKa of a base = _____

A

pH of the medium + Log I/N

Pharmacology (12 decks)

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