Biopharmaceutics Flashcards

1
Q

What is the focus of biopharmaceutics?

A

The study of how the physicochemical properties of a drug, its dosage form, and route of administration affect the rate and extent of drug absorption.

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2
Q

What is pharmacokinetics?

A

The study and characterization of the time course of drug absorption, distribution, metabolism, and elimination.

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3
Q

What is pharmacodynamics?

A

The study of the biochemical and physiological effects of the drug on the body.

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4
Q

List the four main processes involved in pharmacokinetics.

A

Absorption, Distribution, Metabolism, and Excretion (usually by the kidney).

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5
Q

What happens to polar drugs in the body?

A

They are usually excreted in urine; if needed, the liver metabolizes them to make them more polar.

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6
Q

What factors govern drug distribution in the body?

A

Affinity for various tissues, aqueous or lipid solubility, binding to extracellular substances (e.g., proteins), and intracellular uptake.

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7
Q

What is passive diffusion?

A

The movement of molecules via a concentration gradient across a membrane, without a carrier, non-saturable, and with low structural specificity.

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8
Q

How do most drugs gain access to the body?

A

Through passive diffusion.

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9
Q

What is the composition of cell membranes in living organisms?

A

They are composed of a lipid bilayer, which also applies to sub-cellular structures.

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10
Q

What function does the lipid bilayer serve in cell membranes?

A

It acts as a barrier, preventing ions, proteins, and other molecules from diffusing in or out of cells.

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11
Q

Why are most water-soluble molecules unable to pass directly through the lipid bilayer?

A

The bilayer is impermeable to them, so cells use ion pumps to regulate salt concentrations and pH by moving ions across the membrane.

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12
Q

What are natural bilayers primarily made of?

A

Phospholipids with a hydrophilic head and two hydrophobic tails.

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13
Q

Why do polar molecules have low permeability across the lipid bilayer?

A

They have low solubility in the hydrocarbon core of the lipid bilayer, resulting in low permeability coefficients.

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14
Q

What does the lipid:aqueous drug partition coefficient describe?

A

It describes the ease with which a drug moves between aqueous and lipid environments

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15
Q

Why is the ionization state of a drug important?

A

It determines how well the drug will move across a lipid membrane; charged drugs have difficulty diffusing through lipid environments.

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16
Q

How do pH and drug pKa influence drug absorption?

A

They determine the drug’s ionization state, which significantly affects its transport across membranes.

17
Q

Which equation is used to determine the ionization state of a drug?

A

The Henderson-Hasselbalch equation.

18
Q

How do water-soluble drugs penetrate the cell membrane?

A

They penetrate through aqueous channels.

19
Q

What is Facilitated Diffusion?

A
  • Involves Carrier protein and is a saturable process
  • No extra energy needed
    E.g Large water soluble/ Polar compound
20
Q

What is Active Transport?

A
  • Requires Energy
  • Transport is against the concentration gradient
21
Q

Why is Active transport important?

A

Important mechanism for passage of larger drug molecules
-carriers involved

22
Q

What is Endocytosis and Exocytosis

A

They mediate the entry into cells by very large substances
-e.g movement across Intestinal wall into blood of vitamin B12 complexed with its binding protein
-e.g solid particles/ Oil Particles, 1-100nm

23
Q

What is Bioavailability

A

It’s the measure of the mount of drug from the formulation appears in the plasma (systemic circulation)
I.e measure the rate and extent of absorption

24
Q

What does a therapeutic response on a drug depend on

A

Adequate concentration at site of action

25
Q

How is Bioavailability calculated?

A

It’s calculated by determining the AUC from a blood plasma drug concentration V.S. time plot
- Non I.V.: Ranges from 0 to 100%
- IV : 100%

26
Q

What does MEC mean?

A

Minimum Effective Concentration
-Required for the desired Pharmacological effect

27
Q

What does MSC mean?

A

Maximum Safe Concentration - above which toxic effect occur

28
Q

What does the Therapeutic Window mean?

A

Desired response with no toxic effects

29
Q

What does Bioequivalence mean?

A

Comparing two dosage forms containing same drug are equivalent in terms of rate and extent of absorption

30
Q

What does bioequivalence use?

A

Uses AUC, Cmax, tmax