Introduction To Pharmokinetics Flashcards

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1
Q

What is pharmacokinetics?

A

The movement of drugs within the body

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2
Q

What is pharmacodynamics?

A

The effect of drugs on the body

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3
Q

What is bioavailability?

A

The fraction of the drug that reaches the systemic circulation as intact drug

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4
Q

What is drug disposition?

A

All processes by which the body handles drugs

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5
Q

What is the ADME model?

A

A bsorption, D istribution, M etabolism, and E limination

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6
Q

What are most drugs classed as?

A

Weak acids or weak bases

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7
Q

What is drug-protein binding?

A

The reversible interactions of drugs with proteins.

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8
Q

What is the first-pass effect?

A

The extent to which a drug is removed by the liver during its first passage into the portal vein

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9
Q

What is the function of the epithelial cell layer?

A

To define the boundary of the body

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10
Q

What is the largest constituent of the human body?

A

Plasma

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11
Q

What are the different proteins that drugs can bind to

A

Proteins in the plasma, tissue components, RBCs.

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12
Q

What is the definition of pKa?

A

The pH where ionised and unionised forms of the weak acid or base are equal

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13
Q

What is absorption?

A

The extent to which intact drug is absorbed from the gut lumen into the portal vein

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14
Q

What separates each compartment?

A

Various barriers e.g epithelial cells

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15
Q

What are the non-covalent bonding forces involved in drug-protein binding?

A

Van der Waal’s forces, ionic bonding, hydrogen bonding.

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16
Q

What are cell membranes?

A

Barriers between compartments in the body

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17
Q

What are the different routes of drug administration?

A

Subcutaneous, Intramuscular, Oral, Intravenous, Intraarterial, Rectal, Vaginal, Transdermal, Sublingual, Intranasal, Intravitreal, Inhalational,

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18
Q

What is the volume of distribution

A

Extent of distribution in the body

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19
Q

What are the components of cell membranes?

A

Lipids, proteins, and carbohydrates

20
Q

How is cell membrane formed

A

Lipid bilayer

21
Q

How does the pKa value affect the strength of an acid or base?

A

Lower pKa value indicates a stronger acid or base, while higher pKa value indicates a weaker acid or base

22
Q

What is the function of the intestinal wall and liver?

A

To prevent entry of xenobiotics into the body

23
Q

Which proteins have binding sites selective for basic drugs?

A

Alpha 1-acid glycoproteins and Beta-globulins.

24
Q

How is the volume of distribution used?

A

To calculate the dose for therapeutic drug concentration

25
Q

What is the function of cholesterol in the cell membrane?

A

Affects membrane fluidity and stability

26
Q

What is lipophilicity?

A

The ability of a molecule to dissolve in lipids

27
Q

Where do lipid soluble drugs partition?

A

Into the lipid bilayer.

28
Q

How is lipophilicity measured?

A

By the partition coefficient (Log P)

29
Q

What determines the adequate drug concentration at the site of action?

A

Absorption and distribution

30
Q

What does a higher Log P value indicate?

A

Higher lipophilicity and permeability

31
Q

What is the volume of distribution (V)

A

The relationship between the total amount of drug in the body and the concentration of drug in the plasma.

32
Q

What is the general rule for absorption of weak acids and weak bases in the intestine?

A

Weak acids are well absorbed from the acidic environment of the intestine as a larger fraction exists as the unionised form, while weak bases are absorbed more slowly as a larger fraction exists in the ionised form

33
Q

What are the barriers to getting drugs into the systemic circulation following oral administration?

A

Cell membrane barriers

34
Q

What is the principle of minimum hydrophobicity?

A

Designing drugs with low hydrophobicity to reduce toxicity

35
Q

Give the equation for the volume of distribution

A

equation: V = Total amount of drug / Concentration of drug in plasma.

36
Q

What is distribution in pharmacology?

A

The movement of drug molecules from the circulating blood to other areas of the body

37
Q

What factors determine the ability of a drug to permeate the cell membrane barriers?

A

Lipophilicity and ionisation status

38
Q

What is the volume of distribution of a drug if it is 100 L and the blood plasma concentration is 10 mg/L?

A

1000mg

39
Q

What is the volume of distribution referred to as?

A

The ‘apparent’ volume of distribution.

40
Q

What factors does drug distribution depend on?

A

Blood flow, concentration gradient, permeability of cell membranes, drug binding to plasma proteins or tissue components

41
Q

What is the bioavailability of a drug?

A

The amount of drug that reaches the systemic circulation

42
Q

What do proteins binding drugs act as?

A

A reservoir for drug transport and a pharmacologically inactive mass-transit unit

43
Q

What is the effect of first-pass metabolism on drugs?

A

It reduces the bioavailability of drugs

44
Q

What does distribution depend on?

A

Blood flow and protein binding

45
Q

What is route of drug through oral administration and dissolution?

A

Mouth, oesophagus, liver, stomach, small intestine, colon

46
Q

Equation for bioavailability:

A

Fraction absorbed into portal vein x fraction escaping through first pass