Introduction To Pharmokinetics Flashcards

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
What is the function of cholesterol in the cell membrane?
Affects membrane fluidity and stability
26
What is lipophilicity?
The ability of a molecule to dissolve in lipids
27
Where do lipid soluble drugs partition?
Into the lipid bilayer.
28
How is lipophilicity measured?
By the partition coefficient (Log P)
29
What determines the adequate drug concentration at the site of action?
Absorption and distribution
30
What does a higher Log P value indicate?
Higher lipophilicity and permeability
31
What is the volume of distribution (V)
The relationship between the total amount of drug in the body and the concentration of drug in the plasma.
32
What is the general rule for absorption of weak acids and weak bases in the intestine?
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
What are the barriers to getting drugs into the systemic circulation following oral administration?
Cell membrane barriers
34
What is the principle of minimum hydrophobicity?
Designing drugs with low hydrophobicity to reduce toxicity
35
Give the equation for the volume of distribution
equation: V = Total amount of drug / Concentration of drug in plasma.
36
What is distribution in pharmacology?
The movement of drug molecules from the circulating blood to other areas of the body
37
What factors determine the ability of a drug to permeate the cell membrane barriers?
Lipophilicity and ionisation status
38
What is the volume of distribution of a drug if it is 100 L and the blood plasma concentration is 10 mg/L?
1000mg
39
What is the volume of distribution referred to as?
The 'apparent' volume of distribution.
40
What factors does drug distribution depend on?
Blood flow, concentration gradient, permeability of cell membranes, drug binding to plasma proteins or tissue components
41
What is the bioavailability of a drug?
The amount of drug that reaches the systemic circulation
42
What do proteins binding drugs act as?
A reservoir for drug transport and a pharmacologically inactive mass-transit unit
43
What is the effect of first-pass metabolism on drugs?
It reduces the bioavailability of drugs
44
What does distribution depend on?
Blood flow and protein binding
45
What is route of drug through oral administration and dissolution?
Mouth, oesophagus, liver, stomach, small intestine, colon
46
Equation for bioavailability:
Fraction absorbed into portal vein x fraction escaping through first pass