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M & R (Semester 2) > Pharmokinetics > Flashcards

Pharmokinetics Flashcards

1
Q

What factors can affect the pharmaceutical process?

A

The formulation of the drug (tablet/liquid) and the compliance of the patient.

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2
Q

What is the name of the process by which a drug gets to its site of action?

A

Pharmacokinetic

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3
Q

What is a pharmacodynamic process?

A

This is the process by which a drug exerts it’s therapeutic effect.

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4
Q

How can we reduce systemic side effects?

A

We can change site of administration so that the drug is more targeted to where it is needed.

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5
Q

What is oral bioavailability?

A

This is the proportion of drug given which reaches the systemic circulation unchanged.

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6
Q

What is LD50?

A

This is the maximum tolerated dose of a drug.

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7
Q

How can we calculate therapeutic ratio?

A

LD50/ED50, where ED50 is the minimum effective dose.

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8
Q

What consideration needs to be made to drugs being given at intervals?

A

This means that drug concentrations in the systemic system will fluctuate, and this must be maintained below the toxic concentration.

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9
Q

What factors alter the pharmacokinetic process of a drug?

A

1st pass metabolism and absorption in the gut.

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10
Q

Name three routes of drug administration which avoid 1st pass metabolism

A

Rectal, sublingual and Parietal (e.g. IV, IM/SC)

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11
Q

What is volume of distribution?

A

This is a theoretical volume in which a drug has become distributed throughout if this happened instantaneously. This will vary depending on how lipid soluble a drug is.

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12
Q

In what cases can drug bind to receptors?

A

When the drug is free and not bound to any other plasma proteins.

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13
Q

What are the potential problems with drugs binding to proteins?

A

If there is a high percentage of binding, or if the therapeutic ratio is small or the volume of Distribution is small then displacement of drugs from plasma proteins can be very detrimental.

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14
Q

What is the difference between a class I and class II drug?

A

A class one drug is used at lower conc than the number of binding sites while a class II drug is used at higher concentrations and so displaces the class I drug.

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15
Q

What is another name for a class II drug?

A

Precipitant.

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16
Q

How is the steady state of a drug quickly reached?

A

Free drug levels rise, and with this, receptor action also rises. Elimination rate rises and so steady state is restored.

17
Q

What is 1st order kinetics?

A

This is when elimination rate is proportional to drug concentration.

18
Q

What controls 0 order kinetics?

A

This is controlled by the number of elimination sites, and it where the same amount of drug is eliminated per unit time with no changes caused by changing concentrations.

19
Q

How many half lives are needed with repeated drug administration to reach steady state for a 1st order kinetic drug?

A

5

20
Q

If we want a fast action for a drug with a long half life, what do we administer?

A

We can administer a large loading dose, and then smaller maintenance doses.

21
Q

How can drugs be eliminated from the body?

A

They can be metabolised in the liver or excreted by the kidneys

22
Q

Why are mixed functional oxidases in the liver important?

A

These have low specificity, affinity for lipid soluble drugs and are inducible and inhibitable

23
Q

When are drug interactions in metabolism important?

A

When min drug conc is used, when there is a low therapeutic ratio or when metabolism follows zero order kinetics.

24
Q

What can cause quicker drug degeneration?

A

Enzyme inducers

25
Q

When are enzyme inducers a problem?

A

They cause problems when drugs are used at low concentrations

26
Q

What can enzyme inhibitors cause?

A

These can cause toxic drug levels to present.

27
Q

What fraction of drug can be excreted in the kidneys?

A

Only the free fraction is affected by the kidneys

28
Q

What factors affect the amount of lipid soluble drug reabsorbed in the kidney? Where in the kidney may this occur?

A

pH and concentrations, this can occur in the collecting duct.

29
Q

What ionisation state must a lipid soluble drug be to be reabsorbed in the kidney?

A

Non ionised

30
Q

If a drug is a weak acid, what state must the urine be for increase reabsorption?

A

Acidic so that the drug is in its non-ionised form

31
Q

When a drug is a weak base and present in acidic urine, will there be increase or decreased reabsoprtion?

A

Decreased because more of the drug will be in the ionised form and therefore unable to cross the phospholipid bilayer.

32
Q

What two effects does renal disease have on a drug?

A

It increases the half life and therefore increases the time take to reach steady state.

M & R (Semester 2) (13 decks)

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