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Pathology > Pharmacology Class 2020 Pharmacokinetics > Flashcards

Pharmacology Class 2020 Pharmacokinetics Flashcards

1
Q

Pharmacokinetics

A

What does the body do to the drug.Concerns the relationship of the drug with the absorption, distribution, metabolism, elimination processes to the intensity and time course of pharmacologic effects of drugs and chemicals.

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2
Q

What variables affect pharmacokinetics?

A

Age
Organ Function
Health

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3
Q

Absorption

A

is the movement of a drug from its site of administration into the central compartment which is the blood stream.

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4
Q

Bioavalability

A

F is the fraction of unchanged drug reaching systemic circulation following administration by any route.

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5
Q

Which route of administration provides 100% bioavalability?

A

IV

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6
Q

How does pH affect drug passing through barriers?

A

Change in pH affects ionization to pass through.

A more acidic drug will accumulate on the more basic side of membrane and a more basic drug will accumulate on more acidic side of the membrane.

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7
Q

Which drugs pass through rapidly through diffusion?

A

Lipid soluble

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8
Q

Henderson Hasselbach

A

Depending on pKa of drug

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9
Q

What is the main way of transport of drugs?

A

Passive Diffusion which is where a drug molecule penetrates by diffusion along a concentration gradient

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10
Q

What is active transport?

A

Requires energy to move a drug against an electrochemical gradient.

Example: sodium potsssium ATPase

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11
Q

Concentration

A

Rate of diffusion away from the site of administration is directly proportional to the concentration

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12
Q

Which part of gut has most absorption capacity?

A

Small intestine due to Surface Area is large compared to the small surface area of the stomach.

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13
Q

The factor that affect the release of the drug from stomach to small intestine can affect what?

A

Absorption can be affected by delayed gastric emptying

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14
Q

What can influence late gastric emptying?

A

High fats and High carbs

Intense Exercise

Cold beverages

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15
Q

What accelerates gastric emptying?

A

Moderate Exercise
Hot beverages
Recumbent position

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16
Q

How does slow gastric emptying affect aspirin?

A

More stomach irritation

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17
Q

How does slow gastric emptying affect penicillin?

A

It is sensitive to pH and it is less efficient.

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18
Q

Tissues that are highly vascular have more extensive absorption.

True or False

A

True

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19
Q

Inflammation increases absorption

A

True

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20
Q

Edematous areas increase absorption

A

False.

Decrease

21
Q

There is less vascularity around gluteus muscle so why would the rate of absorption be affected?

A

Fat is not highly vascular like muscle

22
Q

What drug is most difficult to pass through the plasma membrane?

A

Ionized and hydrophilic

23
Q

What drug type passes through the blood brain barrier, placenta, fat and skin?

A

Lipophilic drugs

24
Q

Ficks Law of Diffusion

A

The rate of diffusion is proportional to thickness of the area you are dealing with. The thicker the area the slower the rate and the larger the area the greater the area of absorption will be.

25
Q

Distribution

A

The partitioning of a drug between the blood and extravascular tissue. How well it distributes determines how well it works

26
Q

Where is the drug contained the most initially in distribution?

A

Most perfuse organ such as

Brain
Kidney

27
Q

How does the size of the organ affect distribution of the drug?

A

Determines the concentration gradient between the blood and the organ.

The larger it is the higher the capacity of distribution into the organ.

Example:

Skeletal muscle has higher capacity than the brain because brain is smaller.

28
Q

Where is albumin found?

A

A lot of drugs will bind to albumin within the blood

29
Q

What is solubility?

A

Organs with high lipid content will dissolve a high concentration of lipid soluble agents rapidly.

30
Q

Volume of Distribution

A

Relates to the amount of drug in the body to the concentration of drug in the blood

31
Q

What is Vd?

A

Apparent Volume of Distribution which comes from the blood divided by the concentration

1000mg drug A
Sample of blood 100mg/L

Vd= 10L

32
Q

Two Compartment Model

A

A two compartment model considers the movement of drugs between the central compartment and the peripheral compartment

Once injected the highly perfused areas get the drug first and then the distribution phase happens where the central compartment equilibrates with the peripheral compartment.

33
Q

Distribution Phase

A

Plasma concentration is highest immediately after the IV bolus but then rapidly decreases as the drug distributes into the peripheral compartment.

34
Q

Elimination Phase

A

After a distribution reaches equilibrium and the plasma concentration decreases at a constant rate

Drug introduced into central compartment and equilibrates with peripheral compartment causing a decline on the graph. Where the decline on the graph f line decline slows down is elimination phase.

Elimination paths:

Fecal
Lungs

35
Q

Thiopental

A

General Anesthetic

Shortly after injection, the drug level in the blood is high initially and then it drops and you see an increase in the concentration in other parts of the body such as in the brain where it reaches max concentration.

Redistribution terminates drug action or effect through distribution into other tissues

36
Q

Protein Binding is important because it inhibits the action of the drug.The level of protein in plasma affects free drug concentration.

True or False

A

True

37
Q

What medical condition increases the amount of free drug?

A

Hypoalbuminemia caused by

Cirrhosis
CHF
Malnutrition

38
Q

More Free Drug equals more effect

A

Yes

39
Q

What is the negative effect of free drug high concentration?

A

Side effects

40
Q

Which molecule affect the binding of basic drugs to proteins?

A

alpha 1 acid glycoprotein

41
Q

What factors determine the fraction of bound drug?

A

Drug Concentration
Affinity of Binding Sites
Number of Binding Sites

42
Q

If a drug does not distribute within the tissue, what can happen?

A

Accumulation which cause toxicity.

Ototoxicity and Renal Toxicity

43
Q

What drug can inhibit bone growth?

A

Tetracycline and heavy metals

44
Q

Where in the body is a drug’s effect most potent

A

Blood Stream

45
Q

What type of drugs do Albumin bind?

A

Acidic drugs which are most drugs

46
Q

When a drug binds to a plasma protein like albumin, what happens to its capacity to exert an effect?

A

It is bound so its effect goes down

47
Q

Only the free drug exerts a biological effect.

True or False

A

True

48
Q

What is Albumin’s main role in the body?

A

To preserve the oncotic pressure of plasma which is why it stays only in the blood.

Pathology (10 decks)

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