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Pharmacology > Pharmacokinetics + Pharmacodynamics > Flashcards

Pharmacokinetics + Pharmacodynamics Flashcards

1
Q

List the phases of drug absorption (4)

A
  1. Absorption
  2. Clinical effect
  3. Metabolism
  4. Excretion
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2
Q

Define enteral drug administration

A

Administered via the gut

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3
Q

Define parental drug administration

A

Not administered via the gut

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4
Q

List forms of drug administration (5)

A
  1. Oral
  2. Intravenous
    - Injected through a vein straight into bloodstream
  3. Intramuscular
    - Injected through a muscle
  4. Subcutaneous
    - Injected under skin to fatty tissue
  5. Inhalation
    - Absorbed through lungs
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5
Q

What form of parenteral drug administration works slowly?

A

Subcutaneous- has to pass through more

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6
Q

Advantages of oral administration

A

Socially acceptable

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7
Q

Disadvantages of oral administration (4)

A
  1. Slow onset
  2. Variable absorption
  3. Gastric acid may destroy drug
  4. 1st pass metabolism
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8
Q

List some other factors affecting oral drug absorption (5)

A
  1. Lipid solubility and ionisation
  2. Drug formulation
  3. Gastrointestinal motility
  4. Interactions with other substances in the gut
  5. GI tract disease
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9
Q

Define 1st pass metabolism

A

When drug conc is greatly reduced before it reaches the systemic circulation

  • Because the liver metabolises the drug
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10
Q

Where does all blood from the GI tract drain to?

A

Hepatic portal vein

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11
Q

What veins in the GI tract do not drain to the hepatic portal vein?

A

Sublingual and rectal veins

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12
Q

What does the HPV drain to

A

Liver

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13
Q

What happens when the liver inactivates the drug?

A

More needed by oral route to get desired effect (e.g. glyceryl trinitrate)

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14
Q

What happens when the liver activates the drug?

A

Makes an active form of an inactive drug
Less needed by oral route
(e.g.Valaciclovir —> Aciclovir )

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15
Q

Disadvantages of non oral drug administration (3)

A
  1. Allergic reactions most severe
  2. Access difficulties/self medication
  3. Drug cost higher
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16
Q

What are the advantages of non oral drug administration?

A

Predictable plasma levels

No first pass metabolism

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17
Q

1st pass metabolisism is important when considering drug dosage

What can abnormal liver function cause? (3)

A
  1. Extremes of life
  2. Liver disease
  3. Drug interactions changing drug metabolism
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18
Q

Why is there a difference in severity with relation to oral and non-oral drug administration?

A

ORAL
- Allergic reaction not as dangerous as there could be 30 minutes before the drug has an effect

NON ORAL
- Allergic reaction more severe as the drug goes straight to the blood so there is less time to act

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19
Q

Define the term bioavailability

A

Proportion of an ingested drug that is available for clinical effect

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20
Q

What factors modify the bioavailability?

A
  1. Dosage form
  2. Destruction in the gut
  3. Poor absorption
  4. 1st pass metabolism
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21
Q

When would you want the bioavailability of a drug to be as low as 0%?

A

If you want to keep the drug working in the gut and not have it go into the bloodstream

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22
Q

Define drug distribution

A

How much of the body is the drug diluted in?

23
Q

Where in the body are drugs diluted in?

A

Vascular
Tissues
CNS

24
Q

How does lipid binding affect the volume of distribution?

A

Creates a slow release from accumulation

25
Q

What happens if a drug bound to a plasma protein is inactive?

A

Can act as a reservoir

26
Q

How can plasma proteins act as a reservoir for drugs?

A

If the drug is used up, the plasma protein releases more so allows the reaction to act for much longer

27
Q

Give examples of drugs that can interact by competitive binding.

A

Warfarin + Aspirin

28
Q

Define drug metabolism

A

Preparing the drug from elimination from the body

29
Q

Give examples of phase 1 reactions of drug metabolism (3)

A
  • Oxidation
  • Reduction
  • Hydrolysis
30
Q

What is the effect of phase 1 metabolism?

A

Conversion to metabolites of lesser, equal or greater activity- changes its shape

31
Q

Give examples of phase 2 reactions of drug metabolism (4)

A
  • Conjugation
  • Sulphation
  • Methylation
  • Acetylation
32
Q

What is the effect of phase 2 metabolism?

A

Conversion to inactive metabolites- add to larger molecule that the body naturally eliminates

33
Q

List examples of drug excretion (5)

A
  1. Renal - urine
  2. Liver - bile
  3. Lungs - exhale gas
  4. Sweat
  5. Saliva
34
Q

List disorders of excretion (2)

A
  1. Renal disease

2. Liver disease

35
Q

How does chronic renal failure (from renal disease) affect drug administration?

A

Drug doses must be reduced

36
Q

How does liver failure (from liver disease) affect drug administration?

A

Drug doses must be reduced

37
Q

Do drugs distribute themselves evenly around the body?

A

No- normally go to places where blood flow is higher and eventually even out

38
Q

What is planning drug use based on?

A

The idea of body compartments

39
Q

How does the drug behave in a single compartment model?

A

Drug behaves as if it is evenly distributed throughout the body

40
Q

How does the drug behave in a two compartment model?

A

Drug behaves as if it is in equilibrium with different tissues in the body

41
Q

Define pharmacokinetics

A

Study of how an organism affects the drug

42
Q

How is pharmacokinetics studied? (2)

A
  1. Drug clearance

2. Repeated drug dosing

43
Q

What features are involved in drug clearance? (3)

A
  1. Plasma half life (time for 1/2 drug to be removed)
  2. 1st order kinetics
  3. 0 order kinetics
44
Q

What form of diffusion does drug elimination/absorption occur through?

A

Passive diffusion

45
Q

How is drug removal related to the drug concentration in first order kinetics? (2)

A
  • Drug removal is proportional to the drug concentration

- Logarithmic graph of elimination is a straight line

46
Q

What can drug elimination be saturated by?

A

High drug concentrations

47
Q

What happens during zero order kinetics in relation to drug elimination?

A

Constant amount of drug is eliminated per unit time

48
Q

What happens during a paracetamol overdose? (3)

A
  • Can cause irreversible liver damage which can affect blood clotting
  • It is metabolised by zero order kinetics
  • It is toxic to the liver but not many other places
49
Q

What could too frequent a dosing schedule of drugs result in?

A

Plasma levels that may be toxic

50
Q

What does the dosing schedule of drugs depend on?

A

The drugs therapeutic index

51
Q

What could too infrequent a dosing schedule of drugs result in?

A

Sub-therapeutic plasma levels and no clinical effect

52
Q

How can drugs affect each other?

A

One drug may increase or decrease the metabolism of another

53
Q

What form of drug absorption is the least reliable?

A

Oral route

Pharmacology (3 decks)

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