PED2001 Distribution Flashcards

1
Q

What are the four main compartments of drug distribution in bodily fluids?

A

Intracellular, extracellular, transcellular, intravascular

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2
Q

What percentage of body weight does water comprise?

A

50% to 70%

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3
Q

What are the components of extracellular fluid and their approximate percentages of body weight?

A
  • Blood plasma: about 4.5%
  • Interstitial fluid: 16%
  • Lymph: 1.2%
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4
Q

What percentage of body water does intracellular fluid constitute?

A

30-40%

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5
Q

What is transcellular fluid and its approximate percentage of body water?

A

Encompasses various specialized compartments and constitutes 2.5%

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6
Q

What forms do drugs exist in within aqueous compartments?

A

Free and bound forms

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7
Q

What influences the equilibrium of weak acids or bases in bodily fluids?

A

Fluid pH and drug pK

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8
Q

Who introduced the concept of the blood-brain barrier (BBB)?

A

Paul Ehrlich

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9
Q

What characterizes the structure of the blood-brain barrier?

A

Continuous endothelial cell layer with tight junctions, surrounded by pericytes

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10
Q

What is the primary limitation of the blood-brain barrier?

A

Many drugs with low lipid solubility cannot penetrate

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11
Q

What can disrupt the integrity of the blood-brain barrier?

A

Inflammation

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12
Q

What is the volume of distribution (Vd) mathematically represented as?

A

Vd = Q/Cp

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13
Q

What does apparent volume of distribution represent?

A

The volume that would contain the total body content of the drug at a concentration equal to that in the plasma

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14
Q

What is the approximate plasma volume per kilogram of body weight?

A

0.05 L/Kg

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15
Q

What are Class 1 and Class 2 drugs based on plasma albumin binding?

A
  • Class 1: Dose < binding capacity of albumin
  • Class 2: Dose > binding capacity of albumin
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16
Q

What is the total extracellular volume per kilogram of body weight?

A

0.2 L/Kg

17
Q

What type of compounds have a volume of distribution close to extracellular volume?

A

Many polar compounds such as vecuronium, gentamycin, and carbenicillin

18
Q

What is the volume of distribution for many drugs that readily cross cell membranes?

A

Approx. 0.55 L/Kg

19
Q

What factors can increase the volume of distribution?

A
  • Drug binding outside the plasma compartment
  • Partitioning into body fat
20
Q

What happens to drugs with a volume of distribution greater than total body volume during overdose?

A

Haemodialysis filters blood plasma, making it unhelpful in managing overdose with such agents

21
Q

What can slow gastrointestinal absorption?

A

Drugs inhibiting gastric emptying like atropine or opiates

22
Q

What is an example of drugs that can retard absorption through insoluble complexes?

A

Ca2+ and Fe2+ with tetracycline

23
Q

What is a physiological effect on drug absorption mentioned in the text?

A

Adrenaline added to local anaesthetic injections causes vasoconstriction, slowing anaesthetic absorption

24
Q

What are pro-drugs?

A

Inactive precursors metabolised to active metabolites

25
Q

What is an example of a drug that is a pro-drug and its active metabolite?

A

Cyclophosphamide metabolises to active metabolites

26
Q

What is the purpose of antibody-drug conjugates in cancer chemotherapy?

A

Improve selectivity of cytotoxic drugs

27
Q

What is the size range of liposomes?

A

0.1-1 um in diameter

28
Q

What are coated implantable devices used for?

A

Localized drug delivery from implants

29
Q

What is the purpose of embedding sirolimus in drug-eluting stents?

A

Prevent re-stenosis

30
Q

Fill in the blank: The volume of distribution for drugs like phenytoin and ethanol is close to _______.

A

Total body water volume

31
Q

True or False: Drug interactions caused by altered absorption can be due to physiological effects.

A

True

32
Q

What are some examples of drugs that act as displacing agents in plasma?

A
  • Sulphonamides
  • Choral hydrate
  • Trichloroacetic acid