06 - Drug distribution & elimination Flashcards

1
Q

Enterohepatic recirculation can extend the…

A

Half-life of a drug

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2
Q

Describe the stages of enterohepatic recirculation (6)…

A
  1. Drug given orally
  2. Moves through the gut
  3. Absorbed into blood
  4. Travels via hepatic portal vein
  5. Tramsfered tp gall bladder in bile
  6. Secreted back into intestine (back to step 2)
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3
Q

The ability of a drug to bind to blood plasma proteins affects…

A

Distribution

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4
Q

At equilibrium, the rate of clearance from the plasma (is greater than / less than / equal to) rate of clearence from the blood…

A

Equal to

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5
Q

To move from blood vessels into the tissues, drug can exit via…

A

Slit junctions (which are gaps between endothelial cells)

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6
Q

Drugs with a high molecular weight…

a) Do not bind to plasma proteins
b) Bind less readily to plasma proteins
c) Always bind to plasma proteins
d) Are highly bound to plasma proteins

A

d) Are highly bound to plasma proteins

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7
Q

If a drug is highly bound to plasma proteins, it tends to stay in the plasma, leading to poor…

A

Distribution

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8
Q

Only a ( bound / unbound) drug can partition into tissues/organs

A

Unbound

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9
Q

2 important plasma proteins…

A
  • Alpha-1 acid glycoprotein (AAG)

* Albumin (Human serum albumin, HSA)

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10
Q

AAG binds mostly ( acidic / basic ) drugs…

A

Basic (and some neutral)

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11
Q

Higher levels of AAG are found in (2)…

A

Cancer and inflammatory diseases

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12
Q

If AAG levels are raised (such as by cancer), the dose may need to be ( increased / decreased )…

A

Increased

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13
Q

Albumin binds mostly ( acidic / basic ) drugs…

A

Acidic

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14
Q

Malnutrition and cirrhosis tend to ( increase / decrease ) HSA levels…

A

Decrease

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15
Q

If HSA levels are decreased (such as by cirrhosis), the dose may need to be ( increased / decreased )…

A

Decreased

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16
Q

Volume of distribution is a dilution factor which relates the amount of drug in the whole body to the amount…

A

Found in a sample of plasma

17
Q

Vd =

A

total dose / plasma drug concentration

18
Q

The liver is a major site of…

A

Metabolism

19
Q

Prodrugs are drugs that must be…

A

Metabolised into their actrive form

20
Q

Prodrugs can help reduce…

A

Side effects (as they can be targeted more specifically)

21
Q

The mechanism of elimination depends on the…

A

Physiochemical properties of the drug and its metabolites

22
Q

Elimination parameters are (3)…

A
  • Clearence (CL)
  • Elimation rate constant (K el)
  • Half life (t 1/2)
23
Q

Generally, drug levels are negligible after how many half lives?

A

6 half lives

24
Q

Maintainence doses are usually administered after how many half lives?

A

4 half lives

25
Q

The elimination constant is the…

A

Fraction of drug removed per unit time

26
Q

t 1/2 =

A

ln2 / K el

27
Q

ln2 =

A

0.693

28
Q

Clearance =

A

Dose given / total exposure

29
Q

Fenestrated

A

Perforated (such as endothelia with gaps)

30
Q

Enterohepatic circulation

A

Cycling of drug between gut and liver

31
Q

Partitioning

A

The movement of unbound drug from plasma into tissues