week 18 p2 Flashcards

1
Q

What does bioavailability mean

A
  • Reflects the fraction of drug absorbed in the systemic circulation when the drug is given orally
    • Total Available of drug that reaches the systemic circulation
    • Neglects absorption
    • Measures by comparing area-under0the curve (AUC) of the drug when measurement of the plasma are made from orally
    • Reduction in total drug delivered to the systemic circulations first pass effect
    • Reason why its known as that it losses the drug via first through GI tissues and liver before the systemic circulation
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2
Q

What is the equation for Bioavaiblity

A

• BA=AUCo/AUCiv x100
• AUOo= oral
AUCiv= intravenous

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3
Q

What happens after the drug is in system circulation

A

drug distribution in tissues

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4
Q
  1. What is distribution and modulation factors mean
A

• The process of transferring drug/chemical from the bloodstream to tissues- known as Distribution

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5
Q

What is distribution effected by

A

ionisation state and pH of the environment: ions trapping, non ionised drugs and chemical can cross cell membrane by passive diffusion

. Lipophilicity: Lipophilicity drugs that can cross cells membrane and blood and brain stream ( as its more preamble) and lipophilicity drugs accumulate in the fattest fat tissue e.g. breast

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6
Q

How is disruption of drugs effected

A
  • Through binding of drugs to proteins
    • In the blood drugs are transported in free unbound drug and reversable bond to blood components
    • E.g. albumin, alpha-1 and lipoprotein
    • Acidic drugs usually bound to albumin
    • Basic drugs usually bound to apha-1 and lipoprotein or both
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7
Q

Another way that distribution is affected

A

• Binding of tissues
• Accumulation of drugs in tissues can prolong drug action
• Due to the tissues this releases accumulated drug as the plasma drug decreases
Lead to toxicity

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8
Q

What is the threptic effects of binding of tissues

A

• Bisphonate compound bine to bone matric cells
• Rifanmoin and accumulated in the brain
Digitoxin accumulation in heart muscle

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9
Q
  1. How is the distributions of drugs get into the tissues effected
A

• Rate of of blood flow to tissues- perfusion
• Tissue mass
Characteristics between blood and tissue

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10
Q
  1. What does distribution equilibrium mean
A

• Enter and exit rate are the same between blood and tissue

Is reached more in rich vascularised areas

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11
Q

What does distribution after equilibrium mean

A

• Drug concentrate and in extracellular fluid are reflected by plasma concentration

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12
Q

What does it mean by volume of distribution

A

• Volume fluid into the total drug administrated would have to be diluted to produce the concnetration in plasma

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13
Q

Why is plasma concentration important in this

A

• Retention of a drug in the plasma reflect binding to plasma protein

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14
Q

Equation of volume of distribution

A

• Concentration= amount of drug/volume

Volume= concentration x amount of drug

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15
Q

Eg of VOD

A

• if I five you 100mg of drug after that I take a blood sample and measure the plasma concentration is 10mg/l
100mg / 10mg/l = 100l

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16
Q
  1. What does it means If the drugs are highly bound to tissues or proteins
A

• Very little drug in the circulation
• Low plasma concentration
Higher volume of distribution

17
Q
  1. What happens when drugs stay in prophetically stay in the circulation
A

Higher plasma concertation

Lower volume of distribution

18
Q

What is therapy successful

A

• is linked to unbound drug

19
Q

What is real vod

A

• Vd can also be related to body weight

• E.g. 70kg
Volume of distribution is related in liters or litres per body weight (kg/l)

20
Q
  1. Ego volume for distribution is 5L and Herceptin is suppose to be4L
A

• High molecular weight drugs

Drugs can bind to plasma extensively

21
Q
  1. E.g. the VD is 6-14L and ethanol drug is suppose to be 7-14L
A

• Lower molecular weight

But are hydrophilic