01.2 Pharmacokinetics Flashcards

1
Q

Define bioavailability

A

The fraction of the dose that enters circulation

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2
Q

What is the bioavailability of an IV drug?

A

100%

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3
Q

How is oral bioavailability calculted from a plasma concentration against time graph?

A

The area under the curve is the bioavailability

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4
Q

What factors alter bioavailability?

A

First pass effect
Age
Drug formulation

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5
Q

What factors affect drug distribution?

A

Lipophilicity
Plasma protein binding
Tissue protein binding
Density of bind sites on tissues

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6
Q

How is volume of distribution calculated from a Vd time graph?

A

By extrapolating the curve back to time 0

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7
Q

What is Vd when the drug is only in the plasma?

A

~5L

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8
Q

What is Vd when the drug is in the ECF and ICF?

A

10-30L

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9
Q

What is Vd when the drug is very lipophillic and bound to tissue proteins?

A

100+ L

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10
Q

What are some cytochrome P450 inducers?

A
Carbamazepine
Rifampicin
Barbituates
Phenytoin
St Johns Wort
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11
Q

What are some cytochrome P450 inhibitors?

A
Sodium valproate
Ciprofloxacin
Sulphonamide
Cimetidine
Antifungals
Amiodarone
Isoniazid
Erythromycin
Clarythromycin
Grapefruit juice
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12
Q

What is clearance of drugs dependant on?

A

Hepatic clearance
Renal clearance
Heart maintaining output so renal perfusion is maintained

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13
Q

How is half life associated with clearance?

A

Half life is inversely propoertional to clearance

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14
Q

What is 1st order kinetics?

A

Rate of elimination proportional to drug level

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15
Q

What is 0 order kinetics?

A

Rate of elimination is constant

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16
Q

What are a few reasons you would monitor drug levels?

A
Zero order kinetics
Long half life
Narrow therapeutic window
Risk of DDI
Known toxicity
Monitoring therapeutic effect
17
Q

How many half lives does it take of repeated dosing to reach a steady state?

A

3-5 half lives

18
Q

What needs to happen with each dose if a drug has a very short half life (such as penecillin) and doesn’t reach a steady state?

A

Each dose must reach a therapeutic level

19
Q

How is loading dose calculated?

A

Vd multiplied by Target concentration of drug