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Box 9.

7 PHARMACOKINETICS
The study of how a drug reaches its target and what happens to it in the body is
known as pharmacokinetics. This information is important in the pharmaceutical
industry when a new drug is being developed. There is no point in perfecting the
structure of a new compound to bind to a specific receptor site, if the compound has
no chance of reaching it.
There are four stages to consider:

Drug absorption: this is the route by which the drig reaches the bloodstream
from the pount of administration;
Drug distribution: once absorbed, the drug is distributed around the body in
the blood supply and then more slowly from there to the tissues and organs;
Drug metabolism: this is the breaking down of the drug in the body due to
the action of enzymes;
Drug excretion: the main route for excretion is via the kidneys and bladder.

The aim is to design a drug with an optimum lifetime in the body one that is long
enough for it to reach its target and be effective, but short enough to ensure it does
not build up in the body.
Questions:
The breakdown in the body of the chemotherapy drug, cisplatin, is found to follow
first order kinetics. The rate constant at body temperature is 1.87 x 1013 /min. The

concentration of the drug in the body of a cancer patient is 5.16 x 104 mol /dm 3 .
What will the concentration be after 24 hours?
Solution:
Given:first-order kinetics

( 241hours 60 min
3

K=
1.87 x 10
min t = 1 day day )( 1 hr )
=1440 min

let [ cisplatin ] =[ A ]
4
[ A ] o= 5.15 x 103 mol
dm

[ A ] t=? (after 1440 min)

4
5.15 x 10 mol [ (1.87 x 10
3
) ( 1440 )
]
[ A ] t= [ A ]o e kt
= 3
e
dm

3.493 x 105 mol


[ A ] t=
dm 3
The concentration of the cisplatin drug will be 3.493 x 105 mol/ dm 3
after 1 day (1440 minutes).

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