Pharmacokinetics 37
The figure shows the different types of
drugs with different plasma half life, but the
steady state concentration is maintained on
repetitive dosing in all the three type of drug.
A B C
Toxic level
Steady state
concentration
Therapeutic
level
Blood concentration
Time (hour)
Fig. 1.4.3: Drug concentration vs time curve of
repeated dosing.
Drug : A = Drug with long plasma half life given
in initial loading dose followed by
constant maintenance dose.
B = Drug with short plasma half life given
in constant repetitive dose.
C = Drug with long plasma half life given
in constant repetitive dose.
LOADING DOSE
It is a single or many quickly repeated
doses given in the beginning of treatment
to achieve target concentration rapidly.
DOSAGE INTERNAL
Most of the drugs are given in divided
dose daily, the dosing interval is determined
by the plasma half life. The drugs with long
half lives may be given once or twice daily
while drugs with shorter plasma half lives
may require constant dosing or with short
dosing interval.
When any drug is administered, it
produces its desired effect in a particular
time at receptor site and remain there at
therapeutic level for particular time and
after that its therapeutic efficacy declines.
So the next dose should be given in
between this period so that the steady state
concentration is maintained and no toxic
effects are produced due to high dose.
The graph shows that the drug reaches
at the therapeutic level in 3½ hours after oral
administration and achieve its peak
concentration in 4½ hours and decreases
below the mini-mum effective concentration
(MEC) in 10 hours.
1
2
3
4
5
6
7
2468 10 12 14 16 18 20
Toxic level
[Minimum toxic
concentration (MTC)]
Therapeutic level
[Minimum effective
concentration (MEC)]
Plasma concentration (μg/ml)
Time (hr.)
Fig. 1.4.4: Drug concentration in plasma vs time curve
of drug administered orally.
Now for maintaining the serum concen-
tration above the MEC for longer duration,
the second dose of drug should be given
about 7 to 8 hours after the first dose,
otherwise when it is given after 7 to 8 hours
it will take extra time to reach the MEC or if
it is given prior to 7 to 8 hours the second
dose in combination with the first dose effect
crosses the minimum toxic concentration
(MTC).