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Clearance (1)
Is
The
Clearance (2)
Clearance (3)
The
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Clearance (4)
Drug
Clearance (5)
For
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20
10
10
12
14
16
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Time (Hours)
AUC yang dihitung dengan menggunakan rumus luas trapesium (g/ml x jam)
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Volume of distribution
Is
Volume of distribution
Many
Volume of distribution
Vd
Volume of Distribution
The
Kompartemen Perifer
Kompartemen Sentral
V1
Dosis
C1
ke
k12
k21
V2
C2
Volume of distribution
The decline of plasma concentration with time for a
drug introduced into one-compartment model :
Ct = (Dose/Vd) . exp(-kt) (1-5)
Ct = C0 . exp(-kt)
k = 0.693/t1/2
(1-6)
k = the rate constant for elimination that reflects
the fraction of drug removed from the
compartment per unit of time.
The one-compartment model is sufficient to apply
to most clinical situation for most drugs
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Co
Vd = Dose/Co
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t
0
10
12
Time (Hours)
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Half-Life (t1/2)
It
Half-life (t1/2)
CL
T1/2
Half-Life (t1/2)
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Bioavailability
Is
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plasma concentration of
theophylline of 15 mg/l is desired to relieve acute
bronchiale asthma in a 68-kg patient. If the
patient does not smoke and is otherwise normal
except for asthmatic condition, one can use a
mean theophylline clearance of 0.65 ml/min/kg.
F = 1 because the drug is to be given
intravenously.
Dosing rate = Target . CL/F = 15 ug/ml x 0.65
ml/min/kg = 9.75 ug/min/kg = 40 mg/h for a 68kg patient.
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Loading Dose
A loading
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If
(%)
Urinary excretion (%)
Bound in plasma (%)
Clearance (ml/min/kg/BW)
Volume of distribution (L/kg BW)
Half-life (hours)
Effective concentration (g/ml)
Toxic concentration (g/ml)
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Examples of
pharmacokinetic calculation
The Vd and clearance of theophylline
is 35 L and 3 L/h respectively in a 70
kg person. If the target concentration
is 10 ugr/ml, then the loading dose is :
Loading dose = Target Cp . Vss/F
= 10 g/ml . 35 L = 350 mg
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Examples of pharmacokinetic
calculation
Maintenance dose rate = clearance .
concentration
= 3 l/h . 10 mg/l = 30 mg/h
= 720 mg/day
Half-life = 0.693 . Vd/CL = 0.693 . 35 L/ 31/h
= 8 hours
The expected time to achieve 90 % Css is
about 4 half-lives or 32 hours
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