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7/28/2019 Organized Part 1
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Volume of distribution (Vd)It is the proportionality constant that relates
drug concentration in a reference fluid, typicallyplasma, to the amount of drug distributed
throughout the body.
Vd =
ClearanceIt is the most useful pharmacokinetic
indicator of irreversible loss of drug from the
body and refers to a volume of fluid from which
drug appears to be removed in a given amountof time.
Clearance =
amount of drug in the bodydrug concentration
Rate of distributionConcentration
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Zero-Order KineticIt is typically found when an enzyme or
transport system becomes saturated & the rateprocess becomes constant & cannot be increased
by increases in the concentration of substrate.
Zero- order rate processes are typically of
constant rate intravenous infusions andprolonged release dosage forms.
If the amount of the drug that is converted to
a metabolite is constant with respect to time, the
reaction is said to be zero-order and expressedas:
-dD/dt = koWhere Ko is the zero-order rate constant with
the units as mass per time (mg/ml).
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First Order KineticIt is when the amount of the drug in the body
is converted to a metabolite at a rate that is aconstant fraction of the amount of the drug in
the body, the conversion of D to M.
kD= dD/ dtwhere k is the first order rate constant
expressed in units of reciprocal time (min-1)
Loading DoseIt is a dose of medication administered for
the purpose of establishing a therapeutic level of
the mediaction.
Loading Dose =(C) (V)F
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Steady-State ConcentrationThe concentration of a drug or chemical in a
body fluid usually plasma at the time asteady state has been achieved, and rates of
drug administration and drug elimination are
equal. It is a value approached as a limit and is
achieved, theoretically, following the last of aninfinite number of equal doses given at equal
intervals.
Css= Km x RVmax - R
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pH negative logarithm of Hyrdronium ionconcentration
pH Normality interms ofHydroniumIonNormality interms ofHyrdroxyl Ion
0 1 10-14
1 10-1 10-132 10-2 10-12Increasing 3 10-3 10-11acidity 4 10-4 10-105 10-5 10-9
6 10-6 108Neutral point 7 10-7 10-78 10-8 10-6
9 10-9 10-5
10 10-10
10-4
11 10-11 10-3Increasing 12 10-12 10-2alkalinity 13 10-13 10-114 10-14 1
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pKa Values of Some Common DrugsDrugs pKa value
Acidic drugsAspirin 3.5
Paracetamol 9.5
phenobarbital 7.4 (first
ionization)
Basic drugs
Cocaine 8.6
Diazepam 3.3Diphynhydramine 90
Amphoteric drugs
Morphine 8.0 (amine),
9.9 (phenol)Adrenaline
(epinephrine)
8.7 (amine),
10.2, 12.0
(phenols)
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FOR WEAK ACIDS
pH = pKa compound is approximately 50%
ionized
pH = pKa +1 compound is approximately 90%
ionized
pH = pKa + 2 compound is approximately 99%
ionized
pH = pKa +3 compound is approximately 99.9%
ionizedPh = pKa + 4 compound is approximately 99.99%
ionized
FOR WEAK BASES
pH = pKa compound is approximately 50%ionized
pH =pKa compound is approximately 90%
ionized
pH = pKa compound is approximately 99%
ionized
pH = pKa compound is approximately 99.9%ionised
pH = pKa compound is approximately
99.99% ionised
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Percent IonizationIt is the percentage of weak electrolyte that
ionizes in a solution of given concentration.
Partition CoefficientIt is the ratio of the concentration of a
chemical species absorbed or dissolved by 1
phase to the concentration of the species in
other phase.
K= [Organic acid in oil][ Organic acid in water] by mass