2. Introduction
● Initial definition:
A pharmacologically inactive chemical entity that when metabolized or
chemically transformed by a mammalian system is converted into a
pharmacologically active substance
● “Drug Latentiation” – included later
Process of purposely designing and synthesizing a molecule that specifically requires
“bioactivation” to a pharmacologically active substance
● Why use prodrugs?
Improve patient acceptability (decrease pain on injection)
Alter and improve absorption
Alter biodistribution
Alter metabolism
Alter elimination
3. Conversions of prodrug
● Metabolism (enzyme dependant)
● Chemical Methods (non-dependant)
– Hydrolysis
– Decarboxylation
– NOT patient dependant!
– Stability/Storage issues
4. ●
A prodrug is a precursor chemical compound of a drug.
●
Instead of administering a drug, a prodrug might be used instead to
improve how a medicine is A, D, M, E.
● Prodrugs are often designed to improve bioavailability when a drug
itself is poorly absorbed from the gastrointestinal tract.
● A prodrug may be used to improve how selectively the drug
interacts with cells or processes that are not its intended target.
●
This reduces adverse or unintended effects of a drug, especially
important in treatments like chemotherapy, which can have severe
unintended and undesirable side effects.
5. Classification
● Prodrugs can be classified into two major types, based on how the body
converts the prodrug into the final active drug form:
Type I
● prodrugs are bioactivated inside the cells (intracellularly).
● Examples of these are anti-viral nucleoside analogs that must be
phosphorylated and the lipid-lowering statins.
Type II
● prodrugs are bioactivated outside cells (extracellularly), especially in
digestive fluids or in the body's circulation system, particularly in the blood.
● Examples of Type II prodrugs are salicin and certain antibody-, gene- or
virus-directed enzyme prodrugs used in chemotherapy or immunotherapy.
6. Examples
● 6-Monoacetylmorphine (6-MAM) is a heroin
metabolite which converts into active morphine
in vivo.
● Diethylpropion is a diet pill that does not
become active as a monoamine releaser or
reuptake inhibitor until it has been N-
dealkylated to ethylpropion.
8. Introduction
● Endogenous, in biology is defined as “growing
or originating from within an organism.”
● Endogenous compounds are drugs that are
already present in the body either because the
body produces them or they are present in the
normal diet.
9. ● These compounds are identical to the drug that
is being administered, determining the amount
of drug released from the dosage form and
absorbed by each subject can be difficult.
● There are tests to be done to consider all those
compounds which are present in the body and
can act as a drug, or help other compounds act
as a drug.
10. ● These compounds are identical to the drug that
is being administered, determining the amount
of drug released from the dosage form and
absorbed by each subject can be difficult.
● There are tests to be done to consider all those
compounds which are present in the body and
can act as a drug, or help other compounds act
as a drug.
