Study Set Content:
metabolic products of drugs
that lacks the pharmacological activity of a drug.
INACTIVE METABOLITES-
undergo
glucuronidation it will transform into
an inactive metabolite, that is rapidly
eliminated.
Acetaminophen-
metabolic products of drugs
that has the pharmacological activity of a drug.
ACTIVE METABOLITES-
Codeine- demethylated it will
transform into an active analgesic
which is
morphine
Finally, drug-metabolizing enzymes have been exploited
in the design of pharmacologically inactive prodrugs that
are converted to (blank) in the body.
active molecules
Water Is a polar molecule because of the way the atoms bind in the
molecule such that there are excess (blank)on the Oxygen side
and a lack or (blank) on the Hydrogen side of the
molecule.
electrons , excess of positive charges
is a polar molecule with positive charges on one
side and negative on the other
water
molecule is one that the electrons are distributed more
symmetrically and thus does not have an abundance of charges at
the opposite sides. The charges all cancel out each other
NON-POLAR MOLECULE:
Most metabolic biotransformations occur between
absorption and renal elimination.
Few transformations occur in the
intestinal lumen or
intestinal wall.
In general, all oof these reactions can be assigned to
one of two major categories:
PHASE I and PHASE II
reactions.
PHASE I
usually convert the parent drug to a more polar metabolite
by introducing or unmasking a
functional group
Often these metabolites are inactive, although in some
instances activity is only
modified or even enhanced
If phase I metabolites are sufficiently polar, they may be
readily
excreted
However, many phase I products are not
eliminated rapidly and undergo a subsequent reaction in which an
endogenous substrate such as(blank) combines with the newly incorporated
functional group to form a highly polar conjugate.
glucuronic acid, sulfuric acid, acetic
acid, or an amino acid
Process involved: phase 1
Oxidation (most common)
Reduction
Hydrolysis
Introduction of OH
Oxidation (most common)
Enzymes:
mixed- function oxidases,
monooxygenases, cytchrome P450 association with
reductase enzyme ( contains NADP- co factor)
Reduction of aldehyde, ketone, nitro and azo
groups observed
Reduction
Reduction enzymes
reductase
