DRUGS THAT
INTERFERE WITH NOREPINEPHRINE SYNTHESIS
Metyrosine (Demser) is an example of this class of
drugs. Chemically, metyrosine is -methyl tyrosine. The drug blocks the action
of tyrosine hydroxylase, the rate-limiting enzyme in the synthesis of
catecholamines. Unlike α-methyldopa, metyrosine is not itself incorpo-rated into the
catecholamine synthetic pathway. The ul-timate action of the drug is to
decrease the production of catecholamines.
Metyrosine is well absorbed
from the gastrointesti-nal tract and is excreted in the urine largely as
un-changed drug.
Metyrosine is not employed
for the treatment of es-sential hypertension but rather is used for the
manage-ment of pheochromocytoma. It is useful for preopera-tive treatment and
for long-term therapy when surgery is not feasible.
Sedation is the most common
adverse effect of metyrosine. Other CNS disturbances, such as anxiety,
confusion, and disorientation, have also been reported. Symptoms of sympathetic
nervous system depression in general, such as nasal congestion and dryness of
mouth, can also occur.
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