Declinax: Full Drug Profile

Declinax - General Information

An adrenergic neuron-blocking drug similar in effects to guanethidine. It is also noteworthy in being a substrate for a polymorphic cytochrome P-450 enzyme. Persons with certain isoforms of this enzyme are unable to properly metabolize this and many other clinically important drugs. They are commonly referred to as having a debrisoquin 4-hydroxylase polymorphism. [PubChem]

Pharmacology of Declinax

Declinax is an adrenergic neuron-blocking drug similar in effects to guanethidine. It is a substrate for a polymorphic cytochrome P-450 enzyme. Persons with certain isoforms of this enzyme are unable to properly metabolize this and many other clinically important drugs. They are commonly referred to as having a debrisoquin 4-hydroxylase polymorphism.

Additional information about Declinax

Declinax Indication

For the treatment of moderate and severe hypertension, either alone or as an adjunct, and for the treatment of renal hypertension.

Mechanism Of Action

Declinax acts at the sympathetic neuroeffector junction by inhibiting or interfering with the release and/or distribution of norepinephrine, rather than acting at the effector cell by inhibiting the association of norepinephrine with its receptors. In contrast to ganglionic blocking agents, debrisoquin suppresses equally the responses mediated by alpha-and beta-adrenergic receptors but does not produce parasympathetic blockade. Since sympathetic blockade results in modest decreases in peripheral resistance and cardiac output, debrisoquin lowers blood pressure in the supine position. It further reduces blood pressure by decreasing the degree of vasoconstriction that normally results from reflex sympathetic nervous activity upon assumption of the upright posture, thus reducing venous return and cardiac output more.

Food Interactions

Take without regard to meals.

Generic Name

Debrisoquin

Synonyms

Debrisochinum; Debrisoquin hemisulfate; Debrisoquin sulfate; Debrisoquina [inn-spanish]; Debrisoquine; Debrisoquine sulfate; Debrisoquinum [inn-latin]; Isocaramidine; Isocaramidine sulfate

Drug Category

Adrenergic Agents; Antihypertensive Agents; Sympatholytics

Drug Type

Small Molecule; Approved

Other Brand Names containing Debrisoquin

Declinax; Equitonil; Tendor;

Biotransformation

Hepatic.

Chemical IUPAC Name

3,4-dihydro-1H-isoquinoline-2-carboximidamide

Chemical Formula

C10H13N3

Organisms Affected

Humans and other mammals