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RX BIN: 015558RX PCN: HTGroup ID: DDN6600Card Holder ID: DDN6600
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Guanethidine volume of distribution

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2018 Statistics

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Clients Benefit 29%


Total savings $4,735,080

What is Guanethidine

An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues.

Guanethidine mechanism of action

Guanethidine 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. It is taken up by norepinephrine transporters. It becomes concentrated in NE transmitter vesicles, replacing NE in these vesicles. This leads to a gradual depletion of NE stores in the nerve endings. Once inside the terminal it blocks the release of noradrenaline in response to arrival of an action potential. In contrast to ganglionic blocking agents, Guanethidine 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, Guanethidine 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.

Dosage forms of Guanethidine

Tabletoral10 mg
Tabletoral25 mg

Prescription Generics


International Brands

Apo Guanethidine Sulfate Tab 10mg


(2-(hexahydro-1(2h)-azocinyl)ethyl)guanidine (2-(Octahydro-1-azocinyl)ethyl)guanidine


Apotex Inc

CAS number






Affected organisms

Humans and other mammals

Indication of Guanethidine

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

Toxicity of Guanethidine

Side effects include drowsiness, dizziness, tiredness or confusion. LD sub50 /sub=1000 mg/kg (mouse, oral)

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