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Guanethidine chemical structure
| CAS number |
| ATC code |
| PubChem |
| DrugBank |
|Molecular weight||198.309 g/mol|
|Elimination half-life||1.5 days|
|Routes of administration|
Guanethidine is transported by uptake 1 into the presynaptic terminal. (In this it competes with noradrenaline so can potentiate exogenously applied noradrenaline). Once inside the terminal it blocks the release of noradrenaline in response to arrival of an action potential. Spontaneous release is not affected.
Guanethidine was once a mainstay for hypertension resistant to other agents, but it is now rarely used in the US due to side effects and because substantially better drugs are available. It is still licensed in some countries, e.g. UK, for the rapid control of blood pressure in a hypertensive emergency.
- ↑ Joyce PI, Rizzi D, Caló G, Rowbotham DJ, Lambert DG (November 2002). The effect of guanethidine and local anesthetics on the electrically stimulated mouse vas deferens. Anesth. Analg. 95 (5): 1339–43, table of contents.