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guanethidine

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Also known as SU-5864, N-(2-perhydroazocin-1-ylethyl)guanidine, 1-(2-guanidinoethyl)-heptamethylenimine, {2-[hexahydro-1(2H)-azocinyl]ethyl}-guanidine, 1-(2-guanidinoethyl)octahydroazocine, 2-(1-N,N-heptamethyleneimino)ethylguanidine, 2-(1′-azacyclooctyl)ethylguanidine, [2-(octahydro-1-azocinyl)ethyl]guanidine

Guanethidine is an antihypertensive drug that reduces the release of catecholamines, such as norepinephrine. Guanethidine is transported across the sympathetic nerve membrane by the same mechanism that transports norepinephrine itself (NET, uptake 1), and uptake is essential for the drug's action. Once guanethidine has entered the nerve, it is concentrated in transmitter vesicles, where it replaces norepinephrine. It may also inhibit the release of granules by decreasing norepinephrine.

Research

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Encyclopedic overview

4 sections
Contents
  • Medical uses
  • Side effects
  • Pharmacology
  • References

Guanethidine is an antihypertensive drug that reduces the release of catecholamines, such as norepinephrine. Guanethidine is transported across the sympathetic nerve membrane by the same mechanism that transports norepinephrine itself (NET, uptake 1), and uptake is essential for the drug's action. Once guanethidine has entered the nerve, it is concentrated in transmitter vesicles, where it replaces norepinephrine. It may also inhibit the release of granules by decreasing norepinephrine.

==Medical uses== Guanethidine was once a mainstay for hypertension resistant to other agents, and was often used safely during pregnancy, but it is no longer used in the US due to lack of availability. It is still licensed in some countries, e.g., UK, for the rapid control of blood pressure in a hypertensive emergency.

Excerpted from Wikipedia’s “guanethidine” article, available under the CC BY-SA 4.0 licence.