Guanadrel: Difference between revisions
Gerald Chi (talk | contribs) mNo edit summary |
Rabin Bista (talk | contribs) No edit summary |
||
| Line 1: | Line 1: | ||
{{chembox | {{chembox new | ||
| Verifiedfields = changed | | Verifiedfields = changed | ||
| Watchedfields = changed | | Watchedfields = changed | ||
| Line 5: | Line 5: | ||
| UNII = 765C9332T4 | | UNII = 765C9332T4 | ||
| verifiedrevid = 407386127 | | verifiedrevid = 407386127 | ||
|ImageFile=Guanadrel.png | |ImageFile=Guanadrel Wiki str.png | ||
|ImageSize= | |ImageSize= | ||
|IUPACName=2-(1,4-Dioxaspiro[4.5]decan-2-ylmethyl)guanidine | |IUPACName=2-(1,4-Dioxaspiro[4.5]decan-2-ylmethyl)guanidine | ||
| Line 49: | Line 49: | ||
}} | }} | ||
__NOTOC__ | __NOTOC__ | ||
{{SI}} | |||
{{CMG}} | {{CMG}} | ||
==Overview== | ==Overview== | ||
| Line 66: | Line 66: | ||
{{Reflist|2}} | {{Reflist|2}} | ||
[[Category:drug]] | |||
[[Category:Ketals]] | [[Category:Ketals]] | ||
[[Category:Guanidines]] | [[Category:Guanidines]] | ||
[[Category:Antihypertensive agents]] | [[Category:Antihypertensive agents]] | ||
Revision as of 13:10, 15 April 2015
|
WikiDoc Resources for Guanadrel |
|
Articles |
|---|
|
Most recent articles on Guanadrel |
|
Media |
|
Evidence Based Medicine |
|
Clinical Trials |
|
Ongoing Trials on Guanadrel at Clinical Trials.gov Clinical Trials on Guanadrel at Google
|
|
Guidelines / Policies / Govt |
|
US National Guidelines Clearinghouse on Guanadrel
|
|
Books |
|
News |
|
Commentary |
|
Definitions |
|
Patient Resources / Community |
|
Patient resources on Guanadrel Discussion groups on Guanadrel Directions to Hospitals Treating Guanadrel Risk calculators and risk factors for Guanadrel
|
|
Healthcare Provider Resources |
|
Causes & Risk Factors for Guanadrel |
|
Continuing Medical Education (CME) |
|
International |
|
|
|
Business |
|
Experimental / Informatics |
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]
Overview
Guanadrel is an antihypertensive agent.[1] It is used in the form of its sulfate.
Mechanism of action
Guanadrel is a postganglionic adrenergic blocking agent. Uptake of guanadrel and storage in sympathetic neurons occurs via the norepinephrine pump; guanadrel slowly displaces norepinephrine from its storage in nerve endings and thereby blocks the release of norepinephrine normally produced by nerve stimulation. The reduction in neurotransmitter release in response to sympathetic nerve stimulation, as a result of catecholamine depletion, leads to reduced arteriolar vasoconstriction, especially the reflex increase in sympathetic tone that occurs with a change in position. Guanadrel is rapidly and well absorbed from gastrointestinal tract.[2]
In 1981 the JAMA reported guanadrel as an effective step II or step III treatment of hypertension.[3]
Chemistry
Guanadrel can be synthesized when cyclohexanone undergoes ketalization by 3-chloro-1,2-propanediol, forming 2-chloromethyl-1,4-dioxyspiro[4,5]decane, which is further reacted with sodium phthalimide.[4][5][6] After alkaline hydrazinolysis, the resulting phthalimide derivative is transformed into 2-aminomethyl-1,4-dioxyspiro[4,5]decane, which is reacted with S-methylthiourea, giving the desired guanadrel.
References
- ↑ Oren A, Rotmensch HH, Vlasses PH; et al. (1985). "A dose-titration trial of guanadrel as step-two therapy in essential hypertension". J Clin Pharmacol. 25 (5): 343–6. doi:10.1002/j.1552-4604.1985.tb02852.x. PMID 4031111.
- ↑ Guanadrel, from Pharmacogenetics Knowledge Base
- ↑ M. I. Dunn and J. L. Dunlap (1981). "Guanadrel. A new antihypertensive drug". JAMA. 245 (16): 1639–42. doi:10.1001/jama.1981.03310410017019. PMID 7206175.
- ↑ W.R. Hardie, J.E. Aaron, FR 1522153 (1968)
- ↑ W.R. Hardie, J.E. Aaron, S. Afr. Pat. 67 06.328 (1968)
- ↑ J.E. Aaron, W.R. Hardie, Template:US Patent (1970)