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Chemical Compound Review

Hyperium     N-(dicyclopropylmethyl)-4,5- dihydro-1,3...

Synonyms: Rilmenidia, Rilmenidene, Rilmenidine, Rilmenidinum, Oxaminozoline, ...
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Disease relevance of C11120

  • Rilmenidine is a novel antihypertensive agent related to alpha 2-adrenoceptor agonist, used in the treatment of mild or moderate hypertension at the oral dose of 1 mg once a day or 1 mg twice a day [1].
  • It showed stable plasma concentrations of rilmenidine during a six-month treatment in hypertensive patients with renal insufficiency, reflecting the absence of accumulation of the drug [2].
  • In conclusion, this study confirmed the good acceptability of rilmenidine in hypertensive patients with chronic renal insufficiency [2].
  • METHODS AND RESULTS: Rilmenidine micro-injected into the rostral ventrolateral medulla produced hypotension and inhibition of renal sympathetic nerve activity with doses an order of magnitude lower than those required in the nucleus tractus solitarius [3].
  • CONCLUSIONS: These results suggest that the hypotension and bradycardia induced by intravenous administration of moxonidine and rilmenidine were mediated mainly by actions on central imidazoline receptors whereas clonidine appears to act predominantly on central alpha 2-adrenoceptors [4].

Psychiatry related information on C11120

  • The level of vigilance was first determined by assessing drowsiness using visual analogue scales and/or by several psychometric tests in four pharmacoclinical studies in healthy subjects or in hypertensive patients: three studies with single administration of rilmenidine (0.5 to 3.0 mg) and one study with repeated administration for three days [5].
  • Nevertheless, although it binds to alpha 2-adrenoceptors, rilmenidine did not cause sedation in animal models: at doses up to 10 mg/kg in mice and rats, it did not prolong the barbiturate-induced sleeping time and did not modify the spontaneous locomotor activity in rats at doses up to 2.5 mg/kg [6].
  • Cessation of rilmenidine infusion resulted in somewhat similar cardiovascular and behavioral disturbances, but unlike clonidine there was a return to normal rapid eye movement sleep without rebound [7].

High impact information on C11120


Chemical compound and disease context of C11120


Biological context of C11120


Anatomical context of C11120


Associations of C11120 with other chemical compounds


Gene context of C11120


Analytical, diagnostic and therapeutic context of C11120

  • Plasma concentrations of rilmenidine were measured by gas chromatography combined with mass spectrometry at Days 0, 1, 5, 7, 9, and 11, and Months 1.5, 3, 4.5, and 6 before administration [2].
  • DESIGN AND METHODS: We used a randomized, double-blind, 6-week cross-over study, with a 1-week placebo run-in period, two 2-week active treatment intervals (rilmenidine 1 mg twice daily or placebo) and intervening 1-week placebo washout [25].
  • Recordings were obtained from eight subjects, using a Portapres during two 24-h hospitalizations: the first after the inclusion visit and the second 4 weeks after starting rilmenidine treatment (1 or 2 mg/day) [26].
  • Renal denervation altered the hemodynamic and renal effects following intracerebroventricular administration of the I1-imidazoline receptor agonist, rilmenidine, in pentobarbital anaesthetized rats [27].
  • Systemic rilmenidine (600 microg/kg i.v.) elicited hypotension and bradycardia along with significant elevation in MAPK(p42/44), detected by immunohistochemistry, in RVLM neurons [28].


  1. Pharmacokinetics of rilmenidine. Genissel, P., Bromet, N. Am. J. Med. (1989) [Pubmed]
  2. Acceptability of rilmenidine and long-term surveillance of plasma concentrations in hypertensive patients with renal insufficiency. Lins, R.L., Daelemans, R., Dratwa, M., Verbeelen, D., Sennesael, J., Brisgand, B., Lameire, N. Am. J. Med. (1989) [Pubmed]
  3. Relative importance of medullary brain nuclei for the sympatho-inhibitory actions of rilmenidine in the anaesthetized rabbit. Head, G.A., Burke, S.L. J. Hypertens. (1998) [Pubmed]
  4. Relative importance of central imidazoline receptors for the antihypertensive effects of moxonidine and rilmenidine. Chan, C.K., Head, G.A. J. Hypertens. (1996) [Pubmed]
  5. Rilmenidine and vigilance. Review of clinical studies. Mahieux, F. Am. J. Med. (1989) [Pubmed]
  6. Recent advances in the pharmacology of rilmenidine. Montastruc, J.L., Macquin-Mavier, I., Tran, M.A., Damase-Michel, C., Koenig-Berard, E., Valet, P. Am. J. Med. (1989) [Pubmed]
  7. Effects of continuous infusions (10 days) and cessation of infusions of clonidine and rilmenidine (S 3341) on cardiovascular and behavioral parameters of spontaneously hypertensive rats. Jarrott, B., Lewis, S.J., Doyle, A.E., Louis, W.J. Am. J. Cardiol. (1988) [Pubmed]
  8. Treatment of hypertension in diabetic patients. Lambert, A.E., Mpoy, M., Vandeleene, B., Ketelslegers, J.M. Am. J. Med. (1989) [Pubmed]
  9. Effort blood pressure control in the course of antihypertensive treatment. de Divitiis, O., Di Somma, S., Liguori, V., Petitto, M., Magnotta, C., Ausiello, M., Natale, N., Brignoli, M., Galderisi, M. Am. J. Med. (1989) [Pubmed]
  10. Rilmenidine: a novel antihypertensive agent. Safar, M.E. Am. J. Med. (1989) [Pubmed]
  11. Antihypertensive drugs and baroreflex sensitivity. Effects of rilmenidine. Harron, D.W. Am. J. Med. (1989) [Pubmed]
  12. Drugs acting on imidazoline receptors: a review of their pharmacology, their use in blood pressure control and their potential interest in cardioprotection. Bousquet, P., Feldman, J. Drugs (1999) [Pubmed]
  13. Remodelling of the heart in DOCA-salt hypertensive rats by propranolol and by an alpha-2 agonist, rilmenidine. Callens-el Amrani, F., Paolaggi, F., Swynghedauw, B. J. Hypertens. (1989) [Pubmed]
  14. Renal excretory actions of antihypertensive agents. Effects of rilmenidine. Leary, W.P. Am. J. Med. (1989) [Pubmed]
  15. Protective effects of rilmenidine and AGN 192403 on oxidative cytotoxicity and mitochondrial inhibitor-induced cytotoxicity in astrocytes. Choi, D.H., Kim, D.H., Park, Y.G., Chun, B.G., Choi, S.H. Free Radic. Biol. Med. (2002) [Pubmed]
  16. Rilmenidine elevates cytosolic free calcium concentration in suspended cerebral astrocytes. Ozog, M.A., Wilson, J.X., Dixon, S.J., Cechetto, D.F. J. Neurochem. (1998) [Pubmed]
  17. Sympathetic modulation of renal blood flow by rilmenidine and captopril: central vs. peripheral effects. Janssen, B.J., Lukoshkova, E.V., Head, G.A. Am. J. Physiol. Renal Physiol. (2002) [Pubmed]
  18. Regulation of phenylethanolamine N-methyltransferase gene expression by imidazoline receptors in adrenal chromaffin cells. Evinger, M.J., Ernsberger, P., Regunathan, S., Reis, D.J. J. Neurochem. (1995) [Pubmed]
  19. Contribution of imidazoline receptors and alpha2-adrenoceptors in the rostral ventrolateral medulla to sympathetic baroreflex inhibition by systemic rilmenidine. Chan, C.K., Burke, S.L., Head, G.A. J. Hypertens. (2007) [Pubmed]
  20. Haemodynamic and metabolic effects of rilmenidine in hypertensive patients with metabolic syndrome X. A double-blind parallel study versus amlodipine. De Luca, N., Izzo, R., Fontana, D., Iovino, G., Argenziano, L., Vecchione, C., Trimarco, B. J. Hypertens. (2000) [Pubmed]
  21. Imidazoline receptor antisera-selected (IRAS) cDNA: cloning and characterization. Piletz, J.E., Ivanov, T.R., Sharp, J.D., Ernsberger, P., Chang, C.H., Pickard, R.T., Gold, G., Roth, B., Zhu, H., Jones, J.C., Baldwin, J., Reis, D.J. DNA Cell Biol. (2000) [Pubmed]
  22. The hypotensive action of rilmenidine is dependent on functional N-methyl-D-aspartate receptor in the rostral ventrolateral medulla of conscious spontaneously hypertensive rats. Zhang, J., Abdel-Rahman, A.A. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
  23. [3H]Rilmenidine-labelled imidazoline-receptor binding sites co-localize with [3H]2-(benzofuranyl)-2-imidazoline-labelled imidazoline-receptor binding sites and monoamine oxidase-B in rabbit, but not rat, kidney. King, P.R., Suzuki, S., Hosseini, A.R., Iakovidis, D., Nero, T.L., Jackman, G.P., Louis, W.J., Gundlach, A.L. J. Auton. Nerv. Syst. (1998) [Pubmed]
  24. Involvement of phosphatidylcholine-selective phospholipase C in activation of mitogen-activated protein kinase pathways in imidazoline receptor antisera-selected protein. Li, F., Wu, N., Su, R.B., Zheng, J.Q., Xu, B., Lu, X.Q., Cong, B., Li, J. J. Cell. Biochem. (2006) [Pubmed]
  25. Rilmenidine sympatholytic activity preserves mental stress, orthostatic sympathetic responses and adrenaline secretion. Esler, M., Lux, A., Jennings, G., Hastings, J., Socratous, F., Lambert, G. J. Hypertens. (2004) [Pubmed]
  26. Effects of rilmenidine on 24-h rhythmicity of blood pressure and spontaneous baroreflex sensitivity in essential hypertensive subjects. Finta, E., Laude, D., Alföldi, S., Farsang, C., Elghozi, J.L. J. Hypertens. (2006) [Pubmed]
  27. Renal denervation altered the hemodynamic and renal effects following intracerebroventricular administration of the I1-imidazoline receptor agonist, rilmenidine, in pentobarbital anaesthetized rats. Penner, S.B., Smyth, D.D. Neurochem. Int. (1997) [Pubmed]
  28. Mitogen-activated protein kinase phosphorylation in the rostral ventrolateral medulla plays a key role in imidazoline (i1)-receptor-mediated hypotension. Zhang, J., Abdel-Rahman, A.A. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
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