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Author: Admin | 2025-04-28
From Wikipedia, the free encyclopedia RilmenidineClinical dataTrade namesAlbarelAHFS/Drugs.comInternational Drug NamesRoutes ofadministrationOralATC codeC02AC06 (WHO) Legal statusLegal statusIn general: ℞ (Prescription only)Pharmacokinetic dataProtein binding7%MetabolismMinimalElimination half-life8 hoursExcretionRenal, unchangedIdentifiersIUPAC nameN-(dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amineCAS Number54187-04-1 PubChem CID68712ChemSpider61963 UNIIP67IM25ID8ChEMBLChEMBL289480 CompTox Dashboard (EPA)DTXSID3045194 ECHA InfoCard100.053.638 Chemical and physical dataFormulaC10H16N2OMolar mass180.251 g·mol−13D model (JSmol)Interactive imageSMILESO1CCN=C1NC(C2CC2)C3CC3InChIInChI=1S/C10H16N2O/c1-2-7(1)9(8-3-4-8)12-10-11-5-6-13-10/h7-9H,1-6H2,(H,11,12) Key:CQXADFVORZEARL-UHFFFAOYSA-N (what is this?) (verify)Rilmenidine is a prescription medication for the treatment of hypertension.[1] It is taken orally and marketed under the brand names Albarel, Hyperium, Iterium and Tenaxum.Mechanism of action[edit]Rilmenidine, an oxazoline compound with antihypertensive properties, acts on both medullary and peripheral vasomotor structures. Rilmenidine is a imidazoline analog and shows greater selectivity for imidazoline receptors than for cerebral alpha2-adrenergic receptors, distinguishing it from reference alpha2-agonists, and conferring additional anti-inflammatory actions not shared with most other antihypertensive drugs.[2][3][4][5]Severe depression, severe kidney failure (creatinine clearance Dosage and route of administration[edit]The recommended dosage is 1 tablet per day as a single morning administration. (Each tablet contains 1.544 mg rilmenidine dihydrogen phosphate, an amount equivalent to 1 mg of rilmenidine base.) If results are not adequate after 1 month of treatment, the dosage may be increased to 2 tablets per day, given in divided doses (1 tablet morning and evening) before meals. As a result of its good clinical and biological acceptability, rilmenidine may be administered to both elderly and diabetic hypertensive patients. In patients with kidney failure, no dosage adjustment is necessary in principle when the creatinine clearance is greater than 15 mL/min. Treatment may be continued indefinitely. As with all antihypertensive agents, regular medical monitoring is required when rilmenidine is administered to patients with a recent history of cardiovascular disease (stroke, myocardial infarction).Alcohol consumption should be avoided during treatment.In patients with kidney failure, no dosage adjustment is necessary if creatinine clearance is greater than 15 mL/min.In the absence of documented experiments in this area, rilmenidine is not recommended for prescription to children.Pregnancy: as with all new molecules, administration of rilmenidine should be avoided in pregnant women, although no teratogenic or embryotoxic effects have been observed in animal studies.Lactation: rilmenidine is excreted in breast milk, and its use is therefore not recommended during lactation.Effects on the ability to drive motor vehicles or operate machinery: double-blind, placebo-controlled studies have not shown rilmenidine to have any effect on alertness at therapeutic doses (1 or 2 daily administrations of 1 mg). If these doses are exceeded, or if rilmenidine is combined with other drugs capable of reducing alertness, vehicle drivers
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