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20-September-2008 09:55:49 - Rilmenidine Rilmenidine Systematic IUPAC name N-dicyclopropylmethyl-4,5-dihydro-1,3-oxazol-2-amine Identifiers CAS number 54187-04-1 ATC code C02AC06 PubChem 68712 Chemical data Formula C10H16N2O Mol. mass 180.247 g/mol Pharmacokinetic data Bioavailability ? Protein binding 7% Metabolism Minimal Half life 8 hours Excretion Renal, unchanged Therapeutic considerations Pregnancy cat. ? Legal status Routes Oral Rilmenidine is a prescription medication administered to treat hypertension.1 It is marketed under the brand name HYPERIUM. Contents 1 Form and composition 2 Mode of action 3 Indications 4 Contraindications 5 Warning 6 Precautions 7 Drug interactions 8 Side effects 9 Dosage and route of administration 10 Overdosage 11 References Form and composition Each tablet contains 1.544 mg rilmenidine dihydrogen phosphate, an amount equivalent to 1 mg rilmenidine base. Mode of action Hyperium, an oxazoline compound with antihypertensive properties, acts on both medullary and peripheral vasomotor structures. Hyperium shows greater selectivity for imidazoline receptors than for cerebral alpha2-adrenergic receptors, distinguishing it from reference alpha2-agonists. Indications Hypertension. Contraindications Severe depression, severe renal failure creatinine clearance 15 ml/min, as a precaution in the absence of currently available studies. Warning Therapy should never be interrupted suddenly; the dosage should be reduced gradually. Precautions As with all antihypertensive agents, regular medical monitoring is required when Hyperium is administered to patients with a recent history of cardiovascular disease stroke, myocardial infarction. Alcohol consumption should be avoided during treatment. In patients with renal failure, no dosage adjustment is necessary if creatinine clearance is greater than 15 mL/min. In the absence of documented experiments in this area, Hyperium is not recommended for prescription to children. Pregnancy: as with all new molecules, administration of Hyperium should be avoided in pregnant women, although no teratogenic or embryotoxic effects have been observed in animal studies. Lactation: Hyperium 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 Hyperium to have any effect on alertness at therapeutic doses 1or 2 daily administrations of 1 mg. If these doses are exceeded, or if Hyperium is combined with other drugs capable of reducing alertness, vehicle drivers or machine operators should be warned of the possibility of drowsiness. Drug interactions Combinations not recommended: combination with MAOIs is not recommended; combination with tricyclic antidepressants requires prudence, as the antihypertensive activity of Hyperium may be partly antagonized. Side effects At a dose of 1 mg given as a single daily administration during controlled trials, the incidence of side effects was comparable to that observed with placebo. At a dose of 2 mg per day of Hyperium, controlled comparative studies versus clonidine 0.15 to 0.30 mg/day or alpha2-methyldopa 500 to 1000 mg/day demonstrated that the incidence of side effects was significantly lower with Hyperium than with either clonidine or a-methyldopa. Side-effects are rare, non-severe, and transient at therapeutic doses: asthenia, palpitations, insomnia, drowsiness, fatigue on exercise, epigastric pain, dryness of the mouth, diarrhea, skin rash; and exceptionally, cold extremities, postural hypotension, sexual disorders, anxiety, depression, pruritus, edema, cramps, nausea, constipation, hot flushes. Dosage and route of administration The recommended dosage is 1 tablet per day as a single morning administration. 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, Hyperium may be administered to both elderly and diabetic hypertensive patients. In patients with renal failure, no dosage adjustment is necessary in principle when the creatinine clearance is greater than 15 mL/min. Treatment may be continued indefinitely. Overdosage No cases of massive absorption have been reported. Likely symptoms in such an eventuality would be marked hypotension and lowered alertness. In addition to gastric lavage, sympathomimetic agents may also required. Hyperium is only slightly dialysable. References ^ Remková A, Kratochvíl'ová H August 2002. Effect of the new centrally acting antihypertensive agent rilmenidine on endothelial and platelet function in essential hypertension. J Hum Hypertens 16 8: 549-55. doi:10.1038/sj.jhh.1001427. PMID 12149660. v d e Adrenergic agonists models/most important in CAPS α α1 METHOXAMINE - Methylnorepinephrine - Oxymetazoline - PHENYLEPHRINE - Metaraminol α2 4-NEMD - CLONIDINE - Guanfacine - Guanabenz - Guanoxabenz - Guanethidine - Xylazine - METHYLDOPA - Apraclonidine - Brimonidine - Detomidine - Dexmedetomidine - Lofexidine - Romifidine - Tizanidine - Xylometazoline Undetermined/ unsorted Amidephrine - Amitraz - Anisodamine - Ergotamine - Indanidine - Medetomidine - Mephentermine - Midodrine - Mivazerol - Naphazoline - Norfenefrine - Octopamine - Phenylpropanolamine - Rilmenidine - Synephrine - Talipexole - Tetrahydrozoline - Xylometazoline β β1 DOBUTAMINE - Dopamine - Denopamine - Xamoterol β2 Short acting β2-agonists: SALBUTAMOL/Levosalbutamol - Fenoterol - TERBUTALINE - Pirbuterol - Procaterol - Bitolterol - Rimiterol - Carbuterol - Tulobuterol - Reproterol - Dopexamine Long acting β2-agonists LABA: Arformoterol - Bambuterol - Clenbuterol - Formoterol - Salmeterol Orciprenaline/metaproterenol - Ritodrine - Hexoprenaline - Indacaterol β3 Amibegron - Solabegron Undetermined/ unsorted Arbutamine - Befunolol - Isoxsuprine - Nylidrin - Oxyfedrine - Prenalterol - Ractopamine - Bromoacetylalprenololmenthane - Broxaterol - Cimaterol - Higenamine - Mabuterol - Methoxyphenamine - Tretoquinol - Zinterol Nonselective β ISOPRENALINE/ISOPROTERENOL α and β Epinephrine α1+2, β1+2 - Norepinephrine α1+2, β1 - Cirazoline - Etilefrine Indirect/ mixed Indirect presynaptic norepinephrine release: Amphetamine - Tyramine Mixed: Ephedrine - Pseudoephedrine Cocaine see also monoamine oxidase inhibitor v d e Antihypertensives C02 and diuretics C03 Sympatholytic agents Centrally acting/antiadrenergics α2 agonist Clonidine, Guanfacine, Methyldopa imidazoline receptor agonist Moxonidine, Rilmenidine adrenergic uptake inhibitor Rescinnamine, Reserpine Ganglion-blocking/nicotinic antagonist Mecamylamine, Trimethaphan Peripherally acting/antiadrenergics α1 blockers: Prazosin Indoramin Trimazosin Doxazosin Urapidil Guanidine derivatives: Betanidine Guanethidine Guanoxan Debrisoquine Guanoclor Guanazodine Guanoxabenz Vasodilators Diazoxide hydrazinophthalazine Hydralazine, Dihydralazine, Endralazine, Cadralazine Minoxidil Nitroprusside Phentolamine Other antihypertensives serotonin antagonist Ketanserin endothelin receptor antagonist Bosentan, Ambrisentan, Sitaxsentan MAOI Pargyline THI Metirosine Diuretics Low ceiling Thiazides at DCT Bendroflumethiazide Hydroflumethiazide Hydrochlorothiazide Chlorothiazide Polythiazide Trichlormethiazide Cyclopenthiazide Methyclothiazide Cyclothiazide Mebutizide Sulfonamides Quinethazone Clopamide Chlortalidone Mefruside Clofenamide Metolazone Meticrane Xipamide Indapamide Clorexolone Fenquizone Other Mersalyl Theobromine Cicletanine osmotic Mannitol, Urea carbonic anhydrase inhibitor at PT Acetazolamide High ceiling Loop diuretic at AL Bumetanide, Furosemide, Torasemide, Ethacrynic acid Potassium-sparing at CD ESC blockers Amiloride, Triamterene aldosterone antagonists Spironolactone, Eplerenone, Potassium canrenoate, Canrenone Retrieved from http://en..org/wiki/Rilmenidine Categories: Antihypertensive agents Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page This page was last modified on 22 July 2008, at 18:35
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