Rilmenidine

Overview

Rilmenidine is an imidazoline receptor agonist medication prescribed for the treatment of hypertension. It is taken orally and marketed under the brand names Albarel, Hyperium, Iterium and Tenaxum.[1] WP

Uses, dosage and effects

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 be required. Rilmenidine is only slightly dialysable. WP

Risks and side effects

Contraindications

Severe depression, severe kidney failure (creatinine clearance <15 ml/min), as a precaution in the absence of currently available studies. WP

Precautions

• 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). WP
• Alcohol consumption should be avoided during treatment. WP
• In patients with kidney failure, no dosage adjustment is necessary if creatinine clearance is greater than 15 mL/min. WP
• In the absence of documented experiments in this area, rilmenidine is not recommended for prescription to children. WP
• 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. WP
• Lactation: rilmenidine is excreted in breast milk, and its use is therefore not recommended during lactation. WP
• 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 or machine operators should be warned of the possibility of drowsiness. WP

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. WP
• At a dose of 2 mg per day of rilmenidine, controlled comparative studies versus clonidine (0.15 to 0.30 mg/day) or alpha-methyldopa (500 to 1000 mg/day) demonstrated that the incidence of side effects was significantly lower with rilmenidine than with either clonidine or a-methyldopa. WP⚠ Wikipedia itself has flagged this text: citation needed.

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. WP

Interactions

Drug interactions

Combination with MAOIs is not recommended; combination with tricyclic antidepressants requires prudence, as the antihypertensive activity of rilmenidine may be partly antagonized. WP

Pharmacology

Mechanism of action

Rilmenidine, an oxazoline compound with antihypertensive properties, acts on both medullary and peripheral vasomotor structures. WP

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.[2–5] WP

Research

Research

The drug has been shown to mimic the lifespan-extending effects of calorie restriction in cell cultures and in the worm C. elegans.[4] WP

Chemistry

Formula

C10H16N2O PC

CAS number

54187-04-1 PC

Molar mass (g/mol)

180.25 PC

IUPAC name (computed by PubChem)

N-(dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amine PC

SMILES

C1CC1C(C2CC2)NC3=NCCO3 PC

InChIKey

CQXADFVORZEARL-UHFFFAOYSA-N PC

PubChem CID

68712

IUPAC name

N-(dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amine WP

Harm reduction information

No harm reduction data is on file for this compound yet. That means no dose, timing or combination data from PsychonautWiki or TripSit. Please don't guess a dose from similar compounds. If you have taken it and feel unwell, contact emergency services or a poison control center.

User reports

Pop culture

No references added yet.

Sources

1. Journal / agency Remková A, Kratochvíl'ová H. Effect of the new centrally acting antihypertensive agent rilmenidine on endothelial and platelet function in essential hypertension. Journal of Human Hypertension. August 2002. doi:10.1038/sj.jhh.1001427 · PMID 12149660
2. Journal / agency Cobos-Puc L, Aguayo-Morales H. Cardiovascular Effects Mediated by Imidazoline Drugs: An Update. Cardiovascular & Hematological Disorders Drug Targets. 2019. doi:10.2174/1871529X18666180629170336 · PMID 29962350
3. Journal / agency Bousquet P, Hudson A, García-Sevilla JA, Li JX. Imidazoline Receptor System: The Past, the Present, and the Future. Pharmacological Reviews. January 2020. doi:10.1124/pr.118.016311 · PMID 31819014
4. Journal / agency Bennett DF, Goyala A, Statzer C, Beckett CW, Tyshkovskiy A, Gladyshev VN, Ewald CY, de Magalhães JP. Rilmenidine extends lifespan and healthspan in Caenorhabditis elegans via a nischarin I1-imidazoline receptor. Aging Cell. February 2023. doi:10.1111/acel.13774 · PMID 36670049 · PMC9924948
5. Journal / agency Yalçın MB, Bora ES, Çakır A, Akbulut S, Erbaş O. Autophagy and anti-inflammation ameliorate diabetic neuropathy with Rilmenidine. Acta Cirurgica Brasileira. 2023. doi:10.1590/acb387823 · PMID 38055406 · PMC10691181

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