Rilmenidine

ATC code

C02AC06

Therapeutic class

Imidazoline receptor agonist · Centrally acting antihypertensive

Forms

oral tablet

Brand names

Rilmenidine Zydus (FR) · Hyperium (International) · Albarel (International)

Overall confidence

medium

Regulatory sources consulted

ANSM SPC for RILMENIDINE ZYDUS 1 mg (CIS: 69070613)
PubMed PMID:38807350 ↗
PubMed PMID:42414242 ↗
PubMed PMID:38126098 ↗
ANSM BDPM · CIS 69070613 ↗
RxNorm rxcui 55679 ↗
PubMed PMID:40722780 ↗

Approved indications

Arterial hypertension.
Potential anti-aging agent (calorie restriction mimetic). · investigational

Contraindications

Absolute

Hypersensitivity to rilmenidine or any of the excipients.
Severe depressive states.
Severe renal impairment (creatinine clearance < 15 ml/min).

Clinical warnings

Major warning · Never stop treatment abruptly; decrease the dose progressively to avoid rebound hypertension. — ANSM SPC
Risk of bradycardia. Use with caution in patients with pre-existing bradycardia or risk factors (e.g., elderly, sick sinus syndrome, AV block). — ANSM SPC
Alcohol consumption is not recommended during treatment due to potentiation of the sedative effect. — ANSM SPC

Drug interactions

HighBeta-blockers (except esmolol)C07
Mechanism: Risk of severe rebound hypertension upon abrupt withdrawal of the central antihypertensive while the patient is on beta-blocker therapy.
Recommendation: Avoid abrupt withdrawal of rilmenidine. Close clinical monitoring is required if discontinuation is necessary.
ANSM SPC
ModerateAlcoholV03AB
Mechanism: Potentiation of the sedative effect of rilmenidine.
Recommendation: Avoid consuming alcoholic beverages and medications containing alcohol during treatment.
ANSM SPC
HighSodium oxybateN07XX04
Mechanism: Increased central nervous system depression.
Recommendation: Association not recommended. Impaired alertness can make driving and using machinery dangerous.
ANSM SPC

Adverse events

Common (≥1%)

palpitations · somnolence · headache · dry mouth · asthenia · dizziness · gastralgia · anxiety · insomnia

Rare but serious

bradycardia · orthostatic hypotension · rebound hypertension (upon abrupt withdrawal)

Pregnancy and lactation

Pregnancy: Limited data. Avoid as a precaution. Lactation: Excreted in animal milk. Should not be used during breastfeeding.

Recent literature (PubMed)

Not first-line antihypertensive agents, but still effective-The efficacy and safety of imidazoline receptor agonists: A network meta-analysis.
Érszegi A, et al. · Pharmacol Res Perspect · 2024 · Relevance 5/5
Meta-análisis en red que evalúa la eficacia y seguridad de los agonistas de receptores de imidazolina. Concluye que son casi tan efectivos como los fármacos de primera línea (ej. enalapril) para reducir la presión arterial, pero su uso está limitado por efectos adversos como la boca seca (menor con rilmenidina que con clonidina) y la somnolencia. Se consideran una opción viable en hipertensión resistente, no en monoterapia de primera línea.
Pharmacology, Medicinal Chemistry, and Therapeutic Potential of Imidazoline Receptor Ligands.
Kouridaki ME, et al. · ChemMedChem · 2026 · Relevance 4/5
Revisión sobre la farmacología de los ligandos de receptores de imidazolina. Destaca que la rilmenidina, como ligando selectivo de I1R, muestra efectos antihipertensivos, metabólicos y neuroprotectores con una mejor selectividad sobre los receptores α2-adrenérgicos en comparación con agentes más antiguos. El sistema de receptores de imidazolina presenta oportunidades terapéuticas para trastornos cardiovasculares, metabólicos y neurodegenerativos.
New anti-aging strategies: a narrative review.
Stojić V, et al. · Acta Dermatovenerol Alp Pannonica Adriat · 2023 · Relevance 3/5
Revisión narrativa sobre estrategias antienvejecimiento. Menciona la rilmenidina como un mimético de la restricción calórica, que actúa como activador de AMPK e inhibidor de mTOR. Este mecanismo es una nueva área de investigación para el fármaco, más allá de su uso antihipertensivo.