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rilmenidine
Indications:
- treatment of hypertension
Contraindications:
- severe depression
- chronic renal failure stage 5 (eGFR < 15 mL/min) [3]
- avoid in pregnant women & in lactation*
* no teratogenic or embryotoxic effects have been observed in animal studies
* rilmenidine is excreted in breast milk
Dosage: 1-2 mg QD in morning
tablets: 1 mg
- do not discontinue abruptly, reduce dosage gradually
Dosage adjustment in renal failure:
- none if eGFR > 15 mL/min
Adverse effects:
- rare, non-severe, & transient at therapeutic doses:
- asthenia, palpitations, insomnia, drowsiness, fatigue on exercise, epigastric pain, dry mouth, diarrhea, skin rash
- cold extremities, postural hypotension, sexual disorders, anxiety, depression, pruritus, edema, cramps, nausea, constipation, hot flushes
- 2 mg dose of rilmenidine with fewer & less severe adverse effects vs clonidine (0.15-0.30 mg/day) or alpha-methyldopa (500-1000 mg/day)
* overdose:
- no cases of massive overdose reported
- hypotension & drowsiness anticipated
- gastric lavage recommended
- sympathomimetics may be required
- rilmenidine is only slightly dialysable
Drug interactions:
- combination with MAOIs is not recommended
- caution when used in combination with tricyclic antidepressants
- avoid in combination with alcohol
Mechanism of action:
- nischarin agonist
- activation of nischarin by rilmenidine increases phosphorylation of mitogen-activated protein kinases MAPK1 & MAPK3 in rostral ventrolateral medulla neurons that exhibit rilmenidine-evoked hypotension
- also effects peripheral vasomotor structures
- greater selectivity for imidazoline receptors than for cerebral alpha2-adrenergic receptors
- anti-inflammatory properties
Comparative biology:
- rilmenidine extends lifespan of C elegans
- rilmenidine-induced longevity requires transcription factors FOXO/DAF-16 & NRF1,2,3/SKN-1
- autophagy signaling is also needed for rilmenidine-induced longevity
- AMPK signaling plays no significant role in longevity
Interactions
drug adverse effects of antihypertensive agents
General
antihypertensive agent
Database Correlations
PUBCHEM cid=68712
References
- Reid JL.
Rilmenidine: a clinical overview.
Am J Hypertens. 2000 Jun;13(6 Pt 2):106S-111S.
PMID: 10921529 Review.
- Reid JL.
Update on rilmenidine: clinical benefits.
Am J Hypertens. 2001 Nov;14(11 Pt 2):322S-324S.
PMID: 11721891 Review.
- Bennett DF, Goyala A, Statzer C et al
Rilmenidine extends lifespan and healthspan in Caenorhabditis elegans
via a nischarin I1-imidazoline receptor.
Aging Cell. 2023 Feb;22(2):e13774.
PMID: 36670049 PMCID: PMC9924948 Free PMC article
- Wikipedia: Rilmenidine
https://en.wikipedia.org/wiki/Rilmenidine