Rilmenidine
Rilmenidine.svg
Clinical data
Trade namesAlbarel
AHFS/Drugs.comInternational Drug Names
Routes of
administration
Oral
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Protein binding7%
MetabolismMinimal
Elimination half-life8 hours
ExcretionRenal, unchanged
Identifiers
  • N-(dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amine
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.053.638 Edit this at Wikidata
Chemical and physical data
FormulaC10H16N2O
Molar mass180.251 g·mol−1
3D model (JSmol)
  • N\1=C(\OCC/1)NC(C2CC2)C3CC3
  • InChI=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) checkY
  • Key:CQXADFVORZEARL-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Rilmenidine is a prescription medication for the treatment of hypertension.[1] It is marketed under the brand names Albarel, Hyperium, Iterium and Tenaxum.

Form and composition

Each tablet contains 1.544 mg rilmenidine dihydrogen phosphate, an amount equivalent to 1 mg of rilmenidine base.

Mode of action

Rilmenidine, an oxazoline compound with antihypertensive properties, acts on both medullary and peripheral vasomotor structures. Rilmenidine shows greater selectivity for imidazoline receptors than for cerebral alpha2-adrenergic receptors, distinguishing it from reference alpha2-agonists.

Indications

Hypertension.

Contraindications

Severe depression, severe kidney 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.[citation needed]

Precautions

Drug interactions

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

Side effects

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, 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.

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. Rilmenidine is only slightly dialysable.

See also


References

  1. ^ Remková A, Kratochvíl'ová H (August 2002). "Effect of the new centrally acting antihypertensive agent rilmenidine on endothelial and platelet function in essential hypertension". Journal of Human Hypertension. 16 (8): 549–55. doi:10.1038/sj.jhh.1001427. PMID 12149660.