|AHFS/Drugs.com||International Drug Names|
|Elimination half-life||8 hours|
|CompTox Dashboard (EPA)|
|Chemical and physical data|
|Molar mass||180.251 g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Rilmenidine is a prescription medication for the treatment of hypertension. It is marketed under the brand names Albarel, Hyperium, Iterium and Tenaxum.
Each tablet contains 1.544 mg rilmenidine dihydrogen phosphate, an amount equivalent to 1 mg of rilmenidine base.
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.
Severe depression, severe kidney failure (creatinine clearance <15 ml/min), as a precaution in the absence of currently available studies.
Therapy should never be interrupted suddenly; the dosage should be reduced gradually.
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 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.
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.
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.