Rilmenidine
Rilmenidine is a prescription medication for the treatment of hypertension. It is taken orally and marketed under the brand names Albarel, Hyperium, Iterium and Tenaxum.
Mechanism of action
Rilmenidine, an oxazoline compound with antihypertensive properties, acts on both medullary and peripheral vasomotor structures.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.
Contraindications
Severe depression, severe kidney failure, as a precaution in the absence of currently available studies.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 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.
Precautions
- As with all antihypertensive agents, regular medical monitoring is required when rilmenidine is administered to patients with a recent history of cardiovascular disease.
- Alcohol consumption should be avoided during treatment.
- In patients with kidney failure, no dosage adjustment is necessary if creatinine clearance is greater than 15 mL/min.
- In the absence of documented experiments in this area, rilmenidine is not recommended for prescription to children.
- 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.
- Lactation: rilmenidine is excreted in breast milk, and its use is therefore not recommended during lactation.
- 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. 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.
Drug interactions
Combination with MAOIs is not recommended; combination with tricyclic antidepressants requires prudence, as the antihypertensive activity of rilmenidine may be partly antagonized.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.
- At a dose of 2 mg per day of rilmenidine, controlled comparative studies versus clonidine or alpha-methyldopa demonstrated that the incidence of side effects was significantly lower with rilmenidine than with either clonidine or a-methyldopa.