Rilmenidine: a novel antihypertensive agent

Article Abstract:

A wide range of drugs is now available for the treatment of elevated blood pressure. It is no longer adequate for an antihypertensive drug to reduce blood pressure; it must preserve normal physiological functions as much as possible. Rilmenidine, the first oxazoline derivative developed for this purpose, has several pharmacologic properties which recommend it as a first-line treatment of mild and moderate hypertension. Previous studies, including a multicenter trial involving 126 mild-to-moderate hypertensive patients, demonstrated that rilmenidine is effective in reducing blood pressure. Furthermore, sedation, which is a common side effect of alpha-2-adrenoreceptor agonists (used in antihypertensive therapy), was no different from placebo effects in these studies. The antihypertensive effect of rilmenidine was long-lasting, and there was no effect on the strength of muscle contraction, as observed with some other drugs. No intolerance of rilmenidine was found in long-term studies, and rilmenidine was also well-tolerated by high risk patients, such as diabetics and the elderly. While rilmenidine has acquired impressive credentials in clinical studies, comparisons with other drugs such as beta-blockers, angiotensin-converting enzymes, and calcium antagonists need to be conducted to learn more about the precise influence of this new drug on the cardiovascular system. (Consumer Summary produced by Reliance Medical Information, Inc.)

Hypertension, Drug therapy

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Recent advances in the pharmacology of rilmenidine

Article Abstract:

Rilmenidine is an oxazoline derivative closely related to the imidazoline drugs, such as clonidine. In both short-term and long-term animal models, rilmenidine produces a dose-dependent reduction in heart rate and blood pressure. Injection of rilmenidine directly into the vertebral artery, which feeds the brainstem, reduces blood pressure at lower doses than does rilmenidine injected intravenously, suggesting that the drug works directly on the central nervous system. However, additional peripheral actions may also be at work. Rilmenidine reduces the outflow of noradrenaline from some peripheral organs, including the adrenal medulla. This may contribute to the blood-pressure-reducing effects of rilmenidine. Although it is clear that rilmenidine shares with clonidine specific receptors in the brainstem provisionally called imidazoline receptors, there are some significant differences between the drugs; the sedative effect of clonidine and its relatives is not observed with rilmenidine. (Consumer Summary produced by Reliance Medical Information, Inc.)

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Pharmacokinetics of rilmenidine

Article Abstract:

Rilmenidine is a new antihypertensive drug similar to, but not identical to, clonidine and alpha-2-adrenoreceptor agonists in its effects. The pharmacokinetics of absorption and metabolism of this drug were studied in 65 healthy volunteers. Although intravenous injection raised the blood level of rilmenidine more quickly than did an oral dose, the rate of the drug's disappearance from the blood was essentially the same regardless of the route of administration. Likewise, taking an oral dose with food delayed the appearance of the drug in the blood, but otherwise had little effect. Rilmenidine was not significantly metabolized by the body and appeared in the urine as an unchanged compound. Metabolites of rilmenidine did not appear. The elimination of rilmenidine from the body, which was essentially complete 36 hours after a 1 mg dose, was handled by the kidneys, which actively worked to excrete the drug rather than passively remove it by filtration. (Consumer Summary produced by Reliance Medical Information, Inc.)

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