Pharmacokinetics of rilmenidine in patients with chronic renal insufficiency and in hemodialysis patients

Aparicio, M; Dratwa, Max; Esper, N. El; Fillastre, J P; Levaltier, B.; Lins, Robert; Meyrier, Alain; Mignon, F; Ryckelynck, J. P.; Sennesael, J.

doi:10.1016/0002-9149(94)90041-8

Cited by 17 publications

(17 citation statements)

References 17 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The concentrations at time near to c max were 3.51 and 3.59 ng/ml in patients using 1 mg per day while ranging between 6.70 and 7.20 ng/ml in patients using 1 mg of rilmenidine twice daily. These values correspond to previously reported c max levels in healthy volunteers [6,7,9] and also demonstrate a linear, dosedependent increase of drug concentration in the serum. The drug wileyonlinelibrary.com/journal/jms concentrations of the two patients at 12 h post-dose were 0.33 and 0.39 ng/ml, respectively.…”

Section: Application Of the Methodssupporting

confidence: 91%

“…The calibration range was defined considering the normal therapeutic concentrations obtained from previously published works. [5,6,9] The working range was extended in comparison to the methods applied in studies with healthy volunteers since overdosed patients are likely to be monitored in real clinical settings.…”

Section: Linearitymentioning

confidence: 99%

“…Absorption of rilmenidine (1 mg) in healthy volunteers is rapid, with t max ranging between 1.33 and 1.94 h [6 -9] and maximal plasma concentration (c max ) between 3.25 and 3.97 ng/ml. [6,7,9] To meet the requirements for preclinical, biopharmaceutical and clinical pharmacology studies, a rapid, selective, sensitive and robust analytical method is highly desirable. Very few analytical procedures, applied mainly to pharmacokinetic studies, have been reported for the determination of rilmenidine, which include gas chromatography-mass spectrometry (GC-MS) [10 -14] and liquid chromatography-tandem mass spectrometry (LC-MS/MS).…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Development of a fast LC–MS/MS method for quantification of rilmenidine in human serum: elucidation of fragmentation pathways by HRMS

et al. 2010

View full text Add to dashboard Cite

Rilmenidine is an alpha 2 adrenoreceptor agonist used in the treatment of mild and moderate hypertension. In this study, a fast and accurate liquid chromatographic method with tandem mass spectrometric detection has been validated in order to assure quantification of rilmenidine in human serum. The fragmentation pathway of protonated rilmenidine was studied using high-resolution mass spectrometry (HRMS). This study compared selectivity, linearity, accuracy, precision, extraction efficiency, matrix effect and sensitivity using common liquid-liquid extraction (LLE) and solid-phase extraction (SPE) procedures. The limit of quantitation for both extraction techniques was 0.1 ng/ml. Several differences between the LLE and SPE have been observed in terms of linearity, accuracy, precision and matrix effect. Additionally, the advantages of SPE included less manual work load and increased recovery of rilmenidine in human serum to approximately 80% (LLE, 57%). The developed method involving SPE was found to be accurate (relative error (RE) < 5%), reproducible (relative standard deviation, RSD < 7%), robust and suitable for quantitative analysis of rilmenidine in serum samples obtained from patients under antihypertensive treatment.

show abstract

Section: Application Of the Methodssupporting

confidence: 91%

Section: Linearitymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Development of a fast LC–MS/MS method for quantification of rilmenidine in human serum: elucidation of fragmentation pathways by HRMS

et al. 2010

View full text Add to dashboard Cite

show abstract

“…This aspect may be of relevance for the sympathicolytic treatment of hemodialysis patients prone to intradialytic hypotension. Low-dose use of moxonidine and rilmenidine [23] in patients with CKD is safe. Both moxonidine and rilmenidine are not available in the USA.…”

Section: How To Fight Sympathetic Hyperactivity In Ckd?mentioning

confidence: 99%

Cause and Consequences of Sympathetic Hyperactivity in Chronic Kidney Disease

Kotanko¹

2005

Blood Purif

View full text Add to dashboard Cite

Patients with chronic kidney disease and patients undergoing hemodialysis treatment show a sustained overactivity of the sympathetic nervous system, which originates from signals arising in the failing kidneys and traveling via afferent renal nerves to cardiovascular centers in the brainstem. Additional important factors are increased levels of angiotensin II and asymmetrical dimethylarginine. The sympathetic overactivity contributes to hypertension and cardiovascular morbidity and mortality in that patient population. Sympathetic overactivity can be reduced by adrenergic receptor blockers, centrally acting sympathicolytic drugs such as moxonidine and rilmenidine, angiotensin-converting enzyme inhibition, and angiotensin II type 1 receptor antagonists. Daily short hemodialysis and long nocturnal hemodialysis may reduce the elevated sympathetic activity, possibly because of an increased clearance of asymmetrical dimethylarginine, an endogenous nitric oxide synthase inhibitor. Prospective trials examining the potential impact of both β-blockers and centrally acting sympatholytic drugs on cardiovascular mortality in chronic kid ney disease and hemodialysis patients are very much needed.

show abstract

“…The pharmacokinetic characteristics of rilmenidine have been studied in some detail 23,24 . Rilmenidine is an oxazoline derivative and it is chemically related to imidazolines 25 .…”

Section: Introductionmentioning

confidence: 99%

Value of rilmenidine therapy and its combination with perindopril on blood pressure and left ventricular hypertrophy in patients with essential hypertension (VERITAS)

Farsang

Lengyel

Borbás

et al. 2003

Current Medical Research and Opinion

View full text Add to dashboard Cite

show abstract

Pharmacokinetics of rilmenidine in patients with chronic renal insufficiency and in hemodialysis patients

Cited by 17 publications

References 17 publications

Development of a fast LC–MS/MS method for quantification of rilmenidine in human serum: elucidation of fragmentation pathways by HRMS

Development of a fast LC–MS/MS method for quantification of rilmenidine in human serum: elucidation of fragmentation pathways by HRMS

Cause and Consequences of Sympathetic Hyperactivity in Chronic Kidney Disease

Value of rilmenidine therapy and its combination with perindopril on blood pressure and left ventricular hypertrophy in patients with essential hypertension (VERITAS)

Contact Info

Product

Resources

About