Pharmacokinetic interactions of the oral renin inhibitor aliskiren with lovastatin, atenolol, celecoxib and cimetidine

Dieterle, W.; Corynen, S; Vaidyanathan, Sujata; Mann, James

doi:10.5414/cpp43527

Cited by 81 publications

(41 citation statements)

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“…However, no interaction of aliskiren with cytochrome P450 (P450) isoenzymes was found in human liver microsomes in vitro , suggesting a low potential for clinically significant drug interactions of aliskiren. Indeed, no clinically relevant pharmacokinetic interactions have been observed between aliskiren and the P450 substrates celecoxib, digoxin, lovastatin, or warfarin, or the P450 inhibitor cimetidine, in healthy volunteers (Dieterle et al, 2004(Dieterle et al, , 2005Dieterich et al, 2006). Animal studies indicate that aliskiren is a substrate for the efflux transporter Pglycoprotein, which may play a role in the hepatobiliary/intestinal excretion of the drug; however, the lack of pharmacokinetic interaction between aliskiren and the P-glycoprotein substrate digoxin indicates that aliskiren does not inhibit P-glycoprotein activity (Dieterich et al, 2006).…”

mentioning

confidence: 99%

Absorption, Distribution, Metabolism, and Elimination of the Direct Renin Inhibitor Aliskiren in Healthy Volunteers

Waldmeier

Glaenzel²,

Wirz³

et al. 2007

Drug Metab Dispos

121

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mentioning

confidence: 99%

Absorption, Distribution, Metabolism, and Elimination of the Direct Renin Inhibitor Aliskiren in Healthy Volunteers

Waldmeier

Glaenzel²,

Wirz³

et al. 2007

Drug Metab Dispos

121

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“…Aliskiren 150-600 mg Aliskiren 300 mg, lowered diastolic but not systolic blood pressure and aliskiren 600 mg was not effective in further reducing blood pressure than the 300-mg 652 Gradman et al [16] 2005 Aliskiren (37.5-300 mg) Dose-dependent reduction in systolic blood pressure 226 Stanton et al [11] 2003 Aliskiren 300 mg Aliskiren showed a similar pharmacokinetic and pharmacodynamic profile in patients with type 2 diabetes as compared with healthy volunteers 60 Zhao et al [62] 2006…”

Section: Modulation Of Endothelial Functionmentioning

confidence: 99%

“…Aliskiren 150 mg Aliskiren did not show pharmacokinetic interactions with lovastatin, atenolol or cimetidine 57 Dieterle et al [60] 2005…”

Section: Modulation Of Endothelial Functionmentioning

confidence: 99%

Aliskiren as a novel therapeutic agent for hypertension and cardio-renal diseases

Rashikh

Ahmad

Pillai

et al. 2011

Journal of Pharmacy and Pharmacology

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Objectives High blood pressure (BP) is a major risk factor for cardiovascular and renal complications. A majority of treated hypertensive patients still complain of high BP. The renin-angiotensin aldosterone system (RAAS) has been a centre-stage target for all the cardiovascular and cardio-renal complications. Aliskiren, is the first direct renin inhibitor (DRI) to be approved by the US FDA. Renin controls the ratelimiting step in the RAAS cascade and hence is the most favorable target for RAAS suppression. Key findings This review article strives to summarize the pharmacokinetic, preclinical and clinical studies done so far pertaining to the efficacy of aliskiren. Further, the pharmacology of aliskiren has been comprehensively dealt with to enhance understanding so as to further research in this unfathomed area in the multitude of cardiovascular disorders and renal diseases. Summary Aliskiren has been shown to have comparable BP-lowering effects to other RAAS inhibitors. Recent clinical trials have indicated that it might contribute significantly in combination with other agents for the protection of end-organ diseases.

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“…Aliskiren is not metabolized by cytochrome P450 thus it shows no clinically relevant interaction with other commonly used drugs such as ramipril, valsartan, hydrochlorothiazide (HCTZ), amlodipine, atenolol, lovastatin, warfarin, cimetidine, celecoxib. Age, gender, ethnicity, renal and hepatic impairment and diabetes do not affect aliskiren pharmacokinetics [Ayalasomayajula et al 2008;Dieterle et al 2005;Vaidyanathan et al 2006Vaidyanathan et al , 2007aVaidyanathan et al , 2007bVaidyanathan et al , 2007cVaidyanathan et al , 2008.…”

Section: Direct Renin Inhibitorsmentioning

confidence: 99%

Oral renin inhibitors in clinical practice: a perspective review

Bonanni

Vestra

2012

Therapeutic Advances in Chronic Disease

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Abstract:Hypertension is an important risk factor for cardiovascular morbidity and mortality. The importance of the renin-angiotensin-aldosterone system (RAAS) in cardiovascular and renal diseases has long been recognized: for this reason the conventional therapies, such as angiotensin-converting enzyme (ACE) inhibitors and angiotensin receptor blockers (ARBs), β-blockers, and aldosterone antagonists represent the backbone of current antihypertensive therapy. Aliskiren is the first direct renin inhibitor (DRI) suitable for oral administration. By achieving more complete renin-angiotensin system inhibition, direct renin inhibitors may afford greater protection from hypertensive complications. Present evidence indicates that aliskiren reduces baseline systolic and diastolic blood pressure greater than placebo and that it is as effective as other first-line antihypertensive agents. Extra advantages can be reached when it is used in combination therapy. Clinical trials and in vitro studies also suggest that aliskiren has several cardioprotective and renoprotective effects. Therapy with aliskiren is well tolerated, but recently some concerns have arisen because of the early termination of the ALTITUDE study due to an increased incidence of adverse effects.

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Pharmacokinetic interactions of the oral renin inhibitor aliskiren with lovastatin, atenolol, celecoxib and cimetidine

Cited by 81 publications

References 0 publications

Absorption, Distribution, Metabolism, and Elimination of the Direct Renin Inhibitor Aliskiren in Healthy Volunteers

Absorption, Distribution, Metabolism, and Elimination of the Direct Renin Inhibitor Aliskiren in Healthy Volunteers

Aliskiren as a novel therapeutic agent for hypertension and cardio-renal diseases

Oral renin inhibitors in clinical practice: a perspective review

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