Abstract

Rosuvastatin is an anti-hypercholesterolemic agent with good anti-inflammatory and antinociceptive responses. The objective of present study was to assess the pharmacological effects of interaction of rosuvastatin with coprescribed ACE inhibitors. For this purpose complexes of Rosuvastatin with enalapril, captopril and lisinopril were synthesized and characterized. Their spectroscopic analyses suggest that hydrogen bonded complexation occurs between rosuvastatin and selected ACE inhibitors at their carboxylic (COOH) and hydroxyl OH sites. The anti-nociceptive effect of complexes was assessed by formalin induced nociception in mice, antiinflammatory effect was evaluated by carrageenan induced paw edema in rats. Neuropharmacological behaviors were also studied on mice. All the complexes of Rosuvastatin showed analgesic behavior in rats and mice. Anti-inflammatory activity of complexes is found insignificant. Enalapril complex keeps sedative activity while complexes with captopril and lisinopril contain anti-depressant behaviors. Results suggest that the interaction of rosuvastatin with ACE inhibitors have consumed the active reacting sites of Rosuvastatin for which its anti-inflammatory, analgesic and gross locomotor behaviors have been affected. So it is suggested that Rosuvastatin should not be co-administered with any of these ACE inhibitors.

Highlights

  • Rosuvastatin being a potent HMG CoA reductase inhibitor in controlling biosynthesis of hepatic cholesterol is used for the treatment of coronary artery disease [1], heart attacks, hyperlipidemia, hypercholesterolemia and hypertriglyceridemia

  • Captopril and lisinopril belong to angiotensin-converting enzyme (ACE) inhibitors (Figure 1)

  • Spectroscopic studies of synthesized compounds IR studies: In the IR spectrum of Rosuvastatin, a broad region of band was seen between 3625-3200 cm-1 that was indication of OH group

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Summary

Introduction

Rosuvastatin being a potent HMG CoA reductase inhibitor in controlling biosynthesis of hepatic cholesterol is used for the treatment of coronary artery disease [1], heart attacks, hyperlipidemia, hypercholesterolemia and hypertriglyceridemia. Continuous dosage of statins causes myositis, rhabdomyolysis [2,3,4], atherosclerosis and liver transaminase elevation in patients with common symptoms of headache, gastrointestinal disorders, rash, diabetes, hypertension and nephrotic disease. Captopril and lisinopril belong to angiotensin-converting enzyme (ACE) inhibitors (Figure 1). They block the conversion of angiotensin I to angiotensin II in hypertension, collagen vascular and cardiovascular disease [5,6], cardiac arrhythmias, myocardial infarction [7] and reduce the activity of blood pressure regulating rennin-angiotensin-converting enzyme in Barter’s syndrome. Pharm Anal Acta 7: 488. doi:10.4172/2153-2435.1000488 that the impact of polypharmacy on the safety profile of statins should be considered deeply

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