Pharmacological and Clinical Profile of Moexipril: A Concise Review

Abstract

Angiotensin-converting enzyme (ACE) inhibitors are effective and safe antihypertensive drugs, with the exception of the rare occasion of angioedema. These drugs have demonstrated additional cardiovascular protective effects to their blood pressure lowering, and their combination with the diuretic hydrochlorothiazide potentiates their antihypertensive effectiveness. Moexipril is a long-acting ACE inhibitor suitable for once-daily administration, and like some ACE inhibitors, moexipril is a prodrug and needs to be hydrolyzed in the liver into its active carboxylic metabolite, moexiprilat, to become effective. Moexipril alone and in combination with low-dose hydrochlorothiazide has been shown in clinical trials to be effective in lowering blood pressure and be well tolerated and safe given in single daily doses. In this review, the pharmacological profile of this drug and its clinical usefulness are discussed.

Moexipril for Treatment of Primary Biliary Cirrhosis in Patients with an Incomplete Response to Ursodeoxycholic Acid

“…In patients with liver cirrhosis [44], single 15-mg doses of moexipril resulted in decreased maximum plasma concentration of its active diacid metabolite moexiprilat by about 50% but increased the area under the plasma-time concentration curve of moexiprilat by almost 30% compared with healthy volunteers. This might offer an explanation of the high incidence of adverse drug events in our patients compared with that reported previously in hypertensive patients [43]. However, the incidence of adverse events in our study was not statistically different between patients with more advanced liver disease as Dig Dis Sci (2010) 55:476-483 481 determined by their histologic stage (stage III-IV) compared with patients with early disease (stage I-II), and there is no clear evidence of dose-response relationships of the adverse drug reactions.…”

“…Although moexipril is quite safe and does not interfere with the action of other drugs, caution should be exercised when moexipril is prescribed in patients with chronic liver disease [43]. In patients with liver cirrhosis [44], single 15-mg doses of moexipril resulted in decreased maximum plasma concentration of its active diacid metabolite moexiprilat by about 50% but increased the area under the plasma-time concentration curve of moexiprilat by almost 30% compared with healthy volunteers.…”

Identification and Characterization of Forced Degradation Products of Moexipril Using LC-ESI-MS/Q-TOF

“…Finally we achieved a good resolution of peaks with acceptable shape with mobile phase consisting of 20 mM ammonium acetate buffer (A), pH adjusted to 6.0 using dilute formic acid and methanol (B) in a gradient elution program. The gradient program for mobile phase solvents was set as follows, (T min / %solution of B): 0-0 /30, 0-5 /65, [5][6][7][8][9][10][11][12][13][14][15] /65, 15-20 /30. The mobile phase flow rate of 1.0 ml/min, column temperature of 25°C and wavelength of 273 nm were found to be suitable for the chromatographic separation of MOX and its DPs.…”

“…Blockage of Angiotensin II limits hypertension within the vasculature. Additionally, MOX has been found to possess cardioprotective properties [4,5]. According to IUPAC, nomenclature of MOX is (3S)-2-[(2S)-2-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2yl]amino}propanoyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-3carboxylic acid (Figure 1).…”

A rapid and sensitive liquid chromatography–tandem mass spectrometric assay for moexipril, an angiotensin‐converting enzyme inhibitor in human plasma

“…Moexipril is a prodrug of moexiprilat, which inhibits ACE in humans and animals. In biological systems it is rapidly de‐esterified by esterases, resulting in its active metabolite moexiprilat (Brogden and Wiseman, ; Chrysant and Chrysant, ). Following oral administration, the moexipril attains peak plasma concentrations within 0.8 h. Over the dose range of 7.5–30 mg, the pharmacokinetics of moexipril is approximately dose‐proportional and is incompletely absorbed, with bioavailability as moexiprilat of about 13% (Grass and Morehead, ).…”