Pharmacology and Clinical Use of the New ACE‐Inhibitor Moexipril

Stimpel, Michael; Bonn, R.; Koch, Brigitte; Dickstein, Kenneth

doi:10.1111/j.1527-3466.1995.tb00304.x

Cited by 19 publications

(15 citation statements)

References 39 publications

(23 reference statements)

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“…Compared to placebo, greater numbers of moexipril patients (51% vs 25%) had a response rate categorised as excellent. These results are similar to those obtained with moexipril in placebo controlled studies in other patient populations 18,21,22 and thereby indicate moexipril as effective in reducing BP in postmenopausal women who concomitantly receive HRT. The effects of HRT per se on BP were not assessed in the study, as HRT regimens were held constant throughout all of the experimental period.…”

Section: Discussionsupporting

confidence: 85%

“…Overall, moexipril was well tolerated among postmenopausal women using HRT, the adverse event rate was similar to previous moexipril studies [18][19][20][21][22] and no new safety risks were identified during the course of this study. Especially, no effect of moexipril on the typical postmenopausal symptoms could be observed.…”

Section: Discussionsupporting

confidence: 82%

“…Moreover, the current study showed that addition of moexipril did not affect any metabolic parameter. ACE inhibitors like moexipril in general are not associated with any metabolic abnormalities [22][23][24] and this study proved that this is also true in combination with HRT. Mean levels of triglycerides, total cholesterol, HDL, LDL, total cholesterol/HDL ratio and glucose remained relatively unchanged throughout the study which indicates that with regard to cardiovascular risk factors both drugs can safely be co-administered.…”

Section: Discussionsupporting

confidence: 63%

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Co-administration of an ACE-inhibitor (moexipril) and hormonal replacement therapy in postmenopausal women

1999

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Co-administration of antihypertensive drug therapy and hormonal replacement therapy (HRT) is frequent in postmenopausal women but it is not known whether HRT interacts with concomitant antihypertensive therapy. The present study was designed to investigate efficacy and safety of the ACE inhibitor moexipril in comparison to placebo in hypertensive, postmenopausal women on HRT.After a 4-week placebo run-in phase, 95 postmenopausal women (35-74 years of age) who had a sitting diastolic blood pressure (BP) of 95-114 mm Hg and were treated with HRT were randomised to a 12-week treatment with moexipril 15 mg or placebo. Efficacy and safety were assessed by measuring changes in sitting BP and metabolic parameters associated with cardiovascular disease including triglycerides, total cholesterol, HDL, LDL, total cholesterol/HDL ratio and glucose. Adverse events were recorded continuously.After 12 weeks of treatment, moexipril 15 mg was significantly more effective in reducing sitting systolic

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Section: Discussionsupporting

confidence: 85%

Section: Discussionsupporting

confidence: 82%

Section: Discussionsupporting

confidence: 63%

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Co-administration of an ACE-inhibitor (moexipril) and hormonal replacement therapy in postmenopausal women

1999

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“…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].…”

Section: Discussionmentioning

confidence: 93%

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

Charatcharoenwitthaya

Talwalkar

Angulo

et al. 2009

Dig Dis Sci

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Blockade of angiotensin II synthesis attenuates hepatic fibrosis in different experimental models of chronic liver injury. We evaluated the safety and efficacy of moexipril, an angiotensin-converting enzyme inhibitor, in patients with primary biliary cirrhosis (PBC) who have had a suboptimal response to ursodeoxycholic acid (UDCA). Twenty PBC patients on UDCA (13-15 mg/kg/day) therapy with an elevation of serum alkaline phosphatase at least twice the upper limit of normal were treated with oral moexipril 15 mg/day for one year. No significant changes in serum alkaline phosphatase (379 +/- 32 vs. 379 +/- 51), bilirubin (0.8 +/- 0.1 vs. 0.9 +/- 0.1), aspartate aminotransferase (60 +/- 8 vs. 63 +/- 9), and Mayo risk score (3.55 +/- 0.2 vs. 3.62 +/- 0.2) was associated with the treatment. Fatigue and health-related quality of life scores during treatment demonstrated a trend toward improvement. Moexipril was not clinically beneficial to PBC patients responding suboptimally to UDCA.

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“…It exerts its antihypertensive action via its active metabolite moexiprilat formed by the hydrolysis of moexipril in liver. It is incompletely absorbed and has a low bioavailability of about 23% [26].…”

Section: Prodrugs Of Ace Inhibitorsmentioning

confidence: 99%

Prodrug Strategies for Antihypertensives

Dhaneshwar¹,

Sharma²,

Patel³

et al. 2011

CTMC

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There is a great emphasis on research to discover methods aimed at enhancing the efficacy of drugs and reducing their toxicity and unwanted side effects. Prodrugs are biologically inactive compounds that are converted to actual drug molecule, through biotransformation, that combine with the receptors to produce the biological action. Prodrugs can thus be considered as drugs containing specialized nontoxic protective groups utilized in a transient manner to alter or eliminate the undesirable properties of the parent drug molecule. Hypertension is one of the leading risk factors for cardiovascular disease and represents a major health and economic burden. Most of the drugs for cardiovascular diseases have low oral bioavailability, short duration of action, first pass metabolism and variable lipohilicities. Out of the need to overcome these limitations, various prodrugs have been designed for antihypertensive agents. This review extensively focuses on various strategies used for design and development of prodrugs for the various classes of antihypertensives, emphasizing on the details regarding the need for prodrug synthesis for each class, structure, type of modification and goal achieved. It also provides an insight into the major advances in the field of antihypertensive prodrug research.

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Pharmacology and Clinical Use of the New ACE‐Inhibitor Moexipril

Cited by 19 publications

References 39 publications

Co-administration of an ACE-inhibitor (moexipril) and hormonal replacement therapy in postmenopausal women

Co-administration of an ACE-inhibitor (moexipril) and hormonal replacement therapy in postmenopausal women

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

Prodrug Strategies for Antihypertensives

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