Moexipril (moexipril HCl)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Moexipril hydrochloride is a non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor.
Moexipril hydrochloride is an angiotensin-converting enzyme (ACE, bradykininase, kininase II) inhibitor. Unlike captopril or lisinopril but similar to benazepril, enalapril, fosinopril, perindopril, quinapril, ramipril, and trandolapril, moexipril is a prodrug and has little pharmacologic activity until hydrolyzed in the liver to moexiprilat. Like benazepril, enalapril, fosinopril, lisinopril, perindopril, quinapril, ramipril, and trandolapril, but unlike captopril, moexipril does not contain a sulfhydryl group.
Moexipril hydrochloride is a prodrug for moexiprilat, which inhibits ACE in humans and animals. The mechanism through which moexiprilat lowers blood pressure is believed to be primarily through inhibition of ACE activity. ACE is a peptidyl dipeptidase that catalyzes the conversion of the inactive decapeptide angiotensin I to the vasoconstrictor substance angiotensin II.
Angiotensin II is a potent peripheral vasoconstrictor that also stimulates aldosterone secretion by the adrenal cortex and provides negative feedback on renin secretion. ACE is identical to kininase II, an enzyme that degrades bradykinin, an endothelium-dependent vasodilator. Moexiprilat is about 1000 times as potent as moexipril in inhibiting ACE and kininase II.
Inhibition of ACE results in decreased angiotensin II formation, leading to decreased vasoconstriction, increased plasma renin activity, and decreased aldosterone secretion. The latter results in diuresis and natriuresis and a small increase in serum potassium concentration (mean increases of about 0.25 mEq/L were seen when moexipril was used alone).
Although the principal mechanism of moexipril in blood pressure reduction is believed to be through the renin angiotensin-aldosterone system, ACE inhibitors have some effect on blood pressure even in apparent low-renin hypertension. As is the case with other ACE inhibitors, however, the antihypertensive effect of moexipril is considerably smaller in Black patients, a predominantly low-renin population, than in non-Black hypertensive patients.
Moexipril's antihypertensive activity is almost entirely due to its deesterified metabolite, moexiprilat. Bioavailability of oral moexipril is about 13% compared to IV moexipril (both measuring the metabolite moexiprilat), and is markedly affected by food, which reduces the peak plasma level and AUC. Moexipril should therefore be taken in a fasting state.
The time-to-peak plasma concentration of moexiprilat is about 1.5 hours. Like all ACE inhibitors, moexiprilat has a prolonged terminal elimination phase with a functional elimination half-life of about 12 hours. Over the dose range of 7.5 to 30 mg, pharmacokinetics are approximately dose proportional.
Moexiprilat is about 50% protein bound. After oral administration, only about 7% of the dose appears in urine as moexiprilat, about 1% as moexipril, with about 5% as other metabolites. Fifty-two percent of the dose is recovered in feces as moexiprilat and 1% as moexipril.
Single and multiple doses of 15 mg or more of moexipril hydrochloride give sustained inhibition of plasma ACE activity of 80 to 90%, beginning within 2 hours and lasting 24 hours (80%). During chronic therapy, the antihypertensive effect of any dose of moexipril hydrochloride is generally evident within 2 weeks of treatment, with maximal reduction after 4 weeks. The antihypertensive effects of moexipril hydrochloride have been proven to continue during therapy for up to 24 months.
USES: This medication is used to treat high blood pressure. Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Moexipril belongs to a class of drugs known as ACE inhibitors.
It works by relaxing blood vessels so blood can flow more easily.
Generic name: moexipril HCl
Pronunciation: (moe-EX-i-pril)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Moexipril
Indications
The following indications are listed for Moexipril:
- Hypertension
Also known as: Elevated Blood Pressure, Essential Hypertension, Hyperpiesia, Hyperpiesis, Hypertensive Disorder, Systemic Arterial Hypertension.
Dosing
Dosage of moexipril hydrochloride is expressed in terms of the salt.
Dosage of moexipril must be adjusted according to patient tolerance and response. Generally, dosage adjustments should be made at intervals of at least 2 weeks and based on blood pressure measured towards the end of the dosing interval.
Moexipril hydrochloride is available as tablets administered orally once or twice daily. The antihypertensive effect may diminish toward the end of the dosing interval and can be addressed in some patients with twice daily dosing.
Because food decreases oral bioavailability (e.g., by 40-50%) and peak plasma concentrations (e.g., 70-80%), the manufacturer recommends that moexipril be taken in a fasting state (e.g., 1 hour before meals).
Store the tablets at 20-25degreesC with excursions permitted to 15-30degreesC. Protect from excessive moisture.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to moexipril.
*History of angioedema related to previous angiotensin-converting enzyme (ACE) inhibitor treatment.
*Concomitant therapy with aliskiren in patients with diabetes mellitus.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects considered at least possibly related to treatment and reported in >1% of patients receiving moexipril include increased cough, dizziness, diarrhea, flu syndrome, fatigue, pharyngitis, flushing, rash, and myalgia.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
The safety and efficacy of moexipril in pediatric patients have not been established.
If oliguria or hypotension occurs in neonates with a history of in utero exposure to moexipril, support blood pressure and renal function; exchange transfusions or dialysis may be required.
Use of drugs that act on the renin-angiotensin system during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death. Resulting oligohydramnios can be associated with fetal lung hypoplasia and skeletal deformations. Potential neonatal adverse effects include skull hypoplasia, anuria, hypotension, renal failure, and death. Discontinue moexipril as soon as possible when pregnancy is detected.
Appropriate management of maternal hypertension during pregnancy is important to optimize outcomes for both mother and fetus. If use of moexipril is deemed necessary, apprise the mother of the risk to the fetus. Perform serial ultrasound examinations to assess the intraamniotic environment. If oligohydramnios is observed, discontinue moexipril unless it is considered lifesaving for the mother. Fetal testing may be appropriate, based on the week of pregnancy. However, oligohydramnios may not appear until after the fetus has sustained irreversible injury. Closely observe infants with histories of in utero exposure to moexipril for hypotension, oliguria, and hyperkalemia.
No teratogenic effects of moexipril were observed in animal studies.
It is not known whether moexipril is excreted in human milk. Exercise caution if administered to a nursing woman.
The manufacturer makes no specific dosage recommendations for geriatric patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Data from clinical studies evaluating moexipril in patients 65 years of age and older are insufficient to determine whether they respond differently than younger adults. Other reported clinical experience has not identified differences in responses between geriatric and younger patients. Because of the greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy in geriatric patients, initiate dosages of moexipril at the lower end of the usual dosage range in such patients.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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