Moexipril tablet
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Ahmed Zaghw, M.D. [2], Amr Marawan, M.D. [3]
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Black Box Warning
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USE IN PREGNANCY
See full prescribing information for complete Boxed Warning.
* When used in pregnancy during the second and third trimesters, ACE inhibitors can cause injury and even death to the developing fetus.
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Overview
Moexipril tablet is an Angiontensin converting enzyme inhibitor that is FDA approved for the {{{indicationType}}} of hypertension. There is a Black Box Warning for this drug as shown here. Common adverse reactions include diarrhea (3.1%), dizziness (4.3%), cough (6.1% ) and Influenza-like symptoms abnormal..
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
Hypertension
- Dosing Information
- Initial dose (not receiving a diuretic): Moexipril 7.5 mg PO qd should be used.
- Initial dose (with receiving a diuretic):
- Moexipril 7.5 mg PO qd and the diuretic should be discontinued 2 to 3 days prior to initiating moexipril.
- Moexipril 3.75 mg PO qd, if the diuretic cannot be discontinued.
- The diuretic may be resumed If blood pressure control is not attained with moexipril alone.
- Maintenance dose: Moexipril 7.5-30 mg PO qd on two divided doses, adjust dose based on response (MAX 60 mg/day)
Off-Label Use and Dosage (Adult)
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
There is limited information regarding Moexipril tablet FDA-Labeled Indications and Dosage (Pediatric) in the drug label.
Off-Label Use and Dosage (Pediatric)
Contraindications
Moexipril hydrochloride is contraindicated in patients who are hypersensitive to this product and in patients with a history of angioedema related to previous treatment with an ACE inhibitor.
Do not co-administer aliskiren with moexipril hydrochloride in patients with diabetes
Warnings
|
USE IN PREGNANCY
See full prescribing information for complete Boxed Warning.
* When used in pregnancy during the second and third trimesters, ACE inhibitors can cause injury and even death to the developing fetus.
|
There is limited information regarding Moexipril tablet Warnings' in the drug label.
Adverse Reactions
Clinical Trials Experience
Moexipril hydrochloride has been evaluated for safety in more than 2500 patients with hypertension; more than 250 of these patients were treated for approximately one year. The overall incidence of reported adverse events was only slightly greater in patients treated with moexipril hydrochloride than patients treated with placebo.
Reported adverse experiences were usually mild and transient, and there were no differences in adverse reaction rates related to gender, race, age, duration of therapy, or total daily dosage within the range of 3.75 mg to 60 mg. Discontinuation of therapy because of adverse experiences was required in 3.4% of patients treated with moexipril hydrochloride and in 1.8% of patients treated with placebo. The most common reasons for discontinuation in patients treated with moexipril hydrochloride were cough (0.7%) and dizziness (0.4%).
All adverse experiences considered at least possibly related to treatment that occurred at any dose in placebo-controlled trials of once-daily dosing in more than 1% of patients treated with moexipril hydrochloride alone and that were at least as frequent in the moexipril hydrochloride group as in the placebo group are shown in the following table:
Other adverse events occurring in more than 1% of patients on moexipril that were at least as frequent on placebo include: headache, upper respiratory infection, pain, rhinitis, dyspepsia, nausea, peripheral edema, sinusitis, chest pain, and urinary frequency. Angioedema, hypotension, neutropenia/agranulocytosis, second and third trimester fetal/neonatal morbidity and mortality, hyperkalemia, and cough.
Other potentially important adverse experiences reported in controlled or uncontrolled clinical trials in less than 1% of moexipril patients or that have been attributed to other ACE inhibitors include the following:
Cardiovascular
Symptomatic hypotension, postural hypotension, or syncope were seen in 9/1750 (0.51%) patients; these reactions led to discontinuation of therapy in controlled trials in 3/1254 (0.24%) patients who had received moexipril hydrochloride monotherapy and in 1/344 (0.3%) patients who had received moexipril hydrochloride with hydrochlorothiazide. Other adverse events included angina/myocardial infarction, palpitations, rhythm disturbances, and cerebrovascular accident.
Renal
Of hypertensive patients with no apparent preexisting renal disease, 1% of patients receiving moexipril hydrochloride alone and 2% of patients receiving moexipril hydrochloride with hydrochlorothiazide experienced increases in serum creatinine to at least 140% of their baseline values.
Gastrointestinal
Abdominal pain, constipation, vomiting, appetite/weight change, dry mouth, pancreatitis, hepatitis.
Respiratory
Bronchospasm, dyspnea, eosinophilic pneumonitis.
Urogenital
Renal insufficiency, oliguria.
Dermatologic
Apparent hypersensitivity reactions manifested by urticaria, rash, pemphigus, pruritus, photosensitivity, alopecia.
Neurological and Psychiatric
Drowsiness, sleep disturbances, nervousness, mood changes, anxiety.
Other
Angioedema , taste disturbances, tinnitus, sweating, malaise, arthralgia, hemolytic anemia.
Clinical Laboratory Test Findings
Serum Electrolytes
Creatinine and Blood Urea Nitrogen
As with other ACE inhibitors, minor increases in blood urea nitrogen or serum creatinine, reversible upon discontinuation of therapy, were observed in approximately 1% of patients with essential hypertension who were treated with moexipril hydrochloride. Increases are more likely to occur in patients receiving concomitant diuretics and in patients with compromised renal function.
Other
Clinically important changes in standard laboratory tests were rarely associated with moexipril hydrochloride administration.
Elevations of liver enzymes and uric acid have been reported. In trials, less than 1% of moexipril-treated patients discontinued moexipril hydrochloride treatment because of laboratory abnormalities. The incidence of abnormal laboratory values with moexipril was similar to that in the placebo-treated group.
Postmarketing Experience
There is limited information regarding Moexipril tablet Postmarketing Experience in the drug label.
Drug Interactions
Diuretics
Excessive reductions in blood pressure may occur in patients on diuretic therapy when ACE inhibitors are started. The possibility of hypotensive effects with moexipril hydrochloride can be minimized by discontinuing diuretic therapy for several days or cautiously increasing salt intake before initiation of treatment with moexipril hydrochloride. If this is not possible, the starting dose of moexipril should be reduced.
Potassium Supplements and Potassium-Sparing Diuretics
Moexipril hydrochloride can increase serum potassium because it decreases aldosterone secretion. Use of potassium-sparing diuretics (spironolactone, triamterene, amiloride) or potassium supplements concomitantly with ACE inhibitors can increase the risk of hyperkalemia. Therefore, if concomitant use of such agents is indicated, they should be given with caution and the patient's serum potassium should be monitored.
Oral Anticoagulants
Interaction studies with warfarin failed to identify any clinically important effect on the serum concentrations of the anticoagulant or on its anticoagulant effect.
Lithium
Increased serum lithium levels and symptoms of lithium toxicity have been reported in patients receiving ACE inhibitors during therapy with lithium. These drugs should be coadministered with caution, and frequent monitoring of serum lithium levels is recommended. If a diuretic is also used, the risk of lithium toxicity may be increased.
Gold
Nitritoid reactions (symptoms include facial flushing, nausea, vomiting and hypotension) have been reported rarely in patients on therapy with injectable gold (sodium aurothiomalate) and concomitant ACE inhibitor therapy including moexipril hydrochloride.
Non-Steroidal Anti-Inflammatory Agents including Selective Cyclooxygenase-2 Inhibitors (COX-2 Inhibitors)
In patients who are elderly, volume-depleted (including those on diuretic therapy), or with compromised renal function, co-administration of NSAIDS, including selective COX-2 inhibitors, with ACE inhibitors, including moexipril, may result in deterioration of renal function, including possible acute renal failure. These effects are usually reversible. Monitor renal function periodically in patients receiving moexipril and NSAID therapy.The antihypertensive effect of ACE inhibitors, including moexipril hydrochloride, may be attenuated by NSAIDS.
Dual Blockade of the Renin-Angiotensin System (RAS)
Dual blockade of the RAS with angiotensin receptor blockers, ACE inhibitors, or aliskiren is associated with increased risks of hypotension, hyperkalemia, and changes in renal function (including acute renal failure) compared to monotherapy. Closely monitor blood pressure, renal function and electrolytes in patients on moexipril hydrochloride and other agents that affect the RAS.
Do not co-administer aliskiren with moexipril in patients with diabetes. Avoid use of aliskiren with moexipril hydrochloride in patients with renal impairment (GFR <60 mL/min).
Other Agents
No clinically important pharmacokinetic interactions occurred when moexipril hydrochloride was administered concomitantly with hydrochlorothiazide, digoxin, or cimetidine.
Moexipril hydrochloride has been used in clinical trials concomitantly with calcium-channel-blocking agents, diuretics, H2 blockers, digoxin, oral hypoglycemic agents, and cholesterol-lowering agents. There was no evidence of clinically important adverse interactions.
Carcinogenesis, Mutagenesis, Impairment of Fertility
No evidence of carcinogenicity was detected in long-term studies in mice and rats at doses up to 14 or 27.3 times the Maximum Recommended Human Dose (MRHD) on a mg/m2 basis.
No mutagenicity was detected in the Ames test and microbial reverse mutation assay, with and without metabolic activation, or in an in vivo nucleus anomaly test. However, increased chromosomal aberration frequency in Chinese hamster ovary cells was detected under metabolic activation conditions at a 20-hour harvest time.
Reproduction studies have been performed in rabbits at oral doses up to 0.7 times the MRHD on a mg/m2 basis, and in rats up to 90.9 times the MRHD on a mg/m2 basis. No indication of impaired fertility, reproductive toxicity, or teratogenicity was observed.
Use in Specific Populations
Pregnancy
Pregnancy Category (FDA):
There is no FDA guidance on usage of Moexipril tablet in women who are pregnant.
Pregnancy Category (AUS):
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Moexipril tablet in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Moexipril tablet during labor and delivery.
Nursing Mothers
There is no FDA guidance on the use of Moexipril tablet in women who are nursing.
Pediatric Use
There is no FDA guidance on the use of Moexipril tablet in pediatric settings.
Geriatic Use
There is no FDA guidance on the use of Moexipril tablet in geriatric settings.
Gender
There is no FDA guidance on the use of Moexipril tablet with respect to specific gender populations.
Race
There is no FDA guidance on the use of Moexipril tablet with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Moexipril tablet in patients with renal impairment.
Hepatic Impairment
There is no FDA guidance on the use of Moexipril tablet in patients with hepatic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Moexipril tablet in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Moexipril tablet in patients who are immunocompromised.
Administration and Monitoring
Administration
There is limited information regarding Moexipril tablet Administration in the drug label.
Monitoring
There is limited information regarding Moexipril tablet Monitoring in the drug label.
IV Compatibility
There is limited information regarding the compatibility of Moexipril tablet and IV administrations.
Overdosage
There is limited information regarding Moexipril tablet overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.
Pharmacology
There is limited information regarding Moexipril tablet Pharmacology in the drug label.
Mechanism of Action
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 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).
Whether increased levels of bradykinin, a potent vasodepressor peptide, play a role in the therapeutic effects of moexipril remains to be elucidated. 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.
Structure
There is limited information regarding Moexipril tablet Structure in the drug label.
Pharmacodynamics
Single and multiple doses of 15 mg or more of moexipril hydrochloride gives sustained inhibition of plasma ACE activity of 80 to 90%, beginning within 2 hours and lasting 24 hours (80%).
Pharmacokinetics
Moexipril's antihypertensive activity is almost entirely due to its deesterified metabolite, moexiprilat. Bioavailability of oral moexipril is about 13% compared to intravenous (I.V.) moexipril (both measuring the metabolite moexiprilat), and is markedly affected by food, which reduces the peak plasma level (C max ) and AUC. Moexipril should therefore be taken in a fasting state. The time of peak plasma concentration (T max ) of moexiprilat is about 1 ½ hours and elimination half-life (t ½ ) is estimated at 2 to 9 hours in various studies, the variability reflecting a complex elimination pattern that is not simply exponential. Like all ACE inhibitors, moexiprilat has a prolonged terminal elimination phase, presumably reflecting slow release of drug bound to the ACE. Accumulation of moexiprilat with repeated dosing is minimal, about 30%, compatible with a functional elimination t ½ of about 12 hours. Over the dose range of 7.5 to 30 mg, pharmacokinetics are approximately dose proportional.
Absorption
Moexipril is incompletely absorbed, with bioavailability as moexiprilat of about 13%. Bioavailability varies with formulation and food intake which reduces C max and AUC by about 70% and 40% respectively after the ingestion of a low-fat breakfast or by 80% and 50% respectively after the ingestion of a high-fat breakfast.
Distribution
The clearance (CL) for moexipril is 441 mL/min and for moexiprilat 232 mL/min with a t ½ of 1.3 and 9.8 hours, respectively. Moexiprilat is about 50% protein bound. The volume of distribution of moexiprilat is about 183 liters.
Metabolism and Excretion
Moexipril is relatively rapidly converted to its active metabolite moexiprilat, but persists longer than some other ACE inhibitor prodrugs, such that its t ½ is over one hour and it has a significant AUC. Both moexipril and moexiprilat are converted to diketopiperazine derivatives and unidentified metabolites. After I.V. administration of moexipril, about 40% of the dose appears in urine as moexiprilat, about 26% as moexipril, with small amounts of the metabolites; about 20% of the I.V. dose appears in feces, principally as moexiprilat. 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.
Pharmacokinetic Interactions With Other Drugs
No clinically important pharmacokinetic interactions occurred when moexipril hydrochloride was administered concomitantly with hydrochlorothiazide, digoxin, or cimetidine.
Nonclinical Toxicology
There is limited information regarding Moexipril tablet Nonclinical Toxicology in the drug label.
Clinical Studies
There is limited information regarding Moexipril tablet Clinical Studies in the drug label.
How Supplied
There is limited information regarding Moexipril tablet How Supplied in the drug label.
Storage
There is limited information regarding Moexipril tablet Storage in the drug label.
Images
Drug Images
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Package and Label Display Panel
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Patient Counseling Information
There is limited information regarding Moexipril tablet Patient Counseling Information in the drug label.
Precautions with Alcohol
Alcohol-Moexipril tablet interaction has not been established. Talk to your doctor regarding the effects of taking alcohol with this medication.
Brand Names
There is limited information regarding Moexipril tablet Brand Names in the drug label.
Look-Alike Drug Names
There is limited information regarding Moexipril tablet Look-Alike Drug Names in the drug label.
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.