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Pronunciation |
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(mo
EKS i
pril) |
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U.S. Brand
Names |
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Univasc® |
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Generic
Available |
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No |
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Synonyms |
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Moexipril Hydrochloride |
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Pharmacological Index |
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Angiotensin-Converting Enzyme (ACE) Inhibitors |
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Use |
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Treatment of hypertension, alone or in combination with thiazide diuretics;
treatment of left ventricular dysfunction after myocardial
infarction |
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Pregnancy Risk
Factor |
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C/D (2nd and 3rd trimesters) |
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Contraindications |
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Hypersensitivity to moexipril, moexiprilat, or any component;
hypersensitivity or allergic reactions or angioedema related to previous
treatment with an ACE inhibitor; pregnancy (2nd or 3rd
trimester) |
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Warnings/Precautions |
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Anaphylactic reactions can occur. Angioedema can occur at any time during
treatment (especially following first dose). Careful blood pressure monitoring
with first dose (hypotension can occur especially in volume depleted patients).
Dosage adjustment needed in renal impairment. Use with caution in hypovolemia;
collagen vascular diseases; valvular stenosis (particularly aortic stenosis);
hyperkalemia; or before, during, or immediately after anesthesia. Avoid rapid
dosage escalation which may lead to renal insufficiency.
Neutropenia/agranulocytosis with myeloid hyperplasia can rarely occur. If
patient has renal impairment then a baseline WBC with differential and serum
creatinine should be evaluated and monitored closely during the first 3 months
of therapy. Hypersensitivity reactions may be seen during hemodialysis with
high-flux dialysis membranes (eg, AN69). Deterioration in renal function can
occur with initiation. Use with caution in unilateral renal artery stenosis and
pre-existing renal insufficiency. |
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Adverse
Reactions |
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1% to 10%:
Cardiovascular: Hypotension, peripheral edema
Central nervous system: Headache, dizziness, fatigue
Dermatologic: Rash, alopecia, flushing, rash
Endocrine & metabolic: Hyperkalemia
Gastrointestinal: Diarrhea, nausea, heartburn
Genitourinary: Polyuria
Neuromuscular & skeletal: Myalgia
Renal: Reversible increases in creatinine or BUN
Respiratory: Cough, pharyngitis, upper respiratory infection, sinusitis
<1% (Limited to important or life-threatening symptoms): Chest pain,
myocardial infarction, palpitations, arrhythmias, syncope, cerebrovascular
accident, orthostatic hypotension, hypercholesterolemia, anemia, elevated LFTs,
hepatitis, oliguria, proteinuria, bronchospasm, dyspnea, eosinophilic
pneumonitis |
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Overdosage/Toxicology |
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Mild hypotension has been the only toxic effect seen with acute overdose;
bradycardia may also occur; hyperkalemia occurs even with therapeutic doses,
especially in patients with renal insufficiency and those taking NSAIDs
Following initiation of essential overdose management, toxic symptom
treatment and supportive treatment should be initiated; hypotension usually
responds to I.V. fluids or Trendelenburg positioning. |
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Drug
Interactions |
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Allopurinol: Potential for allergic reactions increased with moexipril.
Alpha1 blockers: Hypotensive effect increased.
Aspirin and NSAIDs may decrease ACE inhibitor efficacy and/or increase
potential to alter renal function.
Diuretics: Hypovolemia due to diuretics may precipitate acute hypotensive
events or acute renal failure.
Insulin: Risk of hypoglycemia may be increased.
Lithium: Risk of lithium toxicity may be increased; monitor lithium levels,
especially the first 4 weeks of therapy.
Mercaptopurine: Risk of neutropenia may be increased.
Potassium-sparing diuretics (amiloride, potassium, spironolactone,
triamterene): Increased risk of hyperkalemia.
Potassium supplements may increase the risk of hyperkalemia.
Probenecid: Blood levels of moexipril are increased (may occur with other ACE
inhibitors).
Trimethoprim (high dose) may increase the risk of hyperkalemia.
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Mechanism of
Action |
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Competitive inhibitor of angiotensin-converting enzyme (ACE); prevents
conversion of angiotensin I to angiotensin II, a potent vasoconstrictor; results
in lower levels of angiotensin II which causes an increase in plasma renin
activity and a reduction in aldosterone secretion |
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Pharmacodynamics/Kinetics |
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Peak concentrations: 1-2 hours
Duration: >24 hours
Absorption: Food decreases bioavailability (AUC decreased by ~40%)
Distribution: Vd (moexiprilat): 180 L
Protein binding (plasma): Moexipril: 90%; Moexiprilat: 50% to 70%
Metabolism: Parent drug is metabolized in liver and small intestine to
moexiprilat, the 1000 times more potent diacid metabolite; both parent
Bioavailability (moexiprilat): 13%
Half-life: Moexipril: 1 hour; Moexiprilat: 2-10 hours
Time to peak: 1.5 hours
Elimination: 50% appears in the feces |
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Usual Dosage |
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Adults: Oral: Initial: 7.5 mg once daily (in patients not receiving
diuretics), 1 hour prior to a meal or 3.75 mg once daily (when combined
with thiazide diuretics); maintenance dose: 7.5-30 mg/day in 1 or 2 divided
doses 1 hour before meals |
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Dietary
Considerations |
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Administer on an empty stomach |
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Monitoring
Parameters |
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Blood pressure, heart rate, electrolytes, CBC, symptoms of
hypotension |
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Test
Interactions |
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Increases BUN, creatinine, potassium, positive Coombs' [direct]; decreases
cholesterol (S); may cause false-positive results in urine acetone
determinations using sodium nitroprusside reagent |
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Cardiovascular
Considerations |
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ACE inhibitors decrease morbidity and mortality in patients with asymptomatic
and symptomatic left ventricular dysfunction. In this situation, they decrease
hospitalizations for, and retard progression to, congestive heart failure. ACE
inhibitors are also indicated in patients postmyocardial infarction in whom left
ventricular ejection fraction is <40%. When used in patients with heart
failure, the target dose should be achieved, if possible. Lower daily doses of
ACE inhibitors have not demonstrated the same cardioprotective effects.
Moexipril has not been as extensively studied in this setting as other ACE
inhibitors and therefore should be titrated to the maximum or maximum tolerated
dose. ACE inhibitors have renal protective effects in patients with proteinuria
and possibly cardioprotective effects in high-risk patients.
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Mental Health: Effects
on Mental Status |
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May cause drowsiness or dizziness; may rarely cause anxiety or mood
changes |
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Mental Health:
Effects on Psychiatric
Treatment |
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May cause neutropenia; use caution with clozapine and carbamazepine; may
decrease lithium clearance resulting in an increase in serum lithium levels and
potential lithium toxicity; monitor serum lithium levels |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Take exactly as directed; do not discontinue without consulting prescriber.
Take first dose at bedtime. This drug does not eliminate need for diet or
exercise regimen as recommended by prescriber. Do not take potassium supplements
or salt substitutes containing potassium without consulting prescriber. May
cause dizziness, fainting, lightheadedness (use caution when driving or engaging
in tasks that require alertness until response to drug is known); postural
hypotension (use caution when rising from lying or sitting position or climbing
stairs); nausea, vomiting, abdominal pain, dry mouth, or transient loss of
appetite (small frequent meals, frequent mouth care, sucking lozenges, or
chewing gum may help) - report if these persist. Report chest pain or
palpitations; difficulty in breathing or unusual cough; or other persistent
adverse reactions. Pregnancy/breast-feeding precautions: Do not get
pregnant while taking this medication; use appropriate barrier contraceptive
measures. If you are, or plan to be pregnant, notify your prescriber at once.
Consult prescriber if breast-feeding. |
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Nursing
Implications |
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Observe for symptoms of severe hypotension, especially within the first 2
hours following the initial dose or subsequent increases in dose as well as for
signs of hyperkalemia or cough; administer on an empty
stomach |
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Dosage Forms |
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Tablet, as hydrochloride: 7.5 mg, 15 mg |
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References |
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Konstam MA, Drakup K, Baker DW, et al,
"Heart Failure: Evaluation and Care of Patients With Left Ventricular Systolic Dysfunction,"
Clinical Practice Guideline No 11, Rockville, MD: Agency for Health Care
Policy and Research, Public Health Service, U.S. Department of Health and Human
Services, 1994.
Lewis EJ, Hunsicker LG, Bain RP, et al,
"The Effect of Angiotensin-Converting Enzyme Inhibition on Diabetic Nephropathy,"
N Engl J Med, 1993, 329(20):1456-62.
McAreavey D and Robertson JIS,
"Angiotensin Converting Enzyme Inhibitors and Moderate Hypertension,"
Drugs, 1990, 40(3):326-45.
Williams JF, Bristow MR, Fowler MB, et al,
"Guidelines for the Evaluation and Management of Heart Failure: Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee on Evaluation and Management of Heart Failure),"
J Am Coll Cardiol, 1995, 26:1376-8.
Woo OF, "Captopril and Related Drugs," Poisoning and Drug Overdose,
2nd ed, Olson KR, ed, East Norwalk, CT: Appleton and Lange, 1994, 117-8.
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