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Brand names,
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Analogs
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Brand Names Mixture
- Lotensin HCT (Benazepril Hydrochloride + Hydrochlorothiazide)
- Lotrel (Benazepril Hydrochloride + Amlodipine Besylate)
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Chemical_Formula
C24H28N2O5
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RX_link
http://www.rxlist.com/cgi/generic/benaz.htm
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fda sheet
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msds (material safety sheet)
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Synthesis Reference
U.S.pat.4,410,520(1983)
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Molecular Weight
424.49 g/mol
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Melting Point
148-149 oC
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H2O Solubility
2.229 mg/L
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State
Solid
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LogP
3.217
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Dosage Forms
Tablet (5 mg, 10 mg, 20 mg, 40 mg)
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Indication
For the treatment of hypertension. It may be used alone or in combination with thiazide diuretics.
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Pharmacology
Benazepril, an angiotensin-converting enzyme (ACE) inhibitor, is a prodrug which, when hydrolyzed by estarases to its active Benazeprilat, is used to treat hypertension and heart failure, to reduce proteinuria and renal disease in patients with nephropathies, and to prevent stroke, myocardial infarction, and cardiac death in high-risk patients. Benazepril and Benazeprilat inhibit angiotensin-converting enzyme (ACE) in human subjects and animals. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II. Angiotensin II also stimulates aldosterone secretion by the adrenal cortex.
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Absorption
Peak in plasma within 0.5-1.0 hours. The extent of absorption is at least 37% as determined by urinary recovery and is not significantly influenced by the presence of food in the GI tract.
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side effects and Toxicity
Symptoms of overdose include swelling of face, mouth, hands, or feet, trouble in swallowing or breathing (sudden), hoarseness, fever and chills.
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Patient Information
Pregnancy
Female patients of childbearing age should be told about the consequences of second- and
third-trimester exposure to ACE inhibitors, and they should also be told that these consequences do not appear to
have resulted from intrauterine ACE inhibitor exposure that has been limited to the first trimester. These patients
should be asked to report pregnancies to their physicians as soon as possible.
Angioedema
Angioedema, including laryngeal edema, can occur at any time with treatment with ACE inhibitors.
Patients should be so advised and told to report immediately any signs or symptoms suggesting angioedema (swelling of
face, eyes, lips, or tongue, or difficulty in breathing) and to take no more drug until they have consulted with the
prescribing physician.
Symptomatic Hypotension
Patients should be cautioned that lightheadedness can occur, especially during the first days of
therapy, and it should be reported to the prescribing physician. Patients should be told that if syncope occurs,
Lotensin should be discontinued until the prescribing physician has been consulted.
All patients should be cautioned that inadequate fluid intake or excessive perspiration, diarrhea, or
vomiting can lead to an excessive fall in blood pressure, with the same consequences of lightheadedness and possible
syncope.
Hyperkalemia
Patients should be told not to use potassium supplements or salt substitutes containing potassium
without consulting the prescribing physician.
Neutropenia
Patients should be told to promptly report any indication of infection (e.g., sore throat, fever),
which could be a sign of neutropenia.
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Organisms Affected
Humans and other mammals