《MONOPRIL (fosinopril sodium tablets)》.pdf

Bristol-Myers Squibb Company Rx only MONOPRIL® (fosinopril sodium tablets) USE IN PREGNANCY When used in pregnancy during the second and third trimesters, ACE inhibitors can cause injury and even death to the developing fetus. When pregnancy is detected, MONOPRIL should be discontinued as soon as possible. See WARNINGS: Fetal/Neonatal Morbidity and Mortality. DESCRIPTION ® MONOPRIL (fosinopril sodium tablets) is the sodium salt of fosinopril, the ester prodrug of an angiotensin converting enzyme (ACE) inhibitor, fosinoprilat. It contains a phosphinate group capable of specific binding to the active site of angiotensin converting enzyme. Fosinopril sodium is designated chemically as: L-proline, 4-cyclohexyl-1-[[[2- methyl-1-(1-oxopropoxy) propoxy] (4-phenylbutyl) phosphinyl] acetyl]-, sodium salt, trans-. Fosinopril sodium is a white to off-white crystalline powder. It is soluble in water (100 mg/mL), methanol, and ethanol and slightly soluble in hexane. Its structural formula is: Its empirical formula is C30 H45NNaO7 P, and its molecular weight is 585.65. MONOPRIL is available for oral administration as 10 mg, 20 mg, and 40 mg tablets. Inactive ingredients include: lactose, microcrystalline cellulose, crospovidone, povidone, and sodium stearyl fumarate. CLINICAL PHARMACOLOGY Mechanism of Action In animals and humans, fosinopril sodium is hydrolyzed by esterases to the pharma- cologically active form, fosinoprilat, a specific competitive inhibitor of angiotensin converting enzyme (ACE). ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vaso- constrictor substance, angiotensin II. Angiotensin I