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QuickView for Moexipril (compound)

Name: moexipril
PubChem Compound ID: 4474936
Molecular formula: C27H34N2O7
Molecular weight: 498.568 g/mol
Name: moexipril
Name (isomeric): DB00691
Drug Type: small molecule
Moexiprilum [INN-Latin]; Moexipril HCl; Moexipril hydrochloride
Brand: Univasc
Brand name mixture: Uniretic(moexipril + hydrochlorothiazide)
Category: Angiotensin-converting Enzyme Inhibitors, Antihypertensive Agents
CAS number: 103775-10-6
Indication: For the treatment of hypertension.
Pharmacology: Moexipril is a non-sulfhydryl containing precursor of the active angiotensin-converting enzyme (ACE) inhibitor moexiprilat. It is used to treat high blood pressure (hypertension). It works by relaxing blood vessels, causing them to widen. Lowering high blood pressure helps prevent strokes, heart attacks and kidney problems.
Mechanism of Action:
Moexipril 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....
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Absorption: Moexipril is incompletely absorbed, with bioavailability as moexiprilat of about 13% compared to intravenous (I.V.) moexipril (both measuring the metabolite moexiprilat), and is markedly affected by food, which reduces Cmax 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.
Protein binding: Moexiprilat is approxomately 50% protein bound.
Biotransformation: Rapidly converted to moexiprilat, the active metabolite. Conversion to the active metabolite is thought to require carboxyesterases and is likely to occur in organs or tissues, other than the gastrointestinal tract, in which carboxyesterases occur. The liver is thought to be one site of conversion, but not the primary site.
Route of elimination: Moexiprilat undergoes renal elimination.
Half Life: Moexipril elimination half-life is approximately 1 hour. Moexiprilat elimination half-life is 2 to 9 hours.
Clearance: 441 mL/min
Toxicity: Human overdoses of moexipril have not been reported. In case reports of overdoses with other ACE inhibitors, hypotension has been the principal adverse effect noted. Single oral doses of 2 g/kg moexipril were associated with significant lethality in mice. Rats, however, tolerated single oral doses of up to 3 g/kg. Common adverse effects include cough, dizziness, diarrhea, flu syndrome, fatigue, pharyngitis, flushing, rash, and myalgia
Affected organisms: Humans and other mammals
Food interaction:
High salt intake may attenuate the antihypertensive effect of moexipril.
Moexipril may decrease the excretion of potassium. Salt substitutes containing potassium may increase the risk of hyperkalemia.
Herbs that may attenuate the antihypertensive effect of moexipril include: bayberry, blue cohash, cayenne, ephedra, ginger, ginseng (American), kola and licorice.
Take moexipril one hour before or two hours after meals.
Drug interaction:
LithiumThe ACE inhibitor increases serum levels of lithium
TizanidineTizanidine increases the risk of hypotension with the ACE inhibitor
PotassiumIncreased risk of hyperkalemia
TreprostinilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
QuinupristinThis combination presents an increased risk of toxicity
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