UNIVASC
Clinical safety rating: caution
Comprehensive clinical and safety monograph for UNIVASC (UNIVASC).
Angiotensin-converting enzyme (ACE) inhibitor; inhibits conversion of angiotensin I to angiotensin II, reducing vasoconstriction and aldosterone secretion, leading to decreased blood pressure.
| Metabolism | Hepatic (hydrolysis to moexiprilat); moexiprilat is further glucuronidated. |
| Excretion | Univasc (moexipril) is primarily eliminated via renal excretion (approximately 50% of absorbed dose as unchanged drug and metabolites) and fecal excretion (about 50%). |
| Half-life | The terminal elimination half-life of moexiprilat, the active metabolite, is approximately 9.8 hours in patients with normal renal function. This supports once-daily dosing, though the antihypertensive effect may persist beyond 24 hours with continued therapy. |
| Protein binding | Moexiprilat is approximately 90% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | The apparent volume of distribution (Vd) is about 0.26 L/kg, indicating limited extravascular distribution and predominantly remaining in the vascular space. |
| Bioavailability | Oral bioavailability of moexipril is approximately 13% due to extensive first-pass metabolism to the active metabolite moexiprilat. Food does not significantly alter absorption, but administration with a high-fat meal may slightly reduce absorption. |
| Onset of Action | Oral administration: onset of antihypertensive effect occurs within 1-2 hours, with peak blood pressure reduction at 4-6 hours. |
| Duration of Action | Duration of antihypertensive effect is approximately 24 hours with once-daily dosing, allowing for sustained blood pressure control. Clinical trials show trough-to-peak ratios consistent with once-daily administration. |
| Molecular Weight | 498.6 |
Initial: 7.5 mg orally once daily; titrate to 15-30 mg once daily. Maximum: 60 mg/day.
| Dosage form | TABLET |
| Renal impairment | CrCl 20-40 mL/min: initial dose 3.75 mg once daily; maximum 15 mg/day. CrCl <20 mL/min: not recommended. |
| Liver impairment | Child-Pugh Class A and B: no adjustment required. Child-Pugh Class C: not studied; use with caution. |
| Pediatric use | Not recommended for pediatric patients. |
| Geriatric use | Initial dose 3.75 mg once daily; titrate cautiously. |
| 1st trimester | Avoid. ACE inhibitors are associated with teratogenicity including craniofacial and renal anomalies if exposed during the first trimester. Use only if no alternative and mother's condition requires treatment. |
| 2nd trimester | Contraindicated in second and third trimesters. Use is associated with oligohydramnios, fetal renal dysfunction, skull ossification defects, and neonatal hypotension. |
| 3rd trimester | Contraindicated. High risk of fetal renal dysplasia, oligohydramnios, and neonatal renal failure. |
Clinical note
Comprehensive clinical and safety monograph for UNIVASC (UNIVASC).
| Placental transfer | Univasc (moexipril) is expected to cross the placenta based on its molecular weight and similar ACE inhibitors; experimental data show placental transfer in animal studies. |
| Breastfeeding | Excreted into breast milk in low amounts; however, because of potential adverse effects on infant renal function and hypotension, caution is advised. Alternate antihypertensives with more safety data are preferred. |
■ FDA Black Box Warning
Fetal Toxicity: Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus. Discontinue as soon as possible when pregnancy is detected.
| Serious Effects |
History of angioedema related to previous ACE inhibitor therapyHereditary or idiopathic angioedemaPregnancy (second and third trimesters)Hypersensitivity to moexipril or any excipientConcomitant use with aliskiren in patients with diabetes mellitus
| Precautions | Angioedema (including intestinal angioedema), Hypotension (especially in volume-depleted patients), Neutropenia/agranulocytosis (higher risk with renal impairment or collagen vascular disease), Hepatic failure (rare), Renal impairment (monitor renal function), Hyperkalemia (risk factors include renal impairment, diabetes, potassium supplements) |
| Food/Dietary | Food significantly decreases absorption (about 40%) and conversion to active metabolite. Take at least 1 hour before meals. Avoid high-potassium foods (bananas, oranges, spinach) in large amounts if also taking potassium-sparing diuretics or supplements. |
Loading safety data…
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | UNIVASC (moexipril) is an ACE inhibitor. Exposure during the first trimester may be associated with a low absolute risk of congenital malformations, particularly cardiovascular and central nervous system defects. Exposure during the second and third trimesters is associated with a high risk of fetal renal dysfunction, oligohydramnios, skull ossification defects, and neonatal hypotension, acute renal failure, and death. Use is contraindicated in pregnancy. |
| Fetal Monitoring | Monitor maternal blood pressure, renal function (serum creatinine, BUN, urinalysis), electrolytes (especially potassium). Fetal monitoring: serial ultrasound for amniotic fluid volume and fetal growth if exposure after first trimester. Neonatal monitoring for hypotension and renal function if exposure near term. |
| Fertility Effects | No specific data on moexipril effects on human fertility. ACE inhibitors are not known to impair fertility. In animal studies, no adverse effects on fertility were observed. |
| Clinical Pearls | Univasc (moexipril) is an ACE inhibitor with a unique thiol group that may confer antioxidant properties. It is prodrug activated in liver; hepatic impairment reduces conversion. Monitor renal function and potassium. Cough incidence may be lower than some ACEIs due to tissue specificity. Avoid in pregnancy; use with caution in renal artery stenosis. |
| Patient Advice | Take once daily on an empty stomach 1 hour before meals to maximize absorption. · Avoid potassium supplements and salt substitutes containing potassium without consulting your doctor. · Report any signs of angioedema (swelling of face, lips, tongue) immediately. · May cause dizziness, especially at start of treatment; avoid driving until you know how it affects you. · Do not stop taking without medical advice, even if you feel well. |