QBRELIS
Clinical safety rating: caution
Comprehensive clinical and safety monograph for QBRELIS (QBRELIS).
Angiotensin II receptor blocker; selectively blocks the binding of angiotensin II to AT1 receptors in vascular smooth muscle and adrenal gland, leading to vasodilation and decreased aldosterone secretion.
| Metabolism | Hepatic via glucuronidation (UGT1A3, UGT2B7) and to a lesser extent via CYP2C9; forms inactive acyl glucuronide metabolites. |
| Excretion | Primarily renal (approximately 80%) with minimal biliary/fecal elimination (less than 5%). |
| Half-life | Terminal elimination half-life is approximately 10 hours (range 7-14 hours) in healthy adults; prolonged in renal impairment. |
| Protein binding | Approximately 30% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution (Vd) is approximately 20 L (0.3 L/kg for a 70 kg adult), indicating distribution into extracellular fluid. |
| Bioavailability | Intravenous: 100% (administered as IV infusion). |
| Onset of Action | Intravenous: onset within 15 minutes. |
| Duration of Action | Duration of action is approximately 6-8 hours based on blood pressure reduction; antihypertensive effect correlates with plasma concentrations. |
1 mg/kg intravenously or subcutaneously every 6 hours for acute attacks, maximum 3.3 mL per injection site.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for renal impairment. Safety and efficacy not established in ESRD. |
| Liver impairment | No dose adjustment required for hepatic impairment. |
| Pediatric use | Safety and efficacy in pediatric patients have not been established. |
| Geriatric use | No specific dose adjustment; use with caution due to potential renal and hepatic impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for QBRELIS (QBRELIS).
| Breastfeeding | It is not known if lisinopril is excreted in human breast milk. Due to limited data and potential for serious adverse reactions in nursing infants (hypotension, hyperkalemia), breastfeeding is not recommended by the manufacturer. M/P ratio is not available. |
| Teratogenic Risk | Qbrelis (lisinopril) is an ACE inhibitor. First trimester exposure is associated with a potential increased risk of congenital malformations (cardiovascular, renal). Second and third trimester exposure is associated with fetal hypotension, oligohydramnios, renal failure, skull ossification defects, and anuria. Use is contraindicated in pregnancy. |
■ FDA Black Box Warning
None
| Serious Effects |
["Concomitant use with aliskiren in patients with diabetes","History of hypersensitivity to any component of the formulation","Pregnancy (second and third trimesters)"]
| Precautions | ["Fetal toxicity: Boxed warning for drugs acting on renin-angiotensin system in pregnancy; discontinue if pregnancy occurs.","Hypotension: Symptomatic hypotension may occur, especially in volume-depleted patients or those with heart failure.","Renal impairment: Monitor renal function; risk of acute renal failure.","Hyperkalemia: Monitor potassium levels; increased risk with concomitant use of potassium-sparing diuretics or supplements.","Hepatic impairment: Use with caution in patients with hepatic impairment."] |
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| Fetal Monitoring | Monitor maternal blood pressure, renal function (serum creatinine, BUN), and serum potassium periodically. Monitor fetal growth, amniotic fluid volume, and fetal kidney function via ultrasound. Perform neonatal monitoring for hypotension, oliguria, hyperkalemia, and renal function after delivery. |
| Fertility Effects | Based on preclinical data, no direct effects on fertility have been reported. However, ACE inhibitors may affect the renin-angiotensin system, and in reproductive studies, no impairment of fertility was observed in rats. |