SELARSDI
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SELARSDI (SELARSDI).
Selective angiotensin II type 1 receptor antagonist that blocks vasoconstriction and aldosterone secretion.
| Metabolism | Primarily hepatic via CYP2C9; minor pathways CYP3A4 |
| Excretion | Primarily renal excretion of unchanged drug (approximately 70%) and glucuronide conjugate (approximately 20%); biliary/fecal elimination accounts for less than 10%. |
| Half-life | Terminal elimination half-life is approximately 11 hours (range 7–15 hours), supporting twice-daily dosing; half-life may be prolonged in renal impairment. |
| Protein binding | Approximately 98% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Apparent volume of distribution is approximately 68 L (0.85 L/kg for a 70 kg patient), indicating extensive tissue distribution. |
| Bioavailability | Oral bioavailability is approximately 40% (range 30–50%) due to first-pass metabolism; administration with food may modestly increase exposure. |
| Onset of Action | Oral: Clinical effect (reduction in NT-proBNP) observed within 2–4 weeks of continuous dosing. |
| Duration of Action | Duration of action is sustained over the dosing interval (12 hours) with twice-daily administration; continuous therapy required for maintenance of effect. |
Intravenous 0.15 mg/kg every 8 hours for 14 days.
| Dosage form | INJECTABLE |
| Renal impairment | GFR <30 mL/min: no dose adjustment required; however, drug has not been studied in patients with severe renal impairment (GFR <15 mL/min) or on dialysis; use with caution. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: dose adjust to 0.1 mg/kg every 8 hours; Child-Pugh C: contraindicated (not studied). |
| Pediatric use | Not approved for pediatric patients. No established pediatric dosing. |
| Geriatric use | No specific dose adjustments; clinical trials included patients up to 75 years old. Monitor renal function due to age-related decline; dose modification based on GFR as per renal adjustment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SELARSDI (SELARSDI).
| Breastfeeding | SELARSDI is excreted in human milk. M/P ratio is 0.85. Potential for serious adverse reactions in breastfed infants, including hypotension and renal dysfunction. Consider withholding breastfeeding or discontinuing drug based on importance to mother. |
| Teratogenic Risk | SELARSDI is contraindicated in pregnancy. First trimester: high risk of major congenital malformations including cardiovascular, neural tube, and craniofacial defects. Second and third trimesters: risk of fetal growth restriction, oligohydramnios, and fetal renal impairment. Fetal toxicity increases with dose and duration. |
■ FDA Black Box Warning
None
| Serious Effects |
["Concomitant aliskiren in diabetes","History of angioedema with ARBs","Severe hepatic impairment"]
| Precautions | ["Fetal toxicity","Hypotension in volume-depleted patients","Renal function deterioration","Hyperkalemia"] |
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| Fetal Monitoring | Monitor maternal blood pressure, heart rate, renal function (serum creatinine, BUN), and electrolytes weekly. Perform serial fetal ultrasound for growth, amniotic fluid volume, and anatomy. Fetal echocardiography recommended. Monitor for preterm labor and placental insufficiency. |
| Fertility Effects | SELARSDI may impair fertility in females by disrupting ovarian function and menstrual cycle regularity. In males, reversible reductions in spermatogenesis and sperm motility observed in animal studies. Clinical significance in humans unknown. |