RENORMAX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for RENORMAX (RENORMAX).
Selective beta-1 adrenergic receptor antagonist; reduces cardiac output, heart rate, and blood pressure by blocking catecholamine effects on cardiac beta-1 receptors.
| Metabolism | Hepatic metabolism via CYP2D6 to active metabolite; renal excretion of metabolites. |
| Excretion | Primarily renal (60-70% unchanged; 10-15% as glucuronide conjugate); biliary/fecal (5-10%); 80-85% total recovered in urine and feces within 72 hours. |
| Half-life | Terminal elimination half-life: 8-10 hours in healthy adults. Prolonged to 18-24 hours in moderate renal impairment (CrCl 30-50 mL/min). Provides basis for twice-daily dosing in normal renal function. |
| Protein binding | 92-96% bound, primarily to albumin (HSA) and to a lesser extent alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.25-0.45 L/kg, indicating moderate tissue penetration, consistent with distribution into total body water with some extravascular binding. |
| Bioavailability | Oral: 55-70% due to moderate first-pass metabolism; IM: 80-90% (not a standard route in approved labeling). |
| Onset of Action | IV: 2-5 minutes; Oral: 30-45 minutes; Peak effect: IV 15-30 min, Oral 1-2 hours. |
| Duration of Action | IV: 4-6 hours dependent on renal clearance; Oral: 6-8 hours at steady state. Extended in renal impairment. |
5 mg intravenously every 12 hours
| Dosage form | TABLET |
| Renal impairment | CrCl 30-50 mL/min: 2.5 mg every 12 hours; CrCl <30 mL/min: 2.5 mg every 24 hours; hemodialysis: 2.5 mg after dialysis |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 2.5 mg every 12 hours; Child-Pugh C: contraindicated |
| Pediatric use | 0.1 mg/kg intravenously every 12 hours, maximum 5 mg per dose; not recommended in neonates |
| Geriatric use | Start at 2.5 mg intravenously every 12 hours; titrate based on renal function and response |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for RENORMAX (RENORMAX).
| Breastfeeding | Excretion into breast milk: M/P ratio 0.8. Relative infant dose estimated <2% of maternal weight-adjusted dose. Use with caution in preterm infants or those with renal impairment. |
| Teratogenic Risk | First trimester: Human data insufficient; animal studies show increased fetal resorptions at supratherapeutic doses. Second trimester: No evidence of teratogenicity but may cause fetal tachycardia. Third trimester: Risk of premature closure of ductus arteriosus and neonatal hypotension. |
| Fetal Monitoring |
■ FDA Black Box Warning
No black box warning
| Serious Effects |
Sinus bradycardia, sick sinus syndrome, second- or third-degree AV block (unless pacemaker), cardiogenic shock, decompensated heart failure, severe asthma, hypersensitivity to drug.
| Precautions | May cause bradycardia, heart block, hypotension; avoid abrupt discontinuation (risk of exacerbation of angina or myocardial infarction); caution in asthma, COPD, diabetes, peripheral vascular disease, and thyrotoxicosis. |
Loading safety data…
| Maternal: heart rate, blood pressure, serum electrolytes (potassium, magnesium), renal function (creatinine, BUN). Fetal: ultrasound for growth, amniotic fluid index, fetal heart rate monitoring (non-stress test) weekly or biweekly after 28 weeks gestation. |
| Fertility Effects | No human data; animal studies show no impairment of fertility at therapeutic doses. |