TRASICOR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TRASICOR (TRASICOR).
Non-selective beta-adrenergic antagonist with intrinsic sympathomimetic activity (partial agonist) at beta-1 and beta-2 receptors, reducing heart rate, myocardial contractility, and blood pressure.
| Metabolism | Hepatic metabolism primarily via CYP2D6; active metabolites include oxprenolol's glucuronide conjugates. |
| Excretion | Renal excretion of unchanged drug and metabolites accounts for approximately 80% of elimination, with about 20% appearing as unchanged drug; biliary/fecal excretion accounts for the remaining 20%. |
| Half-life | Terminal elimination half-life is approximately 8-12 hours in patients with normal renal function; may be prolonged in renal impairment, requiring dose adjustment. |
| Protein binding | Approximately 85-90% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 4-6 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral: Approximately 85% due to minimal first-pass metabolism. |
| Onset of Action | Oral: 1-2 hours; Intravenous: 5-15 minutes. |
| Duration of Action | Oral: 12-24 hours; Intravenous: 4-6 hours; clinical effects such as heart rate reduction and antianginal effects persist accordingly. |
20-40 mg orally three times daily, increased to 80-160 mg daily if needed; maximum 320 mg/day.
| Dosage form | CAPSULE |
| Renal impairment | GFR 10-50 mL/min: reduce dose by 50%; GFR <10 mL/min: reduce dose by 75% or use with caution. |
| Liver impairment | Child-Pugh Class A: no adjustment; Class B: reduce dose by 50%; Class C: contraindicated. |
| Pediatric use | 0.5-1 mg/kg/day orally divided every 6-8 hours; maximum 2 mg/kg/day. |
| Geriatric use | Initial dose 10 mg twice daily; titrate slowly due to increased sensitivity and risk of bradycardia. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TRASICOR (TRASICOR).
| Breastfeeding | Excreted in breast milk with M:P ratio approximately 1.5. Monitor infant for bradycardia and hypoglycemia. Consider alternatives with lower milk transfer. |
| Teratogenic Risk | Pregnancy category C. First trimester: No evidence of teratogenicity in animal studies, but human data limited; potential risk of fetotoxicity. Second/third trimester: May cause fetal bradycardia, hypoglycemia, and intrauterine growth restriction. Avoid in preeclampsia due to risk of fetal hypoxia. |
| Fetal Monitoring |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Sinus bradycardia (<45-50 bpm)","Second- or third-degree atrioventricular block (unless paced)","Cardiogenic shock","Decompensated heart failure","Hypersensitivity to oxprenolol or any component","Severe asthma or chronic obstructive pulmonary disease (COPD) with bronchospasm","Severe peripheral arterial disease"]
| Precautions | ["Cardiac failure: May precipitate or worsen heart failure; use cautiously in compensated patients.","Bronchospasm: Avoid in asthma without proper precautions; non-selective beta-blockade may exacerbate bronchospasm.","Abrupt withdrawal: Taper gradually to avoid rebound hypertension, angina, or arrhythmias.","Peripheral vascular disease: May worsen symptoms due to reduced cardiac output.","Hyperthyroidism: May mask symptoms (e.g., tachycardia); abrupt withdrawal may precipitate thyroid storm.","Anaphylactic reactions: May be resistant to epinephrine treatment.","Diabetes mellitus: May mask hypoglycemia symptoms (e.g., tachycardia).","Renal impairment: Dose adjustment may be needed in severe impairment."] |
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| Monitor maternal heart rate, blood pressure, and signs of heart failure. Fetal assessment includes heart rate monitoring, ultrasound for growth, and amniotic fluid index. Neonatal monitoring for bradycardia and hypoglycemia postpartum. |
| Fertility Effects | Beta-blockers may reduce sperm motility and count in males; no significant female fertility impairment reported. Limited data. |