Description
Erythropoietin (EPO – recombinant, 5 000 IU formulation)
Erythropoietin is a glycoprotein hormone that stimulates red‑blood‑cell production by binding the erythropoietin receptor (EPOR) on erythroid progenitors in the bone‑marrow, activating JAK2‑STAT5 signaling and driving proliferation, survival, and maturation of erythroblasts.
| Item | Details |
|---|---|
| Primary indication | Treatment of anemia due to chronic kidney disease, chemotherapy‑induced anemia, HIV‑related anemia, and peri‑operative blood‑conservation. |
| Mechanism of action | EPO → EPOR dimer → JAK2 autophosphorylation → STAT5 translocation → transcription of anti‑apoptotic (Bcl‑xL) and proliferative genes → ↑ reticulocyte output and hemoglobin. |
| Typical dosing (5 000 IU) | • CKD anemia – 5 000 IU subcutaneously (SC) once weekly (or 2 000 IU thrice weekly) titrated to target Hb 10–12 g/dL. • Chemotherapy‑induced anemia – 5 000 IU SC every 2–3 weeks, adjusted based on Hb response. • Surgical blood‑conservation – 5 000 IU IV 48 h before surgery, then 5 000 IU IV 24 h later. |
| Pharmacokinetics | • Absorption – SC peak ≈ 12–18 h; IV peak immediate.<br>• Half‑life – ~4–6 h (IV) vs. 18–24 h (SC) because of glycosylation and renal clearance. • Distribution – Vd ≈ 0.2 L/kg (extracellular fluid). • Metabolism/Elimination – Proteolytic degradation; renal excretion of metabolites. |
| Safety / Common AEs | • Hypertension (dose‑related). • Headache, flushing. • Thromboembolic events (especially if Hb > 12 g/dL). • Pure red‑cell aplasia (rare, antibody‑mediated). |
| Contra‑indications / Precautions | • Uncontrolled hypertension. • Active thromboembolic disease.<br>• Known anti‑EPO antibodies. • Pregnancy – only if benefit outweighs risk. |
| Regulatory status | FDA‑approved (e.g., epoetin alfa, darbepoetin alfa) for the indications above; no over‑the‑counter product. |
| WADA | Not prohibited; however, therapeutic use exemption (TUE) is required for athletes who receive EPO for a legitimate medical condition. |
| Practical notes | • Dose is individualized based on hemoglobin trend and iron status (ensure adequate iron stores).<br>• Monitoring: CBC weekly initially, then every 2–4 weeks; blood pressure each visit.<br>• Avoid exceeding target Hb to reduce thrombosis risk. |
Bottom line: A 5 000 IU dose of recombinant EPO is the standard starting point for most anemia indications, administered subcutaneously or intravenously depending on the clinical scenario. It effectively raises hemoglobin by stimulating erythropoiesis, but careful dosing and monitoring are essential to mitigate hypertension and thrombotic risks.