Usage
- Methoxy polyethylene glycol-epoetin beta is prescribed for the treatment of anemia associated with chronic kidney disease (CKD) in adults and children aged 5-17 years on hemodialysis converting from another erythropoiesis-stimulating agent (ESA).
- Pharmacological Classification: Erythropoiesis-stimulating agent (ESA).
- Mechanism of Action: Methoxy polyethylene glycol-epoetin beta stimulates erythropoiesis by interacting with erythropoietin receptors on progenitor cells in the bone marrow. This interaction promotes the proliferation and differentiation of erythroid precursor cells, leading to increased red blood cell production.
Alternate Names
- Mircera
- Pegzerepoetin alfa
- CERA
How It Works
- Pharmacodynamics: Methoxy polyethylene glycol-epoetin beta increases hemoglobin levels and red blood cell counts. It reduces the need for red blood cell transfusions in patients with CKD.
- Pharmacokinetics:
- Absorption: After subcutaneous administration, absolute bioavailability is approximately 54% in patients not on dialysis and 62% in patients on dialysis.
- Metabolism: Limited information is available on the metabolism of methoxy polyethylene glycol-epoetin beta. However, being analogous to erythropoietin, it is believed to undergo catabolism within the cells of the reticuloendothelial system and kidneys after binding to erythropoietin receptors.
- Elimination: The terminal elimination half-life is approximately 139-142 hours. It is presumably excreted via the kidneys, although detailed elimination pathways are not fully characterized.
- Mode of Action: Binds to erythropoietin receptors on erythroid progenitor cells in the bone marrow, stimulating their proliferation and differentiation, ultimately increasing red blood cell production.
- Receptor Binding/Enzyme Inhibition: Binds to erythropoietin receptors.
- Elimination Pathways: Primarily renal excretion. However, since this drug is a complex molecule with a PEG chain, the exact mechanism of elimination and its distribution in the body requires further research.
Dosage
Standard Dosage
Adults:
- CKD not on dialysis: 1.2 mcg/kg subcutaneously once monthly.
- CKD on dialysis: Initial dose of 0.6 mcg/kg intravenously or subcutaneously every 2 weeks. Once hemoglobin is stabilized, administer dose once monthly using a dose that is twice that of every-two-week dose. Further titration as needed.
Children:
- 5-17 years on hemodialysis converting from another ESA: Dose depends on total weekly ESA dose; administer intravenously every 4 weeks. Safety and efficacy have not been established in children younger than 5 years converting from an ESA, children not converting from another ESA, or children not on hemodialysis.
Special Cases:
- Elderly Patients: No dose adjustment is required.
- Patients with Renal Impairment: Dose adjustments are required, as described above.
- Patients with Hepatic Dysfunction: No information on dose adjustments is available. Use with caution.
- Patients with Comorbid Conditions: Use with caution in patients with uncontrolled hypertension, cardiovascular disease, or history of seizures.
Clinical Use Cases
Dosing for intubation, surgical procedures, mechanical ventilation, ICU use, and emergency situations is not specifically provided in the source material.
Dosage Adjustments
- Dose adjustments may be required based on hemoglobin response, iron status, and other factors.
- Renal impairment necessitates dose adjustments, as outlined above. Limited information is available on dose adjustments for hepatic dysfunction or genetic polymorphisms.
Side Effects
Common Side Effects
- Headache
- Body aches
- Diarrhea
- Vomiting
- Hypertension
- Muscle spasms
- Back pain
- Nasopharyngitis
- Upper respiratory tract infection
- Cough
Rare but Serious Side Effects
- Seizures
- Pure red cell aplasia (PRCA)
- Serious allergic reactions (including anaphylaxis)
- Blood clots (including myocardial infarction, stroke, venous thromboembolism)
- Tumor progression (in cancer patients)
- Severe cutaneous adverse reactions (e.g., erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome)
Long-Term Effects
- Long-term effects of methoxy polyethylene glycol-epoetin beta are not fully known. Potential long-term side effects may include cardiovascular complications and tumor progression in cancer patients.
Adverse Drug Reactions (ADR)
- Serious allergic reactions
- Hypertensive encephalopathy
- Seizures
- PRCA
- Thromboembolic events
Contraindications
- Uncontrolled hypertension
- Pure red cell aplasia after treatment with ESAs
- Serious allergic reactions to methoxy polyethylene glycol-epoetin beta or its components
Drug Interactions
- Limited information on drug interactions is available.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: C (US FDA), B3 (AU TGA)
- Limited data available on use during pregnancy. Potential risks include fetal harm.
- It is unknown whether methoxy polyethylene glycol-epoetin beta is excreted in breast milk.
Drug Profile Summary
- Mechanism of Action: Stimulates erythropoiesis via erythropoietin receptors.
- Side Effects: Headache, body aches, diarrhea, vomiting, serious allergic reactions, blood clots, seizures, PRCA.
- Contraindications: Uncontrolled hypertension, PRCA after ESAs, hypersensitivity to the drug.
- Drug Interactions: Limited data available.
- Pregnancy & Breastfeeding: Limited data, use with caution if potential benefits outweigh risks.
- Dosage: Adults: based on body weight and dialysis status. Children: limited to patients aged 5-17 on hemodialysis, converting from another ESA.
- Monitoring Parameters: Hemoglobin, blood pressure, iron stores, transferrin saturation, serum ferritin, signs and symptoms of seizures and hypersensitivity reactions.
Popular Combinations
- Information on popular drug combinations with methoxy polyethylene glycol-epoetin beta is limited. Supplemental iron therapy is recommended for patients with low ferritin (<100 mcg/L) or low transferrin saturation (<20%).
Precautions
- Monitor blood pressure, hemoglobin levels, and iron status.
- Assess for seizures and hypersensitivity reactions.
- Use with caution in patients with cardiovascular disease or history of seizures.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Methoxy polyethylene glycol-epoetin beta?
A: The dosage varies depending on the patient’s age, kidney function, and dialysis status. Refer to the “Dosage” section above for specific details.
Q2: What are the common side effects of Methoxy polyethylene glycol-epoetin beta?
A: Common side effects include headache, body aches, diarrhea, vomiting, and elevated blood pressure.
Q3: Is Methoxy polyethylene glycol-epoetin beta safe during pregnancy?
A: Limited data are available regarding the use of Methoxy polyethylene glycol-epoetin beta during pregnancy. Use only if the potential benefits outweigh the risks. Consult with a healthcare professional.
Q4: How does Methoxy polyethylene glycol-epoetin beta work?
A: It stimulates erythropoiesis by binding to erythropoietin receptors on bone marrow progenitor cells.
Q5: What are the contraindications to Methoxy polyethylene glycol-epoetin beta?
A: Uncontrolled hypertension, pure red cell aplasia following treatment with ESAs, and known hypersensitivity are contraindications.
Q6: What is the difference between Methoxy polyethylene glycol-epoetin beta and other ESAs?
A: Methoxy polyethylene glycol-epoetin beta is a long-acting ESA, allowing for less frequent administration compared to some other ESAs like epoetin alfa.
Q7: Are there any specific monitoring parameters for patients on Methoxy polyethylene glycol-epoetin beta?
A: Yes, regular monitoring of hemoglobin levels, blood pressure, and iron status is essential.
Q8: Can Methoxy polyethylene glycol-epoetin beta be used in children?
A: Yes, in children of age 5-17 on hemodialysis, who are converting from another ESA.
Q9: What should I do if a patient experiences side effects?
A: The patient should contact their healthcare provider immediately if they experience any side effects, especially severe ones.
