Generic
Peginterferon Alfa-2a
8 brands available in the market
At a glance
Peginterferon Alfa-2a is an interferon protein bound to polyethylene glycol used for the treatment of chronic hepatitis C and chronic hepatitis B.
Description
Peginterferon alfa-2a is a covalent conjugate of recombinant alfa-2a interferon with a single branched bis-monomethoxy polyethylene glycol chain. It has antiviral, antiproliferative, and immune-regulating activity. Interferons are activated when they interact with cells through high-affinity cell surface receptors, inducing gene transcription, inhibiting cellular growth, altering cellular differentiation, interfering with oncogene expression, altering cell surface antigen expression, increasing macrophage phagocytic activity, and augmenting lymphocyte cytotoxicity.
Indications
- Chronic hepatitis C (compensated liver disease)
- Chronic hepatitis B (HBeAg positive and negative)
Therapeutic class
Hepatic viral infections (Hepatitis B & C)
Pharmacological class
Interferon
Pharmacology
Peginterferon alfa-2a is an interferon protein bound to PEG molecules, resulting in higher and more prolonged serum interferon concentrations. It has antiviral, antiproliferative, and immune-regulating activity. Interferons are activated when they interact with cells through high-affinity cell surface receptors, leading to induction of gene transcription, inhibition of cellular growth, alteration of cellular differentiation, interference with oncogene expression, alteration of cell surface antigen expression, increase in macrophage phagocytic activity, and augmentation of lymphocyte cytotoxicity.
Mechanism of action
Activates antiviral, antiproliferative, and immune-regulating activities by binding to cell surface receptors.
Dosage
Adult Dose (Subcutaneous):
- Chronic hepatitis C: 180 mcg once weekly for 48 weeks (monotherapy) OR with ribavirin (Genotypes 1 & 4: 48 weeks; Genotypes 2 & 3: 24 weeks)
- Chronic hepatitis B: 180 mcg once weekly for 48 weeks
- Dose modifications: Neutropenia (ANC <750: 135 mcg; <500: discontinue), Thrombocytopenia (Platelets <50,000: 90 mcg; <25,000: discontinue), Hepatic (ALT rise: 135 mcg; continued rise or bilirubin increase: discontinue)
Pediatric Dose (>5 years): 180 mcg/1.73 m² once weekly with ribavirin; Genotypes 2,3: 24 weeks; Genotypes 1,4: 48 weeks
Administration
- Administer by SC injection once weekly in abdomen or thigh
- Take at the same time each week
- Do not change interferon brands without healthcare provider concurrence
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects (>10%):
- Fatigue (24-67%)
- Headache (27-54%)
- Fever (24-54%)
- Myalgia (26-51%)
- Influenza-like illness (25-47%)
- Neutropenia (21-40%)
- Anxiety (19-33%)
- Irritability (19-33%)
- Diarrhea (11-31%)
- Insomnia (19-30%)
- Arthralgia (22-28%)
- Alopecia (18-28%)
- Nausea and vomiting (5-25%)
- Loss of appetite (16-24%)
- Depression (18-20%)
- Anemia (2-14%)
Precautions & warnings
- Neuropsychiatric disorders: Discontinue treatment with worsening or persistently severe signs/symptoms
- Myelosuppression, anemia (spherocytosis, history of GI bleeding)
- Caution in pulmonary disease, autoimmune disease, cardiovascular disease, diabetes, thyroid disorders
- More frequent monitoring of LFTs and dose reduction in Hepatitis B
- May affect ability to drive or operate machinery
- Hazardous agent; handle and dispose appropriately
Contraindications
- Hypersensitivity to any component of the product
- Autoimmune hepatitis
- Decompensated liver disease in cirrhotic patients (Child-Pugh score >6)
- Decompensated liver disease (Child-Pugh >6, class B and C) in chronic hepatitis C coinfected with HIV
- Neonates and infants
- In combination with ribavirin in pregnant women (Category X)
Drug interactions
- Drugs metabolized by CYP1A2 (theophylline): Monitor serum levels
- Methadone: Monitor for signs of methadone toxicity
- Nucleoside analogues: Monitor for toxicities
- Zidovudine: Monitor for worsening neutropenia and anemia
- Ribavirin: Increased risk of hemolytic anemia, fetal mortality, genotoxicity, mutagenicity, carcinogenicity
- Azathioprine
Food interactions
Avoid ethanol in hepatitis C patients.
Use in pregnancy
Use in Pregnancy: Monotherapy: Category C (teratogenic effects not studied); use effective contraception. With ribavirin: Category X (significant teratogenic and embryocidal effects; contraindicated).
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Unknown if distributed in human breast milk; due to potential for adverse reactions in nursing infants, decide whether to discontinue nursing or discontinue the drug.
Pediatric use
Safety and efficacy not established in children under 5 years.
Geriatric use
Caution required in elderly patients; safety and efficacy not established.
Renal / hepatic impairment
Renal Impairment: CrCl 30-50 mL/min: 180 mcg once weekly; CrCl <30 mL/min (including hemodialysis): 135 mcg once weekly; severe adverse reactions: reduce to 90 mcg.
Hepatic Impairment: ALT progressively rising: 135 mcg/week; continued rise or increased bilirubin/hepatic decompensation: discontinue immediately.
Overdose effects
Limited overdose experience; no serious reactions; no specific antidote; dialysis is not effective.
Storage conditions
Store in refrigerator at 2-8°C; do not freeze or shake; protect from light.
Chemical structure
Peginterferon Alfa-2a