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Interferon Beta-1b

Pronunciation

(in ter FEER on BAY ta won bee)

Index Terms

  • rIFN beta-1b

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Kit, Subcutaneous:

Betaseron: 0.3 mg [contains albumin human]

Kit, Subcutaneous [preservative free]:

Extavia: 0.3 mg [contains albumin human]

Brand Names: U.S.

  • Betaseron
  • Extavia

Pharmacologic Category

  • Interferon

Pharmacology

Interferon beta-1b differs from naturally occurring human protein by a single amino acid substitution and the lack of carbohydrate side chains; mechanism in the treatment of MS is unknown; however, immunomodulatory effects attributed to interferon beta-1b include enhancement of suppressor T cell activity, reduction of proinflammatory cytokines, down-regulation of antigen presentation, and reduced trafficking of lymphocytes into the central nervous system. Improves MRI lesions, decreases relapse rate, and disease severity in patients with secondary progressive MS.

Time to Peak

1-8 hours

Half-Life Elimination

8 minutes to 4.3 hours

Use: Labeled Indications

Multiple sclerosis: Treatment of relapsing forms of multiple sclerosis (MS) to reduce the frequency of clinical exacerbations.

Canadian labeling: Additional use (not in US labeling): Treatment of secondary progressive MS

Contraindications

History of hypersensitivity to natural or recombinant interferon beta, albumin (human), or any component of the formulation.

Documentation of allergenic cross-reactivity for interferons is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.

Canadian labeling: Additional contraindication (not in US labeling): Pregnancy, decompensated liver disease (Betaseron, Extavia); current severe depression and/or suicidal ideation (Extavia)

Dosing: Adult

Note: Analgesics and/or antipyretics may help decrease flu-like symptoms on treatment days:

US labeling:

Multiple sclerosis (relapsing): SubQ: Initial: 0.0625 mg (2 million units [0.25 mL]) every other day; gradually increase dose by 0.0625 mg every 2 weeks to a target dose of 0.25 mg (8 million units [1 mL]) every other day. Note: In clinical trials involving patients with a single clinical event suggestive of MS, dose titration occurred at weekly intervals (Kappos 2006).

Canadian labeling:

Multiple sclerosis (relapsing): SubQ: Initial: 0.0625 mg (2 million units [0.25 mL]) every other day; gradually increase dose by 0.0625 mg every week to a target dose of 0.25 mg (8 million units [1 mL]) every other day. May titrate more slowly if significant adverse reactions occur.

Multiple sclerosis (secondary progressive): SubQ: Initial: 0.125 mg (4 million units [0.5 mL]) every other day for 2 weeks; gradually increase to target dose of 0.25 mg (8 million units [1 mL]) every other day

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer’s labeling. The Canadian labeling contraindicates use in decompensated liver disease.

Reconstitution

To reconstitute solution, inject 1.2 mL of diluent (provided); gently swirl to dissolve, do not shake. Reconstituted solution provides 0.25 mg/mL. Use product within 3 hours of reconstitution. Discard unused portion of vial. Foaming may occur if swirled or shaken too vigorously; allow vial to sit until foam settles.

Administration

For SubQ administration. The first injection should be administered under the supervision of a health care professional. Withdraw dose of reconstituted solution from the vial into a sterile syringe fitted with a 27-gauge (Extavia) or 30-gauge (Betaseron) needle and inject the solution subcutaneously. The Betaconnect autoinjector may be used with prepared Betaseron syringes after health care provider selects proper depth setting and injection technique (see prescribing information for more detailed use of autoinjector). Sites for self-injection include outer surface of the arms, abdomen (except 2-inch area around the navel), buttocks, and thighs. If patient is very thin, only use the thigh or outer surface of arms. Rotate SubQ injection site. Do not inject into area where skin is bruised, infected, or broken. Patient should be well hydrated. If a dose is missed, administer as soon as remembered; do not administer on 2 consecutive days. Time subsequent doses every 48 hours.

Storage

Store intact vials at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) for ≤3 months. If not used immediately following reconstitution, refrigerate solution at 2°C to 8°C (35°F to 46°F) and use within 3 hours; do not freeze or shake solution. Discard unused portion of vial.

Drug Interactions

Theophylline Derivatives: Interferons may decrease the metabolism of Theophylline Derivatives. Exceptions: Dyphylline. Monitor therapy

Zidovudine: Interferons may enhance the adverse/toxic effect of Zidovudine. Interferons may decrease the metabolism of Zidovudine. Monitor therapy

Adverse Reactions

>10%:

Cardiovascular: Peripheral edema (12% to 15%), chest pain (9% to 11%)

Central nervous system: Headache (50% to 57%), pain (42% to 51%), hypertonia (40% to 50%), myasthenia (46%), chills (21% to 25%), dizziness (24%), insomnia (21% to 24%), ataxia (17% to 21%)

Dermatologic: Skin rash (21% to 24%), dermatological disease (10% to 12%)

Gastrointestinal: Nausea (27%), constipation (20%), diarrhea (19%), abdominal pain (16% to 19%), dyspepsia (14%)

Genitourinary: Urinary urgency (11% to 13%), uterine hemorrhage (9% to 11%)

Hematologic & oncologic: Lymphocytopenia (86% to 88%), leukopenia (13% to 18%), neutropenia (13% to 14%)

Immunologic: Antibody development (≤45%; neutralizing; significance not known)

Local: Injection site reaction (78% to 85%; including inflammation [53%], pain [18%], tissue necrosis [4% to 5%], hypersensitivity reaction [4%], swelling [2% to 3%], residual mass [2%])

Neuromuscular & skeletal: Weakness (53% to 61%), arthralgia (31%), myalgia (23% to 27%)

Respiratory: Flu-like symptoms (decreases over treatment course; 57% to 60%)

Miscellaneous: Fever (31% to 36%)

1% to 10%:

Cardiovascular: Vasodilatation (8%), hypertension (6% to 7%), peripheral vascular disease (6%), palpitations (4%), tachycardia (4%)

Central nervous system: Anxiety (10%), malaise (6% to 8%), nervousness (7%)

Dermatologic: Diaphoresis (8%), alopecia (4%)

Endocrine & metabolic: Hypermenorrhea (8%), dysmenorrhea (7%), weight gain (7%)

Genitourinary: Impotence (8% to 9%), cystitis (8%), urinary frequency (7%), pelvic pain (6%), prostatic disease (3%)

Hematologic & oncologic: Lymphadenopathy (6% to 8%)

Hepatic: Increased serum ALT (>5x baseline: 10% to 12%), increased serum AST (>5x baseline: 3% to 4%)

Hypersensitivity: Hypersensitivity (3%)

Neuromuscular & skeletal: Leg cramps (4%)

Respiratory: Dyspnea (6% to 7%)

<1% (Limited to important or life-threatening): Anaphylaxis, anorexia, apnea, ataxia, autoimmune hepatitis, capillary leak syndrome (in patients with preexisting monoclonal gammopathy), cardiac arrhythmia, cardiomegaly, cardiomyopathy, cerebral hemorrhage, coma, confusion, convulsion, deep vein thrombosis, delirium, depersonalization, depression, emotional lability, erythema nodosum, ethanol sensitization, exfoliative dermatitis, gastrointestinal hemorrhage, hallucinations, hematemesis, hemolytic-uremic syndrome, hepatic failure, hepatitis, hepatotoxicity (idiosyncratic) (Chalasani 2014), hyperthyroidism, hyperuricemia, hypocalcemia, increased gamma-glutamyl transferase, increased serum triglycerides, lupus erythematosus, maculopapular rash, manic behavior, myocardial infarction, pancreatitis, pericardial effusion, pneumonia, pruritus, psychosis, pulmonary embolism, rash, sepsis, shock, skin discoloration, skin photosensitivity, suicidal ideation, syncope, SIADH, thrombocytopenia, thrombotic thrombocytopenic purpura, thyroid dysfunction, urinary tract infection, urosepsis, vasculitis, vaginal hemorrhage, vesiculobullous dermatitis, weight loss

Warnings/Precautions

Concerns related to adverse effects:

• Anaphylaxis/hypersensitivity reactions: Allergic reactions (eg, bronchospasm, dyspnea, skin rash, tongue edema, urticaria), including anaphylaxis (rare), have been reported with use; discontinue use if anaphylaxis occurs.

• Drug-induced lupus erythematosus: Cases of drug-induced lupus erythematosus have been reported with some interferon beta products; signs and symptoms include nephritis, polyarthritis, rash, Raynaud phenomenon, and serositis. Positive serologic testing, including positive anti-nuclear and/or anti-double-stranded DNA antibody testing, may occur; discontinue treatment if signs and symptoms of drug-induced lupus erythematosus develop.

• Flu-like symptoms: Associated with a high incidence of flu-like adverse effects; use of analgesics and/or antipyretics on treatment days may be helpful. Improvement in symptoms occurs over time.

• Hepatotoxicity: Has been reported with beta interferons, including rare reports of hepatitis (autoimmune) and hepatic failure requiring transplant; use with caution in patients with concurrent exposure to other hepatotoxic drugs. Monitor liver function tests as clinically necessary. Consider discontinuation if serum transaminase levels increase significantly or are associated with clinical symptoms (eg, jaundice).

• Injection site reactions: Severe injection site reactions (necrosis) may occur which may or may not heal with continued therapy; reactions generally arise within the first 4 months of therapy, but have occurred ≥1 year after initiation. Incidence of reactions tend to improve over time. Patient and/or caregiver competency in injection technique should be confirmed and periodically re-evaluated. Do not inject into affected area until completely healed; if multiple lesions occur, discontinue use until they are fully healed.

• Leukopenia: Leukopenia has been observed; routine monitoring of complete blood counts with differentials is recommended. Dose reduction may be required.

• Neuropsychiatric disorders: Interferons have been associated with severe psychiatric adverse events (psychosis, mania, depression, suicidal behavior/ideation) in patients with and without previous psychiatric symptoms. Avoid use in severe psychiatric disorders and use caution in patients with a history of depression; patients exhibiting symptoms of depression should be closely monitored and discontinuation of therapy should be considered.

• Thrombotic microangiopathy: Cases of thrombotic microangiopathy manifesting as thrombotic thrombocytopenic purpura (TTP) or hemolytic uremic syndrome (HUS) (some fatal) have been reported with interferon beta products. Some cases may occur after several years of therapy. Monitor for new onset hypertension, thrombocytopenia, or impaired renal function; discontinuation of therapy and prompt treatment may be necessary if TTP/HUS are confirmed.

Disease-related concerns:

• Bone marrow suppression: Use with caution in patients with bone marrow suppression; may require increased monitoring.

• Cardiovascular disease: Use with caution in patients with pre-existing cardiovascular disease. Rare cases of new-onset cardiomyopathy and/or HF have been reported. If HF worsens in the absence of another etiology, consider discontinuation of therapy.

• Hepatic impairment: Use with caution in patients with hepatic impairment or in combination with alcohol. The Canadian labeling contraindicates use in patients with decompensated hepatic disease.

• Seizure disorder: Use with caution in patients with a history of seizure disorder.

• Thyroid dysfunction: Thyroid abnormalities may develop with use; may worsen pre-existing thyroid conditions. Monitor thyroid function tests every 6 months or as clinically necessary.

Dosage form specific issues:

• Albumin: Contains albumin, which may carry a remote risk of transmitting Creutzfeldt-Jakob or other viral diseases.

• Latex: Some dosage forms may contain natural rubber latex.

Monitoring Parameters

Complete blood chemistries (including platelet count) and liver function tests are recommended at 1, 3, and 6 months following initiation of therapy and periodically thereafter. Thyroid function should be assessed every 6 months in patients with history of thyroid dysfunction or as clinically necessary. Monitor for flu-like symptoms, allergic or anaphylactic reactions, injection-site reactions, worsening of cardiac symptoms (in HF patients); and for sign/symptoms of depression.

Canadian labeling: Additional monitoring recommendations (not in US labeling): Baseline pregnancy test, chest X-ray, and electrocardiogram

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events have been observed in animal reproduction studies. Spontaneous abortions were reported in 4 women during a clinical trial. Women with multiple sclerosis are generally recommended to discontinue therapy prior to conception (Lu, 2012). The Canadian labeling contraindicates use in pregnant women.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience flu-like symptoms, abdominal pain, insomnia, muscle pain, polyuria, or loss of strength and energy. Have patient report immediately to prescriber signs of infection, signs of thrombotic thrombocytopenic purpura/hemolytic uremic syndrome (bruising or bleeding; severe loss of strength and energy; dark urine or jaundice; pale skin; change in the amount of urine passed; vision changes; change in strength on one side is greater than the other, difficulty speaking or thinking, change in balance; or fever), signs of capillary leak syndrome (abnormal heartbeat; angina; shortness of breath; weight gain; vomiting blood or vomit that looks like coffee grounds; black, tarry, or bloody stools; urinary retention or change in amount of urine passed; hematuria), signs of depression (suicidal ideation, anxiety, emotional instability, or confusion), signs of bleeding (vomiting blood or vomit that looks like coffee grounds; coughing up blood; blood in the urine, black, red, or tarry stools; bleeding from the gums; abnormal vaginal bleeding; bruises without a reason or that get bigger; or any severe bleeding or persistent bleeding), signs of liver problems (dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or jaundice), signs of kidney problems (urinary retention, hematuria, change in amount of urine passed, or weight gain), signs of lupus (rash on the cheeks or other body parts, sunburn easy, muscle or joint pain, angina or shortness of breath, or swelling in the arms or legs), skin discoloration, signs of heart problems (cough or shortness of breath that is new or worse, swelling of the ankles or legs, abnormal heartbeat, weight gain of more than five pounds in 24 hours, dizziness, or passing out), severe injection site reaction, severe injection site irritation, edema, change in balance, seizures, severe headache, discoloration of hands or feet, numbness, pain, tingling, or cold feeling of hands or feet, or sores or wounds on fingers or toes (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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