General

Pronunciation:
go-li-mu-mab

Trade Name(s)

• Simponi
• Simponi Aria
• Simponi IV 

Ther. Class.

antirheumatics

Pharm. Class.

dmards

monoclonal antibodies

anti tnf agents

Indications

• Simponi and Simponi Aria:

  Treatment of the following conditions:

  • Moderately to severely active rheumatoid arthritis (in combination with methotrexate),
  • Active psoriatic arthritis,
  • Active ankylosing spondylitis.
• Simponi: Moderately to severely active ulcerative colitis in patients who have demonstrated corticosteroid dependence or have responded inadequately to immunosuppressants such as aminosalicylates, corticosteroids, azathioprine, or 6–mercaptopurine.
• Simponi Aria: Active polyarticular juvenile idiopathic arthritis.

Action

Inhibits binding of TNFα to receptors inhibiting activity and resulting in anti-inflammatory and antiproliferative activity.

Therapeutic Effect(s):

• Decreased pain and swelling with decreased joint destruction in patients with rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, and polyarticular juvenile idiopathic arthritis.
• Induction and maintenance of clinical remission of ulcerative colitis.

Pharmacokinetics

Absorption: Well absorbed following SUBQ administration. IV administration results in complete bioavailability.

Distribution: Distributed primarily in the circulatory system with limited extravascular distribution.

Metabolism and Excretion: Unknown.

Half-life: 2 wk.

TIME/ACTION PROFILE (improvement)

Contraindication/Precautions

Contraindicated in:

• Active infection (including localized);
• Concurrent use of abatacept or anakinra (↑ risk of infections).

Use Cautiously in:

• History of chronic or recurrent infection or underlying illness/treatment predisposing to infection;
• History of exposure to tuberculosis;
• History of opportunistic infection;
• Patients residing, or who have resided, where tuberculosis, histoplasmosis, coccidioidomycoses, or blastomycosis is endemic;
• History of HF (may worsen);
• Pre-existing CNS demyelinating disorders (including multiple sclerosis or Guillain-Barré syndrome);
• History of cytopenias (may worsen);
• History of psoriasis (may exacerbate);
• Hepatitis B virus carriers (risk of reactivation);
• OB:  Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
• Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
• Pedi:  Safety and effectiveness not established in children <18 yr (rheumatoid arthritis, ankylosing spondylitis, or ulcerative colitis) or <2 yr (psoriatic arthritis or polyarticular juvenile idiopathic arthritis); ↑ risk of lymphoma (including HSTCL), leukemia, and other malignancies in children;
• Geri:  ↑ risk of infection in older adults.

Adverse Reactions/Side Effects

CV: HF, hypertension

Derm: psoriasis

EENT: nasopharyngitis, optic neuritis

GI: ↑ liver enzymes

Hemat: agranulocytosis, aplastic anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia

Local: injection site reactions

Neuro: CENTRAL NERVOUS SYSTEM DEMYELINATING DISORDERS, Guillain-Barre syndrome, multiple sclerosis, paresthesia

Resp: upper respiratory tract infection

Misc: fever, HYPERSENSITIVITY REACTIONS (including anaphylaxis), INFECTION (including reactivation tuberculosis and other opportunistic infections due to bacterial, invasive fungal, viral, mycobacterial, and parasitic pathogens), lupus-like syndrome, MALIGNANCY (including lymphoma, HSTCL, leukemia, and skin cancer)

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

•  Abatacept,  anakinra,  corticosteroids, or  methotrexate  ↑ risk of serious infections; concurrent use with anakinra or abatacept is not recommended.
• Use of  live virus vaccines  or therapeutic infectious agents may ↑ risk of infection; avoid concurrent use.
• Concurrent use with  azathioprine  and/or  6–mercaptopurine  may ↑ risk of HSTCL.
• May normalize previously suppressed levels of CYP450 enzymes, following initiation or discontinuation of golimumab, effects of substrates of this system may be altered and should be monitored, including  warfarin,  theophylline, and  cyclosporine.

Route/Dosage

Rheumatoid Arthritis and Ankylosing Spondylitis

SUBQ (Adults): 50 mg once monthly.

IV (Adults): 2 mg/kg initially and 4 wk later, then 2 mg/kg every 8 wk.

Psoriatic Arthritis

SUBQ (Adults): 50 mg once monthly.

IV (Adults): 2 mg/kg initially and 4 wk later, then 2 mg/kg every 8 wk.

IV (Children ≥2 yr): 80 mg/m²  initially and 4 wk later, then 80 mg/m²  every 8 wk.

Ulcerative Colitis

SUBQ (Adults): 200 mg initially, then 100 mg 2 wk later, then 100 mg every 4 wk.

Polyarticular Juvenile Idiopathic Arthritis

IV (Children ≥2 yr): 80 mg/m²  initially and 4 wk later, then 80 mg/m²  every 8 wk.

Availability

Solution for SUBQ injection (prefilled syringes and autoinjectors): 50 mg/0.5 mL, 100 mg/mL

Solution for intravenous injection (Simponi Aria): 12.5 mg/mL

Assessment

• Assess for signs and symptoms of infection (fever, dyspnea, flu-like symptoms, frequent or painful urination, redness or swelling at the site of a wound) prior to, during, and after therapy. Discontinue therapy if serious or opportunistic infection or sepsis occurs. If new infection develops during therapy, assess patient and institute antimicrobial therapy. Patients who tested negative for latent tuberculosis (TB) prior to therapy may develop TB during therapy. Initiate treatment for latent TB prior to initiating therapy.
• Test for HBV prior to therapy and monitor carriers of HBV for signs of reactivation during and for several mo after therapy. If reactivation occurs, discontinue golimumab and institute antiviral therapy.
• Monitor patients with HF for new or worsening symptoms. Discontinue therapy if symptoms occur.
• Assess for exacerbations and new onset psoriasis. Discontinue therapy if these occur.
• Assess patient for latex allergy. Needle cover of syringe contains latex and should not be handled by persons sensitive to latex.
• Assess for signs and symptoms of systemic fungal infections (fever, malaise, weight loss, sweats, cough, dyspnea, pulmonary infiltrates, serious systemic illness with or without concomitant shock). Ascertain if patient lives in or has traveled to areas of endemic mycoses. Consider empiric antifungal treatment for patients at risk of histoplasmosis and other invasive fungal infections until the pathogens are identified. Consult with an infectious diseases specialist. Consider stopping golimumab until the infection has been diagnosed and adequately treated.
• Observe for signs and symptoms of anaphylaxis (rash, pruritus, laryngeal edema, wheezing). Discontinue drug and notify health care professional immediately if these problems occur. Keep epinephrine, an antihistamine, and resuscitation equipment close by in case of an anaphylactic reaction.
• Rheumatoid Arthritis: Assess pain and range of motion prior to and periodically during therapy.
• Ulcerative Colitis: Assess for signs and symptoms before, during, and after therapy.

Lab Test Considerations:

Monitor liver function tests periodically during therapy. May cause ↑ serum AST and ALT.

• Monitor CBC with differential periodically during therapy. May cause leukopenia, neutropenia, thrombocytopenia, and pancytopenia. Discontinue golimumab if symptoms of blood dyscrasias (persistent fever) occur.
• Monitor for HBV blood tests before starting, during, and for several mo after therapy is completed.

Implementation

• Administer a tuberculin skin test prior to administration of golimumab. Assess if treatment for latent tuberculosis is needed; an induration of 5 mm or greater is a positive tuberculin skin test, even for patients previously vaccinated with Bacille Calmette-Guerin (BCG). Consider antituberculosis therapy prior to therapy in patients with a history of latent or active tuberculosis if an adequate course of treatment cannot be confirmed, and for patients with risk factors for tuberculosis infection.
• Update immunizations before starting therapy following current immunization guidelines for patients receiving immunosuppressive agents.
• Initial injection should be supervised by health care professional.
• Refrigerate solution; do not freeze. Allow prefilled syringe or autoinjector to sit at room temperature for 30 min prior to injection; do not warm in any other way. Do not shake. Solution is clear to slightly opalescent and colorless to light yellow. Do not administer solutions that are discolored, cloudy, or contain particulate matter. Discard unused solution.
• SUBQ Remove the needle cover or autoinjector cap just prior to injection; both caps contain latex. Inject into front of middle thigh or lower part of abdomen 2 inches from navel. Do not inject in areas where skin is tender, bruised, red, scaly, or hard; avoid scars or stretch marks. Press a cotton ball or gauze over injection site for 10 sec; do not rub.
  • Autoinjector:  Press open end of autoinjector against skin at 90° angle. Press button with fingers or thumb; button will stay pressed and does not need to be held. Injection will begin following a loud click. Keep holding the autoinjector against skin until a 2nd loud click is heard (usually 3–6 sec, but may take up to 15 sec). Lift autoinjector from skin following 2nd click. Yellow indicator in viewing window indicates autoinjector worked correctly. If yellow does not appear in viewing window call 1-800-526-7736 for help.
  • Prefilled syringe:  Hold body of syringe between thumb and index finger. Do not pull back on plunger at any time. Pinch skin. Inject all medication by pushing plunger until plunger head is between needle guard wings. Take needle out of skin and let go of skin. Slowly take thumb off plunger to allow empty syringe to move up until entire needle is covered by needle guard.

Patient/Family Teaching

• Instruct patient on correct technique for administration. Review patient information sheet, preparation of dose, administration sites and technique, and disposal of equipment into a puncture-resistant container. Advise patient of risks and benefits of golimumab therapy. Inject missed doses as soon as remembered, then return to regular schedule. Instruct patient to read  Medication Guide before starting therapy and with each Rx refill; new information may be available.
• Caution patient not to share this medication with others, even with the same symptoms; may be harmful.
• Inform patient of increased risk of infections, malignancies, cardiac and nervous system disorders during therapy.
• Caution patient to notify health care professional promptly if any signs of infection, including TB, invasive fungal infections (fever, malaise, weight loss, sweats, cough, dyspnea, pulmonary infiltrates, serious systemic illness with or without concomitant shock), reactivation of HBV (muscle aches, clay-colored bowel movements, feeling very tired, fever, dark urine, chills, skin or eyes look yellow, stomach discomfort, little or no appetite, skin rash, vomiting), hypersensitivity reactions, or nervous system problems (vision changes, weakness in arms or legs, numbness or tingling in any part of the body) develop.
• Advise patient to examine skin periodically during therapy and notify health care professional of any changes in appearance of skin or growths on skin.
• Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
• Inform patient to avoid receiving live vaccinations; other vaccinations may be given.
• Inform patient of increased risk of cancer. Advise patient of need for screening for dysplasia (colonoscopy, skin cancer examinations, biopsy) periodically during therapy.
• Rep:  Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Advise females to notify health care professional if they recently had a baby while taking golimumab. Infants have an increased chance of getting an infection for up to 6 mo after birth; avoid administration of live vaccines to infants for 6 mo after mother's last dose.

Evaluation/Desired Outcomes

• Decreased pain and swelling with decreased rate of joint destruction in patients with rheumatoid arthritis.
• Decreased signs and symptoms, slowed progression of joint destruction, and improved physical function in patients with psoriatic arthritis.
• Reduced signs and symptoms of ankylosing spondylitis.
• Decreased symptoms, maintaining remission, and mucosal healing with decreased corticosteroid use in ulcerative colitis.