Trade Names:Simponi- Injection, solution 50 mg per 0.5 mL
Binds to both soluble and transmembrane bioactive forms of human tumor necrosis factor–alpha (TNF-alpha), preventing the binding of TNF-alpha to its receptors, thereby inhibiting the biological activity of TNF-alpha.
Following subcutaneous injection, T max ranges from 2 to 6 days. C max is approximately 2.5 mcg/mL. Absolute bioavailability is approximately 53%.
Distributed primarily in the circulatory system with limited extravascular distribution.
Mean terminal half-life is approximately 2 wk.
No studies have been conducted.Hepatic Function Impairment
No studies have been conducted.Elderly
No differences were observed based on age.Gender
No dosage adjustment is needed based on gender.Race
No differences in pharmacokinetics have been observed based on race.
Treatment of moderate to severe active rheumatoid arthritis in combination with methotrexate; treatment of active psoriatic arthritis as monotherapy or in combination with methotrexate; treatment of active ankylosing spondylitis.
Subcutaneous 50 mg once per month.
Store refrigerated at 36° to 46°F. Do not freeze. Protect from light. Do not shake.
Do not coadminister with golimumab.CYP substrates with a narrow therapeutic index (eg, cyclosporine, theophylline, warfarin)
Monitor the response and drug concentrations of CYP substrates with a narrow therapeutic index when starting or stopping golimumab.Live vaccines
Do not coadminister live vaccines.TNF antagonists
Risk of infection may be increased; do not coadminister.
None well documented.
Dizziness (2%); paresthesia, pyrexia (1%).
Nasopharyngitis (6%); pharyngitis, rhinitis (1%).
Increased ALT (4%); increased AST (3%).
Injection-site reactions (6%); injection-site erythema (3%).
Upper respiratory tract infection (7%); bronchitis, sinusitis (2%).
Golimumab antibodies (4%); hypertension (3%); influenza (2%); oral herpes (1%).
Patients treated with golimumab are at increased risk for developing serious infections that may lead to hospitalization or death. These patients are frequently taking concomitant immunosuppressants (eg, corticosteroids, methotrexate). Infections include active tuberculosis (TB), invasive fungal infections, or bacterial, viral, or other infections caused by opportunistic pathogens. Discontinue treatment in patients who develop serious infection or sepsis.
Closely monitor for development of signs or symptoms of infection during and after treatment, including possible development of TB in patients who tested negative for latent TB infection prior to initiating therapy. Closely monitor patients who are carriers of hepatitis B virus for signs of active hepatitis B virus infection throughout therapy and for several months after completion of therapy. Closely monitor patients with CHF and discontinue treatment if new or worsening symptoms of CHF appear.
Category B .
Safety and efficacy not established.
No overall differences in safety or efficacy have been observed in patients 65 yr of age and older compared with younger subjects.
Worsening of CHF and new-onset CHF have been reported with TNF-blockers.
Use of TNF-blockers has been associated with new onset or exacerbation of CNS demyelinating disorders (eg, multiple sclerosis).
Pancytopenia, leukopenia, neutropenia, aplastic anemia, and thrombocytopenia have been reported with TNF-blockers during postmarketing experience.
Reactivation of hepatitis B virus has been reported in patients who are chronic hepatitis B carriers.
Needle cover on the prefilled syringe and the prefilled syringe on the auto-injector contain natural rubber, a derivative of latex, which should not be handled by persons sensitive to latex.
Lymphomas have occurred.
Patients may receive vaccinations, except for live vaccines.
There were no overdoses in clinical studies.
Copyright © 2009 Wolters Kluwer Health.