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 ImpairmentNo studies have been conducted.
ElderlyNo differences were observed based on age.
GenderNo dosage adjustment is needed based on gender.
RaceNo 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.
Standard considerations.
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 vaccinesDo not coadminister live vaccines.
TNF antagonistsRisk 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%).
Category B .
Undetermined.
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.