Golimumab

Trade Names:Simponi- Injection, solution 50 mg per 0.5 mL

Pharmacology

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.

Pharmacokinetics

Absorption

Following subcutaneous injection, T _max ranges from 2 to 6 days. C _max is approximately 2.5 mcg/mL. Absolute bioavailability is approximately 53%.

Distribution

Distributed primarily in the circulatory system with limited extravascular distribution.

Elimination

Mean terminal half-life is approximately 2 wk.

Special Populations

No studies have been conducted.

No studies have been conducted.

No differences were observed based on age.

No dosage adjustment is needed based on gender.

No differences in pharmacokinetics have been observed based on race.

Indications and Usage

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.

Contraindications

Standard considerations.

Dosage and Administration

Subcutaneous 50 mg once per month.

General Advice

• Prior to injection, allow the prefilled syringe or auto-injector to sit at room temperature for 30 minutes.
• Discard any leftover product remaining in the prefilled syringe or prefilled auto-injector.
• Do not inject into areas where the skin is tender, bruised, red, or hard.
• Injection sites should be rotated.
• Do not shake.

Storage/Stability

Store refrigerated at 36° to 46°F. Do not freeze. Protect from light. Do not shake.

Drug Interactions

Do not coadminister with golimumab.

Monitor the response and drug concentrations of CYP substrates with a narrow therapeutic index when starting or stopping golimumab.

Do not coadminister live vaccines.

Risk of infection may be increased; do not coadminister.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Dizziness (2%); paresthesia, pyrexia (1%).

EENT

Nasopharyngitis (6%); pharyngitis, rhinitis (1%).

Lab Tests

Increased ALT (4%); increased AST (3%).

Local

Injection-site reactions (6%); injection-site erythema (3%).

Respiratory

Upper respiratory tract infection (7%); bronchitis, sinusitis (2%).

Miscellaneous

Golimumab antibodies (4%); hypertension (3%); influenza (2%); oral herpes (1%).

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

No overall differences in safety or efficacy have been observed in patients 65 yr of age and older compared with younger subjects.

CHF

Worsening of CHF and new-onset CHF have been reported with TNF-blockers.

Demyelinating disorders

Use of TNF-blockers has been associated with new onset or exacerbation of CNS demyelinating disorders (eg, multiple sclerosis).

Hematologic events

Pancytopenia, leukopenia, neutropenia, aplastic anemia, and thrombocytopenia have been reported with TNF-blockers during postmarketing experience.

Hepatitis B reactivation

Reactivation of hepatitis B virus has been reported in patients who are chronic hepatitis B carriers.

Latex

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.

Malignancies

Lymphomas have occurred.

Vaccinations

Patients may receive vaccinations, except for live vaccines.

Overdosage

Symptoms

There were no overdoses in clinical studies.

Patient Information

• Instruct patients to notify their health care provider if they develop any symptoms of infection.
• Advise patients sensitive to latex that the needle cover on the prefilled syringe and the prefilled auto-injector contain natural rubber, a derivative of latex.

Copyright © 2009 Wolters Kluwer Health.