Usage
Golimumab is prescribed for the treatment of various inflammatory conditions, including:
- Rheumatoid Arthritis (RA): In combination with methotrexate, for moderately to severely active RA in adults.
- Psoriatic Arthritis (PsA): For active PsA in adults and children 2 years and older.
- Ankylosing Spondylitis (AS): For active AS in adults.
- Ulcerative Colitis (UC): For moderately to severely active UC in adults.
- Polyarticular Juvenile Idiopathic Arthritis (pJIA): For children with a body weight of at least 40kg.
Pharmacological Classification: Tumor Necrosis Factor-alpha (TNF-α) inhibitor; Disease-modifying antirheumatic drug (DMARD); Biologic.
Mechanism of Action: Golimumab is a human IgG1κ monoclonal antibody that binds with high affinity to both soluble and transmembrane TNF-α, thereby neutralizing its activity. This reduces inflammation and other symptoms associated with the aforementioned diseases.
Alternate Names
Golimumab is also known internationally by the same generic name.
Brand Names: Simponi, Simponi Aria
How It Works
Pharmacodynamics: By neutralizing TNF-α, golimumab disrupts the inflammatory cascade, leading to a reduction in inflammatory markers and improvement in clinical symptoms such as pain, swelling, and stiffness.
Pharmacokinetics:
- Absorption: Following subcutaneous administration, absorption is relatively slow, with peak serum concentrations occurring in approximately 5-7 days. Intravenous administration achieves immediate serum levels.
- Distribution: Distributes throughout the body, with moderate tissue penetration.
- Metabolism: As a monoclonal antibody, metabolism is expected to be similar to endogenous IgG, involving degradation into small peptides and amino acids.
- Elimination: Primarily eliminated through proteolytic catabolism; renal elimination plays a minor role. The half-life of golimumab is approximately 2-3 weeks.
Mode of Action: Golimumab binds specifically to TNF-α, preventing it from interacting with its receptors (TNFR1 and TNFR2) on cell surfaces. This inhibition blocks the downstream signaling pathways responsible for inflammation, cell proliferation, and joint destruction.
Receptor binding: Binds to both soluble and transmembrane TNF-α.
Elimination pathways: Primarily via proteolytic degradation; minimal renal excretion.
Dosage
Standard Dosage
Adults:
- RA, PsA, AS (Subcutaneous): 50 mg once monthly. Patients weighing >100 kg may receive 100 mg monthly.
- RA, PsA, AS (Intravenous - Simponi Aria): 2 mg/kg IV infusion over 30 minutes at weeks 0 and 4, and every 8 weeks thereafter. For patients with RA, should be given in combination with methotrexate.
- UC (Subcutaneous): 200 mg at week 0, 100 mg at week 2, followed by 100 mg every 4 weeks.
Children:
- pJIA, PsA (Intravenous - Simponi Aria): 80 mg/m² IV infusion over 30 minutes at weeks 0 and 4, and every 8 weeks thereafter.
- pJIA (Subcutaneous): 50mg once a month, on the same date each month, for children weighing at least 40 kg.
Special Cases:
- Elderly Patients: No dose adjustment is generally required, but monitor for infections.
- Patients with Renal Impairment: No specific dose adjustments are recommended, but monitor closely.
- Patients with Hepatic Dysfunction: No specific dose adjustments are recommended, but monitor closely.
- Patients with Comorbid Conditions: Exercise caution in patients with chronic infections, heart failure, or demyelinating diseases.
Clinical Use Cases
Golimumab is not typically indicated for acute medical settings such as intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Its use is primarily focused on chronic inflammatory disease management.
Dosage Adjustments
Dose adjustments may be necessary based on individual patient response and tolerability. Monitor patients for efficacy and side effects. No specific adjustments are provided for renal/hepatic impairment.
Side Effects
Common Side Effects
Upper respiratory tract infections, injection site reactions (pain, redness, swelling), viral infections, headache, and abdominal pain.
Rare but Serious Side Effects
Serious infections (e.g., tuberculosis, invasive fungal infections), malignancies (e.g., lymphoma, skin cancer), heart failure, demyelinating disorders, lupus-like syndrome, hepatitis B reactivation, and severe allergic reactions.
Long-Term Effects
Increased risk of infections and malignancies with prolonged use.
Adverse Drug Reactions (ADR)
Severe allergic reactions (anaphylaxis), drug-induced lupus, new or worsening heart failure, and reactivation of hepatitis B.
Contraindications
Active tuberculosis or other severe infections (e.g., sepsis, opportunistic infections); moderate or severe heart failure (NYHA class III/IV); known hypersensitivity to golimumab.
Drug Interactions
- Biologic DMARDs and JAK inhibitors: Avoid concomitant use.
- Live vaccines: Not recommended during treatment.
- Therapeutic infectious agents: Avoid concurrent use.
- Methotrexate: Concomitant use may increase golimumab levels, but dose adjustments are generally not required.
- CYP450 interactions: TNF-α inhibition can affect CYP450 activity.
- Consult a drug interaction checker for a comprehensive list.
Pregnancy and Breastfeeding
- Pregnancy: Golimumab crosses the placenta, especially during the third trimester, posing a potential risk of infection to the newborn. Use only if clearly needed. Live vaccines are not recommended for infants exposed to golimumab in utero for 6 months after birth.
- Breastfeeding: Golimumab is present in breast milk at low concentrations. Use with caution, especially while nursing a newborn or preterm infant. Shared decision-making with the mother regarding breastfeeding or continuing golimumab should be undertaken.
Drug Profile Summary
- Mechanism of Action: TNF-α inhibitor.
- Side Effects: Infections, injection site reactions, malignancies, heart failure, demyelinating disorders.
- Contraindications: Active serious infections, moderate to severe heart failure.
- Drug Interactions: Biologics, live vaccines, therapeutic infectious agents.
- Pregnancy & Breastfeeding: Use with caution; potential risks to fetus and infant.
- Dosage: Variable based on indication and route of administration. See dosage section for details.
- Monitoring Parameters: Signs of infection, complete blood counts, liver function tests, and monitoring for malignancies.
Popular Combinations
- Methotrexate: Commonly used with golimumab in RA, PsA, and AS to enhance efficacy.
Precautions
- General Precautions: Screen for latent tuberculosis and hepatitis B before starting treatment. Monitor closely for infections during therapy.
- Specific Populations: See Pregnancy and Breastfeeding section.
- Lifestyle Considerations: Patients should be advised on infection prevention strategies.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Golimumab?
A: The dosage varies depending on the condition and route of administration. See the detailed dosage section above.
Q2: What are the most common side effects of Golimumab?
A: Common side effects include upper respiratory infections, injection site reactions, and viral infections.
Q3: What are the serious side effects of Golimumab?
A: Serious side effects may include infections, malignancies, heart failure, and demyelinating disorders.
Q4: Can Golimumab be used during pregnancy?
A: It should be used during pregnancy only if clearly needed due to potential risks to the fetus.
Q5: Can Golimumab be used during breastfeeding?
A: It can be used with caution during breastfeeding; shared decision-making with the patient is crucial.
Q6: How does Golimumab work?
A: It works by neutralizing TNF-α, a key mediator of inflammation in several diseases.
Q7: What are the contraindications for Golimumab use?
A: Contraindications include active severe infections and moderate to severe heart failure.
Q8: Does Golimumab interact with other medications?
A: Yes, it can interact with other medications, including biologics, live vaccines, and therapeutic infectious agents.
Q9: What precautions should be taken when administering Golimumab?
A: Screen for latent tuberculosis and hepatitis B before treatment and monitor closely for infections during therapy.
Please note that this information is current as of February 16, 2025, and may change with time. Always consult the latest prescribing information and clinical guidelines for the most up-to-date recommendations.
