HUMIRA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for HUMIRA (HUMIRA).
Tumor necrosis factor alpha (TNF-α) inhibitor; a recombinant human IgG1 monoclonal antibody that binds to soluble and membrane-bound TNF-α, preventing its interaction with p55 and p75 TNF receptors, thereby reducing inflammation and immune activation.
| Metabolism | Degraded via proteolysis into small peptides and amino acids; no involvement of CYP450 enzymes. |
| Excretion | Adalimumab is primarily eliminated via reticuloendothelial system degradation; no significant renal or biliary excretion. <1% excreted unchanged in urine. |
| Half-life | Terminal elimination half-life is approximately 14 days (range 10–20 days) in adults, supporting a subcutaneous dosing interval of every 2 weeks. Longer half-life in older patients. |
| Protein binding | Mostly bound to albumin; approximately 90% protein-bound. |
| Volume of Distribution | Vd is approximately 5–6 L, similar to plasma volume, indicating limited extravascular distribution. Not computed per kg body weight. |
| Bioavailability | Subcutaneous: 64% (range 50–70%) relative to intravenous administration. |
| Onset of Action | Subcutaneous: Clinical improvement in rheumatoid arthritis may be observed within 1–2 weeks, with maximal effect by 12 weeks. |
| Duration of Action | Single subcutaneous dose provides therapeutic concentrations for approximately 2–4 weeks. Steady-state achieved by 12 weeks of every-other-week dosing. Duration of clinical effect extends beyond serum levels due to immunomodulation. |
Adult: 40 mg subcutaneously every other week. For ulcerative colitis: initial dose 160 mg on day 1, then 80 mg on day 15, then 40 mg every other week starting day 29.
| Dosage form | VIAL |
| Renal impairment | No specific GFR-based dose adjustments. Use caution in severe renal impairment due to limited data. |
| Liver impairment | No specific Child-Pugh based adjustments. Use caution in severe hepatic impairment. |
| Pediatric use | Juvenile idiopathic arthritis (≥2 years): weight 10-<15 kg: 20 mg subcutaneously every other week; 15-<30 kg: 30 mg every other week; ≥30 kg: 40 mg every other week. Pediatric Crohn's disease (≥6 years): weight 17-<40 kg: initial 80 mg day 1, 40 mg day 15, then 20 mg every other week; ≥40 kg: same as adult dosing. |
| Geriatric use | No specific dose adjustment, but higher incidence of infections; monitor closely. Start at lower end of dosing range if frail. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for HUMIRA (HUMIRA).
| Breastfeeding | Minimal transfer into breast milk; M/P ratio unknown. Not expected to cause harm, but caution advised due to potential immune suppression in infant. |
| Teratogenic Risk | First trimester: Limited data, no clear increase in major malformations. Second and third trimesters: Known to cross placenta; increased risk of infection in infant. Avoid live vaccines for first 6 months. |
| Fetal Monitoring |
■ FDA Black Box Warning
SERIOUS INFECTIONS: Increased risk of serious infections including tuberculosis, bacterial sepsis, invasive fungal infections (e.g., histoplasmosis, coccidioidomycosis, blastomycosis), and opportunistic infections. Discontinue if serious infection develops. Test for latent TB prior to use; treat latent TB before therapy. MALIGNANCY: Lymphoma and other malignancies, some fatal, have been reported in children and adolescents treated with TNF blockers, including HUMIRA.
| Serious Effects |
["Severe, active infections (including localized infections)","Moderate to severe heart failure (NYHA class III/IV)","Known hypersensitivity to adalimumab or any component of the formulation","Concurrent use with anakinra (increased risk of serious infections)","Concurrent use with abatacept (increased risk of serious infections)"]
| Precautions | ["Serious infections (bacterial, mycobacterial, fungal, viral, protozoal, opportunistic)","Reactivation of hepatitis B virus (HBV) - test for HBV before starting therapy; discontinue if reactivation occurs","Hypersensitivity reactions (anaphylaxis, angioedema)","Neurologic reactions (new onset or exacerbation of demyelinating disorders, including multiple sclerosis)","Hematologic reactions (pancytopenia, aplastic anemia)","Congestive heart failure (new onset or worsening)","Lupus-like syndrome","Immunosuppression (avoid live vaccines)","Malignancy risk, especially in children and adolescents"] |
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| Monitor for maternal infections. Infant: watch for infections; avoid live vaccines until 6 months after last in utero exposure. |
| Fertility Effects | No evidence of impaired fertility in human studies. Animal studies show no effects. |