OLUMIANT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for OLUMIANT (OLUMIANT).
Janus kinase (JAK) inhibitor; selectively inhibits JAK1 and JAK2, modulating cytokine signaling involved in inflammation.
| Metabolism | Primarily metabolized by CYP3A4, with minor contributions from CYP2C19 and CYP2D6. |
| Excretion | Approximately 70% excreted renally as unchanged drug, with about 20% as inactive metabolites; fecal excretion accounts for <10%. |
| Half-life | Terminal half-life is approximately 12.5 hours in healthy subjects, supporting once-daily dosing. |
| Protein binding | ~52% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 0.4 L/kg, indicating distribution mainly in extracellular fluid. |
| Bioavailability | Oral bioavailability is approximately 76% under fasting conditions; no significant food effect. |
| Onset of Action | Clinical improvement (e.g., reduction in joint pain/swelling) may be observed as early as 1 week after starting oral therapy; maximal effect typically by 12 weeks. |
| Duration of Action | Pharmacodynamic effects (e.g., JAK-STAT inhibition) persist over the 24-hour dosing interval; clinical effects wane if doses are missed; steady state achieved by ~3 days. |
| Action Class | Janus kinase inhibitors |
2 mg orally once daily; may increase to 4 mg once daily based on clinical response.
| Dosage form | TABLET |
| Renal impairment | eGFR 30-60 mL/min/1.73m2: 2 mg once daily. eGFR 15-29 mL/min/1.73m2: 2 mg every other day. eGFR <15 mL/min/1.73m2 or on dialysis: not recommended. |
| Liver impairment | Child-Pugh Class A: 2 mg once daily. Child-Pugh Class B: 2 mg once daily (use with caution). Child-Pugh Class C: not recommended. |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No specific dose adjustment required; monitor for adverse effects given higher risk of infections and malignancies. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for OLUMIANT (OLUMIANT).
| Breastfeeding | Baricitinib is excreted in rat milk; human data absent. M/P ratio unknown. Due to potential for serious adverse reactions in nursing infants, breastfeeding is not recommended during therapy and for 4 weeks after last dose. |
| Teratogenic Risk | In animal studies, baricitinib was embryotoxic and teratogenic at exposures higher than human therapeutic doses. In pregnant women, inadequate data. Use is not recommended during pregnancy. First trimester: potential for structural anomalies; second and third trimesters: risk of low fetal weight and possibly impaired immune development. |
■ FDA Black Box Warning
Increased risk of serious infections, including tuberculosis (TB), invasive fungal infections, bacterial, viral, and other opportunistic pathogens. Malignancies including lymphoma and other solid tumors have been observed. Thrombosis, including deep vein thrombosis (DVT) and pulmonary embolism (PE), has occurred. Increased all-cause mortality, especially in rheumatoid arthritis patients >50 years with at least one cardiovascular risk factor. Major adverse cardiovascular events (MACE) such as cardiovascular death, myocardial infarction, and stroke were observed.
| Serious Effects |
["Hypersensitivity to baricitinib or any excipient.","Use with other JAK inhibitors, biologic DMARDs, or potent immunosuppressants (e.g., azathioprine, cyclosporine).","Severe hepatic impairment (Child-Pugh Class C).","Pregnancy (limited data; potential fetal harm)."]
| Precautions | ["Serious infections: monitor for signs/symptoms; discontinue if infection develops.","Thrombosis: use with caution in patients with risk factors; discontinue if symptoms occur.","Malignancy: periodic skin exams; avoid in patients with known malignancy unless treated.","Cardiovascular risk: increased MACE and mortality; avoid in patients >50 with at least one CV risk factor.","Gastrointestinal perforations: monitor for symptoms.","Laboratory abnormalities: monitor neutrophils, lymphocytes, hemoglobin, liver enzymes, and lipids.","Vaccinations: update immunizations before therapy; avoid live vaccines during treatment.","Hypersensitivity: angioedema and urticaria reported; discontinue if serious reaction occurs."] |
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| Fetal Monitoring |
| Monitor for maternal infections, hematologic parameters (CBC with differential), liver function tests, and lipid profile. In case of accidental pregnancy exposure, perform fetal ultrasound to assess for anomalies and monitor growth. |
| Fertility Effects | In animal studies, no adverse effects on male or female fertility were observed. Human data are insufficient. Baricitinib may impair fertility in females due to hormonal effects; consider impact on ovulation and menstruation. |