Nurses Compass
Drug Guide
Tofacitinib Citrate
Classification
Therapeutic: Immunosuppressant, Disease-modifying Antirheumatic Drug (DMARD)
Pharmacological: Janus kinase (JAK) inhibitor
FDA Approved Indications
- Moderate to severe rheumatoid arthritis in adults
- Active psoriatic arthritis in adults
- Ulcerative colitis in adults
Mechanism of Action
Tofacitinib inhibits Janus kinase enzymes (primarily JAK1 and JAK3), which are involved in the inflammatory process by interfering with the JAK-STAT signaling pathway, leading to reduced cytokine activity and immune response.
Dosage and Administration
Adult: Typically 5 mg twice daily; dosage may be adjusted based on response and tolerability.
Pediatric: Not approved for pediatric use.
Geriatric: Use with caution; adjust dose based on renal and hepatic function.
Renal Impairment: Adjustment may be needed; consult specific guidance.
Hepatic Impairment: Use caution; dose adjustment may be necessary, especially in severe impairment.
Pharmacokinetics
Absorption: Rapidly absorbed with peak concentrations within 0.5 to 1 hour.
Distribution: Vd approximately 87 L; approximately 40% bound to plasma proteins.
Metabolism: Primarily metabolized by hepatic CYP3A4 and to a lesser extent by CYP2C19.
Excretion: Excreted primarily in feces (~70%) and urine (~30%).
Half Life: Approximately 3 hours.
Contraindications
- Active infections including tuberculosis
- Known hypersensitivity to tofacitinib or components.
Precautions
- Screen for latent TB before initiation; monitor for infections during therapy.
- Use caution in patients with hepatic impairment, blood dyscrasias, or recent live vaccines.
- Risk of thrombosis; use cautiously in patients with risk factors for blood clots.
Adverse Reactions - Common
- Upper respiratory infections (Frequent)
- Nasopharyngitis (Frequent)
- Increased cholesterol levels (Less frequent)
Adverse Reactions - Serious
- Serious infections (e.g., bacterial, viral, fungal) (Less frequent)
- Blood clots (thrombosis) (Rare)
- Gastrointestinal perforation (Rare)
- Liver enzyme elevations (Less frequent)
Drug-Drug Interactions
- May decrease effectiveness of vaccines; avoid live vaccines during treatment.
- CYP3A4 inhibitors (e.g., ketoconazole) may increase tofacitinib levels; dose adjustment needed.
Drug-Food Interactions
- No significant interactions established.
Drug-Herb Interactions
- Limited data; use caution with herbal supplements that affect immune function or CYP enzymes.
Nursing Implications
Assessment: Monitor for signs of infection, blood counts, liver function, lipid profile, and blood clots.
Diagnoses:
- Impaired immune response related to immunosuppressive therapy.
- Risk for infection.
Implementation: Educate patient on signs of infection, importance of regular blood tests, and avoiding live vaccines.
Evaluation: Assess efficacy in symptom control and monitor for adverse effects.
Patient/Family Teaching
- Report signs of infection immediately.
- Adhere to scheduled lab tests.
- Inform about potential side effects, including increased infection risk and lipid changes.
Special Considerations
Black Box Warnings:
- Serious infections, including tuberculosis and invasive fungal infections; Malignancy and thrombosis risk.
Genetic Factors: No specific genetic testing required.
Lab Test Interference: May alter lipid profiles, blood counts, liver enzymes, and infection markers.
Overdose Management
Signs/Symptoms: Nausea, vomiting, diarrhea, dizziness, increased risk of infection.
Treatment: Supportive care; no specific antidote. Consider activated charcoal if ingestion is recent; monitor and provide symptomatic treatment.
Storage and Handling
Storage: Store at room temperature, 20–25°C (68–77°F); protect from moisture.
Stability: Stable under recommended storage conditions for the duration of the labeled shelf life.