ACTINIB
TOFACITINIB · by SEARLE
Composition
Tab 5mg: Tofacitinib Citrate 5 mg
Indications & Dosage
Moderate to severe rheumatoid arthritis, Psoriatic arthritis (specialist use only): Adult: 5 mg twice daily, alternatively, 11 mg modified-release tab once daily. Moderate to severe ulcerative colitis (specialist use only): Adult: Initially 10 mg twice daily for 8 wks, repeat for another 8 wks if adequate response is not achieved, maintenance dose 5 mg twice daily. discontinue treatment if no response after 16 wks.
Contraindications
Absolute lymphocyte count less than 750 cells/mm3, absolute neutrophil count less than 1000 cells/mm3, active infection, active tuberculosis, haemoglobin less than 9 g/dL, risk factors for venous thromboembolism, severe hepatic impairment.
Precautions
Previous or current malignancy, raised serum transaminases, elderly (over65years), recurrent infection or history of serious infection, risk factors for venous thromboembolism, risk of diverticulitis, risk of gastrointestinal perforation, risk of viral reactivation, tuberculosis exposure. Vaccinate before treatment if required; live vaccines should be given at least 2-4 wks, before treatment initiation. Anti-tuberculosis therapy to be given prior to initiation of tofacitinib in patients with a history of latent or active tuberculosis or in patients at risk of tuberculosis infection. Use effective contraception during and for at least 4 weeks after treatment in women of child-bearing potential. Reduce dose in moderate hepatic impairment. Reduce dose in severe renal impairment. Evaluate for tuberculosis and viral hepatitis before treatment. Monitor for symptomsof infection during and after treatment. Periodic examination in patients at risk for skin cancer. Monitor liver function; monitor lipid profile 8 weeks after treatment initiation. Monitor lymphocytes at baseline and every 3 months thereafter; neutrophils and haemoglobin should be monitored at baseline, after 4 to 8 weeks of treatment and every 3 months thereafter.
Interactions
CYP3A4 inhibitors, CYP2C19 inhibitor, BCG, Natalizumab, Tacrolimus, Leflunomide, Pimecrolimus, Roflumilast, Denosumab, Dasatinib, Ivacaftor, Sitaxsentan, Mifepristone, Fluconazole.
Pregnancy
Avoid
Lactation
Avoid
Side Effects
Anaemia, headache, abdominal pain, diarrhoea, nausea, dyspepsia, fatigue, fever, GI disorders, hypertension, infection, influenza, joint disorders, peripheral oedema, pharyngitis, sinusitis, skin reactions, vomiting, decreased leucocytes, deep vein thrombosis (discontinue permanently), dehydration, dyslipidaemia, dyspnoea, hepatic steatosis, insomnia, ligament sprain, muscle strain, musculoskeletal pain, myocardial infarction, neoplasms, neutropenia, paraesthesia, pulmonary embolism (discontinue permanently), sinus congestion, tendinitis, venous thromboembolism (discontinue permanently), viral infection, weight increased, ulcerative colitis aggravated. Rare: Meningitis cryptococcal, sepsis, angioedema, BK virus infection, interstitial lung disease, malignancy.