Tofatin 5 - Tablet Tofacitinib - 5mg 10 Tablet(s) / Box Ziska Pharmaceuticals Ltd. Introduction: Tofatin 5 is used to treat moderate to severe rheumatoid arthritis. It helps decrease pain, tenderness and swelling in the joints by reducing inflammation. It also helps slow the progression of bone and joint damage. Tofatin 5 may be prescribed by itself or in combination with another medicine. The tablets can be taken with or without food and it is best to take them at the same time each day. Your dose will depend on your condition and what other medicines you are taking. You should use it as your doctor tells you to. Do not stop taking this medicine... Uses of Tofatin 5: Rheumatoid arthritis Side effects of Tofatin 5: DiarrheaHeadacheHigh blood pressureNasal congestion (stuffy nose)Runny noseSore throatUpper respiratory tract infection How to use Tofatin 5: Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Tofatin 5 may be taken with or without food, but it is better to take it at a fixed time. How Tofatin 5 works: Tofatin 5 is an Janus kinase inhibitor. It works by blocking the action of the enzyme, Janus kinase. This decreases inflammation and joint damage in rheumatoid arthritis. Indication: Rheumatoid Arthritis, Tofacitinib is indicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to methotrexate. It may be used as monotherapy or in combination with methotrexate or other nonbiologic disease-modifying antirheumatic drugs (DMARDs). Administration: May be taken with or without food. Adult Dose: Rheumatoid Arthritis Indicated as second-line treatment for moderate-to-severe active rheumatoid arthritis in patients with an inadequate response or intolerance to methotrexate; may be used as monotherapy or in combination with methotrexate or other nonbiologic DMARDs Adult: Recommended Dose: 5 mg twice daily. Hepatic impairment Mild: No dosage adjustment required Moderate: Not to exceed 5 mg qDay Severe: Not recommended Child Dose: Safety and efficacy not established Renal Dose: Renal impairment Mild: No dosage adjustment required Moderate-to-severe: Not to exceed 5 mg qDay Contraindication: Hypersensitivity to the active substance or to any of the excipients. Mode of Action: Janus kinases (JAKs) pathways inhibitor; JAK consists of a group of intracellular tyrosine kinases that transmit signals from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoieses and immune cell function. Within the signaling pathway, JAKs phosphorylate and activate signal transducers and activators of transcription (STATs) which modulate intracellular activity including gene expression; tofacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs. These signals are essential in maintaining the inflammatory condition in rheumatoid arthritis (RA); inhibition of JAKs reduces production of and modulates proinflammatory cytokines central... Precaution: Serious Infections – Do not administer Tofacitinib during an active infection, including localized infections. If a serious infection develops, interrupt Tofacitinib until the infection is controlled. Lymphomas and other malignancies have been reported in patients treated with Tofacitinib Gastrointestinal Perforations – Use with caution in patients that may be at increased risk. Laboratory monitoring –Recommended due to potential changes in lymphocytes, neutrophils, hemoglobin, liver enzymes and lipids. Immunizations –Live vaccines should not be given concurrently with Tofacitinib Do not initiate therapy in patients w/ an active infection including localized infections, chronic or recurrent infections, or those who have been exposed... Side Effect: >10% Overall infections (20-22%) 1-10% URTI (4.5%),Headache (4.3%),Diarrhea (4%),Nasopharyngitis (3.8%),UTI (2%),Hypertension (1.6%) <1% ANC <500/mm³ (0.07%),Lymphocytes <500/mm³ (0.04%) Frequency Not Defined Serious infections: 1.7 events per 100 patient-years Malignancies: 0.3 events per 100 patient-years Pregnancy Category Note: Pregnancy There is a pregnancy exposure registry that monitors pregnancy outcomes in women during pregnancy; patients can call the toll free number 1-877-311-8972 There are no adequate and well-controlled studies therapy in pregnant women In the tofacitinib clinical development programs, birth defects and miscarriages were reported Animal data Based on animal studies, tofacitinib has the potential to affect a developing fetus Based on findings in rats, females of reproductive potential taking tofacitinib may result in reduced fertility Contraception Advise females of reproductive potential to use effective contraception during treatment and for >4 weeks after the last dose Advise females to... Interaction: Increased exposure w/ potent CYP3A4 inhibitors (eg, ketoconazole), moderate CYP3A4 inhibitors & potent CYP2C19 inhibitors (eg, fluconazole). Decreased exposure w/ potent CYP inducers (eg, rifampin). Increased AUC & decreased Cmax w/ tacrolimus & cyclosporine. Decreased AUC & Cmax of MTX.