Tofanib XR 11mg

Description

Pharmacology

Tofacitinib is a JAK inhibitor that is partially reversible and prevents the body from responding to cytokine signals. Tofacitinib prevents STAT phosphorylation and activation by inhibiting JAK. The JAK-STAT signaling pathway regulates cell transcription in hematopoietic and immune cell functions. Tofacitinib works as an anti-inflammatory agent by inhibiting the JAK-STAT pathway. However, there is evidence that it can also have other healing effects.

Rheumatoid arthritis is an autoimmune disease characterized by pro-inflammatory cytokine dysregulation, including IL7, IL15, IL21, IL6, IFN, and IFN. (3) Through the Janus kinase signaling pathway, cytokine signaling promotes the recruitment and activation of immune cells, resulting in tissue inflammation and joint damage.

Dosage & Administration

Tofacitinib 5 mg twice daily or Tofacitinib 11 mg once daily for rheumatoid arthritis. Tofacitinib 5 mg once daily is recommended in patients with moderate to severe renal impairment or moderate hepatic impairment.

Tofacitinib 5 mg twice daily or Tofacitinib 11 mg once daily for psoriatic arthritis (in combination with nonbiologic DMARDs). Tofacitinib 5 mg once daily is recommended in patients with moderate to severe renal impairment or moderate hepatic impairment.

Tofacitinib 10 mg twice daily for at least 8 weeks, followed by 5 or 10 mg twice daily. If an adequate therapeutic benefit is not obtained after 16 weeks of 10 mg twice daily, discontinue. To maintain response, use the lowest effective dose.

Interaction

Cytochrome P450 3A4 (CYP3A4) inhibitors of high potency (e.g., Ketoconazole)
Tofacitinib 5 mg once daily is the recommended dose: One or more concurrent medications that result in both moderate CYP3A4 inhibition and potent CYP2C19 inhibition (e.g., fluconazole)
Tofacitinib 5 mg once daily is the recommended dose. Rifampin and other CYP inducers: Clinical response may be lost or reduced as a result.

Side Effects

Upper respiratory tract infections, headache, diarrhea, and nasopharyngitis were the most commonly reported adverse reactions during the first 3 months of controlled clinical trials (occurring in more than or equal to 2% of patients treated with Tofacitinib monotherapy or in combination with DMARDs).

Pregnancy & Lactation

Pregnancy category C. There are no adequate and well-controlled studies of pregnant women. Tofacitinib should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is unknown whether tofacitinib is excreted in human milk. Since many drugs are excreted in human milk, and because tofacitinib may have serious adverse reactions to nursing babies, it is necessary to decide whether to stop breastfeeding or the drug, taking into account the importance of the drug for breastfeeding.

Precautions & Warnings

• Tofacitinib should not be used during active severe infections, including local infections.
  Use with caution in patients at high risk of gastrointestinal perforation.
  Laboratory testing is advised because lymphocytes, neutrophils, hemoglobin, liver enzymes, and lipids can all change.
  Vaccine: Tofacitinib should not be used with live vaccines.
  If the absolute lymphocyte count (ALC) is less than 500 cells/mm3, the absolute neutrophil count (ANC) is less than 1000 cells/mm3, or the hemoglobin level is less than 9 g/dL.

Storage Conditions

Do not store at temperatures above 30°C. Keep out of children’s reach.