Baricitinib

Generic Details

Generic Name

Baricitinib

Other Names

  • Olumiant

Drug Class

  • Janus Kinase (JAK) Inhibitor

Chemical Formula

C16H17N7O2S

Molecular Weight

371.42 g/mol

Mechanism of Action

  • Inhibits Janus Kinase (JAK) enzymes, specifically JAK1 and JAK2, which play a role in the signaling pathways of cytokines involved in inflammatory and immunological responses.

Indications

  • Rheumatoid arthritis
  • Moderate to severe active rheumatoid arthritis in adults who have responded inadequately to, or who are intolerant to one or more disease-modifying anti-rheumatic drugs (DMARDs)

Common Dosage Forms

  • Tablet

Typical Dosage

  • 2 mg once daily

Pediatric Dosage

  • Safety and efficacy not established in children

Geriatric Dosage

  • Dose adjustment may be required in elderly patients based on individual patient factors

Side Effects

  • Upper respiratory tract infections
  • Nausea
  • Increased cholesterol levels
  • Headache
  • Herpes zoster infection
  • Elevated liver enzymes

Contraindications

  • Hypersensitivity to baricitinib or any component of the formulation

Pregnancy Category

  • Category C - Potential risk to the fetus

Lactation Safety

  • Not recommended during breastfeeding

Drug Interactions

  • Strong CYP3A4 inhibitors may increase baricitinib concentration
  • Live vaccines should be avoided during treatment

Overdose Symptoms

  • Increased risk of infections
  • Liver enzyme abnormalities

Antidote for Overdose

  • No specific antidote, supportive treatment recommended

Storage Conditions

  • Store at room temperature (20-25°C)

Pharmacokinetics

  • Absorption: Rapidly absorbed after oral administration with peak plasma concentrations reached in approximately 1 hour
  • Distribution: Widely distributed with a volume of distribution of approximately 76 L
  • Metabolism: Primarily metabolized by CYP3A4 and to a lesser extent by CYP2C19
  • Excretion: Mainly excreted in urine (69%) and feces (24%)

Precautions

  • Risk of serious infections
  • Thrombosis risk
  • Hepatic and lipid monitoring recommended

Warnings

  • Increased risk of serious infections including tuberculosis and herpes zoster

Others

  • Close monitoring of blood counts and liver function tests recommended during treatment