PULMOFIB

200/400

COMPOSITION:

PULMOFIB 200                                                                          

Each film coated tablet contains Pirfenidone IP 200mg                                                                  

PULMOFIB 400                                                                       

Each film coated tablet contains Pirfenidone IP 400mg                                                                           

Colour: Titanium Dioxide IP            

CLINICAL PHARMACOLOGY:

Pirfenidone is an anti-inflammatory, antioxidant, and anti-fibrotic agent that may improve lung function and reduce acute exacerbations in idiopathic pulmonary fibrosis (IPF). It suppresses TGF-β1, downregulates pro-inflammatory cytokines, and inhibits inflammation and vascular permeability in animal models.

Pharmacokinetics: 

Absorption: Cmax occurs 0.5–4 hours post-dose, delayed and reduced by food (Cmax ↓49%, AUC ↓16%). Absolute bioavailability is unknown.

Distribution: Binds 58% to plasma proteins (mainly albumin) with a volume of distribution of 59–71 L.

Metabolism: Forms four metabolites; only pirfenidone and 5-carboxy-pirfenidone are significant in plasma (metabolite-to-parent ratio: 0.6–0.7).

Elimination: Half-life ~3 hours; excreted mainly as 5-carboxy-pirfenidone in urine (~80% of dose, 99.6% of recovered metabolites).

INDICATIONS AND USAGE:

Pirfenidone tablets are indicated for the treatment of idiopathic pulmonary fibrosis (IPF). 

DOSAGE AND ADMINISTRATION:

Pirfenidone is taken orally with food, starting at 600 mg/day (200 mg three times daily), gradually increasing over two weeks to a maintenance dose of 2400 mg/day (800 mg three times daily). If treatment is interrupted for 14+ days, reinitiate with dose titration; for shorter interruptions, resume the previous dose. Missed doses should not be doubled, and doses must be spaced at least 3 hours apart.

CONTRAINDICATIONS:

Hypersensitivity to the active substance or to any of the excipients, concomitant use of fluvoxamine, severe hepatic impairment or end stage liver disease, severe renal impairment (CrCl <30 ml/min) or end stage renal disease requiring dialysis. 

WARNINGS AND PRECAUTIONS: 

Warnings: Pirfenidone may cause elevated liver enzymes (ALT, AST, bilirubin), photosensitivity, rash, and gastrointestinal issues like nausea and diarrhea, requiring monitoring and possible dose adjustments.

Precautions: Sun protection is advised, and temporary dose reductions or discontinuations may be necessary for managing side effects.

ADVERSE REACTIONS:

Common: nausea, rash, abdominal pain, upper respiratory tract infection, diarrhea, fatigue, headache, dyspepsia, dizziness, vomiting, anorexia, sinusitis, insomnia, weight decrease, and arthralgia.

Rare: photosensitivity reaction, decreased appetite, pruritus, asthenia, and non-cardiac chest pain.

DRUG INTERACTIONS:

CYP1A2 inhibitors, such as fluvoxamine, increase Pirfenidone exposure and may require dose adjustments or fluvoxamine discontinuation. For strong inhibitors, reduce Pirfenidone to 267 mg three times daily. Taking Pirfenidone with food lowers the incidence of adverse reactions compared to fasting.

USE IN SPECIFIC POPULATIONS:

Pregnancy: Pirfenidone's safety in pregnant women is unknown; animal studies show potential placental transfer and accumulation. Avoid use during pregnancy as a precaution.

Nursing Mothers: It is unclear if Pirfenidone is excreted in human milk; animal studies indicate potential excretion and accumulation. Decide between discontinuing breastfeeding or Pirfenidone therapy based on benefits to mother and child.

Pediatrics Use: Safety and effectiveness in children and adolescents are unknown.

Geriatric Use: No specific information provided regarding use in the elderly

OVERDOSAGE:

Limited clinical data exist on Pirfenidone overdose; doses up to 4806 mg/day in healthy adults caused only mild, transient adverse reactions similar to its known side effects.

STORAGE: Store protected from moisture.

PRESENTATION: 

PULMOFIB* 200/ PULMOFIB* 400: Carton containing 10 blisters of 10 tablets each.