Pulfibro 801 mg Tablet 10's pack

Pulfibro 801 mg Tablet 10's pack

Indications

Pirfenidone is indicated in adults for the treatment of mild to moderate Idiopathic Pulmonary Fibrosis (IPF).

Pharmacology

Pirfenidone is an orally active, small molecule that shows a wide range of biologic activity. In vitro evidence has shown that pirfenidone inhibits collagen synthesis, down-regulates profibrotic cytokines and decreases fibroblast proliferation. Pirfenidone leads to a reduction of TGF-beta2 mRNA levels and of the mature TGF-beta2 protein due to decreased expression and direct inhibition of the TGF-beta pro-protein convertase furin. In addition, pirfenidone reduces the protein levels of the matrix metalloproteinase (MMP)-11, a TGF-beta target gene and furin substrate involved in carcinogenesis.

Dosage & Administration

Treatment with Pirfenidone should be initiated and supervised by specialist physicians experienced in the diagnosis and treatment of IPF. Upon initiating treatment, the dose should be titrated to the recommended daily dose of nine 267 mg tablets or one 801 mg tablet per day over a 14-days period for adult as follows.

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.

Side Effects

The safety of Pirfenidone has been evaluated in clinical studies including 1345 healthy volunteers and patients. The most commonly reported (10%) adverse reactions during clinical study experience with Pirfenidone at a dose of 2403 mg/day compared to placebo, respectively, were nausea (32.8% versus 13.3%), rash (28.7% versus 8.6%), fatigue (22.3% versus 13.3%), diarrhoea (21.7% versus 13.5%), dyspepsia (16.8% versus 5.5%), and photosensitivity reaction (12.2% versus 1.7%). Serious adverse reactions were recorded at similar frequencies among patients treated with 2403 mg/day of Pirfenidone and placebo in clinical studies. The adverse reactions reported at a frequency of 2% in 345 patients receiving Pirfenidone at the recommended dose of 2403 mg/day in two pivotal Phase 3 studies. Adverse reactions from post-marketing experience are also listed. Adverse reactions are listed by System Organ Class (SOC) and within each frequency grouping the adverse reactions are presented in order of decreasing seriousness.

Pregnancy & Lactation

Pregnancy: There are no data from the use of Pirfenidone in pregnant women. In animals placental transfer of pirfenidone and/or its metabolites occurs with the potential for accumulation of pirfenidone and/or its metabolites in amniotic fluid. At high doses (1000 mg/kg/day) rats exhibited prolongation of gestation and reduction in fetal viability. As a precautionary measure, it is preferable to avoid the use of Pirfenidone during pregnancy.

Lactation: It is unknown whether pirfenidone or its metabolites are excreted in human milk. Available pharmacokinetic data in animals have shown excretion of pirfenidone and/or its metabolites in milk with the potential for accumulation of pirfenidone and/or its metabolites in milk. A risk to the suckling child cannot be excluded. A decision must be made whether to discontinue breast-feeding or to discontinue from Pirfenidone therapy, taking into account the benefit of breast-feeding for the child and the benefit of Pirfenidone therapy for the mother.

Fertility: No adverse effects on fertility were observed in preclinical studies. Effects on ability to drive and use machines: No studies on the effects of the ability to drive and use machines have been performed. Pirfenidone may cause dizziness and fatigue, which could influence the ability to drive or use machines.

Overdose Effects

There is limited clinical experience with overdose. Multiple doses of pirfenidone up to a dose of 4806 mg/day were administered as six 267 mg capsules three times daily to healthy adult volunteers over a 12-day dose escalation period. Adverse reactions were mild, transient, and consistent with the most frequently reported adverse reactions for pirfenidone.