pirfenidone (Esbriet)

Pirfenidone (Esbriet) is a prescription medicine used to prevent and improve lung function in idiopathic pulmonary fibrosis, a type of serious lung disease in which the lung progressively develops scar tissue.

The mechanism of action of pirfenidone is not understood. Scientists believe that pirfenidone prevents lung damage by inhibiting the production of tissue-destructive chemicals such as reactive oxygen species, inflammatory chemicals like tumor necrosis factor-alpha (TNF-alpha), and pro-inflammatory growth factor-beta (TGF-beta).

In clinical studies pirfenidone was better than placebo in improving lung function; however, it did not improve survival in people with idiopathic pulmonary fibrosis. Pirfenidone was approved by tche FDA in October, 2014.

What brand names are available for pirfenidone (Esbriet)?

Esbriet

Is pirfenidone esbriet available as a generic drug?

No

Do I need a prescription for pirfenidone (Esbriet)?

Yes

Common side effects of pirfenidone include:

• rash,
• headache,
• upper respiratory infections,
• diarrhea,
• nausea,
• vomiting,
• indigestion,
• heartburn, and
• stomach pain.

Pirfenidone may cause liver problems and sensitivity to sunlight.

Liver tests are required before starting treatment with pirfenidone because of the potential for liver damage.

The recommended dose of pirfenidone in patients with idiopathic pulmonary fibrosis is 801 mg (three 276 mg capsules) three times a day with food for a total daily dose of 2,403 mg. Patients should take pirfenidone with food to help decrease nausea and dizziness. Pirfenidone may make the skin more sensitive to the sun, light from sunlamps, and tanning beds. To avoid serious sunburns or related injury, patients are advised to use sunscreen (SPF 50) and wear protective clothing.

When starting treatment, patients are started at a low dose followed by gradual increase to the recommended daily dose. The recommended initiation of treatment with pirfenidone is 1 capsule three times a day with food on days 1-7, then 2 capsules by mouth three times a day with food on days 8-14, then 3 capsules by mouth three times a day with food thereafter.

Patients restarting treatment after taking a break of 14 days or more should re-initiate treatment by following the recommended regimen.

The dose of pirfenidone may need to be lowered or treatment may need to be temporarily or permanently stopped if abnormally high levels of liver enzymes or bilirubin occur. Significant increases in liver enzymes or bilirubin may indicate serious liver damage. Patients experiencing unexplained symptoms including jaundice (yellowing of the skin or the white part of the eyes), dark or brown colored urine, pain on the upper right side the stomach, bleeding more easily than normal, or feeling unusually tired should contact their doctor right away as these may be signs and symptoms of serious liver damage.

Pirfenidone should be used cautiously in patients with mild (Child-Pugh Class A) to moderate (Child-Pugh Class B) liver disease. Use of pirfenidone should be avoided in patients with severe liver disease (Child-Pugh Class C).

Smoking may decrease blood levels of pirfenidone. Since reduced blood levels of pirfenidone may decrease the effectiveness of treatment, smoking should be avoided when using pirfenidone.

The safety and effectiveness of pirfenidone has not been established in pediatric patients.

Pirfenidone is extensively metabolized or broken down by the CYP1A2 type liver enzymes.

Administration of pirfenidone with strong CYP1A2 enzyme inhibitors is not recommended because they may cause significant increases in blood levels of pirfenidone. If pirfenidone must be taken with strong CYP1A2 inhibitors such as fluvoxamine (Luvox) or enoxacin (Penetrex), doses of pirfenidone should be reduced to one capsule three times daily. The dose should be reduced to two capsules three times daily if used with ciprofloxacin (Cipro) 750 mg, a moderate CYP1A2 inhibitor.

Similarly, use of pirfenidone should be avoided with strong CYP1A2 inducers. Strong CYP1A2 inducers may decrease blood levels of pirfenidone and consequently decrease the effectiveness of treatment.

Pirfenidone is classified as FDA pregnancy risk category C, a designation which indicates harm is shown in animal studies, but no adequate studies in pregnant women exist. Due to the lack of conclusive safety data, pirfenidone should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus.

It is not known if pirfenidone is excreted in human milk. As many drugs can enter breast milk and have the potential of causing harm to the nursing infant, pirfenidone should be used cautiously in nursing mothers.

What preparations of pirfenidone (Esbriet) are available?

Oral capsules: 267 mg.

How should I keep pirfenidone (Esbriet) stored?

Capsules should be stored at room temperature, between 15 C to 30 C (59 F to 86 F).