pirfenidone (Rx)

Brand and Other Names:Esbriet
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 267mg

tablet

  • 267 mg
  • 801 mg
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Idiopathic Pulmonary Fibrosis

Initial dose titration

  • Take with food
  • Days 1-7: 267 mg PO TID (801 mg/day)
  • Days 8-14: 534 mg PO TID (1602 mg/day)
  • Day 15 and thereafter (maintenance): 801 mg PO TID; not to exceed 2403 mg/day

Dosing Considerations

Conduct liver function tests before initiating therapy (also see Dosage Modifications and Cautions)

Dosage Modifications

If patients experience significant adverse reactions (ie, gastrointestinal, photosensitivity reaction, rash), consider temporary dosage reductions or therapy interruptions of pirfenidone to allow for resolution of symptoms; discontinue if symptoms persist despite these interventions

CYP1A2 inhibitors

  • Strong inhibitors (eg, fluvoxamine, enoxacin): Reduce maintenance dose to 267 mg (1 capsule) TID
  • Moderate inhibitors (eg, ciprofloxacin): Reduce maintenance dose to 534 mg (2 capsules) TID (with ciprofloxacin 750 mg BID)

Elevated liver enzymes

  • AST/ALT >3 to ≤5 x ULN (without symptoms): Discontinue confounding medications, exclude other causes, repeat liver function tests as needed; the full daily dosage may be maintained, if clinically appropriate, or reduced or interrupted (eg, until liver chemistry tests are within normal limits), with subsequent retitration to the full dosage as tolerated
  • AST/ALT >5 x ULN or >3 times ULN with signs/symptoms of severe liver damage: Permanently discontinue; do not rechallenge

Hepatic impairment

  • Mild-to-moderate (Child Pugh A or B): Use caution; monitor and consider dosage modification or discontinuation as needed
  • Severe (Child Pugh C): Not recommended (not studied)

Renal impairment

  • Mild, moderate, or severe: Use caution; monitor and consider dosage modification or discontinuation as needed
  • ESRD requiring dialysis: No recommended (not studied)

Safety and efficacy not established

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Interactions

Interaction Checker

and pirfenidone

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            Adverse Effects

            >10%

            Nausea (36%)

            Rash (30%)

            Upper respiratory tract infection (27%)

            Diarrhea (26%)

            Abdominal pain (24%)

            Headache (22%)

            Dyspepsia (19%)

            Dizziness (18%)

            Vomiting (13%)

            GERD (11%)

            Sinusitis (11%)

            1-10%

            Insomnia (10%)

            Weight decreased (10%)

            Arthralgia (10%)

            Photosensitivity (9%)

            Decreased appetite (8%)

            Pruritus (8%)

            Asthenia (6%)

            Dysgeusia (6%)

            Noncardiac chest pain (5%)

            AST/ALT ≥3 x ULN (3.7%)

            <1%

            AST/ALT ≥10 x ULN (0.3%)

            Postmarketing Reports

            Blood and lymphatic system disorders: Agranulocytosis

            Immune system disorders: Angioedema

            Hepatobiliary disorders: Bilirubin increased in combination with increases of ALT and AST

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            Warnings

            Contraindications

            None

            Cautions

            Conduct liver function tests (ALT, AST, and bilirubin) before initiating, monthly for 6 months, and then q3months thereafter and,as clinically indicated; dosage modifications, interruption, or discontinuation may be necessary for liver enzyme elevation (see Dosage Modifications)

            Photosensitivity and rash reported; avoid exposure to sunlight and sunlamps and wear protective clothing daily; temporary dosage reductions or discontinuations may be required

            Nausea, vomiting, diarrhea, dyspepsia, gastroesophageal reflux disease, and abdominal pain reported; temporary dosage reductions or discontinuations may be required

            Pirfenidone is a CYP1A2 substrate; discontinue moderate or strong CYP1A inhibitors before initiating pirfenidone and avoid use during therapy; if unable to avoid, pirfenidone dose reduction required

            Discontinue strong CYP1A2 inducers before initiating pirfenidone and avoid use during therapy; likely to decrease exposure and lead to loss of pirfenidone efficacy

            Smoking associated with decreased systemic exposure; encourage patient to quit smoking

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            Pregnancy & Lactation

            Pregnancy: Data in pregnant women are insufficient to inform on drug associated risks for major birth defects and miscarriage

            Lactation: No information is available on presence of pirfenidone in human milk, effects of drug on breastfed infant, or effects of drug on milk production; lack of clinical data during lactation precludes clear determination of risk of pirfenidone to infant during lactation; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and potential adverse effects on breastfed child from pirfenidone or from underlying maternal condition

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Precise mechanism by which pirfenidone may work in pulmonary fibrosis has not been established

            Inhibits transforming growth factor (TGF)-beta, a chemical mediator that controls many cell functions including proliferation and differentiation

            Also inhibits the synthesis of TNF-alpha, a cytokine that is known to have an active role in inflammation

            Absorption

            Peak plasma time: 0.5-4 hr

            Food decreased the rate and extent of absorption; Cmax and AUC decreased by ~49% and 16% with food, respectively

            A reduced incidence of adverse reactions was observed in the fed group when compared with the fasted group; administered with food in clinical trials

            Distribution

            Protein bound: 58%

            Vd: 59-71 L

            Metabolism

            Metabolized in the liver by CYP1A2 to inactive metabolites

            Elimination

            Half-life: 3 hr

            Majority of dose excreted as 5-carboxy-pirfenidone metabolite (99.6%)

            Excretion: 80% urine

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            Administration

            Oral Administration

            Take with food

            Take doses at same time each day

            Missed doses

            • If ≥14 days: Reinitiate treatment by undergoing the initial 2-week titration regimen up to the full maintenance dosage
            • If <14 days: Resume the dosage prior to the interruption
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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.