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Pirfenidone
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Prescribing Information for Pirfenidone:
Pirfenidone is a drug used in conditions of idiopathic pulmonary fibrosis. The medication was developed and is mainly produced by InterMune company. Pirfenidone is also made in Europe under the brand name Esbriet, as Pirespa in Japan, its indian analog is called Pifinex. Production of the medication in China has started in September 2011 and has been approved by State Food and Drug ADministration.
Pirfenidone was added to the list of drugs approved by European Medicines Agency and is considered the most effective medication in conditions of IPF.
Pharmacokinetics
As a result of some studies main consistent properties of Pirfenidone useful in treatment of animal models of fibrosis were proved, in particular, it stimulates the excertion of collagen and decreases generation of fibrogenic (TGF-β) and inflammatory mediators (TNF-α and IL-1β). Pirfenidone is prescribed to take orally after food as the presence of food greatly reduces the level of absorption and causes such undesired effects as nausea and giddiness. In case of proper use of the drug about 80% of the prescribed dose of Pirfenidone is excreted with the urine within twenty-four hours after intake. 60% of the substance is bound to the blood plasma proteins. Moreover the half of the dose is transformed into inactive metabolite 5-carboxypirfenidone.
Interaction with other drugs
Pirfenidone interactions are mediated by various enzymes of cytochrome (CYP) since the drug is metabolised through the enzyme pathway CYP1A2. Thus the medication inhibiting this type of enzymes are to be avoided (fluvoxamine) and some of them should be taken with special care (propafenone, amiodarone). Not the less attention requires the usage of CYP1A2 inducers (omeprazole, etc.), since the drugs of the type reduce the level of plasma circulation.
Cigarette smoking is also forbidden while taking pirfenidone since the nicotine increases the clearance of the drug through inducing the CYP1A2 enzymes thus decreasing the exposure to the medicine. The patients should be advised to restrain from smoking during the course.
Precautions and side effects
First Pirfenidone side effects include nausea, changes in appetite, increased AST, itchiness, increased light sensitivity, initial skin yellowing and upset stomach. Contact your prescriber if you notice hypersensitive or allergic reactions, the possible symptoms may include skin eruption, throat and tongue swelling, dizziness, breathing worsening, hives.
It’s strongly recommended to use the medication only as instructed by attending physician or prescriber and not to alter the recommended doses unless prescribed to do so. Patients usually have good tolerance to the drug. Usage of Pirfenidone often depends on the medical history of a certain patient, current health condition and severity of present symptoms of IPF.
Before using Pirfenidone ensure you doctor is aware that you:- don’t have any allergies to components of the drug
- are using any other drugs or medication that can inhibit Pirfenidone
- are using any supplements and vitamins
- are pregnant or breastfeeding