Trade name : Pirfenex
Active ingredient : Pirfenidone
Strength availability : 200mg
Manufactured by : Cipla Ltd
Dosage Form : film coated tablet
Category : anti inflammatory and anti fibrotic activity for MORE INFORMATION !!!
Tablet Pirfenex is an effective drug, but it causes some life threatening conditions. It causes an abnormal chromosomal structure, patient who are getting Tablet Pirfenex; exposing to light in genotoxicity tests. Patient must have knowledge about the potential of the drug Pirfenex which causes carcinogenesis in skin on exposed to light. Tablet Pirfenex should be prescribed under the supervision of medical practitioner who is familiar with the idiopathic pulmonary fibrosis therapy. Tablet Pirfenex is anti fibrotic agent involved in the treatment of idiopathic pulmonary fibrosis (lung disease).
Tablet Pirfenex is primarily used in the condition of Idiopathic Pulmonary Fibrosis (IPF).
Pirfenex, the mechanism of action of the drug is not completely established. Tablet Pirfenex is an effective anti-fibrotic and anti inflammatory agent. Anti fibrotic activity of Pirfenex is mainly taken into consideration. Pirfenex, number of cell based therapy takes place. It leads to reduce fibroblast proliferation, prohibits TGF-β accelerated collagen production, and decrease the synthesis of fibrogenic mediators like TGF-β (transforming growth factor). Pirfenex has activity to reduce production of inflammatory mediators like TNF-α (tumor necrosis factor) and IL-1β (interleukin 1 beta).
The absorption of drug Pirfenidone is varying among the condition of the patient. In healthy persons, absorption occurs within 20-60mins. If tablet Pirfenex taken with food somewhat decrease the absorption. But in older adults, tablet Pirfenex is co administered with food leads to increase tolerability.
Tablet Pirfenex binds to plasma proteins, majorly with serum albumin. Within 1-3 hours of administration, protein binding was 54-62%.
Drug Pirfenidone is metabolized by liver. Approximately 48% of drug is metabolized via CYP1A2 with other CYP isoenzymes. The major metabolite is 5-carboxy-pirfenidone.
The elimination half life is around 2.4 hours. About 80% of the metabolites cleared in urine within 24 hours. Tablet Pirfenex after administration, excreted as major metabolite 5-carboxy-pirfenidone (95%), with less than 1% of drug Pirfenidone excreted consistent as well in the urine. Plasma concentration of the tablet Pirfenex (with or without meals), because of food C¬¬max and AUC decreased, Tmax is significantly delayed.
The recommended dose of tablet Pirfenex in adolescent is 200mg for three times a day (TID), 600mg/day.
Depending upon the severity of the condition (IPF), dosage may adjust up to 1800mg/day.
Dosage of the tablet Pirfenex depending up on symptom.
Initially patient starts with 200mg TID, after 2 weeks, dose may gradually increase to 600mg at a time (1800mg/day).
Dose adjustment and other consideration for safe use :
Gastro intestinal events :
Patient, during therapy with tablet Pirfenex may affected by gastrointestinal side effects, so patient advice by taking tablet Pirfenex with food. If a symptom endures means, dose may reduce to 1-2 tablets given for 2-3 times a day with food. Photo sensitive reactions: If rashes sustains for 7 days, tablet Pirfenex should be discontinued for 14 days. It is continued by the guidance of health care providers.
WARNING & SAFETY MEASURES
Pirfenex tablets should be taken with caution; In the conditions like; While patient taking tablet Pirfenex, they may leads to, Elevation of liver enzymes Photosensitivity and rash Gastro intestinal disorder Consumption of grapefruit juice: leads to inhibit CYP1A2. It should be avoided during the treatment.
Tablet Pirfenex has some of drug interactions, which is propitiating by cytochrome enzymes :
CYP1A2 inhibitors :
Tablet Pirfenex is metabolized through the CYP1A2 enzyme pathway. The various drug which inhibits this cytochrome enzyme leads to accumulation of toxicity of Pirfenidone. Some of the CYP1A2 inhibitors medicines like Fluoxamine, ciprofloxacin, amiodarone etc. CYP inhibitors: these are strong inhibitors like paroxetine, fluconazole, and chloramphenicol
CYP1A2 inducers :
Omeprazole is used cautiously with tablet Pirfenex, might have chance to reduce the plasma level of the drug Pirfenidone.
Cigarette smoking :
Smoking during the treatment with tablet Pirfenex causes increased clearance of Pirfenidone.
Pirfenex tablets are contraindicated to the patient having hypersensitivity to active ingredient Pirfenidone. Other conditions : Angioedema with Pirfenidone Adjuvant use of Fluoxamine Severe hepatic and renal impairment
If a dose is missed, then have the dose as soon as possible before the next dose timing or skip the missed dose and continue daily schedule. Do have extra dose for any cost Please consult with the doctor for further details.
Most common side effects caused by Pirfenex include :
Photosensitivity reactions like rashes, Loss of appetite, Stomach discomfort, Nausea, Increased AST and ALT levels, Fatigue, Diarrhea, Dyspepsia. ADVERSE REACTIONS :
Infections and infestation: upper respiratory tract infections, UTI
Blood & lymphatic system: agranulocytosis
Immune system: angioedema
Metabolism & nutrition: anorexia, weight decreased, loss of appetite
CNS: headache, dizziness, somnolence, dysgeusia, lethargy
Heart problems: hot flush
Pulmonary: dyspnea, cough
GIT: gastro esophageal reflux, vomiting, constipation, gastritis.
Hepatobiliary: ALT, AST increased, serum albumin increased.