Description
Generic Name:
Pirfenidone
Dosage form:
Tablet
Strength:
200mg
Brand Name:
Pircare
Company:
ARLAK BIOTECH
Pircare (Pirfenidone) exerts anti-inflammatory and antifibrotic activities. Widely used in the treatment of idiopathic pulmonary fibrosis (IPF). Available in oral tablet form. Pircare (Pirfenidone) works by inhibiting collagen synthesis, decreasing the production of cytokines, and hindering the proliferation of fibroblasts.
Indications:
- Mild to moderate idiopathic pulmonary fibrosis (scarring of the lungs with an unknown cause)
Pharmacology
Class:
- Anti-inflammatory agent
- Antifibrotic agent
Mechanism of Action
In spite of the fact that clear and accurate mechanisms of action of pirfenidone have not been established, the molecule has shown antifibrotic and anti-inflammatory properties in cell-based studies in many in vitro systems and animal models of fibrotic scarring. Pirfenidone performs its anti-fibrotic action by suppressing transforming growth factor-β1( TGF-β1), an important cytokine associated with fibrogenesis and extracellular matrix production, and increases the production of collagen.
It is also witnessed that pirfenidone decreases the release of influential pro-inflammatory mediators, including Tumor necrosis Factor-alpha (TNF-α), interleukin 1L-1β, and interferon-gamma (IFNγ). In separate cultured human peripheral blood cells, pirfenidone inhibits the entry of inflammatory mediators in cells and stimulates pulmonary vascular permeability.
Pharmacokinetics
The medication is to be taken after food, to lessen nausea and dizziness related to the drug. However, the presence of food strikingly decreases the rate of absorption.
The volume of Distribution Vd
The constant volume of distribution of pirfenidone after oral administration is about 59 to 70L.
Metabolism
50% of the drug metabolism occurs by cytochrome liver enzymes, CYP1A2 converts the pirfenidone into 5-carboxy pirfenidone, the inactive metabolite.
Excretion
More than 80% of the administered drug is excreted through urine within 24 hours of intake.
Peak Time
The peak concentration of pirfenidone in plasma if taken on an empty stomach is 0.5 hours. If the drug is taken with the food, the peak time is 3 hours.
Half-life
2.2 to 3 hour
Protein Binding
Pirfenidone has 60% plasma protein binding mainly binds to albumin protein.
Contraindications
No contraindications
Adverse Effects
Besides its needed effects, a drug might cause some undesirable effects. However not all of these adverse effects may occur, but if they do occur some of them might need medical attention.
Call your doctor straight away if any of the following side effects happen
More common
- Diarrhea
- Skin rash
- Nausea
- Photosensitivity
- stomach upset
- vomiting
