|Accession Number||DB00885 (APRD00394)|
Pemirolast potassium is a slightly yellow powder that is soluble in water. It is a mast cell stabilizer that acts as an antiallergic agent. As an ophthalmic aqueous sterile solution, pemirolast is used for the prevention of itching of the eyes caused by allergies such as hay fever, and allergic conjunctivitis. Pemirolast is potentially useful for prophylaxis of pulmonary hypersensitivity reactions to drugs such as paclitaxel.
|External IDs||BMY 26517 / DE 068 / TBX|
|Approved Prescription Products||Not Available|
|Approved Generic Prescription Products||Not Available|
|Approved Over the Counter Products||Not Available|
|Unapproved/Other Products||Not Available|
|Brand mixtures||Not Available|
|Weight||Average: 228.2101 |
For the prevention of itching of the eyes caused by allergies such as hay fever, and allergic conjunctivitis
|Structured Indications||Not Available|
Pemirolast is used for the prophylactic treatment of itching of the eye associated with allergic conjunctivitis. Pemirolast potassium is a mast cell stabilizer that inhibits the in vivo Type I immediate hypersensitivity reaction. Pemirolast inhibits the antigen-induced release of inflammatory mediators (e.g., histamine, leukotriene C4, D4, E4) from human mast cells. Allergic reactions lead to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H1-receptors, produces pruritis and vasodilatation (allowing blood fluids to enter the area to cause swelling). Pemirolast is a histamine H1 antagonist. It competes with histamine for the normal H1-receptor sites on effector cells of blood vessels to provide effective, temporary relief of watery and itchy eyes.
|Mechanism of action|
Pemirolast binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Pemirolast has also been observed to inhibit antigen-stimulated calcium ion influx into mast cells through the blockage of calcium channels. Pemirolast inhibits the chemotaxis of eosinophils into ocular tissue, and prevents inflammatory mediator release from human eosinophils.
|Volume of distribution||Not Available|
|Protein binding||Not Available|
|Route of elimination|
Following topical administration, about 10-15% of the dose was excreted unchanged in the urine.
4.5 hours (Ophthalmic)
|Pharmacogenomic Effects/ADRs||Not Available|
|Food Interactions||Not Available|
Graziano Castaldi, "Process for the preparation of high purity pemirolast." U.S. Patent US20030032805, issued February 13, 2003.US20030032805
|ATC Codes||Not Available|
|AHFS Codes||Not Available|
|PDB Entries||Not Available|
|FDA label||Download (372 KB)|
|Dosage forms||Not Available|
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|Predicted ADMET features|
|Mass Spec (NIST)||Not Available|
|Description||This compound belongs to the class of chemical entities known as pyridopyrimidines. These are compounds containing a pyridopyrimidine, which consists of a pyridine fused to a pyrimidine. Pyridine is 6-membered ring consisting of five carbon atoms and a nitrogen atom. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions.|
|Super Class||Organic compounds|
|Alternative Parents||Pyrimidones / Methylpyridines / Tetrazoles / Heteroaromatic compounds / Lactams / Azacyclic compounds / Organopnictogen compounds / Organooxygen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives|
|Substituents||Pyridopyrimidine / Pyrimidone / Methylpyridine / Pyridine / Pyrimidine / Azole / Tetrazole / Heteroaromatic compound / Lactam / Azacycle/ Organic oxide / Organopnictogen compound / Organic oxygen compound / Organic nitrogen compound / Organooxygen compound / Organonitrogen compound / Hydrocarbon derivative / Aromatic heteropolycyclic compound|
|Molecular Framework||Aromatic heteropolycyclic compounds|
|External Descriptors||Not Available|