pemirolast

{{Short description|Chemical compound}}

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{{Drugbox

| Verifiedfields = changed

| verifiedrevid = 408530718

| IUPAC_name = 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one

| image = Pemirolast.svg

| tradename = Alamast

| Drugs.com = {{drugs.com|monograph|pemirolast-potassium}}

| pregnancy_AU =

| pregnancy_US = C

| pregnancy_US_comment = {{cite web | title=Pemirolast ophthalmic (Alamast) Use During Pregnancy | website=Drugs.com | date=2 September 2020 | url=https://www.drugs.com/pregnancy/pemirolast-ophthalmic.html | access-date=13 September 2020}}

| pregnancy_category =

| legal_AU =

| legal_CA =

| legal_UK =

| legal_US = Rx-only

| legal_status = Rx-only

| routes_of_administration = Oral, ophthalmic

| bioavailability =

| protein_bound =

| metabolism =

| elimination_half-life =

| excretion =

| IUPHAR_ligand = 7329

| CAS_number_Ref = {{cascite|correct|??}}

| CAS_number = 69372-19-6

| ATC_prefix = none

| ATC_suffix =

| ATC_supplemental =

| PubChem = 57697

| DrugBank_Ref = {{drugbankcite|changed|drugbank}}

| DrugBank = DB00885

| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}

| ChemSpiderID = 51990

| UNII_Ref = {{fdacite|changed|FDA}}

| UNII = 2C09NV773M

| KEGG_Ref = {{keggcite|correct|kegg}}

| KEGG = D07476

| ChEMBL_Ref = {{ebicite|changed|EBI}}

| ChEMBL = 1201198

| chemical_formula =

| C=10 | H=8 | N=6 | O=1

| smiles = CC1=CC=CN2C1=NC=C(C2=O)C3=NNN=N3

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Pemirolast (INN) is a mast cell stabilizer used as an anti-allergic drug therapy. It is marketed under the tradenames Alegysal and Alamast.

Clinical trials studying treatments for allergic conjunctivitis have found that an ophthalmic solution containing levocabastine with pemirolast potassium may be more effective in alleviating symptoms than levocabastine alone.{{cite journal |vauthors=Castillo M, Scott NW, Mustafa MZ, Mustafa MS, Azuara-Blanco A |title= Topical antihistamines and mast cell stabilisers for treating seasonal and perennial allergic conjunctivitis |journal=Cochrane Database Syst Rev|volume=2015 |issue= 6 |pages= CD009566 |date=2015 |pmid= 26028608 |doi= 10.1002/14651858.CD009566.pub2|pmc= 10616535 |hdl= 2164/6048 |hdl-access= free }}

It has also been studied for the treatment of asthma.

Pemirolast has appeared as a possible candidate for SARS-CoV-2 (COVID-19) spike protein disruption and interference. Such results were ascertained by molecular dynamics calculations executed on the Summit supercomputer. By simulating compounds with FDA or similar regulatory approval, the authors found 4 interfacial molecules that could potentially disrupt the SARS-CoV-2 interface with ACE-2 receptors, suggesting that such small molecules could mitigate SARS-CoV-2 infection. The 4 candidate interfacial molecules included pemirolast, isoniazid pyruvate, nitrofurantoin, and eriodictyol.{{cite journal |vauthors=Smith, MD, Smith JC |title=Repurposing Therapeutics for COVID-19: Supercomputer-Based Docking to the SARS-CoV-2 Viral Spike Protein and Viral Spike Protein-Human ACE2 Interface |journal=Preprint |pages=1–28 |date=April 2020 |doi=10.26434/chemrxiv.11871402.v4 |url=https://chemrxiv.org/articles/Repurposing_Therapeutics_for_the_Wuhan_Coronavirus_nCov-2019_Supercomputer-Based_Docking_to_the_Viral_S_Protein_and_Human_ACE2_Interface/11871402/4|doi-access=free }}

References

{{reflist}}

  • {{cite journal |vauthors=Tinkelman DG, Berkowitz RB |title=A pilot study of pemirolast in patients with seasonal allergic rhinitis |journal=Ann Allergy |volume=66 |issue=2 |pages=162–5 |date=February 1991 |pmid=1994787 }}
  • {{cite journal |vauthors=Kawashima T, Iwamoto I, Nakagawa N, Tomioka H, Yoshida S |title=Inhibitory effect of pemirolast, a novel antiallergic drug, on leukotriene C4 and granule protein release from human eosinophils |journal=Int. Arch. Allergy Immunol. |volume=103 |issue=4 |pages=405–9 |year=1994 |pmid=8130655 |doi= 10.1159/000236662}}
  • {{cite journal |vauthors=Abelson MB, Berdy GJ, Mundorf T, Amdahl LD, Graves AL |title=Pemirolast potassium 0.1% ophthalmic solution is an effective treatment for allergic conjunctivitis: a pooled analysis of two prospective, randomized, double-masked, placebo-controlled, phase III studies |journal=J Ocul Pharmacol Ther |volume=18 |issue=5 |pages=475–88 |date=October 2002 |pmid=12419098 |doi=10.1089/10807680260362759 }}
  • {{cite journal |vauthors=Kemp JP, Bernstein IL, Bierman CW, etal |title=Pemirolast, a new oral nonbronchodilator drug for chronic asthma |journal=Ann Allergy |volume=68 |issue=6 |pages=488–91 |date=June 1992 |pmid=1610024 }}