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OverviewMechanism of ActionHow To UseUsesBenfitsIndicationsMethod of AdministrationDosage StrengthsDosage FormsDietary RestrictionsContraindicationsWarnings and Precautions for usingAdverse ReactionsSide EffectsUse of Pemirolast in Specific PopulationsOverdosage Clinical Pharmacology Authored by Reviewed by References
Pemirolast

Pemirolast

Indications, Uses, Dosage, Drugs Interactions, Side effects
Pemirolast
Medicine Type :
Allopathy
Prescription Type:
Prescription Required
Approval :
DCGI (Drugs Controller General of India)
Schedule
Schedule H
Pharmacological Class:
Mast cell stabilizers,
Therapy Class:
Antiallergic, Antiasthmatic,

Pemirolast belongs to the pharmacological class of Mast cell stabilizers. Pemirolast appears to have anti-allergy effects such as hay fever and allergic conjunctivitis.

Pemirolast has been approved for relieving symptoms as well as for the treatment and maintenance of episodes of allergic rhinitis, allergic conjunctivitis, and asthma.

Pemirolast is poorly absorbed in the gastrointestinal tract after oral administration. As a result of poor absorption of about 1%, the remainder of the drug is excreted in the feces.

The common side effects of Pemirolast are irregular nausea, dysmenorrhea, bronchitis, sinusitis, cold/flu, and fever.

Pemirolast is found to be available in the form of Ophthalmic solution and oral formulation. Pemirolast is available in the U.S., Canada, E.U., India, Australia, and Japan.

Pemirolast belongs to the pharmacological class of Mast cell stabilizers. Pemirolast appears to have anti-allergy effects such as hay fever and allergic conjunctivitis.

Pemirolast is found to bind to the histamine H1 receptor. This in turn blocks the action of endogenous histamine, which subsequently leads to the temporary relief of the negative symptoms brought on by the histamine. Pemirolast has also been found to inhibit antigen-stimulated calcium ion influx into the mast cells through the blockage of the calcium channels. Pemirolast also inhibits the chemotaxis of eosinophils into ocular tissue and prevents inflammatory mediator release from human eosinophils.

Pemirolast had been approved for relieving symptoms as well as also for the treatment and maintenance of episodes of allergic rhinitis, allergic conjunctivitis, and asthma

The half-life of the ophthalmic solution of pemirolast is found to be 4.5 hrs. A 10 mg pemirolast potassium dose after being taken orally caused a peak plasma concentration of 0.723 μ g/ml.

The onset of action of pemirolast is said to be within a few days.

Pemirolast is available in ophthalmic solutions and oral formulations.

Pemirolast can be used in the treatment of the following conditions:

  • Allergic rhinitis
  • Allergic conjunctivitis
  • Asthma

Pemirolast can help to relieve symptoms and also for the treatment and maintenance of hay fever, allergic rhinitis, and asthma

Pemirolast is approved for use in the following clinical indications/conditions:

  • Allergic rhinitis
  • Allergic conjunctivitis
  • Asthma

Ophthalmic drops

1 or 2 drops to be installed in the eye four times a day.

Oral

To be administered with water.

Ophthalmic

Prophylaxis of allergic conjunctivitis

Adult: As 0.1% ophthalmic solution: Instill 1-2 drops into the affected eye(s) 4 times daily.

Child: >3 yr: As 0.1% ophthalmic solution: Instill 1-2 drops into the affected eye(s) 4 times daily.

Oral

Allergic rhinitis

Adult: Usual dose: 5 mg bid.

Child: 1-4 yr: 1.25 mg bid; 5-10 yr: 2.5 mg bid.

Oral

Chronic asthma

Adult: Usual dose: 10 mg bid.

Child: 1-4 yr: 2.5 mg bid; 5-10 yr: 5 mg bid.

Ophthalmic solution and oral.

  • Dosage Adjustments in Pediatric Patients:

In Pediatric patients 1-4 yrs

Chronic asthma: 2.5mg twice a day

Allergic rhinitis: 1.5 mg twice a day

Ophthalmic: At less than three years old, 0.1% of the drug is instilled in the eye.

Smoking cessation and maintaining health are a must.

Caffeine should be avoided or limited to use as it might lead to the risk of nausea, palpitations, nervousness, rapid heartbeat, etc.

Alcohol intake should be avoided in patients, especially those with an underlying liver disorder or liver dysfunction.

A diet containing food with a high sugar content as well as carbohydrates should be restricted. This includes candies, chips, pies, cakes, honey, cookies, jams and bread. It is also advised to limit ore reduce the intake of cholesterol and saturated fat and instead chooses lean meat, poultry,poultry, or fish.

The dietary restrictions should be individualized as per the patient's requirements.

Pemirolast may be contraindicated under the following conditions:

  • Hypersensitivity to the ingredients of the medication.

Safety and efficacy in children <3 Years of age have not been established; not for injection or oral use; ophthalmic use only; not indicated to treat contact lens irritation; do not wear contact lens if the eye is red. In non-red eyes, soft contact lenses should not be applied for 10 minutes after the instillation of pemirolast potassium to avoid absorption of lauralkonium chloride.

Alcohol Warning

Avoid alcohol usage while on Pemirolast medication, as alcohol can worsen the effects of any underlying disease condition, including conditions such as dizziness, blurred vision, etc.

Breast Feeding Warning

There are no adequate studies on women to determine infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Pregnancy Warning

Pregnancy Category C.

Animal studies had shown an adverse effect, as well as there are no adequate studies in pregnant women, or no animal studies had been conducted, and there are found to be no adequate studies in pregnant women.

Food Warning

No sufficient scientific evidence is traceable regarding the use and safety of Pemirolast in concurrent use with any particular food.

The adverse reactions related to Pemirolast can be categorized as follows:

  • Headache
  • Rhinitis
  • Cold /flu
  • Fever
  • Dysmenorrhea
  • Back pain
  • Bronchitis
  • Cough

The common side effects of Pemirolast include the following:

  • Headache
  • Rhinitis
  • Cold /flu
  • Fever
  • Dysmenorrhea
  • Back pain
  • Bronchitis
  • Cough

Pregnancy

Pregnancy Category C

Animal studies had shown an adverse effect, as well as there are no adequate studies in pregnant women, or no animal studies had been conducted, and there are found to be no adequate studies in pregnant women.

Nursing Mothers

There are no adequate studies on women to determine infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Pediatric Use

Pemirolast Potassium has been tested in children three years of age and older and, in effective doses, has not been shown to cause different side effects or problems than it does in adults.

Geriatric Use

There is no specific information available comparing the use of Pemirolast Potassium in the elderly with use in other age groups.

No reports of overdose. A 10 mL bottle is equal to 10 mg of pemirolast potassium if ingested orally.

Pharmacodynamics

Pemirolast is found to inhibit the antigen-induced release of inflammatory mediators e.g., histamine, leukotriene C4, D4, E4 from the human mast cells. Allergic reactions lead to cell degranulation and the release of histamine and other chemical mediators from the mast cell or basophil.

Pharmacokinetics

Topical ocular administration of 1 to 2 drops of Pemirolast ophthalmic solution in each eye 4 times daily in sixteen healthy volunteers for 2 weeks resulted in detectable concentrations in the plasma. The mean (±SE) peak plasma level of 4.7 ±0.8 ng/mL had occurred at 0.42 ±0.05 hours, and the mean t1/2 was foudn to be 4.5 ±0.2 hours. When a single 10 mg pemirolast potassium dose was taken orally, a peak plasma concentration of 0.723 μ g/mL had been reached.

  1. httphttps://www.drugs.com/mtm/pemirolast-ophthalmic.html#side-effects
  2. s://www.mims.com/philippines/drug/info/pemirolast?mtype=generic
  3. https://www.ndrugs.com/?s=pemirolast potassium&t=overdose
  4. https://www.syrianclinic.com/med/en/ProfDrugs/Pemirolastpd.html
  5. https://www.rxlist.com/alamast-drug.htm#clinpharm
  6. httpshttps://docs.google.com/document/d/1pnxhHCWiBscLXc87C0rsQhS3iJysX5Yq/edit
  7. ://www.drugs.com/monograph/pemirolast.html
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Sonali R Muralidhar
I am Sonali R Muralidhar currently residing at Madurai.I have completed my Master’s in Pharmacy with my core subject as Pharmaceutics. I am interested in Pharmaceutical research , medical content writing, Biopharmaceutics , regulatory affairs , novel drug delivery, targeted drug delivery.
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Dr JUHI SINGLA
Dr JUHI SINGLA has completed her MBBS from Era’s Lucknow Medical college and done MD pharmacology from SGT UNIVERSITY Gurgaon. She can be contacted at editorial@medicaldialogues.in. Contact no. 011-43720751
Published on: 28 Jan 2023 5:45 PM GMT
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