ALAMAST® (pemirolast potassium ophthalmic solution) is a sterile, aqueous ophthalmic solution with a pH of approximately 8.0 containing 0.1% of the mast cell stabilizer, pemirolast potassium, for topical administration to the eyes.

Pemirolast potassium is a slightly yellow, water-soluble powder with a molecular weight of 266.3.

The chemical structure is presented below:

C₁₀H₇KN₆O

Chemical name

9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-α] pyrimidin-4-one potassium

Each mL contains: ACTIVE: pemirolast potassium 1 mg (0.1%); PRESERVATIVE: lauralkonium chloride 0.005%; INACTIVES: glycerin, dibasic sodium phosphate, monobasic sodium phosphate, phosphoric acid and/or sodium hydroxide to adjust pH, and purified water. The osmolality of ALAMAST® oph-thalmic solution is approximately 240 mOsmol/kg.

Last updated on RxList: 12/30/2008

ALAMAST® ophthalmic solution is indicated for the prevention of itching of the eye due to allergic conjunctivitis. Symptomatic response to therapy (decreased itching) may be evident within a few days, but frequently requires longer treatment (up to four weeks).

The recommended dose is one to two drops in each affected eye four times daily.

Symptomatic response to therapy (decreased itching) may be evident within a few days, but frequently requires longer treatment (up to four weeks).

ALAMAST® (pemirolast potassium ophthalmic solution) 0.1% is supplied as follows:

10 mL in a white, low density polyethylene bottle with a controlled dropper tip, and a white polyethylene screw cap.

NDC 68669-711-10 10 mL fill in 11 cc container

Storage

Store at 15°–25°C (59°–77°F).

Manufactured by: Santen Oy, PO Box 33, FIN-33721 Tampere, Finland. February 2005 Version. Marketed by: VISTAKON® Pharmaceuticals, LLC Jacksonville, FL 32256 USA. Licensed from Mitsubishi Pharma Corporation Japan. FDA revision date: 5/12/2005

Last updated on RxList: 12/30/2008

In clinical studies lasting up to 17 weeks with ALAMAST® ophthalmic solution, headache, rhinitis, and cold/flu symptoms were reported at an incidence of 10–25%. The occurrence of these side effects was generally mild. Some of these events were similar to the underlying ocular disease being studied.

The following ocular and non-ocular adverse reactions were reported at an incidence of less than 5%:

Ocular: burning, dry eye, foreign body sensation, and ocular discomfort.

Non-Ocular: allergy, back pain, bronchitis, cough, dysmenorrhea, fever, sinusitis, and sneezing/nasal congestion.

No information provided.

Last updated on RxList: 12/30/2008

For topical ophthalmic use only. Not for injection or oral use.

Carcinogenesis, mutagenesis, impairment of fertility

Pemirolast potassium was not mutagenic or clasto-genic when tested in a series of bacterial and mammalian tests for gene mutation and chromosomal injury in vitro nor was it clastogenic when tested in vivo in rats.

Pemirolast potassium had no effect on mating and fertility in rats at oral doses up to 250 mg/kg (approximately 20,000 fold the human dose at 2 drops/eye, 40 μL/drop, QID for a 50 kg adult). A reduced fertility and pregnancy index occurred in the F₁ generation when F₀ dams were treated with 400 mg/kg pemirolast potassium during late pregnancy and lactation period (approximately 30,000 fold the human dose).

Pregnancy

Teratogenic effects: Pregnancy Category C.

Pemirolast potassium caused an increased incidence of thymic remnant in the neck, interventricular septal defect, fetuses with wavy rib, splitting of thoracicvertebral body, and reduced numbers of ossified sternebrae, sacral and caudal vertebrae, and metatarsi when rats were given oral doses ≥ 250 mg/kg (approximately 20,000 fold the human dose at 2 drops/eye, 40 μL/drop, QID for a 50 kg adult) during organogenesis. Increased incidence of dilation of renal pelvis/ureter in the fetuses and neonates was also noted when rats were given an oral dose of 400 mg/kg pemirolast potassium (approximately 30,000 fold the human dose). Pemirolast potassium was not teratogenic in rabbits given oral doses up to 150 mg/kg (approximately 12,000 fold the human dose) during the same time period. There are no adequate and well-controlled studies in pregnant women. Because animal reproductive studies are not always predictive of human response, ALAMAST® ophthalmic solution should be used during pregnancy only if the benefit outweighs the risk.

Non-teratogenic effects

Pemirolast potassium produced increased pre- and post-implantation losses, reduced embryo/fetal and neonatal survival, decreased neonatal body weight, and delayed neonatal development in rats receiving an oral dose at 400 mg/kg (approximately 30,000 fold the human dose). Pemirolast potassium also caused a reduction in the number of corpus lutea, the number of implantations, and number of live fetuses in the F₁ generation in rats when F₀ dams were given oral dosages ≥ 250mg/kg (approximately 20,000 fold the human dose) during late gestation and the lactation period.

Nursing Mothers

Pemirolast potassium is excreted in the milk of lactating rats at concentrations higher than those in plasma. It is not known whether pemirolast potassium is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when ALAMAST® ophthalmic solution is administered to a nursing woman.

Pediatric Use

Safety and effectiveness in pediatric patients below the age of 3 years have not been established.

Last updated on RxList: 12/30/2008

No accounts of ALAMAST® ophthalmic solution overdose were reported following topical ocular application.

Oral ingestion of the contents of a 10 mL bottle would be equivalent to 10 mg of pemirolast potassium.

ALAMAST® ophthalmic solution is contraindicated in patients with previously demonstrated hypersensitivity to any of the ingredients of this product.

Last updated on RxList: 12/30/2008

Mechanism of Action

Pemirolast potassium is a mast cell stabilizer that inhibits the in vivo Type I immediate hypersensitivity reaction.

In vitro and in vivostudies have demonstrated that pemirolast potassium inhibits the antigen-induced release of inflammatory mediators (e.g., histamine, leukotriene C₄,D₄,E₄) from human mast cells.

In addition, pemirolast potassium inhibits the chemotaxis of eosinophils into ocular tissue and blocks the release of mediators from human eosinophils.

Although the precise mechanism of action is unknown, the drug has been reported to prevent calcium influx into mast cells upon antigen stimulation.

Pharmacokinetics

Topical ocular administration of one to two drops of ALAMAST® ophthalmic solution in each eye four times daily in 16 healthy volunteers for two weeks resulted in detectable concentrations in the plasma. The mean (±SE) peak plasma level of 4.7 ±0.8 ng/mL occurred at 0.42 ±0.05 hours and the mean t1/2 was 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 was reached.

Clinical Studies

In clinical environmental studies, ALAMAST® was significantly more effective than placebo after 28 days in preventing ocular itching associated with allergic conjunctivitis.

Last updated on RxList: 12/30/2008

To prevent contaminating the dropper tip and solution, do not touch the eye-lids or surrounding areas with the dropper tip. Keep the bottle tightly closed when not in use.

Patients should be advised not to wear contact lenses if their eye is red. ALAMAST® should not be used to treat contact lens related irritation. The preservative in ALAMAST® , lauralkonium chloride,may be absorbed by soft contact lenses.Patients who wear soft contact lenses and whose eyes are not red should be instructed to wait at least ten minutes after instilling ALAMAST® before they insert their contact lenses.

Last updated on RxList: 12/30/2008

IMPORTANT NOTE: This is a summary and does not contain all possible information about this product. For complete information about this product or your specific health needs, ask your health care professional. Always seek the advice of your health care professional if you have any questions about this product or your medical condition. This information is not intended as individual medical advice and does not substitute for the knowledge and judgment of your health care professional. This information does not contain any assurances that this product is safe, effective, or appropriate for you.

PEMIROLAST - OPHTHALMIC

(pem-EER-oh-last)

COMMON BRAND NAME(S): Alamast

USES: Pemirolast is used to prevent itching of the eyes caused by allergies (allergic conjunctivitis). This medication is known as a mast cell stabilizer. It works by blocking certain natural substances (histamine, leukotriene) that cause allergic symptoms.

Do not use this medication to treat redness and irritation due to wearing contact lenses.

HOW TO USE: To apply eye drops, wash your hands first. To avoid contamination, do not touch the dropper tip or let it touch your eye or any other surface.

Remove contact lenses before applying the eye drops. Wait at least 10 minutes after using this medication before inserting contact lenses.

This medication is used in the affected eye(s), usually 4 times daily or as directed by your doctor.

Tilt your head back, look upward, and pull down the lower eyelid to make a pouch. Hold the dropper directly over the eye and place 1 drop into the pouch. Look downward and gently close your eyes for 1 to 2 minutes. Place one finger at the corner of the eye near the nose and apply gentle pressure. This will prevent the medication from draining away from the eye. Try not to blink and do not rub the eye. Repeat these steps if your dose is for more than 1 drop and for the other eye if so directed.

Do not rinse the dropper. Replace the dropper cap tightly after each use.

If you are using another kind of eye medication (e.g., drops or ointments), wait at least 5 minutes before applying other medications. Use eye drops before eye ointments to allow the eye drops to enter the eye.

Use this medication regularly in order to get the most benefit from it. To help you remember, use it at the same times each day. Continue using it for the full time prescribed.

It may take up to several days of continued use to see a relief in symptoms and up to 4 weeks for full benefit. If immediate relief of symptoms (itching) is needed, use other quick-relief medication (such as eye drops containing antihistamines, decongestants, or nonsteroidal anti-inflammatory drugs-NSAIDs) as directed by your doctor. Tell your doctor if your condition persists or worsens.

SIDE EFFECTS: Headache, runny nose, eye burning/discomfort, feeling as if something is in your eye, or dry eyes may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any of the following symptoms of a serious allergic reaction: rash, itching, swelling, severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Contact your doctor for medical advice about side effects. The following numbers do not provide medical advice, but in the US you may report side effects to the Food and Drug Administration (FDA) at 1-800-FDA-1088. In Canada, you may call Health Canada at 1-866-234-2345.

PRECAUTIONS: Before using pemirolast, tell your doctor or pharmacist if you are allergic to it; or to preservatives (e.g., lauralkonium chloride); or if you have any other allergies.

Before using this medication, tell your doctor or pharmacist your medical history.

After you apply this drug, your vision may become temporarily blurred. Use caution while driving, using machinery, or doing any other activity that requires clear vision.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

It is not known whether this drug passes into breast milk. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with them first.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use.

Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: This medicine may be harmful if swallowed. If swallowing or overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center.

NOTES: Avoid allergens that may be the cause of your allergies. Some common allergens that cause allergic conjunctivitis include pollen, grasses, weeds, dust mites, and pet dander.

Do not share this medication with others.

This medication has been prescribed for your current condition only. Do not use it later for another condition unless directed to do so by your doctor. A different medication may be necessary in that case.

MISSED DOSE: If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

STORAGE: Store dropper bottle upright at room temperature between 59-77 degrees F (15-25 degrees C). Do not store in the bathroom. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised July 2008 Copyright(c) 2008 First DataBank, Inc.