Flunisolide

Avoid being near people who are sick or have infections. Steroid medicine can lower the blood cells that help your body fight infections. This can make it easier for you to get sick from being around others who are ill. Call your doctor for preventive treatment if you are exposed to chicken pox or measles. These conditions can be serious or even fatal in people who are using steroid medicine.

There may be other drugs that can interact with flunisolide inhalation. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.

Follow all directions on your prescription label. Do not use this medicine in larger or smaller amounts or for longer than recommended.

Flunisolide inhalation will not work fast enough to treat an asthma attack. Use only a fast acting inhalation medicine for an asthma attack. Tell your doctor if it seems like your asthma medications don't work as well.

This medicine comes with patient instructions for safe and effective use. Follow these directions carefully. Ask your doctor or pharmacist if you have any questions.

To reduce the chance of developing a yeast infection in your mouth, rinse with water after using flunisolide inhalation. Do not swallow.

Use flunisolide inhalation regularly to get the most benefit. Asthma is usually treated with a combination of drugs. Use all medications as directed by your doctor. Read the medication guide or patient instructions provided with each medication.

It may take up to 2 or more weeks before your symptoms improve. For best result, keep using the medicine as directed.

Call your doctor if your symptoms do not improve after 4 weeks of treatment.

Your dose needs may change if you have surgery, are ill, are under stress, or have recently had an asthma attack. Do not change your medication dose or schedule without your doctor's advice.

Seek medical attention if you think your asthma medications are not working as well. An increased need for medication could be an early sign of a serious asthma attack.

If you switched to flunisolide inhalation from an oral (taken by mouth) steroid, you may need to restart the oral medicine if you are under stress or have an asthma attack or other medical emergency. Wear a medical alert tag or carry an ID card stating that you may need an oral steroid in an emergency.

Store at room temperature away from moisture and heat.

Do not try to clean or take apart the inhaler device. Do not float the medicine canister in water. Get your prescription refilled before you run out of medicine completely. Always use the new inhaler device provided with your refill.

Keep the medicine canister away from open flame or high heat, such as in a car on a hot day. The canister may explode if it gets too hot. Do not puncture or burn an empty inhaler canister.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

An overdose of flunisolide inhalation is not expected to produce life threatening symptoms. However, long term use of high steroid doses can lead to symptoms such as thinning skin, easy bruising, changes in the shape or location of body fat (especially in your face, neck, back, and waist), increased acne or facial hair, menstrual problems, impotence, or loss of interest in sex.

Use the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not use extra medicine to make up the missed dose.

Flunisolide, the active component of NASAREL nasal spray, is an anti-inflammatory glucocorticosteroid with the chemical name: 6(alpha)-fluoro-11(beta),16(alpha),17,21 tetrahydroxypregna-1,4-diene-3,20-dione cyclic 16,17-acetal with acetone, hemihydrate. It has the following chemical structure:

Flunisolide is a white to creamy white crystalline powder with a molecular weight of 443.51 and molecular formula of C 24 H 31 FO 6 . It is soluble in acetone, sparingly soluble in chloroform, slightly soluble in methanol, and practically insoluble in water. It has a melting point of about 245°C. The octanol:water partition coefficient is 2.17 at neutral pH.

NASAREL is a metered dose manual pump spray unit containing 0.025% w/w flunisolide in an aqueous medium containing benzalkonium chloride, butylated hydroxytoluene, citric acid, edetate disodium, polyethylene glycol 400, polysorbate 20, propylene glycol, sodium citrate dihydrate, sorbitol and purified water. Sodium hydroxide and/or hydrochloric acid may be added to adjust the pH to a target of 5.2. Each 25 mL spray bottle contains 6.25 mg of flunisolide.

After initial priming (5 to 6 sprays), each spray of the pump spray unit delivers a metered spray of 100 mg formulation containing 29 mcg of flunisolide. The size of 99.5% of the droplets produced by the unit is greater than 8 microns. The contents of one nasal spray bottle delivers 200 sprays in addition to the priming sprays.

The replacement of a systemic corticosteroid with topical corticoid can be accompanied by signs of adrenal insufficiency, and in addition some patients may experience symptoms of withdrawal, e.g., joint and/or muscular pain, lassitude and depression. Patients previously treated for prolonged periods with systemic corticosteroids and transferred to NASAREL should be carefully monitored to avoid acute adrenal insufficiency in response to stress.

Careful attention must also be given to patients who have associated asthma or other clinical conditions where too rapid a decrease in systemic corticosteroids may exacerbate their symptoms.

The use of NASAREL with systemic prednisone as alternate day therapy or with daily doses of less than 7.5 mg could increase the likelihood of hypothalamic-pituitary-adrenal axis suppression compared to a therapeutic dose of either one alone. Therefore, NASAREL treatment should be used with caution in patients already on prednisone regimens for any disease.

Persons who are on drugs which suppress the immune system are more susceptible to infections than healthy individuals. Chicken pox and measles, for example, can have a more serious or even fatal course in nonimmune pediatric patients or adults on corticosteroids. In such pediatric patients or adults who have not had these diseases, particular care should be taken to avoid exposure. How the dose, route and duration of corticosteroid administration affects the risk of developing a disseminated infection is not known. The contribution of underlying disease and/or prior corticosteroid treatment to the risk is also not known. If a nonimmune patient is exposed to chicken pox, prophylaxis with varicella zoster immune globulin (VZIG) may be indicated. If exposed to measles, prophylaxis with pooled intramuscular immunoglobulin (IG) may be indicated. (See the respective package insert for complete VZIG and IG prescribing information). If chicken pox develops, treatment with antiviral agents may be considered.

Flunisolide is a prescription medication used to treat chronic asthma. Flunisolide is also used to manage nasal allergy symptoms including sneezing, itching, and runny or stuffed nose.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

No formal drug interaction studies performed to date.106

Metabolism thought to occur mainly via CYP3A4.105

Drugs Affecting Hepatic Microsomal Enzymes

Concomitant use of flunisolide and drugs that affect CYP3A4 could alter flunisolide metabolism, but orally inhaled flunisolide has limited potential to cause interactions with CYP3A4 at plasma concentrations achieved clinically.106

Adverse reactions reported in controlled clinical trials and long-term open studies in 595 patients treated with Flunisolide Nasal Solution are described below. Of these patients, 409 were treated for 3 months or longer, 323 for 6 months or longer, 259 for 1 year or longer, and 91 for 2 years or longer.

In general, side effects elicited in the clinical studies have been primarily associated with the nasal mucous membranes. The most frequent complaints were those of mild transient nasal burning and stinging, which were reported in approximately 45% of the patients treated with Flunisolide Nasal Solution in placebo-controlled and long-term studies. These complaints do not usually interfere with treatment; in only 3% of patients was it necessary to decrease dosage or stop treatment because of these symptoms. Approximately the same incidence of mild transient nasal burning and stinging was reported in patients on placebo as was reported in patients treated with Flunisolide Nasal Solution in controlled studies, implying that these complaints may be related to the vehicle or the delivery system. The incidence of complaints of nasal burning and stinging decreased with increasing duration of treatment.

Other side effects reported at a frequency of 5% or less were: nasal congestion, sneezing, epistaxis and/or bloody mucous, nasal irritation, watery eyes, sore throat, nausea and/or vomiting, and headaches. As with other nasally inhaled corticosteroids, nasal septal perforations have been reported in rare instances with the use of Flunisolide Nasal Solutions. Temporary or permanent loss of the sense of smell and taste have also been reported with the use of Flunisolide nasal solutions.

Systemic corticosteroid side effects were not reported during the controlled clinical trials. If recommended doses are exceeded, or if individuals are particularly sensitive, symptoms of hypercorticism, i.e., Cushing’s syndrome, could occur. Cases of growth suppression have been reported for intranasal corticosteroids (including Flunisolide Nasal Solution) (see PRECAUTIONS, Pediatric Use).

To report SUSPECTED ADVERSE REACTIONS, contact Bausch + Lomb, a division of Valeant Pharmaceuticals North America LLC at 1-800-321-4576 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Do not spray in eyes.

Flunisolide Nasal Solution, USP 0.025% is supplied in a nasal pump dispenser with dust cover and with patient instructions in the following size:

25 mL bottle – NDC 24208-344-25

Each 25 mL Flunisolide Nasal Solution spray bottle contains 6.25 mg (0.25 mg/mL), 200 metered sprays of Flunisolide.

Store between 15°-25°C (59°-77°F).

KEEP OUT OF REACH OF CHILDREN.

Bausch + Lomb, a division of
Valeant Pharmaceuticals North America LLC
Bridgewater, NJ 08807 USA

©Bausch & Lomb Incorporated

Revised: June 2016

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