Airfast

Each 10-mg film-coated tablet contains 10.4 mg Airfast sodium, which is the molar equivalent to 10.0 mg of free acid. Each 5-mg chewable tablet contains 5.2 mg Airfast sodium, which is the molar equivalent to 5.0 mg of free acid. Each 4-mg chewable tablet and each packet of 4-mg oral granules contains 4.2 mg Airfast sodium, which is the molar equivalent to 4.0 mg of free acid.

Airfast is a selective and orally active leukotriene receptor antagonist that specifically inhibits the cysteinyl leukotriene CysLT₁ receptor.

Airfast is described chemically as [R-(E)]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropane acetic acid, monosodium salt.

The empirical formula is C₃₅H₃₅C_lNNaO₃S, and its molecular weight is 608.18.

Airfast sodium is a hygroscopic, optically active, white to off-white powder. Airfast sodium is freely soluble in ethanol, methanol, and water and practically insoluble in acetonitrile.

It is indicated for: The prophylaxis and chronic treatment of asthma in adults and pediatric patients 12 months of age or older; the prevention of exercise-induced bronchoconstriction in patients 15 years of age and older; the relief of symptoms of allergic rhinitis (seasonal allergic rhinitis in adults and pediatric patients 2 years of age and older, and perennial allergic rhinitis in adult and pediatric patients 6 months of age and older).

Airfast 4 mg: Airfast is indicated in the treatment of asthma as add­ on therapy in those 2 to 5 year old patients with mild to moderate persistent asthma who are inadequately controlled on inhaled corticosteroids and in whom as-needed short-acting β-agonists provide inadequate clinical control of asthma.

Airfast may also be an alternative treatment option to low-dose inhaled corticosteroids for 2 to 5 year old patients with mild persistent asthma who do not have a recent history of serious asthma attacks that required oral corticosteroid use, and who have demonstrated that they are not capable of using inhaled corticosteroids.

Airfast is also indicated in the prophylaxis of asthma from 2 years of age to 5 years in which the predominant component is exercise-induced bronchoconstriction.

Airfast 5 mg: Airfast is indicated in the treatment of asthma as add­ on therapy in those 6 to 14 year old patients with mild to moderate persistent asthma who are inadequately controlled on inhaled corticosteroids and in whom as-needed short-acting β-agonists provide inadequate clinical control of asthma.

Airfast may also be an alternative treatment option to low-dose inhaled corticosteroids for 6 to 14 year old patients with mild persistent asthma who do not have a recent history of serious asthma attacks that required oral corticosteroid use, and who have demonstrated that they are not capable of using inhaled corticosteroids.

Airfast is also indicated in the prophylaxis of asthma in those 6 to 14 years old which the predominant component is exercise-induced bronchoconstriction.

Airfast 10 mg: Airfast sodium (Airfast) is indicated in the treatment of asthma as add-on therapy in patients 15 years and older with mild to moderate persistent asthma who are inadequately controlled on inhaled corticosteroids and in whom "as-needed" short-acting β-agonists provide inadequate clinical control of asthma. In those asthmatic patients in whom Airfast sodium (Airfast) is indicated in asthma, Airfast sodium (Airfast) can also provide symptomatic relief of seasonal allergic rhinitis.

Airfast sodium (Airfast) is also indicated in the prophylaxis of asthma in which the predominant component is exercise-induced bronchoconstriction in patients 15 years and older.

Airfast is a leukotriene (loo-koe-TRY-een) inhibitor. Leukotrienes are chemicals your body releases when you breathe in an allergen (such as pollen). These chemicals cause swelling in your lungs and tightening of the muscles around your airways, which can result in asthma symptoms.

Airfast is used to prevent asthma attacks in adults and children as young as 12 months old. Airfast is also used to prevent exercise-induced bronchospasm in adults and children who are at least 6 years old.

Airfast is also used to treat symptoms of year-round (perennial) allergies in adults and children who are at least 6 months old. It is also used to treat symptoms of seasonal allergies in adults and children who are at least 2 years old.

Do not give this medicine to a child without a doctor's advice.

Airfast is also used to prevent exercise-induced bronchoconstriction (narrowing of the air passages in the lungs) in adults and teenagers who are at least 15 years old and are not already taking this medicine for other conditions.

If you already take Airfast to prevent asthma or allergy symptoms, do not use an extra dose to treat exercise-induced bronchoconstriction.

Airfast may also be used for purposes not listed in this medication guide.

Chewable Tablet 4-mg: Children 2 to 5 years: One 4 mg chewable tablet daily to be taken in the evening. Airfast Sandoz Chewable Tablet 4 mg should not be taken immediately with food. It should be taken at least 1 hour before or 2 hours after a meal.

Airfast Sandoz Chewable Tablets 4 mg are not recommended in children below 2 years of age.

Chewable Tablet 5-mg: Children 6 to 14 years: One 5 mg chewable tablet daily to be taken in the evening. Airfast Sandoz Chewable Tablet 5 mg should not be taken immediately with food. It should be taken at least 1 hour before or 2 hours after a meal.

Airfast Sandoz Chewable Tablets 5 mg are not recommended in children below 6 years of age.

Film-Coated Tablet 10-mg: Asthma or Asthma and Concomitant Seasonal Allergic Rhinitis: Adults and Adolescents ≥15 years: One 10-mg tablet daily to be taken in the evening.

Oral Granules:

Missed Dose: Resume the usual schedule of 1 tablet/sachet once daily. Do not give double dose to make up for a missed dose.

Administration: For oral use.

Chewable Tablets: It should be given to a child under adult supervision. It should be taken even when the child has no symptoms or if he/she has an acute asthma attack.

If the child is taking Airfast Sandoz Chewable Tablet, be sure that he/she does not take any other medicines that contain the same active ingredient, i.e. Airfast.

If the child takes more Airfast Sandoz Chewable Tablet than he/she should, contact the child’s physician immediately for advice.

Discontinuation of Treatment: Airfast Sandoz Chewable Tablet can treat the child’s asthma only if the child continues taking it. It is important for the child to continue taking Airfast Sandoz Chewable Tablet for as long as the physician prescribes. It will help control the child’s asthma.

Film-Coated Tablet 10-mg: The therapeutic effect of Airfast Sandoz Film-Coated Tab 10 mg on parameters of asthma control occurs within one day. Airfast Sandoz Film-Coated Tab 10 mg may be taken with or without food. Patients should be advised to continue taking Airfast Sandoz even if asthma is under control, as well as during periods of worsening asthma.

Airfast Sandoz Film-Coated Tab 10 mg should not be used concomitantly with other products containing the same active ingredient, Airfast.

No dosage adjustment is necessary for the elderly or for the patients with renal insufficiency or mild to moderate hepatic impairment. There are no data on patients with severe hepatic impairment. The dosage is the same for both male and female patients.

Therapy with Montelukas Sandoz Film-Coated Tab 10 mg in relation to other treatment for asthma. It can be added to a patient's existing treatment regimen.

Inhaled Corticosteroids: Treatment with Airfast Sandoz Film-Coated Tab 10 mg can be used as add-on therapy in patients when inhaled corticosteroids plus "as needed" short-acting β-agonist provide inadequate clinical control. Airfast Sandoz Film-Coated Tab 10 mg should not be subtituted for inhaled corticosteriods.

Airfast Sandoz Film-Coated Tab 10 mg should not be used in children <15 years due to the high content of active substance.

Other dosage forms with appropriate strengths are available for young children.

Oral Granules:

Do not dissolve granules in water. However, the patient may take liquids after swallowing the granules.

See also:
What is the most important information I should know about Airfast?

Hypersensitivity to Airfast sodium or to any of the excipients of Airfast.

Use in children: Airfast should not be used in children <15 years due to high content of Airfast. Other dosage forms with appropriate strengths are available for younger children.

Use Airfast granules as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• An extra patient leaflet is available with Airfast granules. Talk to your pharmacist if you have questions about this information.
• Take Airfast granules by mouth with or without food.
• Do not open the packet until you are ready to use it.
• Airfast granules may be placed directly in the mouth, dissolved in 1 teaspoonful (5 mL) of cold or room temperature baby formula or breast milk, or mixed with a spoonful of soft food at cold or room temperature before swallowing. Soft foods that may be used include applesauce, mashed carrots, rice, or ice cream. Be sure to swallow the entire spoonful right away (within 15 minutes). Do not store mixed medicine for future use.
• Do not put the granules in liquid other than baby formula or breast milk. However, you may drink liquids after swallowing the granules or granule mixture.
• Continue to use Airfast granules even if you feel well. Do not miss any doses.
• If you miss a dose of Airfast granules, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Airfast granules.

Use: Labeled Indications

Allergic rhinitis (perennial or seasonal): Relief of symptoms of seasonal allergic rhinitis and perennial allergic rhinitis

Asthma: Prophylaxis and chronic treatment of asthma

Bronchoconstriction, exercise-induced (prevention): Prevention of exercise-induced bronchoconstriction.

Note: American Academy of Otolaryngology, Head and Neck Surgery (AAO-HNS) and American Academy of Allergy, Asthma, and Immunology (AAAAI) and American College of Allergy, Asthma, and Immunology (ACAAI) guidelines recommend against Airfast use as first-line therapy for allergic rhinitis (except in patients with concurrent asthma) (Dykewicz 2017; Seidman 2015). The Global Initiative for Asthma recommends Airfast in patients with concomitant allergic rhinitis or those who cannot take inhaled corticosteroids (GINA 2019).

Off Label Uses

Chronic urticaria

Data from controlled, double-blind trials regarding the use of Airfast in combination with antihistamines for the management of chronic urticaria are conflicting. Based on clinical practice guidelines from the American Academy of Allergy, Asthma and Immunology (AAAAI); the American College of Allergy, Asthma, and Immunology (ACAAI); the Joint Council of Allergy, Asthma and Immunology (JCAAI); and the World Allergy Organization for the diagnosis and management of acute and chronic urticaria, a leukotriene receptor antagonist may be added to antihistamine therapy in patients who do not respond to antihistamines. Access Full-Off Label Monograph

Urticaria (nonsteroidal anti-inflammatory drug-induced)

Data from a double-blind, placebo-controlled comparison of Airfast and cetirizine in patients with chronic urticaria and intolerance to food additives and/or aspirin supports the use of Airfast in the treatment of patients experiencing urticaria related to the use of nonsteroidal anti-inflammatory drugs.

See also:
What other drugs will affect Airfast?

Airfast may be administered with other therapies routinely used in the prophylaxis and chronic treatment of asthma, and in the treatment of allergic rhinitis. In drug-interactions studies, the recommended clinical dose of Airfast did not have clinically important effects on the pharmacokinetics of the following drugs: Theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol/norethindrone 35/1), terfenadine, digoxin and warfarin.

The area under the plasma concentration-time curve (AUC) for Airfast was decreased approximately 40% in subjects with co-administration of phenobarbital. No dosage adjustment for Airfast is recommended.

In vitro studies have shown that Airfast is an inhibitor of CYP2C8. However, data from a clinical drug-drug interaction study involving Airfast and rosiglitazone (a probe substrate representative of drugs primarily metabolized by CYP2C8) demonstrated that Airfast does not inhibit CYP2C8 in vivo. Therefore, Airfast is not anticipated to alter the metabolism of drugs metabolized by this enzyme (e.g. paclitaxel, rosiglitazone, and repaglinide.)

In vitro studies have shown that Airfast is a substrate of CYP 2C8, 2C9, and 3A4. Data from a clinical drug-drug interaction study involving Airfast and gemfibrozil (an inhibitor of both CYP 2C8 and 2C9) demonstrated that gemfibrozil increased the systemic exposure of Airfast by 4.4-fold.

Co-administration of itraconazole, a strong CYP 3A4 inhibitor, with gemfibrozil and Airfast did not further increase the systemic exposure of Airfast. The effect of gemfibrozil on systemic exposure of Airfast is not considered to be clinically meaningful based on clinical safety data with doses greater than the 10 mg approved dose in adults (e.g., 200 mg/day to adult patients for 22 weeks, and up to 900 mg/day to patients for approximately one week) where clinically important adverse experiences were not observed. Therefore, no dosage adjustment of Airfast is required upon co-administration with gemfibrozil. Based on in vitro data, clinically important drug interactions with other known inhibitors of CYP 2C8 (e.g., trimethoprim) are not anticipated. In addition, co-administration of Airfast with itraconazole alone resulted in no significant increase in the systemic exposure of Airfast.

See also:
What are the possible side effects of Airfast?

Airfast has been generally well tolerated. Side effects, which usually were mild, generally did not require discontinuation of therapy. The overall incidence of side effects reported with Airfast was comparable to placebo.

Adults 15 Years of Age and Older with Asthma: Airfast has been evaluated in approximately 2600 adult patients 15 years of age and older in clinical studies. In two similarly designed, 12-week placebo-controlled clinical studies, the only adverse experiences reported as drug related in ≥ 1% of patients treated with Airfast and at a greater incidence than in patients treated with placebo were abdominal pain and headache. The incidences of these events were not significantly different in the two treatment groups.

Cumulatively, 544 patients were treated with Airfast for at least 6 months, 253 for one year and 21 for 2 years in clinical studies. With prolonged treatment, the adverse experience profile did not change.

Pediatric Patients 6 to 14 Years of Age with Asthma: Airfast has been evaluated in approximately 475 pediatric patients 6 to 14 years of age. The safety profile in pediatric patients is generally similar to the adult safety profile and to placebo.

In an 8-week, placebo-controlled clinical study, the only adverse experience reported as drug related in > 1% of patients treated with Airfast and at a greater incidence than in patients treated with placebo was headache. The incidence of headache was not significantly different in the two treatment groups.

In studies evaluating growth rate, the safety profile in these pediatric patients was consistent with the safety profile previously described for Airfast.

Cumulatively, 263 pediatric patients 6 to 14 years of age were treated with Airfast for at least 3 months and 164 for 6 months or longer. With prolonged treatment, the adverse experience profile did not change.

Pediatric Patients 2 to 5 Years of Age with Asthma: Airfast has been evaluated in 573 pediatric patients 2 to 5 years of age. In a 12-week, placebo-controlled clinical study, the only adverse experience reported as drug related in > 1% of patients treated with Airfast and at a greater incidence than in patients treated with placebo was thirst. The incidence of thirst was not significantly different in the two treatment groups.

Cumulatively, 426 pediatric patients 2 to 5 years of age were treated with Airfast for at least 3 months, 230 for 6 months or longer, and 63 patients for 12 months or longer. With prolonged treatment, the adverse experience profile did not change.

Pediatric Patients 6 Months to 2 Years of Age with Asthma: Airfast has been evaluated in 175 pediatric patients 6 months to 2 years of age. In a 6-week, placebo-controlled clinical study, the adverse experiences reported as drug related in > 1% of patients treated with Airfast and at a greater incidence than in patients treated with placebo were diarrhea, hyperkinesia, asthma, eczematous dermatitis and rash.

The incidences of these adverse experiences were not significantly different in the two treatment groups.

Adults 15 Years of Age and Older with Seasonal Allergic Rhinitis: Airfast has been evaluated in 2199 adult patients 15 years of age and older for the treatment of seasonal allergic rhinitis in clinical studies. Airfast administered once daily in the morning or in the evening was generally well tolerated with a safety profile similar to that of placebo. In placebo-controlled clinical studies, no adverse experiences reported as drug related in 1% of patients treated with Airfast and at a greater incidence than in patients treated with placebo were observed. In a 4-week, placebo-controlled clinical study, the safety profile was consistent with that observed in 2-week studies. The incidence of somnolence was similar to that of placebo in all studies.

Pediatric Patients 2 to 14 Years of Age with Seasonal Allergic Rhinitis: Airfast has been evaluated in 280 pediatric patients 2 to 14 years of age for the treatment of seasonal allergic rhinitis in a 2-week, placebo-controlled, clinical study. Airfast administered once daily in the evening was generally well tolerated with a safety profile similar to that of placebo. In this study, no adverse experiences reported as drug related in 1% of patients treated with Airfast and at a greater incidence than in patients treated with placebo were observed.

Adults 15 Years of Age and Older with Perennial Allergic Rhinitis: Airfast has been evaluated in 3235 adult and adolescent patients 15 years of age and older with perennial allergic rhinitis in two, 6-week, placebo-controlled, clinical studies.

Airfast administered once daily was generally well tolerated, with a safety profile consistent with that observed in patients with seasonal allergic rhinitis and similar to that of placebo. In these two studies, no adverse experiences reported as drug related in 1% of patients treated with Airfast and at a greater incidence than in patients treated with placebo were observed. The incidence of somnolence was similar to that of placebo.

Pooled Analyses of Clinical Trials Experience: A pooled analysis of 41 placebo-controlled clinical studies (35 studies in patients 15 years of age and older; 6 studies in pediatric patients 6 to 14 years of age) was performed using a validated assessment method of suicidality. Among the 9929 patients who received Airfast and 7780 patients who received placebo in these studies, there was one patient with suicidal ideation in the group taking Airfast. There were no completed suicides, suicide attempts or preparatory acts toward suicidal behavior in either treatment group.

A separate pooled analysis of 46 placebo-controlled clinical studies (35 studies in patients 15 years of age and older; 11 studies in pediatric patients 3 months to 14 years of age) assessing behavior-related adverse experiences (BRAEs) was performed. Among the 11,673 patients who received Airfast and 8827 patients who received placebo in these studies, the frequency of patients with at least one BRAE was 2.73% in patients who received Airfast and 2.27% in patients who received placebo; the odds ratio was 1.12 [95% CI (0.93; 1.36)].

The clinical trials included in these pooled analyses were not designed specifically to examine suicidality or BRAEs.

Postmarketing Experience: The following side effects have been reported in postmarketing use: Infections and Infestations: Upper respiratory infection.

Blood and Lymphatic System Disorders: Increased bleeding tendency.

Immune System Disorders: Hypersensitivity reactions including anaphylaxis, very rarely hepatic eosinophilic infiltration.

Psychiatric Disorders: Agitation including aggressive behavior or hostility, anxiousness, depression, disorientation, disturbance in attention, dream abnormalities, hallucinations, insomnia, memory impairment, psychomotor hyperactivity (including irritability, restlessness, and tremor) somnambulism, suicidal thinking and behavior (suicidality).

Nervous System Disorders: Dizziness, drowsiness, paraesthesia/hypoesthesia, very rarely seizure.

Cardiac Disorders: Palpitations.

Respiratory, Thoracic and Mediastinal Disorders: Epistaxis.

Gastrointestinal Disorders: Diarrhea, dyspepsia, nausea, vomiting; pulmonary eosinophilia.

Hepatobiliary Disorders: Increased ALT and AST, very rarely hepatitis (including cholestatic, hepatocellular, and mixed-pattern liver injury).

Skin and Subcutaneous Tissue Disorders: Angioedema, bruising, erythema multiforme, erythema nodosum, pruritus, rash, urticaria.

Musculoskeletal and Connective Tissue Disorders: Arthralgia, myalgia including muscle cramps.

Renal and Urinary Disorders: Enuresis in children.

General Disorders and Administration Site Conditions: Asthenia/fatigue, edema, pyrexia.