Montek-LC

Levocetirizine dihydrochloride (Montek-LC) is a third-generation non-sedative antihistamine indicated for the relief of symptoms associated with seasonal and perennial allergic rhinitis and uncomplicated skin manifestations of chronic idiopathic urticaria. It was developed from the second-generation antihistamine cetirizine. Levocetirizine dihydrochloride (Montek-LC) is the R-enantiomer of the cetirizine racemate. Levocetirizine dihydrochloride (Montek-LC) is an inverse agonist that decreases activity at histamine H1 receptors. This in turn prevents the release of other allergy chemicals and increased blood supply to the area, and provides relief from the typical symptoms of hay fever. It does not prevent the actual release of histamine from mast cells. Levocetirizine dihydrochloride (Montek-LC) was approved by the United States Food and Drug Administration on May 25, 2007 and is marketed under the brand Levocetirizine dihydrochloride (Montek-LC)® by sanofi-aventis U.S. LLC.

Each 10-mg film-coated tablet contains 10.4 mg Montelukast (Montek-LC) sodium, which is the molar equivalent to 10.0 mg of free acid. Each 5-mg chewable tablet contains 5.2 mg Montelukast (Montek-LC) 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 Montelukast (Montek-LC) sodium, which is the molar equivalent to 4.0 mg of free acid.

Montelukast (Montek-LC) (Montelukast (Montek-LC)) is a selective and orally active leukotriene receptor antagonist that specifically inhibits the cysteinyl leukotriene CysLT₁ receptor.

Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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.

Montelukast (Montek-LC) sodium is a hygroscopic, optically active, white to off-white powder. Montelukast (Montek-LC) sodium is freely soluble in ethanol, methanol, and water and practically insoluble in acetonitrile.

Seasonal Allergic Rhinitis

Levocetirizine dihydrochloride (Montek-LC) is indicated for the relief of symptoms associated with seasonal allergic rhinitis in adults and children 2 years of age and older.

Perennial Allergic Rhinitis

Levocetirizine dihydrochloride (Montek-LC) is indicated for the relief of symptoms associated with perennial allergic rhinitis in adults and children 6 months of age and older.

Chronic Idiopathic Urticaria

Levocetirizine dihydrochloride (Montek-LC) is indicated for the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children 6 years of age and older.

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).

Montelukast (Montek-LC) 4 mg: Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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.

Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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.

Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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.

Montelukast (Montek-LC) 5 mg: Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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.

Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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.

Montelukast (Montek-LC) (Montelukast (Montek-LC)) is also indicated in the prophylaxis of asthma in those 6 to 14 years old which the predominant component is exercise-induced bronchoconstriction.

Montelukast (Montek-LC) 10 mg: Montelukast (Montek-LC) sodium (Montelukast (Montek-LC)) 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 Montelukast (Montek-LC) sodium (Montelukast (Montek-LC)) is indicated in asthma, Montelukast (Montek-LC) sodium (Montelukast (Montek-LC)) can also provide symptomatic relief of seasonal allergic rhinitis.

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

Levocetirizine dihydrochloride (Montek-LC) is an antihistamine that reduces the effects of natural chemical histamine in the body. Histamine can produce symptoms of sneezing, itching, watery eyes, and runny nose.

Levocetirizine dihydrochloride (Montek-LC) is 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.

Levocetirizine dihydrochloride (Montek-LC) is also used to treat itching and swelling caused by chronic urticaria (hives) in adults and children who are at least 6 months old.

Levocetirizine dihydrochloride (Montek-LC) may also be used for purposes not listed in this medication guide.

Montelukast (Montek-LC) 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.

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

Montelukast (Montek-LC) 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.

Montelukast (Montek-LC) 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 Montelukast (Montek-LC) to prevent asthma or allergy symptoms, do not use an extra dose to treat exercise-induced bronchoconstriction.

Montelukast (Montek-LC) may also be used for purposes not listed in this medication guide.

Levocetirizine dihydrochloride (Montek-LC) is available as 2.5 mg/5 mL (0.5 mg/mL) oral solution and as 5 mg breakable (scored) tablets, allowing for the administration of 2.5 mg, if needed. Levocetirizine dihydrochloride (Montek-LC) can be taken without regard to food consumption.

Adults And Children 12 Years Of Age and Older

The recommended dose of Levocetirizine dihydrochloride (Montek-LC) is 5 mg (1 tablet or 2 teaspoons [10 mL] oral solution) once daily in the evening. Some patients may be adequately controlled by 2.5 mg (½ tablet or 1 teaspoon [5 mL] oral solution) once daily in the evening.

Children 6 To 11 Years Of Age

The recommended dose of Levocetirizine dihydrochloride (Montek-LC) is 2.5 mg (½ tablet or 1 teaspoon [5 mL] oral solution) once daily in the evening. The 2.5 mg dose should not be exceeded because the systemic exposure with 5 mg is approximately twice that of adults.

Children 6 Months To 5 Years Of Age

The recommended initial dose of Levocetirizine dihydrochloride (Montek-LC) is 1.25 mg (½ teaspoon oral solution) [2.5mL] once daily in the evening. The 1.25 mg once daily dose should not be exceeded based on comparable exposure to adults receiving 5 mg.

Dose Adjustment For Renal And Hepatic Impairment

In adults and children 12 years of age and older with:

• Mild renal impairment (creatinine clearance [CLCR] = 50-80 mL/min): a dose of 2.5 mg once daily is recommended;
• Moderate renal impairment (CLCR = 30-50 mL/min): a dose of 2.5 mg once every other day is recommended;
• Severe renal impairment (CLCR = 10-30 mL/min): a dose of 2.5 mg twice weekly (administered once every 3-4 days) is recommended;
• End-stage renal disease patients (CLCR < 10 mL/min) and patients undergoing hemodialysis should not receive Levocetirizine dihydrochloride (Montek-LC).

No dose adjustment is needed in patients with solely hepatic impairment. In patients with both hepatic impairment and renal impairment, adjustment of the dose is recommended.

How supplied

Dosage Forms And Strengths

Levocetirizine dihydrochloride (Montek-LC) oral solution is a clear, colorless liquid containing 0.5 mg of Levocetirizine dihydrochloride (Montek-LC) per mL.

Levocetirizine dihydrochloride (Montek-LC) tablets are white, film-coated, oval-shaped, scored, imprinted (with the letter Y in red color on both halves of the scored tablet) and contain 5 mg Levocetirizine dihydrochloride (Montek-LC).

Storage And Handling

Levocetirizine dihydrochloride (Montek-LC) tablets are white, film-coated, oval-shaped, scored, imprinted (with the letter Y in red color on both halves of the scored tablet) and contain 5 mg Levocetirizine dihydrochloride (Montek-LC). They are supplied in unit of use HDPE bottles.

90 Tablets (NDC 50474-920-90)

Levocetirizine dihydrochloride (Montek-LC) oral solution is a clear, colorless liquid containing 0.5 mg of Levocetirizine dihydrochloride (Montek-LC) per mL.

Oral Solution in 5 oz polypropylene bottles (

Storage

Store at 20 to 25°C (68 to 77°F); excursions permitted to 15 to 30°C (59 to 86°F).

Manufactured for: UCB, Inc., Smyrna, GA 30080. Revised: June 2016

Chewable Tablet 4-mg: Children 2 to 5 years: One 4 mg chewable tablet daily to be taken in the evening. Montelukast (Montek-LC) 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.

Montelukast (Montek-LC) 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. Montelukast (Montek-LC) 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.

Montelukast (Montek-LC) 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 Montelukast (Montek-LC) Sandoz Chewable Tablet, be sure that he/she does not take any other medicines that contain the same active ingredient, i.e. Montelukast (Montek-LC).

If the child takes more Montelukast (Montek-LC) Sandoz Chewable Tablet than he/she should, contact the child’s physician immediately for advice.

Discontinuation of Treatment: Montelukast (Montek-LC) 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 Montelukast (Montek-LC) 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 Montelukast (Montek-LC) Sandoz Film-Coated Tab 10 mg on parameters of asthma control occurs within one day. Montelukast (Montek-LC) Sandoz Film-Coated Tab 10 mg may be taken with or without food. Patients should be advised to continue taking Montelukast (Montek-LC) Sandoz even if asthma is under control, as well as during periods of worsening asthma.

Montelukast (Montek-LC) Sandoz Film-Coated Tab 10 mg should not be used concomitantly with other products containing the same active ingredient, Montelukast (Montek-LC).

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 Montelukast (Montek-LC) 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. Montelukast (Montek-LC) Sandoz Film-Coated Tab 10 mg should not be subtituted for inhaled corticosteriods.

Montelukast (Montek-LC) 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 Levocetirizine dihydrochloride (Montek-LC)?

The use of Levocetirizine dihydrochloride (Montek-LC) tablets is contraindicated in:

Patients With Known Hypersensitivity

Patients with known hypersensitivity to Levocetirizine dihydrochloride (Montek-LC) or any of the ingredients of Levocetirizine dihydrochloride (Montek-LC) tablets, or to cetirizine. Observed reactions range from urticaria to anaphylaxis.

Patients With End-Stage Renal Disease

Patients with end-stage renal disease (CLCR < 10 mL/min) and patients undergoing hemodialysis.

Pediatric Patients With Impaired Renal Function

Children 6 months to 11 years of age with impaired renal function.

See also:
What is the most important information I should know about Montelukast (Montek-LC)?

Hypersensitivity to Montelukast (Montek-LC) sodium or to any of the excipients of Montelukast (Montek-LC).

Use in children: Montelukast (Montek-LC) should not be used in children <15 years due to high content of Montelukast (Montek-LC). Other dosage forms with appropriate strengths are available for younger children.

Use Levocetirizine dihydrochloride (Montek-LC) as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Take Levocetirizine dihydrochloride (Montek-LC) by mouth with or without food. Take it in the evening unless your doctor tells you otherwise.
• Use a measuring device marked for medicine dosing. Ask your pharmacist for help if you are unsure of how to measure your dose.
• If you miss a dose of Levocetirizine dihydrochloride (Montek-LC), take it as soon as possible. If it is almost time for your next dose, 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 Levocetirizine dihydrochloride (Montek-LC).

Use Montelukast (Montek-LC) granules as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• An extra patient leaflet is available with Montelukast (Montek-LC) granules. Talk to your pharmacist if you have questions about this information.
• Take Montelukast (Montek-LC) granules by mouth with or without food.
• Do not open the packet until you are ready to use it.
• Montelukast (Montek-LC) 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 Montelukast (Montek-LC) granules even if you feel well. Do not miss any doses.
• If you miss a dose of Montelukast (Montek-LC) 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 Montelukast (Montek-LC) granules.

Levocetirizine dihydrochloride (Montek-LC) is used to treat symptoms of allergic conditions such as allergic fever (hay fever), year-round allergies like dust or pet allergies and chronic nettle rash.

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 Montelukast (Montek-LC) use as first-line therapy for allergic rhinitis (except in patients with concurrent asthma) (Dykewicz 2017; Seidman 2015). The Global Initiative for Asthma recommends Montelukast (Montek-LC) 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 Montelukast (Montek-LC) 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 Montelukast (Montek-LC) and cetirizine in patients with chronic urticaria and intolerance to food additives and/or aspirin supports the use of Montelukast (Montek-LC) in the treatment of patients experiencing urticaria related to the use of nonsteroidal anti-inflammatory drugs.

See also:
What other drugs will affect Levocetirizine dihydrochloride (Montek-LC)?

No interaction studies have been performed with Levocetirizine dihydrochloride (Montek-LC) (including no studies with CYP3A4 inducers); studies with the racemate compound cetirizine demonstrated that there were no clinically relevant adverse interactions (with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam).

Theophylline: A small decrease in the clearance of cetirizine (16%) was observed in a multiple dose study with theophylline (400 mg once a day); while the disposition of theophylline was not altered by concomitant cetirizine administration.

Ritonavir: In a multiple dose study of ritonavir (600 mg twice daily) and cetirizine (10 mg daily), the extent of exposure to cetirizine was increased by about 40% while the disposition of ritonavir was slightly altered (-11%) further to concomitant cetirizine administration.

Food: The extent of absorption of Levocetirizine dihydrochloride (Montek-LC) is not reduced with food, although the rate of absorption is decreased.

Alcohol: In sensitive patients the simultaneous administration of cetirizine or Levocetirizine dihydrochloride (Montek-LC) and alcohol or other CNS depressants may have effects on the central nervous system, although it has been shown that the racemate cetirizine does not potentiate the effect of alcohol.

See also:
What other drugs will affect Montelukast (Montek-LC)?

Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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 Montelukast (Montek-LC) 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 Montelukast (Montek-LC) was decreased approximately 40% in subjects with co-administration of phenobarbital. No dosage adjustment for Montelukast (Montek-LC) (Montelukast (Montek-LC)) is recommended.

In vitro studies have shown that Montelukast (Montek-LC) is an inhibitor of CYP2C8. However, data from a clinical drug-drug interaction study involving Montelukast (Montek-LC) and rosiglitazone (a probe substrate representative of drugs primarily metabolized by CYP2C8) demonstrated that Montelukast (Montek-LC) does not inhibit CYP2C8 in vivo. Therefore, Montelukast (Montek-LC) 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 Montelukast (Montek-LC) is a substrate of CYP 2C8, 2C9, and 3A4. Data from a clinical drug-drug interaction study involving Montelukast (Montek-LC) and gemfibrozil (an inhibitor of both CYP 2C8 and 2C9) demonstrated that gemfibrozil increased the systemic exposure of Montelukast (Montek-LC) by 4.4-fold.

Co-administration of itraconazole, a strong CYP 3A4 inhibitor, with gemfibrozil and Montelukast (Montek-LC) did not further increase the systemic exposure of Montelukast (Montek-LC). The effect of gemfibrozil on systemic exposure of Montelukast (Montek-LC) 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 Montelukast (Montek-LC) 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 Montelukast (Montek-LC) with itraconazole alone resulted in no significant increase in the systemic exposure of Montelukast (Montek-LC).

See also:
What are the possible side effects of Levocetirizine dihydrochloride (Montek-LC)?

Use of Levocetirizine dihydrochloride (Montek-LC) has been associated with somnolence, fatigue, asthenia, and urinary retention.

Clinical Trials Experience

The safety data described below reflect exposure to Levocetirizine dihydrochloride (Montek-LC) in 2708 patients with seasonal or perennial allergic rhinitis or chronic idiopathic urticaria in 14 controlled clinical trials of 1 week to 6 months duration.

The short-term (exposure up to 6 weeks) safety data for adults and adolescents are based upon eight clinical trials in which 1896 patients (825 males and 1071 females aged 12 years and older) were treated with Levocetirizine dihydrochloride (Montek-LC) 2.5, 5, or 10 mg once daily in the evening.

The short-term safety data from pediatric patients are based upon two clinical trials in which 243 children with seasonal or perennial allergic rhinitis (162 males and 81 females 6 to 12 years of age) were treated with Levocetirizine dihydrochloride (Montek-LC) 5 mg once daily for 4 to 6 weeks, one clinical trial in which 114 children (65 males and 49 females 1 to 5 years of age) with allergic rhinitis or chronic idiopathic urticaria were treated with Levocetirizine dihydrochloride (Montek-LC) 1.25 mg twice daily for 2 weeks, and one clinical trial in which 45 children (28 males and 17 females 6 to 11 months of age) with symptoms of allergic rhinitis or chronic urticaria were treated with Levocetirizine dihydrochloride (Montek-LC) 1.25 mg once daily for 2 weeks.

The long-term (exposure of 4 or 6 months) safety data in adults and adolescents are based upon two clinical trials in which 428 patients (190 males and 238 females) with allergic rhinitis were exposed to treatment with Levocetirizine dihydrochloride (Montek-LC) 5 mg once daily. Long term safety data are also available from an 18-month trial in 255 Levocetirizine dihydrochloride (Montek-LC)-treated subjects 12 to 24 months of age.

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trial of another drug and may not reflect the rates observed in practice.

Adults and Adolescents 12 Years of Age and Older

In studies up to 6 weeks in duration, the mean age of the adult and adolescent patients was 32 years, 44% of the patients were men and 56% were women, and the large majority (more than 90%) was Caucasian.

In these trials 43% and 42% of the subjects in the Levocetirizine dihydrochloride (Montek-LC) 2.5 mg and 5 mg groups, respectively, had at least one adverse event compared to 43% in the placebo group.

In placebo-controlled trials of 1 to 6 weeks in duration, the most common adverse reactions were somnolence, nasopharyngitis, fatigue, dry mouth, and pharyngitis, and most were mild to moderate in intensity. Somnolence with Levocetirizine dihydrochloride (Montek-LC) showed dose ordering between tested doses of 2.5, 5 and 10 mg and was the most common adverse reaction leading to discontinuation (0.5%).

Table 1 lists adverse reactions that were reported in greater than or equal to 2% of subjects aged 12 years and older exposed to Levocetirizine dihydrochloride (Montek-LC) 2.5 mg or 5 mg in eight placebo-controlled clinical trials and that were more common with Levocetirizine dihydrochloride (Montek-LC) than placebo.

Additional adverse reactions of medical significance observed at a higher incidence than in placebo in adults and adolescents aged 12 years and older exposed to Levocetirizine dihydrochloride (Montek-LC) are syncope (0.2%) and weight increased (0.5%).

Pediatric Patients 6 to 12 Years of Age

A total of 243 pediatric patients 6 to 12 years of age received Levocetirizine dihydrochloride (Montek-LC) 5 mg once daily in two short-term placebo controlled double-blind trials. The mean age of the patients was 9.8 years, 79 (32%) were 6 to 8 years of age, and 50% were Caucasian. Table 2 lists adverse reactions that were reported in greater than or equal to 2% of subjects aged 6 to 12 years exposed to Levocetirizine dihydrochloride (Montek-LC) 5 mg in placebo-controlled clinical trials and that were more common with Levocetirizine dihydrochloride (Montek-LC) than placebo.

Pediatric Patients 1 to 5 Years of Age

A total of 114 pediatric patients 1 to 5 years of age received Levocetirizine dihydrochloride (Montek-LC) 1.25 mg twice daily in a two week placebo-controlled double-blind safety trial. The mean age of the patients was 3.8 years, 32% were 1 to 2 years of age, 71% were Caucasian and 18% were Black. Table 3 lists adverse reactions that were reported in greater than or equal to 2% of subjects aged 1 to 5 years exposed to Levocetirizine dihydrochloride (Montek-LC) 1.25 mg twice daily in the placebo-controlled safety trial and that were more common with Levocetirizine dihydrochloride (Montek-LC) than placebo.

Pediatric Patients 6 to 11 Months of Age

A total of 45 pediatric patients 6 to 11 months of age received Levocetirizine dihydrochloride (Montek-LC) 1.25 mg once daily in a two week placebo-controlled double-blind safety trial. The mean age of the patients was 9 months, 51% were Caucasian and 31% were Black. Adverse reactions that were reported in more than 1 subject (i.e. greater than or equal to 3% of subjects) aged 6 to 11 months exposed to levoceterizine dihydrochloride 1.25 mg once daily in the placebo-controlled safety trial and that were more common with levoceterizine dihydrochloride than placebo included diarrhea and constipation which were reported in 6 (13%) and 1 (4%) and 3 (7%) and 1 (4%) children in the Levocetirizine dihydrochloride (Montek-LC) and placebo-treated groups, respectively.

Long-Term Clinical Trials Experience

In two controlled clinical trials, 428 patients (190 males and 238 females) aged 12 years and older were treated with Levocetirizine dihydrochloride (Montek-LC) 5 mg once daily for 4 or 6 months. The patient characteristics and the safety profile were similar to that seen in the short-term studies. Ten (2.3%) patients treated with Levocetirizine dihydrochloride (Montek-LC) discontinued because of somnolence, fatigue or asthenia compared to 2 (< 1%) in the placebo group.

There are no long term clinical trials in children below 12 years of age with allergic rhinitis or chronic idiopathic urticaria.

Laboratory Test Abnormalities

Elevations of blood bilirubin and transaminases were reported in < 1% of patients in the clinical trials. The elevations were transient and did not lead to discontinuation in any patient.

Postmarketing Experience

In addition to the adverse reactions reported during clinical trials and listed above, adverse events have also been identified during post-approval use of Levocetirizine dihydrochloride (Montek-LC). Because these events are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Adverse events of hypersensitivity and anaphylaxis, increased appetite, angioedema, fixed drug eruption, pruritus, rash and urticaria, convulsion, paraesthesia, dizziness, tremor, dysgeusia, vertigo, movement disorders (including dystonia and oculogyric crisis), aggression and agitation, hallucinations, depression, insomnia, suicidal ideation, visual disturbances, blurred vision, palpitations, tachycardia, dyspnea, nausea, vomiting, hepatitis, dysuria, urinary retention, myalgia, and edema have been reported.

Besides these events reported under treatment with Levocetirizine dihydrochloride (Montek-LC), other potentially severe adverse events have been reported from the postmarketing experience with cetirizine. Since Levocetirizine dihydrochloride (Montek-LC) is the principal pharmacologically active component of cetirizine, one should take into account the fact that the following adverse events could also potentially occur under treatment with Levocetirizine dihydrochloride (Montek-LC): orofacial dyskinesia, severe hypotension, cholestasis, glomerulonephritis, still birth, tic, myoclonus, and extrapyramidal symptoms.

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What are the possible side effects of Montelukast (Montek-LC)?

Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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 Montelukast (Montek-LC) (Montelukast (Montek-LC)) was comparable to placebo.

Adults 15 Years of Age and Older with Asthma: Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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 Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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 Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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: Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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 Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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 Montelukast (Montek-LC) (Montelukast (Montek-LC)).

Cumulatively, 263 pediatric patients 6 to 14 years of age were treated with Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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: Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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 Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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 Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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: Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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 Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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: Montelukast (Montek-LC) (Montelukast (Montek-LC)) has been evaluated in 2199 adult patients 15 years of age and older for the treatment of seasonal allergic rhinitis in clinical studies. Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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 Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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: Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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. Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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 Montelukast (Montek-LC) (Montelukast (Montek-LC)) and at a greater incidence than in patients treated with placebo were observed.

Adults 15 Years of Age and Older with Perennial Allergic Rhinitis: Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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.

Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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 Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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 Montelukast (Montek-LC) (Montelukast (Montek-LC)) and 7780 patients who received placebo in these studies, there was one patient with suicidal ideation in the group taking Montelukast (Montek-LC) (Montelukast (Montek-LC)). 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 Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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 Montelukast (Montek-LC) (Montelukast (Montek-LC)) 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.