Olopatadine/ Mometasone Furoate

Registered South African indications:

• Symptoms associated with allergic rhinitis and rhinoconjunctivitis

Registered South African contraindications

• Hypersensitivity to the active ingredient or to any of the excipients in this combination product
• Pregnancy
• Breastfeeding
• Immunisation with live viral/bacterial vaccines
• Active or quiescent Mycobacterium tuberculosis infections
• Untreated local or systemic fungal or bacterial infections, systemic viral or parasitic infections irrespective of anatomical site

South African recommendations

Hypersensitivity reactions

• Hypersensitivity reactions, including wheezing, may occur after intranasal administration of mometasone furoate monohydrate. Discontinuation of the medicine is required if such reactions occur

Immunosuppression

• Olopatadine/ mometasone furoate may suppress the immune system, patients are more susceptible to infections. Prophylaxis (with varicella zoster immune globulin (VZIG) or immunoglobulin (IG)) may be indicated after exposure to chickenpox or measles, respectively
• The medication should not be used in patients with active or quiescent tuberculous infections, untreated local or systemic fungal or bacterial infections, systemic viral or parasitic infections, or ocular herpes simplex due to the risk of worsening these infections
• Caution is also advised in patients with HIV infection

Hypothalamic-pituitary-adrenal (HPA) axis effects

• Systemic corticosteroid effects, such as hypercorticism and adrenal suppression, may occur with intranasal steroids, particularly with higher-than-recommended dosages or in susceptible individuals at recommended dosages
• Be alert for evidence of systemic effects, especially in chronically treated patients
• Caution is required when transferring patients from systemic steroids to olopatadine/mometasone furoate if adrenal function is impaired. Patients being transferred may experience symptoms of withdrawal (e.g. joint/muscle pain, depression) or unmasking of previously suppressed allergic conditions

Local nasal effects

• Adverse events reported include nasal ulceration, nasal septal perforation, and epistaxis
• Due to the inhibitory effect of corticosteroids on wound healing, patients with recent nasal septal ulcers, nasal surgery, or nasal trauma should avoid using olopatadine/mometasone furoate until healing is complete
• Localised infections of the nose and pharynx with Candida albicans may occur, potentially requiring appropriate local therapy and discontinuation of the medicine

Glaucoma and cataracts

• The use of nasal corticosteroids may lead to the development of glaucoma and/or cataracts. Close monitoring is warranted for patients with a change in vision or with a history of increased intraocular pressure, glaucoma, and/or cataracts

Effect on growth

• Intranasal corticosteroids, such as those in olopatadine/mometasone furoate, may cause a reduction in growth velocity when administered to patients less than 18 years of age. The growth of paediatric patients receiving this medication should be monitored

Somnolence

• Somnolence (drowsiness) has been reported. The concurrent use of olopatadine/mometasone furoate with alcohol or other central nervous system (CNS) depressants should be avoided as it may cause additional reductions in alertness and further impairment of CNS performance

Paediatric use

• The safety and effectiveness of olopatadine/mometasone furoate have not been established in patients below the age of 6 years. Safety in children aged 6 to 11 years has not been studied beyond 2 weeks of use or in perennial allergic rhinitis
• Due to the risk of retardation of growth rate with intranasal corticosteroids, particularly at high doses for prolonged periods, the growth of paediatric patients must be routinely monitored. For the 6 to 11 age group, clinical review, the pursuit of the lowest effective dose, and consideration of adjunctive treatment are recommended

Effects on ability to drive and use machines

• Olopatadine/ mometasone furoate may cause side effects such as somnolence and dizziness
• Patients should be cautioned against engaging in hazardous activities requiring complete mental alertness and motor coordination, such as operating machinery or driving a motor vehicle, after administration of olopatadine/ mometasone furoate

Forms avail. in SA and covered in this monograph: nas

South African registered indications and dosages

Symptoms associated with allergic rhinitis and rhinoconjunctivitis

Olopatadine/ Mometasone Furoate
600/25 (µg)

• Nasal (nas): 2 sprays per nostril, twice dly

Method of administration: Shake the bottle well before each use; prime olopatadine/mometasone furoate nasal spray before initial use by releasing 6 sprays; If olopatadine/mometasone furoate has not been used for 14 days or more, re-prime by releasing 2 sprays or until a fine mist appears. See Additional Prescriber Points for Instruction for use

Avoid spraying into the eyes or mouth. Administer by the intranasal route only

Paed. forms avail. in SA and covered in this monograph: nas

South African registered indications and dosages

Symptoms associated with allergic rhinitis and rhinoconjunctivitis

Olopatadine/ Mometasone Furoate
600/25 (µg)

Nasal (nas)

• Younger than 6 years: Not established for use
• Between 6-11 years: 1 spray per nostril, twice dly; Treatment duration: Safety beyond 2 weeks of use or in perennial allergic rhinitis has not been assessed
• 12 years and older: See adult dosage

Periodic clinical review, pursuit of lowest effective dosing, and consideration of adjunctive treatment modalities are recommended in paediatric patients aged 6 to 11 years

Method of administration: Shake the bottle well before each use; prime olopatadine/mometasone furoate nasal spray before initial use by releasing 6 sprays; If olopatadine/mometasone furoate has not been used for 14 days or more, re-prime by releasing 2 sprays or until a fine mist appears. See Additional Prescriber Points for Instruction for use

Avoid spraying into the eyes or mouth. Administer by the intranasal route only

Pregnancy

South African recommendations

• Contraindicated
• Animal studies have revealed evidence of embryo-foetal toxicity and malformations

Breastfeeding

South African recommendations

• Contraindicated
• Olopatadine/ mometasone furoate is not for use by mothers who are breastfeeding their infants. Corticosteroids such as mometasone furoate are excreted in breast milk

Fertility

South African recommendations

• No information available

South African recommendations

• No dose adjustment recommended
  Based on data from the individual components, no adjustment of the dosing regimen of the nasal spray formulation is warranted in patients with renal impairment

South African recommendations

• No dose adjustment recommended
  Based on data from the individual components, no adjustment of the dosing regimen of the nasal spray formulation is warranted in patients with hepatic impairment

South African recommendations

• No dose adjustment recommended
  No overall differences in safety or efficacy were observed in data collected from 145 patients aged 65 years and older versus younger patients who were treated with the nasal spray formulation in placebo and active-controlled studies

Infections and Infestations

Uncommon

• Pharyngitis
• Respiratory tract infection

Nervous System Disorders

Common

• Dysgeusia (unpleasant taste)

Uncommon

• Dizziness
• Lethargy
• Somnolence
• Anxiety
• Insomnia

Respiratory, Thoracic and Mediastinal Disorders

Uncommon

• Cough
• Nasal dryness
• Nasal discomfort
• Throat irritation
• Wheezing

Gastrointestinal Disorders

Uncommon

• Dry mouth
• Abdominal discomfort
• Vomiting

Skin and Subcutaneous Tissue Disorders

Uncommon

• Rash
• Pruritus
• Contact dermatitis

Adverse reactions related to local corticosteroid use may occur:

• Nasal ulcerations
• Nasal septal perforations
• Epistaxis
• Impaired wound healing
• Candida albicans infection
• Glaucoma and cataracts
• Immunosuppression
• HPA axis effects, including growth reduction

Olopatadine/ Mometasone Furoate

• Immunisation with live viral/bacterial vaccines

Mometasone furoate

• Ketoconazole (potent CYP3A4 inhibitor)

• Eye examination
  - Monitor patients with a change in vision or a history of increased intraocular pressure, glaucoma, and/or cataracts. The use of nasal corticosteroids may lead to the development of glaucoma and/or cataracts

Additional Observations

• Hypothalamic-Pituitary-Adrenal (HPA) axis effect
  - Be alert for evidence of systemic corticosteroid effects, such as hypercorticism and adrenal suppression, especially in chronically treated patients or susceptible individuals using higher-than-recommended dosages
• Growth
  - Monitor the growth of paediatric patients less than 18 years of age receiving intranasal corticosteroids, including olopatadine/ mometasone furoate
• Hypersensitivity reactions
  - Monitor for hypersensitivity reactions, including wheezing. Olopatadine/ mometasone furoate should be discontinued if such reactions occur

Instructions for use 

• Shake the bottle before use and remove the purple plastic over cap from the spray pump tip of the bottle
• To prime the olopatadine/ mometasone furoate pump before first use, hold the nasal spray bottle firmly and upright with your index and middle finger on either side of the applicator (on finger rests) while supporting the grooved base of the bottle with your thumb. Push down on the pump quickly and firmly 6 times, releasing the spray into the air, away from the eyes and face, until a fine mist appears
• If the nasal spray is not used for 14 days, the bottle will need to be shaken and the pump primed with 2 sprays or until a fine mist appears. It is now ready for use
• Gently blow the nose to clear the nostrils
• Hold the bottle firmly with the index and middle finger on either side of the applicator (on finger rests) while supporting the grooved base of the bottle with the thumb
• Close 1 nostril with a finger, insert the end of the nasal tip into the other nostril, while pointing it slightly toward the outside of the nose, away from the nasal septum
• Tilt the head forward slightly. Keep the bottle upright and press down once quickly and firmly on the finger rests to activate the pump. Breathe in gently through the nose as you spray. Then breath out through your mouth. Try not to get any spray in the eyes or directly on your nasal septum
• Repeat the above steps 4-6 and deliver a second spray in the same nostril
• Repeat with 2 sprays in the other nostril
• Avoid blowing your nose for the next 15 minutes
• Do not tip your head back right after using to prevent nasal solution from going into your throat. After use, wipe the tip with a clean dry tissue or cloth
• Push the purple over cap back on the spray tip of the bottle until a noticeable click sound is heard
• Each bottle of olopatadine/ mometasone furoate contains enough medicine for 7 or 14 days of regular use depending on the pack size (56 or 120 sprays after priming)
• The bottle should be discarded after 30 days of use or upon expiration

Olopatadine
Olopatadine is a histamine H1 receptor antagonist.

Mometasone furoate
Mometasone furoate is a corticosteroid with anti-inflammatory properties. The precise mechanism of corticosteroid action on allergic rhinitis is not known. Corticosteroids have been shown to have a wide range of effects on multiple cell types (e.g. mast cells, eosinophils, neutrophils, macrophages, and lymphocytes) and mediators (e.g. histamine, eicosanoids, leukotrienes, and cytokines) involved in inflammation.