Dosing & Uses
Dosage Forms & Strengths
olopatadine/mometasone
intranasal spray
- (665mcg/25mcg)/spray
Seasonal Allergic Rhinitis
Indicated for symptoms of seasonal allergic rhinitis
2 sprays per nostril BID
Dosage Modifications
Hepatic impairment
- Not studied; however, increasing concentrations of mometasone have been reported with severity of hepatic impairment
Renal impairment
- Mometasone: Not studied
-
Olopatadine
- Mild, moderate, or severe (single dose): No change in peak plasma concentration for single dose
- Severe (CrCl <30 mL/min/1.73 m2) at steady-state: AUC 2-fold higher and peak plasma concentration ~10-fold higher
Dosage Forms & Strengths
olopatadine/mometasone
intranasal spray
- (665mcg/25mcg)/spray
Seasonal Allergic Rhinitis
Indicated for symptoms of seasonal allergic rhinitis in adult and pediatric patients aged ≥12 years
<12 years: Safety and efficacy not established
≥12 years: 2 sprays per nostril BID
Dosage Modifications
Hepatic impairment
- Not studied; however, increasing concentrations of mometasone have been reported with severity of hepatic impairment
Renal impairment
- Mometasone: Not studied
-
Olopatadine
- Mild, moderate, or severe (single dose): No change in peak plasma concentration for single dose
- Severe (CrCl <30 mL/min/1.73 m2) at steady-state: AUC 2-fold higher and peak plasma concentration ~10-fold higher
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (1)
- desmopressin
mometasone, intranasal increases toxicity of desmopressin by Other (see comment). Contraindicated. Comment: Increases risk of severe hyponatremia.
Serious - Use Alternative (0)
Monitor Closely (19)
- atazanavir
atazanavir will increase the level or effect of mometasone, intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ceritinib
mometasone, intranasal increases toxicity of ceritinib by Other (see comment). Modify Therapy/Monitor Closely. Comment: May increase risk of hyperglycemia.
- clarithromycin
clarithromycin will increase the level or effect of mometasone, intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- clobazam
olopatadine intranasal, clobazam. Other (see comment). Use Caution/Monitor. Comment: Concomitant administration can increase the potential for CNS effects (e.g., increased sedation or respiratory depression).
- cobicistat
cobicistat will increase the level or effect of mometasone, intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- darunavir
darunavir will increase the level or effect of mometasone, intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF will increase the level or effect of mometasone, intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- idelalisib
idelalisib will increase the level or effect of mometasone, intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- indinavir
indinavir will increase the level or effect of mometasone, intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- itraconazole
itraconazole will increase the level or effect of mometasone, intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ketoconazole
ketoconazole will increase the level or effect of mometasone, intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- levoketoconazole
levoketoconazole will increase the level or effect of mometasone, intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lopinavir
lopinavir will increase the level or effect of mometasone, intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- mifepristone
mifepristone will increase the level or effect of mometasone, intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nefazodone
nefazodone will increase the level or effect of mometasone, intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nelfinavir
nelfinavir will increase the level or effect of mometasone, intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC)
ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC) will increase the level or effect of mometasone, intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- oxymetazoline intranasal
oxymetazoline intranasal, olopatadine intranasal. Other (see comment). Modify Therapy/Monitor Closely. Comment: Oxymetazoline has been known to slow the rate, but not affect the extent of absorption of concomitantly administered intranasal products. Do not administer other intranasal products with oxymetazoline intranasal.
- posaconazole
posaconazole will increase the level or effect of mometasone, intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
Minor (0)
Adverse Effects
1-10%
Dysgeusia (3%)
Epistaxis (1%)
Nasal discomfort (1%)
Warnings
Contraindications
Hypersensitivity to any ingredients of nasal spray
Cautions
May cause somnolence; avoid operating heavy machinery or engaging in tasks that require mental alertness and coordination; caution patients against engaging in hazardous occupations requiring complete mental alertness and motor coordination (eg, operating machinery, driving a motor vehicle) after administration
Avoid concurrent use with alcohol or other central nervous system (CNS) depressants; additional reductions in alertness and additional impairment of CNS performance may occur
Glaucoma and/or cataracts may develop; closely monitor patients with vision changes or history of increased intraocular pressure, glaucoma, and/or cataracts
Hypersensitivity reactions, including wheezing, have occurred after nasal administration of mometasone; discontinue therapy if such reactions occur
Nasal corticosteroids may cause reduction in growth velocity when administered to pediatric patients; routinely monitor growth of pediatric patients; safety and efficacy not established in pediatric patients aged <12 years; not indicated for use in this population
Hypercorticism and adrenal suppression may occur when nasal corticosteroids are misused by taking higher-than-recommended dosages or in patients at risk for such effects
Local nasal adverse reactions
- Epistaxis, nasal ulceration, and nasal septal perforation reported
- Periodically monitor for signs of adverse effects on nasal mucosa
- Corticosteroids may impair wound healing; avoid use in patients who have experienced recent nasal septal ulcers, nasal surgery, or nasal trauma until resolved
- Localized Candida infections of the nose and pharynx have occurred from mometasone intranasal; if infection occurs, discontinue therapy, and treat appropriately; examine periodically for evidence of Candida infection if use is over several months or longer
Immunosuppression and risk of infections
- Immunosuppressive drugs (eg, corticosteroids) may increase susceptibility to infection
- Chickenpox and measles may be more serious or even fatal in susceptible children or adults using corticosteroids
- Risk of developing an infection based on therapy (ie, dose, duration, route), underlying disease, and/or prior corticosteroid use is unknown
- If exposed to chickenpox, prophylaxis with varicella zoster immune globulin may be indicated; if exposed to measles, prophylaxis with pooled IM immunoglobulin may be indicated; if chickenpox develops, consider treating with antiviral agents
- Use with caution in active or quiescent tuberculous infections of the respiratory tract, untreated local or systemic fungal or bacterial infections, systemic viral or parasitic infections, or ocular herpes simplex
Drug interaction overview
-
CNS depressants
- Avoid coadministration
- Alcohol and other CNS depressants may potentiate somnolence and CNS depression
-
Strong CYP3A4 inhibitors
- Use with caution
- Strong CYP3A4 inhibitors may inhibit metabolism of, and increase mometasone furoate plasma concentration, and potentially increase risk for adverse reactions
Pregnancy & Lactation
Pregnancy
Data are unavailable on use in pregnant females to evaluate for drug-associated risks of major birth defects, miscarriage, or other adverse maternal or fetal outcomes
Animal data
- Olopatadine: Oral administration of olopatadine to pregnant rats and rabbits caused a decrease in number of live fetuses at maternal doses 120x and 1600x the maximum recommended human daily intranasal dose (MRHDID) on a mg/m2 basis, respectively
- Mometasone: Administration of mometasone to pregnant rats and rabbits caused increased fetal malformations and decreased fetal survival and growth at doses that produced exposures 1-16x the MRHDID on a mcg/m2 or AUC basis
Lactation
Data are unavailable on presence of drug in human milk, effects on breastfed children, or on milk production
Other corticosteroids are excreted in human milk
Olopatadine has been identified in milk of nursing rats following oral administration; unknown whether topical nasal administration could result in sufficient systemic absorption to produce detectable quantities in human breast milk
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Olopatadine: Antihistamine (H1 antagonist); inhibits release of histamine from mast cells
Mometasone: Corticosteroid with potent anti-inflammatory properties; elicits effects on various cells, including mast cells and eosinophils; also elicits effects on inflammatory mediators (eg, histamine, eicosanoids, leukotrienes, cytokines)
Absorption
Peak plasma time: 1 hr
Peak plasma concentration
- Olopatadine: 19.8 ng/mL
- Mometasone: 9.92 pg/mL
AUC
- Olopatadine: 88.77 ng·hr/mL
- Mometasone: 58.4 pg·hr/mL
Distribution
Protein bound
- Olopatadine: 55% (binds primarily to serum albumin)
- Mometasone: 98-99%
Metabolism
Olopatadine
- Not extensively metabolized
- Metabolites: Olopatadine N-oxide and N-desmethyl olopatadine; at least 6 minor metabolites circulate in human plasma
Mometasone
- Metabolized by CYP3A4
- Metabolites: No major metabolites detectable in plasma; 6ß-hydroxy-mometasone furoate (minor metabolite)
Elimination
Half-life
- Olopatadine: 9 hr
- Mometasone: 18 hr
Excretion
- Olopatadine: 70% (urine [86% unchanged]); 17% (feces)
- Any absorbed drug is excreted as metabolites mostly via the bile, and to a limited extent, into the urine
Administration
Intranasal Preparation
Priming
- Shake bottle gently before each use
- Prime bottle before initial use by releasing 6 sprays
- Reprime bottle if unused for >14 days by spraying 2 sprays or until fine mist appears
Intranasal Administration
Gently blow nose to clear nostrils
Administer by intranasal route only
Hold 1 nostril closed with finger and insert spray pump tip into other nostril, pointing it slightly toward outside of nose, away from nasal septum
Avoid spraying into eyes or mouth
Do not blow nose for at least 15 minutes after administration
Storage
Store upright with dust cap on at room temperature (20-25ºC [68-77ºF]; excursions permitted at 15-30ºC [59-86ºF])
Do not freeze or refrigerate
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Formulary
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