DULERA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DULERA (DULERA).
DULERA is a combination of formoterol fumarate, a long-acting beta2-adrenergic agonist (LABA), and mometasone furoate, a corticosteroid. Formoterol acts by relaxing bronchial smooth muscle via beta2-receptor activation. Mometasone furoate reduces inflammation in the lungs by inhibiting inflammatory mediators and suppressing immune responses.
| Metabolism | Mometasone furoate is extensively metabolized via CYP3A4 to multiple metabolites. Formoterol is primarily metabolized by direct glucuronidation and O-demethylation via CYP2D6 and CYP2C19, but CYP3A4 and CYP2C9 also contribute. |
| Excretion | Formoterol: 10-15% renal as unchanged drug and metabolites, remainder hepatically cleared; Mometasone: >99% biliary/fecal as metabolites, <1% renal unchanged. |
| Half-life | Formoterol: terminal half-life 10-14 hours (supports twice-daily dosing); Mometasone: terminal half-life 13.8 hours (range 10-20 hours) after inhalation. |
| Protein binding | Formoterol: 61-64% bound to albumin; Mometasone: 98-99% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Formoterol: 3.4-4.5 L/kg; Mometasone: 332-580 L (not corrected for weight; corresponds to extensive tissue distribution). |
| Bioavailability | Inhalation: Formoterol systemic bioavailability ~10-18%; Mometasone systemic bioavailability <1% due to extensive first-pass metabolism and low lung absorption. |
| Onset of Action | Formoterol: bronchodilation within 1-3 minutes; Mometasone: no acute bronchodilator effect, clinical improvement over days to weeks. |
| Duration of Action | Formoterol: bronchodilation lasting 12 hours (twice-daily dosing); Mometasone: sustained anti-inflammatory effect with regular use, maximal benefit after 1-2 weeks. |
| Molecular Weight | 430.53 |
| Action Class | Corticosteroid/Beta2-Agonist Combination |
Inhalation: 2 inhalations twice daily (morning and evening). Each inhalation delivers mometasone furoate 100/200 mcg and formoterol fumarate 5 mcg.
| Dosage form | AEROSOL, METERED |
| Renal impairment | No specific dose adjustment required for renal impairment based on GFR. |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh C). For moderate impairment (Child-Pugh B), use with caution; no specific dose adjustment defined, but monitor for systemic effects. |
| Pediatric use | Approved for children 12 years and older: Same as adult dose. For children <12 years, safety and efficacy not established. |
| Geriatric use | No specific dose adjustment. Use lowest effective dose due to potential for increased sensitivity and comorbidities. |
| 1st trimester | Data are insufficient to determine risk; use only if benefit outweighs risk. |
| 2nd trimester | No known teratogenic effects; use if clearly needed. |
| 3rd trimester | May cause fetal tachycardia or hypoglycemia with high doses; use with caution. |
Clinical note
Comprehensive clinical and safety monograph for DULERA (DULERA).
| Placental transfer | Both formoterol and budesonide cross the placenta. Budesonide is extensively metabolized, reducing fetal exposure. Formoterol has limited data but likely crosses. |
| Breastfeeding | Excretion into breast milk is likely minimal; however, systemic corticosteroids can be detected. Use with caution, especially with high doses or prolonged treatment. |
| Lactation Rating |
■ FDA Black Box Warning
LABA increase the risk of asthma-related death. When used without an inhaled corticosteroid, LABA are contraindicated in asthma. DULERA should only be used in patients not adequately controlled on a long-term asthma controller medication or whose disease severity warrants initiation of both an inhaled corticosteroid and LABA.
| Common Effects | Nasopharyngitis, Headache, Upper respiratory tract infection, Sinusitis, Throat irritation, Cough, Dysphonia, Musculoskeletal pain, Nausea, Vomiting |
| Serious Effects | Increased risk of asthma-related death (formoterol component), Adrenal insufficiency (especially during stress or upon withdrawal), Hypercorticism (Cushing's syndrome) with high doses or prolonged use, Serious allergic reactions (e.g., anaphylaxis, angioedema), Cardiovascular effects (e.g., hypertension, tachycardia, QT prolongation, cardiac arrest), Hypokalemia and hyperglycemia (formoterol-related), Osteoporosis with long-term use, Growth suppression in children, Glaucoma and cataracts, Eosinophilic conditions (e.g., Churg-Strauss syndrome) |
Hypersensitivity to any componentStatus asthmaticusPrimary treatment of acute asthma exacerbation
| Precautions |
Loading safety data…
| L3 (Moderately Safe) |
| Teratogenic Risk | DULERA (mometasone furoate + formoterol fumarate) is classified as FDA Pregnancy Category C. No adequate human studies exist. In animal studies, inhaled corticosteroids at high doses caused teratogenic effects (cleft palate, delayed ossification). Formoterol showed no teratogenicity in rats at 16x MRHD, but beta-agonists may cause uterine relaxation and premature labor. Risk is likely low at therapeutic doses, but benefits must outweigh potential risks. First trimester: theoretical risk of malformations. Second/third trimester: possible fetal growth restriction and adrenal suppression with chronic corticosteroid use. |
| Fetal Monitoring | Monitor maternal pulmonary function, asthma control, signs of adrenal insufficiency, blood glucose, and BP. Fetal monitoring: serial growth ultrasound for intrauterine growth restriction (IUGR), nonstress test/biophysical profile if poor control. Monitor for neonatal hypoglycemia, respiratory depression, and adrenal suppression postpartum. |
| Fertility Effects | No human studies. Animal studies: mometasone furoate reduced fertility in rats at 5x MRHD; formoterol had no effect on fertility in rats. Inhaled corticosteroids may affect ovulation at high doses. Beta-agonists generally not associated with fertility impairment. |
| Risk of asthma-related death from LABA, Candidiasis of mouth and pharynx, Pneumonia in patients with COPD (not indicated for COPD), Hypersensitivity reactions including anaphylaxis, Adrenal insufficiency during transfer from systemic corticosteroids, Hypercorticism and adrenal suppression with excessive doses, Paradoxical bronchospasm with immediate discontinuation required, Cardiovascular effects: increased pulse, blood pressure, QT interval prolongation, Hypokalemia and hyperglycemia, Reduced bone mineral density with long-term use, Growth suppression in children, Glaucoma and cataracts, Eosinophilic conditions and Churg-Strauss syndrome |
| Food/Dietary | No significant food interactions reported. Avoid known dietary asthma triggers (e.g., sulfites, histamine-rich foods) as they may exacerbate underlying condition. |
| Clinical Pearls | DULERA is a fixed-dose combination of mometasone furoate (an inhaled corticosteroid) and formoterol fumarate (a long-acting beta2-agonist). It is indicated for the maintenance treatment of asthma in patients aged 5 years and older, not for acute bronchospasm. Post-administration rinse mouth to prevent oral candidiasis. Do not use as rescue therapy; separate doses by 12 hours. Monitor for paradoxical bronchospasm and signs of adrenal insufficiency when switching from systemic corticosteroids. Formoterol may increase risk of asthma-related death; use lowest effective dose. |
| Patient Advice | Use exactly as prescribed; do not exceed 2 inhalations twice daily. · Rinse your mouth with water after each use to reduce risk of fungal infection. · Do not use DULERA for sudden asthma symptoms; have a rescue inhaler available. · Continue taking other asthma medications unless instructed otherwise. · Seek medical help if symptoms worsen or you need more rescue inhaler than usual. · Avoid foods or drinks that trigger your asthma; no general food interactions. · Inform your doctor about all medications, especially beta-blockers and diuretics. · Store at room temperature, away from heat and open flames; do not puncture canister. |