ALLERNAZE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ALLERNAZE (ALLERNAZE).
Competitive antagonist at histamine H1 receptors, preventing histamine-mediated symptoms such as itching, sneezing, and vasodilation.
| Metabolism | Primarily hepatic via CYP450 isoenzymes, including CYP3A4 and CYP2D6. |
| Excretion | Primarily renal (70-80% as unchanged drug and metabolites), with approximately 5-10% biliary/fecal elimination. |
| Half-life | Terminal elimination half-life is 12-15 hours. Clinical context: Allows for twice-daily dosing in allergic rhinitis; steady-state reached in 2-3 days. |
| Protein binding | Approximately 88-92%, primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd is 3-5 L/kg, indicating extensive tissue distribution beyond total body water. |
| Bioavailability | Oral: 40-60% (due to first-pass metabolism); Intranasal: 70-80%; Ophthalmic: negligible systemic absorption. |
| Onset of Action | Oral: 1-2 hours; Intranasal: 15-30 minutes; Ophthalmic: 10-15 minutes. |
| Duration of Action | Oral: 12-24 hours; Intranasal: 12 hours; Ophthalmic: 8-12 hours. Clinical notes: Duration may be shorter in patients with hepatic impairment or those on CYP3A4 inducers. |
| Molecular Weight | Fluticasone propionate: 500.6 Da; Salmeterol xinafoate: 603.8 Da |
5 mg orally once daily at bedtime, maximum 10 mg per day.
| Dosage form | SPRAY, METERED |
| Renal impairment | GFR < 10 mL/min: contraindicated; GFR 10–30 mL/min: 5 mg every other day; GFR > 30 mL/min: no adjustment. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 5 mg every other day; Child-Pugh C: contraindicated. |
| Pediatric use | Children 2–6 years: 2.5 mg orally once daily at bedtime; 6–12 years: 5 mg orally once daily at bedtime; >12 years: adult dosing. |
| Geriatric use | Initiate at 5 mg orally once daily at bedtime; titrate cautiously due to increased risk of sedation and falls. |
| 1st trimester | Avoid due to teratogenic risk; fluticasone propionate and salmeterol xinafoate combination is not recommended in first trimester unless benefit outweighs risk. |
| 2nd trimester | Use with caution; consider alternative therapies. Animal studies show no major teratogenicity but limited human data. |
| 3rd trimester | Use with caution; may cause fetal growth restriction or preterm labor due to beta-agonist effects. |
Clinical note
Comprehensive clinical and safety monograph for ALLERNAZE (ALLERNAZE).
| Placental transfer | Fluticasone propionate crosses placenta; salmeterol crosses placenta; both are detected in fetal plasma in animal studies. |
| Breastfeeding | Fluticasone propionate and salmeterol are excreted in breast milk in low amounts. Consider benefit vs risk; monitor infant for adverse effects. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to fluticasone, salmeterol, or any excipientStatus asthmaticusAcute asthma exacerbation requiring intensive care
| Precautions | Avoid use in patients with severe hepatic impairment, May cause drowsiness; avoid driving or operating heavy machinery, Use caution in elderly patients due to increased risk of sedation and falls |
| Food/Dietary | No known significant food interactions. Alcohol may potentiate sedation. |
| Clinical Pearls | ALLERNAZE is an intranasal antihistamine (azelastine). Onset of action is within 15-30 minutes. Bitter taste if drips into throat; advise patients to tilt head forward and sniff gently. Can be used with intranasal corticosteroids for additive effect. Avoid alcohol and CNS depressants due to potential additive sedation. Do not exceed recommended dose to minimize somnolence. |
Loading safety data…
| Lactation Rating |
| L3 - Moderately Safe |
| Teratogenic Risk | FDA Pregnancy Category C. First trimester: no adequate studies; potential teratogenic risk based on animal studies showing skeletal abnormalities at high doses. Second and third trimesters: no documented fetal abnormalities, but use only if clearly needed due to potential antihistamine effects on newborn respiratory and neurological status. |
| Fetal Monitoring | Monitor maternal blood pressure and heart rate. Assess fetal heart rate and growth if used chronically. Observe newborn for sedation, apnea, or paradoxical excitation after delivery if used near term. |
| Fertility Effects | No documented clinically significant effects on human fertility. Animal studies show no impairment at therapeutic doses. |
| Patient Advice | Use in each nostril as directed; do not spray into eyes or mouth. · Wait 10 minutes before using another nasal spray if needed. · Common side effects include bitter taste, nasal burning, or sneezing. · May cause drowsiness; avoid driving or operating machinery if affected. · Clean nozzle weekly with warm water; do not share dispenser. |