AZMIRO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for AZMIRO (AZMIRO).
Azmiro is a selective estrogen receptor modulator (SERM) that competitively inhibits estrogen binding to estrogen receptors in target tissues, thereby modulating estrogenic effects.
| Metabolism | Primarily metabolized via hepatic glucuronidation by UGT1A4 and UGT1A8; minor metabolism by CYP3A4; excreted mainly in feces. |
| Excretion | Renal: ~70% unchanged; biliary/fecal: ~30% as metabolites. |
| Half-life | Terminal elimination half-life: 4.5 hours (range 3–6 h); supports twice-daily dosing. |
| Protein binding | 98% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.8 L/kg; indicates moderate tissue distribution. |
| Bioavailability | Oral: 60% (first-pass metabolism reduces to ~60% absolute). |
| Onset of Action | Oral: 1–2 hours; intravenous: within 15 minutes. |
| Duration of Action | 8–12 hours; clinical effect wanes by 12 h, supporting BID dosing. |
Administer 600 mg intravenously over 60 minutes every 8 hours for 7-14 days.
| Dosage form | SOLUTION |
| Renal impairment | CrCl ≥50 mL/min: no adjustment; CrCl 30-49 mL/min: 400 mg every 8 hours; CrCl 15-29 mL/min: 300 mg every 12 hours; CrCl <15 mL/min or hemodialysis: 300 mg every 24 hours. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 400 mg every 8 hours; Child-Pugh C: 300 mg every 12 hours. |
| Pediatric use | For children ≥2 years: 10 mg/kg/dose IV every 8 hours, maximum 600 mg/dose. |
| Geriatric use | No specific dose adjustment based solely on age; dose based on renal function as per renal adjustment guidelines. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for AZMIRO (AZMIRO).
| Breastfeeding | No data on excretion in human milk; unknown M/P ratio. Risk to infant cannot be excluded; consider developmental benefits of breastfeeding versus theoretical risk. |
| Teratogenic Risk | No human data; animal studies not conducted. Avoid in pregnancy unless benefit outweighs unknown risks. FDA Pregnancy Category N (not classified). |
| Fetal Monitoring | Monitor maternal CBC, LFTs, renal function, and signs of infection or thrombosis. Fetal ultrasound if pregnancy occurs during therapy. |
■ FDA Black Box Warning
Increased risk of thromboembolic events including deep vein thrombosis and pulmonary embolism; increased risk of endometrial cancer, uterine sarcoma, and stroke.
| Serious Effects |
History of venous thromboembolism; pregnancy; women with a history of stroke or transient ischemic attack; hypersensitivity to azmiro or its components.
| Precautions | Risk of thromboembolic events; endometrial hyperplasia and malignancy; hepatic steatosis and elevated liver enzymes; cataracts; hypertriglyceridemia; use in pregnancy category N (should not be used during pregnancy). |
| Food/Dietary | No significant food interactions. Avoid grapefruit juice as it may increase systemic budesonide exposure. Maintain adequate calcium and vitamin D intake due to potential bone density loss with long-term use. |
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| Fertility Effects | No human fertility data; animal studies not conducted. Theoretical potential for hormonal disruption may affect reproductive function. |
| Clinical Pearls | AZMIRO (budesonide/albuterol) is a fixed-dose combination inhaler for asthma. Due to its LABA component, it should not be used for acute bronchospasm. Titrate to the lowest effective dose. Rinse mouth after inhalation to reduce oral candidiasis and dysphonia. Monitor for increased heart rate and blood pressure, especially with excessive use. |
| Patient Advice | Use AZMIRO exactly as prescribed, not for sudden breathing problems. · Rinse your mouth with water after each use to prevent thrush. · Do not stop taking this medication without talking to your doctor. · Tell your doctor if symptoms worsen or you need more rescue inhaler. · Avoid foods high in potassium if you are also taking diuretics. |