NOXIVENT
Clinical safety rating
cautionComprehensive clinical and safety monograph for NOXIVENT (NOXIVENT).
Noxivent is a synthetic analog of epinephrine that acts as a non-selective alpha and beta adrenergic receptor agonist. It binds to alpha-1 receptors causing vasoconstriction, alpha-2 receptors reducing insulin secretion, beta-1 receptors increasing heart rate and contractility, and beta-2 receptors causing bronchodilation and vasodilation. Its primary effect in septic shock is increasing mean arterial pressure via vasoconstriction.
| Metabolism | Primarily metabolized by monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT) in the liver and other tissues. Also undergoes oxidation and conjugation. |
| Excretion | Primarily renal (70-80% unchanged), with 10-15% biliary/fecal. Minor metabolism via ester hydrolysis. |
| Half-life | Terminal elimination half-life 4-6 hours; prolonged in renal impairment (up to 12 hours) requiring dose adjustment. |
| Protein binding | 85-90% bound to albumin; reduced binding in hypoalbuminemia. |
| Volume of Distribution | 0.8-1.2 L/kg; suggests extensive tissue distribution (e.g., lung, liver). |
| Bioavailability | Oral: 50-60% (first-pass metabolism); Sublingual: 70-80%; No data for other routes. |
| Onset of Action | IV: 5-10 minutes; Oral: 30-60 minutes; Onset correlates with peak plasma concentration. |
| Duration of Action | 4-6 hours for bronchodilation; prolonged in hepatic impairment (up to 8 hours). |
| Molecular Weight | 312.4 |
700 mg orally twice daily with food.
| Dosage form | GAS |
| Renal impairment | GFR 30-59 mL/min: 350 mg twice daily; GFR <30 mL/min or on dialysis: 350 mg once daily. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 350 mg twice daily; Child-Pugh C: not recommended. |
| Pediatric use | Not approved for pediatric use. |
| Geriatric use | No specific dose adjustment; monitor renal function and use lowest effective dose. |
| 1st trimester | Avoid due to risk of fetal malformations; no adequate human data. |
| 2nd trimester | Use only if clearly needed; may cause fetal respiratory depression. |
| 3rd trimester | Avoid near term; risk of neonatal respiratory depression and withdrawal. |
Clinical note
Comprehensive clinical and safety monograph for NOXIVENT (NOXIVENT).
| Placental transfer | Rapidly crosses placenta; high fetal exposure. |
| Breastfeeding | Not recommended; excreted in breast milk with potential for infant sedation. |
| Lactation Rating | L4 |
| Teratogenic Risk | NOXIVENT is a combination of a long-acting beta-agonist (LABA) and an inhaled corticosteroid (ICS). Inhaled beta-agonists have low systemic bioavailability and are generally considered low risk in pregnancy. Studies with inhaled corticosteroids (budesonide, fluticasone) show no increased risk of major malformations. First-trimester exposure data for LABAs are limited but do not indicate a significant teratogenic risk. However, high-dose systemic corticosteroids are associated with cleft palate. Inhaled doses minimize systemic exposure. Overall, NOXIVENT is considered safe for use in pregnancy when asthma control is necessary. |
| Fetal Monitoring | Monitor maternal asthma control (peak flow, symptoms, pulmonary function tests). Assess fetal growth and well-being with serial ultrasounds if asthma is poorly controlled. Monitor for maternal adverse effects such as tachycardia, hypertension, or hyperglycemia, especially with high doses of beta-agonist component. No specific fetal monitoring required but usual prenatal care. |
| Fertility Effects | No known adverse effects on fertility. Inhaled beta-agonists and corticosteroids do not impair fertility in animal studies. In humans, well-controlled asthma is associated with normal fertility. Uncontrolled asthma may lead to hypoxia and stress, potentially affecting fertility. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to NOXIVENTAcute asthma attackSevere hepatic impairment
| Precautions | May cause severe hypertension, cardiac arrhythmias (especially with pre-existing conditions), tissue ischemia due to vasoconstriction, and exacerbation of heart failure. Use with caution in patients with hyperthyroidism, diabetes (as it increases blood glucose), and history of coronary artery disease. |
| Food/Dietary | No specific food interactions reported. Grapefruit juice may increase formoterol levels (avoid if possible). Take with or without food. |
| Clinical Pearls | NOXIVENT (formoterol + glycopyrrolate) is a fixed-dose LABA/LAMA combination for COPD. Avoid use in asthma due to increased risk of asthma-related death. Monitor for paradoxical bronchospasm; discontinue immediately if occurs. Assess renal function before initiating glycopyrrolate (primarily renally excreted). Not for acute bronchospasm relief. |
| Patient Advice | Use exactly as prescribed; do not exceed recommended dose or frequency. · This medication is for maintenance treatment of COPD, not for acute symptoms. Always have a rescue inhaler (e.g., albuterol) available. · Rinse mouth with water after each dose to prevent thrush (oral candidiasis). · Report worsening breathing, chest tightness, or signs of allergic reaction (rash, hives, swelling) immediately. · Do not stop using NOXIVENT without consulting your doctor, even if you feel better. |
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