Pritish Mondal1, Bhargava Kandala2, Richard Ahrens3, Sarah E Chesrown4, Leslie Hendeles5. 1. Pulmonary Division, Department of Pediatrics, University of Florida, Gainesville, Fla. 2. Department of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, Fla. 3. Allergy/Pulmonary Division, Department of Pediatrics, University of Iowa, Iowa City, Iowa. 4. Department of Pediatrics, Emeritus, University of Florida, Gainesville, Fla. 5. Pulmonary Division, Department of Pediatrics, University of Florida, Gainesville, Fla; Department of Pharmacotherapy and Translational Research, College of Pharmacy, University of Florida, College of Pharmacy, Gainesville, Fla. Electronic address: hendeles@cop.ufl.edu.
Abstract
BACKGROUND: Inhaled racepinephrine (RE) (Asthmanefrin) became available in September 2012 as a nonprescription treatment for bronchospasm based on a 1986 US Food and Drug Administration rule. It contains 11.25 mg RE in 0.5 mL and is delivered by a handheld electronic nebulizer. In 2001, we conducted a pilot study that was never published. Now that the product is promoted as a replacement for epinephrine chlorofluorocarbon metered-dose inhaler (Primatene), we provide the results of that study. Methacholine challenge was used as a bioassay. OBJECTIVE: To determine the dose of RE that is equivalent to nebulized albuterol. METHODS: Four subjects, 18 to 45 years old, with mild stable asthma completed the pilot study. Methacholine challenge was performed on the first screening day, without pretreatment, and then on different days, 15 minutes after 1.25 mg albuterol and 2.5, 5, 10, and 20 mg RE delivered by a Pari LC Plus nebulizer. The end point was the provocative concentration of methacholine that caused a 20% decrease in FEV1. Data were log transformed and analyzed by an ANOVA for repeated measures. RESULTS: There was a significant dose response for RE. The geometric mean provocative concentration of methacholine that caused a 20% decrease in FEV1 was 44 mg/mL (95% CI, 23-85 mg/mL) after albuterol, and 10.2 mg/mL (95% CI, 3.5-30 mg/mL) after the 10-mg dose of RE (approximate nonprescription dose) (P = .001). There were no adverse effects. CONCLUSION: RE provides less bronchoprotection from methacholine than does albuterol and may be less effective in treating acute bronchospasm.
BACKGROUND: Inhaled racepinephrine (RE) (Asthmanefrin) became available in September 2012 as a nonprescription treatment for bronchospasm based on a 1986 US Food and Drug Administration rule. It contains 11.25 mg RE in 0.5 mL and is delivered by a handheld electronic nebulizer. In 2001, we conducted a pilot study that was never published. Now that the product is promoted as a replacement for epinephrinechlorofluorocarbon metered-dose inhaler (Primatene), we provide the results of that study. Methacholine challenge was used as a bioassay. OBJECTIVE: To determine the dose of RE that is equivalent to nebulized albuterol. METHODS: Four subjects, 18 to 45 years old, with mild stable asthma completed the pilot study. Methacholine challenge was performed on the first screening day, without pretreatment, and then on different days, 15 minutes after 1.25 mg albuterol and 2.5, 5, 10, and 20 mg RE delivered by a Pari LC Plus nebulizer. The end point was the provocative concentration of methacholine that caused a 20% decrease in FEV1. Data were log transformed and analyzed by an ANOVA for repeated measures. RESULTS: There was a significant dose response for RE. The geometric mean provocative concentration of methacholine that caused a 20% decrease in FEV1 was 44 mg/mL (95% CI, 23-85 mg/mL) after albuterol, and 10.2 mg/mL (95% CI, 3.5-30 mg/mL) after the 10-mg dose of RE (approximate nonprescription dose) (P = .001). There were no adverse effects. CONCLUSION: RE provides less bronchoprotection from methacholine than does albuterol and may be less effective in treating acute bronchospasm.