Identification
- Summary
Racepinephrine is a bronchodilator used to treat intermittent asthma.
- Brand Names
- Asthmanefrin, S-2
- Generic Name
- Racepinephrine
- DrugBank Accession Number
- DB11124
- Background
Racepinephrine is a racemic mixture consisting of d-Epinephrine and l-Epinephrine enantiomers. Epinephrine is a non-selective α- and β-adrenergic receptor agonist. It is a bronchodilator used in the temporary relief of mild symptoms of intermittent asthma including wheezing, tightness of chest and shortness of breath. It is an active ingredient in oral inhalation over-the-counter products as racepinephrine hydrochloride.
- Type
- Small Molecule
- Groups
- Approved
- Synonyms
- Not Available
Pharmacology
- Indication
Indicated for temporary relief of mild symptoms of intermittent asthma.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Symptomatic treatment of Asthma ••• ••• •••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Epinephrine acts on α- and β-adrenergic receptors. When given subcutaneously or intramuscularly, epinephrine has a rapid onset and short duration of action Label. Epinephrine induces bronchial smooth muscle relaxation to relieve respiratory distress in asthma. In a clinical trial of paediatric patients with bronchiolitis, administration of aerosolized racemic epinephrine via inhalation resulted in improved clinical symptoms such as wheezing and retractions 1. The clinical efficacy of racemic epinephrine was comparable to that of salbutamol or albuterol, which are commonly used bronchodilators 1,2.
- Mechanism of action
Epinephrine is a non-selective agonist at α- and β-adrenergic receptors, which are all G-protein-coupled receptors. The main therapeutic effect of epinephrine arises from its agonist action on β2-adrenergic receptors, which activate adenylyl cyclase and increase intracellular cyclic AMP production. Epinephrine causes smooth muscle relaxation on various tissues, including bronchial smooth muscles 3. As a result, epinephrine serves to alleviate bronchospasm, wheezing and tightness of chest that may occur during asthmatic attacks Label. Via its relaxer effects on the smooth muscle of the stomach, intestine, uterus and urinary bladder, epinephrine may also alleviate pruritus, urticaria, and angioedema and may relieve gastrointestinal and genitourinary symptoms associated with anaphylaxis.
Epinephrine also acts on the α-adrenergic receptors on vascular smooth muscles, particularly in the skin and splanchnic vascular beds, to cause constriction. Epinephrine is thought to reduce capillary leakage by constricting precapillary arterioles, reducing hydrostatic pressure and consequently bronchial mucosal edema 1.
Target Actions Organism AAlpha-1A adrenergic receptor agonistHumans AAlpha-1B adrenergic receptor agonistHumans AAlpha-2A adrenergic receptor agonistHumans AAlpha-2B adrenergic receptor agonistHumans AAlpha-2C adrenergic receptor agonistHumans ABeta-1 adrenergic receptor agonistHumans ABeta-2 adrenergic receptor agonistHumans AAlpha-1D adrenergic receptor antagonistHumans ABeta-3 adrenergic receptor agonistHumans - Absorption
To refer to the pharmacokinetic data of L-epinephrine, refer to the drug entry for Epinephrine.
- Volume of distribution
To refer to the pharmacokinetic data of L-epinephrine, refer to the drug entry for Epinephrine.
- Protein binding
To refer to the pharmacokinetic data of L-epinephrine, refer to the drug entry for Epinephrine.
- Metabolism
To refer to the pharmacokinetic data of L-epinephrine, refer to the drug entry for Epinephrine.
- Route of elimination
To refer to the pharmacokinetic data of L-epinephrine, refer to the drug entry for Epinephrine.
- Half-life
To refer to the pharmacokinetic data of L-epinephrine, refer to the drug entry for Epinephrine.
- Clearance
To refer to the pharmacokinetic data of L-epinephrine, refer to the drug entry for Epinephrine.
- Adverse Effects
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Oral LD50 of racepinephrine hydrochloride in mouse is 90 mg/kg MSDS.
Overdosage of epinephrine may cause extremely elevated arterial pressure, which may further lead to cerebrovascular hemorrhage, particularly in elderly patients. Peripheral vascular constriction in conjunction with cardiac stimulation may produce pulmonary oedema. Treatment consists of rapidly acting vasodilators or alpha-adrenergic blocking drugs and/or respiratory support. Transient bradycardia followed by tachycardia may also be observed, and may be accompanied by potentially fatal cardiac arrhythmias. remature ventricular contractions may appear within one minute after injection and may be followed by multifocal ventricular tachycardia (prefibrillation rhythm). Subsidence of the ventricular effects may be followed by atrial tachycardia and occasionally by atrioventricular block. In case of arrhythmias, treatment should involve administration of a beta adrenergic blocking drug such as propranolol. Overdosage may also produce extreme pallor and coldness of the skin, metabolic acidosis, and kidney failure, which should each be treated with suitable corrective measures Label.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAcebutolol The therapeutic efficacy of Acebutolol can be increased when used in combination with Racepinephrine. Aceclofenac The risk or severity of hypertension can be increased when Aceclofenac is combined with Racepinephrine. Acemetacin The risk or severity of hypertension can be increased when Racepinephrine is combined with Acemetacin. Acetazolamide The risk or severity of Cardiac Arrhythmia can be increased when Racepinephrine is combined with Acetazolamide. Acetyldigitoxin The risk or severity of Cardiac Arrhythmia can be increased when Racepinephrine is combined with Acetyldigitoxin. - Food Interactions
- Avoid caffeine.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Racepinephrine hydrochloride 336096P2WE 329-63-5 ATADHKWKHYVBTJ-UHFFFAOYSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Cord No2 Gingival Retraction Packing 0.5 mg / 2.54 cm Dental Gingi Pak Labs, Division Of Belport Co., Inc. 1979-12-31 2004-08-16 Canada 
Cord No3 Packing 0.5 mg / 2.54 cm Dental Gingi Pak Labs, Division Of Belport Co., Inc. 1979-12-31 2004-08-16 Canada Cotton Coil Packing 3 mg / 2.54 cm Dental Gingi Pak Labs, Division Of Belport Co., Inc. 1979-12-31 2004-08-16 Canada Crown Pak Retraction Cord Packing 0.5 mg / 2.54 cm Dental Gingi Pak Labs, Division Of Belport Co., Inc. 1979-12-31 2004-08-16 Canada Epidri 6% 2.1 mg Dental Pascal International Corporation 1951-12-31 2005-06-23 Canada - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Asthmanefrin Solution 11.25 mg/0.5mL Respiratory (inhalation) Nephron Pharmaceuticals Corporation 2012-08-01 Not applicable US 
Epi-Mist Aerosol, spray .594 mg/.120mL Respiratory (inhalation) Drnaturalhealing Inc 2015-05-15 Not applicable US Racepinephrine Solution 11.25 mg/0.5mL Respiratory (inhalation) Nucare Pharmaceuticals,inc. 2000-01-01 Not applicable US S2 Solution 11.25 mg/.5mL Respiratory (inhalation) Cardinal Health 2000-01-01 2018-07-31 US S2 Solution 11.25 mg/0.5mL Respiratory (inhalation) Nephron Sc, Inc. 2000-01-01 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Blue Gel Anesthetic Racepinephrine hydrochloride (0.1 mg/1g) + Lidocaine hydrochloride (50 mg/1g) + Tetracaine hydrochloride (10 mg/1g) Gel Topical Dermal Source, Inc. 2022-06-07 Not applicable US Gingibraid W Alum Pot Sulf and Epin 0e Racepinephrine hydrochloride (0.2 mg / 2.5 cm) + Potassium alum (0.15 mg / 2.5 cm) Packing Dental Van R Dental Products Inc. 1981-12-31 2007-07-31 Canada Gingibraid W Epineph and Alum 1e Racepinephrine hydrochloride (0.4 mg / 2.5 cm) + Potassium alum (0.25 mg / 2.5 cm) Packing Dental Van R Dental Products Inc. 1981-12-31 2007-07-31 Canada Gingibraid W Epineph and Alum 2e Racepinephrine hydrochloride (0.6 mg / 2.5 cm) + Potassium alum (0.35 mg / 2.5 cm) Packing Dental Van R Dental Products Inc. 1981-12-31 2007-07-31 Canada Gingibraid W Epineph and Alum 3e Racepinephrine hydrochloride (0.9 mg / 2.5 cm) + Potassium alum (0.55 mg / 2.5 cm) Packing Dental Van R Dental Products Inc. 1981-12-31 2007-07-31 Canada - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Blue Gel Anesthetic Racepinephrine hydrochloride (0.1 mg/1g) + Lidocaine hydrochloride (50 mg/1g) + Tetracaine hydrochloride (10 mg/1g) Gel Topical Dermal Source, Inc. 2022-06-07 Not applicable US
Categories
- Drug Categories
- Adrenergic Agents
- Adrenergic Agonists
- Adrenergic alpha-1 Receptor Agonists
- Adrenergic alpha-2 Receptor Agonists
- Adrenergic alpha-Agonists
- Adrenergic beta-1 Receptor Agonists
- Adrenergic beta-2 Receptor Agonists
- Adrenergic beta-3 Receptor Agonists
- Adrenergic beta-Agonists
- Agents producing tachycardia
- Agents that produce hypertension
- Alcohols
- Alpha-and Beta-adrenergic Agonists
- Amines
- Amino Alcohols
- Anti-Asthmatic Agents
- Autonomic Agents
- Benzene Derivatives
- Biogenic Amines
- Biogenic Monoamines
- Bronchodilator Agents
- Cardiovascular Agents
- Catecholamines
- Catechols
- Epinephrine and similars
- Ethanolamines
- Mydriatics
- Neurotransmitter Agents
- Peripheral Nervous System Agents
- Phenols
- Respiratory System Agents
- Sympathomimetics
- Vasoconstrictor Agents
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- Not Available
- CAS number
- 329-65-7
References
- General References
- Langley JM, Smith MB, LeBlanc JC, Joudrey H, Ojah CR, Pianosi P: Racemic epinephrine compared to salbutamol in hospitalized young children with bronchiolitis; a randomized controlled clinical trial [ISRCTN46561076]. BMC Pediatr. 2005 May 5;5(1):7. doi: 10.1186/1471-2431-5-7. [Article]
- Reijonen T, Korppi M, Pitkakangas S, Tenhola S, Remes K: The clinical efficacy of nebulized racemic epinephrine and albuterol in acute bronchiolitis. Arch Pediatr Adolesc Med. 1995 Jun;149(6):686-92. [Article]
- 14. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 174-175, 181-182). Edinburgh: Elsevier/Churchill Livingstone. [ISBN:978-0-7020-3471-8]
- DailyMed: Asthmanefrin (racepinephrine) solution [Link]
- External Links
- PubChem Substance
- 347911128
- 66887
- Wikipedia
- Epinephrine_(medication)
- FDA label
- Download (625 KB)
- MSDS
- Download (59.9 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Unknown Status Treatment Bronchiolitis 1 3 Completed Prevention Ulcerative Colitis 1 3 Completed Treatment Human Immunodeficiency Virus (HIV) Infections 1 3 Completed Treatment Hypogonadism 1 3 Completed Treatment Ulcerative Colitis 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Gel Topical Packing Dental 3 mg / 2.54 cm Aerosol, spray Respiratory (inhalation) .594 mg/.120mL Solution / drops Ophthalmic 0.5 % Solution / drops Ophthalmic 1 % Solution / drops Ophthalmic 2 % Liquid Intracardiac; Intravenous 0.1 mg / mL Packing Topical .5 mg / 2.54 cm Packing Dental .55 mg / 2.5 cm Packing Dental 1.05 mg / 2.5 cm Packing Dental 1.95 mg / 2.5 cm Liquid Dental .2 % Liquid Dental 8 % Swab Dental .7 mg / pad Packing Dental 1.15 mg / sut Solution Respiratory (inhalation) 11.25 mg Packing Dental .5 mg / 2.54 cm Solution Respiratory (inhalation) 11.25 mg/.5mL Solution Respiratory (inhalation) 11.25 mg/0.5mL Solution Respiratory (inhalation) 22.5 mg/1mL Packing Dental .197 mg / cm Packing Dental .33 mg / cm Packing Dental 0.5 mg / 2.54 cm Packing Dental Packing Dental .054 mg / cm Solution Respiratory (inhalation) 2.25 % - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Not Available
- Experimental Properties
Property Value Source melting point (°C) 157 MSDS water solubility Soluble MSDS - Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Protein heterodimerization activity
- Specific Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
- Gene Name
- ADRA1A
- Uniprot ID
- P35348
- Uniprot Name
- Alpha-1A adrenergic receptor
- Molecular Weight
- 51486.005 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Protein heterodimerization activity
- Specific Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
- Gene Name
- ADRA1B
- Uniprot ID
- P35368
- Uniprot Name
- Alpha-1B adrenergic receptor
- Molecular Weight
- 56835.375 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Thioesterase binding
- Specific Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
- Gene Name
- ADRA2A
- Uniprot ID
- P08913
- Uniprot Name
- Alpha-2A adrenergic receptor
- Molecular Weight
- 48956.275 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Epinephrine binding
- Specific Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine...
- Gene Name
- ADRA2B
- Uniprot ID
- P18089
- Uniprot Name
- Alpha-2B adrenergic receptor
- Molecular Weight
- 49565.8 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Protein homodimerization activity
- Specific Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
- Gene Name
- ADRA2C
- Uniprot ID
- P18825
- Uniprot Name
- Alpha-2C adrenergic receptor
- Molecular Weight
- 49521.585 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Receptor signaling protein activity
- Specific Function
- Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately e...
- Gene Name
- ADRB1
- Uniprot ID
- P08588
- Uniprot Name
- Beta-1 adrenergic receptor
- Molecular Weight
- 51322.1 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Protein homodimerization activity
- Specific Function
- Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately ...
- Gene Name
- ADRB2
- Uniprot ID
- P07550
- Uniprot Name
- Beta-2 adrenergic receptor
- Molecular Weight
- 46458.32 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Alpha1-adrenergic receptor activity
- Specific Function
- This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
- Gene Name
- ADRA1D
- Uniprot ID
- P25100
- Uniprot Name
- Alpha-1D adrenergic receptor
- Molecular Weight
- 60462.205 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Protein homodimerization activity
- Specific Function
- Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. Beta-3 is involved in the regulation of lipolysis and thermogenesis.
- Gene Name
- ADRB3
- Uniprot ID
- P13945
- Uniprot Name
- Beta-3 adrenergic receptor
- Molecular Weight
- 43518.615 Da
Drug created at December 03, 2015 16:51 / Updated at February 20, 2024 23:54