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Hormone · Profile

Epinephrine

Adrenaline · EpiPen · Adrenalin

Adrenal HormonesApproved
MW
183.2g/mol
Formula
C9H13NO3

Epinephrine, also known as adrenaline, is a catecholamine hormone produced by the adrenal medulla, the inner part of the adrenal glands located atop the kidneys. Researchers primarily study epinephrine for its critical role in the acute management of severe allergic reactions, particularly anaphylaxis. Key findings indicate that epinephrine is the first-line intervention for anaphylaxis, with studies suggesting that prompt administration can significantly reduce morbidity and mortality associated with this life-threatening condition. Additionally, clinical evidence indicates that variations in pharmacokinetics and delivery methods, such as intranasal versus intramuscular administration, are areas of ongoing research aimed at optimizing its use in emergency settings. Current research continues to explore the safety, efficacy, and accessibility of epinephrine delivery devices, highlighting its vital importance in both clinical and community healthcare contexts.

Overview

Übersicht

Epinephrine, also known as adrenaline, is a naturally occurring hormone and neurotransmitter produced by the adrenal medulla. It belongs to the catecholamine chemical class and can also be synthesized for medical use. This compound plays a crucial role in the body's 'fight-or-flight' response, preparing the body to react to stress or danger.

The primary physiological roles of epinephrine include increasing heart rate, constricting blood vessels, dilating air passages, and participating in the fight-or-flight response. It is extensively researched in the context of anaphylaxis, cardiac arrest, and bronchospasm. Researchers have observed its critical role in managing severe allergic reactions and its use in emergency medicine.

Epinephrine acts on both alpha and beta-adrenergic receptors. Activation of these receptors leads to a cascade of biological effects, including increased cardiac output, bronchodilation, and vasoconstriction. These actions collectively contribute to its efficacy in treating anaphylaxis and cardiac events.

Pharmacokinetically, epinephrine has a short half-life, with rapid metabolism primarily by the liver and other tissues. Its bioavailability varies significantly depending on the route of administration, with intramuscular and intravenous routes being most effective for rapid action.

Clinically, epinephrine is a first-line treatment for anaphylaxis and is available in various forms, including auto-injectors like the EpiPen. It is approved by regulatory agencies worldwide for emergency use in allergic reactions and cardiac arrest. Researchers have found that its availability in auto-injector form has improved community-based management of anaphylaxis, though challenges remain in optimizing its use and ensuring accessibility.

Chemical profile

Chemische Struktur

Chemical structure of Epinephrine
FormelC9H13NO3
Molekulargewicht183.2g/mol
CAS-Nummer51-43-4
PubChem CID5816
Mechanism

Wirkmechanismus

Epinephrine acts on alpha and beta-adrenergic receptors, leading to increased cardiac output, bronchodilation, and vasoconstriction. This activation triggers a biological cascade that prepares the body for rapid response to stress or allergic reactions.

Mechanism

Signalweg

Epinephrine primarily acts as an agonist at adrenergic receptors, specifically the α1, β1, and β2 subtypes, leading to various physiological responses. Activation of β2 receptors stimulates the cAMP/PKA pathway, resulting in smooth muscle relaxation and bronchodilation, while α1 receptor activation causes vasoconstriction through phospholipase C signaling, increasing intracellular calcium levels. Additionally, β1 receptor stimulation enhances cardiac output by increasing heart rate and contractility, collectively contributing to the rapid reversal of anaphylactic symptoms and stabilization of mast cells.

Half-Life & Pharmacokinetics

ENEndogenous

Circulating half-life ~2 minutes

IMIntramuscular

~10-20 minutes

IVIntravenous

~2 minutes

POOral

Poor bioavailability due to first-pass metabolism

Epinephrine is rapidly metabolized by the liver and other tissues, primarily through the actions of catechol-O-methyltransferase (COMT) and monoamine oxidase (MAO).

Storage

Temperature

Store at room temperature (15-30C)

Light

Protect from light

Form

Aqueous solution: use within specified expiration date

Notes

Ensure the solution is clear and colorless before use. Discard if discolored or contains particulate matter.

Solubility

Löslichkeit

Epinephrine is soluble in water, which is relevant for its formulation in aqueous solutions for injection.

Legal Status

🇩🇪DE

Verschreibungspflichtig (prescription only). Not a controlled substance under BtMG.

🇺🇸US

FDA approved for emergency treatment of allergic reactions. Prescription required.

🇦🇺AU

TGA Schedule 4: Prescription Only Medicine.

🇬🇧UK

Prescription Only Medicine (POM) under MHRA regulations.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

Open Questions

Offene Forschungsfragen

Current evidence is limited regarding the optimal dosing strategies for epinephrine in anaphylaxis, particularly in terms of pharmacokinetics and pharmacodynamics across different delivery methods, such as intranasal versus intramuscular administration. Further research is needed through larger randomized controlled trials (RCTs) to assess the long-term safety and efficacy of epinephrine autoinjectors and alternative delivery systems like neffy in diverse populations, including infants and obese adults. Additionally, studies are required to clarify the clinical implications of poor responses to epinephrine, including the need for emergency medical services activation and the impact on patient outcomes and quality of life.

107 Research Publications

2,051

Total Citations

49

Human/RCT

2.5

Avg. Influence

2023

Latest

Sort
Filter
#01

First aid anaphylaxis management in children who were prescribed an epinephrine autoinjector device (EpiPen).

Case ReportInfluence7.0
248
The study demonstrated that the EpiPen autoinjector was infrequently used during recurrent anaphylaxis episodes, indicating a need for improved parental education on its use.
#02

Adrenaline in the treatment of anaphylaxis: what is the evidence?

ReviewInfluence9.0
248
The review demonstrated that adrenaline is the recommended first-line treatment for anaphylaxis, highlighting its safety and efficacy based on current evidence.
#03

Low chance of survival among patients requiring adrenaline (epinephrine) or intubation after out-of-hospital cardiac arrest in Sweden.

Case ReportInfluence1.0
144
The study demonstrated that administration of epinephrine during out-of-hospital cardiac arrest was associated with lower survival rates, indicating the need for further research on its efficacy.
#04

Parental use of EpiPen for children with food allergies.

SurveyInfluence3.0
112
Researchers observed that parental empowerment significantly correlates with comfort in administering EpiPen to children with food allergies, highlighting the importance of education and training.
#05

EpiPen Jr versus EpiPen in young children weighing 15 to 30 kg at risk for anaphylaxis.

HumanInfluence5.0
111
Researchers observed that EpiPen administration resulted in higher systolic blood pressure in children compared to EpiPen Jr, but also caused more adverse effects following epinephrine injection.
#06

Outdated EpiPen and EpiPen Jr autoinjectors: past their prime?

AnimalInfluence3.0
103
Researchers observed that outdated EpiPen and EpiPen Jr auto-injectors showed significantly reduced epinephrine bioavailability, suggesting the importance of using in-date devices for effective anaphylaxis management.
#07

Epinephrine in the Management of Anaphylaxis.

Brown Julie C, et al. · The journal of allergy and clinical immunology. In practice · 2020

ReviewInfluence2.0
87
Researchers observed that epinephrine is the only first-line medication for anaphylaxis, requiring prompt administration to minimize morbidity and mortality, with a need for improved dosing strategies.

Key findings

  1. 01Epinephrine is the first-line treatment for anaphylaxis.
  2. 02Prompt administration is crucial for minimizing health risks.
  3. 03There is a need for improved access and usability of epinephrine autoinjectors for all patients.
#08

Analysis of the burden of treatment in patients receiving an EpiPen for yellow jacket anaphylaxis.

HumanInfluence1.0
80
Researchers observed that most patients with venom allergy found the EpiPen burdensome compared to venom immunotherapy, with many preferring the latter after one year of carrying the EpiPen.
#09

Patients' ability to treat anaphylaxis using adrenaline autoinjectors: a randomized controlled trial.

HumanInfluence4.0
60
The study demonstrated that AAI device design significantly influenced successful adrenaline administration, with Auvi-Q showing higher success rates compared to other devices after switching without specific training.
#10

Epinephrine and vasopressin during cardiopulmonary resuscitation.

ReviewInfluence2.0
52
The study demonstrated that while epinephrine and vasopressin are commonly studied vasopressors in cardiac arrest, their clinical benefits remain unclear, necessitating further research.

Clinical Trials (15)

Preclinical
Phase I
Phase II
Phase III
Approved

15

Total Trials

1,267

Total Enrolled

Two Approaches in Enhancing the Efficacy of Inferior Alveolar Nerve Block During Treatment of Mandibular First Permanent Molars With Symptomatic Irreversible Pulpitis

Sponsor

Minia University

Enrollment

180

Started

2022

Primary outcome

Pain assessment

Pain, Procedural

Effect of Adrenaline (1:80,000) Containing Local Anesthesia on Glycemic Level of Diabetic and Healthy Individuals Undergoing Tooth Extraction

NCT07633106ACTIVE_NOT_RECRUITING
Sponsor

Dow University of Health Sciences

Enrollment

90

Started

2026

Primary outcome

Effect of adrenaline (1:80,000) containing local anesthesia on glycemic level of diabetic patients and healthy individuals undergoing tooth extraction

Glycemic Level

Posterior Capsular Injection With Femoral Nerve Block for Total Knee Arthroplasty

NCT02701296COMPLETED
Sponsor

Trinity Health Of New England

Enrollment

80

Started

2011

Primary outcome

Pain Intensity

Posterior Knee Infiltration

A Randomized, Double-Blind, Trial Comparing Epinephrine Versus Phenylephrine as a Vasoconstrictor in Regional Anesthesia for Upper Extremity Surgery

NCT00225043COMPLETED
Sponsor

New York Presbyterian Brooklyn Methodist Hospital

Enrollment

60

Started

2005

Healthy

Effect of a Vibration System on Pain Reduction During Injection of Local Dental Anaesthesia in Children

NCT03953001COMPLETED
Sponsor

Imam Abdulrahman Bin Faisal University

Enrollment

51

Started

2018

Primary outcome

Self Reported pain intensity: Visual analogue scale (VAS) of pain intensity

Local AnaestheticDental Anxiety

Non-opioid Anesthesia Based on Thoracic Paravertebral Block During Laparoscopic Sleeve Gastrectomy

NCT07084753NOT_YET_RECRUITING
Sponsor

IVO JURISIC

Enrollment

36

Started

2025

Primary outcome

a) Postoperative pain levels measured by the 0-10 Numerical rating scale (NRS). b) Opioid analgesic consumption (Morphine milligram equivalents- MME).

Obese PatientsBariatric Surgical PainBariatric Surgery (Sleeve Gastrectomy )Non-Opioid Pain ManagementPONVPostoperative AnalgesiaPostoperative PainThoracic Paravertebral BlockOpioid Free Anesthesia

Testing the Anesthetic Effectiveness of Buffered Articaine Injected Next to a Lower First Molar.

NCT01862614Phase 4COMPLETED
Sponsor

Ohio State University

Enrollment

80

Started

2013

Primary outcome

Number of Participants Achieving Pulpal Anesthesia.

Anesthetic Effectiveness

Comparison of Infraclavicular And Supraclavicular Block

NCT04784104Phase 4UNKNOWN
Sponsor

Bozyaka Training and Research Hospital

Enrollment

70

Started

2021

Primary outcome

Block Formation Time

Anesthesia ConductionUpper Extremity SurgeryPain, PostoperativeAnesthesia and AnalgesiaNerve BlockBrachial Plexus Block

Comparison of Epinephrine and Phenylephrine/Ketorolac With Regards to Pupil Size

NCT02895035Phase 4TERMINATED
Sponsor

Milton S. Hershey Medical Center

Enrollment

59

Started

2016

Primary outcome

Mean Area Under the Curve Change From Baseline in Pupil Diameter Over Time to the End of Cataract Surgery

Cataract

Bupivacaine in the Treatment of Postoperative Pain of Impacted Third Molar Extraction

NCT03950700Phase 4COMPLETED
Sponsor

CES University

Enrollment

40

Started

2019

Primary outcome

Change in Pain Intensity Measure: pain visual analog scale

Teeth, Impacted

Extended Delivery of Bupivacaine Study in Herniorrhaphy

NCT04102267Phase 4COMPLETED
Sponsor

Heron Therapeutics

Enrollment

32

Started

2018

Primary outcome

Mean area under the curve (AUC) of the Numeric Rating Scale of pain intensity scores with activity (NRS-A) through 72 hours (AUC0-72)

Analgesia

Three-level Injection Paravertebral Block vs General Anesthesia in Mastectomy

NCT02065947Phase 1/2COMPLETED
Sponsor

Ramathibodi Hospital

Enrollment

60

Started

2013

Primary outcome

postoperative analgesia requirement (opioids + nonsteroidal antiinflammatory drug)

Radical Mastectomy

Safety Study of Long-Acting Local Anesthetic

NCT01786655Phase 1COMPLETED
Sponsor

Charles Berde

Enrollment

105

Started

2013

Primary outcome

Presence or absence of Adverse Events as a function of NeoSTX dose

Safety of Neosaxitoxin in Healthy Volunteers

Study of Inhaled DMC-IH1 and Intramuscular (EpiPen®) Epinephrine in Healthy Male and Female Participants.

NCT06013150Phase 1COMPLETED
Sponsor

De Motu Cordis

Enrollment

24

Started

2023

Primary outcome

Number of participants with adverse events (AEs)

Anaphylactic Reaction

Control of Iatrogenic Endobronchial Bleeding by Tranexamic Acid, Adrenalin and Hemagglutinase

NCT06149091Early Phase 1UNKNOWN
Sponsor

China-Japan Friendship Hospital

Enrollment

300

Started

2023

Primary outcome

Intratracheal bleeding control rate

Iatrogenic Endobronchial Bleeding

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This page is for informational and research purposes only. All information is based on published scientific literature and does not constitute medical advice, diagnosis, or treatment recommendations. Many substances listed may not be approved for human use and may be subject to drug regulation laws (e.g., AMG in Germany, FDA in the US). PepStack does not encourage the use of any substance on humans. Always consult a qualified healthcare professional before making any health-related decisions. Use of this information is entirely at your own risk. PepStack assumes no liability for the accuracy, completeness, or timeliness of the content provided. Full disclaimer