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epinephrine; adrenaline (Sus-Phrine, Vapronefrin, Epifrin, Glaucon, Auvi-Q, Allerject)

Pharmacology: Indications: - acute bronchospasm, status asthmaticus - dyspnea & wheezing due to severe asthma - bronchiolitis - severe allergic reaction, anaphylaxis, anaphylactive reactions - cardiac arrest, cardiopulmonary resuscitation - hypotension, shock syndromes - cardiac arrhythmias - local anesthesia - in combination with local anesthetics to reduce vascular absorption of the anesthetic - management of open-angle glaucoma - mydriasis [7] Benefit/risk: - bronchiolitis - number needed to treat to prevent 1 hospital admission = 17 [8] Dosage: Pressor activity: - Infusion 1 mg in 250 mL D5W (4 ug/mL) at 1-4 ug/min (15-60 mL/hr). Injection: - solution: - SC: 1 mg/mL (1:1000) (1 mL & 30 mL) - IV: 0.1 mg/mL (1:10,000) (10 mL) - IM: (anaphylaxis) - suspension: 1.5 mg/0.3 mL (1:200) (5 mL) - auto-injector: 0.15 mg/dose, 0.3 mg/dose - auto-injector Auvi-Q comes with audio & visual cues on how to administer the medication properly [5] Asthma: 0.01 mL/kg up to 0.3-0.5 mL (0.3-0.5 mg) of 1:1000 solution SC. - Injectable allergy kit: Tradenames: Ana-kit, Epipen. - Sustained epinephrine: Tradename: Sus-Phrine. - 0.05 mL/kg up to 0.15 mL of 1:200 solution - SC every 6 hours. Racemic epinephrine. Tradename: Vapronefrin. - Croup: 8-15 drops nebulized. , Intranasal: neffy, an intranasal epinephrine delivery device [10] - comparable or more effective than approved injection products [10] - FDA-approved: 2 mg only currently available dose - patients should have access to two neffy devices - a second device can be used in the same nostril after 5 minutes, if needed Ophthalmic: Epifrin eyedrops: 0.5%, 1% & 2% (10 mL). - Adjunctive treatment of open-angle glaucoma. - 1-2 drops OU QD/BID. Cautions: 1) gonioscopy required before initiation of treatment 2) do not use in closed-angle glaucoma Pharmacokinetics: 1) onset of action is < 5 minutes 2) metabolism a) liver, kidneys, adrenergic nerve terminals & plasma b) monoamine oxidase (MAO) c) catechol O-methyltransferase (COMT) d) metabolites: homovanillic acid (HVA) & norepinephrine 3) eliminated in the urine 4) 1/2life 2-10 minutes 5) ophthalmic agent (Epifrin) a) initial reduction in intraocular pressure within 1 hour b) maximal effect in 4-8 hours c) duration of action 12-24 hours Adverse effects: 1) common (> 10%) - tachycardia, nervousness, restlessness, palpitations 2) less common (1-10%) - dizziness, lightheadedness, flushing, headache, increased sweating, hypertension, nausea/vomiting, trembling, insomnia, paleness, weakness 3) uncommon (< 1%) - chest pain, arrhythmias, wheezing, dry mouth or throat, sudden death, anxiety, urinary retention 4) other a) increased myocardial oxygen consumption b) decreased renal & splanchnic blood flow c) ventricular ectopy d) increased systolic blood pressure e) disorientation f) shortness of breath g) facilitates AV conduction - may cause rapid ventricular response in patients with atrial fibrillation h) contains sulfite (asthmatics may be sensitive) i) gangrene of extremities & ears j ophthalmic agent: (Epifrin) - exacerbation of narrow-angle glaucoma - macular edema (30%) Drug interactions: 1) alpha & beta blockers antagonize effects of epinephrine 2) tricyclic antidepressants (TCA) increase cardiac irritability by inhibiting re-uptake 3) general anesthetics increase cardiac irritability Mechanism of action: 1) full sympathetic agonist, alpha 1 & 2, beta 1 & 2 2) affinity for adrenergic receptors [9] - beta-1 adrenergic receptor > beta-2 adrenergic receptor - alpha-1 adrenergic receptor = beta-1 adrenergic receptor 3) respiratory effects a) beta-2 agonist activity relaxes bronchial smooth muscle b) constricts bronchial arterioles c) relieves bronchospasm d) reduces congestion & edema e) increases tidal volume f) no respiratory effects are durable g) antagonizes histamine release & binding 4) cardiovascular effects a) beta-1 agonism produces positive inotropic & chronotropic effects b) increased systemic vascular resistance 5) ophthalmic agent (Epifrin) a) reduction of aqueous humor production b) increased aqueous outflow

Interactions

molecular events drug adverse effects (more general classes)

Related

adrenergic receptor epinephrine in plasma epinephrine metabolism

Specific

adrenochrome epinephrine inhaler (Asthmanefrin, Primatene Mist)

General

beta-adrenergic receptor agonist catecholamine vasoconstrictor agent or vasopressor

Properties

AGONIST-FOR: beta adrenergic receptor MISC-INFO: elimination route PLASMA pregnancy-category C safety in lactation -

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Saunders Manual of Medical Practice, Rakel (ed), WB Saunders, Philadelphia, 1996, pg 67
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  4. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  5. Press Release August 13, 2012 SANOFI ANNOUNCES FDA APPROVAL FOR AUVI-Q , FIRST VOICE-GUIDED EPINEPHRINE AUTO-INJECTOR FOR PATIENTS WITH LIFE-THREATENING ALLERGIES http://sanofi.mediaroom.com/index.php?s=33507&item=131480 - Auvi-Q Website https://www.auvi-q.com/
  6. Prescriber's Letter 20(3): 2013 New Talking Epinephrine Auto-Injectors: Auvi-Q and Allerject Detail-Document#: 290311 (subscription needed) http://www.prescribersletter.com
  7. Deprecated Reference
  8. The NNT: Inhaled Epinephrine with or without Steroids for Bronchiolitis. http://www.thennt.com/nnt/inhaled-epinephrine-steroids-for-bronchiolitis/ - Hartling L, Bialy LM, Vandermeer B et al Epinephrine for bronchiolitis. Cochrane Database Syst Rev. 2011 Jun 15;(6):CD003123 PMID: 21678340
  9. Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015
  10. Casale TB, Ellis AK, Nowak-Wegrzyn A et al Pharmacokinetics/pharmacodynamics of epinephrine after single and repeat administration of neffy, EpiPen, and manual intramuscular injection. J Allergy Clin Immunol. 2023 Aug 19:S0091-6749(23)01059-X. PMID: 37604314 Free article. - Herpen R FDA approves epinephrine nasal spray for anaphylaxis. Healio. August 09, 2024 https://www.healio.com/news/allergy-asthma/20240809/fda-approves-epinephrine-nasal-spray-for-anaphylaxis - FDA News Release. August 09, 2024 FDA Approves First Nasal Spray for Treatment of Anaphylaxis. https://www.fda.gov/news-events/press-announcements/fda-approves-first-nasal-spray-treatment-anaphylaxis

Component-of

articaine/epinephrine (Septocaine) bupivacaine/epinephrine bupivacaine/epinephrine/fentanyl epinephrine autoinjector (Epipen, Symjepi) epinephrine/etidocaine epinephrine/lidocaine/tetracaine epinephrine/lidocaine; lidocaine (Xylocaine) with epinephrine epinephrine/pilocarpine (E-Pilo-x PxEx) epinephrine/prilocaine epinephrine/zinc chloride epinephrine/zinc phenolsufonate insect sting or anaphylaxis kit (Ana-Kit) lidocaine/epinephrine topical (LidoSite)