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Epinephrine

Pronunciation

Pronunciation: ep-i-NEF-rin
Class: Sympathomimetic, Vasopressor used in shock

Trade Names

Adrenalin Chloride
- Solution, intranasal 1:1,000 (1 mg/mL) as hydrochloride
- Injection, solution 1:1,000 (1 mg/mL) as hydrochloride

Epinephrine
- Injection, solution 1:10,000 (0.1 mg/mL) as hydrochloride
- Injection, solution 1:1,000 (1 mg/mL) as hydrochloride
- Injection, solution 1:1,000 (0.3 mg per 0.3 mL) single-dose prefilled syringe
- Aerosol, inhalation 0.22 mg/spray

EpiPen
- Injection, solution 1:1,000 (0.3 mg per 0.3 mL)

EpiPen Jr.
- Injection, solution 1:2,000 (0.15 mg per 0.3 mL)

Primatene Mist
- Aerosol, inhalation 0.22 mg of epinephrine per spray

S2
- Solution, inhalation 1.125% (2.25% racepinephrine hydrochloride)

Twinject
- Injection, solution 1:1,000 (0.15 mg per 0.15 mL)
- Injection, solution 1:1,000 (0.3 mg per 0.3 mL)

Pharmacology

Stimulates alpha and beta receptors (alpha receptors at high doses; beta- 1 and beta- 2 receptors at moderate doses) within the sympathetic nervous system. Relaxes smooth muscle of bronchi and iris, and is an antagonist of histamine.

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Pharmacokinetics

Metabolism

Inactivated by enzymatic transformation to metabephrine or normetanephrine; these are subsequently conjugated and excreted in the urine.

Elimination

Mostly excreted in urine as inactive metabolites; remainder is excreted as unchanged drug or is conjugated.

Onset

5 to 10 min (subcutaneous), 1 to 5 min (inhalation).

Duration

4 to 6 h (subcutaneous), 1 to 4 h (IM), 1 to 3 h (inhalation).

Indications and Usage

Epinephrine 1:1,000 injection

Relief of respiratory distress due to bronchospasm; to provide rapid relief of hypersensitivity reactions to drugs and other allergens (eg, anaphylactic reactions to drugs, animal serums, insect stings); to prolong the action of local and regional anesthetics; restore cardiac rhythm in cardiac arrest due to various causes; treatment of mucosal congestion of hay fever, rhinitis, and acute sinusitis; relieve bronchial asthmatic paroxysms; symptomatic relief of serum sickness, urticaria, angioneurotic edema; for relaxation of uterine musculature and to inhibit uterine contractions; epinephrine injection can be used as a hemostatic agent; in syncope due to complete heart block or carotid sinus hypersensitivity; for resuscitation in cardiac arrest following anesthetic accidents; used in open-angle glaucoma.

Epinephrine 1:1,000 (auto-injector) and 1:2,000 (auto-injector), Prefilled syringe

Emergency treatment of allergic reactions (type I) including anaphylaxis to insect stings (eg, bees, fire ants, hornets, yellow jackets, wasps) and biting insects (eg, mosquitoes), allergen immunotherapy, foods, drugs, diagnostic testing substances (eg, radiocontrast media), and other allergens, as well as idiopathic anaphylaxis or exercise-induced anaphylaxis. The auto-injectors and prefilled syringes are intended for immediate self-administration in patients who are at increased risk for anaphylaxis, including individuals with a history of anaphylactic reactions. Auto-injectors and prefilled syringes are for immediate use and are not a substitute for immediate medical attention.

Epinephrine 1:10,000 injection

Treatment and prophylaxis of cardiac arrest in the absence of ventricular fibrillation and attacks of transitory atrioventricular heart block with syncopal seizures; to stimulate the heart in syncope due to complete heart block or carotid sinus hypersensitivity; for resuscitation in cardiac arrest following anesthetic accidents; in cardiopulmonary resuscitation, intracardiac puncture and intramyocardial injection of epinephrine may be effective when external cardiac compression and attempts to restore the circulation by electrical defibrillation or use of pacemaker fail; seldom used as a vasopressor except in the treatment of anaphylactic shock and under certain conditions in insulin shock.

Nasal solution

Nasal decongestant.

Oral inhalation

Temporary relief of shortness of breath, tightness of chest, and wheezing due to bronchial asthma; temporary relief of bronchial asthma; easing breathing for asthma patients by reducing spasms of bronchial muscles.

Unlabeled Uses

Endoscopic injection for the management of acute lower GI bleeding; overdosage of beta-blockers, calcium channel blockers, and tricyclic antidepressants (and other sodium channel blockers); symptomatic bradycardia or hypotension that did not respond to atropine and transcutaneous pacing.

Contraindications

Note: There are no absolute contraindications to use in a life-threatening situation. Narrow-angle glaucoma; shock (nonanaphylactic); during general anesthesia with halogenated hydrocarbons or cyclopropane; individuals with organic brain damage; local anesthesia of certain areas (eg, fingers, toes); use during labor; use in cardiac dilation and coronary insufficiency; situations in which vasopressor drugs may be contraindicated (eg, diabetes, hypertension and other CV disorders, obstetrics when maternal BP is in excess of 130/80, in thyrotoxicosis); hypersensitivity to sympathomimetic amines.

Dosage and Administration

Allergic Emergencies/Anaphylaxis
Adults and Children

IM/Subcutaneous EpiPen , Twinject , prefilled syringe: Patients weighing 30 kg (66 lb) or more - 0.3 mg. EpiPen Jr , Twinject : Patients weighing 15 to 30 kg (33 to 66 lb) - 0.15 mg.

Adults

IM/Subcutaneous 1:1,000 (1 mg/mL) solution: 0.2 to 1 mg (mL), repeated every 10 to 15 min as needed. IV 1:10,000 (0.1 mg/mL) solution: 0.1 to 0.25 mg (1 to 2.5 mL), administered slowly over 5 min. Repeat every 5 to 15 min as needed.

Children

Subcutaneous 1:1,000 (1 mg/mL) solution: 0.01 mg/kg (or 0.3 mg/m 2 ) (max 0.5 mg/dose). May be repeated every 15 min for 2 doses, then every 4 h as needed. IV 1:10,000 (0.1 mg/mL): 0.3 mg (3 mL) administered slowly. Repeat every 15 min for 3 or 4 doses as needed.

Asthma
Adults and Children 4 Yr of Age and Older

Oral inhalation Primatene Mist : Start with 1 inhalation, then wait 1 min. If not relieved, use once more. Do not use again for at least 3 h (OTC). S2 : Add 0.5 mL (contents of 1 vial) of solution to nebulizer. Use 1 to 3 inhalations not more often than every 3 h (OTC).

Adults

IM/Subcutaneous 1:1,000 (1 mg/mL) solution: 0.2 to 1 mg (mL). Start with a small dose and increase if required. IV 1:10,000 (0.1 mg/mL) 0.1 to 0.25 mg (1 to 2.5 mL) injected slowly.

Children

Subcutaneous 1:1,000 (1 mg/mL) 0.01 mg/kg (or 0.3 mg/m 2 ) (max 0.5 mg/dose) every 4 h as needed.

Cardiac Arrest
Adults

IV 1:10,000 (0.1 mg/mL) solution: 0.1 to 1 mg (1 to 10 mL), repeated every 5 min, if necessary. Alternatively, in intubated patients, epinephrine can be injected via the endotracheal tube directly into the bronchial tree at the same dose as for IV injection. Intracardiac 1:10,000 (0.1 mg/mL) solution: 0.3 to 0.5 mg (3 to 5 mL). This route should only be used if there is insufficient time to establish an IV route and should only be administered by personnel well trained in this technique.

Children

IV 1:10,000 (0.1 mg/mL): 0.005 to 0.01 mg/kg.

Intraspinal
Adults

Intraspinal 1:1,000 (1 mg/mL) injection solution (preservative free, sulfite free) 0.2 to 0.4 mg added to anesthetic spinal fluid mixture. Epinephrine 1:100,000 (0.01 mg/mL) to 1:20,000 (0.05 mg/mL) is the usual concentration employed with local anesthetics.

Nasal Congestion
Adults and Children 6 yr of age and older

Topical Apply as drops, spray, or with sterile swab as needed.

Ophthalmologic Use for Producing Conjunctival Decongestion, to Control Hemorrhage, to Produce Mydriasis, to Reduce Intraocular Pressure

Ophthalmic Use concentrations of 1:10,000 to 1:1,000.

General Advice

Multiple concentrations and dosage forms are available. Ensure the proper concentration and doseform are being used.

Injection
  • Incompatibilities: Epinephrine is destroyed by alkalines and oxidizing agents (eg, bromine, chlorine, chromates, iodine, nitrates, oxygen, permanganates, salts of easily reducible metals [eg, iron]).
  • Subcutaneous is the preferred route of administration. For medical emergencies, the IV route is usually used. If given IM, avoid injection into the buttocks.
  • Subcutaneous injection results in slower absorption.
  • Inspect visually for particulate matter and discoloration whenever solution and container permit.
  • Cardiac resuscitation: In adults, the effect of IV epinephrine (1:10,000) may only last a few minutes; therefore, the IV dose may be followed by 0.3 mg of 1:1,000 (1 mg/mL) subcutaneously.
  • Note: Intracardiac injection is no longer recommended in Advanced Cardiac Life Support (ACLS) guidelines.
Auto-injector, Prefilled syringe
  • Only inject into the anterolateral aspect of the thigh, through clothing if necessary.
  • Auto-injector: Do not inject IV. Only inject into the anterolateral aspect of the thigh. Do not inject into the buttock; this may not provide effective treatment for anaphylaxis.
  • According to ACLS guidelines, IM injection is the preferred route of administration for patients with anaphylaxis with signs of systemic reaction.
Solution
  • Do not use an epinephrine solution if it is pinkish or darker than slightly yellow or if it contain a precipitate.

Storage/Stability

Adrenalin nasal solution

Store at 59° to 77°F. Protect from light. Protect from freezing.

Epinephrine injection, auto-injectors, and prefilled syringes

Store at 59° to 86°F. Protect from light. Protect from freezing. Discard vial and contents 30 days after initial use.

Primatene Mist

Store at 68° to 77°F.

S2

Store at 36° to 68°F. Protect from light. Avoid excessive heat.

Drug Interactions

Alpha-adrenergic blocking agents (eg, phentolamine), ergot derivative (eg, ergotamine), nitrites, phenothiazines (eg, chlorpromazine)

May counteract the epinephrine pressor effects.

Antihistamines (eg, chlorpheniramine, diphenhydramine), COMT inhibitors (eg, entacapone, tolcapone), levothyroxine, linezolid, MAOIs (eg, phenelzine), tricyclic antidepressants (amitriptyline)

Epinephrine effects may be potentiated.

Beta-adrenergic blockers (eg, propranolol)

Beta-adrenergic effects of epinephrine may be blocked, resulting in hypertension.

Diuretics

May decrease vascular response to epinephrine.

Drugs that sensitize the heart to arrhythmias (eg, antiarrhythmics, digitalis, diuretics, quinidine)

Epinephrine may precipitate or aggravate angina pectoris or produce ventricular arrhythmias.

Furazolidone, methyldopa, rauwolfia alkaloids (eg, alseroxylon, rauwolfia)

Risk of hypertension may be increased.

General anesthetics (eg, cyclopropane, halothane)

Coadministration is contraindicated; may induce cardiac arrhythmias.

Guanethidine

Neuronal blockade may be antagonized by epinephrine, resulting in decreased antihypertensive effect and requiring subsequent dosage adjustments.

Oxytocic drugs

Severe persistent hypertension may occur; rupture of a cerebral blood vessel may occur during the postpartum period.

Sympathomimetic agents (eg, isoproterenol)

Possible additive effects and increased toxicity (eg, serious cardiac arrhythmias); administer alternatively when the preceding effect of the other drug has subsided, not concurrently.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Angina; cardiac arrhythmias including fatal ventricular fibrillation; excessive and/or rapid rise in BP; palpitations.

CNS

Anxiety; apprehension; cerebral hemorrhage; dizziness; fear; headache; hemiplegia; restlessness; subarachnoid hemorrhage; tremor; weakness.

Dermatologic

Sweating.

GI

Nausea; vomiting.

Local

Necrosis.

Respiratory

Respiratory difficulty.

Miscellaneous

Pallor.

Precautions

Monitor

Monitor patient's respiratory status during each treatment with inhalation solution and aerosol. If bronchospasm worsens during a treatment, discontinue the treatment.


Pregnancy

Category C .

Lactation

Excreted in breast milk.

Children

Administer drug with caution. Syncope has occurred in asthmatic children.

Labor and Delivery

Do not use when maternal BP exceeds 130/80 mm Hg; may delay second stage or induce uterine atony.

Renal Function

Parenterally administered epinephrine initially may produce constriction of renal blood vessels and decease urine blood flow.

Special Risk Patients

Use with caution in elderly patients; in patients with CV disease, diabetes, hypertension or hyperthyroidism, and psychoneurotic individuals; in patients with long-standing bronchial asthma and emphysema who have developed degenerative heart disease; in patients with ventricular fibrillation; in patients with prefibrillatory rhythm; and in pregnancy.

Sulfite Sensitivity

Some products contain sulfites; in serious allergic, emergency, or life-threatening situations, use with caution in sulfite-sensitive individuals.

CV effects

Inadvertently induced high arterial BP may result in angina pectoris or aortic rupture; potentially serious cardiac arrhythmias may occur in patients not suffering from heart disease and patients with organic heart disease or who are receiving drugs that sensitize the myocardium; a paradoxical but transient lowering of BP, bradycardia, and apnea may occur immediately after injection.

Cerebrovascular hemorrhage

May result from overdosage or inadvertent IV injection.

Extravasation

Tissue necrosis may develop if extravasation occurs.

Hypovolemia

Epinephrine use is not a replacement for blood, plasma, fluids, and electrolytes, which should be restored promptly when loss has occurred.

Pulmonary edema

May cause fatalities because of peripheral constriction or cardiac stimulation.

Overdosage

Symptoms

Cerebrovascular hemorrhage from extremely elevated arterial pressure, dyspnea, elevated BP, extreme pallor and coldness of the skin, fatal cardiac arrhythmia, headache, kidney failure, metabolic acidosis, pulmonary edema, precordial distress, premature ventricular contractions followed by multifocal ventricular tachycardia and occasionally by AV block, transient bradycardia, vomiting.

Patient Information

  • Injection
  • Advise patient, family, or caregiver that medication (other than that delivered by auto-injector or prefilled syringe) will be prepared and administered by a health care provider in a medical setting.
  • Advise patient using the auto-injector or prefilled syringe ( Adamis Laboratories ) to go immediately to the nearest emergency room for further treatment of anaphylaxis.
  • Ensure patient using auto-injector understands how to store, prepare the auto-injector or prefilled syringe, administer the injection, and dispose of used equipment.
  • Ensure patient using auto-injector or prefilled syringe understands how and when to use oral medications for allergic reactions (eg, antihistamines, corticosteroids) if prescribed or recommended by health care provider.
  • Inhalation Solution and Aerosol
  • If using solution for inhalation, ensure patient or caregiver can prepare, use, and clean the nebulizer without difficulty. If using the aerosol, ensure patient understands how to store and use the inhaler properly.
  • Instruct patient not to mix with other nebulizer medications unless advised by health care provider.
  • Instruct patient not to exceed prescribed dose or frequency of use. Advise patient to contact health care provider if this medication no longer seems to control asthma symptoms or if increasing doses of the medicine are needed. This may indicate worsening asthma.
  • Advise patient using more than 1 inhaled medication to use this medication first if needed. Inhaled corticosteroids or other inhaled controller medications should be taken last.
  • Advise patient that if breathing symptoms worsen during or immediately after using this medication to stop using it and inform health care provider immediately.
  • Caution patient not to use solution if it is pinkish or darker than slightly yellow, or if it contains a precipitate.
  • Caution patient not to puncture canister, dispose of used aerosol canister in incinerator, or store canister near open flame or heat above 120°F.
  • Topical Solution
  • Ensure patient or caregiver understands how and when to apply topical solution as drops, spray, or directly on mucosal surface with sterile swab, as directed.
  • Advise patient or caregiver not to increase the frequency of use if symptoms of congestion do not improve or worsen but to notify health care provider.

Copyright © 2009 Wolters Kluwer Health.

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