Yes

Alpha/Beta Agonist; Antidote; Ophthalmic Agent, Antiglaucoma

Treatment of bronchospasms, anaphylactic reactions, cardiac arrest, management of open-angle (chronic simple) glaucoma

C

Clinical effects on the fetus: Crosses the placenta. Reported association with malformations in 1 study; may be secondary to severe maternal disease.

Breast-feeding/lactation: No data on crossing into breast milk or clinical effects on the infant

Hypersensitivity to epinephrine or any component; cardiac arrhythmias, angle-closure glaucoma

Use with caution in elderly patients, patients with diabetes mellitus, cardiovascular diseases (angina, tachycardia, myocardial infarction), thyroid disease, or cerebral arteriosclerosis, Parkinson's; some products contain sulfites as preservatives. Rapid I.V. infusion may cause death from cerebrovascular hemorrhage or cardiac arrhythmias. Oral inhalation of epinephrine is not the preferred route of administration.

>10%:

Cardiovascular: Tachycardia (parenteral), pounding heartbeat

Central nervous system: Nervousness, restlessness

1% to 10%:

Cardiovascular: Flushing, hypertension

Central nervous system: Headache, dizziness, lightheadedness, insomnia

Gastrointestinal: Nausea, vomiting

Neuromuscular & skeletal: Weakness, trembling

Miscellaneous: Diaphoresis (increased)

<1%: Pallor, tachycardia, chest pain, increased myocardial oxygen consumption, cardiac arrhythmias, sudden death, anxiety, xerostomia, dry throat, decreased renal and splanchnic blood flow, acute urinary retention in patients with bladder outflow obstruction, precipitation of or exacerbation of narrow-angle glaucoma, wheezing

Hypertension which may result in subarachnoid hemorrhage and hemiplegia; symptoms of overdose include arrhythmias, unusually large pupils, pulmonary edema, renal failure, metabolic acidosis

There is no specific antidote for epinephrine intoxication and the bulk of the treatment is supportive. Hyperactivity and agitation usually respond to reduced sensory input; however, with extreme agitation, haloperidol (2-5 mg I.M. for adults) may be required. Hyperthermia is best treated with external cooling measures; or when severe or unresponsive, muscle paralysis with pancuronium may be needed. Hypertension is usually transient and generally does not require treatment unless severe. For diastolic blood pressures >110 mm Hg, a nitroprusside infusion should be initiated. Seizures usually respond to diazepam I.V. and/or phenytoin maintenance regimens.

Increased toxicity: Increased cardiac irritability if administered concurrently with halogenated inhalational anesthetics, beta-blocking agents, alpha-blocking agents

Epinephrine is sensitive to light and air; protection from light is recommended

Oxidation turns drug pink, then a brown color; solutions should not be used if they are discolored or contain a precipitate

Stability of injection of parenteral admixture at room temperature (25°C) or refrigeration (4°C): 24 hours

Standard diluent: 1 mg/250 mL NS

Compatible with dopamine, dobutamine, diltiazem

Incompatible with aminophylline, sodium bicarbonate or other alkaline solutions

Stimulates alpha-, beta₁-, and beta₂-adrenergic receptors resulting in relaxation of smooth muscle of the bronchial tree, cardiac stimulation, and dilation of skeletal muscle vasculature; small doses can cause vasodilation via beta₂-vascular receptors; large doses may produce constriction of skeletal and vascular smooth muscle; decreases production of aqueous humor and increases aqueous outflow; dilates the pupil by contracting the dilator muscle

Onset of bronchodilation: Subcutaneous: Within 5-10 minutes; Inhalation: Within 1 minute

Conjunctival instillation: Onset of effect: Intraocular pressures fall within 1 hour; Peak effect: Within 4-8 hours

Duration of ocular effect: 12-24 hours

Absorption: Orally ingested doses are rapidly metabolized in the GI tract and liver; pharmacologically active concentrations are not achieved

Distribution: Crosses the placenta; appears in breast milk

Metabolism: Following administration, drug is taken up into the adrenergic neuron and metabolized by monoamine oxidase and catechol-o-methyltransferase; circulating drug is metabolized in the liver

Elimination: Inactive metabolites (metanephrine and the sulfate and hydroxy derivatives of mandelic acid) and a small amount of unchanged drug is excreted in urine

Neonates: Cardiac arrest: I.V.: Intratracheal: 0.01-0.03 mg/kg (0.1-0.3 mL/kg of 1:10,000 solution) every 3-5 minutes as needed; dilute intratracheal doses to 1-2 mL with normal saline

Infants and Children:

Bronchodilator: S.C.: 10 mcg/kg (0.01 mL/kg of 1:1000) (single doses not to exceed 0.5 mg) or suspension (1:200): 0.005 mL/kg/dose (0.025 mg/kg/dose) to a maximum of 0.15 mL (0.75 mg for single dose) every 8-12 hours

Bradycardia:

I.V.: 0.01 mg/kg (0.1 mL/kg of 1:10,000 solution) every 3-5 minutes as needed (maximum: 1 mg/10 mL)

Intratracheal: 0.1 mg/kg (0.1 mL/kg of 1:1000 solution every 3-5 minutes); doses as high as 0.2 mg/kg may be effective

Asystole or pulseless arrest:

I.V. or intraosseous: First dose: 0.01 mg/kg (0.1 mL/kg of a 1:10,000 solution); subsequent doses: 0.1 mg/kg (0.1 mL/kg of a 1:1000 solution); doses as high as 0.2 mg/kg may be effective; repeat every 3-5 minutes

Intratracheal: 0.1 mg/kg (0.1 mL/kg of a 1:1000 solution); doses as high as 0.2 mg/kg may be effective

Hypersensitivity reaction: S.C.: 0.01 mg/kg every 15 minutes for 2 doses then every 4 hours as needed (single doses not to exceed 0.5 mg)

Refractory hypotension (refractory to dopamine/dobutamine): Continuous I.V. infusions of 0.1-1 mcg/kg/minute; titrate dosage to desired effect

Nebulization: 0.25-0.5 mL of 2.25% racemic epinephrine solution diluted in 3 mL normal saline, or L-epinephrine at an equivalent dose; racemic epinephrine 10 mg = 5 mg L-epinephrine; use lower end of dosing range for younger infants

Intranasal: Children greater than or equal to 6 years and Adults: Apply locally as drops or spray or with sterile swab

Adults:

Asystole:

I.V.: 1 mg every 3-5 minutes; if this approach fails, alternative regimens include:

Intermediate: 2-5 mg every 3-5 minutes

Escalating: 1 mg, 3 mg, 5 mg at 3-minute intervals

High: 0.1 mg/kg every 3-5 minutes

Intratracheal: 1 mg (although optimal dose is unknown, doses of 2-2.5 times the I.V. dose may be needed)

Bronchodilator: I.M., S.C. ( 1:1000): 0.1-0.5 mg every 10-15 minutes to 4 hours

Hypersensitivity reaction: I.M., S.C.: 0.2-0.5 mg every 20 minutes to 4 hours (single dose maximum: 1 mg)

Refractory hypotension (refractory to dopamine/dobutamine): Continuous I.V. infusion 1 mcg/minute (range: 1-10 mcg/minute); titrate dosage to desired effect; severe cardiac dysfunction may require doses >10 mcg/minute (up to 0.1 mcg/kg/minute)

Nebulization: Instill 8-15 drops into nebulizer reservoirs; administer 1-3 inhalations 4-6 times/day

Ophthalmic: Instill 1-2 drops in eye(s) once or twice daily; when treating open-angle glaucoma, the concentration and dosage must be adjusted to the response of the patient

No data reported

Pulmonary function, heart rate, blood pressure, site of infusion for blanching, extravasation; cardiac monitor and blood pressure monitor required

Therapeutic: 31-95 pg/mL (SI: 170-520 pmol/L)

bilirubin (S), catecholamines (U), glucose, uric acid (S)

Nervousness and restlessness are common; may cause insomnia

None reported; however, use cautiously with psychotropics that block alpha receptors (phenothiazines); may produce paradoxical hypotension

No information available to require special precautions

No effects or complications reported

Use this medication exactly as directed; do not take more than recommended dosage. Avoid other stimulant prescriptive or OTC medications to avoid serious overdose reactions. You may experience dizziness, blurred vision, restlessness (use caution when driving or engaging in tasks requiring alertness until response to drug is known); or difficulty urinating (empty bladder immediately before taking this medication). Report excessive nervousness or excitation, inability to sleep, facial flushing, pounding heartbeat, muscle tremors or weakness, chest pain or palpitations, bronchial irritation or coughing, or increased sweating.

Aerosol: Use aerosol or nebulizer as per instructions. Clear as much mucus as possible before use. Rinse mouth following each use. If more than one inhalation is necessary, wait 1 minute between inhalations. May cause restlessness or nervousness; use caution when driving or engaging in hazardous activities until response to medication is known. Report persistent nervousness, restlessness, sleeplessness, palpitations, tachycardia, chest pain, muscle tremors, dizziness, flushing, or if breathing difficulty persists.

Nasal: Instill 1 spray into each nostril 3-4 times a day. Report if symptoms worsen or nasal passages become irritated.

Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Consult prescriber if breast-feeding.

Patients should be cautioned to avoid the use of over-the-counter epinephrine inhalation products; beta₂-adrenergic agents for inhalation are preferred

Aerosol, oral:

Bitartrate (AsthmaHaler®, Bronitin®, Medihaler-Epi®, Primatene® Suspension): 0.3 mg/spray [epinephrine base 0.16 mg/spray] (10 mL, 15 mL, 22.5 mL)

Bronkaid®: 0.5% (10 mL, 15 mL, 22.5 mL)

Primatene®: 0.2 mg/spray (15 mL, 22.5 mL)

Auto-injector:

EpiPen®: Delivers 0.3 mg I.M. of epinephrine 1:1000 (2 mL)

EpiPen® Jr.: Delivers 0.15 mg I.M. of epinephrine 1:2000 (2 mL)

Solution:

Inhalation:

Adrenalin®: 1% [10 mg/mL, 1:100] (7.5 mL)

AsthmaNefrin®, microNefrin®, Nephron®, S-2®: Racepinephrine 2% [epinephrine base 1.125%] (7.5 mL, 15 mL, 30 mL)

Vaponefrin®: Racepinephrine 2% [epinephrine base 1%] (15 mL, 30 mL)

Injection:

Adrenalin®: 0.01 mg/mL [1:100,000] (5 mL); 0.1 mg/mL [1:10,000] (3 mL, 10 mL); 1 mg/mL [1:1000] (1 mL, 2 mL, 30 mL)

Suspension (Sus-Phrine®): 5 mg/mL [1:200] (0.3 mL, 5 mL)

Nasal (Adrenalin®): 0.1% [1 mg/mL, 1:1000] (30 mL)

Ophthalmic, as borate (Epinal®): 0.5% (7.5 mL); 1% (7.5 mL)

Ophthalmic, as hydrochloride (Epifrin®, Glaucon®): 0.1% (1 mL, 30 mL); 0.5% (15 mL); 1% (1 mL, 10 mL, 15 mL); 2% (10 mL, 15 mL)

Topical (Adrenalin®): 0.1% [1 mg/mL, 1:1000] (10 mL, 30 mL)

American College of Cardiology, American Heart Association Task Force, "Adult Advanced Cardiac Life Support" and "Pediatric Advanced Life Support Guidelines," JAMA, 1992, 268(16):2199-241 and 2262-75.

Cydulka R, Davison R, Grammer L, et al, "The Use of Epinephrine in the Treatment of Older Adult Asthmatics," Ann Emerg Med, 1988, 17(4):322-6.

Illi A, Sundberg S, Ojala-Karlsson P, et al, "The Effect of Entacapone on the Disposition and Hemodynamic Effects of Intravenous Isoproterenol and Epinephrine," Clin Pharmacol Ther, 1995, 58(2):221-7.

Klein JS, Rich MR, and Yunginger JW, "Myocardial Ischemia Without Coronary Artery Disease After Epinephrine Overdose for Insect Sting Reaction," J Allergy Clin Immunol, 1995, 95(2):371.

Kuracheck SC and Rockoff MA, "Inadvertent Intravenous Administration of Racemic Epinephrine," JAMA, 1984, 253(10):1441-2.

Murphy FT, Manown TJ, Knutson SW, et al, "Epinephrine-Induced Lactic Acidosis in the Setting of Status Asthmaticus," South Med J, 1995, 88(5):577-9.

Nicholson KE and Rogers JE, "Cocaine and Adrenaline Paste: A Fatal Combination?," BMJ, 1995, 311(6999):250-1.

Riou B, Barriot P, Rimailho A, et al, "Treatment of Severe Chloroquine Poisoning," N Engl J Med, 1988, 318(1):1-6.

Scalzo A, Keith G, and Thompson M, "Fatal Outcome After Massive Epinephrine Overdose by Intravenous Injection of an OTC Asthma Inhaler," Clin Toxicol, 1995, 33(5):501-2.

Waisman Y, Klein BL, Boenning DA, et al, "Prospective Randomized Double-Blind Study Comparing L-Epinephrine and Racemic Epinephrine Aerosols in the Treatment of Laryngotracheitis (Croup)," Pediatrics, 1992, 89(2):302-6.