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|Epinephrine

Epinephrine

Trade Names:
Adrenalin Chloride
- Solution for injection 1 mg/mL (1:1,000) as hydrochloride
- Solution for injection 10 mg/mL (1:100) as hydrochloride

Trade Names:
EpiPen
- Solution 1 mg/mL (1:1,000)

Trade Names:
EpiPen Jr.
- Solution 0.5 mg/mL (1:2,000)

Trade Names:
microNefrin
- Solution for inhalation 2.25% racepinephrine hydrochloride

Trade Names:
Primatene Mist
- Aerosol 0.22 mg epinephrine per spray

Trade Names:
S2
- Solution for inhalation 2.25% racepinephrine hydrochloride

Mechanism of Action

Pharmacology

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

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 excreted as unchanged drug or conjugated.

Onset

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

Duration

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

Indications and Usage

Treatment and prophylaxis of cardiac arrest and attacks of transitory AV heart block; treatment of Adams-Stokes syndrome; treatment of hay fever; relief of bronchial asthma; treatment of syncope caused by heart block or carotid sinus hypersensitivity; symptomatic relief of serum sickness, urticaria, and angioedema; relaxation of uterine musculature; anaphylaxis; allergic reactions (eg, bronchospasm, urticaria, pruritus, angioneurotic edema, swelling of the lips, eyelids, tongue, and nasal mucosa) because of anaphylactic shock caused by stinging insects (primarily of the order Hymenoptera , which includes bees, wasps, hornets, yellow jackets, bumble bees, and fire ants); severe allergic or anaphylactoid reactions caused by allergy injections; exposures to pollens, dusts molds, foods, drugs; exercise; unknown substances (so-called idiopathic anaphylaxis); severe, life-threatening asthma attacks characterized by wheezing, dyspnea, and inability to breathe.

Treatment of nasal congestion; relief of eustachian tube congestion.

Temporary relief from acute paroxysms of bronchial asthma and other states; treatment of postintubation and infectious croup.

Contraindications

Hypersensitivity to epinephrine; narrow-angle glaucoma; concomitant use during general anesthesia with halogenated hydrocarbons or cyclopropane; cerebral arteriosclerosis or organic brain damage; use with anesthesia for fingers and toes; use during labor; phenothiazine-induced circulatory collapse; MAO inhibitor therapy; nonanaphylactic shock during general anesthesia with halogenated hydrocarbons or cyclopropane; organic heart disease; cardiac dilation and coronary insufficiency.

Dosage and Administration

IV/Intracardiac 0.5 to 1 mg (5 to 10 mL of 1:10,000 solution) q 5 minute as needed. Myocardial injection usually given in left ventricular chamber by trained personnel at dose of 0.3 to 0.5 mg.

IV 1 mg in 250 mL of D5W (4 mcg/mL) for infusion at 1 to 4 mcg/min (15 to 60 mL/hr).

Intraspinal 0.2 to 0.4 mL of 1:1,000 solution added to anesthetic spinal fluid mixture. Epinephrine 1:100,000 to 1:200,000 is usual concentration employed with local anesthetics.

IM ( Epipen ) Usual dose is 0.3 mg.

IM ( Epipen or Epipen Jr ) 0.01 mg/kg is recommended.

Nasal Apply as drops, spray, or with sterile swab as required.

Inhalation Hand pump nebulizer : Place 0.5 mL (approximately 8 to 10 drops) of racemic epinephrine into nebulizer reservoir. Squeeze bulb 1 to 3 times in partially opened mouth. If relief does not occur within 2 to 3 minutes, administer 2 to 3 additional inhalations. Do not administer more often than q 3 hr. Aerosol-nebulizer : Add 0.5 mL (approximately 10 drops) racemic epinephrine to 3 mL of diluent or 0.2 to 0.4 mL (approximately 4 to 8 drops) of MicroNefrin to 4.6 to 4.8 mL water. Administer for 15 minutes q 3 to 4 hr. Aerosol : Start with 1 inhalation, then wait at least 1 minute; repeat once more if needed. Do not use again for at least 3 hr.

Subcutaneous/IM Solution (1:1,000) : 0.2 to 1 mL (0.2 to 1 mg); repeat q 4 hr. IV Solution (1:10,000) : 0.1 to 0.25 mg (1 to 2.5 mL) injected slowly.

Subcutaneous Solution (1:1,000) : 0.01 mL/kg or 0.3 mL/m ² (0.01 mg/kg or 0.3 mg/m ² ); repeat q 20 minutes to 4 hr. Do not exceed 0.5 mL (0.5 mg) in single dose. IV Solution (1:10,000) : 0.01 mg/kg to 0.05 mg repeated at 20 to 30 minute intervals.

General Advice

Multiple concentrations and dosage forms are available. Ensure the proper concentration and dose form is being used.

• Do not administer if particulate matter, cloudiness, or discoloration noted.
• Preferred route of administration is subcutaneous or IM. IV administration is usually used for medical emergencies (eg, cardiac arrest, life-threatening bronchospasm, anaphylaxis). Injection solution also can be administered via endotracheal tube directly into bronchial tree, if ordered, when using for cardiac resuscitation.
• Rotate subcutaneous administration sites to reduce chance of injection-site reaction.
• Discard any unused solution when using single-dose vials or ampules.

• Do not use if solution is pinkish or darker than slightly yellow, or if it contains a precipitate.

• Have patient inhale 1 spray. Repeat 1 time if symptoms are not relieved after 1 minute.

Storage/Stability

Store inhalation solution and inhalation aerosol at controlled room temperature (68° to 77°F). Store all other dose forms at controlled room temperature (59° to 86°F). Protect from light, extreme heat, and freezing. Do not remove ampules or syringes from carton until ready to use.

Drug Interactions

Vasoconstricting and hypertensive effects are antagonized.

Epinephrine effects may be potentiated.

May decrease effects of these agents, resulting in hypertension.

Vascular response may be decreased.

Pressor effects of epinephrine may be reversed.

May cause hypertension.

The potential for the myocardium to be sensitized to the effects of sympathomimetic amines is increased. Arrhythmias may result with coadministration and may respond to beta-blockers.

May increase pressor response.

Epinephrine effects may be potentiated.

May cause severe persistent hypertension.

May potentiate epinephrine"s vasopressive effects.

Incompatibility

Epinephrine is unstable in alkaline solutions (eg, sodium bicarbonate); avoid admixture.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Cardiac arrhythmias and excessive hypertension; palpitations (especially in hyperthyroid and hypertensive patients); tachycardia; anginal pain in predisposed patients; cerebral and subarachnoid hemorrhage; flushing.

CNS

Anxiety; headache; restlessness; tremor; weakness; hemiplegia; dizziness; insomnia.

EENT

Nasal use: Local irritation; sneezing; rebound congestion.

GI

Nausea; vomiting.

Genitourinary

Decreased urine formation with initial parenteral use.

Respiratory

Shortness of breath.

Miscellaneous

Severe metabolic acidosis; pallor; urticaria; wheal and hemorrhage at site of injection; necrosis at injection site following repeated injections; sweating; transient elevations of blood glucose; elevated serum lactic acid.

Precautions

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.

Special Risk Patients

Use drug with caution in elderly patients, patients with CV disease, pulmonary edema, hypertension, hyperthyroidism, diabetes, psychoneurotic illness, asthma, prefibrillatory rhythm, or anesthetic cardiac accidents.

Sulfite Sensitivity

Some products contain sulfites; use drug with caution in sulfite-sensitive individuals.

Bronchial asthma/Emphysema

Administer with extreme caution to patients with long-standing bronchial asthma and emphysema who develop degenerative heart disease.

Cerebrovascular hemorrhage

May result from overdosage or inadvertent IV injection.

Fatalities

Death may result from pulmonary edema because of peripheral constriction and cardiac stimulation produced.

Pulmonary edema

May cause fatalities because of peripheral constriction or cardiac stimulation.

Overdosage

Symptoms

Precordial distress, vomiting, headache, shortness of breath, unusually elevated BP, cerebrovascular hemorrhage, pulmonary arterial hypertension, pulmonary edema, ventricular hyperirritability, bradycardia, tachycardia, arrhythmias, extreme pallor, cold skin, metabolic acidosis, kidney failure.

Patient Information

• Explain name, dose, action, and potential side effects of drug.

• Injection
• Advise patient, family, or caregiver that medication (other than that delivered by auto-injector) will be prepared and administered by a health care provider in a medical setting.
• Ensure patient using auto-injector understands how to store, prepare the auto-injector, administer the injection, and dispose of used equipment.
• Ensure patient using auto-injector 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 patients 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.