Wednesday, July 19, 2023

EPINEPHrine (ep-i-nef-rin) Adrenaclick, Adrenalin, Allerject, Anapen, Anapen Junior, AsthmaNefrin, Auvi-Q, EpiPen, S-2 (racepinephrine), Twin-Ject

 Indications

Subcut, IM, IV: Management of severe allergic reactions.

IV, Intracardiac, Intratracheal, Intraosseous

(part of advanced cardiac life support

[ACLS] and pediatric advanced life support

[PALS] guidelines): Management of cardiac arrest

(unlabeled). Subcut, IM: Management of reversible

airway disease due to asthma or COPD (unlabeled).

Inhaln: Management of upper airway obstruction

and croup (racemic epinephrine). Local/Spinal:

Adjunct in the localization/prolongation of anesthesia.

Action

Results in the accumulation of cyclic adenosine monophosphate

(cAMP) at beta-adrenergic receptors. Affects

both beta1(cardiac)-adrenergic receptors and

beta2(pulmonary)-adrenergic receptor sites. Produces

bronchodilation. Also has alpha-adrenergic agonist

properties, which result in vasoconstriction. Inhibits

the release of mediators of immediate hypersensitivity

reactions from mast cells. Therapeutic Effects:

Bronchodilation. Maintenance of heart rate and BP. Localization/

prolongation of local/spinal anesthetic.

Pharmacokinetics

Absorption: Well absorbed following subcut administration;

some absorption may occur following repeated

inhalation of large doses.

Distribution: Does not cross the blood-brain barrier;

crosses the placenta and enters breast milk.

Metabolism and Excretion: Action is rapidly terminated

by metabolism and uptake by nerve endings.

Half-life: Unknown.

TIME/ACTION PROFILE (bronchodilation)

ROUTE ONSET PEAK DURATION

Inhaln 1 min unknown 1–3 hr

Subcut 5–10 min 20 min 1–4 hr

IM 6–12 min unknown 1–4 hr

IV rapid 20 min 20–30 min

Contraindications/Precautions

Contraindicated in: Hypersensitivity to adrenergic

amines; Some products may contain bisulfites and

should be avoided in patients with known hypersensitivity

or intolerance.

Use Cautiously in: Cardiac disease (angina, tachycardia,

MI); Hypertension; Hyperthyroidism; Parkinson’s

disease; Pheochromocytoma; Diabetes; Cerebral

arteriosclerosis; Glaucoma (except for ophthalmic

use); Excessive use may lead to tolerance and paradoxical

bronchospasm (inhaler); OB: Use only if potential

maternal benefit outweighs potential risks to fetus; Lactation:

High intravenous doses of epinephrine mightp

milk production or letdown. Low-dose epidural, topical,

inhaled, or ophthalmic epinephrine are unlikely to

interfere with breast feeding (NIH); Geri: More susceptible

to adverse reactions; may requirepdose.

Adverse Reactions/Side Effects

CNS: nervousness, restlessness, tremor, headache, insomnia.

Resp: PARADOXICAL BRONCHOSPASM (EXCESSIVE

USE OF INHALERS). CV: angina, arrhythmias, hypertension,

tachycardia. Derm: skin and soft tissue infections

(including necrotizing fasciitis and myonecrosis).

GI: nausea, vomiting. Endo: hyperglycemia. 

Interactions

Drug-Drug: Concurrent use with other adrenergic

agents will have additive adrenergic side effects. Use

with MAO inhibitors may lead to hypertensive crisis.

Beta blockers may negate therapeutic effect. Tricyclic

antidepressants enhance pressor response to

epinephrine.

Drug-Natural Products: Use with caffeine-containing

herbs (cola nut, guarana, mate, tea, coffee)

qstimulant effect.

Route/Dosage

Subcut, IM (Adults and Children 30 kg): Severe

anaphylaxis—0.3–0.5 mg (single dose not to exceed

0.5 mg); may repeat every 10–15 min as needed.

Subcut (Children 30 kg): Severe anaphylaxis—

0.01 mg/kg (not to exceed 0.3 mg/dose); may repeat

every 10–15 min as needed.

IV (Adults): Severe anaphylaxis—0.1–0.25 mg

every 5–15 min; may be followed by 1–4 mcg/min

continuous infusion; cardiopulmonary resuscitation

(ACLS guidelines)—1 mg every 3–5 min; bradycardia

(ACLS guidelines)—2–10 mcg/min).

IV (Children): Severe anaphylaxis—0.1 mg (less in

younger children); may be followed by 0.1 mcg/kg/min

continuous infusion (may bequp to 1.5 mcg/kg/min);

symptomatic bradycardia/pulseless arrest (PALS

guidelines)—0.01 mg/kg, may be repeated every 3–5

min, higher doses (up to 0.1–0.2 mg/kg) may be considered;

may also be given by the intraosseous route.

May also be given by the endotracheal route in doses of

0.1–0.2 mg/kg diluted to a volume of 3–5 mL with

normal saline followed by several positive pressure ventilations.

Inhaln (Adults): Inhalation solution—1 inhalation

of 1% solution; may be repeated after 1–2 min; additional

doses may be given every 3 hr; racepinephrine—

Via hand nebulizer, 2–3 inhalations of

2.25% solution; may repeat in 5 min with 2–3 more inhalations,

up to 4–6 times daily.

Inhaln (Children 1 mo): 0.25–0.5 mL of 2.25%

racemic epinephrine solution diluted in 3 mL normal

saline.

IV, Intratracheal (Neonates): 0.01–0.03 mg/kg

every 3–5 min as needed.

Intracardiac (Adults): 0.3–0.5 mg.

Endotracheal (Adults): Cardiopulmonary resuscitation

(ACLS guidelines)—2–2.5 mg.

Topical (Adults and Children 6 yr): Nasal decongestant—

Apply 1% solution as drops, spray, or with a

swab.

Intraspinal (Adults and Children): 0.2–0.4 mL of

1:1000 solution.

With Local Anesthetics (Adults and Children): Use

1:200,000 solution with local anesthetic.

Availability (generic available)

Inhalation solution (racepinephrine): 2.25%.

Intranasal solution: 1 mg/mL (1:1000). Solution

for injection: 0.1 mg/mL (1:10,000), 1 mg/mL

(1:1000). Autoinjector (Auvi-Q, EpiPen): 0.15 mg/

0.15 mL (1:1000), 0.15 mg/0.3 mL (1:2000), 0.3 mg/

0.3 mL (1:1000).

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