ADRENALIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ADRENALIN (ADRENALIN).
Direct-acting sympathomimetic amine that acts on alpha- and beta-adrenergic receptors. Alpha-1 activation causes vasoconstriction, beta-1 activation increases heart rate and contractility, beta-2 activation causes bronchodilation.
| Metabolism | Primarily metabolized by catechol-O-methyltransferase (COMT) and monoamine oxidase (MAO). |
| Excretion | Primarily metabolized in the liver and other tissues by catechol-O-methyltransferase (COMT) and monoamine oxidase (MAO). Renal excretion of metabolites (metanephrine, vanillylmandelic acid) and unchanged drug (<2% as unchanged). Biliary/fecal excretion is minimal (<5%). |
| Half-life | Approximately 2-3 minutes for the parent drug in plasma; clinical effects are short-lived due to rapid uptake and metabolism. In severe shock or hepatic impairment, half-life may be slightly prolonged. |
| Protein binding | Approximately 15-20% bound to plasma proteins, primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Approximately 0.4-0.6 L/kg. This small Vd indicates limited distribution outside the vascular compartment, consistent with its hydrophilic nature and rapid inactivation. |
| Bioavailability | IM: 80-100% (absorption depends on injection site and blood flow); SC: variable, often <50% due to vasoconstriction; Oral: negligible (<2%) due to extensive first-pass metabolism; Inhalation: 10-20% (dependent on device and technique). |
| Onset of Action | Intravenous (IV): <1 minute; Intramuscular (IM): 5-10 minutes; Subcutaneous (SC): 10-20 minutes; Inhalation (nebulized): 1-5 minutes; Endotracheal: 10-15 seconds to 1 minute. |
| Duration of Action | IV: 5-10 minutes; IM: 1-2 hours; SC: 1-2 hours; Inhalation: 1-3 hours. Duration is dose-dependent; higher doses prolong effects but increase risk of adverse events. |
1 mg (1 mL of 1:1000 solution) intramuscularly or subcutaneously every 5-20 minutes as needed; for cardiac arrest: 1 mg intravenously or intraosseously every 3-5 minutes.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No specific dose adjustment guidelines; use caution in severe hepatic impairment. |
| Pediatric use | 0.01 mg/kg (0.01 mL/kg of 1:1000 solution) intramuscularly, maximum single dose 0.3 mg; repeat every 5-20 minutes as needed. |
| Geriatric use | No specific dose adjustment; monitor for hypertension, tachyarrhythmias, and myocardial ischemia due to increased sensitivity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ADRENALIN (ADRENALIN).
| Breastfeeding | Excreted in breast milk in minimal amounts; M/P ratio not established. Use with caution due to potential for infant tachycardia and hypertension. |
| Teratogenic Risk | FDA Pregnancy Category C. First trimester: Limited human data; animal studies show fetal abnormalities (including gastroschisis) at high doses. Second/third trimester: Theoretical risk of uteroplacental vasoconstriction and fetal hypoxia; use only if benefit outweighs risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
None currently.
| Serious Effects |
["Hypersensitivity to epinephrine or any component","Narrow-angle glaucoma (ophthalmic use)","Use during second stage of labor (may delay delivery)","Some formulations contain sulfites, avoid in sulfite-allergic patients unless life-threatening","Hemorrhagic, traumatic, or cardiogenic shock (relative)"]
| Precautions | ["May cause severe hypertension, myocardial ischemia, and arrhythmias","Use with caution in patients with hyperthyroidism, hypertension, cardiovascular disease, diabetes, or pheochromocytoma","May precipitate angina or acute myocardial infarction","Pulmonary edema risk with excessive doses","Tissue necrosis with extravasation","May worsen hyperglycemia"] |
| Food/Dietary | No clinically significant food interactions. However, avoid concomitant use with high-tyramine foods (e.g., aged cheeses, cured meats, fermented products) in patients taking MAOIs, as this may potentiate hypertensive effects. Caffeine-containing products may increase cardiac stimulation. Alcohol may reduce the effectiveness of epinephrine in reversing severe allergic reactions. |
Loading safety data…
| Monitor maternal vital signs (heart rate, blood pressure), fetal heart rate (for tachycardia or distress), uterine activity (for tetanic contractions), and signs of pulmonary edema. Continuous fetal monitoring recommended during labor. |
| Fertility Effects | No known direct effects on human fertility. Animal studies show no impairment at therapeutic doses. |
| Clinical Pearls | For anaphylaxis, administer epinephrine IM into the anterolateral thigh (vastus lateralis) for rapid absorption; avoid SC injection due to erratic absorption. IV administration is reserved for cardiac arrest or severe hypotension under continuous monitoring. Use with extreme caution in patients with coronary artery disease, hypertension, or hyperthyroidism due to risk of myocardial ischemia and hypertensive crisis. Monitor for rebound hypotension or arrhythmias after initial dose. Epinephrine is pregnancy category C; use only if benefit outweighs risk. |
| Patient Advice | Carry your epinephrine auto-injector at all times; check expiration dates monthly. · After using the auto-injector, call 911 or emergency services immediately; do not drive yourself. · Inject into the middle of the outer thigh; can be done through clothing if needed. · Hold the leg firmly during injection and massage the site for 10 seconds after removing the device. · Seek immediate medical attention even if symptoms improve; a second dose may be required. · Avoid placing ice or heat on the injection site. · Inform all healthcare providers of your epinephrine prescription and anaphylaxis history. · Wear a medical alert bracelet or necklace indicating your allergy and need for epinephrine. |