SUS-PHRINE SULFITE FREE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for SUS-PHRINE SULFITE FREE (SUS-PHRINE SULFITE FREE).

How it works

Epinephrine is a sympathomimetic catecholamine that acts as a non-selective agonist at all adrenergic receptors (α1, α2, β1, β2, β3). Its primary therapeutic effects include vasoconstriction (α1-mediated), bronchodilation (β2-mediated), and positive chronotropic/inotropic effects (β1-mediated).

What the body does with it

Metabolism	Epinephrine is rapidly metabolized in the liver and other tissues via the enzymes monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT). Major metabolites include metanephrine, vanillylmandelic acid (VMA), and 3-methoxy-4-hydroxyphenylglycol (MHPG).
Excretion	Primarily renal excretion of metabolites (vanillylmandelic acid, metanephrine, and other conjugates); less than 2% excreted unchanged. Minimal biliary/fecal elimination.
Half-life	2 minutes (initial rapid phase), terminal half-life approximately 1-2 hours (alpha phase). Clinical context: Very short half-life necessitates continuous infusion for sustained effect.
Protein binding	Approximately 50% bound, primarily to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	0.3-0.7 L/kg (low, consistent with limited tissue distribution; largely confined to extracellular fluid and blood).
Bioavailability	IM/SC: nearly 100% (though rapid local metabolism may reduce effective dose; absolute bioavailability not well established).
Onset of Action	IM: within 5-10 minutes; SC: within 5-15 minutes; IV: immediate (within 1 minute).
Duration of Action	IM: 1-2 hours; SC: 1-2 hours; IV: 5-10 minutes (due to rapid metabolism and redistribution).

Classification & Brands

Dosing & administration

0.3-0.5 mg subcutaneously or intramuscularly every 15-20 minutes as needed for anaphylaxis. Maximum single dose: 0.5 mg.

Dosage form	INJECTABLE
Renal impairment	No specific dose adjustment required for renal impairment. Use with caution in severe renal impairment due to potential accumulation of metabolites.
Liver impairment	No specific dose adjustment for Child-Pugh class A or B. For Child-Pugh class C, consider reduced initial dose (e.g., 0.3 mg) due to reduced clearance.
Pediatric use	For anaphylaxis: 0.01 mg/kg (maximum 0.5 mg) subcutaneously or intramuscularly every 15-20 minutes as needed.
Geriatric use	Initial dose: 0.3 mg subcutaneously or intramuscularly. Use lower doses due to increased sensitivity and potential for hypertension or myocardial ischemia.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for SUS-PHRINE SULFITE FREE (SUS-PHRINE SULFITE FREE).

Breastfeeding	Epinephrine is excreted in breast milk in minimal amounts; M/P ratio not established. Short half-life limits infant exposure. Use with caution in nursing mothers; potential for infant tachycardia or hypertension is low at maternal therapeutic doses.
Teratogenic Risk	Epinephrine crosses the placenta. First trimester: Potential risk of uteroplacental vasoconstriction and fetal hypoxia; studies suggest association with gastroschisis. Second/third trimester: Causes uterine relaxation, risk of hemorrhage and reduced placental perfusion. High doses may induce fetal arrhythmias. FDA Pregnancy Category C.

Warnings & precautions

■ FDA Black Box Warning

SUS-PHRINE SULFITE FREE injection should be used with extreme caution in patients with cardiovascular disease, hypertension, diabetes, hyperthyroidism, or in elderly patients. It may cause life-threatening hypertensive crisis or cardiac arrhythmias. Do not inject into digits, nose, or genitalia due to risk of tissue necrosis.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to epinephrine or any component of the formulation.","Narrow-angle glaucoma (for ophthalmic use).","Coronary insufficiency (if expected benefit does not outweigh risk).","Hypovolemic shock (unless as a temporary measure).","Do not use in obstetrics when maternal blood pressure is >130/80 mm Hg (except in emergency)."]

Clinical Precautions

Precautions

["May exacerbate cardiac ischemia, arrhythmias, and hypertension.","Use caution in patients with hyperthyroidism, diabetes, or pheochromocytoma.","May cause pulmonary edema if excessive doses are given.","May cause transient worsening of glaucoma in patients with narrow-angle glaucoma.","Local ischemia and necrosis can occur with extravasation; infiltrate with phentolamine if needed.","Monitor blood pressure, heart rate, and ECG during administration."]

Clinical Tips & Counseling

Drug interactions

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SUS-PHRINE SULFITE FREE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for SUS-PHRINE SULFITE FREE (SUS-PHRINE SULFITE FREE).

How it works

What the body does with it

Metabolism	Epinephrine is rapidly metabolized in the liver and other tissues via the enzymes monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT). Major metabolites include metanephrine, vanillylmandelic acid (VMA), and 3-methoxy-4-hydroxyphenylglycol (MHPG).
Excretion	Primarily renal excretion of metabolites (vanillylmandelic acid, metanephrine, and other conjugates); less than 2% excreted unchanged. Minimal biliary/fecal elimination.
Half-life	2 minutes (initial rapid phase), terminal half-life approximately 1-2 hours (alpha phase). Clinical context: Very short half-life necessitates continuous infusion for sustained effect.
Protein binding	Approximately 50% bound, primarily to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	0.3-0.7 L/kg (low, consistent with limited tissue distribution; largely confined to extracellular fluid and blood).
Bioavailability	IM/SC: nearly 100% (though rapid local metabolism may reduce effective dose; absolute bioavailability not well established).
Onset of Action	IM: within 5-10 minutes; SC: within 5-15 minutes; IV: immediate (within 1 minute).
Duration of Action	IM: 1-2 hours; SC: 1-2 hours; IV: 5-10 minutes (due to rapid metabolism and redistribution).

Classification & Brands

Dosing & administration

0.3-0.5 mg subcutaneously or intramuscularly every 15-20 minutes as needed for anaphylaxis. Maximum single dose: 0.5 mg.

Dosage form	INJECTABLE
Renal impairment	No specific dose adjustment required for renal impairment. Use with caution in severe renal impairment due to potential accumulation of metabolites.
Liver impairment	No specific dose adjustment for Child-Pugh class A or B. For Child-Pugh class C, consider reduced initial dose (e.g., 0.3 mg) due to reduced clearance.
Pediatric use	For anaphylaxis: 0.01 mg/kg (maximum 0.5 mg) subcutaneously or intramuscularly every 15-20 minutes as needed.
Geriatric use	Initial dose: 0.3 mg subcutaneously or intramuscularly. Use lower doses due to increased sensitivity and potential for hypertension or myocardial ischemia.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for SUS-PHRINE SULFITE FREE (SUS-PHRINE SULFITE FREE).

Breastfeeding	Epinephrine is excreted in breast milk in minimal amounts; M/P ratio not established. Short half-life limits infant exposure. Use with caution in nursing mothers; potential for infant tachycardia or hypertension is low at maternal therapeutic doses.
Teratogenic Risk	Epinephrine crosses the placenta. First trimester: Potential risk of uteroplacental vasoconstriction and fetal hypoxia; studies suggest association with gastroschisis. Second/third trimester: Causes uterine relaxation, risk of hemorrhage and reduced placental perfusion. High doses may induce fetal arrhythmias. FDA Pregnancy Category C.