Pharmacology Stimulates alpha and beta receptors (alpha receptors at high doses;
beta- 1 and beta- 2 receptors at moderate doses) within the sympathetic nervous system. Relaxes
smooth muscle of bronchi and iris, and is an 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 is excreted as unchanged drug or is conjugated. Onset 5 to 10
min (subcutaneous), 1 to 5 min (inhalation). Duration 4 to 6?h (subcutaneous), 1 to 4 h (IM), 1
to 3 h (inhalation). Indications and Usage Epinephrine 1:1,000 injection Relief of respiratory
distress due to bronchospasm; to provide rapid relief of hypersensitivity reactions to drugs and
other allergens (eg, anaphylactic reactions to drugs, animal serums, insect stings); to prolong the
action of local and regional anesthetics; restore cardiac rhythm in cardiac arrest due to various
causes; treatment of mucosal congestion of hay fever, rhinitis, and acute sinusitis; relieve
bronchial asthmatic paroxysms; symptomatic relief of serum sickness, urticaria, angioneurotic
edema; for relaxation of uterine musculature and to inhibit uterine contractions; epinephrine
injection can be used as a hemostatic agent; in syncope due to complete heart block or carotid
sinus hypersensitivity; for resuscitation in cardiac arrest following anesthetic accidents; used in
open-angle glaucoma. Epinephrine 1:1,000 (auto-injector) and 1:2,000 (auto-injector), Prefilled
syringe Emergency treatment of allergic reactions (type I) including anaphylaxis to insect stings
(eg, bees, fire ants, hornets, yellow jackets, wasps) and biting insects (eg, mosquitoes), allergen
immunotherapy, foods, drugs, diagnostic testing substances (eg, radiocontrast media), and other
allergens, as well as idiopathic anaphylaxis or exercise-induced anaphylaxis. The auto-injectors
and prefilled syringes are intended for immediate self-administration in patients who are at
increased risk for anaphylaxis, including individuals with a history of anaphylactic reactions.
Auto-injectors and prefilled syringes are for immediate use and are not a substitute for immediate
medical attention. Epinephrine 1:10,000 injection Treatment and prophylaxis of cardiac arrest in
the absence of ventricular fibrillation and attacks of transitory atrioventricular heart block with
syncopal seizures; to stimulate the heart in syncope due to complete heart block or carotid sinus
hypersensitivity; for resuscitation in cardiac arrest following anesthetic accidents; in
cardiopulmonary resuscitation, intracardiac puncture and intramyocardial injection of
epinephrine may be effective when external cardiac compression and attempts to restore the
circulation by electrical defibrillation or use of pacemaker fail; seldom used as a vasopressor
except in the treatment of anaphylactic shock and under .
Pharmacology Stimulates alpha and beta receptors.pdf
1. Pharmacology Stimulates alpha and beta receptors (alpha receptors at high doses;
beta- 1 and beta- 2 receptors at moderate doses) within the sympathetic nervous system. Relaxes
smooth muscle of bronchi and iris, and is an 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 is excreted as unchanged drug or is conjugated. Onset 5 to 10
min (subcutaneous), 1 to 5 min (inhalation). Duration 4 to 6?h (subcutaneous), 1 to 4 h (IM), 1
to 3 h (inhalation). Indications and Usage Epinephrine 1:1,000 injection Relief of respiratory
distress due to bronchospasm; to provide rapid relief of hypersensitivity reactions to drugs and
other allergens (eg, anaphylactic reactions to drugs, animal serums, insect stings); to prolong the
action of local and regional anesthetics; restore cardiac rhythm in cardiac arrest due to various
causes; treatment of mucosal congestion of hay fever, rhinitis, and acute sinusitis; relieve
bronchial asthmatic paroxysms; symptomatic relief of serum sickness, urticaria, angioneurotic
edema; for relaxation of uterine musculature and to inhibit uterine contractions; epinephrine
injection can be used as a hemostatic agent; in syncope due to complete heart block or carotid
sinus hypersensitivity; for resuscitation in cardiac arrest following anesthetic accidents; used in
open-angle glaucoma. Epinephrine 1:1,000 (auto-injector) and 1:2,000 (auto-injector), Prefilled
syringe Emergency treatment of allergic reactions (type I) including anaphylaxis to insect stings
(eg, bees, fire ants, hornets, yellow jackets, wasps) and biting insects (eg, mosquitoes), allergen
immunotherapy, foods, drugs, diagnostic testing substances (eg, radiocontrast media), and other
allergens, as well as idiopathic anaphylaxis or exercise-induced anaphylaxis. The auto-injectors
and prefilled syringes are intended for immediate self-administration in patients who are at
increased risk for anaphylaxis, including individuals with a history of anaphylactic reactions.
Auto-injectors and prefilled syringes are for immediate use and are not a substitute for immediate
medical attention. Epinephrine 1:10,000 injection Treatment and prophylaxis of cardiac arrest in
the absence of ventricular fibrillation and attacks of transitory atrioventricular heart block with
syncopal seizures; to stimulate the heart in syncope due to complete heart block or carotid sinus
hypersensitivity; for resuscitation in cardiac arrest following anesthetic accidents; in
cardiopulmonary resuscitation, intracardiac puncture and intramyocardial injection of
epinephrine may be effective when external cardiac compression and attempts to restore the
circulation by electrical defibrillation or use of pacemaker fail; seldom used as a vasopressor
except in the treatment of anaphylactic shock and under certain conditions in insulin shock.
Nasal solution Nasal decongestant. Oral inhalation Temporary relief of shortness of breath,
tightness of chest, and wheezing due to bronchial asthma; temporary relief of bronchial asthma;
easing breathing for asthma patients by reducing spasms of bronchial muscles. Unlabeled Uses
Endoscopic injection for the management of acute lower GI bleeding; overdosage of beta-
2. blockers, calcium channel blockers, and tricyclic antidepressants (and other sodium channel
blockers); symptomatic bradycardia or hypotension that did not respond to atropine and
transcutaneous pacing. Contraindications Note: There are no absolute contraindications to use
in a life-threatening situation. Narrow-angle glaucoma; shock (nonanaphylactic); during general
anesthesia with halogenated hydrocarbons or cyclopropane; individuals with organic brain
damage; local anesthesia of certain areas (eg, fingers, toes); use during labor; use in cardiac
dilation and coronary insufficiency; situations in which vasopressor drugs may be
contraindicated (eg, diabetes, hypertension and other CV disorders, obstetrics when maternal BP
is in excess of 130/80, in thyrotoxicosis); hypersensitivity to sympathomimetic amines. General
Advice Multiple concentrations and dosage forms are available. Ensure the proper concentration
and doseform are being used. Injection Incompatibilities: Epinephrine is destroyed by alkalines
and oxidizing agents (eg, bromine, chlorine, chromates, iodine, nitrates, oxygen, permanganates,
salts of easily reducible metals [eg, iron]). Subcutaneous is the preferred route of administration.
For medical emergencies, the IV route is usually used. If given IM, avoid injection into the
buttocks. Subcutaneous injection results in slower absorption. Inspect visually for particulate
matter and discoloration whenever solution and container permit. Cardiac resuscitation: In
adults, the effect of IV epinephrine (1:10,000) may only last a few minutes; therefore, the IV
dose may be followed by 0.3 mg of 1:1,000 (1 mg/mL) subcutaneously. Note: Intracardiac
injection is no longer recommended in Advanced Cardiac Life Support (ACLS) guidelines.
Auto-injector, Prefilled syringe Only inject into the anterolateral aspect of the thigh, through
clothing if necessary. Auto-injector: Do not inject IV. Only inject into the anterolateral aspect of
the thigh. Do not inject into the buttock; this may not provide effective treatment for
anaphylaxis. According to ACLS guidelines, IM injection is the preferred route of administration
for patients with anaphylaxis with signs of systemic reaction.
Solution
Do not use an epinephrine solution if it is pinkish or darker than slightly yellow or if it contain a
precipitate.