Used orally as a bronchodilator to relieve shortness of breath, chest tightness, wheezing, and cough associated with bronchial asthma. Improves cough symptoms associated with the common cold, bronchial asthma, or bronchitis.
Administered parenterally for the relief of acute bronchospasm; less effective than epinephrine.
Hypotension
Has been used both for the prevention and treatment of hypotension resulting from spinal anesthesia or other types of nontopical conduction anesthesia.
Routine prophylactic use of any vasopressor in spinal anesthesia has been questioned because hypotension does not always occur during spinal anesthesia and treatment can readily be instituted if necessary; it has been suggested that vasopressors be administered prophylactically only in those cases in which a substantial decrease in BP is expected.
Use of vasopressors to correct hypotension occurring during anesthesia in obstetrical patients is controversial; hypotension can usually be minimized by adequate hydration and changing the position of the patient so that the uterus does not compress the inferior vena cava; if a vasopressor is required, ephedrine is usually preferred.
May be used to treat hypotension following sympathectomy or overdosage of certain drugs (adrenergic and ganglionic blocking agents, veratrum alkaloids, other antihypertensive agents).
Cardiac Arrhythmias and Heart Block
Management of Adams-Stokes syndrome with complete heart block. Electrical cardiac pacemakers have largely replaced drug therapy in third-degree AV block (complete heart block).
CNS Conditions
Treatment of narcolepsy or depressive states; the cardiovascular effects limit usefulness in these conditions.
Obesity
Previously used for self-medication in the management of obesity†.
Dietary supplements containing ephedrine alkaloids are no longer commercially available in the US. (See Risks Associated with Dietary Supplements under Cautions.)
Nasal Congestion
Has been used but of doubtful value when administered orally.
Misuse and Abuse
Has been misused and abused by athletes, bodybuilders, weight lifters, and others, including high school- and college-aged individuals engaged in sports†.
Dietary supplements containing ephedrine alkaloids are no longer commercially available in the US. (See Risks Associated with Dietary Supplements under Cautions.)
Ephedrine has been used in clandestine synthesis of methamphetamine and methcathinone. Federal restrictions to reduce the potential for misuse (diversion) and abuse of ephedrine include limiting the amount that can be purchased to 3.6 g per day or 9 g per month, requiring storage behind the counter or in a locked cabinet, requiring purchasers to provide approved photographic identification, and requiring retail distributors to maintain a written or electronic logbook of purchases for at least 2 years. (For additional information on these and other federal restrictions, visit [http://www.deadiversion.usdoj.gov]). Additional requirements have been enacted in some states; follow state requirements if such requirements are more stringent than federal restrictions.
Dosage and Administration
Administration
Administer orally, IV, IM, or sub-Q.
Administer IV when an immediate effect is desired.
Absorption and onset of action more rapid following IM administration (within 10–20 minutes) than following sub-Q administration.
Oral Administration
Administer orally as a combination preparation.
IV Administration
For solution and drug compatibility information, see Compatibility under Stability.
Administer slowly.
Dosage
Available as ephedrine hydrochloride, ephedrine sulfate, or ephedrine tannate; dosage expressed in terms of the salt.
Pediatric Patients
Bronchospasm
Oral
Ephedrine tannate: Children 2–6 years of age: 2.5–5 mg every 12 hours as needed; administered in fixed combination with other drugs (Rynatuss®).
Ephedrine tannate: Children >6 years of age: 5–10 mg every 12 hours as needed; administered in fixed combination with other drugs (Rynatuss®).
Ephedrine hydrochloride or sulfate self-medication in children ≥12 years of age: 12.5–25 mg every 4 hours as needed; administered in fixed combination with guaifenesin.
IV
Ephedrine sulfate: 0.75 mg/kg or 25 mg/m2 4 times daily or as otherwise determined by patient’s response.
IM
Ephedrine sulfate: 0.5 mg/kg or 16.7 mg/m2 every 4–6 hours.
Sub-Q
Ephedrine sulfate: 0.5 mg/kg or 16.7 mg/m2 every 4–6 hours; alternatively, 0.75 mg/kg or 25 mg/m2 4 times daily or as otherwise determined by patient’s response.
Hypotension
IV
Ephedrine sulfate: 0.75 mg/kg or 25 mg/m2 4 times daily or as otherwise determined by BP response.
IM
Ephedrine sulfate: 0.5 mg/kg or 16.7 mg/m2 every 4–6 hours.
Sub-Q
Ephedrine sulfate: 0.5 mg/kg or 16.7 mg/m2 every 4–6 hours; alternatively, 0.75 mg/kg or 25 mg/m2 4 times daily or as otherwise determined by BP response.
Adults
Bronchospasm
Oral
Ephedrine tannate: 10–20 mg every 12 hours as needed; administered in fixed combination with other drugs (e.g., as Rynatuss®).
Ephedrine hydrochloride or sulfate self-medication: 12.5–25 mg every 4 hours as needed; used in fixed combination with guaifenesin.
Parenteral
Ephedrine sulfate: Usually, 12.5–25 mg; give smallest effective dose. Further dosage should be determined by patient response.
Hypotension
IV
Ephedrine sulfate: 5–25 mg; repeat in 5–10 minutes if necessary. Further dosage should be determined by BP response.
If used during labor, administer only sufficient dosage to maintain BP ≤130/80 mm Hg.
IM or Sub-Q
Ephedrine sulfate: 25–50 mg (range: 10–50 mg). Further dosage should be determined by BP response.
If used during labor, administer only sufficient dosage to maintain BP ≤130/80 mm Hg.
Cardiac Arrhythmias and Heart Block
Adams-Stokes Syndrome
IV
Ephedrine sulfate: 5–25 mg; repeat in 5–10 minutes if necessary.
IM or Sub-Q
Ephedrine sulfate: 25–50 mg (range: 10–50 mg).
Prescribing Limits
Pediatric Patients
Bronchospasm
Oral
Ephedrine hydrochloride or sulfate self-medication in children ≥12 years of age: Maximum 150 mg in any 24-hour period.
Adults
Bronchospasm
Oral
Ephedrine hydrochloride or sulfate self-medication: Maximum 150 mg in any 24-hour period.
Cautions
Contraindications
Concurrent or recent (i.e., within 2 weeks) therapy with an MAO inhibitor.
May cause hypertension and tachycardia; risk of serious adverse effects (e.g., MI, stroke, intracranial hemorrhage, exacerbation of CHF, death). (See Risks Associated with Dietary Supplements under Cautions.)
Risk of anginal pain in patients with coronary insufficiency or ischemic heart disease. Risk of potentially fatal arrhythmias in patients with organic heart disease or in those receiving drugs that sensitize the myocardium (e.g., cyclopropane, halothane).
Caution in patients with cardiovascular disease (e.g., coronary insufficiency, angina pectoris, cardiac arrhythmias, unstable vasomotor system) and in those receiving digitalis.
Concomitant Diseases
Use with caution in patients with CHD, hypertension, hyperthyroidism, diabetes mellitus, or prostatic hypertrophy. Patients with these conditions should consult a clinician before initiating self-medication with ephedrine.
Use for self-medication for bronchospasm only if previously diagnosed with asthma; do not use if previously hospitalized for asthma unless directed by a clinician.
Risks Associated with Dietary Supplements
Dietary supplements containing ephedrine alkaloids have been associated with serious adverse cardiac effects (e.g., hypertension, possibly resulting in MI, stroke, or death), CNS effects, and death.
In February 2004, FDA declared dietary supplements containing ephedrine alkaloids adulterated by virtue of their unreasonable health risks to consumers. Manufacturing, sale, and distribution of all dietary supplements containing ephedrine alkaloids (e.g., Ephedra spp. [“ma huang”], Sida cordifolia, Pinellia spp.) were prohibited after April 12, 2004. This regulation does not apply to traditional Chinese herbal remedies or products regulated as conventional foods (e.g., herbal teas). Ephedra is not generally recognized as safe for foods and not approved for use as a food additive. After litigation, FDA’s rule was upheld, and FDA reiterated its position that no dosage of dietary supplements containing ephedrine alkaloids is safe, and the sale of these products in the US is illegal and subject to FDA enforcement action.
Sensitivity Reactions
Some commercially available preparations may contain the dye tartrazine (FD&C yellow No. 5); possible allergic reactions in susceptible individuals (e.g., those sensitive to aspirin).
General Precautions
When used in fixed combination with other drugs, observe the usual cautions, precautions, and contraindications associated with all drugs in the preparation.
CNS Effects
Nervousness, tremor, or insomnia may occur. Discontinue self-medication and consult a clinician if these symptoms persist or worsen.
GI Effects
Nausea or loss of appetite may occur. Discontinue self-medication and consult a clinician if these symptoms persist or worsen.
Prolonged Use
Prolonged parenteral use may produce a syndrome resembling an anxiety state. Tolerance may develop; effectiveness may return after the drug is withheld temporarily.
Duration of Therapy
Self-medication in asthma: Discontinue and consult a clinician if symptoms are not improved within 1 hour or worsen. Discontinue if cough persists for >7 days, recurs, or is accompanied by fever, rash, or persistent headache.
Misuse and Abuse
Potential for misuse and abuse.
Specific Populations
Pregnancy
Category C.
Parenteral ephedrine should not be used in obstetric patients when maternal BP is >130/80 mm Hg.
Lactation
Distributed into milk. Use not recommended.
Pediatric Use
Parenteral preparations: Safety and efficacy not established. Limited use in pediatric patients; dosage and limitations of use not established.
Should not be used for self-medication in children <12 years of age unless otherwise directed by a clinician.
Risk of overdosage and toxicity (including death) in children <2 years of age receiving OTC preparations containing antihistamines, cough suppressants, expectorants, and nasal decongestants alone or in combination for relief of symptoms of upper respiratory tract infection. Limited evidence of efficacy for these preparations in this age group; appropriate dosages not established. Therefore, FDA recommends not to use such preparations in children <2 years of age; safety and efficacy in older children currently under evaluation. Because children 2–3 years of age also are at increased risk of overdosage and toxicity, some manufacturers of oral nonprescription cough and cold preparations recently agreed to voluntarily revise the product labeling to state that such preparations should not be used in children <4 years of age. During the transition period, some preparations on pharmacy shelves will have the new recommendation (“do not use in children <4 years of age”), while others will have the previous recommendation (“do not use in children <2 years of age”). FDA recommends that parents and caregivers adhere to dosage instructions and warnings on the product labeling that accompanies the preparation and consult a clinician about any concerns. Clinicians should ask caregivers about use of OTC cough/cold preparations to avoid overdosage.
Common Adverse Effects
Parenteral ephedrine: Nervousness, insomnia, restlessness, anxiety, tension, tremor, weakness, dizziness, vertigo, headache, confusion, delirium, hallucination, pallor, respiratory difficulty, hypertension (resulting in cerebral hemorrhage), tachycardia, palpitation, sweating, nausea, vomiting, anorexia, vesical sphincter spasm (resulting in difficult and painful urination), urinary retention (particularly in males with prostatism), precordial pain, cardiac arrhythmias.
Rapidly and completely absorbed following oral, IV, IM, or sub-Q administration. Peak serum concentrations attained within 2.6–3 hours following oral administration.
Onset
Oral administration: Bronchodilation occurs within 15–60 minutes.
IV administration: Pharmacologic effects occur almost immediately.
IM administration: Pharmacologic effects occur within 10–20 minutes.
Duration
Oral administration: Bronchodilation persists for 2–4 hours; pressor and cardiac responses persist for up to 4 hours.
Parenteral administration: Pressor and cardiac responses persist for 1 hour.
Distribution
Extent
Distributed into milk.
Elimination
Metabolism
Slowly metabolized in the liver.
Elimination Route
Ephedrine and its metabolites are excreted in urine; most of the drug is excreted as unchanged ephedrine. The rate of urinary excretion of ephedrine and its metabolites is dependent upon urinary pH.
Half-life
About 3 hours when the urine is acidified to pH 5; about 6 hours when urinary pH is about 6.3.
Stability
Storage
Parenteral
Injection
15–30°C. Protect from light.
Compatibility
For information on systemic interactions resulting from concomitant use, see Interactions.
Sympathomimetic agent; occurs naturally in plants of the genus Ephedra.
Stimulates both α- and β-adrenergic receptors.
Relaxes bronchial smooth muscle, stimulates cardiac muscle (producing positive inotropic effects), constricts arterioles, increases BP, and stimulates the cerebral cortex and subcortical centers.
Relaxes GI smooth muscle. Contracts urinary bladder trigone and sphincter and relaxes the detrusor muscle; may cause urinary retention.
Advice to Patients
For self-medication in asthma, importance of not exceeding recommended dosages or frequency of administration unless otherwise instructed by a clinician.
For self-medication in asthma, importance of discontinuing therapy and contacting a clinician if symptoms are not improved within 1 hour or they become worse.
For self-medication in asthma, importance of discontinuing therapy and contacting a clinician if cough persists for >7 days, recurs, or is accompanied by fever, rash, or persistent headache.
For self-medication in asthma, importance of contacting a clinician if nervousness, tremor, sleeplessness, nausea, or loss of appetite persists or becomes worse.
For asthma, advise that ephedrine should be used for self-medication only if asthma was previously diagnosed by a clinician. Before considering self-medication, inform clinician of any history of hospitalization for asthma.
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and herbal supplements, as well as any concomitant illnesses (e.g., cardiovascular disease). Importance of avoiding MAO inhibitors and allowing 2 weeks to elapse after discontinuing these antidepressants.
Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.
Importance of informing patients of other important precautionary information. (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
In February 2004, FDA issued a final regulation declaring that dietary supplements containing ephedrine alkaloids are adulterated under the Federal Food, Drug, and Cosmetic Act. In August 2006, FDA’s position was upheld by the US Court of Appeals for the 10th Circuit in Denver; sale of these dietary supplements in the US is illegal and subject to FDA enforcement action. (See Risks Associated with Dietary Supplements under Cautions.)
Ephedrine
Routes
Dosage Forms
Strengths
Brand Names
Manufacturer
Bulk
crystals or granules (hydrous or anhydrous)*
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
† Use is not currently included in the labeling approved by the US Food and Drug Administration.
Remember, keep this and all other medicines out of the reach of children,
never share your medicines with others, and use this medication only for the indication prescribed.
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