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Pronunciation |
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(e
FED rin) |
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U.S. Brand
Names |
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Kondon's Nasal®[OTC];
Pretz-D®[OTC] |
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Generic
Available |
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Yes |
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Synonyms |
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Ephedrine Sulfate |
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Pharmacological Index |
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Alpha/Beta Agonist |
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Use |
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Treatment of bronchial asthma, nasal congestion, acute bronchospasm,
idiopathic orthostatic hypotension |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Hypersensitivity to ephedrine or any component, cardiac arrhythmias,
angle-closure glaucoma, patients on other sympathomimetic
agents |
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Warnings/Precautions |
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Blood volume depletion should be corrected before ephedrine therapy is
instituted; use caution in patients with unstable vasomotor symptoms, diabetes,
hyperthyroidism, prostatic hypertrophy, or a history of seizures; also use
caution in the elderly and those patients with cardiovascular disorders such as
coronary artery disease, arrhythmias, and hypertension. Ephedrine may cause
hypertension resulting in intracranial hemorrhage. Long-term use may cause
anxiety and symptoms of paranoid schizophrenia. Avoid as a bronchodilator;
generally not used as a bronchodilator since new beta2 agents are
less toxic. Use with caution in the elderly, since it crosses the blood-brain
barrier and may cause confusion. |
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Adverse
Reactions |
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>10%: Central nervous system: CNS stimulating effects, nervousness,
anxiety, apprehension, fear, tension, agitation, excitation, restlessness,
irritability, insomnia, hyperactivity
1% to 10%:
Cardiovascular: Hypertension, tachycardia, palpitations, elevation or
depression of blood pressure, unusual pallor
Central nervous system: Dizziness, headache
Gastrointestinal: Xerostomia, nausea, anorexia, GI upset, vomiting
Genitourinary: Painful urination
Neuromuscular & skeletal: Trembling, tremor (more common in the elderly),
weakness
Miscellaneous: Diaphoresis (increased)
<1%: Chest pain, arrhythmias, dyspnea |
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Overdosage/Toxicology |
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Symptoms of overdose include dysrhythmias, CNS excitation, respiratory
depression, vomiting, convulsions
There is no specific antidote for ephedrine intoxication and the bulk of the
treatment is supportive. Hyperactivity and agitation usually respond to reduced
sensory input; however, with extreme agitation, haloperidol (2-5 mg I.M. for
adults) may be required. Hyperthermia is best treated with external cooling
measures; or when severe or unresponsive, muscle paralysis with pancuronium may
be needed. Hypertension is usually transient and generally does not require
treatment unless severe. For diastolic blood pressures >110 mm Hg, a
nitroprusside infusion should be initiated. Seizures usually respond to diazepam
I.V. and/or phenytoin maintenance regimens. |
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Drug
Interactions |
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Decreased effect: Alpha- and beta-adrenergic blocking agents decrease
ephedrine vasopressor effects
Increased toxicity: Additive cardiostimulation with other sympathomimetic
agents; theophylline
cardiostimulation; MAO inhibitors
or atropine may increase blood pressure; cardiac glycosides or general
anesthetics may increase cardiac stimulation |
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Stability |
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Protect all dosage forms from light |
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Mechanism of
Action |
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Releases tissue stores of epinephrine and thereby produces an alpha- and
beta-adrenergic stimulation; longer-acting and less potent than
epinephrine |
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Pharmacodynamics/Kinetics |
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Oral:
Onset of bronchodilation: Within 0.25-1 hour
Duration of action: 3-6 hours
Distribution: Crosses the placenta; appears in breast milk
Metabolism: Little hepatic metabolism
Half-life: 2.5-3.6 hours
Elimination: 60% to 77% of dose excreted as unchanged drug in urine within 24
hours |
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Usual Dosage |
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Children:
Oral, S.C.: 3 mg/kg/day or 25-100 mg/m2/day in 4-6 divided doses
every 4-6 hours
I.M., slow I.V. push: 0.2-0.3 mg/kg/dose every 4-6 hours
Adults:
Oral: 25-50 mg every 3-4 hours as needed
I.M., S.C.: 25-50 mg, parenteral adult dose should not exceed 150 mg in 24
hours
I.V.: 5-25 mg/dose slow I.V. push repeated after 5-10 minutes as needed, then
every 3-4 hours not to exceed 150 mg/24 hours |
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Monitoring
Parameters |
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Blood pressure, pulse, urinary output, mental status; cardiac monitor and
blood pressure monitor required |
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Test
Interactions |
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Can cause a false-positive amphetamine EMIT assay |
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Mental Health: Effects
on Mental Status |
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Nervousness, anxiety, agitation, restlessness, and insomnia are
common |
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Mental Health:
Effects on Psychiatric
Treatment |
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Use with MAOIs may produce hypertensive crisis; avoid
combination |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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Use vasoconstrictors with caution since ephedrine may enhance
cardiostimulation and vasopressor effects of sympathomimetics such as
epinephrine |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Use this medication exactly as directed; do not take more than recommended
dosage. Avoid other stimulant prescriptive or OTC medications to avoid serious
overdose reactions. Store this medication away from light. You may experience
dizziness, blurred vision, restlessness (use caution when driving or engaging in
tasks requiring alertness until response to drug is known); or difficulty
urinating (empty bladder immediately before taking this medication). Report
excessive nervousness or excitation, inability to sleep, facial flushing,
pounding heartbeat, muscle tremors or weakness, chest pain or palpitations,
bronchial irritation or coughing, or increased sweating.
Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend
to be pregnant. Breast-feeding is not recommended. |
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Nursing
Implications |
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Do not administer unless solution is clear |
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Dosage Forms |
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Capsule, as sulfate: 25 mg, 50 mg
Injection, as sulfate: 25 mg/mL (1 mL); 50 mg/mL (1 mL, 10 mL)
Jelly, as sulfate (Kondon's Nasal®): 1% (20 g)
Spray, as sulfate (Pretz-D®): 0.25% (15 mL)
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References |
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Pickup ME, May CS, Sendagire R, et al,
"The Pharmacokinetics of Ephedrine After Oral Dosage in Asthmatics Receiving Acute and Chronic Treatment,"
Br J Clin Pharmacol, 1976, 3(1):123-34.
Stein GC, "Requirements for Pharmacists Dispensing Ephedrine Products," Am
J Health Syst Pharm, 1995, 52(15):1630.
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