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ephedrine

Indications: - hypotension & shock - hypotension during anesthesia - unresponsive bronchospasm - bronchitis, bronchial asthma - temporary support of ventricular rate in bradycardia Dosage: 1) adults: a) 10-25 mg IV (slowly) every 5-10 min b) 25-50 mg SC/IM/IV 2) children: -> 3 mg/kg/day or 100 mg/m2 IV/SC divided every 4 hours Injection: 25 mg/mL (1 mL); 50 mg/mL (1 mL) Pharmacokinetics: 1) well absorbed when given SC or IM 2) duration of cardiac effect is 1 hour 3) metabolized by liver 4) eliminated in the urine 5) 1/2life is 3 hours, prolonged with alkaline urine Adverse effects: 1) common (> 10%) - nervousness, restlessness, insomnia 2) less common (1-10%) - painful urination, dizziness, dry mouth, tachycardia, headache, increased sweating, hypertension, anorexia, nausea/vomiting, palpitations, trembling, paleness, weakness 3) uncommon (< 1%) - chest pain, arrhythmias, dyspnea, anxiety, apprehension, fear, tension, agitation, excitation, irritability 4) other [2] - apnea, renal insufficiency, heartburn, urinary retention Drug interactions: 1) beta blockers antagonize the effects of ephedrine 2) MAO inhibitors increase pressor effects & may result in hypertensive crisis Mechanism of action: 1) stimulates both alpha & beta adrenergic receptors 2) indirectly stimulates release of norepinephrine 3) beta-1 agonist activity a) positive inotropic & chronotropic effects b) increases autorhythmicity 4) beta-2 & alpha-1 agonist activity a) vasodilation or constriction b) increased systolic & diastolic blood pressure c) constriction of renal blood vessels 5) beta-2 agonist activity relaxes bronchial smooth muscle 6) CNS stimulation is similar to methamphetamine 7) tachyphylaxis develops rapidly

Interactions

drug adverse effects (more general classes)

Related

ephedra (ma huang)

Specific

N-methylephedrine

General

adrenergic neuron stimulant alpha-1 adrenergic receptor agonist amine analeptic (CNS stimulant) aromatic compound beta-adrenergic receptor agonist vasoconstrictor agent or vasopressor

Properties

AGONIST-FOR: beta adrenergic receptor MISC-INFO: elimination route KIDNEY 1/2life 3 HOURS therapeutic-range 50-100 NG/ML toxic-range >2000 NG/ML pregnancy-category C safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995

Component-of

acetaminophen/chlorpheniramine/ephedrine/guaifenesin acetaminophen/ephedrine/guaifenesin carbetapentane/chlorpheniramine/ephedrine/phenylephrine chlorpheniramine/ephedrine/phenylephrine dyphylline/ephedrine/guaifenesin/phenobarbital ephedra (ma huang) ephedrine/guaifenesin ephedrine/hydroxyzine/theophylline ephedrine/phenobarbital/potassium iodide/theophylline ephedrine/potassium iodide