Monograph
C01CA26 - Ephedrine |
Propably not porphyrinogenic |
PNP |
Rationale
Although only scanty pharmacokinetic information is found for ephedrine, there are no indications that this drug, which has been on the market for several decades, is an inducer or mechanism-based inhibitor of any CYP enzymes.
Continuous attention to ensure a sufficient carbohydrate intake is recommended.
Chemical description
Phenethylamine
Therapeutic characteristics
Ephedrine is a sympathomimetic amine with direct and indirect actions on the adrenergic receptor system. Ephedrine is commonly used as a stimulant, appetite suppressant, concentration aid, decongestant and to treat hypotension associated with anaesthesia.
It is administered orally or intravenously. Side effects such as nausea, vomiting and reduced appetite may be potentially porphyrinogenic through reduction in caloric intake.
Metabolism and pharmacokinetics
After oral or parenteral administration, up to 77% of ephedrine is excreted in unchanged form in the urine. Half-life of elimination is about 3 to 6 hours depending on the urine pH. A smaller portion of the drug is demethylated and deaminated to hippuric acid. (Limberger 2013, SPC, Wilkinson 1968a, 1968b)
Books (1977) found ephedrine to increase the clearance of dexamethasone by 42%, and increase half-life by 36 %, but the mechanism for this effect is uncertain.
Ephedrine is not listed as an inducer or inhibitor of CYP enzymes. Similar substances are neither found to, nor expected to have the capacity to significantly induce or inhibit CYP enzymes (Pelkonen 2008, Preissner 2010, FDA).
References
# | Citation details | PMID |
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* | Scientific articles | |
1. | Limberger, Renata Pereira, et al. Pharmacological Effects of Ephedrine. Natural Products: Phytochemistry, Botany and Metabolism of Alkaloids, Phenolics and Terpenes (2013): 1217-1237.
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2. | Preissner S, Kroll K, et al: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions.
Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. |
|
3. | The effects of ephedrine and theophylline on dexamethasone metabolism in bronchial asthma.
Brooks SM, Sholiton LJ et al. J Clin Pharmacol. 1977 May-Jun;17(5-6):308-18. |
870547 |
4. | Inhibition and induction of human cytochrome P450 enzymes: current status.
Pelkonen O, Turpeinen M, et al. Arch Toxicol. 2008 Oct;82(10):667-715. |
18618097 |
5. | Absorption, metabolism, and excretion of the ephedrines in man. II. Pharmacokinetics. J Pharm Sci. 1968b Nov;57(11):1933-8.
Wilkinson GR, Beckett AH. |
|
6. | I. The influence of urinary pH and urine volume output. Pharmacol Exp Ther. 1968a Jul;162(1):139-47.
Wilkinson GR, Beckett AH. Absorption metabolism and excretion of the ephedrines in man. |
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* | Government bodies | |
7. | U.S Food and Drug Administration (FDA). Last updated 09/16/2011.
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* | Summary of Product Characteristics | |
8. | The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Ephedrine Hydrochloride 3 mg/ml Solution for Injection in Pre-filled Syringe.
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Tradenames and packages
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Netherlands
Efedrine · Efedrine Added Pharma 5 mg/ml, oplossing voor injectie · Efedrine Added Pharma 50 mg/ml, oplossing voor injectie · Efedrine HCl Aguettant 3 mg/ml, oplossing voor injectie in een voorgevulde spuit · Efedrine HCl Teva 50 mg/ml, oplossing voor injectieBelgium
Ephedrine · Ephedrine HCl Aguettant 3 mg/ml sol. inj. i.v. amp. · Ephedrine HCl Aguettant 3 mg/ml sol. inj. i.v. ser. préremplie · Ephedrine HCl Aguettant 30 mg/ml sol. inj. i.v. amp.United Kingdom
Ephedrine · Ephedrine 30mg/10ml solution for injection ampoules · Ephedrine 30mg/10ml solution for injection pre-filled syringes · Ephedrine 30mg/1ml solution for injection ampoules · Ephedrine 30mg/2ml solution for injection ampoulesDenmark
Efedrin · Efedrin "Abboxia" · Efedrin "Aguettant" · Efedrin "SAD" · Efedrin "Unimedic" · Ephedrine · Ephedrine "Sintetica" · SebadrinNorway
Efedrin · Efedrin Abboxia · Efedrin Aguettant · Efedrin SA · Efedrin Unimedic · Ephedrine SinteticaPoland
Ephedrine Kabi · Ephedrini hydrochloridum Sintetica · Ephedrinum Hydrochloricum Aguettant · Noradrenaline AguettantLuxembourg
Ephedrine · Ephedrine HCl AguettantIceland
Efedrin · Efedrin Abboxia · Ephedrine · Ephedrine SinteticaFinland
Efedrin Abboxia · Efedrin Aguettant · Efedrin Unimedic · Ephedrine Sintetica · SebadrinLatvia
Ephedrine · Ephedrine Sintetica
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