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 pharmakokinetics
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
- Scientific articles
- Limberger, Renata Pereira, et al. Pharmacological Effects of Ephedrine. Natural Products: Phytochemistry, Botany and Metabolism of Alkaloids, Phenolics and Terpenes (2013): 1217-1237. #2869
- 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. #2873
- Brooks SM, Sholiton LJ et al. The effects of ephedrine and theophylline on dexamethasone metabolism in bronchial asthma. J Clin Pharmacol. 1977 May-Jun;17(5-6):308-18. PMID 870547. #2868
- Pelkonen O, Turpeinen M, et al. Inhibition and induction of human cytochrome P450 enzymes: current status. Arch Toxicol. 2008 Oct;82(10):667-715. PMID 18618097. #4347
- Wilkinson GR, Beckett AH. Absorption, metabolism, and excretion of the ephedrines in man. II. Pharmacokinetics. J Pharm Sci. 1968b Nov;57(11):1933-8. #2872
- Wilkinson GR, Beckett AH. Absorption metabolism and excretion of the ephedrines in man. I. The influence of urinary pH and urine volume output. Pharmacol Exp Ther. 1968a Jul;162(1):139-47. #2871
- Government bodies
- U.S Food and Drug Administration (FDA). Last updated 09/16/2011. #2874
- Summary of Product Characteristics
- The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Ephedrine Hydrochloride 3 mg/ml Solution for Injection in Pre-filled Syringe. #2870
Similar drugs
© NAPOS 2024