EPHEDRA



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EPHEDRA
Ephedra; al. Meertraübehen; English. Ephedra, joint fir.

Stems air.

The dioecious subshrub with ephedra are thin and angular stems and leaves reduced to scales. The male flowers amentos are grouped into yellowish, female flowers are reduced to ova surrounded by bracts, and fleshy red when ripe.

Source.

The species of interest are all of Asian origin, but the genre, which includes dozens of species, is present on all continents.

Chemical composition.

The active components are arilalquilaminas whose structure is very similar to that of catecholamines. Some consider them as alkaloids, while for others, because the nitrogen is not part of a heterocycles is protoalcaloides. The drug also contains several flavonoids (flavones and flavonols, 0. 3% in stems of E. cynical, C - glucosil flavones) proantocianidolesand polysaccharides.

Protoalcaloides. Its content, which varies depending on the species, is a maximum of 3%. The majority component is almost always the (ephedrine (1R, 2S) 1 phenyl - 2 - methylamino propane - 1 - ol. Different species also contain (pseudoephedrine (1S, 2S) and the related rules and methylated derivatives involved. These bases are accompanied by small amounts (10 - 5 - 10 - 4) cyclic derivatives: 5 - feniloxazolidinas and efedroxano (= (4S, 5R) 3, 4 - dimethyl 5 - feniloxazolidona)

It also notes the presence of macrocyclic alkaloids, derivatives of spermine: orantina in the stems, efedradinas B, C and D in the roots. Within the latter, also has been isolated substances with hypotensive activity: derivatives of histamine, proantocianidoles [630 and ref. mentioned] and an amino acid compounds: the maoconina.

Pharmacological data.

Ephedrine, structurally related to adrenaline, causing a release of endogenous catecholamines postganglionares sympathetic fibers: a sympathomimetic indirect. Breathing speeds up the movement and its intensity increases, stimulates the heart and automatism is vasoconstrictora. Its strong lipophilicity allows you to cross the blood - brain barrier and exert important effects: to increase the vigil, decreasing the feeling of tiredness. The answer adrenergic obtained with a fixed dose of ephedrine, gradually decreases in intensity until it disappeared (a phenomenon of tachyphylaxis)

While ephedrine and pseudoephedrine are identical bronchodilator activity, the activity on the myocardium, the tension and the CNS the first is more important. In the case of drugs entirely, the interference of other components with the intestinal absorption of phenethylamines, quantitatively modifying the action of these, their becoming more gentle and prolonged. The splitting of the methanol extract of E. shows that the primary responsibility for the anti - inflammatory activity is the (pseudoephedrineand to a lesser extent, the efedroxano [626] whose complex pharmacology has been able to demonstrate [634] Polysaccharides are hypoglycemic.

Observations on the Man.

All properties of ephedrine, mentioned above, have been observed in humans and exploited in therapeutics. Its wide variety of activities and the phenomenon of tachyphylaxis have made their therapeutic indications are limited. It presents numerous contraindications coronary heart disease, prostatic hypertrophy, diabetes. It also presents drug interactions: with MAOIs (monoamine oxidase inhibitors) and digitalis. In most usual therapeutic indications (analéptico, antiasmático) ephedrine has been replaced by more manageable molecules. Ephedrine is not without toxicity. It has been described a teratogen in chick embryo. For 5000 years, traditional Chinese medicine uses the stems (ma huang) in the treatment of asthma, bronchitis and numerous ailments. The Eastern tradition gives properties opposite to the bodies underground.

Employment.

Different species of ephedra at present, almost not used for the extraction of ephedrine. Ephedrine and its salts are used only in the formulation of "pectoral syrups" (bronchodilators) This amine is also part of the solution to instillations composition of nasal used in case of rhinorrhea (vasoconstrictora) Prolonged use can lead to the emergence of iatrogenic rhinitis (and also, though more rarely, an iatrogenic arterial hypertension) In children, there may be a risk of CNS depression and cardiovascular reactions. Sympathomimetic activity of the stem provides lipolytic properties and anorectic used in case of excess weight. Criomolida the drug does not produce any toxic event in the trials of acute and subacute (3 g / kg, 300 and 600 mg / kg / day, 6 weeks, rat, per os)

The drug.

Stems air of different species of ephedra are thin, angular and longitudinally striped. The leaves, reduced membranous scales are embedded in pairs at the nodes. The size of internodes varies depending on the species. Anatomically, its sinuous epidermis presents stomata (not very marked) from the division of a stem cell (haploqueílicos stomata) The stalks contain tracheids that dotted by scores of union cross, glasses are almost open or unlocked. The log is sort of gymnosperms. Ephedrine is analyzed by C. C. F. but does not differ from their isomers) To reveal the plates are ninhydrin preferable to use instead of reactive general alkaloids. The H. P. I. C. is very suitable for the determination of alkaloids.

Bibliography.

O. PUREV, F. POSP͊IL and O. Motl.

Flavonoids from Ephedra sinica Stapf.

Coll. Czech. Chem. Comm. 53, 3193 - 3196, 1988.

K. R. MARKHAM.

Distribution of flavonoids in the lower plants and its evolution -

nary significance. In: The flavonoids: advances in research,

since 1980, J. B. Harborne, ed. London, Champman and Hall,

427 - 478, 1988.

C. Konno, T. TAGUCHI, M. Tamada and H. HIKINO.

Ephedroxane, anti - inflammatory herbs principle of Ephedra.

Phytochemistry, 18, 697 - 698, 1979.

M. Tamada, K. ENDO, H. HIKINO and C. Kabuto.

Structure of ephedradine A, a hypotensive principle of Ephedra.

roots.

Tetrahedron Lett. 873, 876, 1979.

H. HIKINO, M. Ogata and C. Konno.

Structure of ephedradine D, a hypotensive principle of Ephedra.

roots.

Heterocycles, 17, 155 - 158, 1982.

H. HIKINO, Y. Kiso, M. Ogata, C. Konno, K. AISAKA,

H. KUBOTA, N. HIROSE and T. Ishihara.

Pharmacological actions of analogues of feruloyl - histamine, an.

imidazole alkalos of Ephedra roots.

Planta Med. 50, 478 - 480, 1984.

Y. And H. KASAHARA HIKINO.

Structure of mahuannin D, a hypotensive principle of Ephedra.

roots.

Heterocycles, 20, 1953 - 1956, 1983, ibid, 19, 1381 - 1384, 1982.

M. IZADDOOST and T. ROBINSON.

Synergism and Antagonismes in the pharmacology of alkaloidal.

plants. In: Herbs, spices, and medicinal plants: recent Advan -

ces in Botany, horticulture, and pharmacology, LE And Crake.

ces in Botany, horticulture, and pharmacology, LE And Crake.

1987.

M. Harada and M. NISHIMURA.

Contribution of alkalos fraction to pressor and hyperglycemic.

Ephedra effect of crude extract in dogs.

J. Pharm. Dyn. 4, 691 - 699, 1981.

H. HIKINO, C. Konno, H. Takata and M. Tamada.

Antiinflammatory principle of Ephedra herbs.

Chem. Pharm. Bull. 28, 2900 - 2904, 1980.

H. HIKINO, K. Ogata, Y. KASAHARA and C. Konno.

Pharmacology of ephedroxanes.

J. of Ethnopharmacology, 13, 175 - 191, 1985.

T. Nishikawa, H. J. BRUYERE, Y. TAKAGI, E. F. And GILBERT.

H. UNO.

Cardiovascular teratogenicity of ephedrine in chick embryos.

Toxicology Letters, 29, 59 - 63, 1985.

H. WAGNER, S. BLADT and E. M. ZGAINSKI.

Plant drug analysis, Berlin, Springer Verlag, 1984.

Zhang Jian, TIAN ZHEN and LOU Zhi - CEN.

Simultaneous determination of six alkaloids in Ephedrae herba.

by High Performance Liquid Chromatography.

Planta Med. 54, 69 - 70, 1988.

ephedra, toxicological dossier Laboratories Arkopharma.

Diseases whose treatment is appropriate in this plant.

Overweight.

Rhinitis.

Asma.


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