Generic Medicines
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Ephedrine stimulates lipolysis by increasing noradrenaline (NA) release from sympathetic nerve terminals. This increase in noradrenaline activates adrenergic receptors which increases cAMP levels in fat cells and muscle cells. This has the effect of increasing lipolysis in fat cells and increasing protein synthesis in muscle tissue. Negative feedback mechanisms are activated as well, and involve the production of phosphodiesterases, adenosine, and prostaglandins. Caffeine has the ability to inhibit phosphodiesterase activity and interfere with the adenosine receptor. This combined with its ability to prevent some NA re-uptake12 increase the effectiveness of ephedrine in a synergistic fashion. Aspirin has been shown to increase the effectiveness of ephedrine in some individuals presumably by its actions as a prostaglandin inhibitor.
Maximum effectiveness is achieved when taking 20 mg ephedrine with 200 mg caffeine and 300 mg aspirin three times a day about one half hour before meals. Common side effects are associated with its sympathetic activity namely, anorexia, initial rise in blood pressure, initial tachycardia, slowed GI motility (constipation), insomnia, agitation, anxiety, nervousness and depression- like withdrawal symptoms. Most all of these symptoms exhibit tachyphylaxis after about 4-6 weeks. Thermogenic activity seems to last upwards of 20 weeks due to its low desensitization properties and beta-3 affinity. About 75% of ephedrine’s effects on weight loss in the obese are due to appetite control.
Anyone considering taking ephedrine, caffeine and aspirin should educated themselves first about the potential side effects. Individuals with pre-existing high blood pressure should not use sympathomimetics such as ephedrine. When taking herbal forms of ephedrine, be sure you understand just how much is in each serving. Be aware that herbal preparations are standardized but you still can not be sure exactly how much you are taking with each capsule.
GENERAL DESCRIPTION & APPLICATIONS
Ephedrine is a sympathomimetic alkaloid originally obtained from species of Ephedra or prepared synthetically. Its action is similar to that of epinephrine (a catecholamine hormone secreted by the adrenal medulla and a neurotransmitter). Its effects, although less powerful, are more prolonged, and it exerts action when administered orally, whereas epinephrine is effective only by injection. It is used as muscle relaxants, central nervous system and cardiac muscle stimulants in combination with others like theophylline. It is used to prevent hypotension during spinal and infiltration anesthesia; and as a mydriatic. There are enantiomers in ephedrine structure. (1R,2S)- and (1S,2R)-enantiomers are designated ephedrine (opposite stereoisomerisms around the chiral center), whereas (1R,2R)- and (1S,2S)-enantiomers are designated pseudoephedrine. Commercial ephedrine is (-)-(1R,2S)-ephedrine [also called (-)-Ephedrine or L-ephedrine], while commercial pseudoephedrine enantiomer is (1S,2S)-pseudoephedrine [(+)-pseudoephedrine or D-pseudoephedrine]. Pseudoephedrine has less pressor action and fewer central stimulant effects than ephedrine. Pseudoephedrine is used as a nasal decongestant and a bronchodilator to relaxe and open the air passages to the lung to increase the flow of air, and thus is used in the treatment and/or prevention of symptoms of bronchial asthma and of reversible bronchospasm associated with chronic bronchitis and emphysema.
Maximum effectiveness is achieved when taking 20 mg ephedrine with 200 mg caffeine and 300 mg aspirin three times a day about one half hour before meals. Common side effects are associated with its sympathetic activity namely, anorexia, initial rise in blood pressure, initial tachycardia, slowed GI motility (constipation), insomnia, agitation, anxiety, nervousness and depression- like withdrawal symptoms. Most all of these symptoms exhibit tachyphylaxis after about 4-6 weeks. Thermogenic activity seems to last upwards of 20 weeks due to its low desensitization properties and beta-3 affinity. About 75% of ephedrine’s effects on weight loss in the obese are due to appetite control.
Anyone considering taking ephedrine, caffeine and aspirin should educated themselves first about the potential side effects. Individuals with pre-existing high blood pressure should not use sympathomimetics such as ephedrine. When taking herbal forms of ephedrine, be sure you understand just how much is in each serving. Be aware that herbal preparations are standardized but you still can not be sure exactly how much you are taking with each capsule.
Presentation
Phedrax Tablets Strip of 20 Tablets