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. | ||||||
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Ephedrine, originally isolated from plants of the Ephedra plant, occurs as the naturally-occurring isomers 1-ephedrine and d-pseudoephedrine, and other pharmacologically active isomers include d-ephedrine and 1-pseudoephedrine. Ephedrine and associated alkaloids are structurally similar to the amphetamines and, by stimulating adrenergic receptors, can increase arterial blood pressure through both peripheral vasoconstriction and cardiac stimulation. Ephedrine compounds are adrenergic sympathomimetic agents and have antihistamine activity; 1-ephedrine is widely used as a bronchodilator, while d-pseudoephedrine is widely used as a decongestant. Compounds of these groups are present in a very wide range of prescription and over-the-counter pharmaceutical formulations. Ephedrine is a typical indirect-acting sympathicomimetic agent. This substance may also be referred to as agonists, where the name agonist is qualified by a descriptor of the receptor stimulated, for example, a beta-agonist. Acting indirectly, the main action of ephedrine is to elicit release of noradrenaline (norepinephrine) from presynaptic sites. This in turn activates both alpha- and beta-adrenoceptors.
It has even been reported that ephedrine may be an example of a trace substance that belongs in the human diet, and that it provides an opportunity to attack obesity at a level that is close to causative. Ephedrine was originally thought to suppress the hunger center in the human brain. However, research has shown that ephedrine acts mainly by stimulating thermogenesis. Namely, it increases the metabolic rate and stimulates lipolysis (fat breakdown). Though it has some central stimulant effect, and thus mediates suppression of hunger, ephedrine’s main mode of action appears to be peripheral and, in part, causative since it offsets the decline in metabolic rate that normally occurs on caloric restriction. The effect of ephedrine on the peripheral metabolic rate is derived from actions on energy-generating tissues combined with stimulation of the release of fat from stored fat depots (adipose tissue). This effect not only increases the generation of energy but also adds the availability of substrates to be utilized for this energy generation. A valuable consequence of these two actions is the sparing of body protein, which, depending on the composition of the diet, may even result in a gain of body protein (anabolic effect). Ephedrine and associated alkaloids are structurally similar to the amphetamines which act on the brain by stimulating the release of norepinephrine and dopamine at the nerve synapses, by stimulating adrenergic receptors, can increase arterial blood pressure through both peripheral vasoconstriction and cardiac stimulation.
Ephedrine stimulates the production of catecholamines such as norepinephrine. Norepinephrine or noradrenaline is thought to start the thermogenic process by stimulating metabolism in fat cells via the neurocrine axis that involves beta-adrenergic receptors. This in turn results in lipolysis, or the liberation of fat in fat cells via an increase in the basal metabolic rate. This pharmacological action results in weight loss effect in obese people. The thermogenic action which results from ephedrine’s effects on metabolic rate and lipolysis persists throughout its use period, and may intensify as use continues. The effects of ephedrine can often be intensified by concomitant use of methylxanthines such as caffeine. Ephedrine products have been often advertised as weight-loss promoters, energy enhancers, and alternatives to illegal psychoactives and have been sold for years without labeling indicating the potential adverse effects, contraindications, or dosage recommendations. Side effects from ephedrine can be variable, and do not always depend on the dose consumed. In addition, ephedrine is dangerous to people with hypertension, heart disease, or diabetes.
Ephedra and Ephedrine Alkaloids for Weight Loss and Athletic Performance
Office of Dietary Supplements • National Center for Complementary and Alternative Medicine • National Institutes of Health
Table of Contents
Key points
Introduction to ephedra and ephedrine alkaloids
Products available for weight loss or athletic enhancement
Overview of the RAND evidence-based review of ephedra and ephedrine alkaloids
References
This document summarizes the results of an evidence-based review on the efficacy and safety of ephedra and ephedrine alkaloids for weight loss or to enhance athletic performance (power and endurance). The report was prepared by the Southern California Evidence-based Practice Center-RAND (RAND) under contract to the Agency for Healthcare Research and Quality (AHRQ) of the U.S. Department of Health and Human Services. This work was sponsored by the Office of Dietary Supplements (ODS) and the National Center for Complementary and Alternative Medicine (NCCAM) of the National Institutes of Health, U.S. Department of Health and Human Services. A summary of this report was published in JAMA and the data described here are drawn from that article .
Key points
* The Chinese botanical ephedra, or ma-huang, is sold as a dietary supplement in the United States. It is a natural source of the alkaloids ephedrine and pseudoephedrine. Some dietary supplement products used for weight loss and to enhance athletic performance contain these alkaloids.
* Synthetic ephedrine and pseudoephedrine are found in over-the-counter decongestants and cold medicines and are used to treat asthma. Ephedrine is not approved in the United States as a drug for weight loss or to enhance athletic performance.
* The use of ephedrine, ephedrine plus caffeine, or dietary supplements containing ephedra and botanicals with caffeine is associated with a modest but statistically significant increase in weight loss over a relatively short time (less than or equal to 6 months). No studies have assessed their long-term effects (greater than 6 months).
* No studies have assessed the effect of dietary supplements containing ephedra and botanicals on athletic performance. The few studies that assessed the effect of ephedrine support a modest effect of ephedrine plus caffeine on very-short-term (1-2 hours after a single dose) athletic performance in a highly selected physically fit population.
* Results of controlled trials show that the use of synthetic ephedrine, ephedrine plus caffeine, or ephedra plus botanicals containing caffeine is associated with 2-3 times the risk of nausea, vomiting, psychiatric symptoms such as anxiety and change in mood, autonomic hyperactivity, and palpitations compared with placebo.
* RAND analyzed adverse event reports filed with the U.S. Food and Drug Administration (FDA) and with a manufacturer of ephedra-containing dietary supplements as well as published case reports. Although this analysis raises concerns about the safety of botanical dietary supplements containing ephedra, most of these case reports are not documented sufficiently to support an informed judgment about the relationship between the use of ephedra-containing dietary supplements or ephedrine and the adverse event in question.
* According to the RAND report, the number of deaths, myocardial infarctions, cerebrovascular accidents, seizures, and serious psychiatric illnesses in young adults is sufficient to warrant further evaluation of the safety of these products in a controlled manner (such as a hypothesis-testing case-control study) to test the possibility that consumption of ephedra or ephedrine causes these serious adverse events.
Introduction to ephedra and ephedrine alkaloids
The Chinese botanical ephedra, or ma-huang, is sold as a dietary supplement in the United States. Ephedra is the common name for three principal species: Ephedra sinica, Ephedra equisentina, and Ephedra intermedia [2]. The active compounds in the plant's stem (about 1.32% by weight) are the phenylalanine-derived alkaloids ephedrine, pseudoephedrine, phenylpropanolamine (norephedrine), and cathine (norpseudoephedrine) [3,4].
Alkaloid content and composition vary by species and growth conditions [5-7]; total alkaloid content can vary from 0.5% to 2.3%. Ephedrine, the most potent alkaloid, can account for up to 90% of the total alkaloid content and pseudoephedrine can account for up to 27% [3,8,9]. The pharmacologic activity of an ephedra sample depends on its alkaloid composition. North American ephedra species, such as E. Nevadensis (known as Mormon tea), contain little or no ephedrine or other alkaloids [10].
Ephedrine is a mixed sympathomimetic agent that enhances the release of norepinephrine from sympathetic neurons and stimulates alpha and beta receptors [11]. Ephedrine stimulates heart rate, thereby increasing cardiac output [11,12]. It causes peripheral constriction resulting in an increase in peripheral resistance that can lead to a sustained rise in blood pressure [13]. It relaxes bronchial smooth muscle [11,12] and is used as a decongestant and for temporary relief of shortness of breath caused by asthma.
Ephedrine acts as a stimulant in the central nervous system [11,12]. Of the ephedra alkaloids, ephedrine is the most potent thermogenic agent. It may function as an anorectic by acting on the satiety center in the hypothalamus
Products available for weight loss or athletic enhancement
Ephedrine or products containing combinations of ephedrine and caffeine are not approved in the United States as drugs for weight loss. Botanical dietary supplements for weight loss may include ephedra (a natural source of ephedrine) and other botanicals that are natural sources of caffeine and salicylic acid. In place of ephedra, manufacturers sometimes substitute botanicals that contain sympathomimetic amines, such as country mallow or bitter orange. Botanicals with diuretic or cathartic action are sometimes also included.
Although ephedrine is not approved in the United States as a drug for athletic performance, athletes have used over-the-counter stimulants containing ephedrine or its related alkaloids to enhance athletic performance. Products containing ephedra alone or combined with vitamins, minerals, or other botanicals are marketed to increase energy and enhance athletic performance.
Overview of the RAND evidence-based review of ephedra and ephedrine alkaloids
ODS and NCCAM sponsored an evidence-based review by RAND to assess the clinical efficacy and safety of products containing ephedra or synthesized ephedrine alkaloids used for weight loss or to enhance athletic performance. RAND, one of 12 centers participating in the AHRQ Evidence-based Practice Program, prepared a report for AHRQ that was released in March 2003. A technical expert panel that included basic scientists and clinicians with a wide range of expertise provided input for the report.
RAND conducted a comprehensive search of published and unpublished sources for controlled clinical trials on ephedra and ephedrine used for weight loss and athletic performance in humans. Each study considered for the review was evaluated according to preestablished criteria. RAND identified 52 controlled clinical trials of synthetic ephedrine or botanical ephedra used for weight loss or athletic performance in humans. Weight-loss studies with at least 8 weeks of follow-up data were reviewed for inclusion in a meta-analysis. Studies of athletic performance used a wide variety of interventions and were not synthesized through meta-analysis.
The strongest level of evidence to show that an adverse event was caused by a particular exposure comes from placebo-controlled randomized trials. Data on adverse events associated with the use of ephedrine or ephedra-containing dietary supplements were collected from 52 randomized controlled trials identified in the literature search. The number of events or people (depending on how the study reported the events) was abstracted for each treatment and placebo group. A meta-analysis was conducted on data from 50 trials for subgroups of adverse events, including psychiatric symptoms, autonomic hyperactivity, nausea/vomiting, palpitations, hypertension, and tachycardia. No serious adverse events (death, myocardial infarction, cerebrovascular/stroke events, seizure, or serious psychiatric events) were reported in the clinical trials. However, because participants in clinical trials must meet eligibility criteria, including the absence of specific underlying health risks, they may not represent the general population.
Case reports were assessed in this review because the total number of patients in the clinical trials was not sufficient for adequately assessing the possibility of rare outcomes. Although such adverse event reports are not conclusive evidence of a cause-and-effect relationship, they can indicate the potential for such a relationship.
The cases came from the published case reports identified in the literature search; case reports from the FDA through September 30, 2001; and case reports from a manufacturer of ephedra-containing dietary supplements. The reports were coded for the type of adverse event; serious adverse events were analyzed further. The goal of the analysis was to identify cases that would be classified medically as idiopathic in etiology (i.e., cause unknown). If use of ephedra or ephedrine-containing products was documented for such cases, then the possibility that ephedra or ephedrine caused the event was considered.
Cases were classified as sentinel events if 1) documentation existed that an adverse event meeting the selection criteria occurred, 2) documentation existed that the person having the adverse event took an ephedra-containing supplement within 24 hours before the event (for cases of death, myocardial infarction, stroke, or seizure), and 3) alternative explanations were investigated and excluded with reasonable certainty. If another condition existed that by itself could have caused the adverse event but may have been precipitated by ephedra or ephedrine, it was classified as a possible sentinel event.
Ephedra Gerardiana capsules home
Latin name: Ephedra Gerardiana
Family: Ephedraceae
Common name: Somlata,
English name: Ephedrine. Epitonin, Ma Huang
Habitat
West Central China, Southern Siberia, Japan.
Ephedra Gerardiana Capsules
Macroscopic identification
It is found on sandy seashores and in temperate climates of both hemispheres. The plant has stamens and pistils on separate flowers--staminate flowers in catkins and a membraneous perianth, pistillate flowers terminal on axillary stalks, within a two-leaved involucre. Fruit has two carpels with a single seed in each and is a succulent cone, branches slender and erect, small leaves, scale-like, articulated and joined at the base into a sheath.
Parts used
Root and ried branch
Pharmacological action
A sympathetic nerve stimulant resembling adrenaline, its effect on the unstriped muscular fibers is remarkable. It acts promptly in relieving swellings of the mucous membrane. It has valuable antispasmodic properties, acts on the air passages and is of benefit in asthma and hay fever; it is also employed for rheumatism; a 5 to 10 per cent solution has mydriatic properties, prophylactically used for low blood pressure in influenza, pneumonia, etc. It is also alterative, diuretic, stomachic and tonic.
Action and uses in Ayurveda
Kaphavatashamak, shothara, vednashamak, shwaskas hara, mutrl and gharbhashyasankochak
Indications
Asthma.
Properties and action
Rasa: kasaya
Guna: laghu,ruksha
Virya: usna
Vipaka: katu
Karma: shwashar
Preparations
Decoction, tincture, alcoholic extract,
Therapeutic classification index:
• Central nervous system: Blood and haemopoeitic tissue:.
• Cardiovascular system: The circulatory stimulation diverts blood flow from the digestive tract and forces more blood to the brain and limbs, thus reducing fatigue and reducing hunger
• Respiratory system: Used to control wheezing. Relaxes the lungs and bronchioles and is useful in affections of respiratory passage
• Nutrition and metabolism: Weight Management: Somlata has a thermogenic effect that is increased by salicylic acid (aspirin) or caffeine (kola nut). This effect is successfully used as part of a weight loss program. It improves digestion and tones up the small intestines
• Genito-urinary system: Opens the pores and promotes sweating. Used for chills, fever, headache and tight, floating pulse. Promotes urination and reduces edema
Ephedrine Resembles Adrenaline
The alkaloid ephedrine contained in the plant has an action nearly akin to that of adrenaline (Dr. Chen. U. Schmidt) when used by mouth hence can be suitably used in place of adrenaline, which acts only when injected. It acts o the sympathetic nervous system, constricts the blood vessels and raises the blood pressure. It stimulates the respiratory centers, uterus, dilates the bronchi and pupils, contracts the intestines and raises blood sugar.
Pseudo ephedrine stimulates both the inhibitory and the accelerator mechanism of the heart and has stimulating influence on myocardium.
Effect of ephedrine on lungs
The pulmonary pressure shows a marked rise, the action resembles that of adrenaline. The rise in pressure is due to contraction of the branches of the pulmonary artery and this also relieves the turgescent of the mucus membrane. Along with this, at the same time there is dilatation bronchioles and both these factors help in relieving paroxysms of asthma.
Ephedra and its alkaloids are effective bronchodilators in the treatment of mild to moderate asthma and hay fever. The peak bronchodilation effect occurs in 1 hour and lasts about 5 hours after administration.
Many believe that the therapeutic effect of Ephedra will diminish if used for a long period of time, owing to a weakening of the adrenal glands caused by ephedrine. But, according to the American Pharmaceutical Association, "there is far more discussion of ephedrine tachyphylaxis [rapid decrease in effectiveness] or tolerance than is evidenced as a significant problem in the scientific literature." A 1977 study of ephedrine therapy in asthmatic children, published in the Journal of the American Medical Association, concluded: "Ephedrine is a potent bronchodilator that, in appropriate doses, can be administered safely along with therapeutic doses of theophylline without the fear of progressive tolerance or toxicity.
Nonetheless, many practitioners of natural medicine prescribe ephedra in combination with substances that support the adrenal glands, such as licorice (Glycyrrhiza glabra) and Panax ginseng and/or supplemental levels of vitamin C, magnesium, zinc, vitamin B6, and pantothenic acid.
The old-time herbal treatment of asthma involves the use of ephedra in combination with herbal expectorants. Expectorants modify the quality and quantity of secretions from the respiratory tract, causing the user to spit up the secretions and ultimately improving respiratory tract function
Effect of ephedrine on heart
The stimulant action of both the chemicals is well known on blood pressure and therefore is used as a cardiac stimulant. Ephedrine in large doses has a depressant action on myocardium. Pseudo ephedrine on the other hand has a stimulant action on heart muscles. Besides its action on the vasomotor endings it also stimulates the muscle fibers of arterioles.
In cases of left heart failure ephedrine tincture proved very effective even when the digitalis and other cardiac stimulant proved ineffective.
Use of Ephedra in weight loss
Ephedra preparations may be useful as a weight loss aid. Although ephedrine does suppress appetite, its main mechanism for promoting weight loss appears to be by increasing the metabolic rate of adipose tissue. Its weight reducing effects are greatest in those individuals with a low basal metabolic rate and/or decreased diet-induced thermo genesis.
Precautions
Because it is such a powerful stimulant and can raise blood pressure, caution is recommended for those who already have high blood pressure or weak internal organs.
Taking too much of ephedra-based products too fast can result in hand tremor, nervousness, restlessness, excessive stimulation, rapid heart rate or insomnia, all similar to the effects of too much coffee, tea or cola drinks. Tolerance usually develops rapidly to these effects, but not to the fat burning benefits. Caffeine will increase both the stimulant and thermogenic effects of ephedra. Do not use this product if you're pregnant or lactating. Persons with high blood pressure, atherosclerosis, heart disease, diabetes, prostatic hypertrophy, glaucoma, hyperthyroidism or psychosis should not take any product containing ephedrine or ephedra herb. Elderly persons may be more sensitive to ephedrine.
Action And Clinical Pharmacology: Ephedrine is an adrenergic drug which exerts peripheral effects resembling those of epinephrine and central effects resembling those of the amphetamines. Ephedrine produces a more sustained action but is less potent than epinephrine. It stimulates both alpha and beta receptors and its peripheral actions are due partly to norepinephrine release and partly to direct effects on receptors. Ephedrine stimulates the heart, elevating the systolic and usually the diastolic blood pressure. Its vasopressor effect results largely from increased cardiac output and to a lesser extent from peripheral vasoconstriction. Ephedrine produces relaxation of bronchial muscle which is more sustained but less pronounced than that produced by epinephrine. It also stimulates the CNS to a greater extent than epinephrine, but its central action is less potent than that of the amphetamines. The central effects of ephedrine are overshadowed to a large extent by its peripheral actions. It produces sympathomimetic effects when administered orally, parenterally or topically. Tag_indicationsindications
Indications And Clinical Uses: Symptomatic relief of nasal congestion associated with a variety of upper respiratory tract illnesses.
Contra-Indications: Known hypersensitivity to pressor amines. Tag_warningwarnings
Manufacturers' Warnings In Clinical States: Do not exceed recommended dosage or take for more than 7 days except on the advice of a physician. Consult a physician prior to use if you have heart or thyroid diseases, high blood pressure, diabetes, glaucoma, difficulty in urination due to an enlargement of the prostate gland or if you are taking any prescription drugs. Do not take if you are currently taking or have recently taken MAO inhibitor drugs. Use only on the advice of a physician.
Precautions: Use with caution in hypersensitive and diabetic patients; patients with latent or clinically recognized angle closure glaucoma, coronary artery disease, congestive heart failure, prostatic hypertrophy, hyperthyroidism, urinary retention.
Pregnancy and Lactation: Safety for use in pregnancy and lactation has not been established.
Geriatrics: The elderly (60 years and older) are more likely to have adverse reactions to sympathomimetics. Overdosage of sympathomimetics in this age group may cause hallucinations, convulsions, CNS depression and death.
Adverse Reactions: Acute toxic reactions are usually extensions of the therapeutic actions of the drug and are most often due to overdosage. Administration of ephedrine may be followed by headache, restlessness, insomnia, anxiety, tension, tremor, weakness, dizziness, confusion, delirium, hallucinations, pallor, respiratory difficulty, palpitation, precordial pain (occasional), sweating, nausea or vomiting. These effects are usually transient and can be minimized by rest and recumbency. Tag_dosagedosage
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