Ephedrine about

The total alkaloidal eontent of Ephedra varies widely, being influeneed by the speeies eolleeted and the seasonal and environmental eonditions, as has been shown by Read and by Chopra and their eolleagues. For speeially eolleeted material yields as high as 2- 56 per cent., of which 1- 8 per cent, is ephedrine, have been recorded, but about 1 per cent, of total alkaloids is not usually exceeded in the commercial product. 

For commercial Ephedra the British Pharmaceutical Codex, 1934, specifies a total alkaloidal content of not less than 1-25 per cent, when assayed by the method therein prescribed. The proportion of Z-ephedrine is generally about 70 per cent. Methods of assay for total alkaloids are described by Feng and Read and by Krishna and Chose, who discuss the various difficulties involved and comments on these and other methods have been made by various workers. Conditions affecting the results of such assays have also been discussed by T ang and Wang, and Brownlee has shown that chloroform is not a suitable medium for the assay since it converts ephedrine quickly and 0-ephedrine slowly to the hydrochloride. 

In a summary of the human abuse literature on anorectic phenylethylamines, Griffiths et al. (1979) found there was a good correlation between the results of self-administration studies in animals and information about the subjective effects and abuse in man. Specifically, amphetamine, diethyl-propion, and phenmetrazine have been associated with numerous clinical case reports involving abuse, and these three compounds as well as benz-phetamine and /-ephedrine have shown similar subjective effects in drug abuser populations (Griffiths et al. 1979). In addition, fenfluramine was associated with low incidence of abuse in humans and did not maintain self-injection responding in animals. Chlorphentermine was similarly associated with low incidence of abuse in man, but did not maintain selfinjection uniformly in animals (Griffiths et al. 1979). 

On the other hand, asymmetric addition of lithium acetylide in the presence of the ephedrine derivative 46 is a homogeneous reaction and reveals great detail about the reaction mechanism. 

Considering that the consumption pattern observed in the area of the Ebro River basin studied, which covers about half of the population living in the basin, could be representative of the whole Spanish country, the estimated average consumption data were used to calculate the annual consumption of each drug in the whole basin and in the Spanish territory. According to the extrapolated figures, which are shown in Table 2, around 21 tons of cocaine, 8 tons of cannabis, 3 tons of amphetamine and ephedrine, 300 kg of ecstasy and heroin, and 7.5 kg of methamphetamine are annually consumed in Spain. These amounts would move in the black market for around 1,100 million Euros. 

In more recent times interest has been shown in the effects of constrained environment on the outcome of such reactions. Some enantioselectivity in the product 308 has been reported following the irradiation of benzonorbornadiene 309 in a T1Y zeolite. (—)-Ephedrine was used as the chiral inductor and sensitization brought about the reaction in 30 min. An ee of about 14% was obtained168. 

Ephedrine. Is a psychotomimetic (gives an amphetamine type high) in larger doses (25 to 100 mg). Can be reduced to memylamphetamine in one step (find a gentle reduction in the reductions chapter and apply it to an equimolar amount of ephedrine) which is psychotomimetic with a dose of about 5 mg. 

Taking North America as a whole, the declines in the USA were partly offset by rising production in a few super-labs in Mexico. The number of methamphetamine laboratories dismantled in Mexico rose from 10 in 2002 to 18 in 2004 and 34 in 2005. Until recently pseudo-ephedrine and ephedrine were fairly readily available in the country. The Mexican authorities, however, have recently taken measures to counter the diversion of the two chemicals. These efforts reduced the import of ephedrine and pseudo-ephedrine by 40 per cent in 2005 (to 133 mt), with a further reduction of almost 50 per cent (to about 70 mt) expected for 2006.13... 

B National Drug Intelligence Centre, National Drug Threat Assessment 2007, Oct. 2006 According to data collected by the INCB, the decline was from 177-8 mt of pseudo-ephedrine in 2004 to 107.7 mt in 2005 and from 118 kg ephedrine in 2004 to 64 kg in 2005, which is also equivalent to an overall decline of about 40 per cent. 

Europe as a whole accounted for about 6 per cent of global ephedrine seizures over the 2004-2005 period. Listed in order of importance, the following European countries reported seizures of methamphetamine precursors over the same period the Czech Republic, Greece, the Russian Federation, the UK, Bulgaria, Germany, Iceland, Romania, Hungary, Slovakia, the Ukraine, France, Norway and Latvia. In 2006, EUROPOL noted increased export, transshipment and diversion of ephedrine and pseudo-ephedrine to the European Union.24... 

Concerns about the safety of ephedrine-containing products date back to 1994, when the FDA noticed an increase in the number of health problems associated with the use of ephedrine, including chest pain, headaches, increased blood pressure, heart attack, hepatitis (inflammation of the liver), stroke, seizures, and sometimes death. In 2001, the National Football League banned the use of ephedrine by professional football players. The National Collegiate Athletic Association (NCAA) and Olympic committees have also banned the use of ephedrine by their athletes. In February 2004, ephedrine was finally banned by the FDA from being sold in the United States. To date, at least 100 deaths have been attributed to ephedrine use in the... 

R)-a-Phenylalkylamines. (R)-a-Phenylethylamine (4) can be prepared in about 97% optical purity by addition of methylmagnesium bromide to the chiral hydrazone obtained from benzaldehyde and the N-amino derivative (1) of D-( —)-ephedrine followed by hydrogenolysis (equation I). Acetophenone is not a suitable starting material because it reacts with 1 to form two isomeric hydrazones. ... 

Local anesthetics block the sodium channels, are cardiac depressants, and bring about a ventricular conduction defect and block that may progress to cardiac and ventilatory arrest if toxic doses are given. In addition, these agents produce arteriolar dilation. Circulatory failure may be treated with vasopressors such as ephedrine, metaraminol (Aramine), or mephentermine (Wyamine). Artificial respiration and cardiac massage may also become necessary. Among the local anesthetics, only cocaine blocks the uptake of norepinephrine, causes vasoconstriction, and may precipitate cardiac arrhythmias. 

In experimental animals the effect of ephedrine administered intravenously is similar to that of epinephrine. The arterial pressure — systolic, diastolic, and mean pressure — rises and vagal slowing occurs. Compared with epinephrine, the pressor response to ephedrine occurs somewhat more slowly and lasts about ten times longer. Furthermore, it requires more ephedrine than epinephrine to obtain an equivalent pressor response. How much more depends on the species tested, type and degree of anesthesia, dose level, and individual variability of the test animal. It is, therefore, almost impossible to give a definite figure for the relative potency of ephedrine and epinephrine. It is commonly accepted that it requires about 250 times more ephedrine than epinephrine to achieve equipressor responses. 

The pressor response to ephedrine is due in part to peripheral constriction and in part to myocardial stimulation. Vasoconstriction can be demonstrated by intra-arterial injection, but compared to epinephrine, ephedrine is only about one thousandth as active. This would imply that the cardiac effect is predominant in increasing the arterial pressure. This, however, is difficult to demonstrate. In perfused hearts, ephedrine produces only minor stimulation and cardiac depression appears if the drug is repeated. 

In complete heart block with Stokes-Adams syncope, ephedrine may prove of value in a manner similar to epinephrine. In the attempt to increase ventricular rate and prevent ventricular asystole, an initial dose of about 8 mg of ephedrine sulfate orally may be tried. Later, the dosage may be increased to 25 mg three or four times daily. Syncope due to ventricular tachycardia can also be prevented in some cases with ephedrine. 

Since 1997, a number of groups have lined up on each side of the ephedra battle. A non-profit group called Halt Ephedrine Abuse Today has spoken out about the dangers of ephedra. On the other side of the battle is the Ephedra Education Council, a group backed and supported by the herbal products industry and supplement manufacturers. Many of the companies that sell products containing ephedra do not want any further restrictions on the products. 

A big concern about ephedra is that drug traffickers and laboratory operators are using ephedrine to make methamphetamines (speed). Consequently, in the United States, ephedrine is subject to regulatory laws. The Drug Enforcement Administration (DEA) carefully monitors medications containing ephedrine. 

Some medical experts have testified about ephedrine s physiological side effects, which include hypertension and an increased risk of heart attack or stroke. The Halt Ephedrine Abuse Today survey found that more than 60% of respondents reported feeling physiological side effects such as a rapid heartbeat, nervousness, headaches, insomnia, shortness of breath, and chest... 

Manufacturers of nutritional supplements containing ephedrine claim that the products can enhance athletic performance and improve physical fitness. Indeed, ephedrine supplements are popular among all sorts of athletes. As health concerns about ephedra grow, however, many professional and amateur athletes will find that they may have to choose between the sport they love and a questionable supplement. 

The NFL instituted the ephedrine ban partly in response to health concerns. NFL doctors warned players about the growing body of evidence linking ephedrine use with strokes, seizures, and fatal heart rhythm. 

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