Physical Insights

An independent scientist’s observations on society, technology, energy, science and the environment. “Modern science has been a voyage into the unknown, with a lesson in humility waiting at every stop. Many passengers would rather have stayed home.” – Carl Sagan

A Rant about Phenylethylamines.

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As a bit of a change today, we’ll have something that is not energy related.

I have a shocking cold/flu at the moment. It’s really not fun. So, today, I went out to grab some of ye olde decongestant tablets, and take them… only to realise that, eight hours and six tablets later, my nose is still running as much as ever. Checking the packet in detail, I realised that I have, for the first time, fallen victim to pharmacology’s answer to the dodgy used-car lemon that doesn’t work as advertised.

That dodgy lemon is called phenylephrine.

Phenylephrine has been making its way into oral cold and allergy medications in response to the perceived “epidemic” of methylamphetamine abuse in Australia (as well as in other Western countries) – but it is typically met with skepticism by pharmacists – because phenylephrine doesn’t bloody work, at least not when given orally at these sorts of doses. This is the first time I’ve actually been given something by a pharmacist which is not psuedoephedrine.

The loser in this war against methylamphetamine abuse will be the general public, if pseudoephedrine is pushed out of the over the counter market, as it is doubtful if the legal restrictions on the sale of pseudoephedrine to the public will reduce the availability of methylamphetamine. There is little evidence that medicines containing pseudoephedrine are used by large scale producers of methylamphetamine.[1]

The general public – the Australian public, the U.S. public, and everyone else – will be deprived of access to an effective nasal decongestant as pharmaceutical companies and pharmacists are pressured into switching to manufacturing and stocking an ineffectual medicine in phenylephrine.[1]

There is little if any clinical support for the efficacy of phenylephrine as a nasal decongestant, and its oral bioavailability is quite limited. In contrast the efficacy of pseudoephedrine as a nasal decongestant is much stronger and its absorption from the gut is uncomplicated.[1]

Oral phenylephrine is used as a decongestant, yet there is no published systematic review supporting its efficacy and safety.

No support has been found in the literature in the public domain for the efficacy of phenylephrine as a nasal decongestant when administered orally.
The only study involving an oral dose of phenylephrine reported that 10 mg phenylephrine (PE) was no more effective than placebo as a nasal decongestant, and a comprehensive recent Cochrane review provides no support for the efficacy of PE. In view of the extensive metabolism of PE in the gut wall, it seems unlikely that PE is an effective oral nasal decongestant. [2]

There is woefully insufficient evidence that oral phenylephrine is effective for nonprescription use as a decongestant, [3], and that’s not good enough. When people are paying for medicine, by rights, by law, they should be getting a product that actually works.

The PSA Code of Professional Conduct for Australian pharmacists states that a pharmacist must not sell any medicinal product where there is reason to doubt its efficacy. It could easily be argued that pharmacists have an obligation to advise patients that oral phenylephrine is not likely to be an effective nasal decongestant – or, to just not dispense it. Certainly, pharmacists are also obliged to avoid inadvertently contributing to the illicit manufacture of methylamphetamine. Does the replacement of psuedoephedrine products with phenylephrine containing products in pharmacies compromise the professional ethics of pharmacists, given that phenylephrine is ineffectual as an orally administered nasal decongestant? Pharmacists need to decide how they will approach this issue in their pharmacies and attempt to find a balance between the professional and legal obligations that surround the supply of psuedoephedrine and the professional and moral obligations of evidence based medicine.

In fact, studies in the USA indicate that restricting the sale of psuedoephedrine to the public as a medicine has had little impact on the morbidity and number of arrests associated with methylamphetamine abuse. [2]

So, you’re depriving people of legitimate, effective medicine, for legitimate use, and accomplishing nothing as a result.

Of course, if you really wanted to, in one fell swoop, completely do away with the whole issue of illicit use of psuedoephedrine as a precursor for methylamphetamine, then all you have to do is market enantiopure (1R,2R)-ephedrine in these medicines – which does have the full therapeutic effectiveness, with zero potential for illicit diversion.

The only question is how expensive the enantiopure drug would be.

It begs the question – will people with a flu pay more for the enantiopure drug if it means they can actually get the drug that is therapeutically effective, with no bullshit, without being treated like criminals?

To end up with the problematic D-methylamphetamine, from ephedrine, you need to start from (1R,2S)-ephedrine, or (1S,2S)-(psuedo)-ephedrine – if you started with (1R,2R)-psuedoephedrine or (1S,2R)-ephedrine, then you only end up with L-methylamphetamine, if you reduce the stuff. (In case you’re getting confused, they call it psuedoephedrine where both the chiral carbons have the same stereochemistry, and call it ephedrine when they’re different.)

L-methylamphetamine is not nearly as addictive or active on the central nervous system as D-methylamphetamine, and only exerts effects on the sympathetic nervous system – it is a useful vasodilator and decongestant, but it is completely useless as a recreational drug.

1: http://www.bmj.com/cgi/eletters/332/7538/382-b
2: http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=200071
3: http://news.ufl.edu/2006/07/19/decongensant/
There are a few more references out there, mainly papers in the scholarly literature, but I won’t link to those as most won’t be able to access them without subscriptions, and they can be found linked via the above-cited pages.

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Written by Luke Weston

September 4, 2008 at 5:02 am

Posted in Uncategorized

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One Response

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  1. The entire hierarchy of “Medicine” features among its most fundamental tenets the validity of the so called “behavior health” sciences with their associated array of kooks and quacks of various designations and specialties–the clinical psychologist (family, cognitive behavioral, Freudian Psychoanlyst-obsolete, psychiatrists and the forensic psychiatrists arrayed like a vast army among the courts of the land). And if there one thing that these pseudo-scientists of mass quackery love more than anything is to convey pseudo-diagnoses by way of their fatuously scientific bible of ill-repute, the so called “Diagnostics and Statistics Manual”. The absurdity of the name being ever so obvious in light of the simple fact that in most every example cited in this ever evolving and growing list of high fallunin terminology that the general public finds so very stultifying upon confronting at first glance there is no such thing as statistical validity by way of the manner that these labels are conferred. Statistical replicability being the very cornerstone of any and all science they may be deemed as legitimate, along with independent replicability, the fact that the most all the so called diagnoses listed can be shown to satisfy either requirement has not stopped these various sundry professions and vast armies of professionals from engaging in their so called “practice” which by definition can not be be classified as anything other than malpractice. Among the list then a most notable sort of transgression among a field of pure transgression has emerged–that of the “delusional disorder” chief among this category has now been applied so as to strip any and all “defendants” in the court of law of their due process rights, that of the so called “conspiracy theorist”. Few will ever venture to actually define the word, and yet the consensus among the cohort of practitioners prevails. And yet what do we see here by way of the pseudoephedrine scandal but the emergence of a true conspiracy. Of note then the very name of Medicine itself–easily split into two words, that of Medici-sin–alludes directly to the series of corrupt popes that carried that very name and are regarded as the renaissance architects of the entire field of so called “Medical” science in general. Hence the emergence of all the claptrap that is pseudo-science, used to exploit, demean, impoverish, injure and kill on a scale not seen since the very inquisition itself. So if you wish to properly contextualize the entire problem as noted in your lovely rant above, there you have it; a family renown as the very pinnacle of the old world “Illuminati” per the grand and ever present menace of the Catholic Church itself, the Vatican and the so called Holy See of the great EYE on the top of the pyramid depicted on the dollar bill itself, is indeed in charge of this horrendous fiasco that we all must endure and will just as likely cause our demise as prevent it. Because no medicine ever approved should ever be intended to work as prescribed, hence the great paranoia of the practitioners themselves, that the patient population might become enlightend to a degree sufficient To SEE the scam for what it is. Sorry to say. For the great spirit of the Holly Roman Inquisitor lives on to this day, albeit via a secular humanist veneer. And therefore we are to be permitted access even to those substances known since deep antiquity–such as the use of marijuana for seizure control and the treatment of neurodegenerative diseases now deemed untreatable by way of contemporary clinical standards. No no. Not so very man years ago I’d purchase an entire bottle of pseudoephedrine pills, for barely but a few pennies per pop. Not anymore. So if you wish to understand the grand scam you must examine the name of the Gil-man, as in Daniel Coit Gilman and the associated cult of the fish, the dogon as it relates to the founding of modern Medici-sin in the contemporary world. The very hats worn by the Pope and his entourage–the fish head with mouth open toward the sky–recapitulates the symbol of The Eye, if you must know. Hence, Gillett (is) the best a man can get” because he is so very Gill-tee. And so it goes. Medici-sin is of the Papal Sin, of the Gilman and the fish, and the razor of the Gill-tee that we pass along our very gullets each and every day, and this in turn is a reference to the symbol so famed for its use in the Freemasonic instigated French Revolution where that cult that goes by the letter G used the Guillotine as its symbol and instrument of terror in the legendary reign of terror that prevailed in the wake of that historical event. The guillotine in the FEMA camp, as such our destiny has been made, rendered in the name of the founder of the Gillette company itself no less–Mr. King Camp Gillett, I can say. Because I am one of these people, this family of such high minded and crafty sin–Medici-sin being but a cover for the deeper theme. So we all must blow our noses in unison so as to salute the clan of that rules the Master Class. The Master Architect who instigates The Great Work of The Craft reigns supreme. And if that means that all of our noses must run, then such is the intent of the Master himself. Any pretext will do. In all avenues of life the same. I kid you not. Would I lie about such a thing? As Lucifer himself is known by any other name as “The Great Deceiver”, one ought not to expect an outcome that reflects any other way. Sorry to say. Thanks then for the info that you have provided, the best remedy in its place I might recommend is a bit of Epsom salt under the tongue. It opens up nasal passages just a bit and lessens the associated itch. Rather primitive a remedy but it’s the best I myself as one likewise under Jack the Rippers blade–Jack and Gill being a legendary pair–have been able to contrive to date. Cheaper. Not as effective. Then again, given the motif and its meaning as so defined, I think we have greater worries on our table to ponder. Best wishes to you from mediocre me. N. G.

    Noel Gillett

    September 29, 2018 at 9:13 am


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