It's just for my...for my headache, officer

Published on 04/03/2007

Although last week I brilliantly finished the semester with a tough exam and, after that, I had a whopping two-days-long holiday, I didn't post on any given day as I hoped I'd have done.

I wrote I was tired, but after sleeping for 9 consecutive hours, I felt fine. Unfortunately, I had to face nasty headache, which began on Wednesday and lasted until this morning.

I guess it was a sort of weekend headache. Annoyingly, it matched what I hoped would have been the "Relax Week": the new semester starting on Thursday, nothing to study and more free time than during the previous three months.

Headache isn't uncommon for me. As the majority of people, I often suffer from common headache. And that's fine because, two years ago, I experienced classic headache too.

Classic headache is characterised by the so-called aura, which is linked to visual and speech abnormalities. I have to add vomiting to the list, too.
I didn't like it...

Headache: trigeminal nerve and CGRP


There's no doubt there are many drugs you can choose to tackle pain. The ultimate, most powerful molecules are, anyhow, the ergot derivatives.
Not that I've ever tested them, but this week the sorrow made me think, often, about their pros and cons.

Mind you, there is a substance we all know for different reasons which, being an ergot derivative, should guarantee exactly the same effectiveness of, say, methysergide.
This molecule was discovered by a Swiss chemist. To be precise, a pharmaceutical chemist.

I am talking about Albert Hofmann and the molecule is, obviously, LSD (lysergic acid diethylamide).

Hofmann's recurrent thought


Theoretically, every ergot derivative could be used for the treatment of headache. Not only do they relieve the pain (like NSAIDs), but they also act presynaptically on 5-HT1 receptors of the trigeminal nerve, so that no more CGRP is released. Amazingly, they even avoid vasodilatation, due to their direct effect.

However, LSD has a much stronger central activity, which explains why it's such a potent hallucinogen. LSD  has, infact, astonishing activity, as agonist, on 5-HT2 receptors.

Here we are: I'm a young pharmaceutical chemist, who suffer from headache. So, there must be a post dedicated to LSD on my blog.

First of all, I've to say I've never tried it and, probably, I'll never, either.
Nevertheless, if I'll do my PhD at prestigious Harvard University, I think, on my first day there, testing it could be the right tribute to Timothy Leary and a sort of initiation to the (old) campus life there.

Many people even ignore he was a brilliant researcher of psychology at Harvard University, before I was "convinced" to get away.
By the way, he is far from being a model for me, unlike Hofmann.

Surprisingly, LSD has huge therapeutic index: 20µg are sufficient to begin the trip, while 200mg are lethal. Not that bad for such a fiercely potent psychoactive drug.

Some effects are experienced after a couple of hours: vertigo, chills but also flushing and tachycardia.
Gradually, the drug begins to induce central effects: the brain gets incredibly more sensitive to stimuli, memory is increased, as well as freedom of thought and clarity of ideas.

The person feels a new sense of well-being. At the same time, anyhow, anxiety and hypomanic exaltation can take place.

Timothy Leary's advice


None of these things are, however, the main reason of the success of LSD. What people look for are, mainly, the subsequent hallucinations and altered sense of time and surrounding space.

Bad trip is the expression which sums up its toxicity: terror, complete (albeit transient) loss of the sense of reality, retrospective sensations and lack of motivations.

You can hear lots of rubbish about LSD causing persistent damage to your neurons. There's nothing to prove it, but, it must be pointed out that this happens with lab animals and there are, undoubtedly, dramatic changes in metabolites of serotonin in humans.

Other ergot derivatives (including a less potent natural version of LSD) have similar hallucinogenic properties. Something which you can appreciate, oddly, in art galleries.

In fact, ergot is a fungus that infests grain: that was a terrible problem in the middle age, when the inhabitants of entire villages could avoid poisoning because they knew nothing about ergot.

Ergot infection


Poisoning is associated with the psychotic effects of LSD and they are particularly well documented in Bruegel's paintings: check this out.


 


Many women were believed to be witches, solely due to behavioural changes.

There is another dreadful side effect of LSD and its congeners: catastrophic vasoconstriction, which leads to gangrene, and uterine contractions, abortifacient, especially for cattle, but also for humans.

Very deadly, but, still, effective for headache.

 


 


Comments

  1. 05/03/2007 | 13:56

    You know, there are people looking into the use of psilcybin and psilocin in the treatment of migraine and "cluster headaches." Their website is www.clusterbusters.com. I found this quote: "The pain of a cluster headache is worse than natural childbirth or even amputation without anesthetic. The pain of a cluster headache commences quickly, without warning, and reaches a crescendo within 2 to 15 minutes. It is often excruciating in intensity, and is deep, nonfluctuating, and explosive in quality." Interesting...Perhaps clinical trials are in order for a new treatment.

  2. 05/03/2007 | 18:00

    Great post and an interesting topic. Headache is one of the most prevalent indications out there, but without the glamour of all the other indications it doesn't seem to get that much attention. Thanks for the history lesson as well.

    How about a post of the cinchona alkaloids and their history?? Tonic water for all!

  3. 29/03/2007 | 13:49

    If you want to be a better scientist, a better human and a better person take LSD when you have a chance.
    If you pass the acid test you will gain priceless insights into yourself and the whole world surounding you.
    HIGLY RECOMENDED, not for the weak though!
    PS. Once you pass your test you cant get back to your previous ignorant self...

  4. 26/07/2007 | 08:15

    I know a man who stopped counting the number of times he had taken LSD at 100.

    He used to be phenomenally intelligent, now he gets lost in supermarkets, but it was not LSD that did him in.

    What ended up ruining his mind, you ask? A Cocaine induced Aneurysm, twenty years later, in a congenitally weak artery. (the idjit got the bright idea into his head to take Cocaine and do push-ups -rolls eyes- )

  5. 04/08/2007 | 19:39

    Dear Albert Hofmann turned a hundred last year

    he looks like a million dollars !

    have a tour of the Albert Hofmann' s foundation site

    the topic is far from being dead...

    and I corroborate

    one day on some nice safe corner of nature

    you may want to indulge...

    at least as a chemist

    you can test your hit.

    The best entheogen ever discovered

    Thank you Albert Hofmann

  6. zac
    17/04/2008 | 00:14

    Wow! that was absolutely amazing. I like how informative it was, but also how confusing it wasn't. ...If that makes sense. Somehow you made that far from boring, and it's one of the first articles that I've read completely. I've had migraines in the past, which the reason i looked it up is because got off work and immediately, after arriving home, fell asleep uncomfortably in my pickup for who knows how long. Went inside the house, (was very hard to do because my leg was dead asleep, probably looked like a drunk man trying to walk up the hill) and went to my bed. I now woke up 4 hours later and my head hurts so much... so i came across your article, and i'm tempted to take LSD :P but the idea of such a thing scares me. i am like you and probably never will take such a drug. But i wanted to give you kudos for such a neat article.

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