Drugs
moleculeoftheday | March 14, 2007Lunesta shares its mechanism of action with the benzodiazepenes - Valium, Rohypnol, Xanax, etc. It doesn't actually belong to the benzodiazepene class of drugs, but they all work on the same system - GABA. Not coincidentally, the much-maligned GHB works by virtue of the fact that it is metabolized to GABA in vivo.
Lunesta belongs to a class of drugs that work similarly to benzodiazepenes but in such a way that they have a lower (but still nonzero) potential for abuse and dependency.
purepedantry | March 9, 2007We all know that inhaled anesthesia is over the short-term impairs neurological function; that is sort of the point using it for surgery.
However, a debate exists about whether inhaled anesthetics have long-term neurological consequences as well. In light of that debate Bianchi et al, publishing in the journal Neurobiology of Aging, have shown that in a mouse model of Alzheimer's disease some anesthetics increase histological measures of severity. Before you get excited though, let me tell you that the results are mixed.
Background
An important point to understand in this paper is that…
moleculeoftheday | March 7, 2007See also: yesterday's entry on folate.
Methotrexate is a mimic of folic acid. Shortly after we discovered what folate was, we started looking into what else we could do with it.
During the 1940's, George Hitchings and Gertrude Elion started work on a number of nucleic acid-related compounds that would prove astonishingly successful and later garner them a piece of a Nobel prize. One of these was methotrexate - the structure of folic acid is below for comparison.
As mentioned yesterday, folate plays a key role in nucleic acid synthesis - something rapidly-dividing cells need by the boatload…
moleculeoftheday | March 2, 2007Vinpotecine is a derivative from a compound found in the lesser periwinkle plant:
If you ever went to one of those "smart bars" in the late 90's, theres a good chance you tippled some vinpocetine. I'm not sure whether it's actually effective, but people have looked at it for everything from Alzheimer's, to a prophylactic drug in stroke patients, to something for people who just want to feel a little smarter ("nootropics").
moleculeoftheday | March 1, 2007Sorry if you're sick of this, but I'm having fun. You might remember my post on Havidol. (see also this follow-up). Justine Cooper (presumably) left a comment on the initial post, plus the prescribing information (PDF) has been updated. It's still not quite right - here, apparently, is your opportunity to make it right, and get a commemorative t-shirt in the process!
Previously, the entry for Havidol gave a name that didn't match the structure. The same was true of the molecular formula and molecular weight:
After making a couple posts to this effect, I got this follow-up:
We at HAVIDOL are…
moleculeoftheday | February 23, 2007See also this followup.
Take another look at the Havidol post's comments. It looks like the chemistry's not only a little bit off - some other parts of the site look a little familiar.
And by the way, it's HCl, not HCI.
moleculeoftheday | February 20, 2007See also the followups (one, two) to this post.
From the taking jokes too seriously department...
Havidol is a fake drug campaign by Justine Cooper that's on display in NY at the Daneyal Mahmood gallery (warning, slow loading, natively embedded video). It seems like a pretty well-done faux-drug site, and the gist seems to be mocking the idea that "lifestyle drugs" are becoming more and more ubiquitous.
I could go on about on the social aspects of this kind of drug and this kind of commentary, but that's not what I'm aiming for. (Besides, plenty of people are on that; even Reuters covered it…
purepedantry | February 16, 2007Dr. Henry Miller, writing in TCS, argues that the FDA has over-reacted to problems with drug safety by excessive regulation:
In spite of increasingly more powerful and precise technologies for drug discovery, purification and production, during the past twenty years development costs have skyrocketed. The trends are ominous: The length of clinical testing for the average drug is increasing, fewer drugs are being approved, and the number of applications to FDA by industry for marketing approval has been decreasing for more than a decade.
In January, the FDA announced new initiatives directed…
moleculeoftheday | February 13, 2007Betaine is a simple little molecule:
It finds use in medicine in treating elevated homocysteine levels - a molecule that deserves its own entry. It also can act as a denaturant - things like urea, formamide, and guanidinium are useful for this in biology. Betaine, at the right concentration, can help to unfold DNA a little bit, while leaving certain DNA polymerases untouched. For this reason, some people use it in DNA amplification by PCR.
moleculeoftheday | February 9, 2007As discussed in the entry on telomestatin, drugs that bind to guanine quadruplexes are of a lot of interest. One model compound is TMPyP (tetrakis(N-methylpyridyl)porphyrin)). The idea is that the big aromatic porphyrin surface stacks on the guanines, and the positive pyridinium moieties are near the negative DNA phosphates for a favorable Coulombic interaction. It's probably the most studied quadruplex ligand.
There isn't a lot I can say about quadruplexes, telomeres, and why they're important that I didn't cover in the telomestatin entry.
mikethemadbiologist | February 9, 2007I'm at a meeting in D.C. about antibiotic resistance, so I've left the Blogerator 9000 to fire up this post from the archives about a drug company executive's explanation of how drugs are priced. It's remarkable--and frustrating--that nobody has picked up on the basic message: drug prices are consumer driven, not R&D expenditure driven.
This is a headline from the June 1st, 2005 edition of ScripNews (subscription only; so I'm a little behind in my reading-what scientist isn't?). Here's the punchline for lazy stupids that don't like to read: the head of Pfizer has admitted that the cost…
moleculeoftheday | January 25, 2007Benzoylecgonine is the primary metabolite of cocaine - it's actually just cocaine minus a methyl group. It's not really used as an intoxicant, but it does have one interesting use: figuring out just how much cocaine people are using.
One study in 2005 in Germany examined the total amount of benzoylecgonine in wastewater (a good chunk of cocaine-derived benzoylecgonine is excreted in urine). Their result suggested the proportion of cocaine users was substantially larger than the 8 per 1,000 previously thought.
moleculeoftheday | January 23, 2007Brodifacoum is warfarin's mean sibling: it is another vitamin K analogue. It's so potent and has such a long half-life (on the order of months!) that it's more of a poison than an anticoagulant. It's used for the expected things; as a rat poison, etc. Interestingly, despite its lavish toxicity, all warfarin-type compounds, including brodifacoum, have an antidote: vitamin K (in controlled doses).
moleculeoftheday | January 22, 2007Warfarin belongs to a previously-covered class of molecules known as the coumarins. Coumarins see use both as anticoagulants (in people) and poisons (in certain small animals).
Warfarin works by inhibiting a crucial step in vitamin K metabolism. Its structure isn't so far off:
Vitamin K is named for the German koagulation. We get a lot of our chemical vocabulary from German - it wasn't that long ago that American chemistry undergrads had to take German as part of their degree. This is no longer the case, and it probably leads to a lot of frustration the first time people are looking over a…
purepedantry | January 19, 2007The Eli Lilly leaked documents story has exploded.
Just to recap, on Dec. 17th last year the NYTimes reported on documents leaked from Eli Lilly that show that the company tried to play down the side effects of Zyprexa, a popular schizophrenia drug. The documents were released by the company to a lawyer suing them on behalf of plaintiffs who got diabetes and other problems while on the drug. These documents were under a court ordered seal.
Then an unrelated lawyer from an unrelated plaintiff case subpoenaed those documents, and he released them to the NYTimes and others. The documents…
moleculeoftheday | January 16, 2007General anaesthesia has come so far, and yet not. Back in the day, we used to use lipophilic compounds like diethyl ether and alkyl halides like chloroform, and now we use...well, lipophilic alkyl halides like desflurane. Fortunately, desflurane doesn't cause so many toxic effects, due largely to the wonderful relative inertness of the C-F bond.
moleculeoftheday | January 11, 2007Despite the name, penicillamine isn't an antibiotic; it's actually a metabolite of penicillin-class drugs. It is given as the pure chemical too.
It is an immunosuppressant, among other things. My favorite medical use of it is its role in chelating copper as a treatment for Wilson's disease, a rare disease caused by an inborn error in metabolism that causes copper to accumulate. Remove the copper, you treat the disease.
scientificactivist | January 10, 2007Mandatory sentencing laws are disliked by many, and for good reason. Judges often criticize these laws for taking away their judicial sovereignty, while others decry the inherent disparity in which they affect minorities and those of lower socioeconomic status. They often lead to inordinately severe punishments for arguably minor, generally drug-related, crimes. The good news is that, as The New York Times reported yesterday, there is reason to believe that some of the more extreme of these mandatory sentencing laws may change under the new Democratic Congress.
Examples of why these laws…
moleculeoftheday | January 9, 2007Last week it was revealed that for just about the entire 1970's, former SCOTUS chief justice Rehnquist was taking Placidyl. This is too long by any measure - it's been unavailable in the States for almost a decade (due to better alternative supplanting it), and even when it was available, it was thought to be less-than-prudent to prescribe it for more than a week. Further, he was taking about triple the recommended dose. He went through some ugly withdrawal symptoms, in one case insisting that the CIA was plotting against him.
It is hard to overstate the importance of the benzodiazepines in…