buspirone pharmacodynamics (mechanisms/methods of action). What BuSpar does and how it does it.



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1.  Working Theory

When you read about the mechanism of action, or how it works, in BuSpar’s PI sheet, it’s almost as vague as how likely it will work. Pretty much every beginning paragraph of the mechanism of action section for every crazy med (and many other non-crazy meds) is a variation on “We don’t know exactly how Panacea, or other drugs like it, works to treat whatever you take it for. In various studies, mostly on rats and other animals, we’ve determined that it does the following…” What you read in the PI sheet is often, but not always the original theorized mechanism of action, or what they thought it does when they started testing the drug for whatever it is now used for1.

After researchers who aren’t being paid by the manufacturer get their hands on med it’s just one study after another, in humans and animals, that supports the original theory. Or determines a precise area in the brain where stuff takes place. Or finds an additional thing the med does. Or finds that it doesn’t do something they originally thought it did. Or finds out that everyone was completely wrong in the first place and the method of action is radically different. That last one does happen. Neurontin (gabapentin) was originally thought to be a synthetic form of GABA that could cross the blood-brain barrier. Turns out that it’s just like every other anticonvulsant and works on voltage channels. Except that it’s unique in that it affects a part of your brain that nothing else touches. Except for Lyrica (pregablin), and a few meds under development (e.g. PD−210714). Still, some people are calling those parts of your brain some people are calling those “gabapentin receptors”, along the lines of benzodiazepine receptors. There supposedly were citalopram receptors as well, but that turned out to be a myth. Ironically gabapentin doesn’t directly affect GABA.

Every day a new peer-reviewed journal is published somewhere adding to our knowledge about how a particular med works, or making us crazier with more contradictory data.

It would be nice if we could break things down into neat parameters like we can with pharmacokinetics, but we can’t. The best we can do is tell you what they originally thought it did, let you know if there are any meds with similar mechanisms / methods (the terms are interchangeable) of action, and give you our best guess as to what it really does based upon more recent research.

2.  How BuSpar (buspirone) Works

2.1  What the PI Sheet Says

2.2  What BuSpar (buspirone) Really Does

as far as we can tell
As with most of these crazy meds it’s easier to say what BuSpar doesn’t do. BuSpar doesn’t do any of the fun benzodiazepene fuck-you-up-and-get-high effects. BuSpar doesn’t knock you out. BuSpar doesn’t hit GABA.

What BuSpar does do is to keep serotonin within the 5HT1A neurons, thus fooling your brain into thinking it has more serotonin than it actually has. BuSpar also does some noticeable dopamine agonism-antagonism on the dopamine D2 receptor. When combined with an SSRI this can help with sexual dysfunction and to prevent SSRI poop-out, per Dr. Stahl in Essential Psychopharmacology.



3.  Functional Equivalence

No two medications will have the exact same mechanisms / methods of action. Sometimes a drug that is developed from the active metabolite of another, essentially inert med e.g. Invega (paliperidone) is a predigested form of Risperdal (risperidone) and is basically the same thing. However there is no good conversion of dosages between the two like there is for Tegretol (carbamazepine) and Trileptal (oxacarbazeine). Like Invega and Risperdal, Pristiq (desvenlafaxine) is the active metabolite of Effexor (venlafaxine), but Pristiq has a somewhat different mechanism of action than Effexor. Mainly it kicks Effexor’s ass when it comes to how potent its inhibition of norepinephrine reuptake is.

All SSRIs are essentially interchangeable, making it possible to work out equivalent dosages so you don’t need to wait until you’ve cleared one drug to start another. But Celexa (citalopram) and Lexapro (escitalopram) are vastly more selective than Prozac (fluoxetine), and so the side effect profiles, and pretty much everything else, are very different when you compare Celexa or Lexapro with other SSRIs, but practically identical when compared with each other. While most people couldn’t tell the difference between Lexapro and Celexa,2 because Lexapro is a derivative of Celexa, a few people will respond differently to the two.

3.1  Drugs with Similar Methods of Action as/That Work Like BuSpar (buspirone)



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4.  References

  1. BuSpar (buspirone) Full US Prescribing Information

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Pharmacokinetics & Noted Drug-Drug Interactions | BuSpar Index | Comments


1 Unlike Lamictal, which was originally thought to be be such a potent folate antagonist that it would work well as a treatment for malaria and similar parasites that took up residence in your brain. Or Topamax, which was originally thought to be an awesome drug for type 2 diabetes, as it looked like it would both control weight and blood sugar.

2 The one real difference used to be cost. Now that Lexapro is available as a generic in the US that difference isn't as great as it once was.


If you have any questions not answered here, please see the Crazymeds BuSpar discussion board. We welcome criticisms of the articles, notifications of bad links, site problems, consumer experiences with medications, etc. I’m not always able to write back. Hence I never answer questions about meds via e-mail that are answered by this or other articles. Especially if they have been repeatedly asked on the forum. That’s why we write these damn things. Questions about which meds are best for your condition should also be asked on the forum; because this is a free site, so the price of admission is making things easier for somebody else searching for the same answer. We don’t deal with children on the forum or in private because after doing this for ten years I don’t have the emotional stamina to deal with kids who have brain cooties. How to contact Crazymeds. — Jerod Poore, CME, Publisher crazymeds.us


Last modified on Monday, 23 September, 2013 at 16:51:14 by JerodPoorePage Authors , Jerod PooreDate created
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BuSpar, and all other drug names on this page and used throughout the site, are a trademark of someone else.

will probably have the name of the manufacturer and trademark owner (they’re not always the same company) at or near the very bottom. Or ask Google who the owner is. The way pharmaceutical companies buy each other and swap products like Monopoly™ real estate, the ownership of the trademark may have changed without my noticing. It may of changed hands by the time you finished reading this article.




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1 While there are plenty of books to help you with hypochondria, for some reason there’s not much in the way of websites. Then again, staying off of the Internet is a large part of curing/managing the disorder.

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