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

Pharmacokinetics & Noted Drug-Drug Interactions | BuSparPagesIndex | Comments
Crazymeds Comprehensive BuSpar pages

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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Pharmacokinetics & Noted Drug-Drug Interactions | BuSpar Index | Comments
Crazymeds Comprehensive BuSpar pages


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.

Date created {{$$newlycreated}} Page Author: Last edited by: JerodPoore on 2014–04–23

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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.

2 Remember kids, Microsloth operating systems are like TOS Star Trek movies with in that every other one sucks way, way more. With TOS Star Trek movies you don’t want to bother watching the odd-numbered ones. With Microsloth OS you don’t want to buy and install the even-numbered ones. Anyone who remembers ME and Vista knows what I mean.

3 Have I mentioned how open source operating systems for commercial applications is one of the dumbest ideas in the history of dumb ideas?
[begin rant] I rent a dedicated server for Crazymeds. It’s sitting on a rack somewhere in Southern California along with a bunch of other servers that other people have rented. The hardware is identical, but no two machines have exactly the same operating systems. I don’t even need to see what is on any of the others to know this. If somebody got their server at the exact same time, with the exact same features as I did, I’m confident that there would be noticeable differences in some aspects of the operating systems. So what does this mean? For one thing it means that no two computers in the same office of a single company have the same operating system, and the techs can spend hours figuring out what the fuck the problem could be based on that alone. It also means that application software like IP board that runs the forum here has to have so many fucking user-configurable bells and whistles that even when I read the manual I can’t find every setting, or every location that every flag needs to be set in order for a feature to run the way I want it to run. And in the real world it means you can get an MBA not only with an emphasis on resource planning, but with an emphasis on using SAP - a piece of software so complex there are now college programs on how to use it. You might think, “But don’t people learn how to use Photoshop or Adobe Illustrator in college?” Sure, in order to create stuff. And in a way you’re creating stuff with SAP. But do you get a Bachelor of Fine Arts degree with an emphasis on Photoshop?
Back in the Big Iron Age the operating systems were proprietary, and every computer that took up an entire room with a raised floor and HVAC system, and had less storage and processing power than an iPhone, had the same operating system as every other one, give or take a release level. But when a company bought application software like SAP, they also got the source code, which was usually documented and written in a way to make it easy to modify the hell out of it. Why? Because accounting principles may be the same the world over, and tax laws the same across each country and state, but no two companies have the same format for their reports, invoices, purchase orders and so forth. Standards existed and were universally ignored. If something went wrong it went wrong the same way for everyone, and was easy to track down. People didn’t need to take a college course to learn how to use a piece of software.
I’m not against the open source concept entirely. Back then all the programmers read the same magazines, so we all had the same homebrew utilities. We even had a forerunner of QR Code to scan the longer source code. Software vendors and computer manufacturers sponsored conventions so we could, among other things, swap recipes for such add-ons and utilities. While those things would make our lives easier, they had nothing to do with critical functions of the operating system. Unless badly implemented they would rarely cause key application software to crash and burn. Whereas today, with open source everything, who the hell knows what could be responsible some part of a system failing. [/end rant]

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