Comprehensive Rundown Page 1 | BuSparPagesIndex

Page two of everything we know about BuSpar (buspirone) on two big-ass pages. From pharmacokinetics to the bibliography, or: the crap 99% of people don’t care about. See the first page for brand / trade names to odds of working and comparisons with other meds.

The titles for most sections link to the pages for those sections. While all the information is on these two comprehensive pages, the individual section pages go into a little more detail about what it all means.

1.  Black Box Warnings, and other Noted Traits and Effects.

Most drugs are known for something. If Viagra or Cialis are mentioned what do you think of first? How effective either one is for erectile dysfunction, the pros and cons of each, Viagra’s weird side effect of cyanopsia (where everything you see is tinted blue), or that your hard-on can last over four hours and if it does you’re supposed to call Dr. Buzzkill about it. That’s what I thought.

1.1  BuSpar (buspirone) is best known for:

Being a total disappointment.

1.2  Black box warnings

1.3  Black box comments

1.4  Unique or Noted Traits and Effects

2.  Pharmacokinetics

Pharmacokinetics (PK) is mostly what your body does to a drug, along with what happens in your liver, kidneys, and other squishy parts that aren’t your brain.

2.1  Plasma half-life


2.2  Estimated elimination time


How BuSpar (buspirone) is metabolized, and what the effects and results of the metabolism are.

This is what pharmacokinetics is all about as far as most people are concerned. How a drug is metabolized in order to be eliminated / cleared from your body. If and how it is transformed into something else and what that is3. How it affects the metabolism of other meds4. To what extent everything is involved. E.g. by the time your liver and kidneys are through with it, 97% of Paxil (paroxetine HCl) has been converted to inactive stuff that gets flushed down the toilet, whereas 70% of the Topamax (topiramate) you take is unchanged in your urine. See the section on CYP450 and UGT enzymes on the Pharmacokinetics page for more details.

2.3  Elimination method(s):

2.4  Transformation method(s):

2.5  Active metabolites:

2.6  Enzymes inhibited, induced, or suppressed:

2.7  Check for drug-drug interactions’s drug-drug and drug-food interaction checker

It’s always a good idea to check for drug-drug interactions yourself. Just because most people in the crazy meds business know about really important interactions (e.g. MAOIs and a lot of stuff,warfarin and everything on the planet) doesn’t mean the person who prescribed your meds told you about them.

2.8  Noted interactions

The really important ones. Also the non-pharmacokinetic interactions besides the boilerplate “taking two or more antidepressants meds can make you extra drowsy/spacey/ready to go on a tri-state multicide spree” you won’t find on any drug-drug interaction checker, and any others we know of that don’t make it into drug-drug interaction checkers.

BuSpar is one of the drugs most affected by grapefruit juice and related foods (pomegranate juice, Earl Grey tea, etc.). You don’t even want to look at grapefruits in the produce section if you’re taking BuSpar. While it may not be that serious, the interaction is strong enough that you shouldn’t even drink Fresca or any other grapefruit flavored beverage.

2.9  Bioavailability, bioequivalence and additional PK data

Bioavailability is how well a drug is distributed through your body after you take it. These are the numbers a generic manufacturer has to meet for a drug to be considered as bioequivalent.

If these data aren’t entered, look them up in the pharmacokinetics section of the PI sheet. These data are usually in the US PI sheets - almost always for newer meds, less often in older ones. These data are now appearing in more and more PI sheets / specifications of product characteristics (SPCs) from other countries as well.

Are the PK affected by doses/dosage?5 
Steady state (Css), in days: 
Time of maximum plasma concentration (Tmax),
in hours:
Peak plasma concentration (Cmax), in ng/ml: 
Area under the curve (AUC0–24), as 
Overall bioavailability %: 
Protein binding %: 
Miscellaneous PK data: 

3.  Mechanism/Methods of Action

It’s often the vaguest section in any drug’s PI sheet. Pretty much every beginning paragraph of the mechanism/methods 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…”

3.1  Original theoretical mechanism of action

3.2  Current theories and our best guess

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.

3.3  Drugs with similar methods of action


4.1  Our Comments

BuSpar is a quirky med, and there’s currently nothing else approved for use in its class of azapirones. At least in English speaking countries.
While BuSpar’s value for some flavors of anxiety is important, more important is its potential to augment an SSRI that was working great and then quit on you, the bastard.
BuSpar is a maintenance med - i.e. you wait for the calming effects to build up and you keep taking it until you either learn to deal with your problems on your own or you live with the fact you’re going to be taking BuSpar for the foreseeable future. Something I feel should be considered as a maintenance medication long before the benzos, as it doesn’t build up tolerance or addiction, and thus avoids many of the problems with long-term benzodiazepine use, particularly as a prophylactic (preventing anxiety before it starts).

4.2  Your Comments

There are 2 reviews of BuSpar (buspirone).

08 July 2011 - 10:56  

14 November 2012 - 17:51  

Enter your own Comments & Experiences here.
You must be a registered member of the Crazymeds Talk forum to post a comment on this page.

5.  Discussion Board, Official Sites, PI Sheets, and other Useful Links

5.1  Discussion Board

Crazymeds’ BuSpar discussion board

5.2  Official US website

All that’s on is a link to the BuSpar PI sheet at BMS’ main site.

5.3  Other official websites

5.4  BuSpar’s Full US Prescribing Information

5.5  PI Sheets for other forms

5.6  Non-US SPCs, PILs, etc.

5.7  Consumer rating/review sites

A word about consumer rating & review sites. They tend to skew negative in a way that isn’t in line with the real world. While more people have negative experiences with meds than big pharma would otherwise have you believe, the drugs are rarely as bad as various sites on the Internet usually make them out to be.

5.8  Other sites of interest’s BuSpar Page

6.  Bibliography

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Comprehensive Rundown Page 1 | BuSpar Index

1 Plasma half-life: how long it takes for half of the drug to clear from your blood stream.

2 This is the "plasma clearance," and is based on Julien's calculations from A Primer of Drug Action. It's basically the plasma half-life multiplied by five and is the generally accepted estimate of how long it takes a med to be eliminated from the system of someone with a normal metabolism. A more accurate number requires a lot more data, including your weight and the dosage you're taking.

3 Because the pill you take is not necessarily the drug that actually does something. Trileptal, Effexor and Risperdal themselves don't do squat, but are each transformed into active metabolites that do the real work. Predigested versions of Risperdal and Effexor are now available as Invega and Pristiq. Other meds, like Wellbutrin, do something and are transformed into one or more active metabolites that also do something.

4 AKA 90% of drug-drug interactions.

5 The PK of some meds is affected by the how much you take (e.g. Cymbalta), or the number of doses (e.g. Lamictal). If it's blank then we don't know. Otherwise:
* No: Dosage / Number of doses doesn't matter
* Dosage Proportional: The dosage affects the PK at a steady rate.
* Dosage Non-liner: The dosage affects the PK, but how it does is complicated, or makes no sense at all.
* Number of Doses: How often you take the med affects the PK.
* Other: There's an effect that isn't like any of the above.
* Unknown: We know that they don't know if there's an effect or not.

Date created {{$$newlycreated}} Page Creator: Jessica Allan Last edited by: JerodPoore on September 23, 2013, at 04:55 PM

BuSpar Bibliography by Jessica Allan is copyright {{$$yearly}} Jessica Allan

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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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