Misc butalbital? And its metabolites? (i.e., "fioricet")

[AlphaOdure]

Does anyone have any knowledge in regards to pharmacologically active butalbital metabolites (if applicable)...? or in general, is anyone aware of more pharmacologically potent/active butalbital metabolites? & if so, anyone aware of any CYP inducers or inhibitors existing that would increase the-said-effects-of-the-more-potent metabolite OR increase the duration of action (whichever is applicable). Or i suppose, anyone aware of any effective drug/dietary supplement/herb that increases butalbital's effects generally speaking? The only information I can seem to find is that butalbital itself is CYP3A4 inducer. Anyone aware of or have any positive experiences with any relative CYP inducers or inhibitors that extend the duration--or the effects--of butalbital (whether through CYP/hepatic action or not)? I am particularly interested in OTC drugs or herbal supplements, although info on scheduled drugs is fine as well.. although leave out benzodiazepines, we all know they potentiate barbiturates.

Background-
I seem to only experience butalbital's therapeutic & psychoactive effects around 15 minutes after dosing, slowly dropping off after 2.5 hours; despite it being a fairly long, or at least intermediate acting barbiturate! Although I do notice accumulative effects at the end of the day after repeated doses, including ataxia, mental confusion, sedation. After periods of abstinence (which are admittedly forced for one reason or another) I notice very intense effects; yet these effects seem to drop off after the 2nd or 3rd day of daily dosing.

I usually dose 200 mg - 500 mg at a time, with a total daily intake of around 1300 mg -1800 mg. The reason i am asking this question is most obviously b/c my tolerance keeps creeping up & up. And I am aware barbiturates can be relatively lethal at higher doses irrelevant of tolerance to psychoactive effects; & i do not care to be on high doses of barbiturates (i've had to experience withdrawal from it.. & to say the least, it was worse than heroin), yet weaning seems to be quite hard. So I am looking for methods & means to successfully increase the drug's efficacy w/o increasing the dose since I do no wish to up my dose anything further. And/or I am looking for any methods to aid in minor withdrawal symptoms if I am able to successfully reduce my dose.

 

[AlphaOdure]

MY PREVIOUS EXPERIENCES W/ BUTALBITAL POLYDRUG USE:
NOTE:I do not condone nor recommend polydrug use, nor do I condone or recommend any of the following combinations.

Diphenhydramine (100 mg per dose; 550 mg maximum daily intake)
Slight increase in duration of side effects; but not necessary duration of psychoactive effects. No impact upon euphoria or therapeutic effect. Minor increase in sedative effect; increase in ataxia in doses of >100 mg of diphenhydramine.

Buprenorphine (1 mg per dose; 4 mg daily)
I am prescribed suboxone; there seems to be little impact buprenorphine has on butalbital; however, a marked increase in opioidergic effects are noticed if butalbital is doses roughly ~10 minutes after insufflation; alternatively, little increase in GABAergic effects are noticed if one precedes dosing butalbital with buprenorphine.

Raw Valerian Root & Valerenic Acid (13.5g raw herb maximum intake; once daily)
Increase in sedation & less potential for redosing of butalbital (due to slight increase in GABAergic effects); but not necessarily an increase in the duration of euphoric and/or therapeutic effects are noticed.

Alprazolam / Xanax (not taken regularly- 1.5 mg per dose; maximum 6 mg daily intake every taken)
Synergetic GABAergic effects- notably increase in anxiolysis, sedation, euphoria, amnesia, ataxia, & euphoria.

Carisoprodol / Soma (1400 mg per dose; 8750 mg - 9800 mg daily intake)
Slightly increased sedation.
Converse effects:
A somewhat overall decrease in GABAergic effects are noticed when taken concurrently; when transitioning from one substance to another (especially from butalbital to carisoprodol) the typical psychoactive effects of GABAergics are noticeably decreased. Higher doses of either substance seems to make little difference (perhaps some hepatic interaction occurring here? Or possibly some antagonistic effect or increased binding affinity of one or the other of these drugs at GABA receptors? But one would assume they would increase each other's neurological effects).

Ethanol / Alcohol (dose & frequency of use varies, maximum dose is 1.5 oz per hour)
Potentiation of butalbital increased; lower doses required; slightly increased euphoria. Additionally- duration of butalbital effects are increased. Increased nausea; severely increased sedation relative to either drug on its own.

Gabapentin / Neurontin (300 mg - 1000 mg per dose, daily intake is the same; usually used sparingly)
Severely increased ataxia; slurred speech; slightly increased euphoria; increased nausea; slight synergetic effects on loss of inhibition.
Converse effects:
insomnia; slight visual hallucinations and/or disturbances; decrease in butalbital dose efficacy roughly during the peroid 12-36 hours proceeding dosing gapapentin. I'm not a pharmacologist nor am an organic chemist, but the effects i've experienced seems this drug has a selective, antagonizing effect at some GABAergic-related recepto(s). [/I]

Trazadone
Increased sedation

 

[AlphaOdure]

UPDATE: http://www.drugbank.ca/drugs/DB00241

By the looks of this website (and others confirming the same information), it seems that roughly half of a given butalbital dose ingested is metabolized into its "parent compound" barbituric acid--just like all other (or at least most other) barbiturates. But barbituric acid is not psychoactive by itself. So a second question: is barbituric acid psychoactive if you bypass first pass metabolism, or perhaps better worded, is barbituric acid's inactivity due to metabolism if taken in its pure form?? Therefore, if it does have some activity in and of itself, is there any known CYP450/CYP3A4 substrates (whether inducers or inhibitors) that increase the intensity ~OR~ duration of the effects of a said-barbiturate by interacting with barbituric acid metabolism (in this case butalbital of course)? OR.. does barbituric acid just not pass the blood-brain-barrier no questions asked, no matter what (and subsequently inducing metabolism into barbituric acid would result in decreased effects; however, if this is the case; it seems inhibition of metabolism would result in severely increased psychoactivity)??

As I research this, I think this question may be more appropriate for the ADD forum....

But any info or experience is still appreciated?

 

[Thorns Have Roses]

Alprazolam / Xanax (not taken regularly- 1.5 mg per dose; maximum 6 mg daily intake every taken)
Synergetic GABAergic effects- notably increase in anxiolysis, sedation, euphoria, amnesia, ataxia, & euphoria.

Not just synergy, barbiturates increase binding affinity of benzodiazepines.
http://www.ncbi.nlm.nih.gov/pubmed/8090834
http://www.ncbi.nlm.nih.gov/pubmed/2906155

 

[AlphaOdure]

Interesting.. but the articles you referenced are the other way around; they show increased binding affinity of benzodiazepines when taken with phenobarbital and pentobarbital; where as I am asking what would potentiate barbiturates (and as i said, not particularly interested in benzo's since its quite obvious, unless someone has some unique, interesting info). I do know both drugs have a pharmacological synergy (and not just a subjective or symptomatic-synergy) with each other though, since they modulate GABA using different mechanisms.

I really did not notice much benefit with alprazolam; it did increase the overall GABAergic effect but nothing of major significance. The pharmacological interaction did not seem as if it significantly increased affinity or GABAergic sensitivity. I used around 15 mg over the course of 5 - 7 days. Although, I did not use high doses (at least for my tolerance) since I do not care for the benzodiazepines "high", specifically the amnesia I do not get with intermediate barbiturates.

(note: i combined alprazolam with butalbital before becoming aware of the pharmacological synergetic profile of these drugs)

~ ~ ~

EDIT: OOPS, NEVERMIND.. BARBITURATES INCREASING THE BINDING AFFINITY OF BENZODIAZEPINES IS WHAT YOU CLAIMED IN THE FIRST PLACE. HOWEVER, I AM ASKING THE ALTERNATIVE QUESTION.. WHAT DRUGS/HERBS HELP WITH INCREASING THE BINDING AFFINITY AND/OR GABAERGIC EFFECTS OF BARBITURATES (OR BUTALBITAL MORE SPECIFICALLY) -- AND AS I MENTIONED, I'M NOT PARTICULARLY INTERESTED IN BENZODIAZEPINES & OTHER CHEMICALS SUCH AS ETHANOL, WHICH I'M SURE IS QUITE OBVIOUS TO MOST OF US.

ALTHOUGH UNIQUE ARTICLES SUCH AS THE ONES YOU POSTED NEVER KNOWS BEST ARE WELCOME...

 

[AlphaOdure]

How about phenibut? Or dextromethorphan (low-level use in 100-200mg range seemed to antagonize the effects of carisoprodol, which also is a GABAergic drug, so I am hesitant to try it)? Or baclofen (even though its hard to come across & may have limited synergy as it is more selective at GABA-b sub receptor sites)? Anyone have any experiences? Either using these substances by themselves (except for DXM, as I am well aware of its effects in and of itself) or preferably using them as barbiturate substitutes, as an aide in weaning, or to increase the barbiturate's effects (again- butalbital is the barb in question here)? I'm also interested in anyone who's combined butalbital or other barbiturates with gabapentin (neurontin)... b/c some of the effects I experienced seemed quite odd and contradictory (see the very first two posts on this thread); as both drugs are GABAergics (although I know, I know, currently there is some debate over gabapentin's efficacy as a GABAergic, but from what i've gathered- it is definitely seen to act as a GABA reuptake inhibitor, albeit this may not be the primary mode of action)

Also, any recommended dosing regimes, since barbiturates are highly interactive w/ CYP450 enzymes & thus metabolism? Currently; I usually dose every 2-5 hours (aside from when i'm sleeping of course), at about 250 - 500 mg per dose (usually). I've experimented with dosing more frequently at lower levels: 200 mg maximum, every 1-2 hours (but with the same daily intake). It seems more beneficial & I seem to get more therapeutic effects; but for some reason it really hasn't seemed to aide whatsoever in my attempts to wean and/or decrease my dose to a more manageable and sane level (i'm guessing this is probably b/c I am taking lower doses, which decreases the duration & more quickly metabolizes/excretes butalbital).

 

[NeighborhoodThreat]

I've actually found baclofen to be a bit closer to the feeling butalbital gives me than say, lorazepam or diazepam. I had a butalbital prescription for many years (ending in the version without caffeine) and, to be honest, it got kind of old. I find lorazepam to be more effective for anxiety and pretty much anything to be more effective for migraines.

On a side note, mixing butalbital (or any barb) with alcohol is an extremely dangerous idea. The dose-response curve is extremely steep and its very easy to take it way too far. I almost ended up in the emergency room because of a butalbital+alcohol overdose a few years back.

It was after that experience that I stopped taking butalbital altogether.

Be careful. Please.

 

[Captain.Heroin]

Just Be Careful with Barbiturates

I have never tried butalbital myself, so I have nothing to add other than; please don't mix a large amount of butalbital with methadone. This is how my friend Chris overdosed and finally died after a few life threatening overdoses. He was a Bluelighter by the name FlyWithCloudNine. I posted his Shrine post.

MY PREVIOUS EXPERIENCES W/ BUTALBITAL POLYDRUG USE:
NOTE:I do not condone nor recommend polydrug use, nor do I condone or recommend any of the following combinations.

Thank you for the forewarning.

 

[AlphaOdure]

I have nothing to add other than; please don't mix a large amount of butalbital with methadone. This is how my friend Chris overdosed and finally died after a few life threatening overdoses.

I am sorry to hear about your loss. Methadone seems to be one of those drugs that manifests unusual (and lethal) properties when used in combination with certain other drugs, an effect that seems not entirely linked to typical opioid activity, or the mu-opioidergic system.

I am on buprenorphine, another drug linked to polydrug induced death w/ benzodiazepines (there is no mention of butalbital or barbiturates, but i'm sure the same would apply). But these deaths are mostly from IV use of benzos and/or buprenorphine, and any potential "increased" reaction is all derived from these few case studies. And also, me thinks the perceived increased lethality of suboxone mixed with CNS depressants is more related to behavior/drug-use patterns its patients typically engage in (since must of us are addicts/recovering addicts) rather than an actual abnormal interaction (how many controlled, double-blind studies exist that mix IV'd benzodiazepines with IV'd buprenorphine/naloxone and assess their effects? that's my point). But all this is purely speculation on my part.

Anyway, sorry.. i tend to go off on tangents; but thanks for your concern Captain.Heroin

I've actually found baclofen to be a bit closer to the feeling butalbital gives me than say, lorazepam or diazepam.

That seems about right. Baclofen is selective to GABA-b; benzo's to GABA-a ... where as barbiturates modulate all of them; so i could see it being "closer" to butalbital than to benzodiazepines.

I had a butalbital prescription for many years (ending in the version without caffeine) and, to be honest, it got kind of old. I find lorazepam to be more effective for anxiety

I am not as much of a fan of benzo's.. but I agree, they do seem to have superior efficacy in treating acute anxiety than barbiturates (unless one would be using an ultra-short acting barbiturate, like the yummy barbiturate-cocktails in lethal injections)

On a side note, mixing butalbital (or any barb) with alcohol is an extremely dangerous idea. The dose-response curve is extremely steep and its very easy to take it way too far. I almost ended up in the emergency room because of a butalbital+alcohol overdose a few years back.

I can definitely attest to this. At least, increasing the effects of alcohol. I'm not a huge drinker, but on this particular occasion I had about 3-4 drinks before bed.. fell asleep with little to no difference; perhaps a bit more light-headed than usual. Then around 4 hours later I woke up vomiting EVERYWHERE uncontrollably. Never has this happened to me. During my past drug use history (which WAS quite extensive)--NEVER have I been unable to hold it in till I get to the toilet.. until this happened. The only thing different I did was consume alcohol, so I assume it was this interaction..?


And NeighborhoodThreat:
I am just curious, what was your typical dose of butalbital? How long were you on it? and what was your highest total daily dosage? Did you wean off? Or transition to another GABAergic? (And if so, to what drug did you transition, at what dose & how successful was this transition in regards to experiencing any withdrawal symptoms--and if you did experience withdrawal, be specific as to the duration & effects of them)? Also, your experience w/ baclofen, did you ever use it concurrently with butalbital or no?

 

[Thorns Have Roses]

Hmm, a quick look shows that mercury poisoning potentiates barbs. But uh, I wouldn't recommend doing this obviously.
http://www.mendeley.com/research/barbiturate-potentiation-mercury-poisoning/

Using PKC activators such as the one listed here has been shown to potentiate them (as well as encourage tumor growth):
http://onlinelibrary.wiley.com/doi/10.1111/j.1471-4159.1993.tb13432.x/abstract

Resperine (used to treat high blood pressure, also some indications in psychiatry) increases the hypnotic effects of barbs.
http://ebm.rsmjournals.com/content/97/1/83.abstract


Overall though, I think the recreational potential of butalbital is limited, and might best be used in low doses as a potentiator of benzos you may enjoy (blah blah it's dangerous and stuff). Or get better barbs (unlikely).

 

[AlphaOdure]

Hmm, a quick look shows that mercury poisoning potentiates barbs. But uh, I wouldn't recommend doing this obviously.

LOL... yea, i'll pass on the mercury poisoning... although i'm sure its symptoms are nothing compared to the absolute HELL that is barbiturate withdrawal

But thanks for the abstract.. it was an interesting read; would be even more interesting to read the whole research article & its findings!


Side Note:
Maybe this will turn into a "big and dandy" butalbital thread? I think its definitely needed, IMO- since butalbital is a somewhat commonly prescribed drug (at least here in the states) -- plus it is easily accessible illicitly online, so I am sure there are MANY users out there. So one would think such a resource of information should exist? And at that, one would think such a resource would be beneficial? Especially in the absence of any significant online references to butalbital's pharmacodynamics, aside from obscure abstracts here & there (which are interesting, don't get me wrong, but they're not very rigorous in divulging the mechanics of the drug, but more so assessing odd observances--such as mercury potentiating barbiturates ..It seems like some of these "studies" probably originated from case-studies or observations by ER nurses, & then pharmacologists, neurologists, & chemists w/ too much free time on their hands decided to pick up on it; b/c i'm sure there are pharmacists & chemists out there who've gotten bored w/ creating gobs and gobs of different kinds of boner pills).

 

[cj]

I really enjoyed floricet got to try it about a month ago. I ended up taking 4 of the pills I dont remember the mgs though I know it had caffiene and tylenol in it. Not a bad high much better than xanax IMO.

 

[AlphaOdure]

And thanks for the extra articles you added to your post NNB.. its unfortunate most of the drugs referenced are either very rare or Rx only though--but then again, what do you expect in an FDA-and-DEA-happy U, S, of A... eh? They are still very interesting reads nonetheless & something to keep in mind if I come across any of these aforementioned drugs in the future.

And yes, highly.. HIGHLY unlikely i'll get my hands on a better barbiturate (or more appropriately worded, a "shorter acting barbiturate" rather).

But again, although increasing it's euphoric & therapeutic effects would be nice... I have the long term intention (or goal? maybe?) of attempting to slowly wean & reduce my dose to sane levels (especially when 300mg is the daily maximum indicated dose and i'm taking as much as 1800 mg daily). However, increasing the psychoactivity, affinity, and/or subjective effects of the drug I assume would greatly aide in weaning & doses reduction, or at least making it less painful!

But I do find it pleasurable! It just seems that once butalbital builds up in your system, it is very hard to "breakthrough" and get those effects akin to when I first took it (or after extended abstinence, at least >36 hours). Mind you I was not dependent upon benzos when i started butalbital; although I was taking 7000mg-8750mg of carisoprodol daily previously, & I literally had to start out at 1250mg of butalbital per day after transitioning... to keep from losing my mind! (so I guess the distinction between "benzo naivety" & my ridiculous levels of carisoprodol use is arbitrary, especially since I could take upwards of 2-3mg of alprazolam at a time during periods when carisoprodol was inaccessible, yet to any observer I seemed completely sober, sane, and normal. So there is definitely some cross tolerance between anxiolytic carbamates & benzodiazepines)!

Back to the point- Even when taking 250% (or 2.5 times) of my usual dose, I don't get much increase in effects (BTW- do not try this at home kiddies. I'm probably lucky i'm still alive for doing something so fucking dumb)--as NeighborhoodThreat previously posted, butalbital does get "old." I don't know if this is just an integral part of the GABAergic system, or if butalbital has some inherent partial agonist/antagonist properties, b/c it reminds me of a CNS-depressant version of buprenorphine but w/ worse propensity for increasing tolerance! (Which reminds me- I read some interesting articles way-back-when: due to barbiturate's generalized effect on the GABAergic system some of it's neurological interactions had antagonistic side-effects--since there are SO many sub-receptors in the GABAergic system; some of which create neuro-excitation when agonized, such as the case with glutamate receptors, or conversely the opposite effect of inhibition & anxiolysis would be the case when actual GABA receptors are agonized. So this could contribute to the feeling of butalbital feeling "old". I'll have to try and find that article)

Crimsonjunk- if you're in the United States; then it was 50 mg per pill. This is the only dose butalbital is made in. For some reason most barbiturates are made this way- with only one dose level. Unlike alprazolam where you can find anywhere from 0.25mg to 2mg per pill; same w/ modern opioid analgesics! Just look at buprenorphine, it is available in formulations in the microgram range when indicated for pain; but is available at levels of 8 mg for dependency treatment.. Oh well, the set-doses of barbiturates reflect the outdated medical practices of their day I suppose.

SIDE NOTE-
It looks like the formulation "Fioricet" (containing butalbital+acetaminophen+caffeine) has the tendency to be HIGHLY hepatotoxic via several modes. First, the inductive effect barbiturates have on the CYP450 liver enzyme system severely increases the amount of acetaminophen metabolized into N-acetyl-p-benzoquinoneimine (i.e., the metabolite mainly responsible for acetaminophen poisoning & it's subsequent liver damage). In otherwise normal circumstances, metabolization of acetaminophen into N-acetyl-p-benzoquinoneimine is minimal, w/ only a 5% metabolic rate.

THEN, according to one study, we have CAFFEINE. if it is taken concurrently with acetaminophen, it can triple the levels of the toxic N-acetyl-p-benzoquinoneimine metabolite (all of this, mind you, is according to Wikipedia & i haven't had a chance to confirm the references in the article).

Wow, I feel so relieved our pharmaceutical companies & our public policies governing big PHARMA (here in the US, at least) have our best interest at heart! ...Combining two chemicals which severely increase hepatotoxicity, decreasing the lethal dose from 10g of acetaminophen to as low as 3g (by my math).. It just makes total sense- they'd rather you just die than (god forbid) you "abuse" a drug and/or use it at doses higher than indicated (especially if your doctor wont listen to you)! I am ranting on this b/c I also take the fioricet formula acquired via online pharmacies since butalbital is not controlled/scheduled if sold with caffeine AND acetaminophen--which makes such a formulation seem even more sadistic! But anyway, I am prescribed 50 mg of just butalbital by my brick-and-mortar doctor: 180 pills three times a month. With the tolerance I mentioned above & my daily intake, you do the math; it doesn't last long--hence the reason for starting this thread! I'd rather not depend upon online pharmacies )

http://en.wikipedia.org/wiki/Acetaminophen_toxicity#Pathophysiology

 

[NeighborhoodThreat]

That seems about right. Baclofen is selective to GABA-b; benzo's to GABA-a ... where as barbiturates modulate all of them; so i could see it being "closer" to butalbital than to benzodiazepines.


I am not as much of a fan of benzo's.. but I agree, they do seem to have superior efficacy in treating acute anxiety than barbiturates (unless one would be using an ultra-short acting barbiturate, like the yummy barbiturate-cocktails in lethal injections)


I can definitely attest to this. At least, increasing the effects of alcohol. I'm not a huge drinker, but on this particular occasion I had about 3-4 drinks before bed.. fell asleep with little to no difference; perhaps a bit more light-headed than usual. Then around 4 hours later I woke up vomiting EVERYWHERE uncontrollably. Never has this happened to me. During my past drug use history (which WAS quite extensive)--NEVER have I been unable to hold it in till I get to the toilet.. until this happened. The only thing different I did was consume alcohol, so I assume it was this interaction..?


And NeighborhoodThreat:
I am just curious, what was your typical dose of butalbital? How long were you on it? and what was your highest total daily dosage? Did you wean off? Or transition to another GABAergic? (And if so, to what drug did you transition, at what dose & how successful was this transition in regards to experiencing any withdrawal symptoms--and if you did experience withdrawal, be specific as to the duration & effects of them)? Also, your experience w/ baclofen, did you ever use it concurrently with butalbital or no?

My typical dose ranged from 50-200mg. Butalbital is a medium-acting barbiturate so taking 100mg one day and then taking 50mg the next day...can have an additive effect. I don't remember the half-life off the top of my head but I know its longer than 24 hours. Certainly something to keep in mind.

I never weened off it, although I never used it for more than 2-3 days in a row. I was prescribed it for migraine headaches and since it didn't really work too well for that purpose I kept it as an "emergency kit" to come down off amphetamines, caffeine, etc. I also didn't use it very often because of its steep dose-response curve when mixed with alcohol. I know this has already been said but...don't mix this stuff with alcohol.

I never used baclofen with butalbital - in fact I haven't used butalbital in years and I just recently was able to try baclofen. There certainly was a similar feeling to the two of them that is hard to put my finger on...as you mentioned it could be due to baclofen's GABA-B activity...and the fact that I was used to benzodiazepines, particularly clonazepam, lorazepam and diazepam.

I never experienced withdrawals because I didn't use it for a long time. I have heard of people getting addicted to butalbital and developing pretty nasty withdrawal symptoms. Similar to ethyl alcohol withdrawal.

Hope this helps

 

[AlphaOdure]

Butalbital is a medium-acting barbiturate...I don't remember the half-life off the top of my head but I know its longer than 24 hours.

Yea, it is a short-to-intermediate acting barbiturate. From what i've read, its half-life is between 25-35 hours. Although, from my experience its psychoactivity peaks relatively quickly; w/ realization of effects starting at around ~15 minutes after oral ingestion, peaking around the 0.5-1.5 hour point, & after 4 hours its psychological effects are largely unnoticeable (however, in regards to the former two statements: intentional cumulative dosing/stacking & its use in GABAergic naive individuals can extend both the peak & overall length of psychological effects). Some people like to compare it to phenobarbital; but i'd say they're not even in the same ballpark (pheno's half life can last as long as 120 hours! & is thus an ultra-long-acting barbiturate) -- Phenobarbital is absolutely worthless for psychoactive and/or immediate anxiolytic purposes, IME. No how matter how much you try to take, you wont get an increased GABAergic effect other than intense sedation.

so taking 100mg one day and then taking 50mg the next day...can have an additive effect...Certainly something to keep in mind.

Definitely agree! In the morning I usually get less of an effect at my normal dosage (200mg-250mg) -- but when dosing in the evening (at the same levels, mind you) I get severely increased effects! I also get severely increased effects with a booster dose of about 100mg-200mg after ~0.5-1 hour(s) after ingestion.

However, keep in mind: a drug's half-life sometimes has little to do w/ its psychotropic duration of action and/or effects, especially if the relative substance has active metabolites which partially contribute to and/or are entirely responsible for its pharmacodynamics (which we don't know if this is the case w/ butalbital.. since this is the primary reason why I started this thread! heh- although i'd like to a see a discussion such as this anyway since there are very little comprehensive resources for butalbital use, even on bluelight).

But if a substance isn't a prodrug for an active metabolite--such as heroin (morphine) or carisoprodol (meprobamate) as alternate examples--I've found that the duration of psychological effects are generally 10%-15% that of the relative drug's half-life (i.e.- this would be 3-4 hours for butalbital, if you average it's half life to be 30 hours). Of course, the duration of action for psychoactivity is even shorter for those who are abusing a drug and/or if they're actively pushing their tolerance. B/c when I was abusing butalbital (I'd like to say i'm more or less "stabilized" on 1500 mg/d nowadays) the noticeable effects lasted about 1.5 hours at first dose; w/ roughly 2-3 hours of noticeable effects after cumulative dosing in the evening after dosing throughout the day (My typical intake is 5-6x a day, not including occasional "boosting").

 

[AlphaOdure]

I never experienced withdrawals because I didn't use it for a long time. I have heard of people getting addicted to butalbital and developing pretty nasty withdrawal symptoms. Similar to ethyl alcohol withdrawal.

I have; and it was pretty nasty. Worse than both heroin and methadone withdrawal; although i've never experienced benzodiazepine withdrawal. I'm sure the high doses I was taking (>2000 mg/d) contributed though. It was especially excruciating- although some physical symptoms opiates-are-renowned for were absent (i.e., sweating, vomiting, the "skin crawling" feeling). But butalbital withdrawal did include anorexic effects far more intense than opioid related withdrawal symptoms; in addition to nausea. The psychological effects (which I would personally classify as "physical" symptoms) were debilitating and included: anxiety, auditory & visual hallucinations, insomnia & an utter lack of physical need for sleep, convulsions (although I only noticed this upon waking from sleep--when I could sleep that is. But I never did experience seizures), extreme mental confusion, extreme paranoia, akathisia, dystonia (involuntary muscle movements or "tics"), dysphoria, paresthesia (particularly "electric shock" feelings & muscle restlessness)and delusions/delusional thinking. I experienced withdrawal for five days until I was able to afford my refill. Anorexic, nauseousness, insomnia, & paranoid symptoms became apparent after about 10 hours, with an ultimate peak at around 72 hours (3 days) after cessation of use. Afterwards, most of these symptoms seemed to slowly decrease.

However, I did not gut out the full withdrawal period; and I have read literature stating that acute withdrawal syndrome from immediate barbiturate cessation lasts for 9-30 days. And withdrawal supposedly also includes two "stages", the second of which purportedly includes increased psychological, hallucinogenic, & excitotoxic effects. While I did notice a decrease in most of the symptoms at around the 4th day; the delusional and hallucinogenic symptoms seemed to persist--if not slowly increase in their intensity throughout the experience. Additionally, substantial an increase in involuntary/automatic akathisia & dystonia were noticed (i.e., "tics" or "twitches") w/o any sort of reduction, as well as increased paresthetic symptoms. Also, the slight decrease in anxiety may have been psychosomatic as I was literally counting down the hours to refill my prescription.

(anyone who is thinking of trying this drug; or who is offered it by their doctor- I recommend to not even risk it if you are a recovering addict. The potential downsides of dependency far outweighs any of this substance's benefits!)

 

[AlphaOdure]

so taking 100mg one day and then taking 50mg the next day...can have an additive effect...Certainly something to keep in mind.

I know you stated you never used butalbital more than two to three days consecutively; but did you experience decreased GABAergic effects after additional doses on your final doses on the second or third day? B/c I have noticed this; although I take this substance every day. The only time I really get significant psychoactivity is when: 1) I take butalbital after extended withdrawal (i.e., after intake cessation for at least 72 hours); 2) Additionally & oddly enough, I've noticed increased effects after reducing--or weaning--my dose (which i've been trying to do lately, i've decreased my ingestion by 100-200 mg/d within the last 5-10 days.. w/ a previous daily dose of 1500 mg at the minimum); and 3) When I only sparingly boost my dose I achieve more psychological & medicinal effects (i've particularly noticed increased psychotropic effects w/ boosting after lowering my daily regime. However, boosting seems to only be effective if done every two-three days. Boosting more often than this only increases tolerance and does not significantly increase psychoactivity, in my experience at least).

Perhaps there is a blockade effect w/ this drug, similar to how methadone acts on OPOIOIDergic receptors at higher doses? I doubt it has selective affinity b/c of its significant synergy w/ other GABAergics--something one doesn't see w/ selective OPIOIDergics which also possess high receptor affinity like buprenorphine (a drug with absolutely no synergy w/ other opioids when used in doses <0.5mg);

Anyway, I'm just interested in your opinion, and/or any experiences if applicable.