Barbituates: Gone for good in America?

[tmr123]

I remember when I was in high school I used to see Fiorinal(sp?) and Fioricet in medicine cabinets. Those contained butalbital if I'm not mistaken, an intermediate acting barbiturate. I have never in my life (born early 80's) seen Seconal, Nembutal, Tuinal, and have only seen phenobarbital prescribed to a dog, and not since high school have I seen a single barb anywhere ever. What happened? Are Barbs CI now? Are they still prescribed AT ALL? Do things like Phenilin + codeine still exist for headache remedies? Even Fioricet?? Would love to discuss...

 

[Dystopia35]

They do still prescribe fioricet for headaches. I actually took 2 tonight. They also have the fioricet with codeine. This and fiorinal are the only ones I have seen. Like I said usually prescribe for headaches.

 

[Kittycat5]

Butalbital containg medicines are still quite commonly used for various headache conditions, but recently have fallen out of style for various reasons. Phenobarbital is still used fairly frequently for seizure disorders, but again, new antiepileptics have somewhat limited its use because they are generally better tolerated. Seconal, while on the market, is really reserved for cases of refactory insomnia and is crazy expensive. Think there are a few more out there, but barbiturates have basically become second line drugs.

 

[paranoid android]

You can still get Butalbital (the Barb in Fiorinal/Fioricet along with generics like Trianal) and Phenobarbital the latter of which is mostly used for Epilepsy and also sometimes alcohol withdrawals, very rarely for benzo wd's and also sometimes for insomnia. Primidone is also still on the market as a anti-Convulsant but the primary active metabolite of that is Phenobarbital so it should have much the same effects. You can still get the Fiorinal-C's here in Canada atleast which have the codeine in them.

Even though they aren't as strong as Nembutal or Seconal but they can still deep 6 you if your not careful with them.

 

[tmr123]

Yeah I've heard all the stories from "the good ol' days" with Tuinals and Seconals and Quaaludes, I also know of another called Phenilin + Codeine which I believe is butalbital. I know that Benzodiazepines have largely replaced them on the anticonvulsant and sedative market (at least sedative anxiety treatment.) Is the abuse potential THAT high that they're not handed out, or is it that it's just too easy to die when taking them? Are there any doctors in the crowd who can comment about prescribing them? I'M NOT SEEKING THEM, MODS!!! NOT A SOLICITATION!!!! I'm curious about prescription rates in the United States, and cannot find the data online, so I was curious to sample the doctors on this board and see if they've ever prescribed seconal or nembutal since AFTER the 70's or 80's.

 

[Nom de Plume]

Barbiturates have almost exclusively become outmoded by the availability of the much safer and more innocuous (in terms of the therapeutic index or the gradient of a drug's dose-response curve) benzodiazepines and nonbenzodiazepines. Since the 1970s, benzodiazepines and the quondam quinazolinones, like methaqualone (a.k.a., Quaaludes), have been used as a stopgap when barbiturates—many of which have greater or equal abuse potential, are more or equipollently reinforcing, and are less forgiving of inadvertent overdoses—are deemed too unsafe to warrant their use in a given patient or for a specific medical condition.

Of course, while a drug may be made illegal or is only rarely prescribed anymore, it's only ever completely and incorrigibly extinct or unresuscitable if the impetus for and knowledge of its synthesis is extinct or lacking. Otherwise, any rarely prescribed or stringently proscribed drug is only ever as dead as the drug market and drug dealers allow it to be.

 

[Kittycat5]

Yeah I've heard all the stories from "the good ol' days" with Tuinals and Seconals and Quaaludes, I also know of another called Phenilin + Codeine which I believe is butalbital. I know that Benzodiazepines have largely replaced them on the anticonvulsant and sedative market (at least sedative anxiety treatment.) Is the abuse potential THAT high that they're not handed out, or is it that it's just too easy to die when taking them? Are there any doctors in the crowd who can comment about prescribing them? I'M NOT SEEKING THEM, MODS!!! NOT A SOLICITATION!!!! I'm curious about prescription rates in the United States, and cannot find the data online, so I was curious to sample the doctors on this board and see if they've ever prescribed seconal or nembutal since AFTER the 70's or 80's.

Im not a doctor, but a pharmacist. In 19 years, Ive filled two prescriptions for Seconal and I have almost always practiced in high volume stores. Fioricet and the like have been a mainstay of headache therapy for years, but recently due to concerns of abuse and misuse as well as the preperations leading to Medication Overuse Headache more commonly than others, rx rates have fallen.

I dont believe the potential for abuse is any greater than benzos, just the risk of overdose is much higher so they basically are never used for anxiety any more.

 

[tmr123]

Im not a doctor, but a pharmacist. In 19 years, Ive filled two prescriptions for Seconal and I have almost always practiced in high volume stores. Fioricet and the like have been a mainstay of headache therapy for years, but recently due to concerns of abuse and misuse as well as the preperations leading to Medication Overuse Headache more commonly than others, rx rates have fallen.

I dont believe the potential for abuse is any greater than benzos, just the risk of overdose is much higher so they basically are never used for anxiety any more.

By the way thanks everyone on this thread for replying, all great info. Jeeze, really Kittycat5? Two Seconal Rx's in 19 years. That's practically an extinct drug. If they're not used as anxiolytics, is their main remaining function headache relief, or are they ever prescribed specifically for sedation?

 

[Jktm]

I got an Rx of #40 Bupap tablets (Butalbital/Paracetamol - 50mg/300 - no cafeine) from an urgent care clinic last week. I take 3 preventative migraine medications (Propranolol 80mg BID, Topiramate 50mg Q-HS, and Memantine HCl 10mg Q-HS); hence the east at which I can get PRN Rx's of Butalbital.

They've reduced prescribing of Butalbital for a number of reasons - one of them being that they've discontinued production of The DEA exempt formula of Fioricet (the ones containing 325mg of Paracetamol); they are still available, but only until pharmaceutical companies run out of their supply.

Butalbital isn't as strong as the short acting barbiturates, but you can't fuck around with it like you can benzodiazepines (unless your tolerance is as God awful as mine). Last time I blacked out involved a gram of Butalbital (the day after taking a gram; 35 hour half-life), 2mg of IV Lorazepam, and 180mg of Diphenoxylate HCl. Don't be stupid and do this type of shit. And especially don't combine benzodiazepines and barbiturates, unless you know without a doubt you can handle it (I've been Rx'd 6mg of Alprazolam, 1050mg Carisoprodol, 4mg Estazolam, 300mg Butalbital, and 450mg Pregabalin daily in the past - and that was just my GABA drugs).

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Barbiturates increase the duration that the Chloride ion channels (Chloride ions entering the cell tbrough the post-synaptic receptor is what causes the inhibitory (sedative/hypnotic) effects of GABA) are open which will increase the efficacy (or maximum effect of) GABA (larger influxes of Chloride ions). Benzodiazepines increase the frequency in which these channels open, thereby increasing the potency of GABA (more frequent influxes of Chloride ions). Benzodiazepines and Barbiturates also bind at separate sites of the GABA receptor so they aren't competitive with each other. This means they'll have additive effects. Also, Barbiturates increase the affinity of the Benzodiazepine receptor site leading to exaggerated effects of Benzodiazepines (if a Barbiturate increases duration of opening by 5x and a Benzodiazepine increases the frequency of opening 3x, then overall functioning of the channel is increased by 15 - fold as opposed to 8-fold.

Another danger with Barbiturates is that they inhibit AMPA activity (an excitatory neurotransmitter) which increases inhibition. At high doses, Barbiturates also inhibit the functioning of Calcium ion channels.
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Stronger Barbiturates just aren't used hardly at all anymore because benzodiazepines are the safer alternative. Seconal (generic : Secobarbital Sodium) (red), Amytal (Amobarbital Sodium) (blue) (more rare in capsulated form), and Nembutal (Pentobarbital Sodium) (yellow) are still available, but rarely used. Tuinal (red and blue) (a combination of Seconal and Amytal in one capsule) was taken off the market by the makers of it due to decreases in prescribing. Though I'm sure it could be compounded for a steep price. These and the ultra - short acting (e.g. Sodium Thiopental) Barbiturates will usually only be used for pre - op sedation. The short acting ones are used for debilitating insomnia, but it's gotta be pretty fucking bad to merit these drugs. The only other use for them are for euthanasia of terminally - ill patients where doctor assisted suicide is legal (like Oregon).

 

[Kittycat5]

Other than Seconal, there are a few that may be used for sedation prior to anesthesia (amobarbital comes to mind) but their use once again is very limited. I imagine only if a patient cannot tolerate other sedatives like benzos or propofol would they be used but I prcatice in a community setting and have little experience with this.

Their only remaining uses really are for headaches as you said and phenobarbital for seizures, but even PB is usually only used as an add-on to other therapies. They are, for all intents and purposes a critically endangered species of drug.

 

[paranoid android]

Yeah I've heard all the stories from "the good ol' days" with Tuinals and Seconals and Quaaludes, I also know of another called Phenilin + Codeine which I believe is butalbital. I know that Benzodiazepines have largely replaced them on the anticonvulsant and sedative market (at least sedative anxiety treatment.) Is the abuse potential THAT high that they're not handed out, or is it that it's just too easy to die when taking them? Are there any doctors in the crowd who can comment about prescribing them? I'M NOT SEEKING THEM, MODS!!! NOT A SOLICITATION!!!! I'm curious about prescription rates in the United States, and cannot find the data online, so I was curious to sample the doctors on this board and see if they've ever prescribed seconal or nembutal since AFTER the 70's or 80's.

The fact that Barbs except for Phenobarbital and Butalbital are rarely used these days or even available on the North American market has more to do with how dangerous they where as opposed to abuse potential. Though from what i have heard fast acting Barbiturates like Seconal, Nembutal and Tuinal (secobarbital and amobarbital in one pill) have much more abuse potential then most benzos which granted is not saying much. But unlike benzos where as long as you aren't mixing them with other CNS depressants you would basically choke on the pills before you ODed and died it didn't take very many Seconal or Tuinal to kill you. And the last thing you want to be giving to a possibly suicidal patient is something that could easily kill them. Old school fast acting Barbiturates such as Seconal and Nembutal where possibly the last group of drugs on the market that could kill you quickly, had no specific anti-dote unlike Benzodiazepines which you can counteract with Flumazenil and was supposed to be a easy way to die. Though how could anyone know as it's not like dead people can complain . Also Methaqualone aka Quaalude's although they acted in much the same way as Barbs was not a Barbiturate. Though it was just as deadly and addictive if not more so.

So yeah the whole death thing combined with the fact that benzos do most of the same things Barbs do except they are much safer is the reason all but a very few Barbiturates are no longer used.

 

[Jktm]

Abuse has to do with it as well. Fast acting Barbiturates are C-II or C-III, which is a big step up from C-IV. Yeah, Butalbital is C-III, but it doesn't behave the same way, has a slightly longer half - life (only slightly longer, probably the reason for the C-III regulation (which mean fuck all for living in Canada - ya, I remember you, from TC, how you been (I'm Doug ). Barbiturates also inhibit a glutamate receptor (AMPA, but that doesn't matter) which illicit a Sodium ion influx which is excitatory for the cell as opposed to inhibitory, as well as blocks Calcium ion influxes at high doses, which also has an excitatory effect. Barbiturates also antagonize NMDA receptors and have anti-cholinergic effects - Nicotinic or Musacarinic, I'm not sure - I'd have to do more research - leading to increased intoxication; thus, leading to a higher potential for abuse.

As I stated in my last post, Barbiturates increase the maximal effect of GABA, while Benzodiazepines increase its potency (more influxes of Chloride as opposed to LARGER influxes of Chloride ions, so a much larger effect happening every time the channel opens.

And while Benzodiazepines don't have much recreational potential to the healthy individual, to someone with severe anxiety issues/PTSD, they have very high abuse potential (from a pseudo - addict's perspective - one who abuses drugs to a clinical point). They're also HIGHLY dependence forming (I believe all Benzodiazepines and Barbiturates, as well as Carisoprodol should be classified as C-II in the US for dependence reasons) - much more so than opioid drugs do (in my opinion having detoxed from all of these on their own as well as simultaneously).

Edit: Barbiturates also have greater analgesic effects than Benzodiazepines.

 

[downerhead]

I'm RXd 8mg of Xanax daily.My psychiatrist knows this does not even make me the least bit drowsy and I'm a terrible insomniac who goes 3 days without sleep regularly.He knows I've been on a galaxy of ssri,snri,tricyclics,antipsychotics etc and have terrible side effects.The Xanax is for severe panic disorder and have been on benzos for years with no ill effects.Last visit he gave me a haldol /cogentin combo and terrible side effects again.It was to help my insomnia.My question is that if I run the idea of seconal,100mg at bedtime(which I've had before in the late 80s/early 90s with great success is it a feasible (could he,under US law)possibility that he would be allowed to RX them.I know they work and they don't react negatively with my benzos and percs.This is not a legal question but nothing else has ever worked as well for sleep and it's a pretty extreme case when you get about 8 hours or less of sleep per week.

 

[Jktm]

We can't tell you what a doctor might give you. I will say that in all likelihood, probably not. Barbiturates are usually Rx'd by pain management specialists and neurologists, and they probably won't Rx it because of your other meds. They do react negatively. Read my last two responses detailing the pharmacology of Barbiturates. Barbiturates combined with Benzodiazepine multiply the functionality illicited on the Chloride ion channels by GABA.

My neurologist wouldn't even Rx Butalbital when I was on an equivalent of 9 mg of Alprazolam as well as other GABAminergic drugs, including Carisoprodol, and Pregabalin in high doses, despite my respiratory and circulatory function, as well as my demeanor on them. Only when everything was being Rx'd by my PCP (internist) was I Rx'd all of it alongside my opioids. An anesthesiologist/neurologist MIGHT consider it, but only after an extensive sleep study with an EEG at the least. More than likely, you would have to be having 60-72 hours between sleep on a majority of nights. They'd probably try 30-60mg of Temazepam, 2-4 mg Estazolam, or .5-1mg Triazolam nightly first, though.

You'd also have to prove yourself in the sleep study by not sleeping while laying in bed and trying to sleep (the one I had, had a camera on me and had me take my home Rx's in front of them); and if they didn't give you the Benzodiazepines before the first night, they would probably give you that for the second try, and then you'd have to prove yourself a second night.

Dt'ing from one of those, let alone both at the doses you would be taking would be atrocious - not to mention asking for a tonic - clonic seizure. I've just gotten lucky in that respect.

This is coming from the guy that took 130mg Alprazolam in 1 night, didn't blackout, and only got 4.5 hours of sleep.

 

[downerhead]

Thanks for the timely reply.I guess my next best hope would be for Soma,which I had after a major surgery and used to get regularly back home.They make you drowsy if you take enough.Thanks again for your helpful reply,I appreciate it.

 

[Jktm]

No doctor will prescribe Soma (Carisoprodol) for insomnia. And at therapeutic doses, they aren't effective hynotics. Have you tried high dose Temazepam (Restoril) , Estazolam (ProSom), or Triazolam (Halcion)? I used to be on 4mg Estazolam (you will have to drop the brand name of it for most doctor's to recognizrecognize it, if they don't have to look it up anyway (it's kinda old school) - and it's ESTAzolam, not ETIzolam - very important. It has higher efficacy than Temazepam, which I've been on up to 45mg, and Triazolam, which I've had up to .5mg and has a longer half - life than both of these combined. While I was still only averaging 5 -6h of sleep (which is more than the 3-4 I average without anything); I fell asleep within 40 minutes after taking it sublingually (about 10-15 minutes after absorption, so 25-30 minutes really) as opposed to 60-120 minutes with nothing; and I was getting QUALITY sleep (I skip SWS (on it I still skipped SWS, but I woke up rested and refreshed, where as with nothing I wake feeling like I'm in a meth comedown).

They would probably start you at 2mg as that's supposed to be the max dos4, but if you start keeping a sleep journal detailing times you went to sleep/woke up and quality of sleep, they MIGHT increase the dose. If you sleep patterns are as bad as mine, you need a sleep study, regardless. I have no circadian rhytm; I just stay up 48-60h most nights and then get 8 -10h out of exhaustion that does nothing for me since I was taken off my benzos.

And just so you get a conversion idea, 2mg Estazolam is equal to 1.3333mg Alprazolam, but has a more hypnotic qualituband less of a sedative quality (more doing what it needs to and less fuck you up; sedatives are to calm, hypnotics are to make induce somnolence).

 

[Mardashian3]

I have been searching for a Pharmacist or Dr. because I have a question....I have had 2 cervical back surgeries resulting in 3 fusions. I was on Nucynta 100mg (4/day) plus Nucynta ER twice per day for 4 years. I began to need more because It stopped working. I was running out early and suffering for days before I could get a script filled. Anyway I am now gradually tapering off all of it and am actually not doing bad at all with withdrawls as of yet. I have daily headaches in the back of my head that radiates down my shoulders and arms. This will be for the rest of my life. My Dr. has now prescribed Fiorinal for the headaches. Is this going to work for me? In comparison to Fioricet, is this the better choice? Is there anything else I can try if this does not work? I am very happy to be getting off of all those narcotics because they were controlling my life honestly. Thank You in advance...Anyone in my position?? Would love to hear from you...

 

[T. Calderone]

^Fioricet contains 325 mg acetaminophen, 50 mg butalbital and 40 mg caffeine. Whereas, fiorinal is the same except has 325 mg aspirin instead of acetaminophen. They both worked pretty much the same for me. Hope you find some pain relief!

 

[J.Del]

Doriden (Glutethimide) and Codeine was the best stone on earth. Doriden was discontinued in '93 , most people started using H including myself, no comparison. The "hits" as they were known in my area of NJ were the greatest, long lasting Euphoria and pure bliss. I still dream about them to this day.