Benzos Abuse liability of Benzos (self-injection levels)

[kokaino]

This study here says that triazolam followed closely by temazepam had by far the highest levels of self-injection, produced the most drug seeking behavior and reinforcing behavior among a very wide variety of benzodiazepines. Euphoria was a common side effect with the administration of both triazolam and temazepam. Other benzos involved in the study are chlordiazepoxide, oxazepam, diazepam, alprazolam, flurazepam, midazolam, flunitrazepam, clonazepam, clorazepate, lorazepam, lormetazepam, quazepam, and others. This was a big study. They were also compared to the barbiturate pentobarbital (Nembutal), but Nembutal showed a higher self-administration and reinforcing behavior than any benzo.

It is a very very interesting study and it is definitely worth a read.

 

[tricomb]

I dont know if it's just me but that link is not working, I downloaded the PDF but my computer can't open it, it says "The file “0059-1.PDF” could not be opened because it is empty"

edit: nvm, it's working now.

 

[kokaino]

^ Okay, good!

 

[tricomb]

Thanks again, looks very interesting I am going to look at this later when I have more time.

So this study is from 1985, damn! Just look at that text/ink.

 

[xxxyyy]

as someone who injected benzos many times (mostly flunitrazepam) i can say that IV administration feels way better than any other ROA. i've not shot too many other benzos (only flurazepam) because of their insolubility in water. god i miss IV flunitrazepam.

 

[mrflowers00]

i'm not lookin' for a high per say with benzos just relief from the freakish anxiety attacks i suffer from on a daily basis

 

[xxxyyy]

i use em mostly for that purpose now too since i've abused them countles times and always got bad rebound symptoms

 

[tricomb]

i'm not lookin' for a high per say with benzos just relief from the freakish anxiety attacks i suffer from on a daily basis

If you're having bad panic attacks every single day then I think it's pretty safe to say that the benzodiazepines are hurting you more than they're helping you. They're preventing you from making personal growth towards overcoming your anxiety and the underlying conditions.

 

[kokaino]

as someone who injected benzos many times (mostly flunitrazepam) i can say that IV administration feels way better than any other ROA. i've not shot too many other benzos (only flurazepam) because of their insolubility in water. god i miss IV flunitrazepam.

Believe it or not, fllunitrazepam ranked quite a bit below both triazolam and temazepam in self-administration and reinforcing behavior. It was all IV - the salt they used for temazepam was "temazepam acetate".

 

[mrflowers00]

@tricomb i've overcome my normal anxiety i used to feel constant anxiety but even after conquering those demons i was left having random reasonless panic attacks

 

[xxxyyy]

yeah i can believe it. not so much with temazepam, as i'd rate that somewhere with zopiclone as a rec. drug, but a lot of people swear by it, although its abuse is not widespread in germany. flunitrazepam was the most widely prescribed benzo for a very long time, and with just about all addicts i talked about this their benzo of choice. like i said, my experience with IV bezos is pretty limited, mostly flunitrazepam (which i dissolved in ethanol), flurazepam, midazolam, diazepam and clorazepate, and of those clorazepate is clearly the least fun, flurazepam and midazolam are both nice but flunitrazepam is hands down the best. it's a practice i encoutered many, many times in my life, that flunitrazepam is intravenously injected with nothing but water as a solvent, and the common myth among junkies is that you have to suck the coating off of them before you can inject them. and off course no amount of reasoning about the solubility (or lack therof) changed any of that. i mean i don't think i have to point out how utterly and hilariously fucked up this 'story' is.

 

[hamwaggle]

I once injected chlordiazepoxide (librium) by dissolving 10 mg in 5ml of water in a very large syringe as I read that it's solubility is 2mg per ml. I made sure to hit a large vein and slowly injected it. Chlordiazepoxide in general is very weak and long acting but I was fairly surprised at the rush and high. I also ate 25mg before. Injecting benzodiazepines in general is a bad idea, unless it's flurazepam which is soluble at 500mg/ml, or unless you have medical grade solvents that usually include ethanol.

 

[xxxyyy]

eh, injecting ethanol is certainly not a good idea, especially not in conjunction with benzos. i was just stating what i used, propylene glycol would be a much better solvent, but i wasn't aware of that back then.

 

[cook]

Too bad the z-drugs werent studied with those benzos listed. Would have been intresting, I bet the injection administration of zolpidem would beat all the traditional benzos at least. Pentobarbital propably would still kick ass more.

 

[xxxyyy]

i've injected zolpidem, and it doesn't compare to benzos favorably in my experience.

 

[kokaino]

yeah i can believe it. not so much with temazepam, as i'd rate that somewhere with zopiclone as a rec. drug, but a lot of people swear by it, although its abuse is not widespread in germany. flunitrazepam was the most widely prescribed benzo for a very long time, and with just about all addicts i talked about this their benzo of choice. like i said, my experience with IV bezos is pretty limited, mostly flunitrazepam (which i dissolved in ethanol), flurazepam, midazolam, diazepam and clorazepate, and of those clorazepate is clearly the least fun, flurazepam and midazolam are both nice but flunitrazepam is hands down the best. it's a practice i encoutered many, many times in my life, that flunitrazepam is intravenously injected with nothing but water as a solvent, and the common myth among junkies is that you have to suck the coating off of them before you can inject them. and off course no amount of reasoning about the solubility (or lack therof) changed any of that. i mean i don't think i have to point out how utterly and hilariously fucked up this 'story' is.

The research study was very very thorough and extensive and flunitrazepam just didn't show the self-administration and reinforcing behavior that triazolam and temazepam did. The reason, according to the study is the pharmacokinetics of the drugs. Triazolam and temazepam, which ranked in that order for self-administration and reinforcing behavior had certain absorption, distribution, metabolism, and excretion (ADME) times and rates that made them more addictive than other benzos. Midazolam was third after temazepam. Flurazepam ranked very low along with oxazepam, chlordiazepoxide and a few other benzos. The study focused totally on psychological dependence liability not physical addiction potential. Physical dependence is most severe among intermediate hypnotics, while ultra-short acting and long acting hypnotics and anxiolytics took longer to produce dependence and produced a less severe physical dependence.

The benzos were matched against pentobarbital, cocaine, methohexital, ethanol, morphine, methaqualone, nalorphine and dextroamphetamine. Of the drugs tested, morphine had the highest self-administration rate followed by dextroamphetamine and then cocaine. Next came pentobarbital, methaqualone, ethanol, triazolam, temazepam, methohexital, nalorphine and then midazolam.

This is a quote from the study:

Two groups have assessed the ability of triazolam to sub- stitute for a barbiturate in barbiturate dependent animals. Yanagita [161.165] reported that triazolam 10.25 and 1.0 mg/kg, PO) suppressed withdrawal signs in rhesus monkeys normally maintained on barbital (75 mg/kg; PC): b.i.d.), Other benzodiazepines were also effective at suppressing barbital withdrawal signs [161]. However, not all sedative drugs studied with this procedure were able to suppress barbital withdrawal signs (e.g., benzoctamine and methaqua- lone [ IIM, 167]

I was very surprised that methaqualone didn't suppress barbiturate withdrawals.

This study below suggests that midazolam and temazepam completely suppress pentobarbital withdrawal.

The ability of temazepam and midazolam to substitute for pentobarbital and thus maintain the physical dependence state was used to assess the potential dependence liability of these two benzodiazepine compounds. Male Sprague-Dawley rats, weighing 175-200 g and having ad lib access to food and water, were determined to be dependent on pentobarbital following 12 days of continuous, intraperitoneal infusion of pentobarbital using an escalating drug infusion schedule. On day 13 (substitution phase) the pentobarbital was replaced with either temazepam, midazolam or vehicle and the rats were infused for an additional 24 hours. This was followed on Day 14 (withdrawal phase) by a 24 hr saline infusion period. Rats were observed for changes in overt behavior and alterations of body weight during both Day 13 and Day 14. Preliminary potency estimation studies had indicated that both drugs were more potent and longer acting than was pentobarbital. Temazepam, in doses of 32.5, 65 and 130 mg/kg/24 hr, was demonstrated to substitute for pentobarbital and provided dose-dependent suppression of overt behavioral signs indicative of withdrawal. Temazepam also suppressed the weight loss typically observed during withdrawal. Substitution of saline for temazepam resulted in an increased incidence of withdrawal signs and an approximate 10% decline in body weight. Midazolam, in doses of 60 and 120 mg/kg/24 hr, also substituted for pentobarbital and suppressed both overt behavior and weight loss. Following saline substitution on Day 14, a mild withdrawal syndrome was evident although body weight was noted to remain near control values.

Source

 

[xxxyyy]

i failed to specify something. flunitrazepam was never the most widely prescribed benzodiazepine, but rather hypnotic benzodiazepine. i believe diazepam was and probably still is the most widely prescribed benzodiazepine. but just to show the supply/demand thing, back when i regularly scored benzos on top of my scripts, 1mg rohypnol-brand flunitrazepam sold for four times as much as 10mg diazepam.
i think the reason i always preferred flunitrazepam to midazolam, although during my IV days i had access to both, is just that flunitrazepam has a longer duration, and that it was potentiated by the ethanol solution i manufactured, something i didn't have to do with midazolam.

 

[kokaino]

Diazepam is definitely the most widely prescribed benzo, especially in Europe. In the United States it is alprazolam (by far). Flunitrazepam is a very nice benzo and I enjoy it very much but it just doesn't have the pharmacokinetics that make it a serious benzo of abuse, unlike triazolam, temazepam or midazolam. However, I wonder how nimetazepam (nitrazepam, which is a similar drug ranked favorably) would've ranked if it was included in the study. I think the results of the study mirror the trend in human abuse of benzos. Triazolam was always a major benzo of abuse, same with temazepam - it obviously caused an epidemic of drug abuse and overdose deaths in Western Europe (especially the UK) and Australia and is among the top benzos abused across Asia, and midazolam is always popular. I speculate that nimetazepam would probably have outranked midazolam. It rules the benzo market across all of East Asia and Southeast Asia. I was surprised that lormetazepam didn't rank very high and lorazepam ranked relatively high. Alprazolam with all its hype ranked very low.

The study basically claims that elimination rate is a determinant of self-administration rates. Findings that triazolam and temazepam maintain higher levels of self-administration rates compared to other benzos, especially benzos which are more slowly eliminated or have active metabolites which are slowly eliminated in man (flunitrazepam is one of those benzos) is consistent with the results of a previous study which showed that midazolam maintained higher levels of intravenous self-injection than clonazepam, clorazepate, diazepam, flurazepam, and medazepam.

 

[xxxyyy]

yeah makes sense to me. the reason i never shot any other benzos is mainly because of their insolubility. flunitrazepam outranked all others as it was a. widely available, b. very potent and c. could be dissolved in ethanol, which most benzos are only sparingly soluble in. i was not saying that flunitrazepam is a more inherently abusable or addiction-inducing substance than temazepam or triazolam, it was just preferred by all benzo users i knew because of its wide availability compared to the benzos most common to the black market here, which are diazepam, and to a lesser degree, clonazepam and oxazepam. flunitrazepam, up until its reschedule last year, was the first-line hypnotic benzodiazepine, and is still widely used in an in-patient setting. when i went in for surgery earlier this year i was given flunitrazepam pre-op. it is, because it is quite notorious in germany, now in the same schedule as potent opioid analgesics and methylphenidate, which will have dropped sales and prescriptions considerably, similar how temazepam was rescheduled in countries where its abuse was widespread.
edit: i think alprazolam is the most useful of anxiolytic benzodiazepines, however, as a recreational drug, i'd probably prefer the short/intermediate acting hypnotics to it.

 

[kokaino]

^ You are right. It is generally the way it goes with benzos - the most widely prescribed benzo will be the one that is most widely abused. In the US, alprazolam is the most widely prescribed and is thus most widely available on the streets. The only exception to this was temazepam where prescriptions for the drug were cut by a considerable margin in the UK and Australia, but pharmacy robberies and prescription forgeries for temazepam became a huge problem, especially in Australia.

Here for example:

Forgery or alteration of prescriptions have been used to obtain benzodiazepines, particularly temazepam capsules (Dobbin 1998; Dobbin et al. 2003). Dobbin et al. (2003) found that in the six months to end of May 2001 there were 185 forged prescriptions reported. Benzodiazepines accounted for 135 (74% ) of these items, and temazepam accounted for 85% of all benzodiazepines. There were no alterations or forgeries for tablets, and all forgeries nominating a dose form were for capsules, indicating an overwhelming preference for capsules. Dobbin (2001) reported how, in one forgery case, a brother and sister presented more than 300 forged prescriptions in the 3 months to the end of February 2001 at 77 different pharmacies using 30 different aliases. Pharmacies involved ranged across Melbourne. Forgeries were written on stolen Benzodiazepine and pharmaceutical opioid misuse and their relationship to crime prescription stationery, some of which were stolen during burglaries. A possible additional 385 prescriptions remain undetected. More recently, a number of computer-generated forgeries have been detected for Normison 20mg capsules x 50 (Dobbin 2001).

Nearly all participants had used prescribed benzodiazepines at some time (93% ), with 39% having injected them. Most (97% ) had also used illicit benzodiazepines at some stage, and 69.5% reported they had injected these drugs. No respondents reported that benzodiazepines were the drugs they had initially injected, with only one percent indicating they had injected them most in the previous month. Four percent ranked these drugs as their most favoured, with temazepam named as the favoured form.

Source