Citat:
Förlåt om jag verkar ignorant. Har inte följt tråden eller diskussionen.. men har har du farmakologisk, farmakinetisk eller farmakodynamiska studier avklarade bakom dig?
Vet inte helt om du kan uttala dig så bestämt om dina påstående eom halveringstid och resten av de som rör riktigt farmaceutisk vetenskap.
Frågar bara. Skäller inte
Vet inte helt om du kan uttala dig så bestämt om dina påstående eom halveringstid och resten av de som rör riktigt farmaceutisk vetenskap.
Frågar bara. Skäller inte
Hej på dig! Jag uttryckte mig nog dåligt, var lite snurrig text det där. Halveringstiden är det ju ingen som vet helt klart men teorierna rör sig om 40-250 timmar och då försökte jag göra en grovt luddig uträkning med den kalkylatorn med dessa teoretiska påståenden eller vad du nu vill kalla det. Omöjligt att veta ändå helt exakt.
Här nedan skall jag posta lite teorier/fakta om man nu kan kalla det så, snarare erfarenheter. Och inget av detta behöver nödvändigtvis betyda att något är sant men jag har kollat upp i princip allt som går att läsa om det och jämfört runt etc. Ni som är intresserade kan ju ta en titt.
Källa: Wikipedia. Den lilla 'fakta' som nu finns.
N-Desalkylflurazepam (also known as Norflurazepam) is a benzodiazepine analog and an active metabolite of several other benzodiazepine drugs including flurazepam,[2] flutoprazepam,[3] fludiazepam,[4] midazolam,[5] quazepam,[6] and ethyl loflazepate.[7][8] It is long-acting, prone to accumulation, and binds unselectively to the various benzodiazepine receptor subtypes.[6] It has been sold as a designer drug from 2016 onward.
Synonymer:
N-1-Desalkylflurazepam
N-Desalkyl-2-oxoquazepam
N-Desalkylflunitrazepam
N-Desalkylflutoprazepam
7-Chloroflubromazepam
Dealkylflurazepam
Desalkylflurazepam
Descarbethoxyloflazepate
Norfludiazepam
Norflurazepam
Norflutoprazepam
Ro 5-3367
TL8002277
Synonymer:
N-1-Desalkylflurazepam
N-Desalkyl-2-oxoquazepam
N-Desalkylflunitrazepam
N-Desalkylflutoprazepam
7-Chloroflubromazepam
Dealkylflurazepam
Desalkylflurazepam
Descarbethoxyloflazepate
Norfludiazepam
Norflurazepam
Norflutoprazepam
Ro 5-3367
TL8002277
En teori/post. Källa: UKchemicalresearch.
FWIW - sadly I had begun to draft a well referenced post that got lost in the woodwork - those with an interest in N-desalkylflurazepam may find it interesting to look into what's published on the respective metabolites of quazepam and of flutoprazepam as well as of flurazepam. From some vast mishmash of the above, the following is more or less the sum of what came to light:
Half life seems to be more widely variable and longer on aggregate than has generally been suggested; I came across a diversity of estimates from 40-160h, but the average in young (i.e. working age) men was found to be around 74 hours (there are multiple estimates around this mark) and in women of similar age, around 90 hours. This is a statistical mean, and the size of the possible variance should not go unnoticed.
Both age and gender are relevant to clearance times, and whilst men show faster clearance times in their prime the decline with age is more marked; 'older' men (not defined by the source in question but 60+ or 65+ is a sensible assumption) had an average elimination HL of 160 hours, versus 120h in older women.
In concordance with the above, it accumulates rather rapidly; I found various estimates of time to steady state but among them, time to steady state of this metabolite from nightly administration of a stable dose was 4-7 days in a group of women aged 24-40, 7-10 days in a number of less specific trials. The maximal concentrations seen in plasma were around 5x-6x higher after 7 nights of consecutive dosing than they were on the first night.
Such an observation can be interpreted as 'good' or 'bad'; in the treatment of severe insomnia it has been observed that decreases in both sleep latency and total wake time increase cumulatively over the first 2-3 days of dosing, and persist for 1-2 days following the end of a short course of treatment.
Accumulation is related to tolerance and/or addiction but it is not a direct synonym; among the data on Toxnet flurazepam (of which this is the primary active metabolite) is claimed - use caution - to retain efficacy for a maximum of four weeks; that is, however, a sufficient timeframe for tolerance and physiological addiction to emerge, for withdrawal symptoms to present and for tapering to become advisable. Whilst we cannot and do not give medical advice, this is one substance where I'd be fairly happy to echo the general advice of the (rather restrictive) UK medical profession that benzodiazepenes should preferentially not be used for a period exceeding two weeks.
To sum up, my reading of God-knows-how-many sources leads me to the view that this is indeed a powerful, long acting and fast accumulating hypnotic, which seems to be the primary mechanism of action of both flurazepam and flutoprazepam, and a minor metabolite of quazepam which, while not the primary mode of action of the latter, accumulates in the same way such that 'within two weeks' consecutive use of quazepam, the accumulation of the present compound is responsible for the bulk of the effect and the non-selective binding of the present compound overtakes the (theoretically) BZ1-specific action of quazepam. One might conclude that the literature describes a strong and increasing efficacy in the short-term treatment of severe insomnia but that this emphasis is quite strongly necessary for this particular compound.
I would have particular concerns about the possible temptation towards sporadic use; subjectively speaking I would not disagree with those who suggested 5mg felt crudely comparable with diazepam or that 10mg is an effective hypnotic (indeed I would also concur with the notion of 10mg being broadly comparable with 16mg of flubromazepam), with faster uptake in line with the direct ingestion of a substance for which the aforementioned compounds serve in varying degrees as a prodrug.
It is suggested that these might very wisely be handled with the very same cautions (and the same observations for good or ill) as are already associated with flubromazepam. We have reports of comparably agreeable anxiolytic effects and of comparably agreeable hypnotic effects, which is not surprising - but when it comes with a comparable half-life and a comparable propensity for accumulation, it's rather apparent to me that very long clearance times would be needed between sporadic uses if accumulation is not to become a problem. And/or that accumulation over the short term could be seen as a positive benefit depending upon intention to treat, but that the sustainability of this (whether for anxiolytic or hypnotic use) can be expected to be rather poor.
The executive summary would be "fast acting flubromazepam", with the full complement both of potential positives and negatives that this implies and the observation that this seems subjectively as valid as in terms of qualitative experience as it does of that which can reasonably be foreseen from the data. It strikes me on the one hand as an extremely worthwhile addition to the RC scene, but also one about which, by now, we should perhaps be highlighting at least a gentle note of caution.
Half life seems to be more widely variable and longer on aggregate than has generally been suggested; I came across a diversity of estimates from 40-160h, but the average in young (i.e. working age) men was found to be around 74 hours (there are multiple estimates around this mark) and in women of similar age, around 90 hours. This is a statistical mean, and the size of the possible variance should not go unnoticed.
Both age and gender are relevant to clearance times, and whilst men show faster clearance times in their prime the decline with age is more marked; 'older' men (not defined by the source in question but 60+ or 65+ is a sensible assumption) had an average elimination HL of 160 hours, versus 120h in older women.
In concordance with the above, it accumulates rather rapidly; I found various estimates of time to steady state but among them, time to steady state of this metabolite from nightly administration of a stable dose was 4-7 days in a group of women aged 24-40, 7-10 days in a number of less specific trials. The maximal concentrations seen in plasma were around 5x-6x higher after 7 nights of consecutive dosing than they were on the first night.
Such an observation can be interpreted as 'good' or 'bad'; in the treatment of severe insomnia it has been observed that decreases in both sleep latency and total wake time increase cumulatively over the first 2-3 days of dosing, and persist for 1-2 days following the end of a short course of treatment.
Accumulation is related to tolerance and/or addiction but it is not a direct synonym; among the data on Toxnet flurazepam (of which this is the primary active metabolite) is claimed - use caution - to retain efficacy for a maximum of four weeks; that is, however, a sufficient timeframe for tolerance and physiological addiction to emerge, for withdrawal symptoms to present and for tapering to become advisable. Whilst we cannot and do not give medical advice, this is one substance where I'd be fairly happy to echo the general advice of the (rather restrictive) UK medical profession that benzodiazepenes should preferentially not be used for a period exceeding two weeks.
To sum up, my reading of God-knows-how-many sources leads me to the view that this is indeed a powerful, long acting and fast accumulating hypnotic, which seems to be the primary mechanism of action of both flurazepam and flutoprazepam, and a minor metabolite of quazepam which, while not the primary mode of action of the latter, accumulates in the same way such that 'within two weeks' consecutive use of quazepam, the accumulation of the present compound is responsible for the bulk of the effect and the non-selective binding of the present compound overtakes the (theoretically) BZ1-specific action of quazepam. One might conclude that the literature describes a strong and increasing efficacy in the short-term treatment of severe insomnia but that this emphasis is quite strongly necessary for this particular compound.
I would have particular concerns about the possible temptation towards sporadic use; subjectively speaking I would not disagree with those who suggested 5mg felt crudely comparable with diazepam or that 10mg is an effective hypnotic (indeed I would also concur with the notion of 10mg being broadly comparable with 16mg of flubromazepam), with faster uptake in line with the direct ingestion of a substance for which the aforementioned compounds serve in varying degrees as a prodrug.
It is suggested that these might very wisely be handled with the very same cautions (and the same observations for good or ill) as are already associated with flubromazepam. We have reports of comparably agreeable anxiolytic effects and of comparably agreeable hypnotic effects, which is not surprising - but when it comes with a comparable half-life and a comparable propensity for accumulation, it's rather apparent to me that very long clearance times would be needed between sporadic uses if accumulation is not to become a problem. And/or that accumulation over the short term could be seen as a positive benefit depending upon intention to treat, but that the sustainability of this (whether for anxiolytic or hypnotic use) can be expected to be rather poor.
The executive summary would be "fast acting flubromazepam", with the full complement both of potential positives and negatives that this implies and the observation that this seems subjectively as valid as in terms of qualitative experience as it does of that which can reasonably be foreseen from the data. It strikes me on the one hand as an extremely worthwhile addition to the RC scene, but also one about which, by now, we should perhaps be highlighting at least a gentle note of caution.
Kortfattat från Sciencedirect, inte helt relevant text men läsvärt:
Quazepam is readily absorbed following oral administration with peak plasma levels being reached in about 2 hours. It has a long half-life and also has the pharmacologically active metabolites, 2 oxo-quazepam, and N-desalkylflurazepam, with half-lives of 43 and 75 hours respectively Chung et al (1984), these metabolites accumulate with chronic use.
Blev för mycket text så kunde inte sätta sista i spoiler, det var från en lite udda hemsida men hade många källhänvisningar och kan vara intressant för den som orkar kolla upp. Det gällde jämförelser med denna och diazepam framförallt vad gällde sömnproblem och bieffekter.
Här är länk: http://journals.sagepub.com/doi/abs/10.1177/030006057900700512?journalCode=imra
Hittade ännu en länk/källa med samma rapport/innehåll: https://www.ncbi.nlm.nih.gov/pubmed/387494
Men om något av detta stämmer måste det betyda att den här har existerat längre på marknaden och kanske använts medicinskt i typ UK i så fall?
Jag känner mig så jävla engagerad i det här alltså. Dels tror och vet jag att detta är förmodligen den bästa RC-benson som kommit än så länge mot medicinskt bruk mot dom vanliga besvären så som sömn, ångest och oro. Jag hämtar nya idag fast 8mg istället, vart några kronor billigare samt att batchen kanske är annorlunda kan vara kul att se. Ska verkligen hålla fingrarna i styr och börja med 8mg, förhoppningen är att jag tar dem varannan dag eller om ens det, vid behov. Men så har man ju sagt förr..

Det roliga när jag försöker hitta lite diverse källor och erfarenheter om just detta preparatet så är ju 90% från Flashback. Grymma vi är ändå. Är det någon mer än jag som medicinerar med centralstimulantia och tar denna samtidigt? Första dagen fick jag känslan av att den slog ut den fullständigt och fick inte den där härliga balansen, det var ett litet minus från min sida. Men man kan ju inte få allt här i världen. Men ärligt kan någon påstå sig här fått ett rus av dessa? Jag har läst om några få som tagit typ 16mg och bara snubblat omkring och varit flöddriga. Jag kan ju berätta att efter jag käkat 120mg under 2 dygn så hade jag ett möte med en person som är en fd missbrukare och jobbar inom den vården och har många fräsiga utbildningar och denna person sa till mig att jag verkade må så mycket gladare, att det skiner om mig och att jag ser frisk och fräsch ut. Och gången innan vi träffades hade jag inte ens tagit något överhuvudtaget.
EDIT:
Nu börjar jag bajsa ord igen. Nej men undrar en kort sak. Det här med mintsmaken, vad är det för snack? Är det typ att kemikalien har en liten smak av mint eller är det snarare bindningsämnen? Dem blåa 4mg jag fick senast smakade lite mint när jag smälte dem under tungan och blå vart jag runt och i hela käften.
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Senast redigerad av 200kg 2017-06-27 kl. 10:58.
Senast redigerad av 200kg 2017-06-27 kl. 10:58.