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Mephedrone FAQ

We should add data on confirmed metabolites, their toxicity, and their relation to protracted, harmful vasoconstriction with prolonged use. Information on activity at various receptors and transporters will be speculative--the research has not yet been done.

ebola

There is finally some science done on it! I think I posted this in ADD, but I'll give it here too.

Abstract

Background and purpose: The designer drug 1-(4-methylphenyl)-2-methylaminopropan-1- one (4-methylmethcathinone, mephedrone) is reported to possess psychostimulant, entactogenic and hallucinogenic effects. The purpose of this study was to examine the effects of acute administration of mephedrone on extracellular levels of dopamine (DA) and serotonin (5-HT) in the nucleus accumbens of awake rats and compare these effects to those induced by 3,4-methylenedioxymethamphetamine (MDMA, ecstasy) and amphetamine.
Experimental approach: Microdialysis sampling was performed while simultaneously
recording locomotor activity in rats and the monoamines were determined by HPLC with electrochemical detection.
Key results: Mephedrone (3 mg.kg-1 s.c.) and (+)-amphetamine (1 mg.kg-1 s.c.) caused rapid increases in extracellular DA levels to 496% and 412%, respectively, whereas MDMA (3 mg.kg-1 s.c.) showed only a moderate effect (235. The corresponding 5-HT levels increased to 941% (mephedrone) and 911% (MDMA), but only to 165% following amphetamine. The calculated half-lives (t1/2) for elimination rate of mephedrone, MDMA and amphetamine-induced increases in extracellular DA levels were 25, 303 and 51 min, the corresponding t1/2 values for 5-HT were 26, 48 and 84 min, respectively.
Locomotor activation was highest for amphetamine, whereas both mephedrone and MDMA showed about three times lower and short-lasting effects.
Conclusions and implications: Mephedrone resembles the neurochemical and functional properties of MDMA, but also shows amphetamine-like effect on rapid release and elimination of DA in the brain reward system, a feature that may contribute to its potent reinforcing properties.
J. Kehra,b*, F. Ichinoseb, S. Yoshitakeb, M. Goinya,b, T. Sievertssonb, F. Nybergc and T. Yoshitakea. Mephedrone, compared to MDMA (ecstasy) and amphetamine, rapidly increases both dopamine and serotonin levels in nucleus accumbens of awake rats. British Journal of Pharmacology April 2011

And some analysis and what not....

So this shows that mephedrone produces peak levels in DA similar to amphetamine, and similar peak levels to MDMA in 5-HT.

From another person:
More peak dopamine release than amphetamine, more serotonin release than MDMA, and a half-life of less than 30 minutes?! Well I think we can see why mephedrone was such a runaway success
 
Okay. I'm going to try to modify this, with my additions integrated.

I had some spare time, so I wrote this draft:


Mephedrone FAQ


1. What is Mephedrone?
Mephedrone, 4-Methylmethcathinone, is a potent CNS stimulant and entactogen/empathogen. It's a potent releaser of dopamine, serotonin, and norepinephrine at typical doses. When reasonably pure, it appears as white powder or crystals, often with a pungent odor, as many ketones have. The compound originated in Israel around 2007.

2. How is it taken?
Mephedrone is generally swallowed and/or insufflated. A few people have taken the compound rectally, reporting good results. Fewer still have taken mephedrone intravenously, but this is NOT recommended: as a potent vasoconstrictor and pressor agent, the risks of cardiotoxicity varied types of inflammation and irritation near the injection site are high.

3. What does it do?
Mephedrone induces dramatic CNS stimulation, dry mouth, increased perspiration, decreased appetite, very dilated pupils, occasional jaw tension and GI discomfort. In terms of mental effects, mephedrone induces euphoric and empathetic feelings. While most report less empathy than with MDMA, such emotional opening is still distinct, but is also accompanied by cocaine like ego-inflation. Short-term memory impairment is to be expected.

Alarmingly, mephedrone induces sores in the mouth and can cause knees and elbows to turn slightly blue or red and blotchy due to severe vasoconstriction, but possibly through additional, undiscovered mechanisms. Alarmingly, these symptoms tend to get worse by far with repeated use, particularly with binging, and these symptoms can by far out-persist mephedrone's presence in the body. Neurologically, many report an MDMA-like hangover, again very severe with binges or addiction. Research very strongly suggests mephedrone's cardio-toxicity, but its neurotoxicity as well (see section on current research).

4. How long does it last?
Mephedrone typically lasts 2-2.5 hours when taken orally, 1-2 hours when insufflated, 1 hour when IVed, and 1-2 hours when administered rectally, though the highly euphoric peak is quite a bit briefer, compelling many users to dose with cocaine-type frequency. Mephedrone's first-order metabolite, 4-methyl-ephedrine, is metabolized far more slowly. Thus, many experience lengthy, dysphoric trailing stimulation.

5. How much is needed for a dose?
Orally: 150-250 mg insufflated: 75-150 mg IV: 50-100mg rectally: 50-100mg
(you likely do NOT want to take a potent vasoconstrictor rectally)

6. Is it dangerous?
Yes: people have reported blue knees and elbows from vasoconstriction, persisting heart palpitations, anxiety, and so on. Mephedrone is very likely harmful to the brain and heart as well as irritating to mucous membranes when insufflated. Few people have died; however, some others have gotten severely ill after their first dose.

7. Is it addictive?
Mephedrone, like other stimulants, does not appear to cause physical dependence, though the compulsion to re-dose is intense. With regular use, dependence similar to that seen with other stimulants occurs readily; however, for the most part, once one has not had Mephedrone for 24-48 hours, cravings severely diminish in presence.

8. What is particularly harmful to mix with Mephedrone?
Stimulants are most dangerous, but not too much is known about combining Mephedrone with other drugs. In general, drugs that prove unsafe in combination with MDMA will also prove unsafe with mephedrone, particularly MAO-inhibitors (the latter presenting the risk of serotonin syndrome).

ebola: can I get someone else's input here? I have little knowledge of what the sum of reported bioassays suggest.

9. What are some beneficial supplements one can take to combat Mephedrone's detrimental health effects?

Tyrosine, Garlic and other vasodilators, Milk, and Fish Oils have been shown most effective thus far.

10. What happens during an overdose?
The user's heartrate will skyrocket and body temperature will increase. Certain places on extremities may turn blue and one may have difficulty breathing or moving.

11. What are current research findings on mephedrone?

In "Beta-keto amphetamines: studies on the metabolism of the designer drug mephedrone and toxicological detection of mephedrone, butylone, and methylone in urine using gas chromatography–mass spectrometry", Meyer et al. confirmed that mephedrone metabolizes to 4-methyl-ephedrine, a highly cardiotoxic compound (2010, Analytical and Bioanalytical Chemistry, Volume 397, Number 3, 1225-1233, DOI: 10.1007/s00216-010-3636-5). 4-methyl-ephedrine is a potent adrenergic agent and vasoconstrictor, with a therapeutic index a couple to a few times more narrow than ephedrine's, and a duration outlasting mephedrone itself by a few times.

In "Mephedrone, compared to MDMA (ecstasy) and amphetamine, rapidly increases both dopamine and serotonin levels in nucleus accumbens of awake rats", Kehr. et al. found mephedrone to be a potent releaser of all three monoamines, with a propensity for dopaminergic release in league with amphetamine, and a propensity to release serotonin in league with MDMA, suggesting a very high likelihood of neurotoxitiy (2011, British Journal of Pharmacology, DOI: 10.1111/j.1476-5381.2011.01499.x).
 
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I hate mephedrone with a passion. Not only do I consider it a dodgy substance that someone decided to popularise to make money from the MDMA drought but I think it harmed the rave scene too.
 
definitely an odd drug. only tried it twice and one of those times was some nasty stuff that was actually red and some berry flavored powder...it was nasty. the other time i tried it was some brand that sold a 1g capsule...i believe it was 1 g anyways...i took about half and felt ok but not much so i took the rest within an hr an was good for 5 or 6 hours it seems...this may not be completely accurate as it was a while back but it was a long time...i only tried it twice bc i didnt find out about the stuff til it was about to be banned...by the way...my capsule was lovey dovey brand
 
In "Beta-keto amphetamines: studies on the metabolism of the designer drug mephedrone and toxicological detection of mephedrone, butylone, and methylone in urine using gas chromatography–mass spectrometry", Meyer et al. confirmed that mephedrone metabolizes to 4-methyl-ephedrine, a highly cardiotoxic compound (2010, Analytical and Bioanalytical Chemistry, Volume 397, Number 3, 1225-1233, DOI: 10.1007/s00216-010-3636-5). 4-methyl-ephedrine is a potent adrenergic agent and vasoconstrictor, with a therapeutic index a couple to a few times more narrow than ephedrine's, and a duration outlasting mephedrone itself by a few times.
so is vasoconstriction in itself damaging to the heart? if not, what causes the permanent damage to the heart that mephedrone and/or 4-methyl-ephedrine cause?
 
None has shown that mephedrone causes permanent damage to the heart. Well, vasoconstriction can severely exacerbate concurrent heart disease...

ebola
 
Hey all - great information in here. I'm going to add it to the Wiki right now and will post back with a direct link if you want to check out the entry. All who contributed significantly will be credited, P.S. =D

~ Vaya
 
I'd like to make a few comments, if I may.

Firstly, I think your dosages, at least for insufflated, which is the method I used virtually every time, are far too large!
When I started using mephedrone we were doing lines of about 75-100mg. But I soon discovered that even 25 or 50mg was sufficient to give a very nice buzz. I don't see much reason why first time users should consider 150mg+ to be an appropriate dose. To be sure, it is more euphoric, but it is far more addictive and not really necessary.
But if you were to buy a bag of 700mg, assuming it to be a gram and do the maths I can see why it would seem like the doses are higher, but frequently the bags are between .2 and .3 (sometimes even .4) underweight. If you are friendly with your dealer you might be able to get a .9 or full gram from time to time. Just my experience

The main other point I want to make is that, in the UK at least, almost all 'MCAT' I have encountered since the ban (excluding the following month where there was a mix of all kinds of random RCs) has not been the real thing, ie, 4-MMC. The 'MCAT' I have had since then in my opinion was probably 4-MEC although I don't know for sure. This is still the main type that is floating around in various cities that I've been to. The dose for this stuff, in my experience, is between 100-150mg although due to my own tolerance I am not sure, because personally I have been upping the dose to extreme levels over time (250 to 800mg per dose). But I do know that when I meet other people using the drug who are not hardened drug users, they tend to use less than 100mg, even with this different drug (4-MEC).

One other thing... Magnesium as a supplement to stimulant drugs is well known to reduce or even eliminate some adrenergic symptoms such as bruxism. It is also suggested to reduce tolerance when used in the interim, but I'm not sure how much this has been validated by anecdotal evidence.
 
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I just saw the dosages posted and imo, they are way too high to be in a newbie FAQ.
 
Dj cosmo is right. In my experience, with low tolerance even doses beneath 50mg can be quite active. Found this out when I shared a ~1g bag with two other guys over the course of 6+ hours. Somehow it lasted and still got us where we wanted to be. New users shouldn't do 100+ mg doses, for simple harm reduction if nothing else.
 
Comments all heard. Can someone re-write a more accurate dosage chart for me? In the meantime ill remove te currently posted information!

Y'all are really working the HR philosophy around here. I dig that :) :)

~ Vaya
 
on insufflation

[b said:
2. How is it taken?[/b]
Mephedrone is generally swallowed and/or insufflated./QUOTE]

Nooooooo no no no. The powder itself is both fluffy and glass like, and insufflation causes an intense and lasting pain that is so potent that it makes it difficult to speak. upon witnessing someone try it, he had to sit down and cry it out a bit, and then an hour and a half later still felt noticeable pain. I would do my best to highly dissuade anyone attempting to insufflate 4-MMC
 
This depends on how processes of crystallization went for a particular batch. Mephedrone is typically well-tolerated insufflated (though at least as painful as MDMA, as a rough level).

ebola
 
Nooooooo no no no. The powder itself is both fluffy and glass like, and insufflation causes an intense and lasting pain that is so potent that it makes it difficult to speak. upon witnessing someone try it, he had to sit down and cry it out a bit, and then an hour and a half later still felt noticeable pain. I would do my best to highly dissuade anyone attempting to insufflate 4-MMC
Do you have something to back this up? I have a a lot of experience with 'drone & have read quite a bit of others use & snorting it is definitely the most popular ROA. That single tear inducing burn is a bittersweet side effect I believe many love rather than hate, in a hurts so good, man, kinda way. It's also gone in about 30 seconds because then you're high as Fuck.



:)
 
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It's hard to tell, as tri-monoaminergic release is profoundly analgesic.

ebola
 
Generally swallowed or snorted my ASS. Not in my home town. bang bang bang. all day. all night. choo choo train. Destroying every vein. No offense. my home town mite be a little (not general)
 
Mephadrone insufflated feels like hammering a nail up your nose, the kind I got from a headshop had a lavender scent, the best way to describe the experience would be to say its like mixing mdma and cocaine. The urge to re-dose is so intense, the come down is terrible and obviously your not going to sleep until your completely detoxed of this substance
 
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