Mephedrone

Mephedrone

Mephedrone (4-methylmethcathinone, 4-MMC) is a research chemical drug of the beta-ketone family, first reported in Israel during the mid-2000's. It is a substituted cathinone and structurally related to both methcathinone and methamphetamine. It is usually taken orally or insufflated with a typical active oral dose ranging from 100 - 250mg. It has euphoric and stimulant properties. A boom in the popularity of this chemical as a recreational drug across the UK, Republic of Ireland and mainland Europe during 2009 attracted substantial media and political interest, and in many nations resulted in possession and distribution of mephedrone being criminalized.

Contents

1Introduction1.1Using Mephedrone1.2Routes of administration1.2.1Oral1.2.2Insufflation1.2.3Intravenous1.2.4Rectal1.3Effects of Mephedrone1.4Combinations with Mephedrone1.5Pharmacology and Pharmacokinetics of Mephedrone1.6Enzyme Inhibition1.7Mephedrone receptor binding1.8Tolerance1.9Interactions1.10The health risks of Mephedrone1.11Cardiovascular1.12Overdose1.13Cytotoxicity1.14Carcinogenic/Mutagenic Properties1.15Producing Mephedrone1.16Chemical Characteristics1.17Marquis Reagent1.18Mecke & Mandelin1.19Simons & Robadope1.20Appearance1.21Legal status of Mephedrone1.22United Kingdom1.23USA1.24EU1.25Ireland1.26Denmark1.27Romania1.28Israel1.29Sweden1.30Norway1.31Germany1.32Finland1.33Poland1.34Australia1.35Related News Threads1.36Mephedrone History1.37More Mephedrone Sections1.38The latest mephedrone threads1.39References

INTRODUCTION

Mephedrone (1-(4-methylphenyl)-2-methylaminopropan-1-one) is a phenethylamine, structurally comparable to cathinone ((S)-2-amino-1-phenyl-1-propanone) and methylone ((±) 2-methylamino-1-(3,4-methylenedioxyphenyl)propan-1-one). The name "mephedrone" was logical (methyl-ephedrone, ephedrone being a name for methcathinone) and probably not just coined to resemble "methylone". While MCat is a name for MethCathinone, the media often mislabels Mephedrone as such. Very little is known about the pharmacology or toxicity of mephedrone, as no studies have been published that establish such characteristics. We’re currently awaiting access to a recently-conducted study that may elucidate such properties.

Using MephedroneThe compound appears to typically be used analogously to other recreational stimulants in a wide variety of settings - from large social groups to isolation. Though reports exist for a number of different methods of administration, mephedrone appears to be most commonly ingested orally and intranasally. Some individuals consider the compound to be strictly stimulant in effect, while many observe pseudo-psychedelic visual and auditory distortion.

Routes of administration

OralTaking a fixed amount orally can help limit the common urge to redose and prevent excess use.

Oral doses can be taken in a variety of ways; the easiest being either mixed with water, or wrapped in a rizzla paper and swallowed.

First time doses should range between 100mg and 150mg and users are advised to try to avoid eating for a few hours before administration as this can dampen the effects.

"250mg is a good oral dose, but the tail end effects will last a lot longer and sleep will be difficult."

A dose of 150mg-250mg is the average, giving a duration of around 2 hours.

Oral doses last longer but also take longer at onset; it is important not to redose early even if users feel it has not affected them. When using a gel capsule, onset of effects can take up to 45 minutes to be felt.

Side-effects from oral dosages can be nausea, stomach cramps and vomiting (especially in larger 250mg+ dosages).

InsufflationInsufflating mephedrone can dramatically increase the urge to redose, therefore it is important users set out a maximum amount for the night and stick to it.

First time doses should range between 25-75mg and can take up to 15 minutes to start working. Crushing/chopping the powder as finely as possible and placing a straw well inside the nostril before snorting can greatly increase the effects.

Many people consider snorting to be a dangerous method of administration; especially for drugs which are active when taken orally, due to increased risk of nose damage. Side-effects from snorting seem to be worse when compared to taking the same total dose orally - it's "harsh" on the body.

It's recommended to not share straws/notes with other people as this can increase the risk of infection. This is particularly important with mephedrone, as nose bleeds and nasal sores are a common complaint compared with many other drugs taken via this route.

IntravenousAdministering intravenous mephedrone is extremely dangerous, and highly enhances the potential for dangerous side-effects. Both sample purity and handling are important factors to consider. Additionally, the drug is observed to be quite addictive by individuals favoring oral and intranasal routes; the addictive components of the effects of the drug are likely to be quite higher, and may compel users to pursue dangerously high levels.

Doses for IV administration of 4-MMC range widely, and have been observed to range from 40mg to approximately 500mg.

RectalRectal administration, otherwise referred to as 'plugging', is characterized by a faster onset relative to oral dosing, requires lower doses, and has been suggested to be characterized as having a more rapid termination of activity relative to oral doses. A dose of 100 mg has been observed to last approximately 20 minutes, but this is quite likely variable between individuals.

Two general methods include the use of a syringe (needle removed) with 200 mg in fewer than 10 mL of water (approaching 5 mL) inserted while lying prone, allowing the solution to absorb over 3-5 min - as well as the use of gelatin caps as a vehicle for the compound to be inserted.

Rectal (plugging) administration of mephedrone

Mephedrone capsule...inserted anally?

Effects of MephedroneThe primary effects tend to reflect those of sympathomimetic stimulants such as amphetamines, cocaine, or MDMA. There appears to be a distinct euphoria and sociability inspired by the compound, as well as a strong urge to ingest large quantities subsequent to initial administration. Recreational doses induce transient anorexia, and appear to affect cardiac activity in typical CNS stimulant patterns.

The after-effects, or 'come-down' associated with mephedrone - occurring immediately subsequent to the duration of effects of the compound - is highly variable, but commonly consists of overall behavioral sedation and a desire to ingest more. There indeed appears to be an effect upon mood that reflects those of other recreational psychomotor stimulantssuch as cocaine or methamphetamine; individuals report 'come-downs' along a range of severity, from mild depression and languid disposition to intense depression. There is discussion of a transient suppression of immune system function, as many observe short periods of illness subsequent to ingestions of over 500 mg.

Side-effects are similarly variable, and include reactions as mild as persistently raised heart rate to severe - such as seizures and a bluing, or apparent bruising, of extremities. Other side-effects include difficulties with memory, persistently low body-temperature, anhedonia, and chest pain.

Mephedrone Experiences & Side-Effects Database

Very grumpy when mephedrone wears off?

Mephedrone comedown or just from sleep deprivation?

Cross Tolerance Mephedrone, Methylone and Ecstasy

Combinations with Mephedrone

While there are reports of combining mephedrone with other compounds, it is important to maintain that none of this information suggests that any of the following combinations are safe.

There are reports of combining mephedrone with the following compounds to no significant side-effect:

Metefepramone

Pthalimidoprodiophenone

Venlafaxine

Cannabis

Metoprolol

Hydrochlorothiazide

Simvastatin

Buproprion

Depatoke

Lisinopril

Niaspan

Opium

Propanolol

Citalopram

Amitriptyline

There are reports of combining mephedrone with the following compounds, observed to generate deleterious or dangerous side-effects:

Imipramine

Amphetamine

Synthetic Cannabinoids

Mephedrone and pharmaceutical combination reports

MDMA & Mephedrone

Pharmacology and Pharmacokinetics of MephedronePharmacology: 4-Methylmethcathinone is sympathomimetic stimulant. From proposed SAR modelling, 4-methylmethcathinone is expected to have similar pharmacological properties to methcathinone, but with increased activity on the serotoninneurotransmitter systems. Methcathinone is suggested as being more potent than its parent cathinone, and methamphetamine [1].

Methcathinone is a drug with a high abuse potential, with prolonged, high dosages known to cause psychosis and withdrawal tremors. Methcathinone is regarded as being similar in profile to methamphetamine in relation to neurotoxicity, with marked decreases in DA levels noted among abstinent users. While generally below levels associated with Parkinsons Disease, this is considered to be demonstrative of permanent, or semi-permanent neurological damage [2]. The compound is considered by some to be more potent than cathinone and methamphetamine. High doses of mephedrone have consistently generated convulsions, addictive tendencies, and symptoms of withdrawal.

Ethcathinone is closely related to mephedrone and causes many side effects: Stroke, Psychosis, Pulmonary hypertension, Tachycardia, hypertension, arrhythmia, chest pain, Bone marrow depression, agranulocytosis, leukopenia, Rash, hives, alopecia, ecchymosis, impotence, dizziness, anxiety, headache, mental depression, seizures, Nausea/vomiting, constipation, abdominal cramps, diarrhea. (From drug info thread)

Enzyme InhibitionAccording to M.R. Meyer, F.T. Peters, H.H. Maurer a number of metabolites are possible, however the n-demethyl metabolite of Mephedrone will be 4-Methylcathinone . This metabolite appears to be nearly inactive as a Monoamine Oxydase Inhibitor

On further metabolism of this metabolite one of the possible metabolites is 4-Methylnorephedrine (compound number 31 in table 3), caused by the reduction of the Keto. This metabolite has almost the same level of MAO-A inhibition as that of Amphetamine

Amphetamine's IC50 is 11, while the 4-Methylnorephedrine metabolite's is 12.

It is currently unclear as to the significance of this in normal recreational doses.

Mephedrone receptor bindingAwaiting cellular/molecular studies.

ToleranceMephedrone exhibits a strong desensitization effect upon repeated dosing, reminiscent of other traditionally addictive psychomotor stimulants. This compound in particular, however, appears to compel users to ingest higher subsequent doses as well as ‘booster-doses’. Physiological desensitization appears to be associated with long-term complications.InteractionsNo conclusive studies have been preformed. Discussion of drug combinations.

The health risks of Mephedrone

CardiovascularMephedrone has been observed to cause cardiovascular abnormalities when administered at doses above 200mg, though this isn’t ubiquitous. These abnormalities include heart palpitations, vasoconstrictive sensations, numbing as well as ‘bluing’ of limbs reminiscent of posturally dependent bruising.

Your BPM on Mephedrone

OverdoseMephedrone presents a very real danger of overdose; the most commonly-reported symptoms of overdose include: bluing limbs at doses above 300mg, numbing limbs at doses above 500mg, paranoia & anxiety at doses above 200mg, tinnitus at doses above 250mg, buccal blisters from insufflated doses, and chest pain at doses above 500mg. However, it’s been noted that overdose symptoms aren’t expressed by many individuals at much higher doses.

Chemical Characteristics

Column 1Column 2Systematic (IUPAC) name:(RS)-2-methylamino-1-(4-methylphenyl)propan-1-oneSynonyms:Molecular Formula:C11H15NO, C11H15NO.HClMolar mass:177.24 g/mol, 213.70 g/mol CAS Registry Number:1189805-46-6, 1189726-24-4 (hydrochloride)Melting Point:Boiling Point:Flash Point:no dataSolubility:Additionnal data:Notes:stability of the mephedrone molecule

Marquis ReagentThe Marquis reagent is a test to facilitate identification of alkaloids, composed of formaldehyde and sulfuric acid. Compounds will produce signature colors characterizing their reactions.

Taken by Viscis:

Mecke & MandelinThe Mecke reagent consists of selenous acid in sulfuric acid, and purportedly offers enhanced capabilities at detecting MDMA. The Mandelin reagent is a 1% solution of ammonium vanadate in sulfuric acid, and similar to both the Marquis and Mecke, different compounds will generate different color reactions.

Simons & Robadope

The Simons reagent is sodium nitroprusside in 50 mL distilled water, with 2 mL acetaldehyde added.

AppearanceMephedrone samples have been observed to vary in physical appearance.

Legal status of Mephedrone

United KingdomMephedrone is a Class B controlled substance, effective 16th April 2010. This came into effect due to an amendment to the Misuse of Drugs Act 1971, which controls a number of synthetic derivatives of cathinone. The penalties for possession and supply of mephedrone are therefore in line with other class B controlled substances. The maximum penalty in a Crown prosecution for possession and supply of mephedrone are 5 years and 14 years imprisonment respectively (plus an unlimited fine in both cases). The maximum penalty for a Magistrates prosecution is 3 months imprisonment plus a fine up to £2,500 for possession of mephedrone, and 6 months imprisonment plus a fine up to £5,000 for supply of mephedrone. Any proceeds from the illicit sale of mephedrone may also be seized under the Proceeds of Crime Act 2002.

Which drugs will likely be outlawed by the cathinone ban?

Call for ban on 'legal high' drug: Mephedrone

UK Mephedrone vendor arrested & charged with harm to public health.

USAMephedrone is a Schedule I controlled substance under Federal law, and also under state law in a majority of US states.

EU

IrelandPurported to remain legal, but there is discussion that this isn't to be assumed.

DenmarkBanned on December 18, 2008

Ban against three new substances (ethylcathinone, mephedrone & flephedrone)

Is Mephedrone Actually Legal in Ireland?

RomaniaWhile some claim the compound remains legal, methcathinone is explicitly prohibited - and so the compound may potentially be considered illegal.

Mephedrone legality in Romania

IsraelBanned in December 2007

SwedenBanned on December 15, 2008, classified as a narcotic on June 15, 2009.

NorwayIllegal under an act similar to the Analog Act

GermanyFrom 22nd January 2010 it will be a controlled substance

Germany Bans Mephedrone

FinlandIllegal to manufacture, import, possess, sell, or transfer without prescriptions.

PolandRemains legal (due to be banned soon, it's inclusion in an amendment to a narcotics bill is confirmed - June 2010).

AustraliaThough not explicitly identified, it's likely to be considered an illegal analogue of methcathinone.