Methylmethcathinone/4-Methylmethcathinone (Mephedrone; Meow Meow; Cat; Drone; Bubbles) is an entactogenic-stimulating substance of the cathinone class. Mephedrone belongs to a group known as substituted cation, which is a derivative of the active substance in the plant cat (cathinone).
2. Medium - 0.95-2.15 mg/kg;
3. High- 2.15 mg/kg or more.
2. Medium - 0.15-0.25 mg/kg;
3. High - more than 0.25 mg/kg.
2. Repeated vomiting;
3. Severe non-localized or localized headache;
4. An acute visual impairment up to its loss and lasting more than 10 minutes;
5. Severe anxiety, psychosis, panic attack;
6. Delirium, incoherent speech, delusions of persecution;
7. Respiratory disorders up to the "inability to breathe”;
8. Hallucinations or visual and auditory illusions lasting more than 20 minutes from the moment of using mephedrone;
9. An increase in body temperature of more than 37.5 C and persistent hyperthermia for more than 6 hours, or an increase in body temperature of more than 38.5 C and persistent hyperthermia for more than 30 minutes without a tendency to decrease.
Special instructions, interaction with other psychoactive substances.
1. The use of mephedrone, theoretically, does not contribute to the development of a metabolic disorder. However, it increases the severity of diabetes symptoms, disrupts the control and compensation systems of regulating the glycemic profile, decreases the effect of pharmacological therapy of diabetes mellitus. Therefore, the use of mephedrone is not recommended for patients with diabetes mellitus.
2. It is not recommended to use mephedrone during any acute illness, regardless of the affected system.
3. The combined use of mephedrone with other psychostimulants increases the risk of severe side effects.
4. The combined use of mephedrone with iMAO and SSRIs increases the risk of serotonin syndrome.
5. The combined use with 25x-NBOMe and 25x-NBOH is not recommended due to the high risk of acute coronary syndrome, severe psychosis.
6. The use of mephedrone together with LSD does not have a "desirable" effect, since mephedrone changes the psychedelic properties of LSD, however, there are some sporadic cases of positive reviews.
7. The combination of mephedrone with MXE, MDMA, DXM leads to an increase in incidence of complications associated with severe side effects, such as persistent increase in blood pressure, hyperthermia, neurotoxicity, ischemic attacks of the brain, acute coronary syndrome.
8. The combined use of mephedrone with alcohol is a potentially dangerous combination due to an increase in the duration of the psychostimulating and euphorogenic effects of mephedrone and a decrease in the degree of alcoholic intoxication, which contributes to the uncontrolled consumption of a large amount of these substances, exposing users to an increased risk of acute intoxication.
9. When using mephedrone together with marijuana, the incidence of developing acute conditions is low.
10. The use of mephedrone with ketamine (in low doses) together is a popular combination. The risks of developing critical conditions are medium or low, and the effect of low doses of ketamine makes the experience of using mephedrone more "hallucinogenic" and "smoothes" the undesirable post-effects of mephedrone at the comedown from the trip.
11. The combined use of mephedrone and opioid receptor agonists is not recommended.
12. The combined use of mephedrone with antibacterial, antifungal and antiviral agents is not recommended.
13. The use of mephedrone during pregnancy and lactation is prohibited.
14. The combined use of mephedrone with drugs of the PDE-5 inhibitor group increases the risk of developing cardiovascular complications with medium risk level.
Terms of detection and storage rules
1. With a single use of mephedrone, the detection period in urine when using an express test is about 2 days (there is often a false positive test for amphetamines, MDMA);
2. When using mephedrone for a long time, the detection period is up to 15-17 days (according to some sources, 7-9 days), and mephedrone metabolites can be detected up to 3 months with systematic use (PFIA method or chromatography-mass spectrometry);
3. Only mephedrone metabolites are identified in the hair, and their detection period is about 2-3 months (more data for 1.5-2 months).
Physical properties and description.
Mephedrone hydrochloride has a characteristic smell of "dill and chemicals" (the smell of the base of 4-methylmethcathinone), and is found either in the form of a white powder (flour) or in the form of crystals (similar to sugar). Mephedrone flour is a white floury powder with an admixture of small crystals, which can clump. This is the first product produced in the synthesis process of mephedrone (first oxidation with the base, then solvent cleaning) - an amorphous precipitate. Mephedrone crystals are colorless, transparent crystals that resemble sugar in appearance. They are obtained by recrystallization of "flour". There are two types of crystals: crystallus-obtained with rapid recrystallization, true crystals - with slow recrystallization.
Other psychoactive substances that can be sold under the name of mephedrone: 4-CMC / 4-chloromethacathinone; 3/4-FMC; 4-emc; 4-CEC / Ethyl-Hexedrone / Hexedrone; 4-ma; 4-FA and 2-FA;
Synthesis of mephedrone from haloketone in ethyl acetate
Synthesis of mephedrone in NMP
Synthesis of mephedrone (bromination in dichlormethane)
Mephedrone is a synthetic molecule of the cathinone family. Cathinones are structurally similar to amphetamines. They contain a phenylethylamine core with a phenyl ring connected to an amine group (NH2) via an ethyl chain with an additional methyl substitution at Ra. Amphetamines and cathinones are alpha-methylated phenylethylamines, cathinones contain an additional carbonyl group on R1. Mephedrone contains an additional methyl substitute for RN, similar to MDMA and methamphetamine, and R4 of its phenyl ring - (RS) - 2-Methylamino-1-(4-methylphenyl)propan-1-one.
Pharmacokinetics and pharmacodynamics of mephedrone.
The mechanism of action of mephedrone consists of several properties: the substance blocks the reverse neuronal capture of monoamines, reduces the rate of synthesis of monoamine oxidase and catecholortomethyltransferase. This leads to an increase in the concentration of monoamines and catecholamines at the same time in the synaptic cleft (the gap is 10-50 nm wide between the membranes, the edges are strengthened by intercellular contacts). In addition, 4-mmc stimulates the postsynaptic membrane receptors (SSDRA).
The maximum concentration in the blood plasma occurs after one hour. When taken orally at an average dosage (150 mg), the half-life of mephedrone is 2.2 hours. Drug addicts do not take mephedrone more than 4 times in one session. Repeated use has intervals more than 2 hours in between.
Various articles published at the end of 2011 studied the effect of mephedrone on rats brain, and also studied the obsessive potential of mephedrone. Using microdialysis, dopamine and serotonin were collected, and dopamine and serotonin gains were measured. The intake of mephedrone led to an increase in dopamine by about 500%, and serotonin by about 950%. They reached their peak concentrations at 40 minutes and 20 minutes and returned to the baseline level 120 minutes after the injection. Analysis of the ratio of dopamine and serotonin levels showed that mephedrone was predominantly influencing (releasing) serotonin at a ratio of 1.22:1 (serotonin vs. dopamine). In addition, half-lives of dopamine and serotonin decay were calculated, 24.5 minutes and 25.5 minutes respectively.
Mephedrone has been proven to affect the following types of receptors in descending order: D2, 5-HT1A, TAAR1, D1/D3, 5-HT2C, 5HT2B, 5-HT2A/B, a1/2A. Mephedrone is mainly metabolized by cytochrome CYP2D6, and its main metabolites are: nor-mephedrone, nor-dihydromephedrone, 4-carboxy-dihydromephedrone, hydroxytolyl-mephedrone, succinyl-normephedrone. The maximum concentration time of mephedrone is about 52.5 minutes, the half-life is 2.21 hours, LC50-4500 ng / ml, LD50-120-150 mg/kg, the permeability coefficient of the blood-brain barrier is 14.0 Pe, the DAT/SERT ratio is 2.41.
Methods of use and doses.
Intranasal use of mephedrone involves the beginning of the effect within five minutes with standard medium doses, the plateau is reached already at 15-20 minutes, and the total time the “expected” effects last is about 40 minutes. With intranasal use, the doses are calculated according to the following gradations:
1. Low- 0.45-0.95 mg/kg;Mephedrone hydrochloride has a characteristic smell of "dill and chemicals" (the smell of the base of 4-methylmethcathinone), and is found either in the form of a white powder (flour) or in the form of crystals (similar to sugar). Mephedrone flour is a white floury powder with an admixture of small crystals, which can clump. This is the first product produced in the synthesis process of mephedrone (first oxidation with the base, then solvent cleaning) - an amorphous precipitate. Mephedrone crystals are colorless, transparent crystals that resemble sugar in appearance. They are obtained by recrystallization of "flour". There are two types of crystals: crystallus-obtained with rapid recrystallization, true crystals - with slow recrystallization.
Other psychoactive substances that can be sold under the name of mephedrone: 4-CMC / 4-chloromethacathinone; 3/4-FMC; 4-emc; 4-CEC / Ethyl-Hexedrone / Hexedrone; 4-ma; 4-FA and 2-FA;
Synthesis of mephedrone from haloketone in ethyl acetate
Synthesis of mephedrone in NMP
Synthesis of mephedrone (bromination in dichlormethane)
Mephedrone is a synthetic molecule of the cathinone family. Cathinones are structurally similar to amphetamines. They contain a phenylethylamine core with a phenyl ring connected to an amine group (NH2) via an ethyl chain with an additional methyl substitution at Ra. Amphetamines and cathinones are alpha-methylated phenylethylamines, cathinones contain an additional carbonyl group on R1. Mephedrone contains an additional methyl substitute for RN, similar to MDMA and methamphetamine, and R4 of its phenyl ring - (RS) - 2-Methylamino-1-(4-methylphenyl)propan-1-one.
Pharmacokinetics and pharmacodynamics of mephedrone.
The mechanism of action of mephedrone consists of several properties: the substance blocks the reverse neuronal capture of monoamines, reduces the rate of synthesis of monoamine oxidase and catecholortomethyltransferase. This leads to an increase in the concentration of monoamines and catecholamines at the same time in the synaptic cleft (the gap is 10-50 nm wide between the membranes, the edges are strengthened by intercellular contacts). In addition, 4-mmc stimulates the postsynaptic membrane receptors (SSDRA).
The maximum concentration in the blood plasma occurs after one hour. When taken orally at an average dosage (150 mg), the half-life of mephedrone is 2.2 hours. Drug addicts do not take mephedrone more than 4 times in one session. Repeated use has intervals more than 2 hours in between.
Various articles published at the end of 2011 studied the effect of mephedrone on rats brain, and also studied the obsessive potential of mephedrone. Using microdialysis, dopamine and serotonin were collected, and dopamine and serotonin gains were measured. The intake of mephedrone led to an increase in dopamine by about 500%, and serotonin by about 950%. They reached their peak concentrations at 40 minutes and 20 minutes and returned to the baseline level 120 minutes after the injection. Analysis of the ratio of dopamine and serotonin levels showed that mephedrone was predominantly influencing (releasing) serotonin at a ratio of 1.22:1 (serotonin vs. dopamine). In addition, half-lives of dopamine and serotonin decay were calculated, 24.5 minutes and 25.5 minutes respectively.
Mephedrone has been proven to affect the following types of receptors in descending order: D2, 5-HT1A, TAAR1, D1/D3, 5-HT2C, 5HT2B, 5-HT2A/B, a1/2A. Mephedrone is mainly metabolized by cytochrome CYP2D6, and its main metabolites are: nor-mephedrone, nor-dihydromephedrone, 4-carboxy-dihydromephedrone, hydroxytolyl-mephedrone, succinyl-normephedrone. The maximum concentration time of mephedrone is about 52.5 minutes, the half-life is 2.21 hours, LC50-4500 ng / ml, LD50-120-150 mg/kg, the permeability coefficient of the blood-brain barrier is 14.0 Pe, the DAT/SERT ratio is 2.41.
Methods of use and doses.
Intranasal use of mephedrone involves the beginning of the effect within five minutes with standard medium doses, the plateau is reached already at 15-20 minutes, and the total time the “expected” effects last is about 40 minutes. With intranasal use, the doses are calculated according to the following gradations:
2. Medium - 0.95-2.15 mg/kg;
3. High- 2.15 mg/kg or more.
Oral use involves the use of gelatin capsules, or mephedrone dissolved in warm water (considering the sediment of mephedrone, which doesn't dissolve). Given the low bioavailability of mephedrone when absorbed into the gastrointestinal tract, the dosage is usually about 1.75 mg/kg. With an increase in the dosage, the risk of severe side effects increases as well. The effect occurs within 15-20 minutes, the plateau is frequently at 40 minutes, and the duration of the effects is about 90 minutes.
Intravenous use is not recommended due to its negative effects on the vessel wall and surrounding soft tissues. The incidence of phlebitis and thrombophlebitis in veins, which mephedrone solution is injected in, is 65-85%, which determines the choice of mainly intranasal use of the substance. The doses of mephedrone for intravenous injection are as follows:
1. Low - 0.15 mg/kg;Intravenous use is not recommended due to its negative effects on the vessel wall and surrounding soft tissues. The incidence of phlebitis and thrombophlebitis in veins, which mephedrone solution is injected in, is 65-85%, which determines the choice of mainly intranasal use of the substance. The doses of mephedrone for intravenous injection are as follows:
2. Medium - 0.15-0.25 mg/kg;
3. High - more than 0.25 mg/kg.
These doses are valid only for pure substance. Typically, the doses of the substance used are 20-30% higher than the ones mentioned, depending on the quality of the product, the presence of tolerance to the substance and other factors. After 3-4 times of using mephedrone in one session, there is no point to use again, since tolerance will be at a maximum, the quality of the "expected" effects and their duration will be minimal, and the severity and duration of side effects will be at a maximum.
There should be at least 4-6 weeks break between sessions of using mephedrone to restore the metabolic processes. Intramuscular use of mephedrone is not recommended due to the almost 100% chance of developing complications in the form of inflammatory infiltrate, postinjection abscess, phlegmon of the gluteal region and other complications. Before using mephedrone, it is recommended to purify it by treatment with ethyl acetate through a chemical filter.
Three to four days before using mephedrone, it is recommended to start taking a course of multivitamins (with the B vitamins present in the composition), magnesium and potassium preparations and disaggregates. During the use of mephedrone, it is necessary to drink a sufficient amount of bicarbonate-sodium chloride water to restore the water-electrolyte balance.
The clinical presentation of mephedrone intoxication, the effects of mephedrone.
1. "Desirable" positive effects of mephedrone: physical and mental stimulation, pronounced euphoria, empathy, increased sociability, ability to work, the effect of "disinhibition”, increased sense of "attachment and empathy", increased motivation.
2. “Undesirable” neutral or positive effects of mephedrone: a decreased pain threshold, a decreased desire for alcohol and leveling its depressive effects, erectile dysfunction, an increase in libido, increased stimulation of the respiratory center during opiate intoxication, a decreased gag reflex, a decrease in aggression, memory and appetite, eccentric behavior, deterioration of short-term memory, weakening of critical thinking, sleep disorders, dizziness, bruxism, tremor and muscle cramps, impaired vision and urination, “strange” bodily sensations, temporary distortion of taste and smell, compulsive desire to take another dose of mephedrone, mydriasis.
3. "Undesirable" negative effects of mephedrone: increased blood pressure and heart rate; hyperthermia; decreased synthesis of bile and hydrochloric acid; increased glucose, ALT and CRP; dysbacteriosis; menstrual cycle disorders; increased gastrointestinal peristalsis; increased thrombosis; increased likelihood of schizoaffective disorder development; increased likelihood of anxiety and panic attack; increased levels of cortisol, ACTH, oxytocin, prolactin, b-endorphin, somatotropin, adrenaline, norepinephrine, histamine, limb numbness, discomfort behind the sternum, delirium of persecution, immunosuppressive effect.
As a rule, an overdose of mephedrone occurs during long-term sessions due to an increase in each next dose, or during "mephedrone marathons". Sometimes an overdose occurs with a single use, when the dose is too high. These are the symptoms of a mephedrone overdose:
1. Loss of consciousness;There should be at least 4-6 weeks break between sessions of using mephedrone to restore the metabolic processes. Intramuscular use of mephedrone is not recommended due to the almost 100% chance of developing complications in the form of inflammatory infiltrate, postinjection abscess, phlegmon of the gluteal region and other complications. Before using mephedrone, it is recommended to purify it by treatment with ethyl acetate through a chemical filter.
Three to four days before using mephedrone, it is recommended to start taking a course of multivitamins (with the B vitamins present in the composition), magnesium and potassium preparations and disaggregates. During the use of mephedrone, it is necessary to drink a sufficient amount of bicarbonate-sodium chloride water to restore the water-electrolyte balance.
The clinical presentation of mephedrone intoxication, the effects of mephedrone.
1. "Desirable" positive effects of mephedrone: physical and mental stimulation, pronounced euphoria, empathy, increased sociability, ability to work, the effect of "disinhibition”, increased sense of "attachment and empathy", increased motivation.
2. “Undesirable” neutral or positive effects of mephedrone: a decreased pain threshold, a decreased desire for alcohol and leveling its depressive effects, erectile dysfunction, an increase in libido, increased stimulation of the respiratory center during opiate intoxication, a decreased gag reflex, a decrease in aggression, memory and appetite, eccentric behavior, deterioration of short-term memory, weakening of critical thinking, sleep disorders, dizziness, bruxism, tremor and muscle cramps, impaired vision and urination, “strange” bodily sensations, temporary distortion of taste and smell, compulsive desire to take another dose of mephedrone, mydriasis.
3. "Undesirable" negative effects of mephedrone: increased blood pressure and heart rate; hyperthermia; decreased synthesis of bile and hydrochloric acid; increased glucose, ALT and CRP; dysbacteriosis; menstrual cycle disorders; increased gastrointestinal peristalsis; increased thrombosis; increased likelihood of schizoaffective disorder development; increased likelihood of anxiety and panic attack; increased levels of cortisol, ACTH, oxytocin, prolactin, b-endorphin, somatotropin, adrenaline, norepinephrine, histamine, limb numbness, discomfort behind the sternum, delirium of persecution, immunosuppressive effect.
As a rule, an overdose of mephedrone occurs during long-term sessions due to an increase in each next dose, or during "mephedrone marathons". Sometimes an overdose occurs with a single use, when the dose is too high. These are the symptoms of a mephedrone overdose:
2. Repeated vomiting;
3. Severe non-localized or localized headache;
4. An acute visual impairment up to its loss and lasting more than 10 minutes;
5. Severe anxiety, psychosis, panic attack;
6. Delirium, incoherent speech, delusions of persecution;
7. Respiratory disorders up to the "inability to breathe”;
8. Hallucinations or visual and auditory illusions lasting more than 20 minutes from the moment of using mephedrone;
9. An increase in body temperature of more than 37.5 C and persistent hyperthermia for more than 6 hours, or an increase in body temperature of more than 38.5 C and persistent hyperthermia for more than 30 minutes without a tendency to decrease.
Special instructions, interaction with other psychoactive substances.
1. The use of mephedrone, theoretically, does not contribute to the development of a metabolic disorder. However, it increases the severity of diabetes symptoms, disrupts the control and compensation systems of regulating the glycemic profile, decreases the effect of pharmacological therapy of diabetes mellitus. Therefore, the use of mephedrone is not recommended for patients with diabetes mellitus.
2. It is not recommended to use mephedrone during any acute illness, regardless of the affected system.
3. The combined use of mephedrone with other psychostimulants increases the risk of severe side effects.
4. The combined use of mephedrone with iMAO and SSRIs increases the risk of serotonin syndrome.
5. The combined use with 25x-NBOMe and 25x-NBOH is not recommended due to the high risk of acute coronary syndrome, severe psychosis.
6. The use of mephedrone together with LSD does not have a "desirable" effect, since mephedrone changes the psychedelic properties of LSD, however, there are some sporadic cases of positive reviews.
7. The combination of mephedrone with MXE, MDMA, DXM leads to an increase in incidence of complications associated with severe side effects, such as persistent increase in blood pressure, hyperthermia, neurotoxicity, ischemic attacks of the brain, acute coronary syndrome.
8. The combined use of mephedrone with alcohol is a potentially dangerous combination due to an increase in the duration of the psychostimulating and euphorogenic effects of mephedrone and a decrease in the degree of alcoholic intoxication, which contributes to the uncontrolled consumption of a large amount of these substances, exposing users to an increased risk of acute intoxication.
9. When using mephedrone together with marijuana, the incidence of developing acute conditions is low.
10. The use of mephedrone with ketamine (in low doses) together is a popular combination. The risks of developing critical conditions are medium or low, and the effect of low doses of ketamine makes the experience of using mephedrone more "hallucinogenic" and "smoothes" the undesirable post-effects of mephedrone at the comedown from the trip.
11. The combined use of mephedrone and opioid receptor agonists is not recommended.
12. The combined use of mephedrone with antibacterial, antifungal and antiviral agents is not recommended.
13. The use of mephedrone during pregnancy and lactation is prohibited.
14. The combined use of mephedrone with drugs of the PDE-5 inhibitor group increases the risk of developing cardiovascular complications with medium risk level.
Terms of detection and storage rules
1. With a single use of mephedrone, the detection period in urine when using an express test is about 2 days (there is often a false positive test for amphetamines, MDMA);
2. When using mephedrone for a long time, the detection period is up to 15-17 days (according to some sources, 7-9 days), and mephedrone metabolites can be detected up to 3 months with systematic use (PFIA method or chromatography-mass spectrometry);
3. Only mephedrone metabolites are identified in the hair, and their detection period is about 2-3 months (more data for 1.5-2 months).
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