In mice, the dose at which acute toxicity occurs with intravenous administration is 40 mg/kg, and with subcutaneous injection (injection into the skin layer just below the dermis and epidermis) 380 mg/kg. [14] The lethal dose of dimethocaine for one mouse is 0.3 g per kilogram of body weight. [15] Dimethocaine and structurally related local anesthetics such as cocaine and procaine inhibit dopamine (DA) absorption by blocking dopamine transporters (DATs). [7] The dopamine transporter controls the dynamics of the neurotransmitter dopamine. This neurotransmitter controls many functions, including movement, cognition, and mood. Drugs such as cocaine and dimethocaine induce a dopamine overflow by inhibiting dopamine transporters, creating a euphoric effect. [8] In addition to inhibiting dopamine intake, dimethocaine has also been shown to inhibit the binding of CFT, another inhibitor of dopamine absorption. [7] These inhibitory properties are responsible for the stimulating effect of dimethocaine on the central nervous system. [5] In vivo and in vitro measurements of dopamine transporter activity have shown that dimethocaine is a potent and effective inhibitor of dopaminergic reuptake (also known as an indirect dopamine agonist). [7] These effects were mainly observed in the nucleus accumbens, a region of the basal forebrain.
[5] The comparison of the pharmacological potencies of different local anesthetics resulted in the following power sequence:[5] Dimethocaine was originally synthesized in 1930 by the Hoffmann-La Roche company. It was sold under the name Larocain market. In the 1930s, dimethocaine gained popularity in the United States as a local anesthetic. Just like cocaine and procaine, it has been used during surgery, especially in dentistry, ophthalmology and otolaryngology. However, in the 1940s, it was withdrawn from the market due to its psychoactive effects and risk of addiction. Nowadays, dimethocaine is abused for these psychoactive effects. It is sold as a substitute for cocaine to circumvent legal problems. [1] [5] [6] In studies on rhesus monkeys, dimethocaine`s affinity for dopamine transporters is lower than that of cocaine, while dimethocaine`s effectiveness in inhibiting dopamine absorption is similar. This means that more dimethocaine is needed to achieve a similar reaction. Peak effects occurred within 10 to 20 minutes of the injection and fell to baseline levels within an hour.
[13] Cocaine, ecstasy and amphetamines should be “nationalized” and legally sold in state pharmacies in order to undermine global drug-related crime, a British charity for drug reform has recommended. The revelation triggers calls for the government to regulate the illegal drug trade “Drug prohibition doesn`t eliminate drugs – it only puts the market back to criminals, making it much dirtier and more dangerous. We know what effective regulation looks like – just look at our world-leading legal industry. When a product sold online in the UK in June 2010 that was advertised as dimethocaine was tested, it turned out to be a mixture of caffeine and lidocaine,[3] and the absence of a dopaminergic stimulant ingredient in such mixtures could explain the limited recreational effects reported by many users. However, other samples tested were shown to contain true dimethocaine and it was found that a branded product containing `bath salts`, which mainly contains dimethocaine as an active ingredient, was particularly abused in Ireland by intravenous drug users. [4] If you have any further questions about drug use and the law, or if you need help with a drug-related legal issue, please read the uk`s press release website which also imported 330kg of legal cocaine in 2016, which is about 83% of global demand and accounted for almost half of medical cocaine use (90kg). Poppers (liquid gold, amyl or butyl nitrite) are not covered by MDA and are not illegal to own or buy. They are often sold in joke and sex shops, but also in some pubs, clubs, tobacconists and sometimes in music or clothing stores used by young people. Although it has not been fully tested in court, the Drug Control Agency has stated that poppers is considered a drug by them and therefore falls under the Medicines Act of 1968.
This only allows licensed outlets, such as chemists, to sell the drug. Poppers are also not controlled under the Psychoactive Substances Act 2016. These drugs have recently been divided into two parts. Part 1 contains most of the smaller sedatives (with the exception of rohypnol and temazepam) and eight other substances. This new planning means that it is now illegal to be in possession of all small sedatives without a prescription. Part 2 Drugs include anabolic steroids, which can be legally possessed in medical form without a prescription, but are illegal to deliver to other people. The UK is the world`s largest exporter of legal cocaine and heroin, according to new figures, prompting campaigners to call on the government to regulate drug trafficking. Cocaine > dimethocaine > tetracaine > procaine > chlorprocaine It is a criminal offence to be responsible for a motor vehicle when it “cannot drive with alcohol or drugs”. Drugs can include illegal drugs, prescribed drugs or solvents. “All this carnage associated with the illicit cocaine and heroin market is useless – we can show that there are these legal markets that are not linked to any of these problems of terrorism, crime and violence, stabbings on the streets of London and everything in between.” The British charity Transform, a British drug reform charity, is calling for cocaine, ecstasy and amphetamines to be “nationalised” and legally sold in government-run pharmacies in order to undermine global drug trafficking and related crime. Dimethocaine is often used as a legal substitute for cocaine. The drug is administered intravenously or nasally, as taking it would lead to rapid hydrolysis.
[5] Its positive effects are euphoria, stimulation, increased conversational capacity and mood brightening. [6] However, because the drug acts in the same way as cocaine, it has comparable negative side effects. These side effects include: tachycardia, difficulty breathing, chest pain, vasoconstriction, insomnia, paranoia and anxiety. [6] Dimethocaine is likely to pose greater health problems than cocaine. This is due to the fact that more dimethocaine must be administered to create the same feeling of euphoria, which leads to an increased risk of negative effects. When inhaled, dimethocaine begins to act in 10-30 minutes, with the highest effects at 60-120 minutes and up to 4-6 hours, there is a phase of action with the “sequelae”. [11] Sequelae include fatigue and mild mental impairment. [6] Drugs formerly known as “legal highs” are chemicals that have similar effects to MDMA, mephedrone or cocaine. Mephedrone itself was a “legal high” before being reclassified, and the entire group was made illegal under the Psychoactive Substances Act of May 2016. In addition, administration of dimethocaine at non-toxic doses in mice has been shown to result in antinoziceptive reactions. [9] These reactions are thought to be caused, at least in part, by the effects of dimethocaine on the central nervous system.
An effect of memory impairment observed in mice after administration of dimethocaine was thought to be due to a non-anesthetic mechanism of action. [10] At the other end of the scale is Appendix 5, which lists drug preparations that are believed to pose a minimal risk of abuse.