Dimethocaine

Dimethocaine: Efficacy, Metabolism

Dimethocaine, sometimes referred to as larocaine or DMC, is a stimulant. Although dimethocaine is less potent, its effect is similar to that of cocaine. Dimethocaine is just as addictive as cocaine because it stimulates the brain’s reward pathway.

Nonetheless, in many nations, dimethocaine is a legitimate substitute for cocaine, and the European Monitoring Centre for Drugs and Drug Addiction (EMCDDA) lists it as a “synthetic cocaine derivative.” Since dimethocaine is an ester of 4-aminobenzoic acid, its structure is similar to that of procaine. At room temperature, it appears as a white powder.

History of Dimethocaine

In 1930, the Hoffmann-La Roche company produced dimethocaine for the first time. The market name for it was larocaine. In the 1930s, dimethocaine became a popular local anesthetic in the United States. It was used during surgery, mostly in ophthalmology, dentistry, and otolaryngology, just like procaine and cocaine.

However, due to its psychotropic properties and potential for addiction, dimethocaine was taken off the market in the 1940s away from those who buy dimethocaine. Because of these psychotropic effects, dimethocaine is abused these days. It is marketed as a cocaine substitute to scale over legal restrictions.

Effectiveness of Dimethocaine

Dimethocaine, just like cocaine, prevents dopamine from being absorbed in the brain. This is done by interfering with the transporters of dopamine. The ability of this medication to block dopamine absorption and its affinity for dopamine transporters is related to its potency.

Dimethocaine has a lower affinity for dopamine transporters than cocaine in experiments with rhesus monkeys, but it has a similar ability to block dopamine uptake. This indicates that additional dimethocaine is required to get a comparable effect. Within 10 to 20 minutes of the injection, the effects reached their peak, and within an hour, they returned to their baseline levels.

Potency of Dimethocaine

According to studies, the potency of dDimethocaine is roughly half that of cocaine. It is sometimes referred to as larocaine or DMC. Despite dimethocaine’s apparent limited potency, this effect is similar to that of cocaine.

Dimethocaine fully inhibits dopamine uptake (0-100 microM measured) and completely displaces [3H]2-beta-carbomethoxy-3-beta-(4-fluorophenyl)tropane 1.5-naphthalenedisulfonate (CFT) binding (0-30 microM tested).

Drugs and Medicines

By inhibiting dopamine transporters (DAT), dimethocaine and structurally related local anesthetics like cocaine and procaine prevent dopamine (DA) from being absorbed. The dynamics of the neurotransmitter dopamine are regulated by the dopamine transporter. This neurotransmitter regulates a variety of processes, including emotion, movement, and thought.

By blocking dopamine transporters, drugs like cocaine and dimethocaine cause dopamine to overflow, thus producing a euphoric sensation.

The metabolism

The many metabolites of dimethicone have been studied in Wistar rats, however, the precise metabolic pathways of the drug have not been investigated. Various metabolites have been discovered and identified in their urine following the intake of dimethocaine. Various metabolic pathways may have been hypothesized as a result of these metabolites. Hydroxylation of the aromatic system, ester hydrolysis, deethylation, or a mixture of these three, make up the primary phase I reactions.

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