Methylphenidate (Ritalin) Anesthesia?

[isthastuff]

Hey bluelighters, I had a quick pharmacological question concerning Methylphenidate (Ritalin) and it's big chemical brother, Dexmethylphenidate (Focalin). Something I've noticed following insufflation of either the racemic Ritalin (dl-TMP) or the right-handed Focalin (d-TMP) is that the subsequent drip causes a small yet noticeable degree of local anesthesia when held at the tip of/just below the tongue. To my knowledge (right or wrong - please correct me in the case of the latter), Ritalin (as either a racemate or (dextrorotatory) enantiopure preparation) is very closely related to Cocaine in terms of both chemical structure and pharmacological effect (noradrenergic and dopaminergic reuptake inhibition and interference at each respective catecholamine's transportive enzymes). In light of these congruences, and with note to cocaine's established property of local anesthesia, my question is for those of you familiar enough with chemistry to hopefully explain to this curious 'new'lighter any/all of the following: 1) the reason for Ritalin's minor anesthetic property and specifically, if this effect is a product of a structural overlap between the two chemicals (explanation appreciated if this is the case) and 2) more broadly, what is it that, specific to structure and the pharmacological consequences thereof, is to blame for the symptom/effect of anesthesia on a local level? My thanks in advance to any willing to give this some time/consideration and in turn, a modicum of solace to my insatiably curious mind. Enjoy your day(s)/daze!

 

[sekio]

Ritalin ain't an anesthetic, you're feeling the burn produced when the HCl salt hits you. Either that or vasoconstriction from the NDRI action/adrenergic receptors(?). When I first opened the thread I thought, hey, methylphenidate as an anesthetic agent? whoa! But alas.

Cocaine is a sodium channel blocker - like lidocaine, ketamine, etc - so it produces the familiar "numbness". Methylphenidate doesn't block the Na+ channel. This was done in the drug design process because sodium channel blocks are usually not too good for your heart tissue.

Focalin (d-TMP) overlays pretty well with cocaine but is missing the ester bridge needed for blocking the sodium channel. In addition it hads very little affinity for the serotonin transporter which cocaine also blocks. Structure-Activity-Relationships *SAR* are harder to predict and less logical than you think because these chemicals are usually interacting with massive proteins...

 

[gman7104]

Yes, I thought I was the only one who noticed this.

When I take concerta sublingually, it always numbs the region where the pill dissolves.

 

[NeighborhoodThreat]

When I take concerta sublingually, it always numbs the region where the pill dissolves.

sekio pretty much hit the nail right on the head. The methylphenidate isn't causing the numbing because methylphenidate (both dextrorotatory and racemate) isn't a sodium channel blocker. Any numbing you're feeling is most likely either due to one of the inactive binders in the Concerta pills or a placebo effect.

 

[K'd-OUT-in-AZ]

No, Methyphenidate doesn't produce anesthesia. It is purely the burn you get from snorting it. It doesn't numb your body in any way.

 

[LogicSoDeveloped]

I insufflated dexmethylphenidate and never got a numbness.

It has similarities to cocaine (from what I've heard, never tried coke and don't plan on it) but anesthesia isn't one of them.