Introduction to Ethylphenidate

Ethylphenidate is a recent research chemical introduced in 2011. Not much is known about it at this moment. It is a potent psychostimulant that acts as both a dopamine reuptake inhibitor and norepinephrine reuptake inhibitor.

Anecdotal evidence suggests it is actually more active as a dopamine reuptake inhibitor than norepinephrine. This produces a less jittery and more euphoric high than methylphenidate (or even cocaine).[1]

Users report a a duration of 1.5 to 3 hours and it comes on almost as quickly as cocaine does (around 5 mins after snorting). The need to re-dose is debatable and probably specific from person to person.

Most information is derived from the Drugs-Forum Ethylphenidate Drug Information thread[2], wikipedia and other fora.

Using Ethylphenidate

Ways of Administration

Intranasal

Ethylphenidate can be in insufflated although users report this is a painful experience. Rinsing the nose is recommended.

Wikipedia has information from another drug related forum stating that damage of perforated septum after fairly low usage. I use this route and flush my nose about 20 minutes later by snorting water from a spoon repeatedly until I feel the pathway is clear. But with this added information, and dosages and effects not much different from sublingually, it is, now the most likely next safest route.

Dosages:
25mg - weak
25-50mg -mild
50-75mg - strong
100mg - very strong

Oral

Dosages are probably comparable to Intranasal route

IV

Ethylphenidate can be injected by dissolving it in water. The dosages are probably a lot lower than other routes. As always injecting is very dangerous and not advised unless the user is absolutely sure about what they're doing.

Intramuscular injection (IM) of ethylphenidate is also possble. The same cautions apply as with IV.

Effects of Ethylphenidate

Although classified as a potent psychoactive stimulant, it has been reported to be more euphoric than other stimulants and some users describe it having less side-effects.

Main effects

• Increased conversation
• Abstract thinking
• Euphoria
• Some stimulation but not like with cocaine or methylphenidate
• Increased music appreciation
• Warm fuzzy body high

side effects

• Jaw tension
• Anxiety
• Penis shrinkage
• Restlessness
• Inability to concentrate on one task
• Slight stomach discomfort from oral dosages which could be when taken at the same time as food.

after effects

• Slight comedown
• Possibility to re-dose. More so at higher doses, although a tolerance builds up quickly if not much time is left between each dose or the dose is high.

Combinations with Ethylphenidate

Different Uses for Ethylphenidate

• Stimulant
• Anti-depressant
• ADHD treatment (?)

Pharmacology of Ethylphenidate

Ethylphenidate is the ethyl ester of 2-phenyl-2-(2-piperidyl)acetic acid, in the similar manner that methylphenidate is the methyl ester.

Ethylphenidate acts as both a dopamine reuptake inhibitor and norepinephrine reuptake inhibitor, meaning it effectively boosts the levels of the norepinephrine and dopamine neurotransmitters in the brain, by binding to, and partially blocking the transporter proteins that normally remove those monoamines from the synaptic cleft.

However, considering the close similarities between ethylphenidate and methylphenidate and the fact that methylphenidate, like cocaine, actually does not primarily act as a "classical" reuptake inhibitor, but rather as an "inverse agonist at the DAT" (also called a "negative allosteric modulator at the DAT"), it is at least very likely that ethylphenidate also primarily acts as an inverse DAT agonist instead of (or at least only secondarily) as a classical reuptake inhibitor (which could be called a "competitive antagonist at the DAT" using a similar terminology as "negative allosteric modulator at the DAT", which per definition means that its mechanism is non-competitive).

In Vivo formation of Ethylphenidate

Most research has been done around the in vivo creation of ethylphenidate by mixing alcohol with methylphenidate.[3] Since the synthetic formulation is novel it is interesting to research the difference between the two ways of experiencing ethylphenidate in the human body.

Chemistry of Ethylphenidate

Column 1	Column 2
Systematic(IUPAC) name:	(RS)-ethyl 2-phenyl-2-piperidin-2-ylacetate
Synonyms:	2-phenyl-2-(2-piperidyl)acetic acid, 2-Piperidineacetic acid, alpha-phenyl-, ethyl ester
Molecular Formula:	C15H21NO2
Molar mass:	247.33 g/mol [1]
CAS Registry Number:	57413-43-1
Melting Point:	no data
Boiling Point:	no data
Flash Point:	no data
Solubility:	no data
Additionnal data:	none
Notes:	none

Reagent test results of Ethylphenidate

Reagent	color produced	picture	video
Marquis	No reaction[2]	-	-

Synthesis of Ethylphenidate

Ethylphenidate is a structural relative of the chemical Methylphenidate. It can be produced by Methylphenidate HCl hydrolyzed to ritalinic acid, and subsequently esterify to ethylphenidate with ethanol HCl.

The Dangers of Ethylphenidate

• Potentially similar to methylphenidate

extremely CAUSTIC!
IMMEDIATE pain when it contacts delicate nasal or rectal tissue so damage is assumed to occur.

Physical Health Risks

<Physical Problem 1 - Please Identify and Add Others As Necessary>

<Physical Problem 2 - Please Identify and Add Others As Necessary>

Overdose

Reported Deaths

Mental Health Risks

After high dosages or repeated redoses and lack of sleep the anxiety, although not overwhelming, can leave a person rather jittery and may find the most simple of tasks much more taxing than it is.

Getting plenty of food before and after can help relieve some of the jitters.

Side Effects

Addiction

Forms of Ethylphenidate

• Crystallized shards
• White Powder

Legal Status of Ethylphenidate

USA

Although it is claimed to be legal, it may be considered to be an analog of the Schedule II controlled substance, methylphenidate. [4]

EU

• UK: Unscheduled
• D: Unscheduled

Other Countries

• CAN: Unscheduled
• UN: Unscheduled

History of Ethylphenidate

This compound only has a very brief history of widespread use, and unfortunately no absolute facts are known about the potential dangers/toxicity that may arise from the recreational abuse/use of ethylphenidate to date.

Most information that is available is about the metabolism of methylphenidate with alcohol into ethylphenidate in the liver. It is however questionable whether the effects are truly the same. Users have reported the contrary, and that it's rather a drug of a class in its own.

It is said to have appeared on the RC market in Dec 2010.

More Ethylphenidate Sections

Ethylphenidate Drug Info
Ethylphenidate Experiences
Ethylphenidate dose discussion.

References

1. ^Williard, R.; Middaugh, L.; Zhu, H.; Patrick, K. (2007). "Methylphenidate and its ethanol transesterification metabolite ethylphenidate: brain disposition, monoamine transporters and motor activity". Behavioural Pharmacology 18 (1): 39–51 PMID 17218796
2. ^https://drugs-forum.com/forum/sho...ixzz1iqgU4vTFv
3. ^J. Markowitz, C. DeVane, D. Boulton, Z. Nahas, S. Risch, F. Diamond, and K. Patrick, “Ethylphenidate formation in human subjects after the administration of a single dose of methylphenidate and ethanol.,” Drug Metab Dispos, vol. 28, no. 6, pp. 620–4, 2000.
4. ^Williard, R.; Middaugh, L.; Zhu, H.; Patrick, K. (2007). "Methylphenidate and its ethanol transesterification metabolite ethylphenidate: brain disposition, monoamine transporters and motor activity". Behavioural pharmacology 18 (1): 39–51 PMID 17218796