Methylphenidate

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methyl phenyl(piperidin-2-yl)acetate

Contents

The Basics

Methylphenidate is a psychostimulant drug approved for treatment of attention-deficit hyperactivity disorder, postural orthostatic tachycardia syndrome, and narcolepsy. It may also be prescribed for off-label use in treatment-resistant cases of lethargy, depression, neural insult and obesity. It is similar in structure as amphetamines however only produce mild effects of amphetamines.

Introduction and Basic Description

Methlphenidate is a stimulant drug commonly known as Ritalin and Concerta. It prescribed to treat ADHD and Narcolepsy. When used recreationaly it produces effects similar to Cocaine

Timeline of Experience

Insufflation produces effects within about 10 minutes, whilst Oral consumption takes approximately 30 minutes. Effects typically last about five hours.

Effects

Effects of Methylphenidate depend on dosage and by person. Effects include

Feelings of increased energy

Feelings of Well-being, euphoria and elation

Talkativeness and increased sociability

Increased Focus and Desire

Decreased Appetite

Decreased desire to sleep

Dosages

When prescribed medically it is used orally at dosages between 5 to 60mg. Recreationaly it is used between 20mg and sometimes as high as 250mg

Method of administration

Method 1

Oral administration produces slower onset of action, and has lower bioavailability than insufflation. Methylphenidate medically is almost always oral,

Method 2

Insufflation is the most common recreational MOA. It has a fast onset of action and considerably higher bioavailability than oral

Slang

Smart pills, ritties, vitamin r

Problems

Contraindications and Overdose

MAOIs, Beta-Blockers, Depressants

Overdose can produce palpitations, anxiety, psychosis, rapid thoughts, slurred speech, seizures, psychosis, heart attacks and death

Negative Short-Term Side Effects

Dialated pupils, insomnia, jitters, agitation, anxiety, rapid heart rate

Negative Long-Term Side Effects

Drug dependance, damage to nasal septum from insufflation

Addiction and Withdrawal Issues

Can produce psychological dependency

Harm Reduction

Never share straws when insufflation as this can produce infections such as hepatitis c. Do not take doses above 150mg as this can cause adverse neurological and caradic effects. Never mix with depressants, MAOIs, and other stimulants

Legal Issues

Methylphenidate is schedule II in the United States, Schedule 8 in Australia, Class B in United Kingdom, Class B in New Zealand. It is restricted in almost every country as a stimulant. Possession and dealing can lead to fines and even imprisonment

Background and Chemistry

History of Drug

Methylphenidate was first synthesized in 1944, and was identified as a stimulant in 1954.

Methylphenidate was synthesized by Ciba (now Novartis) chemist Leandro Panizzon. His wife, Marguerite, had low blood pressure and would take the drug as a stimulant before playing tennis. He named the substance Ritaline, after his wife's nickname, Rita.

Originally it was marketed as a mixture of two racemates, 80% (±)-erythro and 20% (±)-threo. Subsequent studies of the racemates showed that the central stimulant activity is associated with the threo racemate and were focused on the separation and interconversion of the erythro isomer into the more active threo isomer.

Beginning in the 1960s, it was used to treat children with ADHD or ADD, known at the time as hyperactivity or minimal brain dysfunction (MBD). Production and prescription of methylphenidate rose significantly in the 1990s, especially in the United States, as the ADHD diagnosis came to be better understood and more generally accepted within the medical and mental health communities.


Chemistry

Methylphenidate is a benzypiperdine derative. It is a methyl ester of ritalinic acid. Methylphenidate is almost always used as a hydrochloride salt which is a white water soluble solid.

Preparation

Extraction of methylphenidate from tablets. This is for harm reduction.

You will need:

Ritalin or Focalin Instant Release pills, only guaranteed to work well with both the Brandname and TEVA generic version.

95% Ethanol, Everclear works fine. If they don't sell this in your state (don't in mine), 96% Isopropyl alcohol will work as well. Do not use anything thats anything below 90% alcohol, water will pull out binders, we need as little as possible. (note: if you can make your alcohol warm, not hot, even better. do not use a stove or a microwave or anything, but if you can leave it near like, a radiator for a bit, being even just a bit warm will help)

Something to measure liquid in ML, does not need to be super precise, I use a shot glass.

One small glass container/cup and something to stir with

At least one other glass container, with a single coffee filter secured onto it. Preparing 2-4 of these glasses, even if you only plan to use one, is a good idea.

Coffee Filters, folded a few times to create creases and more surface area, made slightly damp to prevent wicking

Teflon pan, wider the better. Pyrex works as well, but Teflon is the best, hands down.

Process:

1. Grind pills extremely fine. No chunks. Pour powder into glass container. For every 5mg you use, add 10ml of your alcohol. Stir this, let it rest, keep restirring, for a little while. Just a minute is fine.

2. Stir hard so all powder is floating in liquid. Depending on the amount you are doing, if theres a lot of liquid, and a lot of powder, it is likely that before long, the powder will build up and make the filtration super slow. If so, this is why I suggested preparing 2-4 of these glasses.

3. If, while being filtered, it gets too clogged with the inactives resting at the bottom, gently, careful not to rip the filter, stirring the powder around so it floats a bit will help. If absolutely stuck, take another glass with a coffee filter mounted inside, and put it next to the jammed up glass. Carefully, remove the filter thats clogged, not spilling/ripping/dropping it. Hold it over, and as far inside the new glass as you can, and squeeze the shit out of it, carefully, but squeeze as much of the alcohol out as you can. Do not just squeeze the clogged filter without having another filter in place, it will push out inactives.

4. Take all filters that were used, and the powder within them, and put them somewhere to dry, and then store them somewhere. Do not toss them.

5. Pour the alcohol and MPH mixture onto your teflon pan.

6. Now, we're basically done, its just a matter of evaporating off our alcohol. Open a window, the more fresh air you can get it, the better, this helps SIGNIFICANTLY, and the alcohol vapors will give you a headache, and could be dangerous if you are stupid and have an open flame near it. A lot of people will put the pan/pyrex dish onto an electric stove or hot plate, but if you take this route, be cautious not to let the alcohol boil. Personally, the room I do this in has EXTREMELY poor ventilation, and I use a hair dryer on and off when my hand gets tired, and for 4 focalin, and 80 ml of alcohol, this takes around 1.5-2.5 hours.

7. When no alcohol can be smelled on your tray, and it visually looks dry, scrape crystals off using card. kind of crush/grind these crystals in a powder. Spread this powder out, as much surface area as possible. This is especially important if you used isopropyl. There is still some alcohol trapped inside of the crystals you have made, so let the crushed crystals dry out ALL the way

8. Done. Make sure to remember, if you used 5 pills, one fifth of this new powder/crystals is the equivalent of 1 pill. Likely, 5 pills, extracted, will look like one pill crushed WITH binders. Dose carefully. There should be no binders/few binders, with a small amount of binders being pulled really only happening for the TEVA generics. You should have extracted 90-95% of the actives from that one pull. Depending on your tolerance, like, the tiniest, tiniest line might be all you need.

Mechanism of Action

Methylphenidate is a norepinephrine and dopamine reuptake inhibitor. It inhibits the Dopamine Transporter enzyme that pumps out dopamine from a synapse for reuse, this leads to increased activation of dopamine receptors. It has a similar effect on the norepinephrine transporter. The latter is responsible for it's feelings of energy and bodily stimulation, whilst the former accounts for euphoria

Trip reports and links

Trip Reports

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