Lisdexamfetamine (Vyvanse)

[moda00]

A friend of mine was recently switched from his methylphenidate prescription to "Vyvanse," which is lisdexamfetamine. He gets 30mg orange and white caps, to be increased as needed over the next few weeks. He is a bit of a crackhead, so take this with a grain of salt, but told me he did some "research" on them online, and that they "affect the same receptors as coke/crack" and that they are "a better smoother high to snort than Adderall (mixed amphetamine salts) or Methylphenidate (aka Ritalin)." Now, I did some research of my own, and it seems to be a very recently released and approved drug, so not much info in the way of recreational use or experience reports. But pharmaceutically, I found out that this is a mixture of d-amphetamine with l-lysine. It's considered a "prodrug" with less abuse potential than traditional add/adhd drugs, and states that since the l-lysine is removed and the amps are absorbed directly in the gastrointestinal tract. It also states it is approved for children age 6-12, but my friend is in his late 20's.. likely off-label Rx'ing. Now, I'll copy and paste what I found below, but was wondering if those with any knowledge of this drug, or of chemistry in general, could give some input.

Anyways, my friend, I'll call her swim, was given some of these pills. She doesn't like high doses of uppers, usually uses orally to help with attention/wakefulness due to hypersomnia associated with a medical condition. She asked me to seek some info on here and advise her to understand more about these pills. Would these pills NOT be active nasally due to the l-lysine formulation or whatever, was her crackhead friend simply getting placebo? What does the "prodrug" designation mean, if the l-lysine molecule is removed with normal use as prescribed? In case anyone is wondering, it is in a capsule, but instead of beads like Adderall, it looks like fine white powder. Would a 30-mg pill have 30mg amphetamines, or 30mg of this combination of amps/l-lysine? Since Adderall is mixed amp salts, and methylphenidate (is it even technically an amphetamine??), how would dosage stack up. Would it be comparable to Dexedrine, which is just dextroamphetamine, in my understanding?? Another site/study I found says something about 25mg lisdexamfetamine being comparable to 10mg dexedrine/dextroamphetamine... and another said a study of euphoric effects placed 150mp lisdexamphetamine with 40mg adderall. But then some of the articles make it sound like the dosages between this new drug and Adderall etc. are the same or in very similar ranges.. And what is the time-release status comparable to similar substances? Anyone with any input- all advice appreciated. Some info copy/pasted below.


Lisdexamfetamine Dimesylate (Vyvanse™)
Date: May 22, 2007
Manufacturer: Shire US Inc.
Lisdexamfetamine dimesylate was FDA approved on February 23, 2007 for the treatment of Attention-Deficit/Hyperactivity Disorder (ADHD; DSM-IV®) in children 6 to 12 years old. Lisdexamfetamine is an inactive prodrug that is converted to dextroamphetamine after absorption through the gastrointestinal tract. Dextroamphetamine blocks the re-uptake of both dopamine and norephinephrine into the presynaptic neuron, thereby increasing their release into the synaptic cleft. However, the precise mechanism for improving ADHD symptoms is unknown. The parent drug, lisdexamfetamine, does not bind reuptake sites in vitro, which may decrease its potential abuse liability.
Lisdexamfetamine is rapidly absorbed from the gastrointestinal tract. L-lysine is cleaved from the parent compound by first-pass intestinal or hepatic metabolism, releasing dextroamphetamine. The time to reach maximum plasma concentrations of dextroamphetamine is 3.5 hours, but can be delayed an additional hour if taken with food. Lisdexamfetamine is not metabolized by cytochrome P450 enzymes. No drug interaction studies are available for dextroamphetamine, although it is a minor inhibitor of CYP2D6, CYP1A2, and CYP3A4. It is 96% renally excreted with an average plasma half life of 10 -13 hours.
Two unpublished randomized, double-blind, placebo-controlled trials in children 6-12 years old assessed the efficacy of lisdexamfetamine. In the first trial, patients were randomized to receive either placebo or fixed doses (30, 50, or 70 mg) of lisdexamfetamine once daily for 4 weeks. Statistically significant improvements in patient behavior (ADHD Rating Scale) were seen and maintained throughout the day with all doses compared to placebo.
The second trial used a cross-over design where patients were first titrated to stable doses of Adderall XR®. Next, patients received lisdexamfetamine (30, 50, or 70mg), placebo, or continued their same dose of Adderall XR®. Each treatment was taken once daily for 1 week. Patients taking lisdexamfetamine or Adderall XR® showed significant improvements in patient behavior (SKAMP-Deportment Rating Scale) vs. placebo. There was no significant difference in improvement between the active treatments.
The most common adverse effects reported with lisdexamfetamine were: decreased appetite (39%), insomnia (19%), irritability (10%), decreased weight (9%), and dizziness (5%). Non-significant differences with lisdexamfetamine vs. placebo include: incidences of upper abdominal pain (12% vs. 6%), vomiting (9% vs. 4%), nausea (6% vs. 3%), headache (12% vs. 10%), and xerostomia (5% vs. 0%). The incidence of adverse effects decreased over time. Ten percent (21/218) of lisdexamfetamine-treated patients discontinued treatment due to adverse effects vs.1% (1/72) of placebo-treated patients.
Urinary acidifying agents (eg ammonium chloride, sodium acid phosphate) increase urinary clearance of lisdexamfetamine, thereby decreasing its efficacy. Since lisdexamfetamine can raise blood pressure, it may decrease the efficacy of antihypertensive medications. The activity of tricyclic antidepressants, meperidine, phenobarbital and phenytoin can be enhanced, so dosage adjustments may be necessary.
Lisdexamfetamine is contraindicated for use during or within 14 days following the administration of monoamine oxidase inhibitors. Other contraindications include: agitation, moderate to severe hypertension, hyperthyroidism, glaucoma, and patients with a history of drug abuse.
Lisdexamfetamine is available as once-daily oral capsules in 30, 50, and 70 mg. Tailor therapy to the patient’s individual requirements using the lowest effective dose. The recommended starting dose is 30 mg/day. The dose may be increased by 20 mg/day in weekly intervals to a maximum dose of 70 mg/day. Instruct patients to take lisdexamfetamine in the morning to minimize the potential for insomnia. It may be taken with or without food.
Lisdexamfetamine is a Schedule II controlled substance and contains a FDA black-box warning about the abuse liability with amphetamines and cardiovascular complications that can result from misuse. Cost data are not yet available for lisdexamfetamine.
In summary, lisdexamfetamine is an FDA approved treatment for ADHD in children 6-12 years old. It has an extended half-life, allowing once-daily dosing. As a dextroamphetamine prodrug, it may also have reduced abuse liability compared to other current therapies. Clinical trials evaluating lisdexamfetamine are unpublished and were not conducted for longer than 4 weeks.
References>

1. Vyvanse™ (lisdexamfetamine dimesylate) package insert. Wayne, A. hire US Inc.; 2007.
2. Blick SK et al. Lisdexamfetamine. Pediatr Drugs 2007; 9(2): 129-135.

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Experience Report with Lisdexamfetamine (Vyvanse)- My friend swim did end up giving these a try. She asked me to share her experience with you all..

Time taken: 7:15 am
Drug: Lisdexamfetamine 30mg capsules
Dosage: 60mg (two of the orange and white 30's)
Route: Oral- capsules intact and taken as directed

Working on the computer and onset of effects first noted after about 45 minutes of ingestion (T+0:45), after eating a light breakfast of a bagel with hummus and some soymilk. Eyes felt very wide open and awake, whereas they had previously felt tired and wanted to go back to sleep. Also a very sexual horny/feeling, quickie session with multiple orgasms 5-6 and very intense. Had some errands to run early morning, which is normally hell for swim, but felt great- very energetic, very talkative when on the phone with people and interacting in public, but not in that "geeked out" way one can sometimes feel on coke or high doses of Adderall (left house around T+1:30, or around 8:45 am and spent about four hours doing errands and such. Overall very comfortable and energetic feeling, and pretty consistent- but not a noticeable rush or overly intense euphoria in any way.. Spent a couple hours driving around town- re-stocking on food and treats for the critters, to the bank, post office, grocery, to help swim's elderly gramps with some things around the house, etc. Got almost everything on the to do list done in one shift, and with no noticeable increase or decrease from that perfect steady energy. Back to swim's place around 1:00pm, or T+5:45- right away decided to do some dope (heroin). Perhaps a bit impulsive from the pills since she has no done heroin regularly in quite awhile. Did a nice shot. Swim felt the great opiate rush and nodded for a little bit, but the amps returned with a vengeance. She would never consider doing a "speedball" ever again, and doesn't touch coke in any form anymore, but she really enjoyed the feeling of the time-released steady up from the pills combined with the wonderful opiate feeling's down. Neither really negated the other, in that swim felt both effects strongly and positively, but the wakefulness effect of the amp definitely took precedence over the sleepy aspect of the dope after the first 10-15 minutes or so. Swim then did some organizing some things around her place- paying bills, making calls, cleaning the apartment, that sort of thing. And spent some time reading as well (T+6-9 hr). At that time swim had to go to a class for a couple hours, so went to that.. not too bad as far as the class went, but she was definitely starting to crash, so took 1 more 30mg Vyvanse(lisdexamfetamine) and 1 200mg Provigil(modafinil) right before the class, and then a 5mg methylphenidate about two hours- halfway- through. She is now officially exhausted, and the drug effects are worn off. She has a bit of a headache and shoulder pain, which could be a come-down/hangover from the upper, but swim thinks its likely just her body's way of telling her she is tired, now that the drugs in her brain aren't convincing her otherwise, as she hasn't gotten the best sleep lately. Oh well, shall catch up tonight, and swim got a ton done today! All around very enjoyable and time seemed to fly. Have not experimented with other routes such as nasal, and am not sure how that would affect someone given the prodrug formulation and the extra l-lysine which is supposedly cleaved from the amphetamines in the gastro-intestinal tract? Who knows? Swim prefers the oral route anyways, as it is smoother, longer lasting, and helps her to function by staying awake and remaining alert. She is afraid if she started using recreationally with such substances, it would likely become both highly addictive (again), and that the specific helpful effects she seeks from stimulant drugs, currently to treat a diagnosed medical condition, would not be compatible with the shorter and more intense rush-crash cycle of intranasal or iv use of uppers. Overall, this drug likely has less abuse potential or recreational value than the more classic and available stims, but is ideal in terms of a long lasting, steady, and strong "boost" for a long workday or a tedious exam. Swim looks forward to hearing from any others who have heard of or tried this prescription drug for add or for other conditions or circumstances, and how they felt about it.

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