Information about Lisdexamfetamine

Lisdexamfetamine (L-lysine-d-amphetamine) is a prodrug of the psychostimulant d-amphetamine coupled with the essential amino acid L-lysine. Lisdexamfetamine was developed so that the psychostimulant is released and activated more slowly as the prodrug molecule is hydrolyzed—consequently cleaving off the amino acid-during the first pass through the intestines and/or the liver.

Vyvanse is the dimesylate salt of lisdexamfetamine marketed by Shire Pharmaceuticals. Vyvanse is FDA approved—in strengths up to 70 mg—for the treatment of attention-deficit hyperactivity disorder in pediatric patients ages 6–12. Not only does Shire aspire to have Vyvanse replace Adderall XR as their flagship ADHD product, they also have their marketing target set at 50% of the ADHD pharmaceutical market share. Shire will be applying for FDA—as well as European—approval for the treatment of adolescents and adult patients with ADHD. Shire has stated prospects of applying Vyvanse for FDA approval for the treatment of depression.

A 25 mg strength Vyvanse capsule is molecularly equivalent to 10 mg Dexedrine Spansules (both the aforementioned pharmaceuticals are about 7.425 mg dextroamphetamine). However, this molecular equivalence is not a bioequivalence ratio; as it turns out, the AUC for the aforementioned pharmaceuticals is equivalent, however, the peak exposure of dextroamphetamine in Vyvanse is about 50% higher than Dexedrine Spansules.[1]

In human oral abuse-liability studies, 150 mg Vyvanse produced a "likeability"—euphoric effect—that was determined to be indistinguishable from 200 mg of the Schedule IV drug diethylpropion hydrochloride or 40 mg of dextroamphetamine.[2]
Enlarge picture
70mg Vyvanse capsules

Notes and references

[2]

A prodrug is a pharmacological substance (drug) which is administered in an inactive (or significantly less active) form. Once administered, the prodrug is metabolised in vivo into the active compound.
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A psychostimulant is a substance that enhances locomotor behavior. Examples of psychostimulants include amphetamine, methamphetamine, cocaine, methylphenidate, and arecoline, the most widely used psychostimulant.
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Dextroamphetamine is a powerful psychostimulant which produces increased wakefulness, energy and self-confidence in association with decreased fatigue and appetite. It is perhaps the archetypal psychostimulant, and drugs with similar psychoactive properties are often referred to as
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An essential amino acid or indispensable amino acid is an amino acid that cannot be synthesized de novo by the organism (usually referring to humans), and therefore must be supplied in the diet.

Essentiality vs.


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Lysine (abbreviated as Lys or K)[1] is an α-amino acid with the chemical formula HO2CCH(NH2)(CH2)4NH2.
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:Not to be confused with electrolysis


Hydrolysis is a chemical reaction or process in which a chemical compound is broken down by reaction with water.[1][2] This is the type of reaction that is used to break down polymers.
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In anatomy, the intestine is the segment of the alimentary canal extending from the stomach to the anus and, in humans and other mammals, consists of two segments, the small intestine and the large intestine.
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liver is an organ present in vertebrates and some other animals. It plays a major role in metabolism and has a number of functions in the body, including glycogen storage, decomposition of red blood cells, plasma protein synthesis, and detoxification.
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Shire plc (formerly: Shire Pharmaceuticals Group Plc)

Public (LSE:  SHP )
Founded 1986
Headquarters Basingstoke, England, UK

Key people James Cavanaugh, Chairman
Matthew Emmens, CEO
Industry Pharmaceuticals
Revenue $1,796.
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Food and Drug Administration (FDA) is an agency of the United States Department of Health and Human Services and is responsible the safety regulation of most types of foods, dietary supplements, drugs, vaccines, biological medical products, blood products, medical devices,
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Pediatrics (also spelled paediatrics) is the branch of medicine that deals with the medical care of infants, children, and adolescents (from newborn to age 14-21, depending on the country).
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Adderall is a pharmaceutical psychostimulant comprising mixed amphetamine salts. The drug is used primarily to treat attention-deficit/hyperactivity disorder and narcolepsy. Adderall has also been used successfully to manage severe cases of treatment-resistant depression.
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A pharmaceutical company, or drug company, is a commercial business whose focus is to research, develop, market and/or distribute drugs, most commonly in the context of healthcare. They can deal in generic and/or brand medications.
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Market share, in strategic management and marketing, is the percentage or proportion of the total available market or market segment that is being serviced by a company.
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Bioequivalence is a term in pharmacokinetics used to assess the expected in vivo biological equivalence of two proprietary preparations of a drug. If two products are said to be bioequivalent it means that they would be expected to be, for all intents and purposes, the
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In the field of pharmacokinetics, the area under the curve (AUC) is the area under the curve in a plot of concentration of drug in plasma against time.

Interpretation and usefulness of AUC values


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The Controlled Substances Act (CSA) was enacted into law by the Congress of the United States as Title II of the Comprehensive Drug Abuse Prevention and Control Act of 1970.
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Diethylcathinone (also called Diethylpropion and Amfepramone), is a sympathomimetic stimulant drug marketed as an appetite suppressant. It is sold under the brand name Tenuate or Tenuate Dospan, and may also be known as Amfepramone.
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Stimulants are drugs that temporarily increase alertness and awareness. They usually have increased side-effects with increased effectiveness, and the more powerful variants are therefore often prescription medicines or illegal drugs.
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Eugeroics are a class of stimulants that produce long-lasting mental arousal. These stimulants tend to increase alertness may not have the peripheral (body) effects or addiction/tolerance/abuse potential of the traditional stimulants.
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Adrafinil is a mild central nervous system stimulant drug used to relieve excessive sleepiness and inattention in elderly patients. It is also used off-label by individuals wishing to avoid fatigue, such as night workers or others who need to stay awake and alert for long periods
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Carphedon (C12H14N2O2, 2-(4-phenyl-2-oxopyrrolidin-1-yl)acetamide) is a derivative of the nootropic drug piracetam. It was developed in Russia, and a small number of low-scale clinical studies have shown possible links between
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Modafinil is a eugeroic drug generally prescribed to treat narcolepsy, made by the pharmaceutical company Cephalon Inc. It is not a typical stimulant and is often described as a "wakefulness promoting agent." The drug is sometimes prescribed off-label for ADD/ADHD.
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Armodafinil (Nuvigil®) is an eugeroic drug produced by the pharmaceutical company Cephalon Inc., which was approved by the FDA on June 15, 2007.

Cephalon plans to conduct clinical trials evaluating the use of Nuvigil as a treatment for serious medical
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Phenethylamine, or β-Phenylethylamine, is an alkaloid and monoamine. In the human brain, it is believed to function as a neuromodulator or neurotransmitter (trace amine).
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4-Fluoroamphetamine, para-fluoroamphetamine or 4-fluoro-alpha-methylphenethylamine (4-FMP), is a central nervous system stimulant. It is a chemical analog of amphetamine, and is also related to other phenethylamines, such as cathinone, methcathinone, and
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4-methylthioamphetamine is a drug known as 4MT, 4-MTA, "Flatliners" or 1-(4-methylthiophenyl)-2-aminopropane. It was developed by the research team led by David E. Nichols, but was intended to be used only as an agent for laboratory research into the serotonin transporter protein,
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Alpha-pyrrolidinopropiophenone (α-PPP) is a stimulant drug. It is similar in structure to the appetite suppressant diethylpropion and has analogous effects in animals.
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