User:Fuse809/sandbox5
Clinical data | |
---|---|
Trade names | Tyvense, Elvanse, Venvanse, Vyvanse |
Other names | (2S)-2,6-diamino-N-[(1S)-1-methyl-2-phenylethyl]hexanamide (2S)-2,6-Bis(azanyl)-N-[(2S)-1-phenylpropan-2-yl]hexanamide |
AHFS/Drugs.com | Monograph |
MedlinePlus | a607047 |
License data |
|
Pregnancy category |
|
Routes of administration | Oral |
ATC code | |
Legal status | |
Legal status |
|
Pharmacokinetic data | |
Bioavailability | 28% |
Metabolism | Gastro-intestinal (initial); Hepatic (extensively CYP2D6) after conversion to d-amphetamine |
Elimination half-life | < 1 hour (prodrug molecule), 10-13 hours (d-amphetamine) |
Excretion | Urine (96%), faeces (minimal) |
Identifiers | |
| |
JSmol) | |
| |
| |
(what is this?) (verify) |
Lisdexamfetamine .
Lisdexamfetamine itself is inactive and acts as a
Lisdexamfetamine is indicated for the treatment of attention deficit hyperactivity disorder (ADHD) in children six to twelve years and in adults as an integral part of a total treatment program that may include other measures (i.e., psychological, educational, social). The safety and the efficacy of lisdexamfetamine dimesylate in patients three to five years old have not been established.[4] Important side effects of therapeutic lisdexamfetamine include stunted growth in young people and, occasionally, a psychosis can occur at therapeutic doses during chronic therapy as a treatment emergent side effect.[5] When abused at high doses the risk of experiencing and the severity of side effects increase.
As opposed to
Medical uses
Lisdexamfetamine is primarily used as a treatment for attention deficit hyperactivity disorder.[8][9][10][11] Lisdexamfetamine is also being investigated for possible treatment of cognitive impairment associated with major depressive disorder,[12] schizophrenia,[13] excessive daytime sleepiness[14] and binge eating disorder.[15]
Side effects
Misuse potential
Lisdexamfetamine has less potential for misuse than its active metabolite (dextroamphetamine) due to being initially inactive upon consumption via all methods, and the drug level of the active metabolite dextroamphetamine reaching a plateau within a therapeutic dosage range (both results of being a prodrug).
Common side effects
Common side effects (side effects that have average rates of presentation; usually presenting in >5% of patients) of lisdexamfetamine use may include:[16][17]
- Discomfort
- Erectile dysfunction
- Dizziness
- Mild agitation (restlessness)
- Nausea
- Xerostomia (dry mouth)
- Bruxism (jaw clenching/grinding)
- Anxiety
- Diarrhea
- Vomiting
- Headache
- Insomnia (inability to sleep)
- Weight loss (resulting from decreased appetite)
- Euphoria
- Diaphoresis(increased sweating)
- Irritability
- Parageusia(unpleasant taste)
- Upper abdominal pain
- Cold feet or hands
- Tachycardia (rapid heart rate)
Severe side effects include
Other side effects can be caused by lisdexamfetamine; these potentially serious reactions may include:[16][17]
- Severe aggression - some patients have reported sudden mood change, inability to control rage, physical abuse of others
- Abnormal tiredness
- swelling.
- Changes in vision
- Dyspnea(shortness of breath)
- Fever
- Severe headache
- Syncope (fainting)
- Angina pectoris(severe chest pain)
- Blurred vision
- Cardiac dysrhythmias- a group of cardiovascular conditions in which the electrical activity of the heart is abnormal with effects ranging from a fast heartbeat to cardiac arrest and sudden death.
- Seizures
- Tics - sudden, stereotyped, nonrhythmic and repetitive motor movements and/or vocalizations.
- Hallucinations
- Muscle tremors
- Severe irritability
- Severe psychomotor agitation
- Altered sexual ability or desire such as hypersexuality, erectile dysfunction, premature ejaculation, etc.
- Tachycardia (fast heartbeat)
- Slowed thinking
- Unstable emotions
Psychosis
Abuse of amphetamines can result in a stimulant psychosis which may present with a variety of symptoms (e.g.,
Although rare,
Mechanism of action
Because lisdexamfetamine is active in the human brain as amphetamine, its mechanism of action is identical tothat of dextroamphetamine.
Although the precise mechanism of action by which amphetamines improve the symptoms of ADHD remains unknown, it is thought that amphetamines decrease ADHD symptoms due to their effects on the central nervous system. Amphetamines act as
Lisdexamfetamine (LDX) is a therapeutically inactive molecule. After oral ingestion, LDX is broken down by enzymes to form l-lysine, a naturally occurring essential amino acid, and active d-amphetamine, which is responsible for the drug’s activity. The conversion of LDX to d-amphetamine is not affected by gastrointestinal pH and is unlikely to be affected by alterations in normal gastrointestinal transit times. LDX was developed with the goal of providing a long duration of effect that is consistent throughout the day, with reduced potential for abuse-related liking. The attachment of the amino acid lysine slows down the relative amount of d-amphetamine available to the blood stream. Because no free d-amphetamine is present in LDX capsules, d-amphetamine does not become available through mechanical manipulation, such as crushing or simple extraction. A relatively sophisticated biochemical process is needed to obtain d-amphetamine from LDX.[2]
History
Vyvanse was developed by New River Pharmaceuticals, who were bought by
On April 23, 2008, Vyvanse received FDA approval for the adult population.[21] In a randomized, double-blind, four-week phase III trial in adult patients with ADHD, dosages of 30, 50 or 70 mg/day of oral lisdexamfetamine caused a significantly greater improvement in ADHD-Rating Scale total score than placebo.[22]
On February 19, 2009, Health Canada approved 30 mg and 50 mg capsules of lisdexamfetamine for treatment of ADHD.[23]
On February 8, 2012, Vyvanse received FDA approval for maintenance treatment of adult ADHD.[24]
In February 2014, Shire announced that two late-stage clinical trials had shown that Vyvanse was not an effective treatment for depression.[25]
See also
- ADHD
- Amphetamine
- Anorectic
- Dopaminergic
- Methamphetamine
- Methylphenidate
- Midodrine
- Recreational drug use
References
- ^ Lisdexamfetamine Dimesylate: A Prodrug Stimulant for the Treatment of ADHD in Children and Adults
- ^ PMID 19329547.
- ^ Human pharmacology of intravenous lisdexamfetamine dimesylate: abuse liability in adult stimulant abusers.
- ^ "Lisdexamfetamine dimesylate (generic)." Brown University Psychopharmacology Update 19.7 (2008): 1-2. Academic Search Premier. EBSCO. Web. 12 Sept. 2010.
- ^ PMID 18698321.
- ^ "Lisdexamfetamine". Drugbank. Retrieved 13 October 2013.
{{cite web}}
:|section=
ignored (help) - ^ "Adderall XR Prescribing Information" (PDF). United States Food and Drug Administration. pp. 1–18. Retrieved 7 October 2013.
- ^ "Vyvanse (lisdexamfetamine) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 19 February 2014.
- ^ "Elvanse 30mg, 50mg & 70mg Capsules, hard - Summary of Product Characteristics". electronic Medicines Compendium. Shire Pharmaceuticals Limited. 28 February 2013. Retrieved 19 February 2014.
- ^ "PRODUCT INFORMATION VYVANSE® (lisdexamfetamine dimesilate)" (PDF). TGA eBusiness Services. Shire Australia Pty. Limited. 22 July 2013. Retrieved 19 February 2014.
- ^ "VYVANSE (LISDEXAMFETAMINE DIMESYLATE) CAPSULE [SHIRE LLC]". DailyMed. SHIRE LLC. December 2013. Retrieved 19 February 2014.
- ^ "Lisdexamfetamine Dimesylate in Residual Symptoms and Cognitive Impairment in Major Depressive Disorder (MDD) Partly Responsive to Selective Serotonin Reuptake Inhibitor (SSRI) or Selective Norepinephrine Reuptake Inhibitor (SNRI) Treatment". ClinicalTrials.gov. National Institute of Health. 17 February 2014. Retrieved 19 February 2014.
- )
- ^ "Shire Reports Positive Signal Finding Study of Investigative Use of Vyvanse® (lisdexamfetamine dimesylate) Capsules CII in Excessive Daytime Sleepiness Model". Shire. Shire. 10 January 2011. Retrieved 19 February 2014.
- ^ "Positive Top-line Results Shown for Vyvanse(R) (lisdexamfetamine dimesylate) Capsules (CII) in Adults with Binge Eating Disorder". Shire. Shire. 5 November 2013. Retrieved 19 February 2014.
- ^ a b Vyvanse (Lisdexamfetamine Dimesylate) Drug Information: Uses, Side Effects, Drug Interactions and Warnings at RxList
- ^ a b Capsules Facts and Comparisons at Drugs.com
- ^ a b Shoptaw SJ, Kao U, Ling W (2009). "Treatment for amphetamine psychosis (Review)". Cochrane Database of Systematic Reviews (1).
{{cite journal}}
: CS1 maint: multiple names: authors list (link) - ^ Hofmann FG. A handbook on drug and alcohol abuse: the biomedical aspects. 2nd Edition. New York: Oxford University Press, 1983.
- ^ Katherine A. Lyseng-Williamson. "Lisdexamfetamine dimesylate: a guide to its use in attention-deficit hyperactivity disorder." Drugs & Therapy Perspectives 26, no. 10 (2010): 1-5.
- ^ FDA Adult Approval of Vyvanse - FDA Label and Approval History
- .
- ^ Health Canada Notice of Compliance - Vyvanse. February 19, 2009, retrieved on March 9, 2009.
- ^ [2]. February 8, 2012, retrieved on February 9, 2012.
- ^ Hirschler, Ben (February 7, 2014). "UPDATE 2-Shire scraps Vyvanse for depression after failed trials". Reuters. Retrieved February 13, 2014.
Category:Amphetamines Category:Euphoriants Category:Prodrugs Category:TAAR1 agonists Category:Amphetamine