Peringatan Keamanan

The LD50 value for lisdexamfetamine dihydrochloride in rats was >1000 mg/kg.L48285

Manifestations of amphetamine overdose include restlessness, tremor, hyperreflexia, rapid respiration, confusion, assaultiveness, hallucinations, panic states, hyperpyrexia and rhabdomyolysis. Fatigue and depression usually follow the central nervous system stimulation. Serotonin syndrome has been reported with amphetamine use, including lisdexamfetamine. Cardiovascular effects include arrhythmias, hypertension or hypotension and circulatory collapse. Gastrointestinal symptoms include nausea, vomiting, diarrhea and abdominal cramps. Convulsions and coma usually precede fatal poisoning. Lisdexamfetamine and d-amphetamine are not dialyzable.L48280

Lisdexamfetamine

DB01255

small molecule approved investigational

Deskripsi

Lisdexamfetamine is a prodrug of dextroamphetamine, a central nervous system stimulant known as d-amphetamine,A40246 covalently attached to the naturally occurring amino acid L-lysine.A2230 Lisdexamfetamine is the first chemically formulated prodrug stimulant A40246 and was first approved by the FDA in April 2008.A2230 It was also approved by Health Canada in February 2009.L48285 Lisdexamfetamine works to treat attention deficit hyperactivity disorder and binge eating disorder A2230 by blocking dopamine and norepinephrine reuptake and increasing their levels in the extraneuronal space.L48280

Struktur Molekul 2D

Berat 263.3785
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Plasma concentrations of unconverted lisdexamfetamine are low and transient, generally becoming non-quantifiable by 8 hours after administration. The plasma elimination half-life of lisdexamfetamine typically averaged less than one hour in volunteers ages six years and older. The plasma elimination half-life of dextroamphetamine was approximately 8.6 to 9.5 hours in pediatric patients six to 12 years and 10 to 11.3 hours in healthy adults.[L48280]
Volume Distribusi Dextroamphetamine, the active metabolite of lisdexamfetamine, easily crosses the blood-brain barrier.[A40243]
Klirens (Clearance) -

Absorpsi

After oral administration, lisdexamfetamine dimesylate is rapidly absorbed from the gastrointestinal tract.A40246, L48285 Following single-dose oral administration of lisdexamfetamine in pediatric patients with ADHD under fasted conditions, Tmax of lisdexamfetamine and dextroamphetamine was reached at approximately one hour and 3.5 hours post-dose, respectively. Weight/Dose normalized AUC and Cmax values were the same in pediatric patients as the adults. Food prolongs Tmax by approximately one hour and may decrease the exposure (Cmax and AUC) of dextroamphetamine.L48280

Metabolisme

Lisdexamfetamine dimesylate is hydrolyzed by red blood cells to dextroamphetamine and l-lysine primarily in the blood. Substantial hydrolysis occurs even at low hematocrit levels.A40246, A40243, L48280 Dextroamphetamine can further be metabolized to form other metabolites, such as hippuric acid.A261640 Lisdexamfetamine is not metabolized by cytochrome P450 enzymes.A2231, L48280

Rute Eliminasi

Following oral administration of a 70 mg dose of radiolabeled lisdexamfetamine dimesylate in six healthy subjects, approximately 96% of the oral dose radioactivity was recovered in the urine, and only 0.3% recovered in the feces over 120 hours. Of the radioactivity recovered in the urine, 42% of the dose was related to amphetamine, 25% to hippuric acid, and 2% to intact lisdexamfetamine.L48280

Interaksi Makanan

3 Data
  • 1. Avoid antacids. Urinary excretion of lisdexamfetamine is elevated when the urine is more acidic. Antacids like sodium bicarbonate alkalinize the urine; therefore, they may reduce lisdexamfetamine elimination.
  • 2. Limit foods and supplements high in vitamin C. Urinary excretion of lisdexamfetamine is elevated when the urine is more acidic. Vitamin C acidifies the urine and, therefore, may increase lisdexamfetamine elimination.
  • 3. Take with or without food. Food prolongs Tmax by approximately one hour, but does not significantly affect drug exposure.

Interaksi Obat

1103 Data
Valsartan Lisdexamfetamine may decrease the antihypertensive activities of Valsartan.
Ramipril Lisdexamfetamine may decrease the antihypertensive activities of Ramipril.
Remikiren Lisdexamfetamine may decrease the antihypertensive activities of Remikiren.
Torasemide Lisdexamfetamine may decrease the antihypertensive activities of Torasemide.
Isradipine Lisdexamfetamine may decrease the antihypertensive activities of Isradipine.
Olmesartan Lisdexamfetamine may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Lisdexamfetamine may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Lisdexamfetamine may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Lisdexamfetamine may decrease the antihypertensive activities of Minoxidil.
Treprostinil Lisdexamfetamine may decrease the antihypertensive activities of Treprostinil.
Amlodipine Lisdexamfetamine may decrease the antihypertensive activities of Amlodipine.
Nimodipine Lisdexamfetamine may decrease the antihypertensive activities of Nimodipine.
Nisoldipine Lisdexamfetamine may decrease the antihypertensive activities of Nisoldipine.
Bendroflumethiazide Lisdexamfetamine may decrease the antihypertensive activities of Bendroflumethiazide.
Fosinopril Lisdexamfetamine may decrease the antihypertensive activities of Fosinopril.
Trandolapril Lisdexamfetamine may decrease the antihypertensive activities of Trandolapril.
Metolazone Lisdexamfetamine may decrease the antihypertensive activities of Metolazone.
Benazepril Lisdexamfetamine may decrease the antihypertensive activities of Benazepril.
Bosentan Lisdexamfetamine may decrease the antihypertensive activities of Bosentan.
Enalapril Lisdexamfetamine may decrease the antihypertensive activities of Enalapril.
Cyclothiazide Lisdexamfetamine may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Lisdexamfetamine may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Lisdexamfetamine may decrease the antihypertensive activities of Mecamylamine.
Losartan Lisdexamfetamine may decrease the antihypertensive activities of Losartan.
Moexipril Lisdexamfetamine may decrease the antihypertensive activities of Moexipril.
Eplerenone Lisdexamfetamine may decrease the antihypertensive activities of Eplerenone.
Lisinopril Lisdexamfetamine may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Lisdexamfetamine may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Lisdexamfetamine may decrease the antihypertensive activities of Metyrosine.
Hydroflumethiazide Lisdexamfetamine may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Lisdexamfetamine may decrease the antihypertensive activities of Cryptenamine.
Perindopril Lisdexamfetamine may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Lisdexamfetamine may decrease the antihypertensive activities of Candesartan cilexetil.
Fenoldopam Lisdexamfetamine may decrease the antihypertensive activities of Fenoldopam.
Indapamide Lisdexamfetamine may decrease the antihypertensive activities of Indapamide.
Tadalafil Lisdexamfetamine may decrease the antihypertensive activities of Tadalafil.
Eprosartan Lisdexamfetamine may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Lisdexamfetamine may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Lisdexamfetamine may decrease the antihypertensive activities of Quinapril.
Telmisartan Lisdexamfetamine may decrease the antihypertensive activities of Telmisartan.
Methyldopa Lisdexamfetamine may decrease the antihypertensive activities of Methyldopa.
Hydrochlorothiazide Lisdexamfetamine may decrease the antihypertensive activities of Hydrochlorothiazide.
Trichlormethiazide Lisdexamfetamine may decrease the antihypertensive activities of Trichlormethiazide.
Irbesartan Lisdexamfetamine may decrease the antihypertensive activities of Irbesartan.
Nitrendipine Lisdexamfetamine may decrease the antihypertensive activities of Nitrendipine.
Deserpidine Lisdexamfetamine may decrease the antihypertensive activities of Deserpidine.
Pentolinium Lisdexamfetamine may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Lisdexamfetamine may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Lisdexamfetamine may decrease the antihypertensive activities of Diazoxide.
Epoprostenol Lisdexamfetamine may decrease the antihypertensive activities of Epoprostenol.
Hydralazine Lisdexamfetamine may decrease the antihypertensive activities of Hydralazine.
Polythiazide Lisdexamfetamine may decrease the antihypertensive activities of Polythiazide.
Cilazapril Lisdexamfetamine may decrease the antihypertensive activities of Cilazapril.
Saprisartan Lisdexamfetamine may decrease the antihypertensive activities of Saprisartan.
Spirapril Lisdexamfetamine may decrease the antihypertensive activities of Spirapril.
Tienilic acid Lisdexamfetamine may decrease the antihypertensive activities of Tienilic acid.
Sitaxentan Lisdexamfetamine may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Lisdexamfetamine may decrease the antihypertensive activities of Ambrisentan.
Diethylnorspermine Lisdexamfetamine may decrease the antihypertensive activities of Diethylnorspermine.
Nilvadipine Lisdexamfetamine may decrease the antihypertensive activities of Nilvadipine.
Pinacidil Lisdexamfetamine may decrease the antihypertensive activities of Pinacidil.
Temocapril Lisdexamfetamine may decrease the antihypertensive activities of Temocapril.
Riociguat Lisdexamfetamine may decrease the antihypertensive activities of Riociguat.
Macitentan Lisdexamfetamine may decrease the antihypertensive activities of Macitentan.
Hexamethonium Lisdexamfetamine may decrease the antihypertensive activities of Hexamethonium.
Aliskiren Lisdexamfetamine may decrease the antihypertensive activities of Aliskiren.
Nicorandil Lisdexamfetamine may decrease the antihypertensive activities of Nicorandil.
Efonidipine Lisdexamfetamine may decrease the antihypertensive activities of Efonidipine.
Lacidipine Lisdexamfetamine may decrease the antihypertensive activities of Lacidipine.
Rauwolfia serpentina root Lisdexamfetamine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Lisdexamfetamine may decrease the antihypertensive activities of Enalaprilat.
Selexipag Lisdexamfetamine may decrease the antihypertensive activities of Selexipag.
Angiotensin 1-7 Lisdexamfetamine may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Lisdexamfetamine may decrease the antihypertensive activities of Imidapril.
BQ-123 Lisdexamfetamine may decrease the antihypertensive activities of BQ-123.
Cicletanine Lisdexamfetamine may decrease the antihypertensive activities of Cicletanine.
Dihydralazine Lisdexamfetamine may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Lisdexamfetamine may decrease the antihypertensive activities of Zofenopril.
Guanoxan Lisdexamfetamine may decrease the antihypertensive activities of Guanoxan.
Delapril Lisdexamfetamine may decrease the antihypertensive activities of Delapril.
Vincamine Lisdexamfetamine may decrease the antihypertensive activities of Vincamine.
Linsidomine Lisdexamfetamine may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Lisdexamfetamine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Lisdexamfetamine may decrease the antihypertensive activities of Tolonidine.
Endralazine Lisdexamfetamine may decrease the antihypertensive activities of Endralazine.
Cadralazine Lisdexamfetamine may decrease the antihypertensive activities of Cadralazine.
Cyclopenthiazide Lisdexamfetamine may decrease the antihypertensive activities of Cyclopenthiazide.
Bietaserpine Lisdexamfetamine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Lisdexamfetamine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Lisdexamfetamine may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Lisdexamfetamine may decrease the antihypertensive activities of Guanoclor.
Muzolimine Lisdexamfetamine may decrease the antihypertensive activities of Muzolimine.
Xipamide Lisdexamfetamine may decrease the antihypertensive activities of Xipamide.
Candesartan Lisdexamfetamine may decrease the antihypertensive activities of Candesartan.
Dexniguldipine Lisdexamfetamine may decrease the antihypertensive activities of Dexniguldipine.
Tocopherylquinone Lisdexamfetamine may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Lisdexamfetamine may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Lisdexamfetamine may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Lisdexamfetamine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Lisdexamfetamine may decrease the antihypertensive activities of Perindoprilat.

Target Protein

Trace amine-associated receptor 1 TAAR1

Referensi & Sumber

Synthesis reference: Michael J. Bauer, Gary Richard Callen, Judi Christine Humphrey, Todd Jeffrey Johnson, Matthew Wendell Schiesher, "Methods and Compositions for Preparing Lisdexamfetamine and Salts Thereof." U.S. Patent US20120157706, issued June 21, 2012.
Artikel (PubMed)
  • PMID: 18548134
    Madaan V: Lisdexamfetamine dimesylate for childhood ADHD. Drugs Today (Barc). 2008 May;44(5):319-24. doi: 10.1358/dot.2008.44.5.1215724.
  • PMID: 17035599
    Krishnan S, Moncrief S: An evaluation of the cytochrome p450 inhibition potential of lisdexamfetamine in human liver microsomes. Drug Metab Dispos. 2007 Jan;35(1):180-4. Epub 2006 Oct 11.
  • PMID: 20514273
    Goodman DW: Lisdexamfetamine dimesylate (vyvanse), a prodrug stimulant for attention-deficit/hyperactivity disorder. P T. 2010 May;35(5):273-87.
  • PMID: 24594478
    Hutson PH, Pennick M, Secker R: Preclinical pharmacokinetics, pharmacology and toxicology of lisdexamfetamine: a novel d-amphetamine pro-drug. Neuropharmacology. 2014 Dec;87:41-50. doi: 10.1016/j.neuropharm.2014.02.014. Epub 2014 Mar 1.
  • PMID: 18991468
    Krishnan SM, Pennick M, Stark JG: Metabolism, distribution and elimination of lisdexamfetamine dimesylate: open-label, single-centre, phase I study in healthy adult volunteers. Clin Drug Investig. 2008;28(12):745-55. doi: 10.2165/0044011-200828120-00002.

Contoh Produk & Brand

Produk: 240 • International brands: 0
Produk
  • Ag-lisdexamfetamine
    Capsule • 10 mg • Oral • Canada • Generic • Approved
  • Ag-lisdexamfetamine
    Capsule • 20 mg • Oral • Canada • Generic • Approved
  • Ag-lisdexamfetamine
    Capsule • 30 mg • Oral • Canada • Generic • Approved
  • Ag-lisdexamfetamine
    Capsule • 40 mg • Oral • Canada • Generic • Approved
  • Ag-lisdexamfetamine
    Capsule • 50 mg • Oral • Canada • Generic • Approved
  • Ag-lisdexamfetamine
    Capsule • 60 mg • Oral • Canada • Generic • Approved
  • Ag-lisdexamfetamine
    Capsule • 70 mg • Oral • Canada • Generic • Approved
  • Apo-lisdexamfetamine
    Capsule • 10 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 240 produk.

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