Tìm theo
Lisdexamfetamine
Các tên gọi khác (3) :
  • Lisdexamfetamine
  • lisdexamfetamine dimesylate
  • NRP104
Thuốc Gốc
Small Molecule
CAS: 608137-32-2
ĐG : New River Pharmaceuticals Inc. , http://www.nrpharma.com
CTHH: C15H25N3O
PTK: 263.3785
Lisdexamfetamine (L-lysine-d-amphetamine) is a prodrug of the psychostimulant d-amphetamine coupled with the essential amino acid L-lysine. It was developed so that the amphetamine 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. Amphetamines target the trace amine-associated receptor 1 (TAAR1). Amphetamine is also believed to exert its effects by binding to the monoamine transporters (the dopamine transporter or DAT) and increasing extracellular levels of the biogenic amines dopamine, norepinephrine (noradrenaline) and serotonin.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H25N3O
Phân tử khối
263.3785
Monoisotopic mass
263.199762437
InChI
InChI=1S/C15H25N3O/c1-12(11-13-7-3-2-4-8-13)18-15(19)14(17)9-5-6-10-16/h2-4,7-8,12,14H,5-6,9-11,16-17H2,1H3,(H,18,19)/t12-,14-/m0/s1
InChI Key
InChIKey=VOBHXZCDAVEXEY-JSGCOSHPSA-N
IUPAC Name
(2S)-2,6-diamino-N-[(2S)-1-phenylpropan-2-yl]hexanamide
Traditional IUPAC Name
lisdexamfetamine
SMILES
C[C@@H](CC1=CC=CC=C1)NC(=O)[C@@H](N)CCCCN
Độ hòa tan
792 mg/mL (dimesylate salt)
logP
1.06
logS
-3.5
pKa (strongest acidic)
15.89
pKa (Strongest Basic)
10.21
PSA
81.14 Å2
Refractivity
78.31 m3·mol-1
Polarizability
31.28 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
3
H Bond Donor Count
3
Physiological Charge
2
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Lisdexamfetamine is a pro-drug of dextroamphetamine. It works primarily by inducing the release of the neurotransmitters dopamine and norepinephrine from their storage areas in nerve terminals. Both of these transmitters contribute to maintaining alertness, increasing focus, and sustaining thought, effort, and motivation.
Cơ Chế Tác Dụng : Lisdexamfetamine (L-lysine-d-amphetamine) is a prodrug of the psychostimulant d-amphetamine coupled with the essential amino acid L-lysine. It was developed so that the amphetamine 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. Amphetamines target the trace amine-associated receptor 1 (TAAR1). Amphetamine is also believed to exert its effects by binding to the monoamine transporters (the dopamine transporter or DAT) and increasing extracellular levels of the biogenic amines dopamine, norepinephrine (noradrenaline) and serotonin. Lisdexamfetamine is a pro-drug of dextroamphetamine. Amphetamines are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space. Norepinephrine and dopamine contribute to maintaining alertness, increasing focus, and sustaining thought, effort, and motivation. However, the exact therapeutic action in ADHD is not known.
Dược Động Học :
▧ Absorption :
After oral administration, lisdexamfetamine is rapidly absorbed from the gastrointestinal tract.
▧ Metabolism :
Lisdexamfetamine is converted to dextroamphetamine and L-lysine, which is believed to occur by first-pass intestinal and/or hepatic metabolism. Lisdexamfetamine is not metabolized by cytochrome P450 enzymes.
▧ Half Life :
The plasma elimination half-life of lisdexamfetamine typically averaged less than one hour.
Độc Tính : Manifestations of acute overdosage with amphetamines include restlessness, tremor, hyperreflexia, rapid respiration, confusion, assaultiveness, hallucinations, panic states, hyperpyrexia and rhabdomyolysis. Fatigue and depression usually follow the central nervous system stimulation. Cardiovascular effects include arrhythmias, hypertension or hypotension and circulatory collapse. Gastrointestinal symptoms include nausea, vomiting, diarrhea, and abdominal cramps. Fatal poisoning is usually preceded by convulsions and coma.
Chỉ Định : For the treatment of Attention Deficit/Hyperactivity Disorder (ADHD) in pediatric populations aged 6 to 12 years.
Tương Tác Thuốc :
  • Tramadol Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Trandolapril Lisdexamfetamine may reduce the efficacy of Trandolapril.
  • Tranylcypromine The MAO inhibitor, Tranylcypromine, may increase the vasopressor effect of the amphetamine, Lisdexamfetamine. Concomitant therapy should be avoided.
  • Triprolidine Triprolidine may reduce the sedative effect of the antihistamine, Lisdexamfetamine.
Liều Lượng & Cách Dùng : Capsule, extended release - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Vyvanse 60 mg capsule
    Giá bán buôn : USD >5.02
    Đơn vị tính : capsule
  • Biệt dược thương mại : Vyvanse 20 mg capsule
    Giá bán buôn : USD >5.26
    Đơn vị tính : capsule
  • Biệt dược thương mại : Vyvanse 40 mg capsule
    Giá bán buôn : USD >5.8
    Đơn vị tính : capsule
  • Biệt dược thương mại : Vyvanse 70 mg capsule
    Giá bán buôn : USD >5.85
    Đơn vị tính : capsule
  • Biệt dược thương mại : Vyvanse 50 mg capsule
    Giá bán buôn : USD >6.02
    Đơn vị tính : capsule
  • Biệt dược thương mại : Vyvanse 30 mg capsule
    Giá bán buôn : USD >6.24
    Đơn vị tính : capsule
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01255
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=11597698
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505358
ChemSpider
http://www.chemspider.com/Chemical-Structure.9772458.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/59417-102-10
PharmGKB
http://www.pharmgkb.org/drug/PA164748975
Wikipedia
http://en.wikipedia.org/wiki/Lisdexamfetamine
RxList
http://www.rxlist.com/cgi/generic/vyvanse.htm
Drugs.com
http://www.drugs.com/cdi/lisdexamfetamine.html
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