Tìm theo
Atomoxetine
Các tên gọi khác (4 ) :
  • (-)-Tomoxetine
  • Tomoxetina
  • Tomoxetine
  • Tomoxetinum
adrenergic uptake inhibitors, antidepressive agents
Thuốc Gốc
Small Molecule
CAS: 82248-59-7
ATC: N06BA09
ĐG : Atlantic Biologicals Corporation , http://www.atlanticbiologicals.com
CTHH: C17H21NO
PTK: 255.3547
Atomoxetine is the first non-stimulant drug approved for the treatment of attention-deficit hyperactivity disorder (ADHD). It is sold in the form of the hydrochloride salt of atomoxetine. This chemical is manufactured and marketed under the brand name Strattera; by Eli Lilly and Company and as a generic Attentin by Torrent Pharmaceuticals. There is currently no generic available within the United States due to patent restrictions. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H21NO
Phân tử khối
255.3547
Monoisotopic mass
255.162314299
InChI
InChI=1S/C17H21NO/c1-14-8-6-7-11-16(14)19-17(12-13-18-2)15-9-4-3-5-10-15/h3-11,17-18H,12-13H2,1-2H3/t17-/m1/s1
InChI Key
InChIKey=VHGCDTVCOLNTBX-QGZVFWFLSA-N
IUPAC Name
methyl[(3R)-3-(2-methylphenoxy)-3-phenylpropyl]amine
Traditional IUPAC Name
atomoxetine
SMILES
CNCC[C@@H](OC1=CC=CC=C1C)C1=CC=CC=C1
Độ hòa tan
27.8 mg/mL
logP
3.9
logS
-4.8
pKa (Strongest Basic)
9.8
PSA
21.26 Å2
Refractivity
79.44 m3·mol-1
Polarizability
29.79 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Atomoxetine is the first non-stimulant drug approved for the treatment of attention-deficit hyperactivity disorder (ADHD). Atomoxetine is classified as a norepinephrine reuptake inhibitor, and is approved for use in children, adolescents, and adults. However, its efficacy has not been studied in children under six years old. Its advantage over stimulants for the treatment of ADHD is that it has less abuse potential than stimulants, is not scheduled as a controlled substance and has proven in clinical trials to offer 24 hour coverage of symptoms associated with ADHD in adults and children.
Cơ Chế Tác Dụng : Atomoxetine is the first non-stimulant drug approved for the treatment of attention-deficit hyperactivity disorder (ADHD). It is sold in the form of the hydrochloride salt of atomoxetine. This chemical is manufactured and marketed under the brand name Strattera; by Eli Lilly and Company and as a generic Attentin by Torrent Pharmaceuticals. There is currently no generic available within the United States due to patent restrictions. [Wikipedia] The precise mechanism by which atomoxetine produces its therapeutic effects in Attention-Deficit/Hyperactivity Disorder (ADHD) is unknown, but is thought to be related to selective inhibition of the pre-synaptic norepinephrine transporter, as determined through in-vitro studies. Atomoxetine appears to have minimal affinity for other noradrenergic receptors or for other neurotransmitter transporters or receptors.
Dược Động Học :
▧ Absorption :
Atomoxetine is rapidly absorbed after oral administration, with absolute bioavailability of about 63% in EMs and 94% in PMs. Drugs that elevate gastric pH (magnesium hydroxide/aluminum hydroxide, omeprazole) have no effect on atomoxetine bioavailability. Absorption is minimally affected by food.
▧ Volume of Distribution :
* 0.85 L/kg
▧ Protein binding :
At therapeutic concentrations, 98% of atomoxetine in plasma is bound to protein, primarily albumin.
▧ Metabolism :
Atomoxetine is primarily metabolized by the CYP2D6 pathway to 4-hydroxyatomoxetine. 4-Hydroxyatomoxetine is equipotent to atomoxetine as an inhibitor of the norepinephrine transporter but circulates in plasma at much lower concentrations (1% of atomoxetine concentration in EMs and 0.1% of atomoxetine concentration in PMs).
▧ Half Life :
5 hours
▧ Clearance :
* 0.35 L/hr/kg [after oral administration in adult extensive metabolizers] * 0.03 L/hr/kg [administration of atomoxetine to poor metabolizers]
Độc Tính : The most commonly reported symptoms accompanying acute and chronic overdoses are somnolence, agitation, hyperactivity, abnormal behavior, and gastrointestinal symptoms.
Chỉ Định : For the treatment of Attention-Deficit/Hyperactivity Disorder (ADHD) alone or in combination with behavioral treatment, as an adjunct to psychological, educational, social, and other remedial measures.
Tương Tác Thuốc :
  • Amiodarone The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
  • Chloroquine The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
  • Cocaine CYP2D6 Inhibitors (Strong) such as cocaine may increase the serum concentration of atomoxetine. Initiate atomoxetine at a reduced dose (patients up to 70kg: 0.5mg/kg/day; patients 70kg or more: 40mg/day) in patients receiving a strong CYP2D6 inhibitor. The dose should only be increased to usual doses if symptoms fail to improve after 4 weeks. Patients established on atomoxetine therapy may require dosage reductions and should be monitored for increased levels/adverse effects with initiation/dose increase of a strong CYP2D6 inhibitor.
  • Dextropropoxyphene The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
  • Diphenhydramine Diphenhydramine, a moderate CYP2D6 inhibitor, may increase the therapeutic and adverse effects of atomoxetine by decreasing its metabolism.
  • Fluoxetine The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
  • Fluphenazine Risk of additive CNS depressant effects. Monitor for increased CNS depression during concomitant therapy.
  • Haloperidol The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
  • Isocarboxazid Possible severe adverse reaction with this combination
  • Lomustine The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
  • Mibefradil The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
  • Paroxetine The CYP2D6 inhibitor, paroxetine, may increase the effect and toxicity of atomoxetine.
  • Perphenazine The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
  • Phenelzine Possible severe adverse reaction with this combination
  • Quinacrine The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
  • Quinidine The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
  • Quinidine barbiturate The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
  • Quinine The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
  • Rasagiline Possible severe adverse reaction with this combination
  • Ritonavir The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
  • Terbinafine Terbinafine, a CYP2D6 inhibitor, may reduce the metabolism and clearance of Atomoxetine. Consider alternate therapy or monitor for therapeutic/adverse effects of Atomoxetine if Terbinafine is initiated, discontinued or dose changed.
  • Thioridazine The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
  • Tranylcypromine The MAO inhibitor, Tranylcypromine, may increase the central neurotoxic effects of the Atomoxetine. These agents should not be administered within 14 days of each other.
  • Triprolidine The CNS depressants, Triprolidine and Atomoxetine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Vinorelbine The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
  • Yohimbine The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Liều Lượng & Cách Dùng : Capsule - Oral
Capsule - Oral - 10 mg
Capsule - Oral - 18 mg
Capsule - Oral - 25 mg
Capsule - Oral - 40 mg
Capsule - Oral - 60 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Attentin
  • Sản phẩm biệt dược : Strattera
  • Công ty :
    Sản phẩm biệt dược : Tomoxetin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00289
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=54841
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506160
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02574
ChemSpider
http://www.chemspider.com/Chemical-Structure.49516.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50133749
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0002-3227-30
PharmGKB
http://www.pharmgkb.org/drug/PA134688071
Wikipedia
http://en.wikipedia.org/wiki/Atomoxetine
RxList
http://www.rxlist.com/cgi/generic3/strattera.htm
Drugs.com
http://www.drugs.com/cdi/atomoxetine.html
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