Tìm theo
Ramelteon
Các tên gọi khác (1) :
  • Rozerem
Thuốc Gốc
Small Molecule
CAS: 196597-26-9
ĐG : Bryant Ranch Prepack , http://bryantranchprepack.com
CTHH: C16H21NO2
PTK: 259.3434
Ramelteon is the first in a new class of sleep agents that selectively binds to the melatonin receptors in the suprachiasmatic nucleus (SCN). It is used for insomnia, particularly delayed sleep onset. Ramelteon has not been shown to produce dependence and has shown no potential for abuse.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H21NO2
Phân tử khối
259.3434
Monoisotopic mass
259.157228921
InChI
InChI=1S/C16H21NO2/c1-2-15(18)17-9-7-12-4-3-11-5-6-14-13(16(11)12)8-10-19-14/h5-6,12H,2-4,7-10H2,1H3,(H,17,18)/t12-/m0/s1
InChI Key
InChIKey=YLXDSYKOBKBWJQ-LBPRGKRZSA-N
IUPAC Name
N-{2-[(8S)-1H,2H,6H,7H,8H-indeno[5,4-b]furan-8-yl]ethyl}propanamide
Traditional IUPAC Name
ramelteon
SMILES
CCC(=O)NCC[C@@H]1CCC2=C1C1=C(OCC1)C=C2
Độ hòa tan
1.64e-02 g/l
logP
2.4
logS
-4.2
pKa (strongest acidic)
15.82
pKa (Strongest Basic)
-0.4
PSA
38.33 Å2
Refractivity
75.52 m3·mol-1
Polarizability
29.99 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Ramelteon is the first selective melatonin agonist. It works by mimicking melatonin (MT), a naturally occuring hormone that is produced during the sleep period and thought to be responsible for the regulation of circadian rhythm underlying the normal sleep-wake cycle. Ramelteon has a high affinity for the MT1 and MT2 receptors. The MT1 and MT2 receptors are located in the brain's suprachiasmatic nuclei (SCN),which is known as the body's "master clock" because it regulates the 24-hour sleep-wake cycle. Ramelteon has an active metabolite that is less potent but circulates in higher concentrations than the parent compound. The metabolite also has weak affinity for the 5HT2b receptor.
Cơ Chế Tác Dụng : Ramelteon is the first in a new class of sleep agents that selectively binds to the melatonin receptors in the suprachiasmatic nucleus (SCN). It is used for insomnia, particularly delayed sleep onset. Ramelteon has not been shown to produce dependence and has shown no potential for abuse. Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 and MT2 receptors, and lower selectivity for the MT3 receptor. Melatonin production is concurrent with nocturnal sleep, meaning that an increase in melatonin levels is related to the onset of self-reported sleepiness and an increase in sleep propensity. MT1 receptors are believed to be responsible for regulation of sleepiness and facilitation of sleep onset, and MT2 receptors are believed to mediate phase-shifting effects of melatonin on the circadian rhythm. While MT1 and MT2 receptors are associated with the sleep-wake cycle, MT3 has a completely different profile, and therefore is not likely to be involved in the sleep-wake cycle. Remelteon has no appreciable affinity for the gamma-aminobutyric acid (GABA) receptor complex or receptors that bind neuropeptides, cytokines, serotonin, dopamine, norepinephrine, acetylcholine, or opiates.
Dược Động Học :
▧ Absorption :
Rapid, total absorption is at least 84%.
▧ Volume of Distribution :
* 73.6 L
▧ Protein binding :
~82% (in human serum)
▧ Metabolism :
Hepatic
▧ Route of Elimination :
Following oral administration of radiolabeled ramelteon, 84% of total radioactivity was excreted in urine and approximately 4% in feces, resulting in a mean recovery of 88%. Less than 0.1% of the dose was excreted in urine and feces as the parent compound.
▧ Half Life :
~1-2.6 hours
Chỉ Định : For the treatment of insomnia characterized by difficulty with sleep onset.
Tương Tác Thuốc :
  • Atazanavir Atazanavir increases levels/toxicity of ramelteon
  • Ciprofloxacin Ciprofloxacin increases levels/toxicity of ramelteon
  • Enoxacin Enoxacin increases levels/toxicity of ramelteon
  • Fluconazole Fluconazole may increase the serum levels and toxcity of ramelteon.
  • Fluvoxamine Fluvoxamine may increase the serum level and toxicity of ramelteon.
  • Ketoconazole Ketoconazole may increase the serum levels and toxicity of ramelteon.
  • Mexiletine Mexiletine increases levels/toxicity of ramelteon
  • Rifampicin Rifampin reduces the levels/effect of ramelteon
  • Tacrine Tacrine increases levels/toxicity of ramelteon
  • Thiabendazole Thiabendazole increases levels/toxicity of ramelteon
  • Triprolidine The CNS depressants, Triprolidine and Ramelteon, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Zileuton Zileuton increases levels/toxicity of ramelteon
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Rozerem 8 mg tablet
    Giá bán buôn : USD >5.17
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Rozerem
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00980
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=208902
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505923
ChemSpider
http://www.chemspider.com/Chemical-Structure.181000.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50118470
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/64764-805-30
PharmGKB
http://www.pharmgkb.org/drug/PA164744896
Wikipedia
http://en.wikipedia.org/wiki/Ramelteon
RxList
http://www.rxlist.com/cgi/generic4/rozerem.htm
Drugs.com
http://www.drugs.com/cdi/ramelteon.html
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