Tìm theo
Naloxone
Các tên gọi khác (9 ) :
  • 1-N-Allyl-14-hydroxynordihydromorphinone
  • 17-Allyl-3,14-dihydroxy-4,5alpha-epoxymorphinan-6-one
  • EN 1530 Base
  • L-Naloxone
  • N-Allylnoroxymorphone
  • Nalossone
  • Naloxona
  • Naloxone
  • Naloxonum
narcotic antagonists, central nervous system depressants
Thuốc Gốc
Small Molecule
CAS: 465-65-6
ATC: V03AB15
ĐG : Amphastar Pharmaceuticals , http://www.amphastar.com
CTHH: C19H21NO4
PTK: 327.3743
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H21NO4
Phân tử khối
327.3743
Monoisotopic mass
327.147058165
InChI
InChI=1S/C19H21NO4/c1-2-8-20-9-7-18-15-11-3-4-12(21)16(15)24-17(18)13(22)5-6-19(18,23)14(20)10-11/h2-4,14,17,21,23H,1,5-10H2/t14-,17+,18+,19-/m1/s1
InChI Key
InChIKey=UZHSEJADLWPNLE-GRGSLBFTSA-N
IUPAC Name
(1S,5R,13R,17S)-10,17-dihydroxy-4-(prop-2-en-1-yl)-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7(18),8,10-trien-14-one
Traditional IUPAC Name
naloxone
SMILES
[H][C@@]12OC3=C(O)C=CC4=C3[C@@]11CCN(CC=C)[C@]([H])(C4)[C@]1(O)CCC2=O
Độ tan chảy
200-205 °C
Độ hòa tan
Soluble
logP
2.09
logS
-1.8
pKa (strongest acidic)
7.27
pKa (Strongest Basic)
10.63
PSA
70 Å2
Refractivity
88.72 m3·mol-1
Polarizability
33.8 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
5
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
5
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Naloxone is an opiate antagonist and prevents or reverses the effects of opioids including respiratory depression, sedation and hypotension. Also, it can reverse the psychotomimetic and dysphoric effects of agonist-antagonists such as pentazocine. Naloxone is an essentially pure narcotic antagonist, i.e., it does not possess the "agonistic" or morphine-like properties characteristic of other narcotic antagonists; naloxone does not produce respiratory depression, psychotomimetic effects or pupillary constriction. In the absence of narcotics or agonistic effects of other narcotic antagonists, it exhibits essentially no pharmacologic activity. When given intravenously, the onset of action is apparent within 2 minutes. The onset of action is slower if given subcutaneously or intramuscularly. The duration of action also differs between sites of injection and dose.
Cơ Chế Tác Dụng : A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors. [PubChem] While the mechanism of action of naloxone is not fully understood, the preponderance of evidence suggests that naloxone antagonizes the opioid effects by competing for the same receptor sites, especially the opioid mu receptor. Recently, naloxone has been shown to bind all three opioid receptors (mu, kappa and gamma) but the strongest binding is to the mu receptor.
Dược Động Học :
▧ Absorption :
Well absorbed following intramuscular injection.
▧ Volume of Distribution :
Following parenteral administration naloxone hydrochloride is rapidly distributed in the body. Naloxone is also very lipophillic and easily crosses the blood-brain-barrier. It can also cross the placenta.
▧ Protein binding :
Plasma protein binding occurs but is relatively weak. Plasma albumin is the major binding constituent but significant binding of naloxone also occurs to plasma constituents other than albumin.
▧ Metabolism :
Naloxone is hepatically metabolized and primarily undergoes glucuronidation to form naloxone-3-glucuronide.
▧ Route of Elimination :
Urine (25%- 40% is excreted as metabolites within 6 hours)
▧ Half Life :
Adults = 30-81 minutes; Neonates = 3.1 ± 0.5 hours.
Độc Tính : LD50, IV administration, mouse = 150 ± 5 mg/kg; LD50, IV administration, rat = 109 ± 4 mg/kg;
Chỉ Định : For the complete or partial reversal of narcotic depression, including respiratory depression, induced by opioids including natural and synthetic narcotics, propoxyphene, methadone and the narcotic-antagonist analgesics: nalbuphine, pentazocine and butorphanol. It is also indicated for the diagnosis of suspected acute opioid overdose. It may also be used as an adjunctive agent to increase blood pressure in the management of septic shock.
Liều Lượng & Cách Dùng : Injection, solution - Parenteral - 0.4 mg/mL, 1 mg/mL
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Evzio
  • Công ty :
    Sản phẩm biệt dược : Nalone
  • Công ty :
    Sản phẩm biệt dược : Narcan
  • Công ty :
    Sản phẩm biệt dược : Narcanti
  • Công ty :
    Sản phẩm biệt dược : Narcon
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01183
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5284596
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508816
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07252
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08249
ChemSpider
http://www.chemspider.com/Chemical-Structure.4447644.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0409-1782-69
PharmGKB
http://www.pharmgkb.org/drug/PA450586
Wikipedia
http://en.wikipedia.org/wiki/Naloxone
RxList
http://www.rxlist.com/cgi/generic3/naloxone.htm
Drugs.com
http://www.drugs.com/cdi/naloxone.html
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