Tìm theo
Levorphanol
Các tên gọi khác (5 ) :
  • Levorfanol
  • Levorfanolo
  • Lévorphanol
  • Levorphanol
  • Levorphanolum
Thuốc giảm đau có opioid
Thuốc Gốc
Small Molecule
CAS: 77-07-6
ĐG : Cardinal Health , http://www.cardinal.com
CTHH: C17H23NO
PTK: 257.3706
A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H23NO
Phân tử khối
257.3706
Monoisotopic mass
257.177964363
InChI
InChI=1S/C17H23NO/c1-18-9-8-17-7-3-2-4-14(17)16(18)10-12-5-6-13(19)11-15(12)17/h5-6,11,14,16,19H,2-4,7-10H2,1H3/t14-,16+,17+/m0/s1
InChI Key
InChIKey=JAQUASYNZVUNQP-USXIJHARSA-N
IUPAC Name
(1R,9R,10R)-17-methyl-17-azatetracyclo[7.5.3.0^{1,10}.0^{2,7}]heptadeca-2(7),3,5-trien-4-ol
Traditional IUPAC Name
levorphanol
SMILES
[H][C@@]12CCCC[C@@]11CCN(C)[C@@H]2CC2=C1C=C(O)C=C2
Độ tan chảy
198-199 °C
Độ hòa tan
1840 mg/L
logP
3.11
logS
-3.2
pKa (strongest acidic)
10.46
pKa (Strongest Basic)
9.66
PSA
23.47 Å2
Refractivity
78.08 m3·mol-1
Polarizability
29.84 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
9.58
Dược Lực Học : Levorphanol is a potent synthetic opioid analgesic indicated for the management of moderate to severe pain or as a preoperative medication where an opioid analgesic is appropriate. Levorphanol is similar to morphine in its actions, however it is up to 8 times more potent than morphine. Levorphanol produces a degree of respiratory depression similar to that produced by morphine at equianalgesic doses, and like many mu-opioid drugs, levorphanol produces euphoria or has a positive effect on mood in many individuals.
Cơ Chế Tác Dụng : A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection. [PubChem] Like other mu-agonist opioids it is believed to act at receptors in the periventricular and periaqueductal gray matter in both the brain and spinal cord to alter the transmission and perception of pain.
Dược Động Học :
▧ Absorption :
Levorphanol is well absorbed after PO administration with peak plasma concentrations occurring approximately 1 hour after dosing.
▧ Volume of Distribution :
* 10 to 13 L/kg
▧ Protein binding :
40%
▧ Metabolism :
Levorphanol is extensively metabolized in the liver and is eliminated as the glucuronide metabolite.
▧ Half Life :
11-16 hours
▧ Clearance :
* 0.78 to 1.1 L/kg/hr
Độc Tính : LD50=150 mg/kg (orally in rats). Signs of overdose include nausea, emesis, dizziness, respiratory depression, hypotension, urinary retention, cardiac arrhythmias, allergic reactions, skin rash, and uticaria.
Chỉ Định : For the management of moderate to severe pain or as a preoperative medication where an opioid analgesic is appropriate
Tương Tác Thuốc :
  • Alvimopan Increases levels by receptor binding competition. Discontinue opioid administration at least 7 days prior to administrating Alvimopan.
  • Eltrombopag Increases levels of Levorphanol via metabolism decrease. UDP-glucuronosyltransferase inhibition with unclear significance.
  • Triprolidine The CNS depressants, Triprolidine and Levorphanol, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Injection, solution - Intramuscular
Injection, solution - Intravenous
Injection, solution - Subcutaneous
Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Aromarone
  • Công ty :
    Sản phẩm biệt dược : Cetarin
  • Công ty :
    Sản phẩm biệt dược : Lemoran
  • Sản phẩm biệt dược : Levo-Dromoran
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00854
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C08014
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50017233
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0187-3072-10
PharmGKB
http://www.pharmgkb.org/drug/PA164744368
Wikipedia
http://en.wikipedia.org/wiki/Levorphanol
RxList
http://www.rxlist.com/cgi/generic2/levorphanol.htm
Drugs.com
http://www.drugs.com/cdi/levorphanol.html
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