Tìm theo
Lofexidine
Các tên gọi khác (3) :
  • 2-(alpha-(2,6-Dichlorophenoxy)ethyl)2-imidazoline
  • Lofexidina
  • Lofexidinum
antihypertensive agents, adrenergic alpha 2 receptor agonists, narcotic antagonists
Thuốc Gốc
Small Molecule
CAS: 31036-80-3
ATC: N07BC04
CTHH: C11H12Cl2N2O
PTK: 259.132
Lofexidine is an alpha2-adrenergic receptor agonist. It can be used as a short acting anti-hypertensive, but is mostly used to help relieve symptoms of heroin or opiate withdrawal in opiate dependency. It is approved in the United Kingdom, but is still undergoing clinical trials in the United States.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C11H12Cl2N2O
Phân tử khối
259.132
Monoisotopic mass
258.03266843
InChI
InChI=1S/C11H12Cl2N2O/c1-7(11-14-5-6-15-11)16-10-8(12)3-2-4-9(10)13/h2-4,7H,5-6H2,1H3,(H,14,15)
InChI Key
InChIKey=KSMAGQUYOIHWFS-UHFFFAOYSA-N
IUPAC Name
2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole
Traditional IUPAC Name
lofexidine
SMILES
CC(OC1=C(Cl)C=CC=C1Cl)C1=NCCN1
Độ tan chảy
221-223
Độ hòa tan
1.47e-01 g/l
logP
2.66
logS
-3.2
pKa (Strongest Basic)
7.67
PSA
33.62 Å2
Refractivity
64.41 m3·mol-1
Polarizability
25.11 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Lofexidine is an orally active imidazoline adrenergic alpha-2-receptor agonist; and is believed to have a high affinity for 2A receptor subtypes resulting in less anti-hypertensive activity than clonidine, a non-selective alpha-2-receptor agonist. Hypotension may occur in susceptible subjects, accompanied by a decrease in heart rate. Abrupt discontinuation of lofexidine has been, in some cases, associated with a transient increase in blood pressure to higher than pre-treatment levels. It selectively stimulates receptors in the brain that monitor catecholamine levels in the blood. These receptors close a negative feedback loop that begins with descending sympathetic nerves from the brain that control the production of catecholamines (epinephrine, also known as adrenaline, and norepinephrine) in the adrenal medulla. By fooling the brain into believing that catecholamine levels are higher than they really are, lofexidine causes the brain to reduce its signals to the adrenal medulla, which in turn lowers catecholamine production and blood levels. The result is a lowered heart rate and blood pressure. This central action is responsible for the suppression of opiate withdrawal symptoms.
Cơ Chế Tác Dụng : Lofexidine is an alpha2-adrenergic receptor agonist. It can be used as a short acting anti-hypertensive, but is mostly used to help relieve symptoms of heroin or opiate withdrawal in opiate dependency. It is approved in the United Kingdom, but is still undergoing clinical trials in the United States. Lofexidine is an alpha2-adrenergic receptor agonist.
Dược Động Học :
▧ Absorption :
Lofexidine is extensively absorbed and achieves peak plasma concentration at 3 hours after administration of a single dose. Bioavailability is over 90% following oral administration.
▧ Protein binding :
80 to 90%
▧ Metabolism :
Lofexidine undergoes extensive metabolism in the liver and excretion is mainly by the kidney.
▧ Half Life :
11 hours
Độc Tính : Lofexidine was tolerated at high dosage in singe dose toxicity studies in animals, the LD50 being >77 mg/kg. With repeat dosing in mice, rats and dogs symptoms related to the pharmacology of the drug (ataxia, sedation, tremor, unkempt appearance and exhaustion) appeared. Overdosage may cause hypotension, bradycardia and sedation.
Chỉ Định : Investigated for use/treatment in addictions and substance abuse.
Liều Lượng & Cách Dùng : Tablet, film coated - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Britannia
    Sản phẩm biệt dược : Britlofex
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04948
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=30668
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508453
ChemSpider
http://www.chemspider.com/Chemical-Structure.28460.html
PharmGKB
http://www.pharmgkb.org/drug/PA164744510
Wikipedia
http://en.wikipedia.org/wiki/Lofexidine
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