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Lorazepam
Các tên gọi khác (7 ) :
  • (±)-Lorazepam
  • Ativan
  • Lormetazepam
  • Methyllorazepam
  • N-Methyllorazepam
  • O-Chlorooxazepam
  • O-Chloroxazepam
Thuốc điều trị về tâm thần
Thuốc Gốc
Small Molecule
CAS: 846-49-1
ATC: N05BA06
ĐG : Actavis Group , http://www.actavis.com
CTHH: C15H10Cl2N2O2
PTK: 321.158
A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H10Cl2N2O2
Phân tử khối
321.158
Monoisotopic mass
320.011932988
InChI
InChI=1S/C15H10Cl2N2O2/c16-8-5-6-12-10(7-8)13(19-15(21)14(20)18-12)9-3-1-2-4-11(9)17/h1-7,15,21H,(H,18,20)
InChI Key
InChIKey=DIWRORZWFLOCLC-UHFFFAOYSA-N
IUPAC Name
7-chloro-5-(2-chlorophenyl)-3-hydroxy-2,3-dihydro-1H-1,4-benzodiazepin-2-one
Traditional IUPAC Name
lorazepam
SMILES
OC1N=C(C2=CC=CC=C2Cl)C2=C(NC1=O)C=CC(Cl)=C2
Độ tan chảy
192-194
Độ hòa tan
80 mg/L
logP
2.39
logS
-3.6
pKa (strongest acidic)
10.61
pKa (Strongest Basic)
-2.2
PSA
61.69 Å2
Refractivity
82.7 m3·mol-1
Polarizability
30.33 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
13
Dược Lực Học : Lorazepam, a benzodiazepine not transformed to active metabolites, is used to treat anxiety, status epilepticus, and for sedation induction and anterograde amnesia.
Cơ Chế Tác Dụng : A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent. [PubChem] Lorazepam binds to an allosteric site on GABA-A receptors, which are pentameric ionotropic receptors in the CNS. Binding potentiates the effects of the inhibitory neurotransmitter GABA, which upon binding opens the chloride channel in the receptor, allowing chloride influx and causing hyperpolerization of the neuron.
Dược Động Học :
▧ Absorption :
Readily absorbed with an absolute bioavailability of 90% when given orally. When intramuscularly administered, lorazepam is completely and rapidly absorbed. It achieves max serum concentration in 3 hours. The max serum concentration of a 4 mg dose is 48 ng/mL.
▧ Volume of Distribution :
1.3 L/kg. Unbound lorazepam can cross the blood-brain-barrier via passive diffusion.
▧ Protein binding :
91±2% bound to plasma proteins when given parenterally. When given orally, it is 85% bound to plasma proteins.
▧ Metabolism :
Lorazepam is hepatically metabolized and is extensively conjugated to the 3-0-phenolic glucuronide. This is an inactive metabolite and is eliminated mainly by the kidneys.
▧ Route of Elimination :
When a single 2 mg oral dose is give to healthy subjects, 88±4% of the administered dose was recovered in urine and 7±2% was recovered in feces. The percent of administered dose recovered in urine as lorazepam glucuronide was 74±4%. Only 0.3% of the dose was recovered as unchanged lorazepam, and the remainder of the radioactivity represented minor metabolites.
▧ Half Life :
Parenteral administration = 14±5 hours; Oral administration = 2 hours.
▧ Clearance :
Total clearance, parenteral administration = 1.1±0.4 mL/min/kg.
Độc Tính : The most important clinical adverse event caused by lorazepam is respiratory depression. LD50, mouse, oral = 1850 mg/kg.
Chỉ Định : For the management of anxiety disorders, and for treatment of status epilepticus.
Tương Tác Thuốc :
  • Clozapine Increased risk of toxicity
  • Kava Kava may increase the effect of the benzodiazepine, lorazepam.
  • Triprolidine The CNS depressants, Triprolidine and Lorazepam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Valproic Acid Valproic acid may increase the serum concentration of Lorazepam by reducing Lorazepam metabolism. The Lorazepam dose should be reduced by 50% during concomitant therapy. Monitor for increased Lorazepam effects and toxicity.
Liều Lượng & Cách Dùng : Injection, solution - Parenteral - 2 mg/mL, 4 mg/mL
Solution, concentrate - Oral - 2 mg/mL
Tablet - Oral - 0.5 mg, 1 mg, 2 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Psyco Remedies
    Sản phẩm biệt dược : Almazine
  • Công ty : U-Liang
    Sản phẩm biệt dược : Anxiedin
  • Công ty : Wyeth
    Sản phẩm biệt dược : Ativan
  • Công ty : Novartis
    Sản phẩm biệt dược : Idalprem
  • Công ty :
    Sản phẩm biệt dược : Lorabenz
  • Công ty : Belupo
    Sản phẩm biệt dược : Lorsilan
  • Công ty :
    Sản phẩm biệt dược : Somagerol
  • Công ty : Wyeth
    Sản phẩm biệt dược : Temesta
  • Công ty : Wyeth KK
    Sản phẩm biệt dược : Wypax
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00186
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3958
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508468
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00365
ChemSpider
http://www.chemspider.com/Chemical-Structure.3821.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0054-3532-44
PharmGKB
http://www.pharmgkb.org/drug/PA450267
Wikipedia
http://en.wikipedia.org/wiki/Lorazepam
RxList
http://www.rxlist.com/cgi/generic/loraz.htm
Drugs.com
http://www.drugs.com/lorazepam.html
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