Tìm theo
Loratadine
Các tên gọi khác (3) :
  • Claritin
  • Loratadina
  • Loratadinum
Thuốc chống dị ứng & dùng trong các trường hợp quá mẫn
Thuốc Gốc
Small Molecule
CAS: 79794-75-5
ATC: R06AX13, R06AX27, C09AA03
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C22H23ClN2O2
PTK: 382.883
Loratadine is a derivative of azatadine and a second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (histamine H1 antagonists) it lacks central nervous system depressing effects such as drowsiness. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H23ClN2O2
Phân tử khối
382.883
Monoisotopic mass
382.144805697
InChI
InChI=1S/C22H23ClN2O2/c1-2-27-22(26)25-12-9-15(10-13-25)20-19-8-7-18(23)14-17(19)6-5-16-4-3-11-24-21(16)20/h3-4,7-8,11,14H,2,5-6,9-10,12-13H2,1H3
InChI Key
InChIKey=JCCNYMKQOSZNPW-UHFFFAOYSA-N
IUPAC Name
ethyl 4-{13-chloro-4-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,12,14-hexaen-2-ylidene}piperidine-1-carboxylate
Traditional IUPAC Name
loratadine
SMILES
CCOC(=O)N1CCC(CC1)=C1C2=C(CCC3=C1N=CC=C3)C=C(Cl)C=C2
Độ tan chảy
134-136 °C
Độ hòa tan
0.000011 mg/ml
logP
5.20
logS
-4.5
pKa (Strongest Basic)
4.33
PSA
42.43 Å2
Refractivity
116.98 m3·mol-1
Polarizability
41.67 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Loratadine is a long acting second generation antihistamine that is similar in structure to cyproheptadine and azatadine. The pharmacology of loratadine is similar to other antihistamines, but unlike other H1-blockers, loratidine is shown to exhibit competitive, specific, and selective antagonism of H1 receptors. The exact mechanism of this interaction is unknown, but disposition of the drug suggests that loratadine's prolonged antagonism of histamine may be due to the drug's slow dissociation from the receptor or the formation of the active metabolite, desloratadine. Loratadine does not penetrate the CNS effectively and has a low affinity for CNS H1-receptors.
Cơ Chế Tác Dụng : Loratadine is a derivative of azatadine and a second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (histamine H1 antagonists) it lacks central nervous system depressing effects such as drowsiness. [PubChem] Loratadine competes with free histamine and exhibits specific, selective peripheral H1 antagonistic activity. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms (eg. nasal congestion, watery eyes) brought on by histamine. Loratadine has low affinity for cholinergic receptors and does not exhibit any appreciable alpha-adrenergic blocking activity in-vitro. Loratadine also appears to suppress the release of histamine and leukotrienes from animal mast cells, and the release of leukotrienes from human lung fragments, although the clinical importance of this is unknown.
Dược Động Học :
▧ Absorption :
Rapidly absorbed following oral administration (40% bioavailability)
▧ Protein binding :
97-99%
▧ Metabolism :
Hepatic
▧ Half Life :
8.4 hours
Độc Tính : somnolence, tachycardia, and headache LD50=mg/kg (orally in rat)
Chỉ Định : A self-medication that is used alone or in combination with pseudoephedrine sulfate for the symptomatic relief of seasonal allergic rhinitis. Also used for the symptomatic relief of pruritus, erythema, and urticaria associated with chronic idiopathic urticaria in patients (not for children under 6 unless directed by a clincian).
Tương Tác Thuốc :
  • Nefazodone Increased risk of cardiotoxicity
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Loratadine, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
  • Trimethobenzamide Trimethobenzamide and Loratadine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Loratadine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
  • Trospium Trospium and Loratadine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Syrup - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
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    Sản phẩm biệt dược : Loratadine antihistamine
  • Công ty :
    Sản phẩm biệt dược : Loratyne
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    Sản phẩm biệt dược : Loritine
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    Sản phẩm biệt dược : Sensibit
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00455
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3957
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507853
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00364
ChemSpider
http://www.chemspider.com/Chemical-Structure.3820.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=22876
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-1925-01
PharmGKB
http://www.pharmgkb.org/drug/PA450266
Wikipedia
http://en.wikipedia.org/wiki/Loratadine
RxList
http://www.rxlist.com/cgi/generic/lorat.htm
Drugs.com
http://www.drugs.com/cdi/loratadine.html
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