Tìm theo
Salmeterol
Các tên gọi khác (9 ) :
  • GR-33343-X
  • GR-33343X
  • Salmaterol
  • Salmeterol
  • Salmeterolum
  • Serevent
  • Serevent diskus
  • SID144207133
  • SID26719802
sympathomimetics, adrenergic beta 2 receptor agonists, bronchodilator agents
Thuốc Gốc
Small Molecule
CAS: 89365-50-4
ATC: R03AC12
ĐG : A-S Medication Solutions LLC , http://orders.a-smeds.com
CTHH: C25H37NO4
PTK: 415.5656
Salmeterol is a long-acting beta2-adrenergic receptor agonist drug that is currently prescribed for the treatment of asthma and chronic obstructive pulmonary disease COPD.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C25H37NO4
Phân tử khối
415.5656
Monoisotopic mass
415.272258677
InChI
InChI=1S/C25H37NO4/c27-20-23-18-22(13-14-24(23)28)25(29)19-26-15-7-1-2-8-16-30-17-9-6-12-21-10-4-3-5-11-21/h3-5,10-11,13-14,18,25-29H,1-2,6-9,12,15-17,19-20H2
InChI Key
InChIKey=GIIZNNXWQWCKIB-UHFFFAOYSA-N
IUPAC Name
4-(1-hydroxy-2-{[6-(4-phenylbutoxy)hexyl]amino}ethyl)-2-(hydroxymethyl)phenol
Traditional IUPAC Name
salmeterol
SMILES
OCC1=C(O)C=CC(=C1)C(O)CNCCCCCCOCCCCC1=CC=CC=C1
Độ tan chảy
75.5-76.5 °C
Độ hòa tan
Sparingly soluble
logP
4.2
logS
-5.3
pKa (strongest acidic)
10.12
pKa (Strongest Basic)
9.4
PSA
81.95 Å2
Refractivity
122.39 m3·mol-1
Polarizability
50.6 Å3
Rotatable Bond Count
16
H Bond Acceptor Count
5
H Bond Donor Count
4
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Salmeterol is a long acting beta2-adrenoceptor agonist (LABA), usually only prescribed for severe persistent asthma following previous treatment with a short-acting beta agonist such as salbutamol and is prescribed concurrently with a corticosteroid, such as beclometasone. The primary noticable difference of salmeterol to salbutamol is that the duration of action lasts approximately 12 hours in comparison with 4-6 hours of salbutamol. When used regularly every day as presecribed, inhaled salmeterol decreases the number and severity of asthma attacks. However, it is not for use for relieving an asthma attack that has already started. Inhaled salmeterol works like other beta 2-agonists, causing bronchodilatation by relaxing the smooth muscle in the airway so as to treat the exacerbation of asthma. Salmeterol is similar in action to formoterol, however formoterol has been demonstrated to have a faster onset of action than salmeterol as a result of a lower lipophilicity, and has also been demonstrated to be more potent - a 12 µg dose of formoterol has been demonstrated to be equivalent to a 50 µg dose of salmeterol.
Cơ Chế Tác Dụng : Salmeterol is a long-acting beta2-adrenergic receptor agonist drug that is currently prescribed for the treatment of asthma and chronic obstructive pulmonary disease COPD. Salmeterol's long, lipophilic side chain binds to exosites near beta(2)-receptors in the lungs and on bronchiolar smooth muscle, allowing the active portion of the molecule to remain at the receptor site, continually binding and releasing. Beta(2)-receptor stimulation in the lung causes relaxation of bronchial smooth muscle, bronchodilation, and increased bronchial airflow.
Dược Động Học :
▧ Absorption :
Because of the small therapeutic dose, systemic levels of salmeterol are low or undetectable after inhalation of recommended doses.
▧ Protein binding :
96%
▧ Metabolism :
Hepatic, metabolized by hydroxylation via CYP3A4
▧ Half Life :
5.5 hours
Độc Tính : Symptoms of overdose include angina (chest pain), dizziness, dry mouth, fatigue, flu-like symptoms, headache, heart irregularities, high or low blood pressure, high blood sugar, insomnia, muscle cramps, nausea, nervousness, rapid heartbeat, seizures, and tremor. By the oral route, no deaths occurred in rats at 1,000 mg/kg (approximately 81,000 times the maximum recommended daily inhalation dose in adults and approximately 38,000 times the maximum recommended daily inhalation dose in children on a mg/m2 basis).
Chỉ Định : For the treatment of asthma and chronic obstructive pulmonary disease (COPD).
Tương Tác Thuốc :
  • Acebutolol Antagonism
  • Atenolol Antagonism
  • Bisoprolol Antagonism
  • Carvedilol Antagonism
  • Conivaptan CYP3A4 Inhibitors (Strong) may increase the serum concentration of Salmeterol. Concurrent use of salmeterol with strong inhibitors of CYP3A4 is not recommended according to salmeterol prescribing information.
  • Esmolol Antagonism
  • Indacaterol Concomitant use with other inhaled, long acting beta2-adrenergic drugs may result in an overdose. Adverse cardiovascular effects and fatalities have been associated with excessive use of inhaled sympathomimetic drugs.
  • Labetalol Antagonism
  • Metoprolol Antagonism
  • Nadolol Antagonism
  • Oxprenolol Antagonism
  • Pindolol Antagonism
  • Propranolol Antagonism
  • Quinupristin This combination presents an increased risk of toxicity
  • Telithromycin Telithromycin may reduce clearance of Salmeterol. Concomitant therapy is contraindicated.
  • Timolol Antagonism
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor may increase the serum concentration of salmeterol by decreasing its metabolism. Consider alternate therapy.
Liều Lượng & Cách Dùng : Powder - Respiratory (inhalation)
Powder - Respiratory (inhalation)
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Aeromax Diskus
  • Công ty :
    Sản phẩm biệt dược : Arial
  • Công ty :
    Sản phẩm biệt dược : Salmetedur
  • Công ty :
    Sản phẩm biệt dược : Serevent
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00938
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5152
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508024
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07241
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D05792
ChemSpider
http://www.chemspider.com/Chemical-Structure.4968.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=25771
PharmGKB
http://www.pharmgkb.org/drug/PA451300
Wikipedia
http://en.wikipedia.org/wiki/Salmeterol
RxList
http://www.rxlist.com/cgi/generic/salmeterol.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/ser1401.shtml
Drugs.com
http://www.drugs.com/cdi/salmeterol.html
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