Tìm theo
Pentamidine
Các tên gọi khác (10 ) :
  • 1,5-Bis(4-amidinophenoxy)pentane
  • 4,4'-(1,5-Pentanediylbis(oxy))bis-benzenecarboximidamide
  • 4,4'-(Pentamethylenedioxy)dibenzamidine
  • 4,4'-Diamidinodiphenoxypentane
  • P,P'-(pentamethylenedioxy)dibenzamidine
  • Pentamidin
  • Pentamidina
  • Pentamidindiisetionat
  • Pentamidine
  • Pentamidinum
antifungal agents, antiprotozoal agents, trypanocidal agents
Thuốc Gốc
Small Molecule
CAS: 100-33-4
ATC: P01CX01
ĐG : APP Pharmaceuticals , http://www.apppharma.com
CTHH: C19H24N4O2
PTK: 340.4195
Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of pneumocystis pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H24N4O2
Phân tử khối
340.4195
Monoisotopic mass
340.189926032
InChI
InChI=1S/C19H24N4O2/c20-18(21)14-4-8-16(9-5-14)24-12-2-1-3-13-25-17-10-6-15(7-11-17)19(22)23/h4-11H,1-3,12-13H2,(H3,20,21)(H3,22,23)
InChI Key
InChIKey=XDRYMKDFEDOLFX-UHFFFAOYSA-N
IUPAC Name
4-{[5-(4-carbamimidoylphenoxy)pentyl]oxy}benzene-1-carboximidamide
Traditional IUPAC Name
pentamidine
SMILES
NC(=N)C1=CC=C(OCCCCCOC2=CC=C(C=C2)C(N)=N)C=C1
Độ tan chảy
186.0 °C (decomposes)
Độ hòa tan
Complete
logP
4
logS
-4.2
pKa (Strongest Basic)
12.13
PSA
118.2 Å2
Refractivity
120.53 m3·mol-1
Polarizability
38.85 Å3
Rotatable Bond Count
10
H Bond Acceptor Count
6
H Bond Donor Count
4
Physiological Charge
2
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Pentamidine is an antiprotozoal agent. It is an aromatic diamidine, and is known to have activity against Pneumocystis carinii. The exact nature of its antiprotozoal action is unknown. in vitro studies with mammalian tissues and the protozoan Crithidia oncopelti indicate that the drug interferes with nuclear metabolism producing inhibition of the synthesis of DNA, RNA, phospholipids and proteins. Little is known about the drug's pharmacokinetics. The medication is also useful in Leishmaniasis and in prophylaxis against sleeping sickness caused by Trypanosoma brucei gambiense. Hydration before treatment lessens the incidence and severity of side effects, which include liver or kidney dysfunction, hypertension, hypotension, hypoglycemia, hypocalemia, leukopenia, thrombcytopenia, anemia, and allergic reaction. It is generally well-tolerated.
Cơ Chế Tác Dụng : Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of pneumocystis pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects. [PubChem] The mode of action of pentamidine is not fully understood. It is thought that the drug interferes with nuclear metabolism producing inhibition of the synthesis of DNA, RNA, phospholipids, and proteins.
Dược Động Học :
▧ Absorption :
Absorbed poorly through the gastrointestinal tract and is usually administered parenterally.
▧ Protein binding :
69%
▧ Metabolism :
Hepatic.
▧ Half Life :
9.1-13.2 hours
Độc Tính : Symptoms of overdose include pain, nausea, anorexia, hypotension, fever, rash, bad taste in mouth, confusion/hallucinations, dizziness, and diarrhea.
Chỉ Định : For the treatment of pneumonia due to Pneumocystis carinii.
Tương Tác Thuốc :
  • Artemether Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Lumefantrine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Mesoridazine Increased risk of cardiotoxicity and arrhythmias
  • Quinupristin This combination presents an increased risk of toxicity
  • Tacrolimus Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Telavancin Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Thioridazine Increased risk of cardiotoxicity and arrhythmias
  • Thiothixene May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
  • Ticlopidine Ticlopidine may decrease the metabolism and clearance of Pentamidine. Consider alternate therapy or monitor for adverse/toxic effects of Pentamidine if Ticlopidine is initiated, discontinued or dose changed.
  • Toremifene Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
  • Trimipramine Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Voriconazole Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Vorinostat Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Zalcitabine Additive risk of pancreatitis. Concomitant therapy should be avoided.
  • Ziprasidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Zuclopenthixol Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Liều Lượng & Cách Dùng : Powder, for solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : APP
    Sản phẩm biệt dược : NebuPent
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Pentacarinat
  • Công ty : Abbot
    Sản phẩm biệt dược : Pentacrinat
  • Công ty : Abbot
    Sản phẩm biệt dược : Pentam
  • Công ty : Abbot
    Sản phẩm biệt dược : Pentam 300
  • Công ty : Abbot
    Sản phẩm biệt dược : Pentamidine isethionate
  • Công ty :
    Sản phẩm biệt dược : Pneumopent
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00738
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4735
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508562
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07420
ChemSpider
http://www.chemspider.com/Chemical-Structure.4573.html
PharmGKB
http://www.pharmgkb.org/drug/PA450850
Wikipedia
http://en.wikipedia.org/wiki/Pentamidine
RxList
http://www.rxlist.com/cgi/generic3/pentam.htm
Drugs.com
http://www.drugs.com/cdi/pentamidine.html
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