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药品详细

Pentamidine(喷他脒)

化学结构式图
中文名
喷他脒
英文名
Pentamidine
分子式
C19H24N4O2
化学名
4-{[5-(4-carbamimidoylphenoxy)pentyl]oxy}benzene-1-carboximidamide
分子量
Average: 340.4195
Monoisotopic: 340.189926032
CAS号
100-33-4
ATC分类
P01C 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

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]

生产厂家
  • App pharmaceuticals llc
  • Armour pharmaceutical co
  • Baxter healthcare corp anesthesia and critical care
  • Hospira inc
  • Watson laboratories inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Nguewa PA, Fuertes MA, Cepeda V, Iborra S, Carrion J, Valladares B, Alonso C, Perez JM: Pentamidine is an antiparasitic and apoptotic drug that selectively modifies ubiquitin. Chem Biodivers. 2005 Oct;2(10):1387-400. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Phenols and Derivatives
  • Ethers
  • Anisoles
  • Phenyl Esters
Substructures
  • Carboxylic Acids and Derivatives
  • Phenols and Derivatives
  • Ethers
  • Benzene and Derivatives
  • Aromatic compounds
  • Carboxamidines
  • Anisoles
  • Imines
  • Phenyl Esters
适应症
药理
Indication For the treatment of pneumonia due to Pneumocystis carinii.
Pharmacodynamics 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.
Mechanism of action 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.
Absorption Absorbed poorly through the gastrointestinal tract and is usually administered parenterally.
Volume of distribution Not Available
Protein binding 69%
Metabolism
Hepatic.
Route of elimination Not Available
Half life 9.1-13.2 hours
Clearance Not Available
Toxicity Symptoms of overdose include pain, nausea, anorexia, hypotension, fever, rash, bad taste in mouth, confusion/hallucinations, dizziness, and diarrhea.
Affected organisms
  • Pneumocystis carinii
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 186.0 °C (decomposes) Not Available
water solubility Complete Not Available
logP 4 Not Available
Predicted Properties
Property Value Source
water solubility 2.36e-02 g/l ALOGPS
logP 1.32 ALOGPS
logP 2.32 ChemAxon
logS -4.2 ALOGPS
pKa (strongest basic) 12.13 ChemAxon
physiological charge 2 ChemAxon
hydrogen acceptor count 6 ChemAxon
hydrogen donor count 4 ChemAxon
polar surface area 118.2 ChemAxon
rotatable bond count 10 ChemAxon
refractivity 120.53 ChemAxon
polarizability 38.85 ChemAxon
药物相互作用
Drug Interaction
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).
食物相互作用
Not Available

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