药品详细

Troleandomycin(醋竹桃霉素)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

醋竹桃霉素

英文名

Troleandomycin

分子式

C₄₁H₆₇NO₁₅

化学名

(3R,5R,6S,7S,8R,11R,12S,13R,14S,15S)-14-{[(2S,3R,4S,6R)-3-(acetyloxy)-4-(dimethylamino)-6-methyloxan-2-yl]oxy}-12-{[(2R,4S,5S,6S)-5-(acetyloxy)-4-methoxy-6-methyloxan-2-yl]oxy}-5,7,8,11,13,15-hexamethyl-4,10-dioxo-1,9-dioxaspiro[2.13]hexadecan-6-yl acetate

分子量

Average: 813.9684
Monoisotopic: 813.451070479

CAS号

2751-09-9

ATC分类

药物类型

small molecule

阶段

approved

商品名

同义名

基本介绍

A macrolide antibiotic that is similar to erythromycin.

生产厂家

Pfizer laboratories div pfizer inc
Pfizer pharmaceuticals inc

封装厂家

参考

Synthesis Reference	Not Available
General Reference	Not Available

剂型

规格

化合物类型

Type	small molecule

Classes

Macrolides

Substructures

Carboxylic Acids and Derivatives
Glycerol and Derivatives
Pyrans
Acetates
Acetals and Derivatives
Lactones
Macrolides
Ethers
Aliphatic and Aryl Amines
Heterocyclic compounds
Epoxides
Ketones

适应症

药理

Indication	For the treatment of Pneumococcal pneumonia due to susceptible strains and group A beta-hemolytic streptococcal infections of the upper respiratory tract.
Pharmacodynamics	Troleandomycin is a macrolide antibiotic that is similar to erythromycin. It is active in vitro against the following gram-positive organisms: Streptococcus pyogenes and Diplococcus pneumoniae.
Mechanism of action	Troleandomycin acts by penetrating the bacterial cell membrane and reversibly binding to the 50 S subunit of bacterial ribosomes or near the "P" or donor site so that binding of tRNA (transfer RNA) to the donor site is blocked. Translocation of peptides from the "A" or acceptor site to the "P" or donor site is prevented, and subsequent protein synthesis is inhibited.
Absorption	Not Available
Volume of distribution	Not Available
Protein binding	Not Available
Metabolism	Not Available
Route of elimination	Not Available
Half life	Not Available
Clearance	Not Available
Toxicity	Symptoms of overdose include diarrhea, nausea, stomach cramps, and vomiting.
Affected organisms	Enteric bacteria and other eubacteria
Pathways	Not Available

理化性质

Properties

State

solid

Experimental Properties

Not Available

Predicted Properties

Property	Value	Source
water solubility	1.92e-02 g/l	ALOGPS
logP	3.76	ALOGPS
logP	4.3	ChemAxon
logS	-4.6	ALOGPS
pKa (strongest acidic)	16.75	ChemAxon
pKa (strongest basic)	7.87	ChemAxon
physiological charge	1	ChemAxon
hydrogen acceptor count	12	ChemAxon
hydrogen donor count	0	ChemAxon
polar surface area	184.19	ChemAxon
rotatable bond count	12	ChemAxon
refractivity	201.15	ChemAxon
polarizability	86.08	ChemAxon

药物相互作用

Drug	Interaction
Aminophylline	The macrolide, troleandomycin, may increase the effect and toxicity of theophylline derivative, aminophylline.
Aprepitant	This CYP3A4 inhibitor increases the effect and toxicity of aprepitant
Astemizole	Increased risk of cardiotoxicity and arrhythmias
Carbamazepine	The macrolide, troleandomycin, may increase the effect of carbamazepine.
Cisapride	Increased risk of cardiotoxicity and arrhythmias
Citalopram	Possible serotoninergic syndrome with this combination
Colchicine	Severe colchicine toxicity can occur
Cyclosporine	The macrolide, troleandomycin, may increase the effect of cyclosporine.
Dihydroergotamine	Possible ergotism and severe ischemia with this combination
Eletriptan	The macrolide, troleandomycin, may increase the effect and toxicity of eletriptan.
Eplerenone	The macrolide, troleandomycin, may increase the effect and toxicity of eplerenone.
Ergotamine	Possible ergotism and severe ischemia with this combination
Erlotinib	This CYP3A4 inhibitor increases levels/toxicity of erlotinib
Fluoxetine	Possible serotoninergic syndrome with this combination
Methysergide	Possible ergotism and severe ischemia with this combination
Oxtriphylline	The macrolide, troleandomycin, may increase the effect and toxicity of the theophylline derivative, oxtriphylline.
Pimozide	Increased risk of cardiotoxicity and arrhythmias
Tacrolimus	The macrolide antibiotic, Troleandomycin, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Troleandomycin therapy is initiated, discontinued or altered.
Terfenadine	Increased risk of cardiotoxicity and arrhythmias
Theophylline	The macrolide, troleandomycin, may increase the effect and toxicity of theophylline.

食物相互作用

Not Available

返回 | 收藏