药品详细

Rolitetracycline(罗利环素)

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

罗利环素

英文名

Rolitetracycline

分子式

C₂₇H₃₃N₃O₈

化学名

(4S,4aS,5aS,6S,12aS)-4-(dimethylamino)-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-N-(pyrrolidin-1-ylmethyl)-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide

分子量

Average: 527.5662
Monoisotopic: 527.226765047

CAS号

751-97-3

ATC分类

J01A 未知

药物类型

small molecule

阶段

approved

商品名

同义名

基本介绍

A pyrrolidinylmethyl tetracycline. [PubChem]

生产厂家

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

Tetracyclines

Substructures

Tetracyclines
Hydroxy Compounds
Benzyl Alcohols and Derivatives
Naphthalenes
Phenols and Derivatives
Amino Ketones
Phenylpropenes
Pyrrolidines
Benzene and Derivatives
Aminals and Derivatives
Aliphatic and Aryl Amines
Alcohols and Polyols
Heterocyclic compounds
Aromatic compounds
Cinnamaldehydes
Ketenes and Derivatives
Phenyl Esters
Enols
Ketones

适应症

药理

Indication	Rolitetracycline is a broad-spectrum antibiotic used in cases needing high concentrations or when oral administration is impractical.
Pharmacodynamics	Not Available
Mechanism of action	Rolitetracycline is a semisynthetic broad-spectrum tetracycline antibiotic used especially for parenteral administration in cases requiring high concentrations or when oral administration is impractical. Rolitetracycline passively diffuses through porin channels in the bacterial membrane and reversibly binds to the 30S ribosomal subunit, preventing binding of tRNA to the mRNA-ribosome complex, and thus interfering with protein synthesis.
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 anorexia, nausea, diarrhoea, glossitis, dysphagia, enterocolitis and inflammatory lesions (with monilial overgrowth) in the anogenital region, skin reactions such as maculopapular and erythematous rashes, exfoliative dermatitis, photosensitivity, hypersensitivity reactions such as urticaria, angioneurotic oedema, anaphylaxis, anaphyl-actoid purpura, pericarditis, and exacerbation of systemic lupus erythematosus, benign intracranial hypertension in adults disappearing on discontinuation of the medicine, haematologic abnormalities such as haemolytic anaemia, thrombocytopenia, neutropenia, and eosinophilia. LD₅₀=262 mg/kg (I.P. in rat).
Affected organisms	Not Available
Pathways	Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
water solubility	5.55E+005 mg/L	MERCK INDEX (1996)

Predicted Properties

Property	Value	Source
water solubility	1.81e+00 g/l	ALOGPS
logP	-0.08	ALOGPS
logP	-3.8	ChemAxon
logS	-2.5	ALOGPS
pKa (strongest acidic)	0.31	ChemAxon
pKa (strongest basic)	8.24	ChemAxon
physiological charge	-1	ChemAxon
hydrogen acceptor count	10	ChemAxon
hydrogen donor count	6	ChemAxon
polar surface area	170.87	ChemAxon
rotatable bond count	4	ChemAxon
refractivity	139.45	ChemAxon
polarizability	54.05	ChemAxon

药物相互作用

Drug	Interaction
Acitretin	Increased risk of intracranial hypertension
Amoxicillin	Possible antagonism of action
Ampicillin	Possible antagonism of action
Carbenicillin	Possible antagonism of action
Clavulanate	Possible antagonism of action
Cloxacillin	Possible antagonism of action
Dicloxacillin	Possible antagonism of action
Ethinyl Estradiol	This anti-infectious agent could decrease the effect of the oral contraceptive
Etretinate	Increased risk of intracranial hypertension
Flucloxacillin	Possible antagonism of action
Isotretinoin	Increased risk of intracranial hypertension
Penicillin G	Possible antagonism of action
Penicillin V	Possible antagonism of action
Piperacillin	Possible antagonism of action
Pivampicillin	Possible antagonism of action
Pivmecillinam	Possible antagonism of action

食物相互作用

Not Available

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