部份中文盐酸头孢替安处方资料（仅供参考） 【中文品名】盐酸头孢替安片 【药效类别】抗生素>头孢菌素类 【通用药名】CEFOTIAM HYDROCHLORIDE 【别　　名】泛司博林，Spizef，Takedrol Halospor，Panrpocin，Abbott-48999，CGP14221/E，SCE963CTM, Cefotiam dihydrochloride 【化学名称】 5-Thia-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylic acid, 7-[[(2-amino-4-thiazolyl)acetyl]amino]-3-[[[2-(dimethylamino)ethyl]-1H-tetrazol-5-yl]thio]methyl]-8-oxo-, dihydrochloride, (6R,7R)- 【CA登记号】[66309-69-1] 【结 构 式】 【分 子 式】C18H23N9O4S3·2HCl 【分 子 量】598.54 【收录药典】JP14 【开发单位】武田药品工业株式会社 (日本) 【首次上市】1981年，日本 【性　　状】 白色或淡黄色结晶或结晶性粉末，略有特异臭。易溶于水、甲醇，难溶于乙醇，几乎不溶于丙酮、乙酸乙酯、氯仿和环己烷。在80~90℃开始熔解，但不完全液化，约97℃发泡分解。[α]20D+60~+72°(按1g干物计，水100ml，l00mm)。 【用　　途】 半合成头孢类抗生素。用于对本品敏感的葡萄球菌、链球菌(肠球菌除外)、肺炎球菌、流感杆菌、大肠杆菌、克雷氏菌、肠杆菌属，柠檬酸细菌属，奇异变形杆菌，普通变形杆菌，雷氏变形杆菌，摩氏变形杆菌所引起的以下感染：败血症、手术后创伤、疖、痈，痈疖、疖脓症，骨髓炎、化脓性关节炎、支气管炎、支气管扩张并发感染、肺化脓症、脓胸、胆管炎、胆囊炎、腹膜炎、肾盂肾炎、膀胱炎、尿道炎、前列腺炎、子宫内感染、骨盆死腔炎、子宫旁组织炎、子宫附件炎、前庭大腺炎、中耳炎、副鼻窦炎等。 【用法用量】 成人一般剂量每次200～400mg，每日3次。 【产品特点】 系注射用头孢替安乙酯化而成的口服抗生素。本品自身并抗菌作用，是口服后在肠道粘膜迅速水解为头孢替安(CTM）而被吸收。CTM对革兰阳性和阴性菌的抗菌活性与以往口服的头孢菌素相同，而且对β-内酰胺酶稳定。 本品对临床分离的金黄色葡萄球菌、凝固酶阴性葡萄球菌、肺炎链球菌、淋球菌、耐氨苄西林淋球菌（ABPC）、卡他莫拉菌、大肠杆菌、枸椽酸菌属、普罗威登斯菌属、化脓性链球菌、乳链球菌、肺炎克雷伯杆菌、奇异变形杆菌、流行性感冒嗜血杆菌，均有较强的抗菌活性，MIC比头胞氨苄、头孢克罗低。饭后1次口服本品100mg、200mg或400mg，血中CTM浓度迅速上升，而且随药量增加而升高。 其Cmax为1.54mg／L、2.73mg／L、4.55mg／L。血浆蛋白结合率为8％。本品在痰、耳漏液、鼻涕、上颌窦粘膜、扁桃体、皮肤、胆汁中转运良好。24h尿排泄率为40％。用餐对本品吸收影响很小。 【包装规格】 100mg（力価）：100錠（10錠×10） 200mg（力価）：100錠（10錠×10）、500錠（10錠×50） 【制造厂商】 武田化学工业有限公司 原药处方资料附件：http://www.info.pmda.go.jp/go/pack/6132012F1025_1_12/ パンスポリンＴ錠100／パンスポリンＴ錠200 Name of drug classification Cephem antibiotic preparation for oral use Sales name Pansporin tablet 100 Common name Cefotiam hexetil hydrochloride (Cefotiam Hexetil Hydrochloride) [JAN] Abbreviation CTM-HE Chemical name (1RS) -1-Cyclohexyloxycarbonyloxyethyl (6R, 7R) -7- [2- (2-aminothiazol-4-yl) acetylamino] -3- [1- (2-dimethylaminoethyl) -1H- tetrazol-5-ylsulfanylmethyl] 8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylate dihydrochloride Molecular formula C27 H 37 N 9 O 7 S 3. 2 HCl Molecular weight 768.76 Melting point Browning and swelling with increasing temperature, no apparent melting point and decomposition point at a temperature of 190 ° C. or lower at which decomposition is obviously observed. Property Cefotiam hexetyl hydrochloride is a white to light yellow powder. It is very soluble in water, methanol or ethanol (95), it is easily dissolved in dimethylsulfoxide, and it is hardly soluble in acetonitrile. It dissolves in 0.1mol/L hydrochloric acid reagent solution. It is hygroscopic. titer It is indicated by weight (titer) as cefotiam (C 18 H 23 N 9 O 4 S 3). 1mg of cefotiam hexetyl hydrochloride standard corresponds to 0.684 mg (potency). composition Active ingredient in 1 tablet Cefotiam hexetyl hydrochloride 100 mg (potency) Additive Anhydrous citric acid, α-cyclodextrin, hydroxypropyl cellulose, light anhydrous silicic acid, magnesium stearate, hypromellose, macrogol 6000, talc, titanium oxide, yellow ferric oxide, crystalline cellulose Contraindications Patients with a history of shock due to ingredients of cisplatin or hydrochloride of Cefotiam Indication or effect Adaptive fungal species Cefotiam is susceptible to Staphylococcus, Streptococcus, Streptococcus, Streptococcus pneumoniae, Neisseria gonorrhoeae, Moraxella (Branhamellara), Catharillis, Escherichia coli, Citrobacter, Klebsiella, Proteus/Mirabilis, Haemophilus influenzae Indication Secondary infections such as superficial skin infections, deep skin infections, lymphatic vessels · lymphadenitis, chronic pyoderma, trauma · burns and surgical wounds Mastitis, perianal abscess Secondary infection of pharyngo / laryngitis, tonsillitis, acute bronchitis, pneumonia, chronic respiratory lesions Cystitis, pyelonephritis, urethritis Dacryocystitis, stomatitis, epididymitis, keratitis (including corneal ulcer) Otitis media, sinusitis ○ Secondary infections such as superficial skin infections, deep skin infections, lymphatic vessels ·lymphadenitis, chronic pyoderma, trauma ·burns and surgical wounds, mastitis, perianal abscess, pharyngo ·laryngitis , In the case of tonsillitis, acute bronchitis, pneumonia, pyelonephritis, cystitis, urethritis, dacryocystitis, stomatitis, epididymitis, keratitis (including corneal ulcer), otitis media, sinusitis Usually, for adults, 300 to 600 mg (potency) of cefotiam hexetyl hydrochloride per day is orally administered in three divided doses. ○ Secondary infection of chronic respiratory lesion Usually, for adults, 600 to 1200 mg (potency) of cefotiam hexetyl hydrochloride per day is divided into three portions and administered orally. In addition, depending on the age and symptoms, 1200 mg (potency) per day is orally administered in three divided doses for cases severely or seemingly insufficiently efficacious, although it will increase or decrease accordingly. For patients with advanced renal impairment, carefully administer dosage and administration intervals appropriately. (See "Pharmacokinetics" section) When using this drug, in order to prevent the development of resistant bacteria etc., in principle, sensitivity should be confirmed and only administration for the minimum period necessary for treatment of disease should be made. Careful Administration Patients with a history of hypersensitivity to penicillin antibiotics A patient having a constitution that is likely to cause an allergic symptom such as bronchial asthma, rash, urticaria or the like by himself, parents or brothers Patients with advanced renal impairment [High blood levels may sustain](See "Pharmacokinetics" section) Patients with esophageal transit disorder [Stop at the esophagus and collapse may cause esophageal ulcers. ] Elderly (see "Administration to the elderly" section) Patients with poor oral intake or parenteral nutrition, patients with poor general condition [Vitamin K deficiency symptoms may appear, so observe thoroughly. ] Serious side effects Because it may cause shock and anaphylactoid symptoms (less than 0.1%), observe thoroughly and feel uncomfortable, oral abnormalities, dizziness, bowel movement, tinnitus, sweating, wheezing, dyspnea, angioedema, generalized flushing · If abnormality such as urticaria is observed, discontinue administration and take appropriate measures. Severe renal disorder (less than 0.1%) such as acute renal failure is reported with cefotiam hydrochloride, so observe thoroughly, if abnormality is found discontinue administration, appropriate Take action. Granulocytopenia (less than 0.1%) may occur, and hemolytic anemia (less than 0.1%) is reported to occur in cefotiam hydrochloride, so if it is found abnormal, administration stops Take appropriate measures such as doing. Serious colitis accompanied by bloody stools such as pseudomembranous colitis (less than 0.1%) may occur. If abdominal pain, frequent diarrhea appears, take appropriate measures such as immediately discontinue administration. Interstitial pneumonia accompanied by fever, cough, dyspnea, chest X-ray abnormality, eosinophilia etc., PIE syndrome (less than 0.1%), etc. may appear, so if such a symptom appears Discontinue administration and take appropriate measures such as adrenocortical hormone drug administration. Skin mucosa ocular syndrome (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell syndrome) (less than 0.1%) may occur, observation is sufficiently done, administration is discontinued when abnormality is found Appropriate measures should be taken. Liver dysfunction accompanied by elevation of AST (GOT), ALT (GPT), jaundice (less than 0.1%) may occur, so observe thoroughly, if abnormalities are observed discontinue administration, Appropriate measures should be taken. Medicinal pharmacology Antibacterial action Gram positive bacteria and gram negative bacteria broadly exhibit antimicrobial activity, especially antibacterial activity against Staphylococcus, Streptococcus pneumoniae, Streptococci, Haemophilus influenza, Escherichia coli, Klebsiella, Proteus · Miraviris, Neisseria gonorrhoeae, Moraxella (Blanhamella) · catarrhalis . Antibacterial activity is also recognized for Citrobacter genus. The antimicrobial action is bactericidal and shows bactericidal action even at the minimum inhibitory concentration. Mechanism of action Cefotiam, an antibacterial activator, inhibits the synthesis of bacterial cell walls. Cefotiam exhibits strong antibacterial activity against gram-positive bacteria and gram-negative bacteria is excellent in permeability to the extracellular membrane, relatively stable to β-lactamase and high affinity for penicillin-binding protein, so cell wall peptidoglycan crosslink formation It is thought that this is due to the strong inhibitory action.