【通用名】盐酸头孢卡品酯
【英文名】cefcapene pivoxil hydrochloride
【商品名】Flomox
【CAS】
135889-00-8 (cefcapene);
105889-45-0 (cefcapene pivoxil);
147816-23-7 (anhydrous cefcapene pivoxil hydrochloride) ;
147816-24-8 (cefcapene pivoxil hydrochloride);
【分子式】C23H29N5O8S2,HCl,H2O
【化学名】Pivaloyloxymethyl (+)-(6R,7R)-7-[(Z)-2-(2-amino-4-thiazolyl)-2-pentenamido]-3-(hydroxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid carbamate monohydrochloride monohydrate
【开发单位】盐野义制药株式会社
【剂型】片剂
【规格】75mg，100mg
【用法用量】口服75mg、150mg
【临床试验】
对153例患者，每天200-600mg、28d，临床有效率胆道感染为95%，急性乳腺炎100%，伤口感染80%，其他皮肤感染80。
【药理作用】
本品是第四代可口服头孢类抗生素，药理研究表明，对好氧革兰阳性菌的MSSA的MIC80为3.13μg/mL，与头孢替安、头孢克洛相同、对肺炎链球菌的MIC80≤0.1μg/mL，优于头孢克洛，与头孢托仑相当，对耐青霉素(含中等程度耐药)的肺炎链球菌的活性很强，MIC80为0.78μg/mL。对革兰阴性菌中的弗氏柠檬酸杆菌、阴沟肠杆菌、雷氏普罗威登斯菌、黏膜炎布兰汉氏球菌、黏质沙雷菌比头孢托仑、头孢替安强。对变形杆菌属、流感嗜血杆菌、摩氏摩根氏菌、淋球菌的活性比头孢克洛、头孢替安强，与头孢特仑相当。对耐氨苄西林的流感嗜血杆菌有很强的活性，MIC80为0.05μg/mL。对厌氧菌的活性是对比药中最强的。
本品是头孢类抗生素的口服前药，口服后在肠道中经酯酶水解，生成活性的头孢菌素化合物S-1006，新戊酸和甲醛。S-1006具有广泛的抗菌作用，对分离得到的金黄色葡萄球菌IC90为2μg/mL，对链球菌A，链球菌B，链球菌C，链球菌F，链球菌G以及肺炎链球菌的IC90≤0.12μg/mL，对所有分离得到的流感嗜血杆菌的IC90≤0.06μg/mL，对肠杆菌科细菌的IC50≤2μg/mL。本品对β-内酰胺酶TEM-1亚型稳定，但会被TEM-3，TEM-5，PSE-1及PSE-4亚型的β-内酰胺酶水解，也可被肠杆菌，摩根氏菌等细菌染色体的β-内酰胺酶所水解。
在动物研究中表明，本品可保护小鼠免遭肺炎链球菌和大肠杆菌的感染，其作用比头孢克罗和头孢地尼强。但抗金黄色葡萄球菌系统感染的作用比二者低。在对临床分离的呼吸道感染细菌的抗菌试验中，本品对青霉素敏感的肺炎链球菌的活性和青霉素，氨苄西林、头孢托仑酯的活性相同；比头孢克罗、头孢地尼和红霉素弱。但对产生β-内酰酶或不产生β-内酰胺酶的流感嗜血杆菌有较好的抗菌作用。
フロモックス錠75mg／フロモックス錠100mg
商標名Flomox
一般的名称：
セフカペン ピボキシル塩酸塩水和物（JAN）［日局］
Cefcapene Pivoxil Hydrochloride Hydrate
略号：
CFPN-PI
化学名：
2,2-Dimethylpropanoyloxymethyl (6R,7R)-7-[(2Z)-2-(2-aminothiazol-4-yl)pent-2-enoylamino]-3-carbamoyloxymethyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate monohydrochloride monohydrate
分子式：
C23H29N5O8S2・HCl・H2O
分子量：
622.11
化学構造式：
性状：
白色～微黄白色の結晶性の粉末又は塊で，わずかに特異なにおいがある。
N,N-ジメチルホルムアミド又はメタノールに溶けやすく，エタノール（99.5）にやや溶けやすく，水に溶けにくく，ジエチルエーテルにほとんど溶けない。
融点：
約135 ℃（分解）
分配係数：
104［pH7，1-オクタノール/緩衝液］
取扱い上の注意
瓶入り－乾燥剤付きの瓶包装としている。
使用の都度密栓すること。
PTP包装－防湿性の高いPTPとアルミ袋により品質保持を図っている。
アルミ袋開封後はPTP包装のまま保存すること。
包装
盐酸头孢卡品酯片75mg：PTP100錠（10錠×10），
盐酸头孢卡品酯片75mg：PTP500錠（10錠×50）
盐酸头孢卡品酯颗粒100mg：瓶500錠
盐酸头孢卡品酯片100mg：PTP100錠（10錠×10），
盐酸头孢卡品酯片100mg：PTP500錠（10錠×50）
详细使用资料附件：http://www.info.pmda.go.jp/go/pack/6132016F1023_1_14/
The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse effects (risks) as well as efficacies (benefits). It is important to minimize adverse effects and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment.
Brand name : FLOMOX Tablets 75mg
Active ingredient: Cefcapene pivoxil hydrochloride hydrate
Dosage form: light red tablet, φ: 8.6 mm, thickness: 3.7 mm
Print on wrapping: (Face) フロモックス 75, (Back) 654・75 フロモックス 75
Effects of this medicine
This medicine is a cephem antibiotic and has an antibacterial effect by inhibiting bacterial cell wall synthesis.
It is usually used for the treatment of a wide range of bacterial infections including skin infections, surgical infections, respiratory infections, urinary tract infections, obstetric and gynecologic infections, ophthalmic infections, otorhinolaryngologic infections, dental and oral surgical infections, etc.
Before using this medicine, be sure to tell your doctor and pharmacist
•If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines.
•If you are pregnant or breastfeeding.
•If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.)
Dosing schedule (How to take this medicine)
•Your dosing schedule prescribed by your doctor is << to be written by a healthcare professional>>
•In general, for adults, take 1 tablet [100 mg (potency) of the active ingredient] at a time, 3 times daily after meals. For patients with refractory infections or those for whom the usual dosage is insufficient, take 150 mg (potency) of the active ingredient at a time, 3 times daily after meals. The dosage may be adjusted according to the disease, age and symptoms. Strictly follow the instructions.
•If you miss a dose, take it as soon as you remember. Thereafter, continue your regular dosing schedule. You should never take two doses at one time.
•If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist.
•Do not stop taking this medicine unless your doctor instructs you to do so.
Precautions while taking this medicine
• Possible adverse effects of this medicine
The most commonly reported adverse reactions include rash, hives, itch, redness, erythema, swelling, fever, joint pain, diarrhea, pain in stomach and nausea. If any of these symptoms occur, consult with your doctor or pharmacist.
The symptoms described below are rarely seen as initial symptoms of the adverse effects indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately.
•feeling ill, swelling around eyes and/or mouth (lips), dizziness[shock, anaphylaxis]
•fever, sore throat, gum bleeding[agranulocytosis, thrombocytopenia, hemolytic anemia]
•fluid-filled blister, inflammation in mucous membrane of eyes, mouth, etc., general redness[toxic epidermal necrolysis, mucocutaneous ocular syndrome, erythroderma (exfoliative dermatitis)]
•breathlessness, fever, dry cough[interstitial pneumonia, eosinophilic pneumonia]
•malaise, anorexia, yellowness in the skin or in the white of eyes[fulminant hepatitis, hepatic function disorder, jaundice]
The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above.
Storage conditions and other information
•Keep the medicine out of the reach of infants and children. Store it at room temperature (1 to 30 degrees Celsius) away from direct sunlight and moisture.
•Discard the remainder. Do not store them.