药品英文名
Lomefloxacin
药品别名
罗美沙星、康力康、宇力、罗氟酸、Bareon、Lomebact、Lomefloxacine、NY-198、Maxaquin
药物剂型
1.片剂：100mg，200mg；
2.薄膜衣片：400mg；
3.口服液：10ml(含本药盐酸盐110.4mg)；
4.胶囊:100mg，200mg。
5.颗粒剂：每包含洛美沙星盐酸盐100mg；
6.注射剂： 200mg（100ml)。
药理作用
本品为较长效的喹诺酮类广谱抗菌剂，可日服1次。对革兰阴性菌具强大的抗菌作用，其MIC大都小于等于2μg/ml；对大肠杆菌、流感杆菌和淋球菌的抗菌作用尤强；对肺炎球菌和其他链球菌的抗菌作用较弱；对大部分耐庆大霉素和哌拉西林的革兰阳性杆菌仍具良好的抗菌活性。本品抗菌作用略逊于环丙沙星，与氧氟沙星相似，稍优于诺氟沙星。其对繁殖期细菌和蛋白质合成抑制期细菌均显示迅速杀菌作用，并具有明显的抗菌药物后效应(PAE)。作用机制同环丙沙星，作用于细菌DNA旋转酶的A亚单位，抑制DNA的合成和复制而导致细菌死亡。体外抗菌活性与氧氟沙星相近，体内抗菌活性较诺氟沙星、氧氟沙星和左氧氟沙星高，但不如氟罗沙星。本药抗菌谱类似氧氟沙星，高度敏感菌有肠杆菌科的多数菌属、奈瑟菌属及军团菌；中度敏感菌含假单胞菌属的多数菌株和不动杆菌属。对葡萄球菌属具有较强抗菌活性，对衣原体、支原体、结核分枝杆菌等也有作用，但不如对革兰阴性和革兰阳性菌的抗菌活性高。对链球菌、肺炎链球菌、洋葱假单胞菌、支原体和厌氧菌均无效。
药动学
本药口服吸收完全，生物利用度为90%～98%。单剂空腹口服本药400mg后，1.5h达血药浓度峰值，约3.0～5.2mg/L。体内代谢少，约为给药量的5%。药物吸收后在体内分布广，大多数组织及体液中药物浓度超过血药浓度。消除半衰期约7～8h。主要自肾排泄，给药后48h以原形从尿中约排出给药量的60%～80%胆汁排泄约10%。老年人(61～76岁)由于肾功能降低，其血药清除率降低约25%，曲线下面积(AUC)增加约33%。临床评价认为本品高效而安全，对中枢神经影响约为依诺沙星的1/10以下。
适应证
可用于敏感菌所致的下列感染：
1.泌尿生殖道感染：包括单纯性或复杂性尿路感染，细菌性前列腺炎、淋球菌尿道炎、肾盂肾炎、非特异性尿道炎(宫颈炎)(包括产酶株所致者)等。
2.呼吸系统感染：包括咽喉炎、扁桃体炎、急性支气管炎及肺部感染等。
3.消化系统感染：包括肠炎、胆囊炎、肛管直肠周围脓肿(肛周脓肿)等。
4.滴眼剂可用于外眼部感染。
5.手术感染的预防。
6.其他：还可用于沙门菌属感染、骨和关节感染、皮肤软组织感染以及败血症等全身感染。
禁忌证
1.对喹诺酮类过敏者。
2.孕妇及哺乳期妇女。
3.16岁以下儿童。
注意事项
1.慎用：
(1)中枢神经系统疾病：
(2)有癫痫史；
(3)严重肾功能减退。
2.交叉过敏：本药与其他喹诺酮类药之间存在交叉过敏。
3.药物对老人的影响：老年患者应用本药时需减量。
4.药物对儿童的影响：18岁以下者应避免应用本药。如细菌仅对氟喹诺酮类敏感，应在权衡利弊后应用。
不良反应
1.消化系统：常见恶心、腹泻，也可有口干、畏食、消化不良、呕吐、腹痛、腹胀、便秘、消化道出血等。
2.精神神经系统：常见头痛、眩晕，也可有失眠、神经质、精神错乱、焦虑、抑郁、激动、噩梦、惊厥、昏迷、震颤等。
3.心血管系统：可有血压波动、水肿、晕厥、心动过速或过缓、期外收缩、发绀、心力衰竭、心绞痛、心肌梗死、肺栓塞、心肌病、脉管炎等。
4.呼吸系统：可有胸痛、呼吸困难、鼻出血、支气管痉挛。咳嗽、痰液增加、喘鸣等。
5.肌肉骨骼：可引起腿痉挛、关节痛、肌痛等。
6.泌尿生殖系统：可有少尿、血尿、无尿、阴道炎、阴道白色念珠菌病、睾丸炎、附睾炎等。
7.血液系统：可引起血红蛋白、血小板、白细胞减少，嗜酸粒细胞、单核细胞增多。
8.内分泌/代谢：可引起痛风、低血糖及血电解质异常等。
9.皮肤：光敏反应较其他喹诺酮类药物常见，发生率高，且其发生率随用药时间延长而增高，偶见皮疹、瘙痒、潮红等。
10.其他：可有多汗、疲乏、畏寒、耳痛、耳鸣、视觉异常、结膜炎、眼痛等。
用法用量
1.成人口服给药：
(1)细菌性支气管感染：每次400mg，每天1次；或每次300mg，每天2次，疗程7～14天；
(2)急性单纯性尿路感染：每次400mg，每天1次，疗程7～10天；
(3)复杂性尿路感染：每次400mg，每天1次，疗程14天；
(4)手术感染的预防：手术前2～6h服400mg。2.肾功能不全时剂量：根据血肌酐清除率酌情调整剂量。3.静脉滴注：每次0.2g，每天2次，稀释于5%葡萄糖注射剂250ml中滴注。
药物相应作用
1.与芬布芬合用，可致中枢兴奋，癫痫发作。
2.丙磺舒可延迟本药的排泄，使平均AUC增大63%，平均达峰时间延长50%，平均血药浓度峰值增高4%。
3.本药可加强口服抗凝血药(如华法林)的抗凝作用，合用时应监测凝血酶原时间。
4.硫糖铝和抗酸药可使本药吸收速率减慢25%，AUC降低约30%，如在服用本药前4h或服用后2h服硫糖铝或抗酸药则影响甚微。
5.本药对茶碱类药物肝内代谢影响小。
6.本药对咖啡因的肝内代谢影响小。
7.食物仅轻度减少本药的吸收。
バレオンカプセル100mg／バレオン錠200mg
商品名 バレオンカプセル１００ｍｇ
一般名
塩酸ロメフロキサシン Lomefloxacin hydrochloride（JAN）
略号
LFLX
化学名
(RS)-1-Ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-piperazin-1-yl)-4-oxoquinoline-3-carboxylic acid monohydrochloride
薬効 6241 ピリドンカルボン酸系製剤
一般名 塩酸ロメフロキサシンカプセル
英名 Bareon
剤形 カプセル
包装規格
バレオンカプセル100mg PTP：100カプセル（10カプセル×10）
バレオンカプセル100mg PTP：500カプセル（10カプセル×50）
バレオンカプセル100mg PTP：1,000カプセル（10カプセル×100）
バレオン錠200mg PTP：100錠（10錠×10）
バレオン錠200mg PTP：300錠（10錠×30）
バレオン錠200mg PTP：900錠（10錠×90）
製造販売
アボット ジャパン株式会社
完整资料附件：http://www.info.pmda.go.jp/go/pack/6241009F1028_2_12/
MAXAQUIN Tablets
SCHEDULING STATUS:
S4
PROPRIETARY NAME
(and dosage form):
MAXAQUIN® Tablets
COMPOSITION:
Each tablet contains lomefloxacin hydrochloride equivalent to 400 mg lomefloxacin base.
PHARMACOLOGICAL CLASSIFICATION:
A 20.1.1 Broad and medium spectrum anti-biotics.
PHARMACOLOGICAL ACTION:
MAXAQUIN, a difluoroquinolone, is a synthetic broad spectrum antimicrobial agent.
Pharmacokinetics:
Lomefloxacin is rapidly and well absorbed from the gastrointestinal tract after oral administration, and is 95 - 98% bioavailable.
There is no first-pass metabolism. Between doses of 100 mg and 400 mg, plasma concentration and AUC increase proportionately with increasing dose.
Maximum plasma concentrations (Cmax) of approximately 2 to 4 micrograms/mL are attained 1 to 1,5 hours (tmax) after a single 400 mg oral dose. Tmaxis independent of dose and dosing frequency.
The elimination half-life (t½) in normal healthy volunteers is approximately 8 hours.
Steady-state concentrations with once-a-day dosing are achieved by the end of the second day of dosing. There is no accumulation with once-a-day dosing in patients with normal renal function.
In healthy volunteers between the ages of 61 and 76 years, the mean t½ and mean Cmax following a single 400 mg dose were similar to those seen in younger volunteers.
Following oral administration, lomefloxacin is widely distributed throughout the body. About 10% is bound to plasma proteins.
Lomefloxacin is minimally metabolised, although five inactive metabolites, accounting for approximately 10% of the dose, have been identified in human urine.
Approximately 65% of an orally administered dose is excreted as unchanged drug in the urine of patients with normal renal function. Following a single 400 mg dose or multiple daily doses of 400 mg, urine concentrations are in excess of 400 mcg/mL by 4 hours post dose and remain above 35mcg/mL for at least 24 hours after dosing.
Urinary excretion is virtually complete within 72 hours after cessation of dosing. The renal clearance exceeds the normal glomerular filtration rate averaging approximately 150mL/min in subjects with normal renal function, indicating tubular secretion.
Approximately 10% of an oral dose is recovered as unchanged drug in the faeces.
The elimination of lomefloxacin is prolonged in patients with renal insufficiency, with increased AUC ant t½ (see Dosage and Directions for Use of dosing recommendations).
No significant change in any pharmacokinetic parameter was observed in patients with hepatic cirrhosis.
Pharmacodynamics:
The bactericidal action of lomefloxacin results from inhibition of the activity of the bacterial enzyme DNA gyrase, needed for the transcription and replication of bacterial DNA. The minimum bactericidal concentration(MBC) generally does not exceed the minimum inhibitory concentration (MIC) by more than a factor of two.
There is cross-resistance between lomefloxacin and other quinolone-class antimicrobial agents.
The minimal dose of UVA light needed to cause erythema is inversely proportional to plasma lomefloxacin concentration. Increasing the interval between lomefloxacin dosing and exposure to UVA light increases the amount of light energy for photoreaction.
INDICATIONS
Treatment:
MAXAQUIN is indicated for the treatment of mild to moderate infections caused by susceptible strains in the conditions listed below:
Uncomplicated urinary tract infections (cystitis) caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Staphylococcus saprophyticus.
Complicated, including recurrent, urinary tract infections caused by Citrobacter diversus, Enterobacter cloacae, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa. In the treatment of infections caused by Pseudomonas aeruginosa, an aminoglycoside must be administered concomitantly.
Acute exacerbation of chronic bronchitis caused by Branhamella catarrhalis [beta lactamase (+) and (-)]. Haemophilus influenzae [beta lactamase (+) and (-)].
Note:
MAXAQUIN is not indicated for the empiric treatment of acute bacterial exacerbation of chronic bronchitis when it is probable that S. pneumoniae is a causative pathogen. S. pneumoniae exhibits in vitro resistance to lomefloxacin. Safety and efficacy of lomefloxacin in the treatment of patients with acute bacterial exacerbation of chronic bronchitis caused by S. pneumoniae have not been demonstrated. If lomefloxacin is to be prescribed for Gram-stain guided empiric therapy of acute bacterial exacerbation of chronic bronchitis, it should be used only if sputum gram stain demonstrates an adequate quality of specimen (>25 polymorphonucleocytes / low power field) and there is both a predominance of gram negative organisms and not a predominance of gram positive organisms.
Prevention:
MAXAQUIN is indicated preoperatively to reduce the incidence of postoperative urinary tract infections in patients undergoing transurethral surgical procedures.
CONTRA-INDICATIONS:
MAXAQUIN is contra-indicated in patients with a history of hypersensitivity to lomefloxacin or to other quinolones. MAXAQUIN is also contra-indicated in pregnancy and lactation as teratogenicity has been shown in experimental animals..
Should not be used in children and growing adolescents.
Severe renal impairment - creatinine clearance <30 mL/min/1,73 m².
DOSAGE AND DIRECTIONS FOR USE:
MAXAQUIN is recommended at the doses and for the durations of treatment listed in the following table, and may be taken with or without food:
Disorder
Dose/RegimenDuration of treatment
Uncomplicated urinary tract infection400 mg once daily3 days
Complicated urinary tract infection400 mg once daily10-14 days
Acute exacerbation of chronic bronchitis400 mg once daily7-10 days
Prophylaxis of urinary tract infection
following transurethral surgery400 mgsingle dose 2-6 hours prior to surgery
The risk of reaction to solar UV light may be reduced by taking lomefloxacin in the evening.
Elderly:
No dosage adjustment is required in elderly patients if creatinine clearance is >30 mL/min/1,73 m2).
SIDE EFFECTS AND SPECIAL PRECAUTIONS:
SIDE EFFECTS:
The most common side-effects seen are headache, nausea, phototoxicity, dizziness, diarrhoea and abdominal pain.
Less frequently occurring side-effects are:
Body as a whole: anaphylaxis
Cardiovascular disorders: cardiopulmonary arrest
Gastro-intestinal system disorders: painful oral mucosa, pseudomembranous colitis
Liver and biliary system disorders: hepatitis
Metabolic and nutritional disorders: hypoglycaemia
Musculoskeletal disorders: tendinitis, tendon rupture
Nervous system disorders: ataxia , convulsions.
Platelet, bleeding and clotting disorders: cerebral thrombosis
Psychiatric disorders: hallucinations, phobia
Red blood cell disorders: haemolytic anaemia
Respiratory system disorders: laryngeal oedema, pulmonary oedema
Skin and appendage disorders: exfoliative dermatitis, hyperpigmentation,
Stevens-Johnson syndrome, toxic epidermal necrolysis
Urinary system disorders: interstitial nephritis, polyuria, renal failure, urinary retentionVascular disorders: vasculitis
Vision disorders: diplopia, photophobia
Other disorders: dysgeusia
IN addition, the following adverse reactions occur with lomefloxacin: anaphylactoid reactions, CNS stimulation, drowsiness, elevation of SGOT(AST), elevation of SGPT (ALT), leucopenia, myalgia.
PRECAUTIONS:
General:
Lomefloxacin has been shown to cause phototoxicity. Patients should be advised to avoid exposure to direct or indirect ultraviolet light (eg. sunlight, sunlamps and solaria), including exposure through glass, while taking lomefloxacin and for a few days after therapy. Phototoxicity has occurred even with use of a sun protective agent.
Lomefloxacin therapy should be discontinued if phototoxicity occurs.
As a class quinolones may cause central nervous system (CNS) stimulation.
Therefore MAXAQUIN should be used with caution in patients with known or suspected CNS disorders such as epilepsy or other conditions which predispose to seizures.
MAXAQUIN may cause tendon rupture. If tendinitis occurs, discontinue lomefloxacin.
Drug interactions:
In comparative clinical studies MAXAQUIN has not been shown to have any interaction with theophylline.
Sucralfate, antacids containing magnesium or aluminium and metal cations from other sources such as mineral supplements, form chelation complexes with lomefloxacin and interfere with its bioavailability. Administration of these agents should precede MAXAQUIN dosing by 4 hours or follow lomefloxacin dosing by at least 2 hours.
Toxicology:
Lomefloxacin and related agents have been shown to cause arthropathy in immature animals.
Effects on ability to drive and use machines:
Because of the potential for CNS effects patients should be cautioned regarding driving and use of machinery during lomefloxacin treatment.
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:Information on overdosage in humans is limited. In the event of acute overdosage, the stomach should be emptied by inducing vomiting or by gastric lavage, and the patient care fully observed and given supportive treatment. Adequate hydration should be maintained. Haemodialysis or peritoneal dialysis is of no benefit. Treatment is supportive and
symptomatic.
IDENTIFICATION:
MAXAQUIN is available in 400 mg white to off-white, oval, biconvex, film coated tablets, scored on one side and debossed Maxaquin 400 on the other.
PRESENTATION:
Blister pack (3 or 5 tablets).
STORAGE INSTRUCTIONS:
Keep out of reach of children.
Protect from light.
Store between 15°C and 30°C.
REGISTRATION NUMBER:
Z/20.1.1/74
