部份中文环丝氨酸处方（仅供参考）
药品英文名
Cycloserine
药品别名
环丝氨酸、太素霉素、东方霉素、氧霉素、杀痨霉素、Antibiotic-5915、Cyclomycin、Closina、Ciclovalidin、Orientomycin、Seromycin、Tisomycin
药物剂型
胶囊：0.25g。
药理作用
本品结构与D-丙氨基酸相似，可抑制结核杆菌的细胞壁合成，干扰结核菌的细胞壁的早期合成，竞争性地抑制细胞浆中的L-丙氨酸消旋酶和D-丙氨酸合成酶，L-丙氨酸消旋酶使L-丙氨酸形成D-丙氨酸，D-丙氨酸合成酶可参与丙氨酸到五肽，为黏肽和菌体细胞壁合成所必需。特别是对链霉素、对氨基水杨酸钠、异烟肼和紫霉素耐药的结核杆菌有效。本品属广谱抗生素，对革兰阳性和阴性菌均有抑制作用，但抑菌力较弱，对结核杆菌有较强抑菌作用，体外最低抑菌浓度为5～20μg/ml。对其他的分枝杆菌、立克次体和某些原虫也有抑制作用。
药动学
口服在胃肠道吸收迅速，血浆药物浓度达峰时间为3～4h。口服每次250mg，每天2次，血药浓度可维持达20～30μg/ml。在体内分布甚广，服后迅速分布于全身组织和体液中，在脑脊液、胸腔积液、胎盘血和母乳中药物浓度与血浆浓度相仿，腹腔积液、胆汁、痰、羊水、肺组织和淋巴组织中均可发现药物，血浆半衰期为2～10h。服药后2～6h排出最多，72h后65%以原形药物由尿液中排出，其余35%在体内代谢分解。由于在尿液中高度浓缩，对尿道结核无须给予大剂量，肾功能不全者可在体内蓄积。
适应证
用于治疗对本品敏感的活动性结核病，但需与其他有效抗结核药物联用。自于可能引起严重精神错乱，故临床应用受到一定限制。
禁忌证
1.患有癫痫、严重忧郁症、烦躁或精神病者禁用。
2.严重肝肾功能损害者禁用。
3.嗜好饮酒者禁用。
注意事项
1.慎用：
心功能不全者慎用。对儿童的安全性尚未明确，妊娠及哺乳妇女慎用。
2.本品的不良反应与血药浓度和给药剂量相关，特别是一日超过500mg时，治疗期间最好能监测血药浓度，并应控制其低于30μg/ml，对测定的血样宜于每天首剂服用前抽取。对肾功能不全者一周监测1次。
3.神经反应包括神经和精神两方面，可出现肌肉抽搐、惊厥发作，一旦出现应立即停药，宜同时给予大剂量的维生素B6以预防。
不良反应
不良反应主要为中枢神经反应，
1.常见头痛、眩晕、嗜睡、行为异常、精神抑郁、定向或记忆障碍、震颤、抽搐、烦躁不安、惊厥或昏迷。
2.偶见加重心力衰竭、发热、恶心、呕吐、腹痛、肝功能异常、AST或ALT升高，本品可诱发精神病性反应，出现精神障碍和自杀倾向。
用法用量
口服：
1.成人每天0.5～1g，分2次服用，初始2周可每次0.25g，每天2次，最大剂量为每天1g。
2.儿童每天5～20mg/kg，分2～4次服用，首剂用半量。
药物相应作用
与异烟肼和乙硫异烟胺不宜联合应用，以免对中枢神经系统发生累加性影响，加大神经毒性。应用期间不宜饮酒。
专家点评
本品抗菌谱较广，但抗菌力不强。抗结核作用远比异烟肼、链霉素弱，其优点是细菌对本品不易产生耐药性。本品为二线抗结核药，因毒性大和不良反应的发生率较高，国内已不生产，主要用于对其他抗结核药耐药的结核感染和肺外结核病。
规格：
每颗胶囊250毫克，12粒每盒
美国生产

Cycloserine Capsules
Dosage Form: capsule
DESCRIPTION SECTION
 Cycloserine, 3-isoxazolidinone, 4-amino –, (R)– is a broad–spectrum antibiotic that is produced by a strain of Streptomyces orchidaceus and has also been synthesized. Cycloserine is a white to off–white powder that is soluble in water and stable in alkaline solution. It is rapidly destroyed at a neutral or acid pH. 
Cycloserine has a pH between 5.5 and 6.5 in a solution containing 100 mg/mL. The molecular weight of cycloserine is 102.09, and it has an empirical formula of C3H6N2O2.
INACTIVE INGREDIENT SECTION
Each capsule contains cycloserine, 250 mg (2.45 mmol); D and C Yellow No. 10, FD and C Blue No. 1, FD and C Red No. 3, FD and C Yellow No. 6, gelatin, iron oxide, talc, titanium dioxide, and other inactive ingredients.
CLINICAL PHARMACOLOGY SECTION
After oral administration, cycloserine is readily absorbed from the gastrointestinal tract, with peak blood levels occurring in 4 to 8 hours.
Blood levels of 25 to 30 μg/mL can generally be maintained with the usual dosage of 250 mg twice a day, although the relationship of plasma levels to dosage is not always consistent. Concentrations in the cerebrospinal fluid, pleural fluid, fetal blood, and mother’s milk approach those found in the serum. Detectable amounts are found in ascitic fluid, bile, sputum, amniotic fluid, and lung and lymph tissues. Approximately 65 percent of a single dose of cycloserine can be recovered in the urine within 72 hours after oral administration. The remaining 35 percent is apparently metabolized to unknown substances. The maximum excretion rate occurs 2 to 6 hours after administration, with 50 percent of the drug eliminated in 12 hours.
MICROBIOLOGY SECTION
Cycloserine inhibits cell–wall synthesis in susceptible strains of gram–positive and gram–negative bacteria and in Mycobacterium tuberculosis.
Susceptibility Tests
Cycloserine clinical laboratory standard powder is available for both direct and indirect methods1 of determining the susceptibility
of strains of mycobacteria. Cycloserine MICs for susceptible strains are 25 μg/mL or lower.
INDICATIONS & USAGE SECTION
Cycloserine is indicated in the treatment of active pulmonary and extrapulmonary tuberculosis (including renal disease) when the causative
organisms are susceptible to this drug and when treatment with the primary medications (streptomycin, isoniazid, rifampin, and ethambutol) has proved inadequate. Like all antituberculosis drugs, cycloserine should be administered in conjunction with other effective chemotherapy and not as the sole therapeutic agent.
Cycloserine may be effective in the treatment of acute urinary tract infections caused by susceptible strains of gram–positive and gram–negative bacteria, especially Enterobacter spp. and Escherichia coli. It is generally no more and is usually less effective than other antimicrobial agents in the treatment of urinary tract infections caused by bacteria other than mycobacteria. Use of cycloserine in these infections should be considered only when more conventional therapy has failed and when the organism has been demonstrated to be susceptible to the drug.
CONTRAINDICATIONS SECTION
Administration is contraindicated in patients with any of the
following:
Hypersensitivity to cycloserine
Epilepsy
Depression, severe anxiety, or psychosis
Severe renal insufficiency
Excessive concurrent use of alcohol
WARNINGS SECTION
Administration of cycloserine should be discontinued or the dosage reduced if the patient develops allergic dermatitis or symptoms of CNS toxicity, such as convulsions, psychosis, somnolence, depression, confusion, hyperreflexia, headache, tremor, vertigo, paresis, or dysarthria.
The toxicity of cycloserine is closely related to excessive blood levels (above 30 μg/mL), as determined by high dosage or inadequate renal clearance. The ratio of toxic dose to effective dose in tuberculosis is small.
The risk of convulsions is increased in chronic alcoholics.
Patients should be monitored by hematologic, renal excretion, blood level, and liver function studies.
PRECAUTIONS SECTION
Before treatment with cycloserine is initiated, cultures should be taken and the organism’s susceptibility to the drug should be established. In
tuberculous infections, the organism’s susceptibility to the other antituberculosis agents in the regimen should also be demonstrated.
Anticonvulsant drugs or sedatives may be effective in controlling symptoms of CNS toxicity, such as convulsions, anxiety, and tremor. Patients receiving more than 500 mg of cycloserine daily should be closely observed for such symptoms. The value of pyridoxine in preventing CNS toxicity from cycloserine has not been proved.
Administration of cycloserine and other antituberculosis drugs has been associated in a few instances with vitamin B12 and/or
folic–acid deficiency, megaloblastic anemia, and sideroblastic anemia. If evidence of anemia develops during treatment, appropriate studies and therapy should be instituted.
LABORATORY TESTS SECTION
Blood levels should be determined at least weekly for patients with reduced renal function, for individuals receiving a daily dosage of more
than 500 mg, and for those showing signs and symptoms suggestive of toxicity. The dosage should be adjusted to keep the blood level below 30 μg/mL.
DRUG INTERACTIONS SECTION
Concurrent administration of ethionamide has been reported to potentiate neurotoxic side effects.
Alcohol and cycloserine are incompatible, especially during a regimen calling for large doses of the latter. Alcohol increases the possibility and risk of epileptic episodes.
Concurrent administration of isoniazid may result in increased incidence of CNS effects, such as dizziness or drowsiness. Dosage adjustments may be necessary and patients should be monitored closely for signs of CNS toxicity.
Carcinogenesis, Mutagenicity, and Impairment of Fertility
Studies have not been performed to determine potential for carcinogenicity. The Ames test and unscheduled DNA repair test were negative. A study in 2 generations of rats showed no impairment of fertility relative to controls for the first mating but somewhat lower fertility in the second mating.
PREGNANCY SECTION
Pregnancy Category C
A study in 2 generations of rats given doses up to 100 mg/kg/day demonstrated no teratogenic effect in offspring. It is not known whether cycloserine can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Cycloserine should be given to a pregnant woman only if clearly needed.
NURSING MOTHERS SECTION
Because of the potential for serious adverse reactions in nursing infants from cycloserine, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
PEDIATRIC USE SECTION
Safety and effectiveness in pediatric patients have not been established.
ADVERSE REACTIONS SECTION
Most adverse reactions occurring during therapy with cycloserine involve the nervous system or are manifestations of drug hypersensitivity. The following side effects have been observed in patients receiving cycloserine:
Nervous system symptoms (which appear to be related to higher dosages of the drug, i.e., more than 500 mg daily)
Convulsions
Drowsiness and somnolence
Headache
Tremor
Dysarthria
Vertigo
Confusion and disorientation with loss of memory
Psychoses, possibly with suicidal tendencies
Character changes
Hyperirritability
Aggression
Paresis
Hyperreflexia
Paresthesia
Major and minor (localized) clonic seizures
Coma
Cardiovascular   
Sudden development of congestive heart failure in patients receiving 1 to 1.5 g of cycloserine daily has been reported
Allergy (apparently not related to dosage)
Skin rash
Miscellaneous
Elevated serum transaminase, especially in patients with preexisting liver disease
OVERDOSAGE SECTION
Acute toxicity from cycloserine can occur if more than 1 g is ingested by an adult. Chronic toxicity from cycloserine is dose related and can occur if more than 500 mg is administered daily. Patients with renal impairment will accumulate cycloserine and may develop toxicity if the dosing regimen is not modified. Patients with severe renal impairment should not receive the drug. The central nervous system is the most common organ system involved with toxicity. Toxic effects may include headache, vertigo, confusion, drowsiness,
hyperirritability, paresthesias, dysarthria, and psychosis. Following larger ingestions, paresis, convulsions, and coma often occur. Ethyl alcohol may increase the risk of seizures in patients receiving cycloserine.
The oral median lethal dose in mice is 5290 mg/kg.
Treatment
To obtain up–to–date information about the treatment of overdose, a good resource is your certified Regional Poison Control Center. Telephone numbers of certified poison control centers are listed in the Physicians’ Desk Reference (PDR). In managing overdosage,
consider the possibility of multiple drug overdoses, interaction among drugs, and unusual drug kinetics in your patient.
Overdoses of cycloserine have been reported rarely. The following is provided to serve as a guide should such an overdose be ecountered.
Protect the patient’s airway and support ventilation and perfusion. Meticulously monitor and maintain, within acceptable limits, the patient’s vital signs, blood gases, serum electrolytes, etc. Absorption of drugs from the gastrointestinal tract may be decreased by giving activated charcoal, which, in many cases, is more effective than emesis or lavage; consider charcoal instead of or in addition to gastric emptying. Repeated doses of charcoal over time may hasten elimination of some drugs that have been absorbed. Safeguard the patient’s airway when employing gastric emptying or charcoal.
In adults, many of the neurotoxic effects of cycloserine can be both treated and prevented with the administration of 200 to 300 mg of pyridoxine daily.
The use of hemodialysis has been shown to remove cycloserine from the bloodstream. This procedure should be reserved for patients with
life-threatening toxicity that is unresponsive to less invasive therapy
DOSAGE & ADMINISTRATION SECTION
Cycloserine is effective orally and is currently administered only by this route. The usual dosage is 500 mg to 1 g daily in divided doses monitored by blood levels.2 The initial adult dosage most frequently given is 250 mg twice daily at 12–hour intervals for the first 2 weeks. A daily dosage of 1 g should not be exceeded.
HOW SUPPLIED SECTION
Cycloserine is available as a 250 mg capsule with an opaque red cap and opaque gray body imprinted with “CHAO” and “F04” in edible black ink on both the cap and the body.
Bottles of 40  NDC 13845-1201-3
Store at controlled room temperature, 20° to 25°C (68° to 77°F) [see USP].

제품명: 사이린캡슐 (Cyrine )
제조 및 수입원: 한국유나이티드제약
판매 회사: 한국유나이티드제약
복지부 분류: 613 - 주로 항간성균에 작용하는 것
영문 성분명: Cycloserine 250 mg
한글 성분명: 시클로세린 250 mg
생산여부: 미생산
미국 FDA 임부안정성: 분류 C - 위험성을 배제할 수 없다. 사람에 대한 연구는 부족하고, 동물연구에서는 태자에 대한 위험성을 보이거나 동물에 대한 연구가 부족하다. 잠재적 위험성에도 불구하고, 약물 사용시의 유익성이 약물사용을 정당화할 수도 있다.
성상: 백색~엷은 황색 분말을 함유하는 상의 핑크색, 하의 백색의 경질캡슐제
효능/효과:
○ 유효균종
결핵균
○ 적응증
결핵
용법/용량:
○ 성인 : 시클로세린으로서 1회 250mg(역가)을 1일 2회 경구투여한다. 
1일 용량이 1g(역가)을 초과해서는 안 된다.
원칙적으로 다른 항결핵제와 병용투여한다.
연령, 증상에 따라 적절히 증감한다.
사용상 주의사항:
1. 다음 환자에는 투여하지 말 것.
1) 이 약에 과민반응 환자
2) 우울증, 간질 환자, 중증 불안 환자, 정신병 환자(간질유사 발작 등의 정신장애를 악화시킬 수 있다.)
3) 중증 신부전 환자
4) 알코올을 과량 섭취한 환자
2. 다음 환자에는 신중히 투여할 것.
1) 본인 또는 부모, 형제가 정신병, 간질의 병력이 있는 환자
2) 신장애 환자(혈중농도가 상승하고 중추신경계 등의 이상반응을 일으킬 수 있다.)
3) 알코올 중독자(알코올의 작용을 증강시킬 수 있다.)
4) 알레르기성 피부염, 혼란, 과다반사, 두통, 떨림, 어지러움, 불완전마비, 말더듬증 등의 중추신경계 독성 증상을 나타내는 환자
3. 이상반응
1) 정신신경계 : 두통, 어지러움, 졸음, 떨림, 우울, 정신착란, 환각, 혼수, 정신병(자살경향가짐), 과다반사, 관절통, 경련, 간질유사 발작, 말초신경염, 불완전마비, 말더듬증, 불면, 성격변화, 과다흥분, 공격성, 감각이상, 대?소간대성발작, 기억력 상실을 수반한 착란 및 방향성 상실을 수반한 착란 및 방향성 상실 등이 나타날 수 있으므로 충분히 관찰하고 이러한 증상이 나타나는 경우에는 투여를 중지한다.
2) 소화기계 : 때때로 구역, 식욕부진, 복통, 변비, 설사 등이 나타날 수 있다.
3) 순환기계 : 1일 1~1.5g 투여 시 갑작스런 울혈성 심부전이 나타났다는 보고가 있다.
4) 혈액계 : 다른 결핵 치료제와 병용투여 시 비타민 B12, 엽산결핍, 거대적아구성 빈혈, 철적모구성 빈혈이 나타날 수 있으므로 빈혈이 나타나면 충분히 관찰하고 적절한 처치를 한다.
5) 과민반응 : 피부발진이 나타날 수 있으며, 알레르기성 피부염이 나타나는 경우에는 감량 또는 투여를 중지한다.
6) 기타 : 혈청트랜스아미나제 증가가 나타날 수 있다(특히 간질환 환자).
4. 일반적 주의
1) 이 약의 사용에 있어서 내성균의 발현 등을 방지하기 위하여 감수성을 확인하고 치료 상의 필요한 최소 기간만 투여하는 것이 바람직하다.
2) 이 약은 1차 치료제(스트렙토마이신, 이소니아지드, 리팜피신, 에탐부톨 등)가 부적절한 경우에 사용한다.
3) 혈중농도 약 30㎍/mL의 이상에서 독성이 있으며 결핵치료 시의 유효량과 중독량의 차이가 작으므로 과량 투여하지 않도록 주의해야 한다.
4) 간, 신장애 환자는 혈액, 신배설, 혈중농도, 간기능 검사를 실시해야 한다.
5. 상호작용
1) 에치온아미드와 병용투여 시 신독성 상승 및 신경계 이상반응을 증강시킬 수 있으므로 신중히 투여한다.
2) 알코올은 간질성 발작 위험을 증가시키므로 감량하는 등 병용투여하지 않는다.
3) 이소니아지드와 병용투여 시 어지러움, 졸음 등 중추신경계에 대한 이상반응을 증가시킬 수 있으므로 감량하는 등 신중히 투여한다.
6. 임부 및 수유부에 대한 투여
1) 임신 중의 투여에 대한 안전성이 확립되어 있지 않으므로 임부 또는 임신하고 있을 가능성이 있는 여성에는 치료 상의 유익성이 위험성을 상회한다고 판단되는 경우에만 투여한다.
2) 모유 중으로의 이행이 보고되어 있으므로 수유부에는 투여하지 않는 것이 바람직하다.
7. 소아에 대한 투여
소아에 대한 안전성 및 유효성이 확립되어 있지 않다.
8. 과량투여시의 처치
1) 증상 : 성인에게 1g이상 사용했다면 급성독성이 나타날 수 있다. 두통, 어지러움, 혼란, 졸음, 과다흥분, 감각이상, 말더듬증, 정신병을 포함한 중추신경계 신경독성, 또는 때때로 과다섭취, 불완전마비, 간질, 혼수 등이 나타날 수 있다.
2) 처치 : 신경독성 대부분은 피리독신을 매일 200~300mg 투여함으로서 치료, 예방될 수 있다. 혈액투석으로 이 약을 제거할 수 있다. 이러한 과정은 침습치료에 반응이 없거나 적은, 생명을 위협하는 독성을 가진 환자에게 사용된다.
9. 보관 및 취급상의 주의사항
흡습성이 있으므로 반드시 밀폐한다.
저장방법: 기밀용기,실온(1~30℃)보관
포장단위:
* KMLE 약품/의약품 설명 및 약품 사진은 참고사항으로만 제공할 뿐, 반드시 의사/약사 및 제조 판매사와 최종 확인 바랍니다. KMLE 의학 검색 엔진은 약품/의약품의 내용에 대한 오류 및 약품 사진에 대한 오류에 대해서 어떤한 법률 책임이 없습니다.