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NAVELBINE 酒石酸长春瑞滨软胶囊

通用名称酒石酸长春瑞滨软胶囊 VINORELBINE TARTRATE
品牌名称NAVELBINE 诺维本
产地|公司法国(France) | 皮尔·法伯(PIERRE FABRE)
技术状态原研产品
成分|含量20mg
包装|存储1粒/盒 2度-8度(冰箱冷藏,禁止冷冻)
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通用中文 酒石酸长春瑞滨软胶囊 通用外文 VINORELBINE TARTRATE
品牌中文 诺维本 品牌外文 NAVELBINE
其他名称
公司 皮尔·法伯(PIERRE FABRE) 产地 法国(France)
含量 20mg 包装 1粒/盒
剂型给药 储存 2度-8度(冰箱冷藏,禁止冷冻)
适用范围 非小细胞肺癌、转移性乳腺癌以及难治性淋巴瘤、卵巢癌、头颈部肿瘤
通用中文 酒石酸长春瑞滨软胶囊
通用外文 VINORELBINE TARTRATE
品牌中文 诺维本
品牌外文 NAVELBINE
其他名称
公司 皮尔·法伯(PIERRE FABRE)
产地 法国(France)
含量 20mg
包装 1粒/盒
剂型给药
储存 2度-8度(冰箱冷藏,禁止冷冻)
适用范围 非小细胞肺癌、转移性乳腺癌以及难治性淋巴瘤、卵巢癌、头颈部肿瘤

使用说明书

(免责声明:本说明书仅供参考,不作为治疗的依据,不可取代任何医生、药剂师等专业性的指导。本站不提供治疗建议,药物是否适合您,请专业医生(或药剂师)决定。)
等待内容更新

中文说明

(免责声明:本说明书仅供参考,不作为治疗的依据,不可取代任何医生、药剂师等专业性的指导。本站不提供治疗建议,药物是否适合您,请专业医生(或药剂师)决定。)

通用名称:酒石酸长春瑞滨软胶囊
英文名称:Vinorelbine Tartrate Soft Capsule

 

 

 

【成份】

本品主要成份是酒石酸长春瑞滨。

【性状】

本品为浅棕色(规格为20mg)或粉红色(规格为30mg)软胶囊。内容物为粘性、澄清的浅黄至橘黄色溶液,基本无可见颗粒。

【功能主治】

本品适用于不可手术切除的局部晚期或转移性非小细胞肺癌,和转移性乳腺癌的单药或联合化疗。

【规格】

(1)20mg(按C45H54N4O3计);(2)30mg(按C45H54N4O3计)

【用法用量】

单药治疗
推荐方案为:
前3个疗程的用药
用药剂量以体表面积计为60 mg/m2,应每周1次服用。每3周为1个疗程。
后续用药
在3个疗程用药之后,建议将本品的剂量增至80 mg/m2,每周1次服用。但前3次应用60 mg/m2剂量时,嗜中性粒细胞若曾有1次低于500/mm3或超过1次低至500 - 1000/mm3间的患者应仍维持使用60 mg/m2剂量。
前三个疗程使用60mg/m2/周药量时
嗜中性粒细胞数量 第四个疗程的建议用药量
(mg/m2/周)
>1000 80
>或=500和<1000(一次发作) 80
>或=500和<1000(两次发作) 60
<500 60
在使用80mg/m2的剂量期间,如果病人的嗜中性粒细胞数量出现低于500/mm3以下的情况或者多次在500~1000/mm3之间,须推迟用药直到嗜中性粒细胞数量恢复正常,再用本药,并且将剂量由80 mg/m2/周减少至60 mg/m2/周。
从第四个疗程起,开始使用80mg/m2/周药量时
嗜中性粒细胞数量 下一个疗程的建议用药量
(mg/m2/周)
>1000 80
>或=500和<1000(一次发作) 80
>或=500和<1000(两次发作) 60
<500 60

 

【不良反应】

本药的副作用的统计来自138位病人的(其中76位患非小细胞支气管癌症,62位患乳腺癌)临床研究(前三个疗程使用60mg/m2每周的剂量,接下来的疗程使用80mg/m2每周的剂量)而得出的结论。
造血系统:限制性毒性为嗜中性白细胞减少症。18.8%的患者达到了三级嗜中性白细胞减少症(嗜中性粒细胞数量在500~1000/mm3之间)。23.2%的患者到达了四级嗜中性白细胞减少症(嗜中性粒细胞数量低于500/mm3),其中3%的患者出现了38℃以上的高烧现象。15.9%的患者出现了感染,但其中只有5.8%的患者感染较严重。
贫血是常见的,但通常只是轻度或中度贫血(72.5%的患者表现出一级或二级贫血症)。
血小板减少症也有发现,但少有严重的状况(8%的患者表现出一级或二级的血小板减少症)。
肠胃系统:一些副反应出现在消化系统。主要是以下现象:恶心(一级或二级:71%;三级:8.1%;四级:0.6%),呕吐(一级或二级:55.8%;三级:4.3%;四级:2.9%),腹泻(一级或二级:44.2%;三级:2.9%;四级:2.2%),以及食欲减退(一级或二级:29.7%;三级:6.5%;四级:1.5%)。在这些不良反应中,程度严重的情况比较少见。
预防性治疗如胃复安(metoclopramide)可以用来减少呕吐的次数。
8.7%的患者服药后出现了轻度或中度的口腔炎(一级或二级)。
周围和中枢神经系统:周围神经毒性反应:神经毒性一般限于深腱反射降低(8%的患者达到了一级或二级),程度严重的情况比较少见。仅有一位患者出现了部分可逆性的三级的运动性共济失调。
消化道自主神经系统:9.4%的患者出现神经源性便秘(一级或二级:9.8%),极少的患者发展成为麻痹性肠梗阻(1.4%)。
曾有报道发生致命后果的麻痹性肠梗阻。因此曾经有便秘史和那些同时接受吗啡或类吗啡药品的患者应适当配一些泻药。
皮肤:25.4%的患者发生脱发,多为轻度(一级或二级:24% ;三级:1.4%)。
其他副作用:接受酒石酸长春瑞滨软胶囊治疗的患者同样可能出现以下不良反应:
疲劳
发热
关节痛,特别会出现下颌骨痛,肌痛,胸部疼痛和肿瘤部位疼痛。
此外,口服长春瑞滨就和用其他长春花生物碱类药品类似,以下的不良作用也不能完全被排除:
心血管系统:偶见缺血性心脏病(心绞痛,心肌梗塞或心电图短暂改变)(参看注意事项/使用须知一栏)
肝脏:肝脏酶有短暂升高的迹象,但没有临床症状。
呼吸系统:和其他长春花生物碱类药品一样,静脉用酒石酸长春瑞滨可能引发呼吸困难,支气管痉挛,少数发展为间质性肺炎的情况,这种情况尤易见于使用酒石酸长春瑞滨注射剂并用丝裂霉素联合治疗的患者。
皮肤:长春花生物碱类药品偶导致全身皮肤不良反应。

 

【禁忌】

绝对禁忌:
对酒石酸长春瑞滨或其他长春花生物碱过敏的病人
消化系统有严重病变影响药物吸收的病人
曾经外科广泛切除过胃或者小肠的病人
与肿瘤无关的肝功能严重不全的病人
在妊娠及哺乳期的病人
黄热病疫苗(参看药物相互作用一栏)
二苯乙内酰脲,用作抗惊厥和抗癫痫的药(参看药物相互作用一栏)
相对禁忌:
减毒的活性疫苗
伊曲康唑

 

【注意事项】

酒石酸长春瑞滨软胶囊须在对化疗有丰富经验的合格医师的指导下使用。
若患者不慎咀嚼或吮吸了酒石酸长春瑞滨软胶囊,立即用清水漱口。如若可能,最好使用生理盐水漱口。
酒石酸长春瑞滨软胶囊表面融化或破损,里面的刺激性液体流出,接触到皮肤,口腔粘膜或眼睛,会产生有害作用。所以表面被损坏的胶囊不能再被服用,须交与药师或医生用适当的方法将被损坏胶囊销毁。如果不慎接触到,须立即用清水冲洗接触部位。如若可能,最好使用生理盐水冲洗。
如果在服药的几个小时之后出现呕吐现象,须停止使用正在使用的剂量。灭吐灵,胃复安(metoclopramide)之类的药品可以用来减轻呕吐症状。
如果嗜中性粒细胞数量低于1500/mm3而且血小板数在75000至100000/ mm3之间,须推迟治疗,直到各项指标恢复正常以后。对患者进行密切观察:参看用药剂量/服用方法一栏。
关于从第四疗程起将用药量从60mg/m2增加至80 mg/m2每星期的情况:参看用药剂量/服用方法一栏。
在使用80mg/m2的剂量期间,如果病人的嗜中性粒细胞数量低于500/ mm3以下或者不止一次在500~1000/ mm3之间,不仅要推迟用药直到嗜中性粒细胞数量恢复正常,并且要将剂量由80 mg/m2减少至60 mg/m2每星期。在以后的治疗中,也可能将剂量重新由60 mg/m2增至80 mg/m2每星期:有关情况参看用药剂量/服用方法一栏。
在临床试验期间,治疗开始就使用了80mg/m2的大剂量,导致部分患者出现嗜中性白血球极度低下。所以建议在治疗初始阶段使用60mg/m2的剂量。在身体可以适应的情况下,再增至80毫克每平方米每星期。
如体内出现感染的症状或体征,应立即进行全面检查。
使用须知
用药期间应密切观察血象变化,每次用药前均应检测血红蛋白、白细胞、嗜中性粒细胞和血小板计数。
有心脏血供不足的患者慎用。(参看副作用一栏)
对肝功能或肾功能不全的患者如何减量使用酒石酸长春瑞滨软胶囊尚不清楚。
既然长春瑞滨只有很小的一部分是通过肾脏系统排泄,那么从药物代谢的角度来说,对肾功能不全的患者减少酒石酸长春瑞滨软胶囊的使用剂量并无必要。
放射包括肝脏的病人不应同时服用酒石酸长春瑞滨软胶囊。

 

【孕妇及哺乳期妇女用药】

妊娠及哺乳期的患者禁止服用酒石酸长春瑞滨软胶囊(参看禁忌症一栏)。

【儿童用药】

儿童对本品的适应能力及疗效尚未有研究结果。

【老年用药】

临床使用中还没有发现老年患者和中青年患者的治疗反应有何不同,但不排除某一些老年患者显得更为敏感,对药物反应更大。

【药物相互作用】

将酒石酸长春瑞滨软胶囊与有骨髓毒性的药物共同使用会产生骨髓抑制。
细胞色素P450的异构体CYP 3A4与酒石酸长春瑞滨的代谢有关。酒石酸长春瑞滨若和此酶的诱导剂或抑制剂合用,如洛赛克LOSEC(OMEPRAZOLE)和氟西汀(fluoxe tine)合用,会影响到药物代谢。
适用于所有的细胞毒药物:因为肿瘤疾病导致形成血栓的风险增大,常配合抗凝药的治疗,但肿瘤病人的血凝状态经常在变化,再加上口服抗凝药和抗癌治疗的影响,因此采用抗凝治疗的病人必须增加INR(INTERNATIONAL NORMALIZED RATIO)的频率。
禁忌情况:
l 苯妥英钠(可预防抗癌药所引起的抽搐),但阿霉素、柔红霉素、卡铂、顺铂、卡氮芥、长春新碱、博米霉素、甲氨蝶呤会减少苯妥英钠的胃肠道吸收而引起抽搐。
l 抗黄热病疫苗:可引起致命的全身性疫苗疾病。
相对禁忌:
l 减毒的活性疫苗(除了抗黄热病疫苗):有引起可能致命的疫苗疾病的风险,此风险主要见于原来疾病已造成免疫抑制的病人。如果可能,尽量使用非活性疫苗(急性脊髓灰白质炎)。
特别谨慎注意:
l 苯妥英钠(化疗前已用),如化疗药给予阿霉素、、柔红霉素、卡铂、顺铂、卡氮芥、长春新碱、博米霉素、甲氨蝶呤:这些药可减少苯妥英钠胃肠道吸收引起抽搐。可以间歇地配合使用苯(并)二氮(镇静药)防止抽搐。
必须注意:
l 环孢菌素(在用阿霉素、依托泊苷时):可引起极度免疫系统抑制并伴有淋巴细胞增加。
l 他克莫司(从环孢菌素推断得出的结论):导致极度免疫系统衰竭并伴有淋巴扩散的危险。
关于长春花生物碱的特别提示:
劝诫情况(相对禁忌):
l 伊曲康唑:由于肝脏代谢减退,增加了抗有丝分裂药物的神经毒性。
必须注意:
l 丝裂霉素C:丝裂霉素和长春花生物碱引起的肺部毒性有增加的风险。
营养与药物的相互作用:
长春瑞滨的药效不受同时进行的食物消化的影响。

 

【药物过量】

人体试验:酒石酸长春瑞滨软胶囊过量使用的情况没有记载。然而,酒石酸长春瑞滨软胶囊的大剂量使用可能会诱发骨髓再生障碍,并可能伴有感染性综合症或麻痹性肠梗阻。
在过量使用的情况下所能采取的措施:总的来说,可以采用的手段也就是输血以及给予全身支持,生血因子或抗生素可由医生自行决定。目前还没有发现酒石酸长春瑞滨软胶囊的过量使用的解毒剂。

【药理毒理】

药理作用:
本药是一种半合成的长春花生物碱,是一种周期特异性抗癌药。作用与长春新碱相似,主要通过与微管蛋白结合,使细胞在有丝分裂过程中微管形成障碍;在高浓度时尚可阻断细胞从G2期进入M期。本药除了作用于有丝分裂的微管以外,也作用于轴突微管,故可引起神经毒性。
毒理研究:
遗传毒性:动物试验显示本品可导致非整数倍数和多倍数染色体的现象。
致癌性:尚不清楚,未见明确的动物研究结果。
生殖毒性:大鼠试验结果显示,本品可导致胚胎死亡或畸形。本品静脉给药0.26mg/kg,每3天1次,大鼠未见明显毒性发生;剂量为1 mg/kg,后代动物出生后至第七周出现体重增长缓慢。
动物的药物过量反应:动物过量用药出现毛发脱落,行为举止异常,体重下降、肺脏损伤和不同程度的骨髓再造障碍。
耐受性:犬以最大剂量给药,未显示对血液动力学有影响,仅出现了少量紊乱,与其它长春碱类药物反应一致。灵长类动物连续用药39周,未发现对心血管系统有影响。

 

【药代动力学】

口服酒石酸长春瑞滨软胶囊80毫克每平方米之后,药品被迅速吸收,血清峰浓度于1.5至3小时(Tmax)后到达,峰值(Cmax)大约为130ng/ml。绝对生物利用度为40%,同时进食不会影响到长春瑞滨的药效。口服长春瑞滨60毫克每平方米或80毫克每平方米可以和静脉注射25毫克每平方米或30毫克每平方米的长春瑞滨达到相同的血浓度。口服后个体间血浓度差异的程度与静脉给药相同。剂量提高后血浓度相应提高。血清蛋白的结合率较低,为13.5%;但是,长春瑞滨和血细胞的结合率很高,特别是和血小板,达到了78%。
长春瑞滨广泛地分布于各器官组织中,平衡后的分布容积很高。静脉注射后达到11~21.1/kg,提示组织摄取是高的。
通过肺部手术时组织切片检测,肺部组织与血浆的浓度比例高于300,提示长春瑞滨在肺部组织里的渗透力很强。
长春瑞滨血浆的清除半衰期约为35至40小时。
口服酒石酸长春瑞滨软胶囊主要通过胆汁排泄,少量随尿液排出。
未发生过变化的长春瑞滨是在服用者的尿液和粪便中发现的主要成份。4-0-脱乙酰基-长春瑞滨是在血液和胆汁中检测到的活性代谢物,并于胆汁中排泄。在长春瑞滨的代谢中,没有葡糖醛酸化合和硫化合的参与。

 

【贮藏】

在2℃至8℃条件下保存(冷藏)。本品应保存于原包装内。

【包装】

可推式PVC/PVDC/铝塑包装。
包装规格:1粒/盒。

 

 

【生产企业】

公司名称:PIERRE FABRE MEDICAMENT
地 址:45,Place Abel Gance F-92100 BOULOGNE-France
生产企业:PIERRE FABRE MEDICAMENT PRODUCTION
地 址:Etablissement Aquitaine Pharm International Avenue du Bearn-64320


外文说明

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Navelbine
Generic Name: Vinorelbine
Other Names: Vinorelbine Tartrate
Drug Type:
Navelbine is an anti-cancer ("antineoplastic" or "cytotoxic") chemotherapy drug.  Navelbine is classified as a "plant alkaloid."
For more detail, see "How Navelbine Works" section below.
What Navelbine Is Used For:
Non-small cell lung cancer
Some healthcare providers may also give Navelbine for breast cancer, ovarian cancer, or Hodgkin's disease.
Note: If a drug has been approved for one use, physicians sometimes elect to use this same drug for other problems if they believe it might be helpful.
How Navelbine Is Given:
Navelbine is given through a vein by intravenous injection (IV push) or infusion (IV).  There is no pill form.
Navelbine is a vesicant.  A vesicant is a chemical that causes extensive tissue damage and blistering if it escapes from the vein. 
The nurse or doctor who gives Navelbine must be carefully trained. 
If you notice pain, redness or swelling at the IV site while you are receiving Navelbine, alert your health care professional immediately.
The amount of Navelbine you will receive depends on many factors, including your height and weight, your general health or other health problems, and the type of cancer being treated.  Your doctor will determine your dose and schedule.
Navelbine Side Effects:
Along with its needed effects, Navelbine may cause some unwanted side effects. Important things to remember about the side effects of Navelbine include:
Most people do not experience all of the side effects listed Side effects are often predictable in terms of their onset and duration
Side effects are almost always reversible and will go away after treatment is complete
There are many options to help minimize or prevent side effects
There is no relationship between the presence or severity of side effects and the effectiveness of Navelbine.
The following side effects are common (occurring in greater than 30%) for patients taking Navelbine:
Low blood counts. Your white and red blood cells may temporarily decrease.  This can put you at increased risk for infection or anemia. 
Nadir: Meaning low point, nadir is the point in time between chemotherapy cycles in which you experience low blood counts.
Onset: 4-7 days
Nadir: 7-10 days
Recovery: 14-21 days
Nausea or vomiting
Muscle weakness
Constipation
The following are less common side effects (occurring in 10-29%) for patients receiving Navelbine:
Pain along the site where Navelbine was given
Peripheral neuropathy (numbness in your fingers and toes) may occur with repeated doses.
This should be reported to your healthcare provider.
Diarrhea
Hair loss
Low platelet (these help to clot the blood) counts.  This can put you at increased risk for bleeding.
Not all side effects are listed above, some that are rare (occurring in less than 10% of patients) are not listed here. 
However, you should always inform your health care provider if you experience any unusual symptoms.
When To Contact Your Doctor or Health Care Provider:Contact your health care provider immediately, day or night, if you should experience any of the following symptoms:
Fever of 100.5º F (38º C) or higher, chills (possible signs of infection)
The following symptoms require medical attention, but are not emergency situations. Contact your health care provider within 24 hours of noticing any of the following.
Nausea (interferes with ability to eat and unrelieved with prescribed medications)
Vomiting (vomiting more than 4-5 times in a 24-hour period)
Unusual bleeding or bruising
Black or tarry stools, or blood in your stools or urine
Constipation
Diarrhea (4-6 episodes in a 24-hour period)
Lip or mouth sores
Always inform your health care provider if you experience any unusual symptoms.
Navelbine Precautions:
Before starting Navelbine treatment, make sure you tell your doctor, as well as all healthcare providers, about any other medications you are taking (including over-the-counter, vitamins, or herbal remedies).  Do not take aspirin or products containing aspirin unless your healthcare provider permits this.
Inform your health care professional if you are pregnant or may be pregnant prior to starting this treatment. Pregnancy category D(Navelbine may be hazardous to the fetus. 
Women who are pregnant or become pregnant must be advised of the potential hazard to the fetus).
For both men and women: Do not conceive a child (get pregnant) while taking Navelbine.
Barrier methods of contraception, such as condoms, are recommended. Discuss with your doctor when you may safely become pregnant or conceive a child after therapy.
Do not breast feed while taking Navelbine.
Navelbine Self Care Tips:
Apply warm compress if you have any pain, redness or swelling at the IV site, and notify your doctor.
Keep your bowels moving. Your health care provider may prescribe a stool softener to help prevent constipation that may be caused by Navelbine. 
If you experience diarrhea of greater than 3-5 stools per day, contact your healthcare provider and increase your fluid intake.
Drink 2 to 3 quarts of fluid every 24 hours, unless you were told to restrict your fluid intake, and maintain good nutrition. This will decrease your chances of being constipated, and prevent dehydration.
You may be at risk of infection so try to avoid crowds or people with colds, and report fever or any other signs of infection immediately to your healthcare provider. 
Wash your hands often.
Use an electric razor and soft toothbrush to minimize bleeding.
Avoid contact sports or activities that could cause injury.
Avoid sun exposure.  Wear SPF 15 (or higher) sun block and protective clothing.
To reduce nausea, take anti-nausea medications as prescribed by your doctor, and eat small, frequent meals.
Keep your mouth clean with baking soda and salt rinses. You can mix 1/4 tsp. of baking soda and 1/4 tsp. salt in 8 ounces of water, and use as a mouthwash, to avoid or decrease the severity of mouth sores. 
In general, drinking alcoholic beverages should be minimized or avoided.  You should discuss this with your doctor.
If you experience symptoms or side effects, be sure to discuss them with your health care team.  They can prescribe medications and/or offer other suggestions that are effective in managing such problems.
Monitoring and Testing While Taking Navelbine:
Periodic blood work will be obtained to monitor your complete blood count (CBC). Your doctor will order blood tests and other tests as needed to monitor side effects and check your response to therapy.
How Navelbine Works:
Cancerous tumors are characterized by cell division, which is no longer controlled as it is in normal tissue.   "Normal" cells stop dividing when they come into contact with like cells, a mechanism known as contact inhibition. 
Cancerous cells lose this ability. 
Cancer cells no longer have the normal checks and balances in place that control and limit cell division.  The process of cell division, whether normal or cancerous cells, is through the cell cycle. 
The cell cycle goes from the resting phase, through active growing phases, and then to mitosis (division).
The ability of chemotherapy to kill cancer cells depends on its ability to halt cell division. 
Usually, the drugs work by damaging the RNA or DNA that tells the cell how to copy itself in division. 
If the cells are unable to divide, they die.  The faster the cells are dividing, the more likely it is that chemotherapy will kill the cells, causing the tumor to shrink. 
They also induce cell suicide (self-death or apoptosis).
Chemotherapy drugs that affect cells only when they are dividing are called cell-cycle specific.  Chemotherapy drugs that affect cells when they are at rest are called cell-cycle non-specific. 
The scheduling of chemotherapy is set based on the type of cells, rate at which they divide, and the time at which a given drug is likely to be effective.  This is why chemotherapy is typically given in cycles.
Chemotherapy is most effective at killing cells that are rapidly dividing.  Unfortunately, chemotherapy does not know the difference between the cancerous cells and the normal cells. The "normal" cells will grow back and be healthy but in the meantime, side effects occur.  The "normal" cells most commonly affected by chemotherapy are the blood cells, the cells in the mouth, stomach and bowel, and
the hair follicles; resulting in low blood counts, mouth sores, nausea, diarrhea, and/or hair loss.  Different drugs may affect different parts of the body.
Navelbine belongs to a class of chemotherapy drugs called plant alkaloids. Plant alkaloids are made from plants.  The vinca alkaloids are made from the periwinkle plant (catharanthus rosea).
The taxanes are made from the bark of the Pacific Yew tree (taxus). 
The vinca alkaloids and taxanes are also known as antimicrotubule agents.
The podophyllotoxins are derived from the May apple plant.
Camptothecan analogs are derived from the Asian "Happy Tree" (Camptotheca acuminata). 
Podophyllotoxins and camptothecan analogs are also known as topoisomerase inhibitors.  The plant alkaloids are cell-cycle specific.  This means they attack the cells during various phases of division.
Vinca alkaloids: Vincristine, Vinblastine and Navelbine
Taxanes:  Paclitaxel and Docetaxel
Podophyllotoxins:  Etoposide and Tenisopide
Camptothecan analogs: Irinotecan and Topotecan
Antimicrotubule agents (such as Navelbine), inhibit the microtubule structures within the cell. 
Microtubules are part of the cell's apparatus for dividing and replicating itself.  Inhibition of these structures ultimately results in cell death.
Note:  We strongly encourage you to talk with your health care professional about your specific medical condition and treatments.
The information contained in this website is meant to be helpful and educational, but is not a substitute for medical advice.