贝卡普勒明(Becaplermin)

商品名：Regranex

开发与上市厂商：(美)Chiron公司研制，美国Johnson & Johnson公司上市。1998年11月在美国首先上市。

药效分类：血小板衍生生长因子激动剂

药理
腿和足的神经病性溃疡是糖尿病的严重并发症。有些因素如周围血管症，神经病以及创口复盖物较厚，均会使溃疡愈合缓慢，且难以处理。当治疗无效时，便会继发感染和坏疽，以致最后必须截肢。
在正常的愈合期中，损伤引起的血块中的血小板可向组织释放各种生长因子，其中包括血小板衍生生长因子(PDGF)。该生长因子是一种有效的巨噬细胞趋化吸引剂，并能促进成纤维细胞，平滑肌细胞和毛细血管内皮细胞的活性，导致创伤肉芽组织的形成，最终达到创面愈合。
PDGF是一种由两个多肽链组成的蛋白质，这种蛋白质不是两个A链(PDGF-AA)，就是两个B链(PDGF-BB)。这种PDGF-BB异构型对成纤维细胞具有更强的影响力。本品就是这种生长因子的基因工程制剂，是将人PDGF的B链插入酵母细胞表达产生的。对在创伤修复中涉及到的细胞，本品具有与内源性PDGF-BB一样的趋化和增生作用，尤其表现在促进肉芽组织的生长上。

临床评价
至少一处达到Ⅲ或Ⅳ级溃疡的118例糖尿病性下肢溃疡病人，病程至少8周，为期20周的多中心双盲对照研究证实，采用本品0.003%凝胶治疗的病人中，达到完全愈合者占48%，接受安慰剂的病人有25%获安全愈合，说明本品对促进糖尿病性溃疡愈合具有明显的作用。另一研究对382例病人进行的类似研究显示，在使用本品0.01%凝胶的病人中的50%完全愈合，对照组愈合者为35%。此外，治疗组对对照组相比，创伤面积明显缩小，前者的愈合速度几乎是后者的两倍。对已达愈合的病人进行的为期3个月的跟踪随访，复发率约为30%。

适应证
本品可用于治疗表面面积低于5cm2的全白增厚，神经病性，慢性糖尿病溃疡的肉芽组织形成和创口愈合。

不良反应
本品可能会引起感染，溃疡，红斑，疼痛，罕见有大泡疹，水肿。在所有临床对照研究中，本品凝胶均易于耐受，两组不良反应率和严重程度均无显著差异。

注意事项
使用本品必须同时给予良好的创伤护理。
必须在切除坏组织的溃疡部位进行清创后才可使用本品，在有效促进溃疡愈合中，清创术具有明显的作用。
在开始治疗前，应排除骨髓炎，周围动脉病和恶性病变；在使用本品治疗开始前，应先治疗感染。
作为生长因子，PDG有可能使某些癌细胞生长。但药动学研究证实，在局疗用药后，仅有不明显的本品进入血液循环中。尚无证据说明本品有诱发全身或局部的突变作用。
避免在同一部位使用其它局用制剂，以防止药物相互作用。
临床溃疡部位有肿瘤存在，已知病人有恶性病变，以及孕妇和哺乳期妇女，18岁以下少年禁用本品。

剂量和用法
用药前先清创，然后将本品在整个溃疡面上涂上薄薄一层，一日1次，用生理盐水敷料覆盖。10周后，如病情未改善则停止治疗；如有改善，持续治疗直到完全愈合，最长疗程为20周。

制剂：凝胶剂，含本品0.01%。

Becaplermin Topical gel

What is this medicine?

BECAPLERMIN (be KAP ler min) is used on the skin to treat ulcers on the lower legs in patients with diabetes.
 
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•cancer at the site of the ulcer
•wounds that are closed by your health care professional
•wounds that show exposed joints, tendons, ligaments, or bone
•an unusual or allergic reaction to becaplermin, parabens, metacresol, or other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

This medicine is for external use only. Follow the directions on the prescription label. Wash your hands before use. Squeeze the prescribed amount of gel onto a clean, non-absorbable surface like wax paper. With a cotton swab, tongue depressor, or a similar application aid, spread an even layer of the gel over the ulcer. Cover the ulcer with a saline-moistened gauze dressing. After 12 hours, remove the gauze dressing and rinse the ulcer with saline or water to remove excess gel. Apply a new piece of saline-moistened gauze dressing to the ulcer. Do not use your medicine more often than directed. Finish the full course of medicine prescribed by your doctor or health care professional even if you think your condition is better.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

Interactions are not expected. Do not use any other skin products on the treated area without asking your doctor or health care professional.

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular checks on your progress. Your doctor or health care professional may change your dose weekly or every other week as the size of your ulcer changes. If your skin ulcer does not get smaller in 10 weeks or does not get better after 20 weeks, ask your doctor or health care professional if you should continue using this medicine.

This medicine works best when used with other methods for good skin ulcer care such as not bearing weight on the leg that has the skin ulcer.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•reddened skin near ulcer
•skin rash near ulcer

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store in the refrigerator at 2 to 8 degrees C (36 to 46 degrees F). Do not freeze. Throw away any unused portion after the expiration date.