药品信息:
药理作用
1. Nateglinide是胺基酸(苯丙胺酸Phenylalanine)的衍生物，在化学上和药理上均不同于其他抗糖尿病药物。它可恢复初期的胰岛素分泌，并使餐后血中的葡萄糖和HbA1C减少。初期的胰岛素分泌，是维持正常血糖控制的必须机转。餐前服用Nateglinide，可恢复第二型糖尿病患者所缺少的初期或第一期胰岛素分泌。这些机转是经由和胰脏β细胞上K⁺ATP通道迅速而短暂交互作用而达成的。电理学的研究证实了，Nateglinide对胰脏β细胞的选择性大于对心血管系统K⁺ATP通道的选择性的300倍。
2. 和其他口服的抗糖尿病药物不同，Nateglinide在餐后15分钟内可显著地引起胰岛素分泌。如此可使餐后血中葡萄糖的高峰变缓。胰岛素的量在3～4小时后回复至基准线，而减少了餐后的胰岛素过多征状，这和延迟性的低血糖有关。
3. 由Nateglinide诱导而分泌胰岛素的胰脏β细胞对葡萄糖是敏感的，因此葡萄糖浓度下降时，胰岛素的分泌也减少。相反地，和食物一起服用或葡萄糖的注入，会使胰岛素分泌明显地增加。当在周围葡萄糖浓度较低时，Starlix刺激胰岛素分泌的作用会减少，如此可提供额外的保护而免于低血糖症。
4. 在临床的研究中，经测量的HbA1C及餐后葡萄糖显示，本品的单独治疗可改善血糖的控制。本品和主要作用于空腹血糖值的Metformin共同治疗，和其中在一种药物单独使用相比较，其对HbA1C之降低具有协同作用，因为这些药物是以互补的机转作用。
适应症
单独治疗或与 METFORMIN 合并使用，以治疗第二型糖尿病病患（非胰岛素依赖型糖尿病）。
用法用量
本品需在饭前服用。通常在餐前立即服用(约1分钟)，也可以在餐前至少30分钟内服用。
1. 单独治疗法：一般的剂量是120mg于餐前服用。剂量的调整需根据周期性的Glycosylated Haemoglobin(HbA1C)的测量。由于本品主要疗效是减少进餐时间血中的葡萄糖，(形成HbA1C的主要原因之一)，可利用餐后1～2小时的葡萄糖值，来监测对本品的治疗反应。在临床的研究中，本品在主餐(早餐、午餐及晚餐)之前投药。
2. 合并疗法：对于以本品单独治疗，且尚需附加用药的病患，可加上Metformin至维持剂量。对于以Metformin单独治疗，且尚附加用药的病患，本品的一般剂量是餐前给予120mg。部份已接近期治疗目标值的病患(如：HbA1C<7.5%)，餐前服用60mg已足够。
药动力学
1. 于餐前口服本品药锭后，Nateglinide迅速地被吸收，达到平均最高药物血中浓度的时间少于1小时。 Nateglinide迅速且几乎完全地(≧90%)自口服溶液中被吸收。绝对口服生体可用率估计为72%。每日在三餐前，给予第二型糖尿病患者60至240mg剂量连续一个星期，Nateglinide对于AUC及Cmax显示出直线的药物动力学，Tmax不受剂量影响。
2. 本品任肝脏进行的氧化代谢，其主要酵素是P450 2C9其次为CYP 3A4；83%由尿液排出，其排除半衰期平均为1.5小时。
副作用
1. 常见的：食欲增加、心悸、恶心、疲劳及虚弱。这些症状通常是轻微的，当必要时可服用糖类而易于处理。临床试验中，有2.4%病患出现经由血浆葡萄糖<3.3mmol/L确认的低血糖症状。
2. 偶见的：有少数肝脏酵素增加的病例报告。但它是轻微且短暂的，而且鲜少造成治疗中断。其他还有：出疹、发痒及荨麻疹的过敏反应，胃肠的病症(如：腹痛、消化不良、腹泻)、头痛，以及这类病患族群可能会伴随出现的呼吸道感染。
交互作用
1. 体外研究指出，Nateglinide主要被细胞色素P450的酵素CYP 2C9(70%)代谢；较少部分被CYP 3A4(30%)代谢。由于它在体外具抑制Tolbutamide代谢的能力，可见Natelinide在体内可能是CYP 2C9的抑制剂。根据体外实验，CYP 3A4代谢反应预期不受抑制。总而言之，这些发现显示临床药物动力学的交互作用可能性不高。
2. Nateglinide对于Warfarin(CYP 3A4及CYP 2C9的受质)、Diclofenac(CYP 2C9的受质)、Troglitazone(CYP 3A4的诱导剂)或毛羊地黄(Digoxin)的药物动力学特性，并无临床上相关影响。因此并用时，本品、Digoxin、Warfarin或Diclofenac的剂量都不需要调整。相似地，本品和其他口服的抗糖尿病药物，如：Metformin、Glibenclamide，均无临床上有意义的药物动力学交互作用。
3. 某些药物，包括非类固醇抗发炎药物、水杨酸盐、单胺氧化酶抑制物(Monoamine Oxidase Inhibitor)及非选择性β-肾上腺素的阻断剂(Non-selective beta-adrenergic)，可能会促进口服抗糖尿病药物降低血糖的作用。
4. 有些药物，包括利尿剂Thiazide、肾上腺皮质素、甲状腺产物及交感神经药，可能会减少口服抗糖尿病药物降低血糖的作用。
禁忌
(1)对于主成分或任何赋形剂过敏的病患。 (2)第一型糖尿病(胰岛素依存型糖尿病，IDDM)患者。 (3)酮酸症糖尿病患。 (4)孕妇及授乳妇。
注意事项
1. 与其他口服抗糖尿病药物并用会增加低血糖的危险性。正在服用乙型阻断剂(β-Blocker)的患者，其低血糖症状，较不易确认。
2. 对于驾驶能力及机器使用的影响─病患应被告知需注意低血糖时，避免驾驶及操作机器。
What is Starlix?
Starlix (nateglinide) is an oral diabetes medicine that helps control blood sugar levels. This medicine helps your body respond better to insulin produced by your pancreas.
Starlix is used together with diet and exercise to treat type 2 diabetes.
Other diabetes medicines are sometimes used in combination with Starlix if needed.
Important information
You should not use Starlix if you have type 1 diabetes, or if you are in a state of diabetic ketoacidosis (call your doctor for treatment with insulin).
Take care not to let your blood sugar get too low. Low blood sugar (hypoglycemia) can occur if you skip a meal, exercise too long, drink alcohol, or are under stress. Symptoms include headache, hunger, weakness, sweating, tremors, irritability, or trouble concentrating. Carry hard candy or glucose tablets with you in case you have low blood sugar. Other sugar sources include orange juice and milk. Be sure your family and close friends know how to help you in an emergency.
Starlix is only part of a complete program of treatment that also includes diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely. Changing any of these factors can affect your blood sugar levels.
Before taking this medicine
You should not use Starlix if you are allergic to nateglinide, or if you have:
type 1 diabetes; or
if you are in a state of diabetic ketoacidosis (call your doctor for treatment with insulin).
To make sure Starlix is safe for you, tell your doctor if you have:
liver disease; or
gout.
It is not known whether Starlix will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medicine.
Nateglinide can pass into breast milk and may harm a nursing baby. You should not breast-feed while using Starlix.
How should I take Starlix?
Take Starlix exactly as prescribed by your doctor. Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.
Starlix is usually taken 3 times daily, within 30 minutes before eating a meal. Follow your doctor's instructions. If you skip a meal, do not take your dose of Starlix. Wait until your next meal.
Your blood sugar will need to be checked often, and you may need other blood tests at your doctor's office.
Low blood sugar (hypoglycemia) can happen to everyone who has diabetes. Symptoms include headache, hunger, sweating, confusion, irritability, dizziness, or feeling shaky. Always keep a source of sugar with you in case you have low blood sugar. Sugar sources include fruit juice, hard candy, crackers, raisins, and non-diet soda. Be sure your family and close friends know how to help you in an emergency.
If you have severe hypoglycemia and cannot eat or drink, use a glucagon injection. Your doctor can prescribe a glucagon emergency injection kit and tell you how to use it.
Check your blood sugar carefully during times of stress, travel, illness, surgery or medical emergency, vigorous exercise, or if you drink alcohol or skip meals. These things can affect your glucose levels and your dose needs may also change. Do not change your dose of Starlix or your dosing schedule without your doctor's advice.
Starlix is only part of a treatment program that may also include diet, exercise, weight control, blood sugar testing, and special medical care. Follow your doctor's instructions very closely.
Store at room temperature away from moisture and heat.
Starlix dosing information
Usual Adult Dose for Diabetes Type 2:
120 mg orally three times daily before meals.
-or-
60 mg three times daily before meals (patients who are near goal HbA1c).
See also: Dosage Information (in more detail)
What happens if I miss a dose?
Take the missed dose as soon as you remember, but only if you are getting ready to eat a meal. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.
What happens if I overdose?
Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.
Symptoms of severe hypoglycemia include extreme weakness, blurred vision, sweating, trouble speaking, tremors, stomach pain, confusion, and seizure (convulsions).
What should I avoid while taking Starlix?
Avoid drinking alcohol. It lowers blood sugar and may interfere with your diabetes treatment.
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