部份中文那格列奈处方资料（仅供参考）
通用名称：那格列奈片
英文名称：Nateglinide Tablet
适应症
本品可以单独用于经饮食和运动不能有效控制高血糖的2型糖尿病病人。也可用于使用二甲双胍不能有效控制高血糖的2型糖尿病病人，采用与二甲双胍联合应用，但不能替代二甲双胍。
用法用量
本品的常用剂量为餐前120mg,可单独应用,也可与二甲双胍联合应用,剂量应根据定期的HbAlc检测结果调整。
不良反应
1.低血糖：与其它抗糖尿病药物一样,服用那格列奈后,可观察到低血糖的症状。这些症状包括出汗、发抖、头晕、食欲增加、心悸、恶心、疲劳和无力。这些症状一般较轻且较易处理,如需要可进食碳水化合物。临床研究报告显示出现低血糖症状,且证实血糖降低（血糖<3.3mmlo/L）的患者比例为2.4%。极少患者出现肝酶增高,其程度较轻且为一过性,很少导致停药。
2.过敏：极少有皮疹、瘙痒和荨床疹等过敏反应的报道。
3.其它反应：临床试验发现的其它不良事件,包括胃肠道反应（腹痛、消化不良、腹泻）、头痛以及糖尿病人群可能同时伴发的一些临床症状（如呼吸道感染）等在那格列奈治疗组与安慰剂治疗组中发生的比例相似。
禁 忌
1.对药物的活性成分或任何赋型剂过敏。
2.1型糖尿病（胰岛依赖型糖尿病）。
3.糖尿病酮症酸中毒。
4.妊娠和哺乳（参看：孕妇及哺乳期妇女用药）。
5.重度感染、手术前后或有严重外伤的患者慎用。
注意事项
1.低血糖：本品可以引起低血糖现象,其发生的频率与糖尿病严重程度、血糖控制水平、以及病人其他相关情况有关。老年病人、营养不良的病人、伴有肾上腺或垂体功能不全的病人对降糖药比较敏感,易发生低血糖。剧烈运动、饮酒、腹泻呕吐、进食减少、或合用其他抗糖尿病药物时,低血糖的危险性增加。对伴有自主神经病变或合并使用β受体阻滞剂者发生低血糖时难以破认识。那格列奈必须餐前口服,以减少低血糖的危险。病人不准备进食时,不可服用那格列奈。那格列奈必须慎用于伴有中重度肝功能损害的病人。
2.血糖控制失常：当病人伴有发热、感染、创伤或手术时血糖可以暂时性升高。此时应使用胰岛素代替那格列奈。那格列奈使用一段时期后,可以发生继发失效或药效减弱。
3.本品具有快速促进胰岛素分泌的作用。该作用点与磺酰脲类制剂相同。但本品与磺酰脲类制剂的相加、相乘的临床效果以及安全性尚未被证实,所以不能与磺酰脲类制剂并用。
4.与其它口服抗糖尿病药物合用可增加低血糖的危险。
5.对驾驶和操作机械能力的影响。
6.应提醒患者驾驶或操纵机器时采取预防措施避免低血糖。
儿童用药
尚未对那格列奈在儿童使用的安全性和有效性进行评价。因此,不推荐儿童使用那格列奈。
老年患者用药
未观察到老年患者和普通人群间在药物安全性和有效性方面有差异。此外年龄不影响那格列奈的药代动力学特征。因此对于老年患者没有必要调整剂量。
孕妇及哺乳期妇女用药
那格列奈对小鼠和兔无致畸作用。尚无妊娠妇女服此药的经验,因此,无法估计人类妊娠时那格列奈的安全性。与其它口服抗糖尿病药物一样,妊娠时不推荐使用那格列奈。那格列奈口服后可自小鼠乳汁中排出。尽管尚不清楚那格列奈是否能从人乳汁中排出,母乳喂养婴儿出现低血糖的可能性是存在的。因此,那格列奈不应用于哺乳期妇女。
药物相互作用
1.体外实验发现其可抑制甲磺西脲的代谢,据此判断那格列奈在体内是CYP2C9的潜在抑制剂。体外实验表明该药对CYP3A4的代谢反应无抑制作用。
2.合用时无论那格列奈、地高辛、华法令或双氯芬酸均无需调整剂量。同样,那格列奈与其它口服抗糖尿病药物,如与二甲双胍或格列苯脲间不存在具有临床意义的药代动力学方面的相互作用。
3.口服抗糖尿病药的降血糖作用可被某些药物所加强,这些药物包括非甾体类抗炎药、水杨酸盐、单胺氧化酶抑制和非选择性β-肾上腺素能阻滞剂。
4.口服抗糖尿病的降血糖作用可被某些药物所削弱,这些药物包括噻嗪类、可的松、甲状腺制剂和类交感神经药。
药物过量
临床研究显示,逐渐增中那格列奈的剂量至每日720毫克共服用7天时患者仍可耐受。无那格列奈过量的临床试验经验。然而,药物过量可增强降血糖作用,出现低血糖症状。对不伴有意识丧失或神经症状的低血糖症门面,均可通过口服葡萄糖、调整药物剂量或/和进食来治疗。出现昏迷、癫痫发作或其它神经症状的低血糖反应需静脉注射葡萄糖来治疗。由于那格列奈的蛋白结合率较高,因此透析不是一个将其从血液中清除的有效方法。
药理毒理
那格列奈为氨基酸衍生物,为口服抗糖尿病药,用于2型糖尿病人的治疗。那格列奈的作用依赖于胰岛β细胞的功能。那格列通过与β细胞上的ATP敏感性K+通道受体结合并将其关闭,使细胞去极化,钙通道开放,钙内流,刺激胰岛素的分泌,降低血糖。那格列奈促胰岛素分泌作用依赖于葡萄糖水平,在葡萄糖水平较低时,促胰岛素分泌减弱。那格列奈有高度的组织选择性,与心肌和骨骼肌的亲和力低。
药代动力学
1.吸收和生物利用度餐前服用那格列奈片后那格列奈迅速吸收,药物浓度平均峰值通常出现在服药1小时内。以溶液形式口服时,那格列奈几乎完全并迅速吸收（≥90%）。口服的绝对生物利用度约为72%。每日三餐前给2型糖尿病患者那格列奈60~240mg共1周后,那格列奈显示出线性的药代动力学特征,AUC和Cmnx均如此。并且Tmnx不依赖于药物剂量。
2.分布依据静脉给药数据估计的那格列奈稳态分布容积大约是10升。体外研究表明那格列奈大部分（97~99%）与血浆蛋白结合,主要是血浆白蛋白和少量的a1酸性糖蛋白。在那格列奈0.1~10kg/ml的测度范围内其与血浆蛋白结合的能力与药物浓度无关。
3.代谢那格列奈在清除前主要通过混合功能氧化酶系代谢。在人主要的代谢产物来自于异丙其侧链的羟化,羟化或发生于次甲基碳原子或发生于某一甲基基团,其活性分别较那格列奈低5-6倍和3倍。较少的代谢产物是那格列奈的二醇、异丙醇和酰基葡萄糖醛酸式。只有那格列奈的少量异丙醇代谢产物具有活性,强度与那格列奈相当。细胞色素P450 CYP2C9是那格列奈代谢主要的催化剂,其次是CYP 3A4,这些结论是用人肝微粒体和含单一表达人CYP同工酶的微粒体进行的体外实验而得出的。
4.排泄那格列奈及其代谢产物的清除迅速彻底。服药后6小时内约75%的[14C]那格列奈可在尿中回收。大部分（83%）的[14C]那格列奈在尿中排泄,另10%在粪便中排泄。大约所服药物的6~16%以原形在尿中排泄。在健康志愿者和2型糖尿病患者中那格列奈血浆浓度迅速降低且那格列奈清除半衰期平均为1.5小时。与较短的清除半衰期相一致,那格列奈剂量加倍至240mg,每日3次也无明显蓄积。
5.食物影响餐后服用那格列奈,其吸收（AUC）程度不受影响。但吸收速度降低,表现为峰浓度（Cmnx）降低和血浆达峰时间（Tmnx）延迟。因此推荐餐前服用那格列奈。通常餐前1分钟服用,也可餐前30分钟内服用。
贮 藏
密封，置阴凉干燥处。
本品完整资料附件：
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5CBDA9BC-3C0D-4D75-A37A-994844680C8C
Starlix Tablet(Nateglinide)
1. DESCRIPTION
Nateglinide is an oral antidiabetic agent used in the management of Type 2 diabetes mellitus [also known as non-insulin dependent diabetes mellitus (NIDDM) or adult-onset diabetes]. Nateglinide, (-)-N-[(trans-4-isopropylcyclohexane)carbonyl]-D-phenylalanine, is structurally unrelated to the oral sulfonylurea insulin secretagogues. The structural formula is as shown:
Nateglinide is a white powder with a molecular weight of 317.43. It is freely soluble in methanol, ethanol, and chloroform, soluble in ether, sparingly soluble in acetonitrile and octanol, and practically insoluble in water. Nateglinide biconvex tablets contain 60 mg, or 120 mg, of nateglinide for oral administration.
Inactive Ingredients: colloidal silicon dioxide, croscarmellose sodium, hydroxypropyl methylcellulose, iron oxides (red or yellow), lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyethylene glycol, povidone, talc, and titanium dioxide.
2. INDICATIONS AND USAGE
Nateglinide is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
3. DOSAGE AND ADMINISTRATION
Nateglinide should be taken 1 to 30 minutes prior to meals.
Monotherapy and Combination with Metformin or a Thiazolidinedione
The recommended starting and maintenance dose of nateglinide, alone or in combination with metformin or a thiazolidinedione, is 120 mg three times daily before meals.
The 60-mg dose of nateglinide, either alone or in combination with metformin or a thiazolidinedione, may be used in patients who are near goal HbA1C when treatment is initiated.
Dosage in Geriatric Patients
No special dose adjustments are usually necessary. However, greater sensitivity of some individuals to nateglinide therapy cannot be ruled out.
Dosage in Renal and Hepatic Impairment
No dosage adjustment is necessary in patients with mild-to-severe renal insufficiency or in patients with mild hepatic insufficiency. Dosing of patients with moderate-to-severe hepatic dysfunction has not been studied. Therefore, nateglinide should be used with caution in patients with moderate-to-severe liver disease (see PRECAUTIONS, Hepatic Impairment).
4. CONTRAINDICATIONS
Nateglinide is contraindicated in patients with:
1. Known hypersensitivity to the drug or its inactive ingredients.
2. Type 1 diabetes.
3. Diabetic ketoacidosis. This condition should be treated with insulin.
5. MECHANISM OF ACTION
Nateglinide is an amino-acid derivative that lowers blood glucose levels by stimulating insulin secretion from the pancreas. This action is dependent upon functioning beta-cells in the pancreatic islets. Nateglinide interacts with the ATP-sensitive potassium (K+ATP) channel on pancreatic beta-cells. The subsequent depolarization of the beta cell opens the calcium channel, producing calcium influx and insulin secretion. The extent of insulin release is glucose dependent and diminishes at low glucose levels. Nateglinide is highly tissue selective with low affinity for heart and skeletal muscle.
6. USE IN SPECIFIC POPULATIONS
6.1 Usage in Pregnancy
Pregnancy Category C
There are no adequate and well-controlled studies in pregnant women. Nateglinide should not be used during pregnancy.
6.2 Labor and Delivery
The effect of nateglinide on labor and delivery in humans is not known.
6.3 Nursing Mothers
It is not known whether nateglinide is excreted in human milk. Because many drugs are excreted in human milk, nateglinide should not be administered to a nursing woman.
6.4 Pediatric Use
The safety and effectiveness of nateglinide in pediatric patients have not been established.
6.5 Geriatric Use
No overall differences in efficacy or safety were observed between these patients and younger patients, but greater sensitivity of some older individuals cannot be ruled out.
7. WARNINGS AND PRECAUTIONS
PRECAUTIONS
Macrovascular Outcomes: There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with nateglinide or any other antidiabetic drug.
Hypoglycemia: All oral blood glucose lowering drugs that are absorbed systemically are capable of producing hypoglycemia. The frequency of hypoglycemia is related to the severity of the diabetes, the level of glycemic control, and other patient characteristics. Geriatric patients, malnourished patients, and those with adrenal or pituitary insufficiency or severe renal impairment are more susceptible to the glucose lowering effect of these treatments. The risk of hypoglycemia may be increased by strenuous physical exercise, ingestion of alcohol, insufficient caloric intake on an acute or chronic basis, or combinations with other oral antidiabetic agents. Hypoglycemia may be difficult to recognize in patients with autonomic neuropathy and/or those who use beta-blockers. Nateglinide should be administered prior to meals to reduce the risk of hypoglycemia. Patients who skip meals should also skip their scheduled dose of nateglinide to reduce the risk of hypoglycemia.
Hepatic Impairment: Nateglinide should be used with caution in patients with moderate-tosevere liver disease because such patients have not been studied.
Loss of Glycemic Control
Transient loss of glycemic control may occur with fever, infection, trauma, or surgery. Insulin therapy may be needed instead of nateglinide therapy at such times. Secondary failure, or reduced effectiveness of nateglinide over a period of time, may occur.
8. ADVERSE REACTIONS
Hypoglycemia was relatively uncommon in all treatment arms of the clinical trials. Only 0.3% of nateglinide patients discontinued due to hypoglycemia. Gastrointestinal symptoms, especially diarrhea and nausea, were no more common in patients using the combination of nateglinide and metformin than in patients receiving metformin alone. Likewise, peripheral edema was no more common in patients using the combination of nateglinide and rosiglitazone than in patients receiving rosiglitazone alone. The following table 1 lists events that occurred more frequently in nateglinide patients than placebo patients in controlled clinical trials.
Table 1. Common Adverse Events (≥2% in Starlix® patients) in Starlix® Monotherapy Trials (% of patients)
During post-marketing experience, rare cases of hypersensitivity reactions such as rash, itching and urticaria have been reported. Similarly, cases of jaundice, cholestatic hepatitis and elevated liver enzymes have been reported.
Laboratory Abnormalities
Uric Acid: There were increases in mean uric acid levels for patients treated with nateglinide alone, nateglinide in combination with metformin, metformin alone, and glyburide alone. The respective differences from placebo were 0.29 mg/dL, 0.45 mg/dL, 0.28 mg/dL, and 0.19 mg/dL. The clinical significance of these findings is unknown.
9. OVERDOSAGE
In a clinical study in patients with Type 2 diabetes, nateglinide was administered in increasing doses up to 720 mg a day for 7 days and there were no clinically significant adverse events reported. There have been no instances of overdose with nateglinide in clinical trials. However, an overdose may result in an exaggerated glucose-lowering effect with the development of hypoglycemic symptoms. Hypoglycemic symptoms without loss of consciousness or neurological findings should be treated with oral glucose and adjustments in dosage and/or meal patterns. Severe hypoglycemic reactions with coma, seizure, or other neurological symptoms should be treated with intravenous glucose. As nateglinide is highly protein bound, dialysis is not an efficient means of removing it from the blood.
10. DRUG INTERACTIONS
Nateglinide is highly bound to plasma proteins (98%), mainly albumin. In-vitro displacement studies with highly protein-bound drugs such as furosemide, propranolol, captopril, nicardipine, pravastatin, glyburide, warfarin, phenytoin, acetylsalicylic acid, tolbutamide, and metformin showed no influence on the extent of nateglinide protein binding. Similarly, nateglinide had no influence on the serum protein binding of propranolol, glyburide, nicardipine, warfarin, phenytoin, acetylsalicylic acid, and tolbutamide in vitro. However, prudent eva luation of individual cases is warranted in the clinical setting.
Certain drugs, including nonsteroidal anti-inflammatory agents (NSAIDs), salicylates, monoamine oxidase inhibitors, and non-selective beta-adrenergic-blocking agents may potentiate the hypoglycemic action of nateglinide and other oral antidiabetic drugs.
Certain drugs including thiazides, corticosteroids, thyroid products, and sympathomimetics may reduce the hypoglycemic action of nateglinide and other oral antidiabetic drugs.
When these drugs are administered to or withdrawn from patients receiving nateglinide, the patient should be observed closely for changes in glycemic control.
Drug/Food Interactions
The pharmacokinetics of nateglinide were not affected by the composition of a meal (high protein, fat, or carbohydrate). However, peak plasma levels were significantly reduced when nateglinide was administered 10 minutes prior to a liquid meal. Nateglinide did not have any effect on gastric emptying in healthy subjects as assessed by acetaminophen testing.
11. PHARMACOKINETICS 
Absorption
Following oral administration immediately prior to a meal, nateglinide is rapidly absorbed with mean peak plasma drug concentrations (Cmax) generally occurring within 1 hour (Tmax) after dosing. When administered to patients with Type 2 diabetes over the dosage range 60 mg to 240 mg three times a day for one week, nateglinide demonstrated linear pharmacokinetics for both AUC (area under the time/plasma concentration curve) and Cmax. Tmax was also found to be independent of dose in this patient population. Absolute bioavailability is estimated to be approximately 73%. When given with or after meals, the extent of nateglinide absorption (AUC) remains unaffected. However, there is a delay in the rate of absorption characterized by a decrease in Cmax and a delay in time to peak plasma concentration (Tmax). Plasma profiles are characterized by multiple plasma concentration peaks when nateglinide is administered under fasting conditions. This effect is diminished when nateglinide is taken prior to a meal.
Distribution
Based on data following intravenous (IV) administration of nateglinide, the steady-state volume of distribution of nateglinide is estimated to be approximately 10 liters in healthy subjects. Nateglinide is extensively bound (98%) to serum proteins, primarily serum albumin, and to a lesser extent α1 acid glycoprotein. The extent of serum protein binding is independent of drug concentration over the test range of 0.1-10 μg/mL.
Metabolism
Nateglinide is metabolized by the mixed-function oxidase system prior to elimination. The major routes of metabolism are hydroxylation followed by glucuronide conjugation. The major metabolites are less potent antidiabetic agents than nateglinide. The isoprene minor metabolite possesses potency similar to that of the parent compound nateglinide.
In-vitro data demonstrate that nateglinide is predominantly metabolized by cytochrome P450 isoenzymes CYP2C9 (70%) and CYP3A4 (30%).
Elimination
Nateglinide and its metabolites are rapidly and completely eliminated following oral administration. Within 6 hours after dosing, approximately 75% of the administered 14C-nateglinide was recovered in the urine. Eighty-three percent of the 14C-nateglinide was excreted in the urine with an additional 10% eliminated in the feces. Approximately 16% of the 14C-nateglinide was excreted in the urine as parent compound. In all studies of healthy volunteers and patients with Type 2 diabetes, nateglinide plasma concentrations declined rapidly with an average elimination half-life of approximately 1.5 hours. Consistent with this short elimination half-life, there was no apparent accumulation of nateglinide upon multiple dosing of up to 240 mg three times daily for 7 days.
Special Populations
Geriatric: Age did not influence the pharmacokinetic properties of nateglinide. Therefore, no dose adjustments are necessary for elderly patients.
Gender: No clinically significant differences in nateglinide pharmacokinetics were observed between men and women. Therefore, no dose adjustment based on gender is necessary.
Race: Results of a population pharmacokinetic analysis including subjects of Caucasian, Black, and other ethnic origins suggest that race has little influence on the pharmacokinetics of nateglinide.
Renal Impairment: Compared to healthy matched subjects, patients with Type 2 diabetes and moderate-to-severe renal insufficiency (CrCl 15-50 mL/min) not on dialysis displayed similar apparent clearance, AUC, and Cmax. Patients with Type 2 diabetes and renal failure on dialysis exhibited reduced overall drug exposure. However, hemodialysis patients also experienced reductions in plasma protein binding compared to the matched healthy volunteers.
Hepatic Impairment: The peak and total exposure of nateglinide in non-diabetic subjects with mild hepatic insufficiency were increased by 30% compared to matched healthy subjects. Nateglinide should be used with caution in patients with chronic liver disease. (See PRECAUTIONS, Hepatic Impairment.)
12. HOW SUPPLIED/STORAGE AND HANDLING
1) How Available:
a) Brand name: STARLIX, by Novartis.
b) Generic drugs: Nateglinide, by various manufacturers.
2) How Supplied:
Nateglinide tablets (by DR REDDY'S LABS) are available as 60 mg white to off-white, round, biconvex tablets embossed with ‘RDY’ on one side and ‘328’ on other side and they are supplied in bottles of 30, 90, 100, 500 and unit dose package of 100 (10 x 10).
Bottles of 30 NDC 55111-328-30
Bottles of 90 NDC 55111-328-90
Bottles of 100 NDC 55111-328-01
Bottles of 500 NDC 55111-328-05
Unit dose package of 100 (10 x 10) NDC 55111-328-78
Nateglinide tablets are available as 120 mg white to off-white, round, biconvex tablets embossed with ‘RDY’ on one side and ‘329’ on other side and they are supplied in bottles of 30, 90, 100, 500 and unit dose package of 100 (10 x 10).
Bottles of 30 NDC 55111-329-30
Bottles of 90 NDC 55111-329-90
Bottles of 100 NDC 55111-329-01
Bottles of 500 NDC 55111-329-05
Unit dose package of 100 (10 x 10) NDC 55111-329-78
3) Storage:
Store at 20°-25°C (68°-77°F); excursions permitted to 15°-30°C (59°-86°F) [See USP Controlled Room Temperature].
This article Department of pharmacists/medical experts original translation finishing, welcome to reprint! At the same time the procurement of domestic scientific research institutions can contact us: 2363244352.3330889895
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产地国家：美国
原产地英文商品名:
Starlix 60mg/Tablet 100Tablet/Bottles
原产地英文药品名:
Nateglinide
中文参考商品译名:
Starlix 60毫克/片 100片/瓶
中文参考药品译名:
那格列奈
生产厂家中文参考译名:
诺华
生产厂家英文名:
Novartis

-------------------------------------------------
产地国家：美国
原产地英文商品名:
Starlix 120mg/Tablet 100Tablet/Bottles
原产地英文药品名:
Nateglinide
中文参考商品译名:
Starlix 120毫克/片 100片/瓶
中文参考药品译名:
那格列奈
生产厂家中文参考译名:
诺华
生产厂家英文名:
Novartis

-------------------------------------------------
产地国家： 瑞士
原产地英文商品名:
Starlix mite Filmtabletten 60mg/Tablet 84Tablet/box
原产地英文药品名:
Nateglinide
中文参考商品译名:
Starlix 60毫克/片 84片/盒
中文参考药品译名:
那格列奈
生产厂家中文参考译名:
诺华制药
生产厂家英文名:
Novartis Pharma Schweiz AG

-------------------------------------------------
产地国家： 瑞士
原产地英文商品名:
Starlix Filmtabletten 120mg/Tablet 84Tablet/box
原产地英文药品名:
Nateglinide
中文参考商品译名:
Starlix 120毫克/片 84片/盒
中文参考药品译名:
那格列奈
生产厂家中文参考译名:
诺华制药
生产厂家英文名:
Novartis Pharma Schweiz AG