Nateglinide

Molecular formula CigH27N03 Molecular weight 317.42 CAS Registry No 105816-04-4 Merck Index 13, 6454 

Sample preparation Mix 50 XL plasma with 10 p,L 5 p,g/mL IS in MeOH and 100 xL MeCN for 10 min, centrifuge at 3000 g for 10 min. Evaporate the supernatant to dr5Uiess under a stream of nitrogen at 50°, reconstitute the residue with 30 xL mobile phase, inject a 20 p,L aliquot. 

Mobile phase MeCN MeOH bufifer 30 8 70 (The buffer was 100 mM potassium hydrogen phosphate (sic) adjusted to pH 4.0 with 30% KOH.) 

StSrmer, E. Kirchheiner, J. Michael, C. Brockmoller, J. Roots, I. Rapid and simple method for the analysis of nateglinide in human plasma using HPLC analysis with UV detection, J.Pharm.Bio-med.Anal., 2003, 31, 551-555. 

Sample preparation Mix 500 gL plasma with IS and 2 mL 50 mM pH 6.6 phosphate buffer, add to a conditioned (unspecified) Sep-Pak SPE cartridge, wash with two 3 mL portions of water, elute with 5 mL MeOH. Evaporate the eluate to dryness, reconstitute the residue with 250 xL mobile phase, mix, centrifuge, inject a 150 xL aliquot. 

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Prandial insulin releasers (meglitinides) Repaglinide, nateglinide Stimulate insulin secretion (rapid and short-acting < 6 h) Oral... 

Repaglinide and nateglinide are rapidly absorbed their binding durations to SUR-1 are much shorter than sulphonylurea binding, and their hepatic metabolism... 

Katp channels are the targets for two classes of therapeutic agents, hypoglycaemic drugs like glibencla-mide or nateglinide and potassium channel openers like... 

Meglitinide contains a benzamide group. Meglitinide-related compounds such as nateglinide are non-sulfonylurea oral hypoglycemic drugs used in the treatment of type 2 (non-insulin dependent) diabetes mellitus. 

SLTR1/Kir6.2 Glibenclamide and glipizide that block pancreatic KAXP channels have been used for the treatment of type II diabetes. New class of insulin secretagogues includes repaglinide and nateglinide, which improve insulin secretion, action and reduce carbohydrate absorption. 

C10H12O2 536-66-3) see Nateglinide cuprous cyanide see under copper(I) cyanide cyanamide... 

C4H5NO3 6066-82-6) see Amprenavir Aspoxicillin Cefotiam Imidapril Nateglinide Ritonavir Romurtide Spirapril... 

C28H, N305 58914-41-3) see Procarbazine methyl 4-(l -methylethyl)cyclohexanecarboxylate (C11H20O2 175284-00-1) see Nateglinide methyl /V-methylglycinate... 

C HiiNOj 63-91-2) see Melphalan Quinapril hydrochloride Saquinavir L-phenylalanine fert-hutyl ester hydrochloride (CijHtoCINOj 15100-75-1) see Alacepril D-phenylalanine methyl ester (CioHijNOj 21685-51-8) see Nateglinide L-phenylalanine methyl ester hydrochloride (C10H14CINO2 7524-50-7) see Angiolensinatnide... 

Nateglinide (N) Starlix 60, 120 120 with meals 120 with meals NA 120 mg three times a day Up to 4 hours Metabolized by cytochrome P450 (CYP450) 2C9 and 3A4to weakly active metabolites renally eliminated... 

Nateglinide (Starlix) dosing is 120 mg three times daily before each meal. The dose may be lowered to 60 mg per meal in patients who are near goal A1C when therapy is initiated. 

Combination therapy - In patients whose hyperglycemia is inadequately controlled with metformin or after a therapeutic response to a thiazolidinedione, nateglinide may be added to, but not substituted for, metformin. 

Do not switch patients whose hyperglycemia is not adequately controlled with glyburide or other insulin secretagogues to nateglinide do not add nateglinide to their treatment regimen. 

Monotherapy and combination with metformin or a thiazolidinedioneiThe recommended starting and maintenance dose of nateglinide, alone or in combination with metformin, is 120 mg 3 times/day before meals. 

Pharmacology Nateglinide lowers blood glucose levels by stimulating insulin secretion from the pancreas. This action is dependent upon functioning beta-cells in the pancreatic islets. 

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 (T ax) f er dosing. Absolute... 

Distribution - Nateglinide is extensively bound (98%) to serum proteins, primarily serum albumin. 

Nateglinide is predominantly metabolized by cytochrome P450 isoenzymes CYP2C9 (70%) and CYP3A4 (30%). 

Excretion - Nateglinide and its metabolites are rapidly and completely eliminated following oral administration, with an average elimination half-life of about 1.5 hours. 

Diet/Exercise Use of nateglinide must be viewed as a treatment in addition to diet and not as a substitute for diet or as a convenient mechanism for avoiding dietary restraint. 

Hepatic function impairment Use nateglinide with caution in patients with chronic liver disease. Use with caution in patients with moderate to severe liver disease because such patients have not been studied. 

Lactation It is not known whether nateglinide is excreted in human milk. Because many drugs are excreted in human milk, do not administer nateglinide to a nursing woman. 

Children The safety and efficacy of nateglinide in pediatric patients have not been established. 

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