REPAGLINIDE tablet

Pays: États-Unis

Langue: anglais

Source: NLM (National Library of Medicine)

Ingrédients actifs:

REPAGLINIDE (UNII: 668Z8C33LU) (REPAGLINIDE - UNII:668Z8C33LU)

Disponible depuis:

AvKARE, Inc.

DCI (Dénomination commune internationale):

REPAGLINIDE

Composition:

REPAGLINIDE 1 mg

Type d'ordonnance:

PRESCRIPTION DRUG

Statut de autorisation:

Abbreviated New Drug Application

Résumé des caractéristiques du produit

REPAGLINIDE - REPAGLINIDE TABLET
AVKARE, INC.
----------
REPAGLINIDE TABLETS, USP
1 MG AND 2 MG
RX ONLY
DESCRIPTION
Repaglinide is an oral blood glucose-lowering drug of the meglitinide
class used in the management of
type 2 diabetes mellitus (also known as non-insulin dependent diabetes
mellitus or NIDDM).
Repaglinide, S(+)2-ethoxy-4(2((3-methyl-1-(2-(1-piperidinyl)
phenyl)-butyl) amino)-2-oxoethyl)
benzoic acid, is chemically unrelated to the oral sulfonylurea insulin
secretagogues.
The structural formula is as shown below:
Repaglinide is a white to off-white powder with molecular formula C
H N O and a molecular
weight of 452.6. Repaglinide tablets contain 1 mg or 2 mg of
repaglinide. In addition each tablet
contains the following inactive ingredients: dicalcium phosphate
(anhydrous), microcrystalline
cellulose, corn starch, meglumine, croscarmellose sodium, povidone,
poloxamer, magnesium stearate,
and colloidal silicon dioxide. The 1 mg and 2 mg tablets contain iron
oxides (yellow and red,
respectively) as coloring agents.
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
Repaglinide lowers blood glucose levels by stimulating the release of
insulin from the pancreas. This
action is dependent upon functioning beta (ß) cells in the pancreatic
islets. Insulin release is glucose-
dependent and diminishes at low glucose concentrations.
Repaglinide closes ATP-dependent potassium channels in the ß-cell
membrane by binding at
characterizable sites. This potassium channel blockade depolarizes the
ß-cell, which leads to an
opening of calcium channels. The resulting increased calcium influx
induces insulin secretion. The ion
channel mechanism is highly tissue selective with low affinity for
heart and skeletal muscle.
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PHARMACOKINETICS
ABSORPTION: After oral administration, repaglinide is rapidly and
completely absorbed from the
gastrointestinal tract. After single and multiple oral doses in
healthy subjects or in patients, peak plasma
drug levels (C
) occur within 1 hour (T
). Repaglinide is rapidly eliminated from t