February 19, 2017
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Janumet XR

"Jan. 29, 2013 -- The American Academy of Pediatrics has issued the first-ever guidelines for the management of type 2 diabetes in children and teens.

Type 2 diabetes is rising rapidly among children and teens because of soaring obesity "...

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Janumet XR

JANUMET® XR
(sitagliptin and metformin HCl) Extended-Release Tablets

WARNING

LACTIC ACIDOSIS

Postmarketing cases of metformin-associated lactic acidosis have resulted in death, hypothermia, hypotension, and resistant bradyarrhythmias. The onset of metformin-associated lactic acidosis is often subtle, accompanied only by nonspecific symptoms such as malaise, myalgias, respiratory distress, somnolence, and abdominal pain. Metformin-associated lactic acidosis was characterized by elevated blood lactate levels (>5 mmol/Liter), anion gap acidosis (without evidence of ketonuria or ketonemia), an increased lactate/pyruvate ratio, and metformin plasma levels generally >5 mcg/mL [see Use In Specific Populations].

Risk factors for metformin-associated lactic acidosis include renal impairment, concomitant use of certain drugs (e.g., carbonic anhydrase inhibitors such as topiramate), age 65 years old or greater, having a radiological study with contrast, surgery and other procedures, hypoxic states (e.g., acute congestive heart failure), excessive alcohol intake, and hepatic impairment.

Steps to reduce the risk of and manage metformin-associated lactic acidosis in these high risk groups are provided in the full prescribing information [see DOSAGE AND ADMINISTRATION, CONTRAINDICATIONS, WARNINGS AND PRECAUTIONS, DRUG INTERACTIONS, and Use In Specific Populations].

If metformin-associated lactic acidosis is suspected, immediately discontinue JANUMET XR and institute general supportive measures in a hospital setting. Prompt hemodialysis is recommended [see Use In Specific Populations].

DRUG DESCRIPTION

JANUMET XR tablets contain two oral antidiabetic medications used in the management of type 2 diabetes: sitagliptin and metformin hydrochloride extended-release.

Sitagliptin

Sitagliptin is an orally-active inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme. Sitagliptin phosphate monohydrate drug substance is used to manufacture JANUMET XR. Sitagliptin phosphate monohydrate is described chemically as 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,813 tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-α]pyrazine phosphate (1:1) monohydrate with an empirical formula of C16H15F6N5O•H3PO4•H2O and a molecular weight of 523.32. The structural formula is:

Sitagliptin - Structural Formula Illustration

Sitagliptin phosphate monohydrate is a white to off-white, crystalline, non-hygroscopic powder. It is soluble in water and N,N-dimethyl formamide; slightly soluble in methanol; very slightly soluble in ethanol, acetone, and acetonitrile; and insoluble in isopropanol and isopropyl acetate.

Metformin Hydrochloride

Metformin hydrochloride (N,N-dimethylimidodicarbonimidic diamide hydrochloride) is a white to off-white crystalline compound with a molecular formula of C4H11N5•HCl and a molecular weight of 165.63. Metformin hydrochloride is freely soluble in water and is practically insoluble in acetone, ether, and chloroform. The pKa of metformin is 12.4. The pH of a 1% aqueous solution of metformin hydrochloride is 6.68. The structural formula is as shown:

Metformin Hydrochloride - Structural Formula Illustration

JANUMET XR

JANUMET XR consists of an extended-release metformin core tablet coated with an immediate-release layer of sitagliptin. The sitagliptin layer is coated with a soluble polymeric film. JANUMET XR is available for oral administration as tablets containing 64.25 mg sitagliptin phosphate monohydrate (equivalent to 50 mg sitagliptin as free base) and either 500 mg metformin hydrochloride extended-release (50 mg/500 mg) or 1000 mg metformin hydrochloride extended-release (50 mg/1000 mg). Additionally, JANUMET XR is available for oral administration as tablets containing 128.5 mg sitagliptin phosphate monohydrate (equivalent to 100 mg sitagliptin as free base) and 1000 mg metformin hydrochloride extended-release (100 mg/1000 mg).

All doses of JANUMET XR contain the following inactive ingredients: povidone, hypromellose, colloidal silicon dioxide, sodium stearyl fumarate, propyl gallate, polyethylene glycol, and kaolin. The JANUMET XR 50 mg/500 mg tablet contains the additional inactive ingredient microcrystalline cellulose. In addition, the film coating for all doses contains the following inactive ingredients: hypromellose, hydroxypropyl cellulose, titanium dioxide, FD&C #2/Indigo Carmine Aluminum Lake and carnauba wax. The JANUMET XR 50 mg/1000 mg tablet film coating also contains the inactive ingredient yellow iron oxide.

Last reviewed on RxList: 1/31/2017
This monograph has been modified to include the generic and brand name in many instances.

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