Rosiglitazone Maleate

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Overview

What is Rosiglitazone Maleate?

Rosiglitazone maleate is an oral antidiabetic agent which acts primarily by increasing iinsulin sensitivity. Rosiglitazone maleate improves glycemic control while reducing circulating insulin levels.

Rosiglitazone maleate is not chemically or functionally related to the sulfonylureas, the biguanides, or the alpha-glucosidase inhibitors.

Chemically, rosiglitazone maleate is (±)-5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-2,4-thiazolidinedione, ()-2-butenedioate (1:1) with a molecular weight of 473.52 (357.44 free base). The molecule has a single chiral center and is present as a racemate. Due to rapid interconversion, the enantiomers are functionally indistinguishable. The structural formula of rosiglitazone maleate is:

The molecular formula is CHNOS•CHO. Rosiglitazone maleate is a white to off-white solid with a melting point range of 122° to 123°C. The pKa values of rosiglitazone maleate are 6.8 and 6.1. It is readily soluble in ethanol and a buffered aqueous solution with pH of 2.3; solubility decreases with increasing pH in the physiological range. Each film-coated tablet contains rosiglitazone maleate equivalent to rosiglitazone, 2 mg, 4 mg or 8 mg, for oral administration.Inactive ingredients are: Lactose monohydrate, lechithinm, magnesium stearate, microcrystalline cellulose, polyethylene glycol 3350, polyvinyl alcohol, red iron oxide, sodium starch glycolate type A, talc, titanium dioxide. The 4 mg tablet also contains FD&C yellow No, 6 aluminum lake and yellow iron oxide.

What does Rosiglitazone Maleate look like?

What are the available doses of Rosiglitazone Maleate?

Oval film-coated tablets in the following strengths::

What should I talk to my health care provider before I take Rosiglitazone Maleate?

How should I use Rosiglitazone Maleate?

Rogislitazone tablets are indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

The management of antidiabetic therapy should be individualized. All patients should start rosiglitazone maleate tablets at the lowest recommended dose. Further increases in the dose of rosiglitazone maleate tablets should be accompanied by careful monitoring for adverse events related to fluid retention .

Rosiglitazone maleate tablets may be administered at a starting dose of 4 mg either as a single daily dose or in 2 divided doses. For patients who respond inadequately following 8 to 12 weeks of treatment, as determined by reduction in fasting plasma glucose (FPG), the dose may be increased to 8 mg daily as monotherapy or in combination with metformin, sulfonylurea, or sulfonylurea plus metformin. Reductions in glycemic parameters by dose and regimen are described under . Rosiglitazone maleate tablets may be taken with or without food.

The total daily dose of rosiglitazone maleate tablets should not exceed 8 mg.

What interacts with Rosiglitazone Maleate?

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What are the warnings of Rosiglitazone Maleate?

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What are the precautions of Rosiglitazone Maleate?

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What are the side effects of Rosiglitazone Maleate?

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What should I look out for while using Rosiglitazone Maleate?

Initiation of rosiglitazone maleate in patients with established New York Heart Association (NYHA) Class III or IV heart failure is contraindicated .

● Thiazolidinediones, including rosiglitazone, cause or exacerbate congestive heart failure in some patients [see Warnings and Precautions (5.1)]. After initiation of rosiglitazone maleate, and after dose increases, observe patients carefully for signs and symptoms of heart failure (including excessive, rapid weight gain, dyspnea, and/or edema). If these signs and symptoms develop, the heart failure should be managed according to current standards of care. Furthermore, discontinuation or dose reduction of rosiglitazone maleate must be considered.

● Rosiglitazone Maleate is not recommended in patients with symptomatic heart failure. Initiation of rosiglitazone maleate in patients with established NYHA Class III or IV heart failure is contraindicated.

● A meta-analysis of 42 clinical studies (mean duration 6 months; 14,237 total patients), most of which compared rosiglitazone maleate to placebo, showed rosiglitazone maleate to be associated with an increased risk of myocardial ischemic events such as angina or myocardial infarction. Three other studies (mean duration 41 months; 14,067 total patients), comparing rosiglitazone maleate to some other approved oral antidiabetic agents or placebo, have not confirmed or excluded this risk. In their entirety, the available data on the risk of myocardial ischemia are inconclusive.

What might happen if I take too much Rosiglitazone Maleate?

Limited data are available with regard to overdosage in humans. In clinical studies in volunteers, rosiglitazone maleate has been administered at single oral doses of up to 20 mg and was well-tolerated. In the event of an overdose, appropriate supportive treatment should be initiated as dictated by the patient’s clinical status.

How should I store and handle Rosiglitazone Maleate?

Store at controlled room temperature 20° to 25°C (68° to 77°F) [see USP] .Tablets:2 mg - Pink oval film coated tablets, engraved with W41; supplied in bottles of 30, 100 and 5004 mg - Orange oval film coated tablets, engraved with W42; supplied in bottles of 30, 100 and 500.8 mg - Brick-red oval film coated tablets, engraved with W43, supplied in bottles of 30, 100 and 500.Store at 25°C (77°F); excursions 15° to 30°C (59° to 86°F). Dispense in a tight, light-resistant container.Tablets:2 mg - Pink oval film coated tablets, engraved with W41; supplied in bottles of 30, 100 and 5004 mg - Orange oval film coated tablets, engraved with W42; supplied in bottles of 30, 100 and 500.8 mg - Brick-red oval film coated tablets, engraved with W43, supplied in bottles of 30, 100 and 500.Store at 25°C (77°F); excursions 15° to 30°C (59° to 86°F). Dispense in a tight, light-resistant container.Tablets:2 mg - Pink oval film coated tablets, engraved with W41; supplied in bottles of 30, 100 and 5004 mg - Orange oval film coated tablets, engraved with W42; supplied in bottles of 30, 100 and 500.8 mg - Brick-red oval film coated tablets, engraved with W43, supplied in bottles of 30, 100 and 500.Store at 25°C (77°F); excursions 15° to 30°C (59° to 86°F). Dispense in a tight, light-resistant container.Tablets:2 mg - Pink oval film coated tablets, engraved with W41; supplied in bottles of 30, 100 and 5004 mg - Orange oval film coated tablets, engraved with W42; supplied in bottles of 30, 100 and 500.8 mg - Brick-red oval film coated tablets, engraved with W43, supplied in bottles of 30, 100 and 500.Store at 25°C (77°F); excursions 15° to 30°C (59° to 86°F). Dispense in a tight, light-resistant container.Tablets:2 mg - Pink oval film coated tablets, engraved with W41; supplied in bottles of 30, 100 and 5004 mg - Orange oval film coated tablets, engraved with W42; supplied in bottles of 30, 100 and 500.8 mg - Brick-red oval film coated tablets, engraved with W43, supplied in bottles of 30, 100 and 500.Store at 25°C (77°F); excursions 15° to 30°C (59° to 86°F). Dispense in a tight, light-resistant container.

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Clinical Information

Chemical Structure

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Clinical Pharmacology

Rosiglitazone, a member of the thiazolidinedione class of antidiabetic agents, improves glycemic control by improving insulin sensitivity. Rosiglitazone is a highly selective and potent agonist for the peroxisome proliferator-activated receptor-gamma (PPARγ). In humans, PPAR receptors are found in key target tissues for insulin action such as adipose tissue, skeletal muscle, and liver. Activation of PPARγ nuclear receptors regulates the transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization. In addition, PPARγ-responsive genes also participate in the regulation of fatty acid metabolism.

Insulin resistance is a common feature characterizing the pathogenesis of type 2 diabetes. The antidiabetic activity of rosiglitazone has been demonstrated in animal models of type 2 diabetes in which hyperglycemia and/or impaired glucose tolerance is a consequence of insulin resistance in target tissues. Rosiglitazone reduces blood glucose concentrations and reduces hyperinsulinemia in the ob/ob obese mouse, db/db diabetic mouse, and fa/fa fatty Zucker rat.

In animal models, the antidiabetic activity of rosiglitazone was shown to be mediated by increased sensitivity to insulin’s action in the liver, muscle, and adipose tissues. Pharmacological studies in animal models indicate that rosiglitazone inhibits hepatic gluconeogenesis. The expression of the insulin-regulated glucose transporter GLUT-4 was increased in adipose tissue. Rosiglitazone did not induce hypoglycemia in animal models of type 2 diabetes and/or impaired glucose tolerance.

Non-Clinical Toxicology

Initiation of rosiglitazone maleate in patients with established New York Heart Association (NYHA) Class III or IV heart failure is contraindicated .

● Thiazolidinediones, including rosiglitazone, cause or exacerbate congestive heart failure in some patients [see Warnings and Precautions (5.1)]. After initiation of rosiglitazone maleate, and after dose increases, observe patients carefully for signs and symptoms of heart failure (including excessive, rapid weight gain, dyspnea, and/or edema). If these signs and symptoms develop, the heart failure should be managed according to current standards of care. Furthermore, discontinuation or dose reduction of rosiglitazone maleate must be considered.

● Rosiglitazone Maleate is not recommended in patients with symptomatic heart failure. Initiation of rosiglitazone maleate in patients with established NYHA Class III or IV heart failure is contraindicated.

● A meta-analysis of 42 clinical studies (mean duration 6 months; 14,237 total patients), most of which compared rosiglitazone maleate to placebo, showed rosiglitazone maleate to be associated with an increased risk of myocardial ischemic events such as angina or myocardial infarction. Three other studies (mean duration 41 months; 14,067 total patients), comparing rosiglitazone maleate to some other approved oral antidiabetic agents or placebo, have not confirmed or excluded this risk. In their entirety, the available data on the risk of myocardial ischemia are inconclusive.

Rosiglitazone maleate, like other thiazolidinediones, alone or in combination with other antidiabetic agents, can cause fluid retention, which may exacerbate or lead to heart failure. Patients should be observed for signs and symptoms of heart failure. If these signs and symptoms develop, the heart failure should be managed according to current standards of care. Furthermore, discontinuation or dose reduction of rosiglitazone must be considered .

Patients with congestive heart failure (CHF) NYHA Class I and II treated with Rosiglitazone maleate have an increased risk of cardiovascular events. A 52-week, double-blind, placebo-controlled echocardiographic study was conducted in 224 patients with type 2 diabetes mellitus and NYHA Class I or II CHF (ejection fraction ≤45%) on background antidiabetic and CHF therapy. An independent committee conducted a blinded evaluation of fluid-related events (including congestive heart failure) and cardiovascular hospitalizations according to predefined criteria (adjudication). Separate from the adjudication, other cardiovascular adverse events were reported by investigators. Although no treatment difference in change from baseline of ejection fractions was observed, more cardiovascular adverse events were observed following treatment with rosiglitazone maleate compared to placebo during the 52-week study. (See Table 1.)

Initiation of rosiglitazone maleate in patients with established NYHA Class III or IV heart failure is contraindicated. Rosiglitazone maleate is not recommended in patients with symptomatic heart failure.

Patients experiencing acute coronary syndromes have not been studied in controlled clinical trials. In view of the potential for development of heart failure in patients having an acute coronary event, initiation of rosiglitazone maleate is not recommended for patients experiencing an acute coronary event, and discontinuation of rosiglitazone maleate during this acute phase should be considered.

Patients with NYHA Class III and IV cardiac status (with or without CHF) have not been studied in controlled clinical trials. Rosiglitazone maleate is not recommended in patients with NYHA Class III and IV cardiac status.

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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Professional

Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72

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Interactions

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