Chapter-3

Drug Profile

DRUG PROFILE

Drug

Rosiglitazone

Chemical Structure

Synonyms

Avandia

Chemical Name

()-5[[4-[2-(methyl-2-pyridinylamino) ethoxy]phenyl]-2,4thiazolidinedione,(Z)-2-butenedioate

Molecular Formula

C18H19N3O3SC4H4O4

Molecular weight

357.428 g/mol.

Description

AVANDIA (rosiglitazone maleate) is an oral

antidiabetic agent which acts primarily by increasing
insulin sensitivity. AVANDIA is used in the management
of type 2 diabetes mellitus.

Protein bindging

99.8%

Biological half-life

3-4 Hours

Excretion

Renal (64%) & Fecal (23%)

Melting point

Range of 122C to 123C

Solubility

Readily soluble in ethanol and buffered aqueous

solution with pH 2.3; solubility decreases with
increasing pH in the physiological range.

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Chapter-3
Drug Profile
Category

Antidiabetics agent

Route of Administration

Oral,

Storage

Store at controlled room temperature 15 C to 30 C.

Dose

AVANDIA tablets contain rosiglitazone maleate equivalent

to 2, 4 or 8 mg rosiglitazone.

Mechanism of Action: - AVANDIA is an oral anti-diabetic agent which acts primarily by

increasing insulin sensitivity in type 2 diabetes. Rosiglitazone, a member of the thiazolidinedione
class of antidiabetic agents, improves glycemic control while reducing circulating insulin levels.
It improves sensitivity to insulin in muscle and adipose tissue and inhibits hepatic
gluconeogenesis. Rosiglitazone is not chemically or functionally related to the sulfonylureas, the
biguanides or the alpha-glucosidase inhibitors. Rosiglitazone is a highly selective and potent
agonist for the peroxisome proliferator- activated receptor gamma (PPAR).
In humans, PPAR receptors are found in key target tissues for insulin action such as
adipose tissue, skeletal muscle and liver. Activation of PPAR nuclear receptors regulates the
transcription of insulin-responsive genes involved in the control of glucose production, transport,
and utilization. In addition, PPAR-responsive genes also participate in the regulation of fatty
acid metabolism and in the maturation of pre adipocytes, predominantly of subcutaneous origin.

Contraindicated
Hypersensitivity; Diabetic ketoacidosis; Clinical evidence of active liver disease or
increased ALT (_2.5 times upper limit of normal); Renal dysfunction (creatinine over 1.5 mg/dL
in males or 1.4 mg/dL in females; OB, Lactation: Potential for fetal or infant harm. Insulin
monotherapy should be used; Pedi: Safety and effectiveness not established.

Interactions
Drug-Drug: Concurrent use with rifampin levels and may effectiveness. Gemfibrozil
levels and may risk of hypoglycemia (

dose of rosiglitazone).

Adverse Reactions/Side Effects

CNS: STROKE
CV: HF, MYOCARDIAL INFARCTION, edema.
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Chapter-3
Drug Profile
EENT: new onset and worsening diabetic macular edema.
Derm: urticaria.
GI: hepatitis, Increase liver enzymes.
Hemat: anemia.

Warnings and precautions

Fluid retention, which may exacerbate or lead to heart failure, may occur. Combination
use with insulin and use in congestive heart failure nyha class i and ii may increase risk
of other cardiovascular effects. (5.1, 5.3)
Increased risk of myocardial ischemic events has been observed in a meta-analysis of 42
clinical trials (incidence rate 2% versus 1.5%). (5.2)
Use of avandia with nitrates is not recommended. (1.2, 5.2)
Co-administration of avandia and insulin is not recommended. (1.2, 5.3)
Dose-related edema (5.4), weight gain (5.5), and anemia (5.9) may occur.
Macular edema has been reported. (5.7)
Increased incidence of bone fracture in female patients. (5.8)
There have been no clinical studies establishing conclusive evidence of macro-vascular
risk reduction with AVANDIA or any other oral anti-diabetic drug.

Marketed formulation
S.NO.

DRUG

DOSE

1.

Metformin HCl. (Tablet)

500mg

2.

Rosiglitazon (Tablet)

500mg

3.

Glimepride (Tablet)

----

4.

Avandamet (Tablet)

-----

5.

Avandarly (Tablet)

-----

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