Thiazolidinediones. (Medication Update).Mode of Action Increase insulin sensitivity, decrease hepatic gluconeogenesis gluconeogenesis /glu·co·neo·gen·e·sis/ (gloo?ko-ne?o-jen´e-sis) the synthesis of glucose from molecules that are not carbohydrates, such as amino and fatty acids. glu·co·ne·o·gen·e·sis n. , and increase insulin-dependent glucose uptake into muscle. The thiazolidinediones do not increase insulin secretion. Indications As an adjunct to diet and exercise to improve glycemic Glycemic The presence of glucose in the blood. Mentioned in: Cholesterol, High glycemic pertaining to the level of glucose in the blood. control in type 2 diabetes type 2 diabetes n. See diabetes mellitus. as monotherapy or in combination with insulin (pioglitazone only), metformin, or a sulfonylurea sulfonylurea /sul·fo·nyl·urea/ (sul?fo-nil-u-re´ah) any of a class of compounds that exert hypoglycemic activity by stimulating the islet tissue to secrete insulin; used to control hyperglycemia in patients with type 2 diabetes mellitus . Contraindications Known hypersensitivity to the particular thiazoladinedione. Do not initiate therapy if baseline liver function tests Liver Function Tests Definition Liver function tests, or LFTs, include tests for bilirubin, a breakdown product of hemoglobin, and ammonia, a protein byproduct that is normally converted into urea by the liver before being excreted by the kidneys. (ie, ALT) are >2.5 times the upper limit of normal. Pregnancy Category: C. Adverse Effects Anemia, edema edema (ĭdē`mə), abnormal accumulation of fluid in the body tissues or in the body cavities causing swelling or distention of the affected parts. , headache, myalgia, upper respiratory tract infection upper respiratory tract infection URI Infectious disease A nonspecific term used to describe acute infections involving the nose, paranasal sinuses, pharynx, and larynx, the prototypic URI is the common cold; flu/influenza is a systemic illness involving the URT , weight gain. Drug-Drug Interactions May decrease effectiveness of oral contraceptives. Drug-Food Interactions May be taken with or without food. Products Available Rosiglitazone (Avandia): Starting doses, 4 mg QD or 2mg BID. Usual dose range, 4-8 mg QD, in single or divided doses. Pioglitazone (Actos): Starting doses, 15-30 mg QD. Usual dose range, 30-45 mg QD. Dosage Forms Available Rosiglitazone: 2 mg, 4 mg, and 8 mg tablets. Pioglitazone: 15 mg, 30 mg, and 45 mg tablets. Manufacturers Rosiglitazone: SmithKline Beecham. Pioglitazone: Takeda Pharmaceutical America, Inc. Other Points of Interest Liver function monitoring should be done before starting therapy with either thiazoladinedione, and it should be done every 2 months for the first 12 months of therapy, then periodically while the patient is being treated. Thiazolidinediones should be discontinued if ALT levels remain elevated above three times the upper limit of normal. Full effects of these drugs may not be see for 8 to 12 weeks after the start of therapy. References (1.) Hutchison TA, Shahan DR, Anderson ML (eds): DRUG-DEX System. MICROMEDEX, Inc, Englewood, Colo. (Edition expires 12/2000) (2.) Hebel SK, Katstrup EK (eds): Drug Facts and Comparisons. St. Louis, Mo. 2001 |
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