Galet Tablet 50 mg

Uses

Galet Tablet 50 mg is used for an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus.

• As monotherapy
• In dual combination with Metformin, a Sulphonylurea, a Thiazolidinedione, or Insulin when diet, exercise and a single antidiabetic agent do not result in adequate glycemic control.

Galet Tablet 50 mg is also used to associated treatment for these conditions: Type 2 Diabetes Mellitus

How Galet Tablet 50 mg works

Glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) are incretin hormones that regulate blood glucose levels and maintain glucose homeostasis. It is estimated that the activity of GLP-1 and GIP contribute more than 70% to the insulin response to an oral glucose challenge. They stimulate insulin secretion in a glucose-dependent manner via G-protein-coupled GIP and GLP-1 receptor signalling. In addition to their effects on insulin secretion, GLP-1 is also involved in promoting islet neogenesis and differentiation, as well as attenuating pancreatic beta-cell apoptosis. Incretin hormones also exert extra-pancreatic effects, such as lipogenesis and myocardial function. In type II diabetes mellitus, GLP-1 secretion is impaired, and the insulinotropic effect of GIP is significantly diminished.

Galet Tablet 50 mg exerts its blood glucose-lowering effects by selectively inhibiting dipeptidyl peptidase-4 (DPP-4), an enzyme that rapidly truncates and inactivates GLP-1 and GIP upon their release from the intestinal cells. DPP-4 cleaves oligopeptides after the second amino acid from the N-terminal end. Inhibition of DPP-4 substantially prolongs the half-life of GLP-1 and GIP, increasing the levels of active circulating incretin hormones. The duration of DPP-4 inhibition by vildagliptin is dose-dependent. Galet Tablet 50 mg reduces fasting and prandial glucose and HbA1c. It enhances the glucose sensitivity of alpha- and beta-cells and augments glucose-dependent insulin secretion. Fasting and postprandial glucose levels are decreased, and postprandial lipid and lipoprotein metabolism are also improved.

Dosage

Galet Tablet 50 mg dosage

The recommended dose of Galet Tablet 50 mg is-

• 50 mg or 100 mg daily for monotherapy.
• 50 mg twice daily (morning and evening) when used in dual combination with Metformin or a Thiazolidinedione;
• 50 mg once daily in the morning when used in dual combination with a Sulphonylurea.

Galet Tablet 50 mg may be taken with or without a meal. No dosage adjustment is required in the elderly, or in patients with mild renal impairment.

Side Effects

The majority of adverse reactions were mild and transient, not requiring treatment discontinuations. Rare case of hepatic dysfunction is seen. Clinical trials of up to and more than 2 years’ duration did not show any additional safety signals or unforeseen risks when use this drug.

Toxicity

The oral Lowest published toxic dose (TDLO) is 0.3 mg/kg in rats and 1 mg/kg in mice.

There is limited information regarding overdose with vildagliptin. In one study, patients experienced muscle pain, mild and transient paresthesia, fever, edema, and a transient increase in lipase levels at a dose of 400 mg. At 600 mg, one subject experienced edema of the feet and hands and increases in creatine phosphokinase (CPK), aspartate aminotransferase (AST), C-reactive protein (CRP) and myoglobin levels. Supportive management is recommended in case of an overdose. There is no known antidote, and vildagliptin and its major metabolite cannot be removed via hemodialysis.

Precaution

Caution should be exercised in patients aged 75 years and older due to limited clinical experience. It is recommended that Liver Function Tests (LFTs) are monitored prior to initiation of Galet Tablet 50 mg, at three monthly intervals in the first year and periodically thereafter. If transaminase levels are increased, patients should be monitored with a second liver function evaluation to confirm the finding and be followed thereafter with frequent liver function tests until the abnormality (ies) return(s) to normal. If AST or ALT persist at 3 x ULN, Galet Tablet 50 mg treatment should be stopped. Patients who develop jaundice or other signs of liver dysfunction should discontinue Galet Tablet 50 mg. Following withdrawal of treatment with Galet Tablet 50 mg and LFT normalization, treatment with Galet Tablet 50 mg should not be reinitiated. Due to limited clinical experience, use with caution in patients with congestive heart failure of New York Heart Association (NYHA) functional class I–II, and do not use in patients with NYHA functional class III-IV. Galet Tablet 50 mg is not recommended in patients with moderate to severe renal impairment.

Interaction

In pharmacokinetic studies, no interactions were seen with pioglitazone, metformin, glibenclamide, digoxin, warfarin, amlodipine, ramipril, valsartan or simvastatin. As with other oral antidiabetic medicinal products the glucose-lowering effect of Galet Tablet 50 mg may be reduced by certain active substances, including thiazides, corticosteroids, thyroid products and sympathomimetics.

Food Interaction

• Take with or without food. Food reduces Cmax and delays Tmax, but not in a clinically significant way.

Volume of Distribution

The mean volume of distribution of vildagliptin at steady-state after intravenous administration is 71 L, suggesting extravascular distribution.

Elimination Route

In a fasting state, vildagliptin is rapidly absorbed following oral administration. Peak plasma concentrations are observed at 1.7 hours following administration. Plasma concentrations of vildagliptin increase in an approximately dose-proportional manner.

Food delays T_max to 2.5 hours and decreases C_max by 19%, but has no effects on the overall exposure to the drug (AUC). Absolute bioavailability of vildagliptin is 85%.

Half Life

The mean elimination half-life following intravenous administration is approximately two hours. The elimination half-life after oral administration is approximately three hours.

Clearance

After intravenous administration to healthy subjects, the total plasma and renal clearance of vildagliptin were 41 and 13 L/h, respectively.

Elimination Route

Galet Tablet 50 mg is eliminated via metabolism. Following oral administration, approximately 85% of the radiolabelled vildagliptin dose was excreted in urine and about 15% of the dose was recovered in feces. Of the recovered dose in urine, about 23% accounted for the unchanged parent compound.

Pregnancy & Breastfeeding use

Pregnancy: There are no adequate data on the use of Galet Tablet 50 mg in pregnant women; hence the potential risk for human is unknown.Lactation: It is not known whether Galet Tablet 50 mg is excreted in human milk. Due to lack of human data, Galet Tablet 50 mg should not be used during lactation.

Contraindication

Galet Tablet 50 mg is contraindicated in patients with:

• Hypersensitivity to the active substance or to any of the excipients
• Patients with type 1 diabetes or for the treatment of diabetic ketoacidosis

Special Warning

Paediatric use: Galet Tablet 50 mg is not recommended in patients 18 years of age

Storage Condition

Store in a cool and dry place. Protect from light and moisture. Keep out of the reach of the children.

Innovators Monograph

You find simplified version here Galet Tablet 50 mg