Lucius Version of Trelagliptin: Dosage and Administration, Indications, Precautions

Lucius Version of Trelagliptin: Dosage and Administration, Indications, Precautions

Indications

Trelagliptin can be used as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Dosage and Administration

For adults, the recommended dose is 100 mg of trelagliptin taken orally once weekly. Do not cut, crush, or chew the tablets.

Use in Specific Populations

Pregnancy

Trelagliptin should not be administered to pregnant women or women who may be pregnant unless the expected therapeutic benefit is deemed to outweigh any potential risks to the mother and fetus. To date, no clinical studies have been conducted to evaluate the effects of trelagliptin in pregnant subjects.

Lactation

Breastfeeding should be avoided if the mother needs to take this medication during trelagliptin treatment. To date, no clinical studies have been conducted to evaluate the effects of trelagliptin in lactating subjects.

Warnings and Precautions

HypoglycemiaConcomitant use of trelagliptin with sulfonylureas or insulin preparations may increase the risk of hypoglycemia. Therefore, consideration should be given to reducing the dose of sulfonylureas or insulin preparations to minimize the risk of hypoglycemia when used in combination with trelagliptin.

Acute PancreatitisPost-marketing cases of acute pancreatitis have been reported with trelagliptin, which has also been associated with other DPP-4 inhibitors. After initiating trelagliptin, patients should be closely monitored for signs and symptoms of pancreatitis. If pancreatitis is suspected, trelagliptin should be discontinued immediately and appropriate treatment initiated.

Drug Interactions

No clinically significant interactions (with drugs or food) have been observed, and no dose adjustments of trelagliptin or other concomitant medications have been found to be necessary.

Trelagliptin is primarily excreted via the kidneys. Metabolism via cytochrome (CYP) P450 is negligible. No significant drug interactions have been observed with tested CYP substrates.

Effects of Other Drugs on Trelagliptin

Results from clinical interaction studies indicate that glimepiride or metformin have no clinically relevant effects on the pharmacokinetics of trelagliptin.

Effects of Trelagliptin on Other Medicinal Products

In vitro studies show that at concentrations achieved with the recommended dose of 100 mg trelagliptin, trelagliptin neither inhibits nor induces CYP450 subtypes. Trelagliptin is a substrate of P-glycoprotein, and in vitro studies demonstrate that it has weak inhibitory effects on the P-glycoprotein-mediated transport of digoxin (IC50 value: 500 µmol/L or higher) or on the uptake of metformin, a substrate of organic cation transporter 2 (OCT2) (IC50: 55.9 µmol/L). In clinical studies, trelagliptin had no clinically relevant effects on the pharmacokinetics of caffeine, tolbutamide, dextromethorphan, midazolam, metformin, or glimepiride, thus providing in vivo evidence of a low propensity for interactions with CYP1A2, CYP2C9, CYP2D6, CYP3A4, or OCT2 substrates.

Contraindications

Patients with severe ketosis, diabetic coma or pre-coma, or type 1 diabetes mellitus (this drug is not suitable as rapid elevation of blood glucose must be managed with intravenous or injectable insulin).

Patients with severe infections, those undergoing surgery (before and after operation), or with severe trauma (this drug is not suitable as blood glucose control requires injectable insulin).

Patients with severe renal impairment or end-stage renal failure on dialysis (since trelagliptin is primarily excreted by the kidneys, delayed excretion may lead to elevated plasma concentrations of the drug).

Patients with a history of hypersensitivity to any component of this drug.

Dosage Form

Tablets.

Storage

Store at 20°C to 25°C (68°F to 77°F); short-term transportation is permitted within a temperature range of 15°C to 30°C (59°F to 86°F).