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Trajenta

 

1. NAME OF THE MEDICINAL PRODUCT

TRAJENTA 5 mg film-coated tablets

 

2. QUALITATIVE AND QUANTITATIVE COMPOSITION

Each tablet contains 5 mg of linagliptin.

For a full list of excipents, see section 6.1

 

3. PHARMACEUTICAL FORM

Film-coated tablet (tablet)

8 mm diameter round, light red film-coated tablet debossed with "D5" on one side and the Boehringer Ingelheim logo on the other.

 

4. CLINICAL PARTICULARS

 

4.1 Therapeutic indications

Linagliptin is indicated in adult patients with type 2 diabetes mellitus (T2DM) to improve glycaemic control in conjunction with diet and exercise, as monotherapy or as add on to metformin, sulphonylureas, or metformin plus sulphonylureas.

 

4.2 Posology and method of administration

Posology

The dose of linagliptin is 5 mg once daily. When linagliptin is added to metformin, the dose of metformin should be maintained, and linagliptin administered concomitantly.

 

When linagliptin is used in combination with a sulphonylurea, a lower dose of the sulphonylurea may be considered to reduce the risk of hypoglycaemia (see section 4.4)

 

Special populations

Renal impairment

For patients with renal impairment, no dose adjustment for TRAJENTA is required.

 

Hepatic impairment

Pharmacokinetic studies suggest that no dose adjustment is required for patients with hepatic impairment but clinical experience in such patients is lacking.

 

Elderly

No dose adjustment is necessary based on age.

However, clinical experience in patients > 75 years of age is limited.

 

Paediatric population

The safety and efficacy of linagliptin in paediatric population has not yet been established. No data are available.

 

Method of administration

TRAJENTA can be taken with or without a meal at any time of the day. If a dose is missed, it should be taken as soon as the patient remembers. A double dose should not be taken on the same day.

 

Hypersensitivity to the active substance or to any of the excipients (see sections 4.8 and 6.1)

 

4.4 Special warnings and precautions for use

General

TRAJENTA should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis.

 

Pancreatitis

There have been post-marketing reports of acute pancreatitis in patients taking linagliptin. If pancreatitis is suspected, TRAJENTA should be discontinued.

 

Hypoglycaemia

Linagliptin alone showed a comparable incidence of hypoglycaemia to placebo.

 

In clinical trials of linagliptin as part of combination therapy with medicinal products not known to cause hypoglycaemia (metformin, thiazolidinediones)rates of hypoglycaemia reported with linagliptin were similar to rates in patients taking placebo.

 

When linagliptin was added to a sulphonylurea (on a background of metformin), the incidence of hypoglycaemia was increased over that of placebo (see section 4.8).

 

Sulphonylureas are known to cause hypoglycaemia. Therefore, caution is advised when linagliptin is used in combination with a sulphonylurea. A dose reduction of the sulphonylurea may be considered (see section 4.2).

 

4.5 Interaction with other medicinal products and other forms of interaction

In vitro assessment of interactions

Linagliptin is a weak competitive and a weak to moderate mechanism-based inhibitor of CYP isozyme CYP3A4, but does not inhibit other CYP isozymes. It is not an inducer of CYP isozymes.

 

Linagliptin is a P-glycoprotein substrate, and inhibits P-glycoprotein mediated transport of digoxin with low potency.

 

Based on these results and in vivo interaction studies, linagliptin is considered unlikely to cause interactions with other P-gp substrates.

 

In vivo assessment of interactions

Effects of other medicinal products on linagliptin

Clinical data described below suggest that the risk for clinically meaningful interactions by coadministered medicinal products is low.

 

Metformin: co-administration of multiple three times daily doses of 850 mg metformin with 10 mg linagliptin once daily did not clinical meaningfully alter the pharmacokinetics of linagliptin in healthy volunteers.

 

Sulphonylureas: the steady-state pharmacokinetics of 5 mg linagliptin was not changed by concomitant administration of a single 1.75 mg dose glibenclamide (glyburide).

 

Thiazolidinediones: Co-administration of multiple daily doses of 10 mg linagliptin (supratherapeutic) with multiple daily doses of 45 mg pioglitazone, a CYP2C8 and CYP3A4 substrate, had no clinically relevant effect on the pharmacokinetics of either linagliptin or pioglitazone or the active metabolites of pioglitazone, indicating that linagliptin is not an inhibitor of CYP2C8-mediated metabolism in vivo and supporting the conclusion that the in vivo inhibition of CYP3A4 by linagliptin is negligible.

 

Ritonavir: co-administration of a single 5 mg oral dose of linagliptin and multiple 200 mg oral doses of ritonavir, a potent inhibitor of P-glycoprotein and CYP3A4, increased the AUC and Cmax of linagliptin approximately twofold and threefold, respectively. The unbound concentrations, which are usually less than 1% at the therapeutic dose of linagliptin, were increased 4-5-fold after coadministration with ritanovir. Simulations of steady-state plasma concentrations of linagliptin with and without ritonavir indicated that the increase in exposure will be not associated with an increased accumulation. These changes in linagliptin pharmacokinetics were not considered to be clinically relevant. Therefore, clinically relevant interactions would not be expected with other Pglycoprotein/CYP3A4 inhibitors.

Rifampicin: multiple co-administration of 5 mg linagliptin with rifampicin, a potent inductor of P-glycoprotein and CYP3A4, resulted in a 39.6% and 43.8% decreased linagliptin steady-state AUC and Cmax, respectively, and about 30% decreased DPP-4 inhibition at trough. Thus, full efficacy of linagliptin in combination with strong P-gp inducers might not be achieved, particularly if these are administered long-term. Co-administration with other potent inducers of P-glycoprotein and CYP3A4, such as carbamazepine, phenobarbital and phenytoin has not been studied.

Effects of linagliptin on other medicinal products
In clinical studies, as described below, linagliptin had no clinically relevant effect on the pharmacokinetics of metformin, glyburide, simvastatin, warfarin, digoxin or oral contraceptives providing in vivo evidence of a low propensity for causing medicinal product interactions with substrates of CYP3A4, CYP2C9, CYP2C8, P-glycoprotein, and organic cationic transporter (OCT).

Metformin: co-administration of multiple daily doses of 10 mg linagliptin with 850 mg metformin, an OCT substrate, had no relevant effect on the pharmacokinetics of metformin in healthy volunteers.


Therefore, linagliptin is not an inhibitor of OCT mediated transport.

Sulphonylureas: co-administration of multiple oral doses of 5 mg linagliptin and a single oral dose of 1.75 mg glibenclamide (glyburide) resulted in clinically not relevant reduction of 14% of both AUC and Cmax of glibenclamide. Because glibenclamide is primarily metabolised by CYP2C9, these data also support the conclusion that linagliptin is not a CYP2C9 inhibitor. Clinically meaningful interactions would not be expected with other sulfonylureas (e.g., glipizide, tolbutamide, and glimepiride) which, like glibenclamide, are primarily eliminated by CYP2C9.

Digoxin: co-administration of multiple of 5 mg linagliptin with multiple doses of 0.25 mg digoxin had no effect on the pharmacokinetics of digoxin in healthy volunteers. Therefore, linagliptin is not an inhibitor of P-glycoprotein-mediated transport in vivo.

 

Warfarin: multiple daily doses of 5 mg linagliptin did not alter the pharmacokinetics of S(-) or R(+) warfarin, a CYP2C9 substrate, administered in a single dose.

 

Simvastatin: multiple daily doses of linagliptin had a minimal effect on the steady state pharmacokinetics of simvastatin, a senstivie CYP3A4 substrate, in healthy volunteers. Following administration of a supratherapeutic dose of 10 mg linagliptin concomitantly with 40 mg of simvastatin daily for 6 days, the plasma AUC of simvastatin was increased by 34%, and the plasma Cmax by 10%.

 

Oral contraceptives: co-administration with 5 mg linagliptin did not alter the steady-state pharmacokinetics of levonorgestrel or ethinylestradiol.

 

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