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Merck Sharp & Dohme Ireland (Human Health) Limited

Merck Sharp & Dohme Ireland (Human Health) Limited
Pelham House, South County Business Park, Leopardstown, Dublin 18, Ireland
Telephone: +353 1 299 8700
Fax: +353 1 299 8701
Medical Information e-mail: medinfo_ireland@merck.com
Summary of Product Characteristics last updated on medicines.ie: 30/09/2011
SPC JANUVIA 100mg

When a pharmaceutical company changes an SPC or PIL, a new version is published on medicines.ie. For each version, we show the dates it was published on medicines.ie and the reasons for change.

Updated on 30/09/2011 and displayed until Current
Reasons for adding or updating:
  • Change to section 4.8 - Undesirable effects
Date of revision of text on the SPC:   24-Aug-2011
Legal Category:   Product subject to medical prescription which may be renewed (B)

Free-text change information supplied by the pharmaceutical company

Update to Section 4.8.
Updated on 07/01/2011 and displayed until 30/09/2011
Reasons for adding or updating:
  • Change to section 4.4 - Special warnings and precautions for use
  • Change to section 4.8 - Undesirable effects
Date of revision of text on the SPC:   26-Nov-2010
Legal Category:   Product subject to medical prescription which may be renewed (B)

Free-text change information supplied by the pharmaceutical company



Sections 4.4 & 4.8 - Label Update- Pancreatitis

Updated on 01/12/2010 and displayed until 07/01/2011
Reasons for adding or updating:
  • Change to section 4.8 - Undesirable effects
Date of revision of text on the SPC:   03-Nov-2010
Legal Category:   Product subject to medical prescription which may be renewed (B)

Free-text change information supplied by the pharmaceutical company



Section 4.8 - Label update vomiting

 

Updated on 01/09/2010 and displayed until 01/12/2010
Reasons for adding or updating:
  • Change to section 4.1 - Therapeutic indications
  • Change to section 4.2 - Posology and method of administration
  • Change to section 4.4 - Special warnings and precautions for use
  • Change to section 4.5 - Interaction with other medicinal products and other forms of interaction
  • Change to section 4.7 - Effects on ability to drive and use machines
  • Change to section 4.8 - Undesirable effects
  • Change to section 4.9 - Overdose
  • Change to section 5.1 - Pharmacodynamic properties
  • Change to section 5.2 - Pharmacokinetic properties
  • Change to section 4.6 - Pregnancy and lactation
Date of revision of text on the SPC:   06-Aug-2010
Legal Category:   Product subject to medical prescription which may be renewed (B)

Free-text change information supplied by the pharmaceutical company



Sections 4.1, 4.2, 4.4, 4.5, 4.6, 4.7, 4.8, 4.9, 5.1, 5.2 - Updated renal impairment information

 

Updated on 30/11/2009 and displayed until 01/09/2010
Reasons for adding or updating:
  • Change to section 4.1 - Therapeutic indications
  • Change to section 4.2 - Posology and method of administration
  • Change to section 4.4 - Special warnings and precautions for use
  • Change to section 4.8 - Undesirable effects
  • Change to section 5.1 - Pharmacodynamic properties
Date of revision of text on the SPC:   09-Nov-2009
Legal Category:   Product subject to medical prescription which may be renewed (B)

Free-text change information supplied by the pharmaceutical company



Add on insulin (II11)
Changes to Sections: 4.1, 4.2, 4.4, 4.8, 5.1

 

4.1 Therapeutic indications

 

For patients with type 2 diabetes mellitus, Januvia is indicated

to improve glycaemic control:

 

as monotherapy

in patients inadequately controlled by

 

to improve glycaemic control when diet and exercise alone and alone do not provide adequate glycaemic control and whenfor whom metformin is inappropriate due to contraindications or intolerance.

 

as dual oral therapy in combination with

to improve glycaemic control in combination with metformin when diet and exercise plus metformin alone do not provide adequate glycaemic control.

to improve glycaemic control in combination with a sulphonylurea when diet and exercise plus maximal tolerated dose of a sulphonylurea alone do not provide adequate glycaemic control and when metformin is inappropriate due to contraindications or intolerance.

a PPAR

 

g agonist (i.e. a thiazolidinedione) when use of a PPARg agonist is appropriate and when diet and exercise plus the PPARg agonist alone do not provide adequate glycaemic control.

 

as triple oral therapy in combination with

to improve glycaemic control in combination with a sulphonylurea and metformin when diet and exercise plus dual therapy with these agents do not provide adequate glycaemic control.

a PPAR

 

g agonist and metformin when use of a PPARg agonist is appropriate and when diet and exercise plus dual therapy with these agents do not provide adequate glycaemic control.

 

For patients with type 2 diabetes mellitus in whom use of a PPAR

g agonist (i.e. a thiazolidinedione) is appropriate, Januvia is indicated:

 

in combination with the PPAR

g agonist when diet and exercise plus the PPARg agonist alone do not provide adequate glycaemic control.

 

in combination with the PPAR

g agonist and metformin when diet and exercise plus dual therapy with these agents do not provide adequate glycaemic control.

 

Januvia is also indicated as add-on to insulin (with or without metformin) when diet and exercise plus stable dosage of insulin do not provide adequate glycaemic control.

 

4.2 Posology and method of administration

The dose of Januvia is 100 mg once daily. When sitagliptin

Januvia is used in combination with metformin and/or a PPARg agonist, the dosage of metformin and/or PPARg agonist should be maintained, and sitagliptinJanuvia administered concomitantly.

 

When Januvia is used in combination with a sulphonylurea

or with insulin, a lower dose of the sulphonylurea or insulin may be considered to reduce the risk of hypoglycaemia. (See section 4.4.)

 

4.4 Special warnings and precautions for use

Hypoglycaemia when used in combination with other anti-hyperglycaemic agents

In clinical trials of Januvia as monotherapy and as part of combination therapy with agents not known to cause hypoglycaemia (i.e. metformin and/or a PPAR

g agonist), rates of hypoglycaemia reported with sitagliptin were similar to rates in patients taking placebo. When sitagliptin was added to a sulphonylurea or to insulin, the incidence of hypoglycaemia was increased over that of placebo (see section 4.8). Therefore, to reduce the risk of hypoglycaemia, a lower dose of sulphonylurea or insulin may be considered (see section 4.2). The use of sitagliptin in combination with insulin has not been adequately studied.

 

4.8 Undesirable effects

In 10

11 large clinical trials of up to 2 years in duration, over 29003200 patients have received treatment with Januvia 100 mg per day alone or in combination with metformin, a sulphonylurea (with or without metformin), insulin (with or without metformin), or a PPARg agent (with or without metformin). In a pooled analysis of 9 of these trials, the rate of discontinuation due to adverse experiences considered drug-related was 0.8 % with 100 mg per day and 1.5 % with other treatments. No adverse reactions considered as drug-related were reported in patients treated with sitagliptin occurring in excess (> 0.2 % and difference > 1 patient) of that in patients treated with control. In an additional combination study with a PPARg agent (rosiglitazone) and metformin, no patients were discontinued due to adverse experiences considered as drug-related.

 

Table 1. The frequency of adverse reactions identified from placebo-controlled clinical studies

 

Adverse Reaction

 

Frequency of adverse reaction by treatment regimen

 

 

Sitagliptin with Metformin

1

Sitagliptin with a Sulfonylurea

Sulphonylurea 2

Sitagliptin with a Sulfonylurea

Sulphonylurea

 

and Metformin

3

Sitagliptin with a PPAR

g Agent (pioglitazone)4

Sitagliptin with a

PPAR

g Agent (rosiglitazone)

 

and Metformin5

 

Sitagliptin with Insulin

(+/-) Metformin)

 

66

Time-point

 

24-week

 

24-week

 

24-week

 

24-week

 

18-week

 

24-week

 

 

             

Investigations

 

blood glucose decreased

 

Uncommon

 

         
             

Nervous system disorders

 

headache

 

       

Common

 

 

Common

 

 

 

somnolence

 

 

Uncommon

 

 

         
             

Gastrointestinal disorders

 

 

diarrhoea

 

 

Uncommon

 

 

     

Common

 

 

 

dry mouth

 

 

 

         

Uncommon

 

 

 

nausea

 

 

Common

 

 

         

flatulence

 

 

     

Common

 

   

constipation

 

 

   

Common

 

 

   

Uncommon

 

 

 

upper abdominal pain

 

 

Uncommon

 

 

         

vomiting

 

 

       

Common

 

 

 
             

Metabolism and nutrition disorders

 

 

hypoglycaemia*

 

 

 

Common

 

 

Very common

Very common

 

 

Common

 

Common

 

 

Common

 

 

 

             

Infections and infestations

 

 

 

influenza

 

 

 

         

Common

 

 

 

             

General disorders

 

 

peripheral oedema

 

 

     

Common

 

Common†

 

 

 

 

 

5 In this study of sitagliptin 100 mg once daily in combination with rosiglitazone and metformin, which continued through 54 weeks, the incidence of adverse reactions considered as drug-related in patients treated with

 

the sitagliptin combination compared to treatment with the placebo combination was 15.3 % and 10.9 %, respectively. Other drug-related adverse reactions reported in the 54-week analysis (frequency common) in patients treated with the sitagliptin combination occurring in excess (> 0.2 % and difference > 1 patient) of that in patients treated with the placebo combination were: headache, cough, vomiting, hypoglycaemia, fungal skin infection, and upper respiratory tract infection.

 

6 In this 24-week study of sitagliptin 100 mg once daily as add-on to insulin therapy (with or without metformin), the incidence of adverse reactions considered as drug-related in patients treated with sitagliptin/insulin (with or without metformin) compared to treatment with placebo/insulin (with or without metformin) was 15.5 % and 8.5 %, respectively. In this study 0.9 % of patients treated with sitagliptin/insulin and 0.0 % of patients treated with placebo/insulin were discontinued due to adverse experiences considered as drug-related.

 

5. PHARMACOLOGICAL PROPERTIES

5.1 Pharmacodynamic properties

Overall, sitagliptin improved glycaemic control when used as monotherapy or in combination treatment (see Table 2).

 

Overall, sitagliptin improved glycaemic control when given as monotherapy, when used in combination with metformin (initial or add-on therapy), in combination with a sulphonylurea (with or without metformin), in combination with a thiazolidinedione, and in combination with a thiazolidinedione and metformin, as measured by clinically relevant reductions in HbA1c from baseline at study endpoint (see Table 2).

 

A 24-week placebo-controlled study was designed to evaluate the efficacy and safety of sitagliptin (100 mg once daily) added to insulin (at a stable dose for at least 10 weeks) with or without metformin (at least 1500 mg). In patients taking pre-mixed insulin, the mean daily dose was 70.9 U/day. In patients taking non-pre-mixed (intermediate/long-acting) insulin, the mean daily dose was 44.3 U/day. The addition of sitagliptin to insulin provided significant improvements in glycaemic parameters. There was no meaningful change from baseline in body weight in either group.

In a 24-week placebo-controlled factorial study of initial therapy, sitagliptin 50 mg twice daily in combination with metformin (500 mg or 1000 mg twice daily) provided significant improvements in glycaemic parameters compared with either monotherapy. The decrease in body weight with the combination of sitagliptin and metformin was similar to that observed with metformin alone or placebo; there was no change from baseline for patients on sitagliptin alone. The incidence of hypoglycaemia was similar across treatment groups.

Table 2. HbA1c results in placebo-controlled monotherapy and combination therapy studies*

 

Study

 

Mean baseline HbA1c (%)

 

Mean change from baseline HbA1c (%)†

 

Placebo-corrected mean change in HbA1c (%)†

(95 % CI)

 

Monotherapy Studies

 

Sitagliptin 100 mg once daily§

(N= 193)

 

8.0

 

-0.5

 

-0.6

‡

 

(-0.8, -0.4)

 

Sitagliptin 100 mg once daily

%

 

(N= 229)

 

8.0

 

-0.6

 

-0.8

‡

 

(-1.0, -0.6)

 

Combination Therapy Studies

 

Sitagliptin 100 mg once daily added to ongoing metformin therapy

%

 

(N=453)

 

8.0

 

-0.7

 

-0.7

‡

 

(-0.8, -0.5)

 

Sitagliptin 100 mg once daily added to ongoing pioglitazone therapy

%

 

(N=163)

 

8.1

 

-0.9

 

-0.7

‡

 

(-0.9, -0.5)

 

Sitagliptin 100 mg once daily added to ongoing glimepiride therapy

%

 

(N=102)

 

8.4

 

-0.3

 

-0.6

‡

 

(-0.8, -0.3)

 

Sitagliptin 100 mg once daily added to ongoing glimepiride + metformin therapy

%

 

(N=115)

 

8.3

 

-0.6

 

-0.9

‡

 

(-1.1, -0.7)

 

Sitagliptin 100 mg once daily added to ongoing rosiglitazone + metformin therapy (N=170)

Week 18

 

Week 54

 

 

 

 

8.8

 

 

8.8

 

 

 

 

 

-1.0

 

 

-1.0

 

 

 

 

 

-0.7

‡

 

(-0.9, -0.5)

 

-0.8

‡

 

(-1.0, -0.5)

 

Initial therapy (twice daily)

%:

 

Sitagliptin 50 mg + metformin 500 mg

(N=183)

 

8.8

 

-1.4

 

-1.6

‡

 

(-1.8, -1.3)

 

Initial therapy (twice daily)

%:

 

Sitagliptin 50 mg + metformin 1000 mg

(N=178)

 

8.8

 

-1.9

 

-2.1

‡

 

(-2.3, -1.8)

 

Sitagliptin 100 mg once daily added to ongoing insulin (+/- metformin) therapy

 

%

 

(N=305)

 

 

8.7

 

 

-0.6¶

 

 

-0.6‡,¶

(-0.7, -0.4)

 

 

 

*

ALL PATIENTS TREATED POPULATION (AN INTENTION-TO-TREAT ANALYSIS).

 

†

LEAST SQUARES MEANS ADJUSTED FOR PRIOR ANTIHYPERGLYCAEMIC THERAPY STATUS AND BASELINE VALUE.

 

‡

P<0.001 COMPARED TO PLACEBO OR PLACEBO + COMBINATION TREATMENT.

 

§

HBA1C (%) AT WEEK 18.

 

%

 

HBA1C (%) AT WEEK 24.

 

¶

 

LEAST SQUARES MEAN ADJUSTED FOR METFORMIN USE AT VISIT 1 (YES/NO), INSULIN USE AT VISIT 1 (PRE-MIXED VS. NON-PRE-MIXED [INTERMEDIATE- OR LONG-ACTING]), AND BASELINE VALUE. TREATMENT BY STRATUM (METFORMIN AND INSULIN USE) INTERACTIONS WERE NOT SIGNIFICANT (P > 0.10).

 

 

 

 

 

Updated on 03/09/2009 and displayed until 30/11/2009
Reasons for adding or updating:
  • Change to section 4.8 - Undesirable effects
  • Change to section 10 - Date of revision of the text
Date of revision of text on the SPC:   31-Aug-2009
Legal Category:   Product subject to medical prescription which may be renewed (B)

Free-text change information supplied by the pharmaceutical company



Updated SPC -

 

additional AE's section 4.8
Addition of 'cutaneous vasculitis' and 'pancreatitis' under Post Marketing Experience in Section 4.8 and date of revision of text.

 

Updated on 17/06/2009 and displayed until 03/09/2009
Reasons for adding or updating:
  • Change to section 4.1 - Therapeutic indications
  • Change to section 4.4 - Special warnings and precautions for use
  • Change to section 4.8 - Undesirable effects
  • Change to section 4.9 - Overdose
  • Change to section 5.1 - Pharmacodynamic properties
Date of revision of text on the SPC:   02-Jun-2009
Legal Category:   Product subject to medical prescription which may be renewed (B)

Free-text change information supplied by the pharmaceutical company



SECTION 4.1: ADD THE TRIPLE COMBINATION USE
Section 4.4 minor text layout change
Section 4.8: was updated to reflect the AEs seen as part of the study conducted to support the triple combination use
Section 4.9 ad 5.1: updated to describe studies

 

 

 

 

Updated on 12/03/2008 and displayed until 17/06/2009
Reasons for adding or updating:
  • Change to section 4.3 - Contraindications
  • Change to section 4.4 - Special warnings and precautions for use
  • Change to section 4.8 - Undesirable effects
Date of revision of text on the SPC:   02/2008
Legal Category:   prescription only

Free-text change information supplied by the pharmaceutical company

Updates to sections 4.3, 4.4 and 4.8 of the SPC to include hypersensitivity reactions and exfoliative skin conditions including Stevens-Johnson syndrome

Updated on 23/01/2008 and displayed until 12/03/2008
Reasons for adding or updating:
  • Change to section 4.1 - Therapeutic indications
  • Change to section 4.2 - Posology and method of administration
  • Change to section 4.4 - Special warnings and precautions for use
  • Change to section 4.8 - Undesirable effects
  • Change to section 5.1 - Pharmacodynamic properties
  • Change to section 10 - Date of revision of the text
Date of revision of text on the SPC:   12/2007
Legal Category:   prescription only

Free-text change information supplied by the pharmaceutical company

The following sections have been updated 4.1, 4.2, 4.4, 4.8, 5.1, 10.

Updated on 21/09/2007 and displayed until 23/01/2008
Reasons for adding or updating:
  • Change to section 4.8 - Undesirable effects
Date of revision of text on the SPC:   08/2007
Legal Category:   prescription only

Free-text change information supplied by the pharmaceutical company

Section 4.8 has been updated to include Post-marketing Experience.

Updated on 30/04/2007 and displayed until 21/09/2007
Reasons for adding or updating:
  • New SPC for new product

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Active Ingredients

 
   sitagliptin phosphate monohydrate

Versions

 
30/09/2011 to Current
07/01/2011 to 30/09/2011
01/12/2010 to 07/01/2011
01/09/2010 to 01/12/2010
30/11/2009 to 01/09/2010
03/09/2009 to 30/11/2009
17/06/2009 to 03/09/2009
12/03/2008 to 17/06/2009
23/01/2008 to 12/03/2008
21/09/2007 to 23/01/2008
30/04/2007 to 21/09/2007
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Registered Address: Franklin House, 140 Pembroke Road, Dublin 4, Ireland
Registered Number: 254776
Tel: (353 1) 6603350 Fax: (353 1) 6686672 Email: info@ipha.ie

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