Consumer medicine information

1. Why am I using Sitagliptin Sandoz Pharma?

Sitagliptin Sandoz Pharma contains the active ingredient sitagliptin (as hydrochloride monohydrate). Sitagliptin Sandoz Pharma is used to lower blood sugar levels in patients with type 2 diabetes mellitus alone or in combination with certain other medicines, when diet plus exercise or the other medicine(s) do not provide adequate blood sugar level control. For more information, see Section 1. Why am I using Sitagliptin Sandoz Pharma? in the full CMI.

2. What should I know before I use Sitagliptin Sandoz Pharma?

Do not use if you have ever had an allergic reaction to Sitagliptin Sandoz Pharma or any of the ingredients listed at the end of the CMI. Talk to your doctor if you have any other medical conditions, take any other medicines, or are pregnant or plan to become pregnant or are breastfeeding. For more information, see Section 2. What should I know before I use Sitagliptin Sandoz Pharma? in the full CMI.

3. What if I am taking other medicines?

Some medicines may interfere with Sitagliptin Sandoz Pharma and affect how it works. A list of these medicines is in Section 3. What if I am taking other medicines? in the full CMI.

4. How do I use Sitagliptin Sandoz Pharma?

• Your doctor will tell you how many tablets to take each day. The standard recommended dose is one 100 mg tablet per day. Your doctor may prescribe a lower dose for you.

• Swallow the tablet whole by mouth, with or without food, with a glass of water and take Sitagliptin Sandoz Pharma at about the same time each day

5. What should I know while using Sitagliptin Sandoz Pharma?

6. Are there any side effects?

Common side effects: signs of an infection of the breathing passages (runny nose, sore throat, cough), soreness in the back of the nose and throat and discomfort when swallowing, headache, flu-like symptoms.
Serious side effects: Low blood sugar (sweating, irritable, fast heartbeat, shaky, nervous or anxious) when Sitagliptin Sandoz Pharma is used in combination with other medicine, skin blisters or breakdown of your skin (bullous pemphigoid), severe allergic reactions (swelling of face, lips, tongue and throat, difficulty breathing or swallowing), severe and persistent stomach pain (pancreatitis). For more information, including what to do if you have any side effects, see Section 6. Are there any side effects? in the full CMI.

1 Name of Medicine

Sitagliptin.

2 Qualitative and Quantitative Composition

Each Sitagliptin Sandoz Pharma film-coated tablet contains either 25 mg, 50 mg or 100 mg sitagliptin (as hydrochloride monohydrate).
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Film-coated tablet.
Sitagliptin Sandoz Pharma 25 mg film-coated tablet are pink, round, with "25" engraved on one side.
Sitagliptin Sandoz Pharma 50 mg film-coated tablet are light beige, round, with "50" engraved on one side.
Sitagliptin Sandoz Pharma 100 mg film-coated tablet are beige, round, with "100" engraved on one side.

4 Clinical Particulars

4.9 Overdose

During controlled clinical trials in healthy subjects, single doses of up to 800 mg sitagliptin were generally well tolerated. Minimal increases in QTc, not considered to be clinically relevant, were observed in one study at a dose of 800 mg sitagliptin (see Section 5.1 Pharmacodynamic Properties, Cardiac electrophysiology). There is no experience with doses above 800 mg in humans. In Phase I multiple-dose studies, there were no dose-related clinical adverse reactions observed with sitagliptin with doses of up to 400 mg per day for periods of up to 28 days.
In the event of an overdose, it is reasonable to employ the usual supportive measures, e.g. remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring (including obtaining an electrocardiogram), and institute supportive therapy if required.
Sitagliptin is modestly dialysable. In clinical studies, approximately 13.5% of the dose was removed over a 3- to 4-hour haemodialysis session. Prolonged haemodialysis may be considered if clinically appropriate. It is not known if sitagliptin is dialysable by peritoneal dialysis.
For information on the management of overdose, contact the Poison Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.3 Preclinical Safety Data

Genotoxicity. Sitagliptin was not mutagenic or clastogenic in a battery of genetic toxicology studies, including the Ames bacterial mutagenicity assay, a chromosome aberration assay in Chinese hamster ovary cells, an in vitro rat hepatocyte DNA alkaline elution assay (an assay which measures the compound's ability to induce single strand breaks in DNA), and an in vivo mouse micronucleus assay.
Carcinogenicity. A two-year carcinogenicity study was conducted in rats given oral doses of sitagliptin of 50, 150, and 500 mg/kg/day. There was an increased incidence of focal eosinophilic cellular alterations in the liver in both sexes at 150 mg/kg/day and at 500 mg/kg/day. There was an increased incidence of basophilic cellular alterations in females at 500 mg/kg/day. Eosinophilic and basophilic cellular alterations are regarded as preneoplastic lesions. There was an increase in hepatic adenomas and carcinomas in males, and hepatic carcinomas in females at 500 mg/kg/day. Systemic exposure in rats at 150 and 500 mg/kg/day are 19 and 58 times, respectively, that of humans at 100 mg/day. The no-observed effect level for induction of hepatic neoplasia in rats was 150 mg/kg/day, producing exposure approximately 19-fold higher than the human exposure at the 100 mg/day clinical dose. The increased incidence of hepatic tumours was likely secondary to chronic hepatic toxicity at this high dose. The clinical significance of these findings for humans is unknown.
In a two-year carcinogenicity study conducted in mice, sitagliptin did not increase tumour incidence at oral doses up to 500 mg/kg/day (approximately 68 times human exposure at the clinical dose of 100 mg/day).

6 Pharmaceutical Particulars

6.7 Physicochemical Properties

Sitagliptin Sandoz Pharma (sitagliptin hydrochloride monohydrate) is an orally-active inhibitor of the dipeptidyl peptidase 4 (DPP-4) enzyme for the treatment of type 2 diabetes. Sitagliptin differs in chemical structure and pharmacological action from GLP-1 analogues, insulin, sulfonylureas or meglitinides, biguanides, peroxisome proliferators-activated receptor gamma (PPARγ) agonists, alpha-glucosidase inhibitors, and amylin analogues.
Sitagliptin hydrochloride monohydrate is a white to almost white, crystalline, slightly hygroscopic powder. It is soluble in water, very slightly soluble in ethanol, and insoluble in hexane. The partition coefficient is 2.055 ± 0.673 and the pKa is 7.20 ± 0.10.
Chemical structure.
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSSIHYMO.gif Chemical name: 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl) butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine hydrochloride monohydrate.
Molecular formula: C₁₆H₁₈ClF₆N₅O₂.
Molecular weight: 461.79.
CAS number. 862156-92-1.

7 Medicine Schedule (Poisons Standard)

S4 - Prescription Only Medicine.

Summary Table of Changes

https://stagingapi.mims.com/au/public/v2/images/fulltablegif/SITSANST.gif