Drug Interaction:
Alcohol, Cimetidine, iodinated constrast agents
ACE inhibitors, potent CYP3A4 inhibitors, digoxin, insulin, sulfonylureas,
diuretics, morphine, procainamide, quinine, quinidine, ranitiditine,
trimethoprin, vancomycin, nifdepine, cimetidine,
betablockers Steroids, estrogens, OCs,
phenothiazines, phenytoin, thyroid products, nicotinic acid,
sympthomimetics, calcium channel blockers, isoniazid
Indication:
U.S.FDA APPROVED DRUGS FROM 01-01-08 TO 31-12-08
Drug name Indication Date of Approval
118. Sitagliptin (as phosphate) 50mg 28-04-08
+Metformin Hcl 500mg/1000mg
film coated tablets
As an adjunct to diet & excercise to improve glycemic
control in patients with type two diabetes mellitus
U.S FDA APPROVED DRUGS DURING 2007
158. Sitagliptin tablet 30-10-07
(25mg/50mg/100mg)
As adjunct to diet and excercise to improve
glycemic control in patients with type II diabetes
New Drugs Approved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
1.Sitagliptin Phosphate 50mg 28-04-2008
+Metformin Hcl 500mg/1000mg
Filmcoated tablet
As an adjunct to diet & excercise to improve Glycemic control in patients
with type 2 Diabetes Mellitus
2.Sitagliptin Tablet 25mg/50mg/100mg 03-07-2010
Addl.Indcn
i.Use of sitagliptin Phosphate in combination with Metaformin and a
APPARr agonist as an adjunct to diet & excercise in Adult Patients
with Type 2 Diabetes Mellitus who are inadequately controlled on
combination therapy with Metformin and APPAR agonist
ii.Use of Sitagliptin Phosphate in combination with Metformin
3.Sitagliptin Tablet 25mg/50mg/100mg 30-10-2007
As an adjunct to diet and excercise to improve Glycemic control in
patients with Type-2 Diabetes
FIXED DOSE COMBINATIONS APPROVED BY DCG(I)
FROM JANUARY 1961 TILL NOVEMBER 2014
Name of Drug Indication Date of Approval
Combipack - Each strip contains 04-06-2014
A. Sitalgliptin phosphate Film coated tablets contains:
Sitalgliptin Phosphate monohydrate eq.to 100mg of
Sitalgliptin
B Metformin Hydrochloride sustained release Tablet IP
Each uncoated tablet contains 1000mg of Metformin Hcl IP
As an adjunct to diet and excercise to improve glycemic
control in adult patients with type 2 Diabetes Mellitus
Addl.Stgth
Type II diabetes inadequately controlled by diet
Adverse Reaction:
Nausea, URTI, Lactic acidosis -discontinue use
Also discontinue use in serious hypersentivity reactions, including anaphylaxis
Stevens- Johnson syndrome Pancreatitis. Nasopharyngitis,
Asthenia With Sulfonyl urea - hypoglycemia, constipation.
With Pioglitazone- Headache, diarrhea, vomiting, peripheral edema
With Insulin- Hypoglycemia
Contra-Indications:
Type 1 diabetes.
Moderate to severe renal or hepatic impairment
Diabetic ketoacidosis or pre-coma Acute conditions predisposing to renal impairment Cardiac or respiratory failure Recent MI Acute alcohol intoxification Septicemia. Concomittant intravascular iodinated contrast agents Suspend during and 48 hours after use
Special precautions-
Confirm normal renal function before starting and monitor atleast annually 2-4 times a year in elderly patients with serum creatinine levels at ULN
Discontinue for 48 hours before and after surgery and measure renal function before resuming therapy CHF -Elderly. Dehydration. Monitor haemotology specially serum vitamin B-12, Stress, fever, infection, trauma
Dosages/ Overdosage Etc:
Indication-
Type II diabetes not controlled by diet
Dosage-
Initially- 1 50mg tab twice daily Max daily dose of Sitalgliptin 100mg
Patients below 18 years not recommended
Pharmacology/ Pharmacokinetics:
Pharmacokinetics-
After oral admin of a 100mg dose to healthy subjects, sitagliptin was rapidly absorbed with
peak plasma concentration (median time to reach maximum concentration) occuring in
1 to 4 hours postdose.
Plasma area under the curve AUC of sitagliptin increased in a dose dependent manner.
Following a single 100mg dose to healthy volunteers , mean AUC of stagliptin was 8.52 M*h
maximum effective plasma concentration Cmax was 950 nM
Apparent terminal half life t 1/2 was 2.4 hrs
Plasma AUC of sitagliptin increased approx 14% following 100mg doses at steady state
compared with first dose. The intra and intersubject coefficients of variation for
sitagliptin AUC were small (5.8% and 15.1%)
