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Diabetes mellitus (DM) is a chronic disease associated with polyurea, polydipsia, and polyphagia. It is associated severe complication if not controlled properly. The probability of developing cardiac arrythmia is more in patients with diabetes compared to general population. Previously, studies which used a maximum dose of 40 mg of Teneligliptin didn’t show any QT prolongation. There are hardly any studies which was done to prove the cardio safety of Teneligliptin. Therefore, we wanted to evaluate the prevalence of QT prolongation with teneligliptin in diabetic patients. MethodsWe analysed all patients who were treated with teneligliptin. We analysed ECG of all patients before and after therapy with teneligliptin. Our main aim was to compare the QT interval in ECG before and at the end of 3 months. We also analysed their HbA1c, fasting plasma glucose (FPG), and postprandial plasma glucose (PPG) before and after therapy. ResultsThe mean age of these patients was 55.5 ± 10.6 years. They were on treatment for diabetes with a mean duration of diabetes of 7.9 ± 5.7 years. All patients responded well to the treatment with a reduction in HbA1c, FBS and PPBS, all of those being statistically significant. When we analysed the QT interval of all patients before and after three months of therapy, there was no significant increase in the mean QTc interval at the end of 3 months. All of them tolerated the drug without any serious adverse effects. ConclusionsTeneligliptin in dose of 20 mg didn’t prolong QTc interval; meanwhile, it was found to be very effective in reducing the HbA1c, fasting plasma glucose, and post prandial plasma glucose at the end of 3 months.
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The gut enzymes are released in response to intake of meal, those are GLP-I (glucagon link peptide-I) & GIP (glucose-dependent insulin tropic polypeptide) along with DPP-4(Dipeptidylpeptidase-4). GLP-I has vital role in control of glucose levels and it may also has capacity reduce body weight and it can manage some micro & macro-vascular complications. Unfortunately it has very shorter half-life 1-2 min, and eventually it was degraded by DPP-4 enzyme. Therefore GLP-I has ineffective to perform its tasks. To overcome this incidence essential to inhibit DPP-4 enzyme is benefited in diabetics and in non diabetics suffering with micro, macro vascular complications. Ubiquitous Dipeptidyl peptidase (DPP) -4 has pleiotropic effects because it is widely distributed other than intestine. DPP-4 enzyme inhibition has a promising effect on glycemic control. DPP-4 inhibition is also involved in the improvement of non-glycemic effects as directly or indirectly the DPP-4 enzyme is linked with some pathological conditions of particular organs, such as DPP-4 is linked with the intestinal secretion of triglycerides, and DPP-4 is expressed in the glomerulus in uncontrolled diabetics which in turn leads to nephritis. DPP-4 release strongly correlates with adipocyte size, potentially representing an important source of DPP-4 in obesity. DPP-4 inhibition produces an anti-inflammatory activity because the activity of DPP-4 results in reduced production of cytokines including interleukins and interferon-G. All these anti-inflammatory agents are inhibited by the DPP-4 enzyme which can lead to pathogenesis of cardiovascular diseases and provokes atherosclerosis & psoriasis. Serum sodium and brain natriuretic peptide (BNP) levels are also regulated by inhibition of the DPP-4 enzyme and which can produce vascular protection & regulates blood pressure. Teneligliptin is a recently developed oral DPP-4 inhibitor indicated for the management of T2DM in adults along with diet and exercise. Teneligliptin is recently available in India and is also available in combination with other oral hypoglycemic agents at affordable prices. This review is aimed at exploring the status of teneligliptin with emphasis on its glycemic effects and non-glycemic clinical benefits associated with increasing GLP-1 & GIP
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Background DPP-4 inhibitors showed analgesic and anti-inflammatory activity in human and animal-studies. DPP-4 inhibitors improved nerve function and thermal nociception in animal models. Aim of the study was to explore analgesic activity of single and multiple doses of teneligliptin 20 mg/day using hot air analgesiometer in healthy human volunteers.Methods: After IEC approval and informed consent, subjects were randomized to receive either teneligliptin 20 mg or placebo in double-blinded manner with standard breakfast. Mean pain threshold and tolerance(sec) using hot air analgesiometer were recorded at baseline and 1 hr, 2 hrs post drug on day 1, for single dose study. Subsequently drugs were administered under supervision daily for 6 days and same procedure repeated on day8 for multiple-dose study. After 2 weeks washout, subjects crossed over in period 2 to receive other formulation and same procedure repeated to determine study parameters. Fasting blood-sugar (FBS) was monitored, ADRs recorded in CRF. Statistical analysis done with SPSS20.0.Results: Twelve-healthy subjects (8 males, 4 females) with mean age 33.08±4.69 years, mean BMI 22.6±1.37kg/m2 participated. Single dose teneligliptin produced significant increase in pain threshold (35.9%) and pain tolerance (25.1%) (p<0.001) at 1hour compared to baseline. With multiple doses, pain threshold increased by 37.1% and pain tolerance by 25.4% (p<0.001) at 1hour compared to baseline. The increase in pain threshold and tolerance values at 1 and 2 hours were similar. There was no significant change in pain threshold(p=0.4135) and tolerance (p=0.4476) at baseline on day1 and day 8. Placebo showed non-significant change in study parameters. Both treatments well tolerated. FBS of volunteers within normal limits during treatment period and no hypoglycemia reported.Conclusions: Results of our study suggest that teneligliptin20mg in healthy subjects demonstrated modest analgesic activity compared to baseline and placebo. Its role in painful diabetic conditions may be further explored.
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Background: Diabetes is a most prevalent chronic disease and has reached to alarming stage in almost all developed and developing countries. Worldwide approximately four hundred millions of people are living with diabetes and it is a leading cause of death. Aims and objectives is to study effectiveness of addition of drug Teneligliptin to Metformin, Glimepiride, Pioglitazone combination in type II Diabetic patients.Methods: This was a cross sectional study carried out in the department of Medicine of a tertiary health care centre during the one year period i.e. January 2017 to January 2018 in the type II diabetic patients. Out of all type II diabetic patients 40 patients who were on the treatment for hypoglycemia with drugs Metformin, Glimepiride, Pioglitazone were selected out of these randomly 20 patients were continued on the previous treatment (Group B) and remaining 20 were given additional drug Teneligliptin (Group A). The statistical analysis was done by unpaired t-test and chi-square test analyzed by SPSS 19 version of software.Results: In this study Authors have seen that the average age in both the groups was comparable i.e. 36.78±6.74 and 38.92±5.87 (p>0.05, t=1.24, df=38), the sex ration was also similar in both the group (p>0.43, χ2=0.43, df=1) and the HbA1C was comparable at 1st Wk. 10±4.56 - 9.87±3.42 (p>0.05, t=1.023, df=38) and 4th Wk. 8±5.23 - 9.67±4.52 (p>0.05, t=1.0804, df=38) but significantly differed at 8th Wk. 7.12±2.34 - 9.92±3.56 (p<0.01, t=3.82, df=38), 12th Wk. 5.98±1.98 - 9.24±2.79 (p<0.001, t=4.26, df=38) respectively in Group A and B.Conclusions: It can be concluded from this study that the addition of Teneligliptin significantly reduced the HbA1c level at the end of 4th wk. and hence superior to conventional Metformin, Glimepiride, Pioglitazone only combination treatment.
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Background: Teneligliptin is a DPP-4 inhibitor with unique chemical structure. Efficacy and safety of Teneligliptin is well established in the patients with type 2 diabetes mellitus (T2DM) in different randomized controlled trials. However, limited real-world data is available for Teneligliptin pertaining to Indian T2DM patient profile such as demographics, duration of disease, currently prescribed anti-hyperglycemic drugs, initiation of Teneligliptin as monotherapy or as an add on therapy.Methods: A cross-sectional, multicenter, non-interventional study was conducted to understand the demographics and clinical profile of Indian T2DM patients (n=5091) who were prescribed Teneligliptin.Results: Majority of patients were male (65.2%) with family history of T2DM present in 43.45% of cases. Age at onset of T2DM was 51.1±11.6 years. Among the T2DM patients, 36.2% of patients were newly diagnosed and more than half of them (54.7%) were uncontrolled with current anti-hyperglycemic drugs. Mean HbA1c level among these patients was 8.09±1.3%. Mean fasting and postprandial blood glucose levels were 170.2±46.9 mg/dl and 255.3±69.3 mg/dl respectively. Teneligliptin was prescribed as monotherapy in 2165 (41.66 %) of patients while as dual, triple and quadruple therapy in 2346 (46.08%) and 551 (10.82%) and 29 (0.56%) respectively. Among the patients on current anti-hyperglycemic treatment, most commonly prescribed drugs along with Teneligliptin were metformin (43.39%) followed by glimepiride (11%) and voglibose (3.42%).Conclusions: Teneligliptin is preferred as monotherapy and combination with metformin and sulfonylureas (mostly glimepiride) in newly diagnosed and uncontrolled T2DM patients in Indian scenario.
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Background: This comparative study was done to evaluate the change from baseline in HbA1c levels with teneligliptin vs. metformin treatments at week 12 among recently diagnosed type 2 DM patients attending Medicine OPD of Dr. B. C. Roy Hospital, Haldia, West Bengal (a tertiary care teaching hospital).Methods: In this prospective parallel group clinical study patients were divided into two groups. Group A patients were on metformin monotherapy therapy and Group B patients were on teneligliptin monotherapy. Data of 40 patients (20 patients in each group) were available for analysis in the present study. Secondary endpoints included changes from baseline FPG and 2h-PPG values at 12 weeks were evaluated. Safety and tolerability were assessed by the incidence of adverse events (AEs) throughout the study period.Results: The mean age of patients was 50.05±12.35 years and out of the entire patient population 70% were males and 30% were females. At the end of 12 weeks or 3 months of metformin therapy, mean HbA1c, FBG, and PPG were significantly reduced by 0.52%, 16.2mg/dL, and 36.8mg/dL, respectively, and 37.75% of patients achieved the HbA1c target of <7%. At the end of 12 weeks or 3 months of teneligliptin therapy, mean HbA1c, FBG, and PPG were significantly reduced by 0.60%, 19.4mg/dL, and 49.8mg/dL, respectively (Table 2), and 40% of patients achieved the HbA1c target of <7%.Conclusions: Teneligliptin, a DPP4 inhibitor reduced HbA1C significantly compared with monotherapy of metformin in treatment naive patients at week 12. It also reduced FBG and 2-h PPBG as compared with metformin at week 12.
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Aim: This study aims to evaluate the effectiveness and safety of teneligliptin when switched from other gliptins in patients notcontrolled on oral antidiabetic drugs in Type 2 diabetes mellitus (T2DM).Methodology: Data of T2DM patients who were switched from other gliptins to teneligliptin uncontrolled by dual or triple drugtherapy. Data of at least 3 months were collected from hospital records and analyzed. Efficacy was evaluated by the changesin fasting blood sugar (FBS), postprandial blood sugar (PPBS), and hemoglobin A1c (HbA1c) from the baseline.Results: A total of 97 patients’ data were collected and were analyzed. The mean age of the patients was 59.9 years andmean duration of diabetes was 16 years. Hypertension (61.9%) was the common comorbid condition with diabetes. Sitagliptinwas most prescribed dipeptidyl peptidase-4 (DPP-4) inhibitors with 65 (67%) patients with a mean dose of 88.5 mg, followedby vildagliptin with 10 (10.3%) patients was prescribed with a mean dose of 95 mg. Metformin and glimepiride were the mostcommon combination used with these DPP-4 inhibitors 91 (93.8%) patients and 69 patients (71.1%) were prescribed, respectively.There was a significant reduction in FBS, PPBS, and HbA1c from the baseline with a difference of 45 mg/dL, 102 mg/dL, and1.6%, respectively, after switching to teneligliptin from other gliptins. Teneligliptin was well tolerated and no serious adverseevents were reported.Conclusion: Teneligliptin was effective in significantly reducing FBS, PPBS, and HbA1c when switching from other gliptins inT2DM patients not controlled with other antidiabetic agents. The drug was well tolerated and no serious adverse events werereported.
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Background and Aim: According to a strict QT/QTc evaluation study and clinical studies for type 2 diabetes conducted in Japanand other countries, NO AEs related to QT prolongation were detected with 40 mg/day of teneligliptin, which is the maximaldosage used in clinical practice. So far, there are no data regarding the safety of teneligliptin in Indian type 2 diabetic patientswith respect to QTc prolongation. Therefore, the study was conducted to evaluate the safety of teneligliptin in type 2 diabeticpatients with respect to QT prolongation.Methods: A retrospective data were collected from type 2 diabetes mellitus patients with electrocardiogram (ECG) recordswho were treated with teneligliptin along with ongoing treatment. Primary endpoint was to compare the change in the ECGat 3 months from the baseline from the collected data. Mean daily dose (MDD) of antidiabetic drugs, HbA1c, fasting plasmaglucose (FPG), and postprandial plasma glucose (PPG) was also analyzed.Results: A total of 49 patients’ data were collected and analyzed with a mean age of 55.5 years and mean duration ofdiabetes 9.3 years. Hypertension was the most common comorbid disease (63.3%) along with diabetes for a mean durationof 10.0 years. Metformin plus glimepiride were the most prescribed dual drugs (63.3%) along with teneligliptin with an overallMDD of metformin (1065.2 mg) and glimepiride (2.1 mg). From the collected data, there was significant reduction in FPG andPPG at 3 months which were 49.6 mg/dL (P < 0.0001) and 100.5 mg/dL (P < 0.0001) reduction observed from the baseline,respectively. Significant changes were observed in the HbA1c from the baseline to 3 months (0.9%, P < 0.0001). There wasno significant increase in the mean QTc interval from baseline to 3 months. No serious adverse events or hypoglycemiawere reported.Conclusion: Teneligliptin was well tolerated with no significant change in QTc prolongation and significantly effective in reducingthe FPG, PPG, and HbA1c at 3 months from the baseline with no adverse events. There was no increase in the mean QT interval.
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Introduction: Type 2 diabetes mellitus (T2DM) with chronic kidney disease (CKD) is dreadful combination necessitatingadequate glycemic control to prevent further complications. Teneligliptin is found to be renal friendly antidiabetic agent whichcan provide effective glycemic control.Objective: The objective of this study was to determine the efficacy of teneligliptin as add-on to existing therapy in patients ofT2DM with CKD.Materials and Methods: This was a retrospective study where patients with T2DM and CKD who received teneligliptin wereincluded in the study. Changes in glycemic parameters such as hemoglobin A1c (HbA1c) (%), fasting plasma glucose (FPG),and postprandial plasma glucose (PPG) and change in estimated glomerular filtration rate (eGFR) were analyzed.Results: In total, 66 patients were included in analysis. Mean age was 57.7 ± 14.0 years and 60.6% were males. BaselineHbA1c, FPG, and PPG levels were 7.8 ± 0.7%, 128.0 ± 25.5 mg/dl, and 214.0 ± 55.9 mg/dl, respectively. There was a significantreduction in HbA1c at 3 and 6 months (mean difference from baseline: −0.9 ± 0.5 and −1.2 ± 0.5 respectively, P < 0.001 forboth). Similarly, mean change in FPG (−28.4 ± 20.9 and −29.9 ± 24.3 mg/dl, respectively) and PPG (−70.5 ± 49.2 and −97.0 ±60.7 mg/dl, respectively) was also significant (P < 0.001 for all comparisons). The change in eGFR was significant at 3 months(P = 0.049) and 6 months (P = 0.014).Conclusion: Teneligliptin is effective in reducing glycemic burden in patients with T2DM and CKD and can be considered asbe considered among first choices for glycemic control in patients with renal impairment.
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@#<p><strong>OBJECTIVES: </strong>Hydroxychloroquine (HCQ) 400 mg is approved by the Drug Controller General of India (DCGI) and recommended by the Research Society for the Study of Diabetes in India (RSSDI) clinical practice recommendations 2017 as add-on therapy after metformin and sulfonylurea in Type 2 Diabetes (T2DM) patients. The aim of this observational study is to compare the efficacy and safety of hydroxychloroquine 400 mg and teneligliptin 20 mg when used as add-on therapy in Indian Type 2 DM patients who were inadequately controlled (HbA1c ?7.5%) with metformin 1000 mg and glimepiride 2 mg combination.</p><p><strong>METHODOLOGY:</strong> This study is a prospective observational study to be conducted in 2 diabetic centres of Patna city between October 2017 and May 2018 involving 180 patients followed up for 6 months. One group (N=90) of patients received hydroxychloroquine 400 mg + metformin 1000 mg + glimepiride 2 mg, the other group (N=90) received teneligliptin 20 mg + metformin 1000 mg + glimepiride 2 mg. Efficacy was assessed by fasting blood glucose (FBG), post prandial blood glucose (PPBG) and glycated haemoglobin (HbA1c) reduction. Safety was evaluated by the number of hypoglycaemic events and changes in serum creatinine levels. Home based glucose monitoring was used to detect the hypoglycaemic events. Patients who had any type of retinopathy/maculopathy were excluded.</p><p><strong>RESULTS:</strong> Mean age of entire population was 66 ± 8 years with mean 6 ± 2 years of DM with 102 males. Mean body weight was 71 ± 12 kg. Baseline HbA1c was 8.1 ± 0.3 in the hydroxychloroquine group and 8.2 ± 0.2 in the teneligliptin group.</p><p>At 24 weeks there were statistically significant reductions in mean HbA1c in the hydroxychloroquine group (1.1 ± 0.3) as compared to the teneligliptin group (0.82 ± 0.3) (P?0.001). The mean FBG and PPBG was 169 ± 18 mg/dl and 232 ± 18 mg/dl respectively in hydroxychloroquine group which was reduced to 121 ± 15 mg/dl and 161 ± 19 mg/dl at the end of 24 weeks. In the teneligliptin group, FBG and PPBG was 171 ± 16 mg/dl and 239 ± 21 mg/dl at baseline, which was reduced to 121 ± 15 mg/dl and 161 ± 19 mg/dl respectively in same period of time (P? 0.005). There were 4 incidences of hypoglycaemic events in the hydroxychloroquine group (4.4%) and 6 in the teneligliptin group (6.67%). No patients required medical assistance for hypoglycaemic events. There was no statistically significant change in body weight in both the groups. No marked changes in creatinine levels were found in patients in both the groups.</p><p><strong>CONCLUSION:</strong> In conclusion, treatment with hydroxychloroquine 400 mg for 24 weeks reduces glycaemic parameters more aggressively than teneligliptin 20 mg in Indian type 2 diabetes patients.</p>
Subject(s)
Humans , HydroxychloroquineABSTRACT
Three new UV spectrophotometric methods namely simultaneous equation, absorbance ratio and first derivative (zero crossing) spectroscopic methods were developed and validated for simultaneous estimation of teneligliptin hydrobromide hydrate and metformin hydrochloride in tablet formulation which were simple, sensitive, precise and accurate. In simultaneous equation method, absorbance was measured at 237 and 246 nm for both the drugs. Teneligliptin hydrobromide hydrate and metformin hydrochloride was estimated using 237 and 247.5 nm in absorbance ratio method. First derivative (zero crossing) method was based on the transformation of UV spectra in to first derivative spectra followed by measurement of first derivative signal at 237 and 246 nm for teneligliptin hydrobromide hydrate and metformin hydrochloride, respectively using 2 nm as wavelength interval (Δλ) and 1 as scaling factor. Developed methods were validated according to ICH guidelines including parameters viz., specificity, linearity and range, precision, accuracy, limit of detection and quantification. All the three methods showed linear response in the concentration range of 1-20 µg/ml for both the drugs. Results of method validation parameters follows ICH guideline acceptable limits. Based on the assay results obtained, methods were compared using one-way ANOVA followed by Bonferroni multiple comparison tests (95% confidence level) using computer based fitting program (Prism, Graphpad version 5, Graphpad Software Inc). Outcome of the statistical analysis proved that there was no considerable dissimilarity between all the developed methods. Methods were found to be simple, fast, highly sensitive, cost effective and hence can be useful for simultaneous estimation of teneligliptin hydrobromide hydrate and metformin hydrochloride in commercial tablet formulation for routine quality control analysis.