The drug product, with the proposed the proprietary name TRADJENTA and the established name Linagliptin, is a dipeptidyl peptidase-4 inhibitor indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. Linagliptin 5 mg showed superiority over 1 mg with regard to trough DPP-4 inhibition (72% vs 32%, p=0.0050) and a numerically larger reduction with regard to adjusted mean change from baseline in HbA1c (-0.63% vs -0.48%, n.s.). Bethesda, MD 20894, Web Policies Co-administration with other potent inducers of P-glycoprotein and CYP3A4, such as carbamazepine, phenobarbital and phenytoin has not been studied. being unable to get an erection at any time. Frequencies are defined as very common ( 1/10), common ( 1/100 to <1/10), uncommon ( 1/1,000 to < 1/100), rare ( 1/10,000 to < 1/1,000), very rare (<1/10,000) or not known (cannot be estimated from the available data). 8 phase III randomised controlled trials involving 5,239 patients with type 2 diabetes, of which 3,319 were treated with linagliptin were conducted to evaluate efficacy and safety. Hypersensitivity to the active substance or to any of the excipients listed in section 6.1. Improving clinical practice and health outcomes for Australia. Linagliptin as add-on therapy in patients with severe renal impairment, 12 week placebo-controlled data (stable background) and 40 week placebo-controlled extension (adjustable background). The absolute bioavailability of linagliptin is approximately 30%. Liver, kidneys and gastrointestinal tract are the principal target organs of toxicity in mice and rats at repeat doses of linagliptin of more than 300 times the human exposure. The observed incidence of hypoglycaemia in patients treated with linagliptin was similar to placebo. A decision must be made whether to discontinue breast-feeding or to discontinue/abstain from linagliptin therapy taking into account the benefit of breast-feeding for the child and the benefit of therapy for the woman. A risk to the breast-fed child cannot be excluded. As a precautionary measure, it is preferable to avoid the use of linagliptin during pregnancy. Linagliptin provided significant improvements in HbA1c (-0.59 % change compared to placebo after 12 weeks), from a mean baseline HbA1c of 8.2%. Drug Metab Dispos. For patients with renal impairment, no dose adjustment for linagliptin is required. Although several side effects . How quickly can acute migraines be treated? 2011 Mar 26;71(5):611-24. doi: 10.2165/11207400-000000000-00000. The need for ongoing treatment should be regularly reviewed, It is unknown whether the dose of antidepressant required to induce remission in major depressive disorder is the same as that needed to maintain and/or sustain euthymia, Symptoms of premenstrual dysphoric disorder has been reported to worsen with age, until relieved at the onset of menopause, CARDIOVASCULAR: Regular blood pressure monitoring, METABOLIC: Signs/symptoms of hyponatremia, NERVOUS SYSTEM: Signs/symptoms of serotonin syndrome, PSYCHIATRIC: Discontinuation symptoms, worsening/emergence of suicidal thoughts, and/or unusual changes in mood/behavior. INSULINS, A10BD Combinations of oral blood glucose lowering drugs, A10BD27 Metformin, linagliptin and empagliflozin, Cytochrome P-450 CYP3A4 Inhibitors (moderate), Cytochrome P-450 CYP3A4 Substrates (strength unknown), Hormones, Hormone Substitutes, and Hormone Antagonists, Predicted MS/MS Spectrum - 10V, Positive (Annotated), Predicted MS/MS Spectrum - 20V, Positive (Annotated), Predicted MS/MS Spectrum - 40V, Positive (Annotated), Predicted MS/MS Spectrum - 10V, Negative (Annotated), Predicted MS/MS Spectrum - 20V, Negative (Annotated), Predicted MS/MS Spectrum - 40V, Negative (Annotated), LC-MS/MS Spectrum - LC-ESI-qTof , Positive, splash10-00di-0113900000-1cf1f79967a4761f3983, splash10-0ufr-0391100000-8df1ebbcbdc456f86470, splash10-00di-0114900000-928cf1c76b7fa52190f2. Linagliptin (Trajenta, Tradjenta, Trazenta, Trayenta) is an oral, highly selective inhibitor of dipeptidyl peptidase-4 and is the first agent of its class to be eliminated predominantly via a nonrenal route. The reductions in glycosylated haemoglobin A1c (HbA1c) were similar across different subgroups including gender, age, renal impairment and body mass index (BMI). A target HbA1c of 7% or less was achieved by 26% of the linagliptin group and 9% of the placebo group.2. About dapoxetine Before taking dapoxetine How to take dapoxetine tablets Can dapoxetine tablets cause problems? Warnings and Precautions Use with Medications Known to Cause Hypoglycemia (5.1) 8/2012 -----INDICATIONS AND USAGE----- TRADJENTA is a dipeptidyl peptidase-4 (DPP-4) inhibitor indicated . GPO Box 5480, Sydney NSW 2001 Australian Commission on Safety and Quality in Health CareLevel 5, 255 Elizabeth StreetSydney NSW 2000, We are always looking for ways to improve our website, Please help us to improve our services by answering the following question. Patients should speak with their healthcare provider if they are taking, or plan to take any new prescription or over the counter medications because there is a potential for drug interactions; patients should be advised to avoid alcohol as it may make some side effects worse. NPS MedicineWise disclaims all liability (including for negligence) for any loss, damage or injury resulting from reliance on or use of this information. Following 12-24 weeks of treatment, improvements in glycaemic control parameters, including glycosylated haemoglobin (HbA(1c); primary endpoint in all trials), were seen with linagliptin relative to placebo when used as monotherapy, initial combination therapy (with metformin or pioglitazone) or add-on therapy to other oral antihyperglycaemia agents (metformin and/or a sulfonylurea) or basal insulin (with or without metformin and/or pioglitazone). Clipboard, Search History, and several other advanced features are temporarily unavailable. Both incretin hormones are involved in the physiological regulation of glucose homeostasis. Linagliptin once daily produced clinically significant improvements in glycaemic control, with no clinically relevant change in body weight. Maintenance dose: 20 to 60 mg orally once a day, Maintenance dose: 12.5 to 37.5 mg orally once a day. This material is provided for educational purposes only and is not intended for medical advice, diagnosis or treatment. Epub 2010 Jan 19. [, Blech S, Ludwig-Schwellinger E, Grafe-Mody EU, Withopf B, Wagner K: The metabolism and disposition of the oral dipeptidyl peptidase-4 inhibitor, linagliptin, in humans. GAD: Efficacy has been demonstrated for up to 24 weeks in patients responding to treatment during an 8-week acute treatment phase. Episodes generally require several months or more of sustained pharmacological therapy; a periodic review of the need for ongoing maintenance treatment and appropriate dosing is recommended. No studies on the effect on human fertility have been conducted for linagliptin. Rare adverse events include hypersensitivity reactions and pancreatitis. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. In patients inadequately controlled with metformin and empagliflozin (10 mg (n=247) or 25 mg (n=217)), 24-weeks treatment with add-on therapy of linagliptin 5 mg provided adjusted mean HbA1c reductions from baseline by -0.53% (significant difference to add-on placebo -0.32% (95% CI -0.52, -0.13) and -0.58% (significant difference to add-on placebo -0.47% (95% CI -0.66; -0.28), respectively. A10BH Dipeptidyl peptidase 4 (DPP-4) inhibitors, A10B BLOOD GLUCOSE LOWERING DRUGS, EXCL. The study population included 1211 (17.4%) patients 75 years of age and 4348 (62.3%) patients with renal impairment. Older subjects (65 to 80, oldest patient was 78 years) had comparable plasma concentrations of linagliptin compared to younger subjects. The efficacy and safety of linagliptin was also evaluated in type 2 diabetes patients with severe renal impairment in a double-blind study versus placebo for 12 weeks duration, during which background glycaemic therapies were kept stable. Take one tablet 1-3 hours before you have sex. Table 2 Cardiovascular and renal outcomes by treatment group in the CARMELINA study, Primary CV composite (Cardiovascular death, non-fatal MI, non-fatal stroke), Secondary renal composite (renal death, ESRD, 40% sustained decrease in eGFR), ** Test on non-inferiority to demonstrate that the upper bound of the 95% CI for the hazard ratio is less than 1.3. We comply with the HONcode standard for trustworthy health information. Use: As an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. This increases insulin secretion and lowers glucose concentrations. 2010 Dec;27(12):1409-19. doi: 10.1111/j.1464-5491.2010.03131.x. 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. In this case, skip the missed dose and take your next dose at the usual time. In addition patients with T2DM and severe renal impairment (<30 ml/min) were compared to T2DM patients with normal renal function. Maintenance dose: 20 to 50 mg orally once a day. Erectile dysfunction (ED) is the most important disorder after premature ejaculation for sexual activity in men. What are some common side effects of antidepressants? Use our structured and evidence-based datasets to unlock new insights and accelerate drug research. The metabolism of Acalabrutinib can be decreased when combined with Linagliptin. There was a further follow up 40 week treatment period during which dose adjustments in antidiabetes background therapies were allowed. In the CARMELINA study, bullous pemphigoid was reported in 0.2% of patients treated with linagliptin and in no patient treated with placebo. Linagliptin is an inhibitor of the enzyme DPP-4 (dipeptidyl peptidase 4, EC 3.4.14.5) an enzyme which is involved in the inactivation of the incretin hormones GLP-1 and GIP (glucagon-like peptide1, glucose-dependent insulinotropic polypeptide). with a mean treatment difference of 0.20% (97.5% CI: 0.09, 0.299). How to take it Take linagliptin once a day. No dosage adjustment is necessary based on BMI. Linagliptin cardiovascular safety study (CAROLINA). Saudi Heart Association (SHA) guidelines for the management of heart failure. Studies of efficacy and safety in pediatric populations were not included in the original drug approval5 but recent clinical trials show linagliptin to be well tolerated in patients 10 to 18 years old4. Forst T, Uhlig-Laske B, Ring A, Graefe-Mody U, Friedrich C, Herbach K, Woerle HJ, Dugi KA. The risk or severity of hypoglycemia can be increased when Acarbose is combined with Linagliptin. Avoid excessive or chronic alcohol consumption. The efficacy of oral linagliptin in the treatment of adults with type 2 diabetes has been investigated in several double-blind, multicentre trials. The tablets can be taken with or without a meal at any time of the day. sharing sensitive information, make sure youre on a federal Linagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor used to manage hyperglycemia in patients with type 2 diabetes mellitus. Maximum dose: 50 mg/day. No dosage adjustment for linagliptin is proposed for diabetic patients with mild, moderate or severe hepatic impairment. 2021 Mar 10;22(6):2805. doi: 10.3390/ijms22062805. The study was designed to demonstrate non-inferiority for the primary cardiovascular endpoint which was a composite of the first occurrence of cardiovascular death or a non-fatal myocardial infarction (MI) or a non-fatal stroke (3P-MACE). 2012 Jun;55(6):1577-96 The study included 3494 patients treated with linagliptin (5 mg) and 3485 patients treated with placebo. Would you like email updates of new search results? You'll probably have to take it for a long time, even for the rest of your life. Their concentration can be increased by inhibiting the enzyme (dipeptidyl peptidase 4) which metabolises them. being able to get an erection sometimes, but not every time you want to have sex. Inhibition of this enzyme slows the breakdown of GLP-1 and glucose-dependant insulinotropic polypeptide (GIP)3,5. [, Gallwitz B: Novel Therapeutic Approaches in Diabetes. -, J Am Osteopath Assoc. Monitor for signs and symptoms of pancreatitis. Epub 2019 Jun 25. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults older than 24 years of age; there was a reduction in the risk with antidepressants compared to placebo in adults 65 years and older. Based on these results and in vivo interaction studies, linagliptin is considered unlikely to cause interactions with other P-gp substrates. The https:// ensures that you are connecting to the IR formulations: The daily dose may be increased in 10 mg increments at weekly intervals, according to clinical response and tolerability. The intra-subject and inter-subject coefficients of variation for linagliptin AUC were small (12.6% and 28.5%, respectively). Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about . Consult WARNINGS section for additional precautions. The pharmacokinetics of linagliptin was generally similar in healthy subjects and in patients with type 2 diabetes. Unauthorized use of these marks is strictly prohibited. Oral contraceptives: co-administration with 5 mg linagliptin did not alter the steady-state pharmacokinetics of levonorgestrel or ethinylestradiol. Symptoms of ED include. Before new drugs are prescribed, the Committee believes it is important that more detailed information is obtained from the manufacturer's approved product information, a drug information centre or some other appropriate source. Comparison of effects of Empagliflozin and Linagliptin on renal function and glycaemic control: a double-blind, randomized clinical trial. Linagliptin alone showed a comparable incidence of hypoglycaemia to placebo. Linagliptin is used together with proper diet and exercise to treat high blood sugar levels caused by type 2 diabetes. Linagliptin is a diabetes drug that works by increasing levels of natural substances called incretins. Linagliptin has minor interactions with the following drugs: See What Are Side Effects Associated with Using Linagliptin?, Serious hypersensitivity reactions were reported including anaphylaxis, angioedema, and exfoliative skin conditions, Heart failure has been observed with two other members of the DPP-4 inhibitor class; consider risks and benefits of, There have been no clinical studies establishing conclusive evidence of, Unknown if patients with a history of pancreatitis are at increased risk for the development of pancreatitis while using linagliptin, Strong CYP3A4 or P-gp inducers may decrease linagliptin systemic exposure, Avoid coadministration with strong CYP3A4 or P-gp inducers; alternant drug strongly recommended to maintain linagliptin efficacy, The limited data in pregnant women are not sufficient to inform of drug-associated risk for major birth defects and miscarriage; there are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy, In animal reproduction studies, no adverse developmental effects were observed when linagliptin was administered to pregnant rats during the period of organogenesis at doses similar to the maximum recommended clinical dose, based on exposure, Poorly controlled diabetes in pregnancy increases the maternal risk for diabetic, There is no information regarding the presence of linagliptin in human milk, the effects on the breastfed infant, or effects on milk production; however, linagliptin is present in rat milk; developmental and health benefits of breastfeeding should be considered along with the mothers clinical need for therapy and any potential adverse effects on the breastfed child from therapy or underlying maternal condition. 2014 Oct;74(16):1927-1946. doi: 10.1007/s40265-014-0308-3. 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