ONGLYZA ® - Saxagliptin

ONGLYZA ® a drug based on Saxagliptin

THERAPEUTIC GROUP: Oral hypoglycemic agents - DPP-4 inhibitors

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications ONGLYZA ® - Saxagliptin

ONGLYZA ® is used as a pharmacological aid for the second type of diabetic pathology, in addition to metformin, sulfonylureas and agonists of PPAR gamma, when single therapies have not produced the desired therapeutic effect.

Mechanism of action ONGLYZA ® - Saxagliptin

Saxagliptin, active ingredient of ONGLYZA ® is a selective inhibitor of DPP-4, enzymes responsible for the irreversible degradation of incretins (GLP-1 and GIP), gastro-intestinal hormones able to modulate pancreatic activity, increasing beta activity cells, resulting in increased concentrations of insulin, and sensitizing those alpha, with a reduction in glucagon secretion, responsible instead of the endogenous production of glucose.

From a metabolic point of view, both effects translate into a significant drop in glycemic levels, due to the doubling of incretin blood concentrations induced by saxagliptin.

Taken orally this active principle reaches the maximum plasma concentration around the third hour, exercising the inhibitory action of DPP-4 for about 24 hours and being subsequently metabolized also at the hepatic level in modestly active metabolites, eliminated mainly through the urine.

Small changes in drug exposure have been observed in patients with reduced liver and kidney function, for whom medical supervision is strictly necessary.

Studies carried out and clinical efficacy

1. THE EFFECTIVENESS OF COMBINED THERAPY

The treatment of the second type diabetic patient with the combined saxagliptin / metformin therapy, ensured excellent glycemic control, reducing by about 2 percentage points the concentrations of glycosylated hemoglobin in 76 weeks of treatment, without clinically relevant side effects. The results obtained were decidedly better than the single therapies.

2. WHICH INHIBITOR TO USE?

The recent development of numerous active ingredients capable of inhibiting the DPP-4 enzyme, and experimenting with new ones, requires a control and algorithms useful to the doctor in the correct prescription of the drug. It is therefore important that there are guidelines, which can help the specialist in formulating the correct treatment plan, safeguarding the patient's health and increasing the effectiveness of the therapy.

3. SAXAGLIPTIN, NOT JUST HYPOGLYCEMISANT

The treatment of second-type diabetic pathology with Saxagliptin was found to be useful not only in improving some markers of glucose metabolism such as glycosylated hemoglobin and fasting and post-prandial glycaemia, but also in modulating and reducing cardiovascular risk.

Method of use and dosage

ONGLYZA ® 5 mg saxagliptin tablets:

the recommended dosage is one tablet, taken independently of meals, in combination therapy with metformin, thiazolidinediones or sulfonylureas.

Although the aforementioned dosage is the most recommended, it is of fundamental importance that your doctor organizes the correct treatment plan based on the physio-pathological characteristics of the patient, on his metabolic picture and on the possible intake of other drugs.

Warnings ONGLYZA ® - Saxagliptin

Drug therapy with ONGLYZA ® should be supported and supported by non-pharmacological measures such as a balanced diet and a healthy lifestyle, useful for combating diabetic pathology.

Close medical supervision is necessary in patients with impaired renal or hepatic function, being treated with sulfonylureas, given the risk of hypoglycemia, and in elderly patients.

ONGLYZA ® contains lactose, therefore the administration in patients with lactase enzyme deficiency, lactose intolerance or glucose / galactose absorption deficiency could be accompanied by the concomitant onset of side effects concentrated mainly on the gastro-intestinal level.

The risk of hypoglycemia, particularly evident in case of concomitant intake of sulfonylureas, could make the use of machinery and driving vehicles dangerous.

PREGNANCY AND BREASTFEEDING

The use of ONGLYZA ® is not recommended in the treatment of gestational diabetes, given the absence of clinical studies able to test the safety profile of the drug on fetal health, and given the possibility of using better characterized drugs.

ONGLYZA ® should not also be taken in the next stage of breastfeeding, given the possibility of finding the active ingredient in breast milk, potentially dangerous for the health of the infant.

Interactions

Although the number of clinically significant interactions is low, pharmacokinetic changes in saxagliptin are described following the concomitant intake of diltiazem, ketoconazole, and rifampicin, potent modulatory drugs of the CYP3A4 enzyme system, which is responsible for the metabolism of saxagliptin.

Contraindications ONGLYZA ® - Saxagliptin

ONGLYZA ® is contraindicated in case of hypersensitivity to the active ingredient or to one of its components and during the period of breastfeeding and pregnancy.

This medicine should not be used for the treatment of diabetic patients of the first type or keto acidosidiabetica, much less in patients with reduced liver and kidney function.

Undesirable effects - Side effects

Data on the saxagliptin safety profile derive essentially from the clinical trial, which tested this active ingredient on more than 3, 000 patients.

Although therapy was found to be well tolerated among the most common adverse reactions, infections of the upper respiratory tract, headache and dizziness, vomiting, diarrhea and constipation, and peripheral edema were observed both in monotherapy and in combination therapy.

More severe clinical pictures have been observed only in rare cases, and in patients hypersensitive to the active ingredient, while hypoglycemic episodes have been described mainly following the combined use of saxagliptin and glibenclamide.