Saxaglyptine (Saxagliptinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Hypoglycemic synthetic and other agents

Included in the formulation
  • Anglis®
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    AstraZeneca UK Ltd     United Kingdom
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    A.10.B.H   Inhibitors of dipeptidyl peptidase 4 (DPP-4)

    A.10.B.H.03   Saxaglyptine

    Pharmacodynamics:Enhances the hypoglycemic effect of endogenous incretins. Inhibits dipeptidyl peptidase-4, suppressing the enzymatic cleavage of endogenous incretins (GLP-1 and HIP), increasing their concentration in blood plasma by an average of 2-3 times.
    Pharmacokinetics:

    Bioavailability with oral administration is 75%. Metabolised in the liver with the formation of an active metabolite. It is excreted mainly by the kidneys, the half-life of saxagliptin is 2.5 h, half-life active metabolite - 3.1 hours Assign 1 time per day.

    Indications:

    - Type 2 diabetes mellitus:

    - in addition to diet and exercise therapy to improve glycemic control as a monotherapy;

    - as a starting combination therapy with metformin;

    - for addition to monotherapy with metformin, thiazolidinediones, sulfonylurea derivatives, in the absence of adequate glycemic control in this therapy.

    ICD-10

    IV.E10-E14.E11.9   Non-insulin-dependent diabetes mellitus without complications

    IV.E10-E14.E11.8   Non-insulin-dependent diabetes mellitus with unspecified complications

    IV.E10-E14.E11.7   Non-insulin-dependent diabetes mellitus with multiple complications

    IV.E10-E14.E11.6   Non-insulin-dependent diabetes mellitus with other specified complications

    IV.E10-E14.E11.5   Non-insulin-dependent diabetes mellitus with peripheral circulatory disorders

    IV.E10-E14.E11.4   Non-insulin-dependent diabetes mellitus with neurological complications

    IV.E10-E14.E11.3   Non-insulin-dependent diabetes mellitus with eye damage

    IV.E10-E14.E11.2   Non-insulin-dependent diabetes mellitus with kidney damage

    IV.E10-E14.E11.1   Non-insulin-dependent diabetes mellitus with ketoacidosis

    IV.E10-E14.E11.0   Non-insulin-dependent diabetes mellitus with coma

    IV.E10-E14.E11   Non-insulin-dependent diabetes mellitus

    Contraindications:Type 1 diabetes mellitus (application not studied); application together with insulin (not studied); diabetic ketoacidosis; pregnancy; lactation period (breastfeeding); children and adolescents under 18 years of age (safety and efficacy not studied); hypersensitivity
    Carefully:

    With moderate and severe renal failure, elderly patients, and also together with sulfonylurea derivatives. Before the start of therapy and periodically during the treatment with the drug, it is recommended to evaluate the function of the kidneys. Derivatives of sulfonylureas can cause hypoglycemia, so reducing the dose of sulfonylurea derivatives may be required to reduce the risk of hypoglycemia when used simultaneously with saxagliptin.

    Do not administer to patients who have experienced severe hypersensitivity reactions with other DPP-4 inhibitors.

    Pregnancy and lactation:

    Action category for the fetus by FDA - X

    Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Inside in a dose of 5 mg 1 time / day.

    For patients with mild renal insufficiency (CK> 50 ml / min), dose adjustment is not required.

    For patients with moderate or severe renal insufficiency (CK ≤50 ml / min), as well as for patients on hemodialysis, the recommended dose is 2.5 mg 1 time / day.

    It should be taken at the end of the hemodialysis session. The use of saxagliptin in patients on peritoneal dialysis has not been studied.

    With simultaneous use with powerful inhibitors of CYP3A4 / 5, such as ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir and telithromycin, the recommended dose of saxagliptin is 2.5 mg 1 time / day.

    Side effects:

    From the endocrine system: hypoglycemia (frequency comparable to placebo).

    From the respiratory system: nasopharyngitis, sinusitis.

    From the digestive system: often - gastroenteritis, vomiting.

    From the nervous system: headache.

    Others: urinary tract infections, hypersensitivity reactions (frequency comparable to placebo), peripheral edema, small decrease in the number of lymphocytes (clinical significance is not known).

    Overdose:

    Not described.

    Interaction:

    In studies involving healthy volunteers, the pharmacokinetic parameters of saxagliptin and its main metabolite did not change significantly under the influence of metformin, glibenclamide, pioglitazone, digoxin, simvastatin, diltiazem, ketoconazole, omeprazole, a combination of aluminum hydroxide, magnesium hydroxide and simethicone, and famotidine.

    Significantly does not change the pharmacokinetic parameters of metformin, glibenclamide, pioglitazone, digoxin, simvastatin,diltiazem or ketoconazole.

    The combined use of saxagliptin and inducers of CYP3A4 / 5 isoenzymes, such as carbamazepine, dexamethasone, phenobarbital, phenytoin and rifampicin, can lead to a decrease in the concentration of saxagliptin in plasma and an increase in the concentration of its main metabolite.

    Special instructions:

    May cause dizziness, which should be considered in patients managing the car and other mechanisms.

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