Saxagliptin

Brand Bristol-Myers Squibb

In stock 973 Items

Available since: 2019-09-19

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Clinical Pharmacology

Onglyza - saxagliptin is a potent selective reversible competitive inhibitor of dipeptidyl peptidase-4 (DPP-4).

In patients with type 2 diabetes, taking saxagliptin results in suppressing the activity of DPP-4 enzyme for 24 hours. After ingestion of glucose orally, inhibition of DPP-4 results in a 2-3-fold increase in the concentration of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (HIP), a decrease in glucagon concentration and an increase in glucose-dependent beta cell response, which leads to an increase in insulin and C-peptide concentration.

The release of insulin by beta cells of the pancreas and a decrease in the release of glucagon from pancreatic alpha cells leads to a reduction in fasting glucose and postprandial glycemia.

The efficacy and safety of using saxagliptin when taken in doses of 2.5 mg, 5 mg and 10 mg 1 time / studied in six double-blind, placebo-controlled studies involving 4148 patients with type 2 diabetes. The drug was accompanied by a statistically significant improvement in glycosylated hemoglobin (HbA1c), fasting plasma glucose (HPP) and postprandial glucose (PPG) plasma compared with the control.

Patients in whom the target level of glycemia could not be reached while taking saxagliptin as monotherapy were additionally prescribed metformin, glibenclamide or thiazolidinediones. When taking saxagliptin at a dose of 5 mg, a decrease in HbA1c was observed after 4 weeks, and HHP - after 2 weeks. In the group of patients who received saxagliptin in combination with metformin, glibenclamide or thiazolidinediones, a decrease in HbA1c was also observed after 4 weeks and HFN - after 2 weeks.

The effect of saxagliptin on the lipid profile is similar to that of placebo. During the therapy with saxagliptin, no increase in body weight was observed.

Indications

Type 2 diabetes in addition to diet and exercise to improve glycemic control as:

monotherapy;
starting combination therapy with metformin;
additions to monotherapy with metformin, thiazolidinedione, sulfonyl urea derivatives, in the absence of adequate glycemic control on this therapy.

Composition

active substance: Saxagliptin 5 mg.

Excipients: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, magnesium stearate, 1 M hydrochloric acid or sodium hydroxide 1 M solution, Opadry II white (polyvinyl alcohol, titanium dioxide, macrogol (PEG 3350), talc), Opadry II yellow (polyvinyl alcohol, polyvinyl alcohol, polyvinyl alcohol, macrogol (PEG 3350), talc) dioxide, macrogol (PEG 3350), talc, iron dye yellow oxide (E172), ink Opacode blue (shellac in ethyl alcohol, FD & C Blue # 2 / indigo carmine aluminum pigment (E132), n-butyl alcohol, propylene glycol, isopropyl alcohol, 28% ammonium hydroxide).

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Dosage and Administration

Adults and children over 12 years old - 100-200 mcg Salamol Eco (1-2 inhalation doses) for stopping asthma attacks.
To control the course of asthma of mild severity - 1-2 doses 1-4 times per day and moderate severity of the disease - in the same dosage in combination with other anti-asthma drugs.
For the prevention of physical asthma - 20-30 minutes before the load of 1-2 doses per dose.
Children from 2 to 12 years with the development of an attack of bronchial asthma, as well as to prevent attacks of bronchial asthma associated with allergen exposure or exercise, the recommended dose is 100-200 mcg (1 or 2 inhalations).
The daily dose of salbutamol should not exceed 800 micrograms (8 inhalations).

Adverse reactions

From the side of the central nervous system: tremor of the hands (a typical side effect for all beta2-adrenergic mimetics), headache, dizziness, irritability, anxiety, sleep disturbances, insomnia. The drug can cause arousal and increased motor activity in children.
Since the cardiovascular system: the expansion of peripheral vessels (flushing of the skin of the face), a slight compensatory increase in heart rate, increased blood pressure. Arrhythmias may occur (including atrial fibrillation, supraventricular tachycardia, and extrasystole).
Allergic reactions: in rare cases - angioedema, urticaria, erythema, nasal congestion, bronchospasm, hypotension, collapse.
From the digestive system: nausea, vomiting, dyspepsia.
On the part of the respiratory system: paradoxical bronchospasm, irritation of the oral mucosa and pharynx (pharyngitis), cough.
Metabolism: possible hypokalemia (may pose a serious danger to the patient), reversible hyperglycemia.
Other: muscle cramps.

Contraindications

- Heart rhythm disorders (paroxysmal tachycardia, polytopic ventricular premature beats), tachyarrhythmias.
- Myocarditis.
- Heart defects, aortic stenosis.
- Coronary heart disease.
- Thyrotoxicosis.
- Decompensated diabetes.
- Glaucoma.
- Epilepsy.
- Pyloroduodenal constriction.
- Liver failure.
- Renal failure.
- Pregnancy.
- Simultaneous reception of non-selective beta-blockers.
- Children's age up to 2 years.
- Hypersensitivity to any component of the drug.
Be wary appoint the drug in the following cases:
- Chronic heart failure.
- Hyperthyroidism.
- Arterial hypertension.
- Pheochromocytoma.

Drug interactions

Theophylline and other xanthines with simultaneous use with salbutamol increase the likelihood of developing tachyarrhythmias; means for inhalation anesthesia, levodopa - severe ventricular arrhythmias. It is not recommended to use both Salamol Eco and non-selective beta-adrenoreceptor blockers such as propranolol. Monoamine oxidase inhibitors and tricyclic antidepressants increase the effects of salbutamol and can lead to a sharp decrease in pressure. Salbutamol enhances the action of central nervous system stimulants, side effects of thyroid hormones, and cardiac glycosides. Reduces the effectiveness of antihypertensive drugs, nitrates. Hypokalemia may be enhanced by the simultaneous use of xanthine derivatives, glucocorticosteroids, diuretics. Simultaneous administration with anticholinergic agents (including inhalants) may contribute to an increase in intraocular pressure.

Pregnancy and Lactation

The drug is contraindicated for use in pregnancy. During lactation (breastfeeding) prescribed only in cases where the expected benefit to the mother outweighs any potential risk to the child.

Special instructions

In patients with severe or unstable bronchial asthma, the use of bronchodilators should not be the main or only method of therapy. If the effect of the usual dose of Salamol Eco becomes less effective or less prolonged (the effect of the drug should last at least 3 hours), the patient should consult a doctor.Frequent use of salbutamol can lead to increased bronchospasm, sudden death, and therefore it is necessary to take breaks of several hours between taking the next dose of the drug. The increased need for the use of inhaled β-2 adrenoreceptor agonists with a short duration of action to control symptoms of bronchial asthma indicates an exacerbation of the disease. In such cases, the patient’s treatment plan should be reviewed and the issue of administering or increasing the dose of inhaled or systemic glucocorticosteroids (GCS) should be decided. Therapy with β-2-adrenoreceptor agonists can lead to hypokalemia. Particular caution is recommended when treating severe attacks of bronchial asthma, since in these cases hypokalemia may increase as a result of the simultaneous use of xanthine derivatives, GCS, diuretics, and also due to hypoxia. In such situations, it is necessary to control the level of potassium in the serum. Spray with Salamol Eco can not be pierced, disassembled or thrown into the fire, even if it is empty. Like most other inhalants in aerosol packages, Salamol Eco may be less effective at low temperatures. When cooling the cartridge, it is recommended to get it out of the plastic case and warm it with your hands for a few minutes.

Overdosage

Symptoms: nausea, vomiting, irritability, hallucinations, tachycardia, ventricular flutter, dilated peripheral vessels, decreased blood pressure, hypoxemia, acidosis, hypokalemia, hyperglycemia, muscle tremor, headache.
Treatment: drug withdrawal, cardioselective beta-blockers; symptomatic therapy. If overdose is suspected, the level of serum potassium should be monitored.

Studies and clinical trials of Saxagliptin (Click to expand)