saxagliptin

Action and Spectrum

Actions and Spectrum: 

The spectrum of saxagliptin is limited to its effects on blood sugar levels. It is not known to have any significant effects on other bodily systems or functions. 

The actions of saxagliptin include: 

• Increasing insulin secretion: saxagliptin helps to stimulate insulin release from the pancreas, which helps lower blood sugar levels. 
• Decreasing glucagon secretion: saxagliptin helps to decrease glucagon production, a hormone that raises blood sugar levels. 
• Slowing digestion: saxagliptin helps to slow down the rate at which food is broken down and absorbed by the body, which helps to regulate blood sugar levels. 

Drug Interaction

Adverse Reaction

Frequency Defined 

1-10% 

Headache (7%) 

Urinary tract infection (7%) 

Gastroenteritis (2%) 

Infection in upper respiratory tract (3%) 

Hypoglycemia (1.6%) 

Urticaria (<4%) 

Facial edema 

Frequency not Defined 

Increased creatinine phosphokinase 

Thrombocytopenic purpura rash 

Increased creatinine 

Black Box Warning

Contraindication / Caution

Contraindication/Caution: 

saxagliptin is generally a safe medication when used as directed, but there are some situations where it may not be appropriate or caution should be exercised. Some contraindications and cautions of saxagliptin include: 

• Allergy or hypersensitivity: saxagliptin should not be used in individuals with known allergies or hypersensitivity to the medication or its components. 
• Type 1 diabetes: saxagliptin is not indicated for treating type 1 diabetes, as it stimulates insulin secretion, which is not present in individuals with this condition. 
• Severe renal impairment: saxagliptin should be used cautiously in individuals with severe renal impairment, as it is primarily eliminated through the kidneys. Dose adjustment may be necessary for these individuals. 
• Pancreatitis: saxagliptin should be used with caution in individuals with a history of pancreatitis, as it may increase the risk of recurrent episodes. 
• Hypoglycemia: saxagliptin may increase the risk of hypoglycemia (low blood sugar) when combined with other diabetes medications that can cause hypoglycemia. Caution should be exercised in these individuals and dose adjustments may be necessary. 
• Pregnancy and breastfeeding: saxagliptin should only be used during pregnancy or breastfeeding if the potential benefits outweigh the potential risks. There is limited data on the safety of saxagliptin in these populations. 

Pregnancy / Lactation

Pregnancy consideration:  

It is not secure to administer saxagliptin during pregnancy. 

Breastfeeding warnings:  

No data is available about the excretion of saxagliptin in breast milk. Avoid using in lactating women. 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: No evidence of risk to the fetus is found in animal reproduction studies, and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a human product; Pregnant women must take care of the potential risks. 
• Category D: There is adequate data with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergencies for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. The drug is not for pregnant women. 
• Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

saxagliptin is an oral antidiabetic drug that belongs to the class of medications known as dipeptidyl peptidase-4 (DPP-4) inhibitors.  

Inhibition of DPP-4 by saxagliptin results in increased levels of GLP-1 and GIP hormones in the bloodstream, which leads to several pharmacological effects. These include: 

• Stimulating insulin secretion: saxagliptin increases insulin secretion from pancreatic beta cells in response to glucose stimulation, which leads to improved glucose control. 
• Decreasing glucagon secretion: saxagliptin decreases glucagon secretion from pancreatic alpha cells, which lowers the amount of glucose released into the bloodstream. 
• Slowing gastric emptying: saxagliptin slows the rate at which food is emptied from the stomach, which reduces the amount of glucose absorbed after a meal and helps to regulate blood glucose levels. 
• Reducing appetite: saxagliptin may also reduce appetite and food intake, which can help to promote weight loss in some individuals with diabetes. 

Pharmacodynamics: 

• Stimulation of insulin secretion: saxagliptin increases insulin secretion from pancreatic beta cells in response to glucose stimulation, leading to improved glucose control. 
• Reduction of glucagon secretion: saxagliptin reduces the secretion of glucagon from pancreatic alpha cells, which lowers the amount of glucose released into the bloodstream. 
• Regulation of gastric emptying: saxagliptin slows the rate at which food is emptied from the stomach, reducing the amount of glucose absorbed after a meal and helping to regulate blood glucose levels. 
• Reduction of hepatic glucose production: saxagliptin also reduces the amount of glucose produced by the liver, which helps to lower blood glucose levels. 
• Improvement of beta-cell function: saxagliptin has been shown to improve beta-cell function, which leads to increased insulin secretion and improved glycemic control. 
• Cardiovascular effects: saxagliptin has been shown to have cardiovascular benefits, including a reduction in blood pressure, improvement of endothelial function, and a decrease in markers of inflammation. 

Pharmacokinetics: 

Absorption 

The peak plasma concentration is achieved in 2 hours (for saxagliptin) and 4 hours (for 5-hyroxy saxagliptin) 

Distribution 

The volume of distribution is negligible 

Metabolism 

The drug is metabolized by hepatic CYP450 3A4/5 to active metabolites  

Elimination and Excretion 

The half-life (of elimination) is 2.5 hours (for saxagliptin); 3.1 hours (for 5-hydroxy saxagliptin) 

The rate of renal clearance is 7.2 L/hr 

The drug is excreted in urine (75%) and in feces (22%) 

Adminstartion

Administration: 

saxagliptin is typically administered orally in tablet form, with or without food. The usual recommended dose of saxagliptin is 5 mg once daily, which can be increased to 10 mg once daily in some patients who require further glycemic control. 

It is essential to take saxagliptin at the same time each day to maintain consistent blood levels of the medication. If a dose is missed, it should be taken as soon as remembered unless it is close to the next scheduled dose, in which case the missed dose should be skipped, and the regular dosing schedule resumed. 

saxagliptin can be taken alone or in combination with other antidiabetic medications, such as metformin, sulfonylureas, or insulin, depending on the patient’s needs and medical history. However, the dose of sulfonylureas or insulin may need to be reduced when combined with saxagliptin to prevent the risk of hypoglycemia. 

saxagliptin tablets should be swallowed whole with a glass of water and not crushed, chewed, or broken. If a patient has difficulty swallowing the tablet, they should consult their healthcare provider for alternative dosing options. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: saxagliptin 

Pronounced: SAX-a-GLIP-tin  

Why do we use saxagliptin? 

saxagliptin is used in the management of type 2 diabetes mellitus. It works by inhibiting the enzyme dipeptidyl peptidase-4 (DPP-4), which is responsible for the breakdown of incretin hormones such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). This results in an increase in the levels of these hormones, which leads to several pharmacological effects, including 

• Stimulation of insulin secretion: saxagliptin increases insulin secretion from pancreatic beta cells in response to glucose stimulation, improving glucose control. 
• Reduction of glucagon secretion: saxagliptin reduces glucagon secretion from pancreatic alpha cells, which lowers the amount of glucose released into the bloodstream. 
• Regulation of gastric emptying: saxagliptin slows the rate at which food is emptied from the stomach, reducing the amount of glucose absorbed after a meal and helping to regulate blood glucose levels.