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- Mechanism of Action
- Pharmacodynamics
- Pharmacokinetics
- Specific Populations
- Drug Interactions
- Glycemic Control in Patients with Type 2 Diabetes Mellitus
- Cardiovascular Outcomes in Patients with Type 2 Diabetes Mellitus
- Chronic Kidney Disease
- Heart Failure
Sodium-glucose cotransporter 2 (SGLT2), expressed in the proximal renal tubules, is responsible for the majority of the reabsorption of filtered glucose from the tubular lumen. Dapagliflozin is an inhibitor of SGLT2. By inhibiting SGLT2, dapagliflozin reduces reabsorption of filtered glucose and thereby promotes urinary glucose excretion. Dapaglifl...
Increases in the amount of glucose excreted in the urine were observed in healthy subjects and in patients with type 2 diabetes mellitus following the administration of dapagliflozin (see Figure 1). Dapagliflozin doses of 5 or 10 mg per day in patients with type 2 diabetes mellitus for 12 weeks resulted in excretion of approximately 70 grams of glu...
Following oral administration of dapagliflozin, the maximum plasma concentration (Cmax) is usually attained within 2 hours under fasting state. The Cmax and AUC values increase dose proportionally with increase in dapagliflozin dose in the therapeutic dose range. The absolute oral bioavailability of dapagliflozin following the administration of a 1...
At steady-state (20 mg once daily dapagliflozin for 7 days), patients with type 2 diabetes with mild, moderate, or severe renal impairment (as determined by eGFR) had geometric mean systemic exposures of dapagliflozin that were 45%, 100%, and 200% higher, respectively, as compared to patients with type 2 diabetes mellitus with normal renal function...
In in vitrostudies, dapagliflozin and dapagliflozin 3-O-glucuronide neither inhibited CYP 1A2, 2C9, 2C19, 2D6, or 3A4, nor induced CYP 1A2, 2B6, or 3A4. Dapagliflozin is a weak substrate of the Pglycoprotein (P-gp) active transporter, and dapagliflozin 3-O-glucuronide is a substrate for the OAT3 active transporter. Dapagliflozin or dapagliflozin 3-...
FARXIGA has been studied as monotherapy, in combination with metformin, pioglitazone, sulfonylurea (glimepiride), sitagliptin (with or without metformin), metformin plus a sulfonylurea, or insulin (with or without other oral antidiabetic therapy), compared to a sulfonylurea (glipizide), and in combination with a GLP-1 receptor agonist (exenatide ex...
Dapagliflozin Effect on Cardiovascular Events (DECLARE, NCT01730534) was an international, multicenter, randomized, double-blind, placebo-controlled, clinical study conducted to determine the effect of FARXIGA relative to placebo on cardiovascular (CV) outcomes when added to current background therapy. All patients had type 2 diabetes mellitus and ...
The Study to Evaluate the Effect of Dapagliflozin on Renal Outcomes and Cardiovascular Mortality in Patients with Chronic Kidney Disease (DAPA-CKD, NCT03036150) was an international, multicenter, randomized, double-blind, placebo-controlled study in patients with chronic kidney disease (CKD) (eGFR between 25 and 75 mL/min/1.73 m2) and albuminuria (...
The efficacy and safety of FARXIGA 10 mg were assessed independently in two Phase 3 studies in patients with heart failure. Dapagliflozin And Prevention of Adverse outcomes in Heart Failure (DAPA-HF, NCT03036124) was an international, multicenter, randomized, double-blind, placebo-controlled study in patients with heart failure (New York Heart Asso...
2022年5月16日 · What Is Norvasc? Norvasc (amlodipine) is a calcium channel blocker (CCB) prescribed for the prevention and treatment of heart pain or chest pain from angina, and for the treatment of high blood pressure. Norvasc is available as a generic drug. What Are Side Effects of Norvasc? Common side effects of Norvasc include: headache,
2022年10月3日 · Plavix (clopidogrel bisulfate) is a thienopyridine class of drug that inhibits platelet aggregation and thus inhibits aspects of blood clotting used to treat patients with acute coronary syndrome, myocardial infarction (MI), peripheral vascular disease and some stroke (ischemic type) patients. Plavix is available in generic form.
2024年4月26日 · Lipitor ( atorvastatin) is a statin used for the treatment of elevated total cholesterol, LDL, triglycerides, and to elevate HDL cholesterol. What Are Side Effects of Lipitor? Lipitor may cause serious side effects including: pain or burning when you urinate, upper stomach pain, weakness, feeling tired, loss of appetite, dark urine,
2024年2月20日 · Januvia ( sitagliptin) is an oral diabetes medicine for people with type 2 diabetes (non- insulin -dependent) diabetes. Januvia is sometimes used in combination with other diabetes medications, but is not for treating type 1 diabetes. What Are Side Effects of Januvia? Many people using Januvia do not have serious side effects.
2023年5月15日 · What Is Singulair? Singulair (montelukast) is a leukotriene receptor antagonist drug used in the treatment of asthma and allergic rhinitis. Singulair is also indicated for prevention of exercise-induced narrowing of the airways. What Are Side Effects of Singulair? Singulair may cause serious side effects including:
