Dapagliflozin

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Dapagliflozin.jpg

[edit] MECHANISM OF ACTION

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 lowers the renal threshold for glucose, and thereby increases urinary glucose excretion

[edit] INDICATIONS

Dapagliflozin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Dapagliflozin is not recommended in patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis.

[edit] DOSAGE

  • The recommended starting dose is 5 mg once daily, taken in the morning, with or without food.
  • Dose can be increased to 10 mg once daily in patients tolerating Dapagliflozin who require additional glycemic control.
  • Assess renal function before initiating Dapagliflozin. Do not initiate Dapagliflozin if eGFR is below 60 mL/min/1.73 m2.
  • Discontinue Dapagliflozin if eGFR falls persistently below 60 mL/min/1.73 m2.

[edit] CONTRAINDICATIONS

History of serious hypersensitivity reaction to Dapagliflozin. Severe renal impairment, end-stage renal disease, or dialysis.

[edit] WARNINGS AND PRECAUTIONS

  • Hypotension: Before initiating Dapagliflozin, assess volume status and correct hypovolemia in elderly, in patients with renal impairment or low systolic blood pressure, and in patients on diuretics. Monitor for signs and symtoms during therapy.
  • Impairment in renal function: Monitor renal function during therapy.
  • Hypoglycemia: In patients taking insulin or an insulin secretagogue with Dapagliflozin, consider a lower dose of insulin or the insulin secretagogue to reduce the risk of hypoglycemia.
  • Genital mycotic infections: Monitor and treat if indicated.
  • Increased LDL-C: Monitor and treat per standard of care.
  • Bladder Cancer: An imbalance in bladder cancers was observed in clinical trials. Dapagliflozin should not be used in patients with active bladder cancer and should be used with caution in patients with a prior history of bladder cancer.
  • Macrovascular outcomes: There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with Dapagliflozin or any other antidiabetic drug.

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US): There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • Nursing Mothers: Discontinue Dapagliflozin or discontinue nursing

[edit] SIDE EFFECTS

The most common adverse reactions associated with Dapagliflozin (5% or greater incidence) were female genital mycotic infections, nasopharyngitis, and urinary tract infections.

[edit] RELATED LINKS


Understanding Type 2 Diabetes
A simple explanation of what diabetes is

[edit] BIBLIOGRAPHY

http://www1.astrazeneca-us.com/pi/pi_farxiga.pdf (Revised: 1/2014)

[edit] REFERENCES

Diabetes (Antidiabetic drugs)
Insulin Secretagogues (drugs that increase insulin release from pancreas) Sulfonylureas Chlorpropamide (Diabinese)   Glibenclamide or Glyburide (Diabeta, Micronase, Glynase, Daonil, Euglycon)   Gliclazide (Diamicron)   Glimepiride (Amaryl, Solosa)   Glipizide (Glucotrol, Minidiab, Glibenese)   Gliquidone (Glurenorm)
Meglitinides Repaglinide (Prandin, Novonorm)   Nateglinide (Starlix)
Dipeptidyl peptidase-4 inhibitors Linagliptin (Trajenta)   Saxagliptin (Onglyza)   Sitagliptin (Januvia)   Vildagliptin (Galvus)
Incretin mimetics (GLP-1 agonists and analogs) Exenatide (Byetta)   Liraglutide (Victoza)   Lixisenatide (Lyxumia)   Dulaglutide (Trulicity)
Insulin Sensitizers (drugs that decrease insulin resistance)
Biguanides Metformin (Glucophage)
Thiazolidinediones Pioglitazone (Actos)
Drugs that retard the digestion and absorption of carbohydrates in the small intestine
Alpha-glucosidase inhibitors Acarbose (Glucobay, Precose)
Drugs that reduce glucose absorption in the kidney and increase glucose excretion in the urine
Sodium glucose cotransporter 2 (SGLT2) inhibitors Canagliflozin (Invokana)   Dapagliflozin (Farxiga)   Empagliflozin (Jardiance, Glyxambi, Synjardi)
Insulin and insulin analogs
Intermediate acting insulins Insulin lispro protamine (Humalog BASAL)   Isophane human insulin : Human insulin protamine (NPH) (Humulin I, Protaphane)
Long-acting insulins‎ Insulin detemir (Levemir)   Insulin glargine (Lantus)
Fast-acting insulins‎ Regular insulin : Insulin (Human recombinant) (Actrapid, Humulin R)
Ultra-rapid-acting insulins‎‎ Insulin aspart (Novorapid)   Insulin glulisine (Apidra)   Insulin lispro (Humalog)   Insulin human (Inhalation Powder) (Afrezza)
Premixed insulin‎‎‎ (ultra-rapid-acting + intermediate acting Insulin aspart / Insulin aspart protamine (Novomix)   Insulin lispro / Insulin lispro protamine (Humalog Mix)
Inhaled Insulin Insulin human (Inhalation Powder) (Afrezza)
Combination therapy
Sulfonylurea + Metformin Glibenclamide / Metformin (Bieuglicon M, Diaglimet, Glibomet, Gliconorm, Glicorest, Suguan M)
Thiazolidinedione + Metformin Pioglitazone / Metformin (Competact, Glubrava)
Thiazolidinedione + Sulfonylurea Pioglitazone / Glimepiride (Tandemact)
Dipeptidyl peptidase-4 inhibitors + Metformin Linagliptin / Metformin (Jentadueto)   Sitagliptin / Metformin (Efficib, Janumet, Velmetia)   Vildagliptin / Metformin (Eucreas)