dapagliflozin


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dapagliflozin

(dap-a-gli-floe-zin),

Farxiga

(trade name)

Classification

Therapeutic: antidiabetics
Pharmacologic: sodium glucose co transporter 2 sglt2 inhibitors
Pregnancy Category: C

Indications

Adjunct to diet and exercise in the management of type 2 diabetes mellitus.May be used with other antidiabetic agents.

Action

Inhibits proximal renal tubular sodium-glucose co-transporter 2 (SGLT2) which determines reabsorption of glucose from the tubular lumen. Inhibits reabsorption of glucose, lowers renal threshold for glucose and increases excretion of glucose in urine.

Therapeutic effects

Improved glycemic control.

Pharmacokinetics

Absorption: 78% absorbed following oral administration.
Distribution: Unknown.
Metabolism and Excretion: Extensively metabolized by UGT1A9 to inactive metabolites which are primarily excreted in urine. 15% excreted in feces as unchanged drug.
Half-life: 12.9 hr

Time/action profile (decrease in HbA1c)

ROUTEONSETPEAKDURATION
POwithin 4 wk12 wkunknown

Contraindications/Precautions

Contraindicated in: Hypersensitivity;Severe renal impairment/end-stage renal disease/dialysis GRF <60 mL/min/1.73 m2;Type 1 diabetes;Diabetic ketoacidosis;Active bladder cancer; Lactation: Avoid use, discontinue breastfeeding or discontinue dapagliflozin.
Use Cautiously in: eGFR <60 mL/min/1.73 m2 (monitor frequently), ↑ risk of adverse reactions related to ↓ intravascular volume; Geriatric: ↑ risk of adverse reactions related to ↓ intravascular volume; Hypotension (correct prior to treatment, especially if eGFR 30–60 mL/min, age >65 yr, or concurrent use of loop diuretics, ACE inhibitors, or ARBs; History of bladder cancer; Obstetric: Use during pregnancy only if potential maternal benefit justifies potential fetal risk; Pediatric: Safe and effective use in children <18 yr has not been established.

Adverse Reactions/Side Effects

Cardiovascular

  • volume depletion

Genitourinary

  • genital mycotic infections
  • ↑ urination
  • renal impairment

Endocrinologic

  • hypoglycemia (with other medications)

Fluid and Electrolyte

  • hyperphosphatemia

Metabolic

  • hyperlipidemia

Interactions

Drug-Drug interaction

↑ risk of hypotension with antihypertensives or diuretics.↑ risk of hypoglycemia with other antidiabetics (dose adjustments maybe required).renal impairment

Route/Dosage

Oral (Adults) 5 mg once daily, may be increased to 10 mg once daily.

Availability

Tablets: 5 mg, 10 mg

Nursing implications

Nursing assessment

  • Observe for signs and symptoms of hypoglycemic reactions (sweating, hunger, weakness, dizziness, tremor, tachycardia, anxiety), especially in patients taking insulin or other hypoglycemic agents.
  • Monitor BP after initiating and periodically during therapy; may cause hypotension.
  • Lab Test Considerations: Monitor serum glucose and glycosylated hemoglobin periodically during therapy to evaluate effectiveness of treatment.
    • Evaluate renal function prior to starting and periodically during therapy; may cause ↑serum creatinine and ↓ eGFR.
    • May cause ↑ LDL cholesterol.
    • May cause an ↑ hematocrit and serum phosphorous.
    • Will cause urine to test positive for glucose.
  • Overdose is manifested by symptoms of hypoglycemia. Mild hypoglycemia may be treated with administration of oral glucose. Treat severe hypoglycemia with IV D50W followed by continuous IV infusion of more dilute dextrose solution at a rate sufficient to keep serum glucose at approximately 100 mg/dL.

Potential Nursing Diagnoses

Imbalanced nutrition: more than body requirements (Indications)
Noncompliance (Patient/Family Teaching)

Implementation

  • high alert: Accidental administration of oral hypoglycemic agents to non-diabetic adults and children has resulted in serious harm or death. Before administering, confirm that patient has Type 2 diabetes.
  • Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin.
  • Oral: Administer once daily in the morning without regard to food.

Patient/Family Teaching

  • Instruct patient to take medication at same time each day. Take missed doses as soon as remembered unless almost time for next dose; do not double doses. Advise patient to read Medication Guide before starting and with each Rx refill in case of changes.
  • Explain to patient that this medication controls hyperglycemia but does not cure diabetes. Therapy is long term.
  • Inform patient dapagliflozin may cause dehydration and hypotension. Maintain adequate hydration and notify health care professional if dizziness, fainting, weakness or orthostatic hypotension occur.
  • Advise patient to notify health care professional if signs and symptoms of genital mycotic infections; females (vaginal odor, white or yellowish vaginal discharge, vaginal itching), males (rash or redness of glans or foreskin of penis, foul smelling discharge from penis, pain in skin around penis) occur. Instruct patient on treatment options and when to notify health care professional.
  • Review signs of hypoglycemia and hyperglycemia with patient. If hypoglycemia occurs, advise patient to drink a glass of orange juice or ingest 2–3 tsp of sugar, honey, or corn syrup dissolved in water or an appropriate number of glucose tablets and notify health care professional.
  • Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hypoglycemic or hyperglycemic episodes.
  • Instruct patient in proper testing of serum glucose and ketones. These tests should be closely monitored during periods of stress or illness and health care professional notified if significant changes occur.
  • Advise patient to inform health care professional of medication regimen prior to treatment or surgery.
  • Advise patient to notify health care professional promptly if signs and symptoms of hypersensitivity reactions (rash; raised red patches on skin; swelling of face, lips, tongue, throat; difficulty breathing or swallowing) or bladder cancer (blood or red color in urine, painful urination) occur.
  • Insulin is the recommended method of controlling blood sugar during pregnancy. Counsel female patients to use a form of contraception other than oral contraceptives and to notify health care professional promptly if pregnancy is planned or suspected. May cause fetal harm in 2nd or 3rd trimester.
  • Advise patient to carry a form of sugar (sugar packets, candy) and identification describing disease process and medication regimen at all times.
  • Emphasize the importance of routine follow-up exams.

Evaluation/Desired Outcomes

  • Control of blood glucose levels without the appearance of hypoglycemic or hyperglycemic episodes.
References in periodicals archive ?
Some of these approved inhibitors are canagliflozin (sold as Invokana or when combined with another drug Invokarnet), dapagliflozin (Farxiga and Xigduo), and empagliflozin Gardiance and Glyxambi).
AstraZeneca today announced that the US Food and Drug Administration (FDA) has issued a Complete Response Letter (CRL) regarding the New Drug Application (NDA) for the investigational fixed-dose combination of saxagliptin and dapagliflozin for the treatment of adult patients with type 2 diabetes.
FDA is continuing to evaluate the risk of bone fractures with other drugs in the SGLT2 inhibitor class, including dapagliflozin (Farxiga, Xigduo XR) and empagliflozin (Jardiance, Glyxambi, Synjardy), to determine if additional label changes or studies are needed," the FDA stated.
There are six new drugs belonging to the endocrine /metabolic pharmacologic class: albiglutide (Tanzeum), dapagliflozin (Farxiga), dulaglutide (Trulicity), eliglustat (Cerdelga), elosulfase alfa (Vimizim), and empagliflozin (Jardiance).
The new drug, dapagliflozin (branded as Forxiga), just approved for use in England and Wales by the National Institute for Health and Care Excellence (NICE), was tested in a number of hospitals including, in Wales, Morriston Hospital in Swansea.
In final draft guidance, the National Institute for Health and Care Excellence (Nice) recommends the use of dapagliflozin for some people who suffer from the condition.
The National Institute for Health and Care Excellence will announce today it is recommending dapagliflozin for some people who suffer from type 2 diabetes.
Forxiga's active substance is dapagliflozin, which is developed from a naturally-occurring sugar compound found in the bark of apple trees.
Food and Drug Administration for their drugs, as was the case with Bristol-Myers' experimental diabetes product dapagliflozin, which failed to win the seal of approval from the FDA earlier this year.
AstraZeneca was out of favour after the US Food and Drug Administration (FDA) announced that it wants more clinical data on its dapagliflozin treatment for type 2 diabetes in adults to assess the "benefit-risk" profile of the drug.
Bailey CJ, Gross JL, Pieters A, Bastien A, List JF Effect of dapagliflozin in patients with type 2 diabetes who have inadequate glycaemic control with metformin: a randomised, double-blind, placebo-controlled trial.
Patients randomly received either 10 milligrams of experimental drug dapagliflozin per day plus metformin, or 20 milligrams of glipizide per day.