Names and pronunciation
(kan′a-gli-floe′zin) Invokana
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Drug reference
(kan′a-gli-floe′zin) Invokana
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Func. class.: Oral antidiabetic
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Chem. class.: Sodium-glucose co- transporter 2 (SGLT2) inhibitor
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ACTION: Blocks glucose reabsorption by the kidney, increases glucose excretion, lowers blood glucose concentrations by inhibiting proximal renal tubular sodium glucose transporter 2 (SGLT2)
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USES: Type 2 diabetes mellitus, with diet and exercise; may use in combination; to reduce CV events in type 2 diabetes mellitus with CV disease
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CONTRAINDICATIONS: Dialysis, renal failure, hypersensitivity, breastfeed- ing, diabetic ketoacidosis Precautions: Pregnancy, children, renal/ hepatic disease, hypothyroidism, hypergly- cemia, hypotension, pituitary insufficiency, type 1 diabetes mellitus, malnutrition, fever, dehydration, adrenal insufficiency, geriat- ric patients
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Black Box Warning: Lower limb amputation Black Box Warning: Lower limb am- putation: Increased risk of amputation; monitor wound and feet closely for com- plications, provide foot care C • Monitor electrolytes, LDL, cholesterol and correct as needed • Fungal infections: usually in those with other infections • Pregnancy/breastfeeding: identify whether pregnancy is planned or sus- pected or if breastfeeding, use only if clearly needed not to use in second/third trimester, do not breastfeed Black Box Warning: Lower limb ampu- tation risk: Inspect feet; monitor for new ulcerations, wounds; educate about foot care, to report injury to limbs, sores • Ketoacidosis: to notify prescriber immediately of nausea, vomiting, lack of appetite, sleepiness, difficulty breathing • Yeast infections (women/men): That yeast infections can occur with this prod- uct (women, vaginal; men, penile); to report discharge, itching, swelling • UTI: to report immediately burning, pain on urination, hematuria, back pain, decreased urine • Pregnancy/breastfeeding: Not to breastfeed; to advise prescriber if preg- nancy is planned or suspected
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SIDE EFFECTS CV: Hypotension, orthostatic hypotension GI: Pancreatitis, nausea, vomiting dehydration GU: Cystitis, candidiasis, urinary fre- quency, polydipsia, polyuria, renal impair- ment UTI, genital fungal infections INTEG: Photosensitivity, rash, pruritus META: Hypercholesterolemia, lipidemia, hypoglycemia, hyperkalemia, hypermag- nesemia, hyperphosphatemia, hypersen- sitivity, ketoacidosis MISC: Bone fractures
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INTERACTIONS Increase: hypoglycemia—sulfonylureas, insulin, MAOIs, salicylates, fibric acid derivatives, bile acid sequestrants, ACE inhibitors, angiotensin II receptor antag- onists, beta-blockers, SSRIs; monitor for hypoglycemia, monitor blood glucose closely, dosage may need to be decreased Increase: hyperkalemia—potassium- sparing diuretics, ACE inhibitors, ARBs, monitor potassium regularly Increase or decrease: glycemic control— androgens, lithium, bortezomib, quino- lones; monitor for glycemic control Decrease: effect hyperglycemia— digestive enzymes, intestinal absorbents, thiazide diuretics, loop diuretics, cortico- steroids, estrogen, progestins, oral contra- ceptives, sympathomimetics, isoniazid, phenothiazines; protease inhibitors, atypi- cal antipsychotics, carbonic anhydrase inhibitors, cycloSPORINE, tacrolimus, baclofen, UGT inducers (PHENobarbital, phenytoin, rifAMPin, ritonavir); dose may need to be increased based on eGFR Drug/Lab Increase: urine glucose, potassium, lipids, cholesterol, magnesium phosphate, uric acid, serum creatinine Decrease: serum glucose, eGFR Drug/Herb Decrease: canagliflozin level—St. John’s wort
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DOSAGE AND ROUTES Type 2 diabetes mellitus with diet and exercise • Adult: PO 100 mg/day, may increase to 300 mg/day if needed Reduction of CV Risk in diabetes mellitus and to reduce risk of ESKD, doubling of serum creati- nine, reduction of HF in hospitalizations, CV death in diabetic neuropathy with albu- minuria ≥ 300 mg/day • Adult: PO 100 mg daily in AM before meal, may increase to 300 mg/day if needed Renal dose • Adult: PO eGFR 30-59 mL/min/1.73 m2, max 100 mg/day; <30 mL/min/1.73 m2 do not use
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Available forms: Tablets 100, 300 mg
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Administer: PO route • Once daily with first meal of the day • Correct volume depletion prior to use • Adjust dose in times of stress, surgery, trauma • Store at room temperature
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Assess: • Hypoglycemia (weakness, hunger, dizziness, tremors, anxiety, tachycardia, sweating), hyperglycemia; even though product does not cause hypoglycemia, if patient is on sulfonylureas or insulin, hypoglycemia may be additive; if hypogly- cemia occurs, treat with dextrose, or, if severe, with IV glucagon • Ketoacidosis: monitor for increased ketone levels; may occur with any glucose level, more common in those with severe illnesses • Necrotizing fasciitis (perineum): requires immediate surgery • Volume depletion: monitor for ortho- static hypotension, weakness, dizziness; may occur after beginning treatment; correct volume depletion before starting treatment • For stress, surgery, or other trauma that may require a change in dose • A1c q3mo; monitor serum glucose 1 hr PP throughout treatment; serum cholesterol, serum creatinine/BUN, serum electrolytes • Hyperkalemia (renal disease): moni- tor potassium closely • Bone fractures: monitor bone density, other conditions that may lead to bone fractures; fractures may occur within 3 mo of starting therapy • Renal impairment: monitor more fre- quently in those with renal disease; in- creased creatinine, eGFR may be decreased; BUN may occur
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Evaluate: • Therapeutic response: improved signs/ symptoms of diabetes mellitus (decreased polyuria, polydipsia, polyphagia); clear sensorium, absence of dizziness, stable gait
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • The symptoms of hypo/hyperglycemia, what to do about each • That medication must be taken as prescribed; explain consequences of discontinuing abruptly; that insulin may need to be used for stress, includ- ing trauma, fever, surgery, to take as soon as remembered if dose is missed unless close to next dose, then skip and take at next scheduled dose, do not double • To avoid OTC medications and herbal supplements unless discussed with health care professional • That diabetes is a lifelong illness; that the diet and exercise regimen must be followed; that this product is not a cure • To carry emergency ID and glucose source • That blood glucose monitoring is required to assess product effect • Renal injury: edema in extremities decreased, dark urine, seek care im- mediately • Necrotizing fasciitis: signs/symptoms of high temperature, genital swelling, pain, redness, seek care immediately • Hypersensitivity: to notify prescriber immediately of itching, hives, rash, swell- ing of face/lips
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PHARMACOKINETICS 99% protein binding, metabolized by UGT1A9, UGT2B4, excreted 33% in urine, peak 1-2 hr, half-life 10.6-13 hr depending on dose
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• Adult: PO 100 mg/day, may increase to 300 mg/day if needed Reduction of CV Risk in diabetes mellitus and to reduce risk of ESKD, doubling of serum creati- nine, reduction of HF in hospitalizations, CV death in diabetic neuropathy with albu- minuria ≥ 300 mg/day
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• Adult: PO 100 mg daily in AM before meal, may increase to 300 mg/day if needed Renal dose
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• Adult: PO eGFR 30-59 mL/min/1.73 m2, max 100 mg/day; <30 mL/min/1.73 m2 do not use
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