Pharm
Bexagliflozin
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Bexagliflozin
, Brenzavvy
See Also
SGLT2 Inhibitor
Type II Diabetes Medications
Canagliflozin
Dapagliflozin
Empagliflozin
Ertugliflozin
Sotagliflozin
Indications
Type 2 Diabetes Mellitus
Management
Comorbid
Chronic Kidney Disease
or
Microalbuminuria
Comorbid
Congestive Heart Failure
Like
GLP-1 Agonist
s,
SGLT2 Inhibitor
s have moved to first-line agents for their effects on conditions comorbid to Diabetes
SGLT2 Inhibitor
s (as with
GLP-1 Agonist
s) may assist with weight loss in
Obesity
SGLT2 Inhibitor
s (as with
GLP-1 Agonist
s) decrease
Cardiovascular Risk
Best evidence for
Empagliflozin
(
Jardiance
)
SGLT2 Inhibitor
s (as with
GLP-1 Agonist
s) decrease
Chronic Kidney Disease
progression
Best evidence for
Empagliflozin
(
Jardiance
),
Canagliflozin
(
Invokana
),
Dapagliflozin
(
Farxiga
)
Contraindications
Type 1 Diabetes Mellitus
Renal dysfunction (CKD Stage 4 or 5, GFR <30 ml/min)
Other relative contraindications (use with caution)
Diabetic Ketoacidosis
(relative contraindication)
Osteoporosis
or
Osteopenia
(low
Bone Mineral Density
)
Diabetic Foot Wound
(
Neuropathic Foot Ulcer
)
Perioperative status (or prolonged
Fastin
g,
Dehydration
)
Hold for at least 3 to 4 days before major surgery
Mechanism
See
SGLT2 Inhibitor
Sodium-Glucose Transporter 2
(SGLT2)
SGLT2 acts in the
Kidney
s to resorb
Glucose
at the proximal tubules
SGLT2 mediates 90% of renal
Glucose
reabsorption from the tubules
SGLT2 Inhibitor
s
Blocks SGLT2, Allowing more
Glucose
to remain in the urine without reabsorption
Results in osmotic diuresis
Efficacy is lower when GFR is decreased
Medications
Bexagliflozin (Brenzavvy)
Released in 2023 at $50/month (compared with other
SGLT2 Inhibitor
s costing $600/month)
May not be initially covered by insurance, resulting in cost higher than other agent copays
(2023) Presc Lett 30(9): 51
Dosing
AM dosing is recommended due to
Diuretic
effect
Taken 30 minutes before first meal of day
Avoid in
Dehydration
Start 20 mg orally once daily in the morning
Pharmacokinetics
Class Effects
See
SGLT2 Inhibitor
SGLT2 Inhibitor
s share similar
Pharmacokinetics
Rapid absorption and peak activity within 2-4 hours
Teminal
Half-Life
12 hours
Efficacy
Similar efficacy to other agents (lowers Hgb A1c 0.5%)
All
SGLT2 Inhibitor
s have lower efficacy in moderate to severe renal
Impairment
Other beneficial class effects that may occur
Decrease weight 5 lb
May lower weight up to 4 to 7 pounds (mean 5 lb, via diuresis)
May lower
Blood Pressure
by 3-5 mmHg (via similar mechanism to weight)
May decrease
Cardiovascular Risk
May decrease
Chronic Kidney Disease
progression
Low risk of
Hypoglycemia
Adverse Effects
See
SGLT2 Inhibitor
Perioperative Recommendations
See
Preoperative Guidelines for Medications Prior to Surgery
Stop
SGLT2 Inhibitor
s 3 days before surgery (due to
Euglycemic Ketoacidosis
risk)
Restart
SGLT2 Inhibitor
s post-operatively when oral intake returns to normal
Urinary Tract Infection
Genital yeast infection
Number needed to harm (NNH) 17 in women, 40 in men
Fournier's Gangrene
https://www.fda.gov/Drugs/DrugSafety/ucm617360.htm
Euglycemic Ketoacidosis
See
Euglycemic Ketoacidosis
Presents with
Anion Gap Metabolic Acidosis
(
Ketoacidosis
despite normal
Serum Glucose
)
Diuretic
effect
Risk of
Dehydration
,
Orthostatic Hypotension
Risk of
Acute Kidney Injury
(see below)
Acute Kidney Injury
Seen with
Canagliflozin
(
Invokana
) and
Dapagliflozin
(
Farxiga
), but likely a class effect due to diuresis
Higher risk when combined with
ACE Inhibitor
s (and ARBs),
NSAID
s and
Diuretic
s and esp. in elderly
Avoid
Hypovolemia
, and consider lowering
Diuretic
dose when on
SGLT2 Inhibitor
Check
Serum Creatinine
before initiating agent, 10-14 days later and again with dose increase
Stop and hold the SGLT2 Inhibitor
Serum Creatinine
rises >30%
http://www.fda.gov/Drugs/DrugSafety/ucm505860.htm
Hyperkalemia
When used in combination with
ACE Inhibitor
s,
Angiotensin Receptor Blocker
s or
Potassium
Sparing
Diuretic
s
May also decrease
Serum Potassium
LDL Cholesterol
increase (4-8 mg/dl)
Bladder Cancer
increased risk
Associated only with
Farxiga
Fracture
s
Upper extremity
Fracture
s most common (and not caused by major
Trauma
)
Number needed to harm 125 for one additional
Fracture
with
Invokana
over 18 months of use
Invokana
and for those with
Renal Insufficiency
,
Farxiga
, have been associated with increased risk
Unknown mechanism (possibly decreased
Bone Mineral Density
, increased
Fall Risk
)
http://www.fda.gov/Drugs/DrugSafety/ucm461449.htm
Acute Pancreatitis
Amputation Risk
Canagliflozin
associated with increased risk of amputations
Relative Risk
: 2.0 (risk of 6 amputations per 1000 on
Canagliflozin
)
May be a
SGLT2 Inhibitor
class effect (unclear mechanism)
See
Amputation Prevention in Diabetes Mellitus
FDA Drug Safety Communication
https://www.fda.gov/Drugs/DrugSafety/ucm557507.htm
Safety
Avoid in
Lactation
Pregnancy
Unknown safety in first trimester
Avoid in second and third trimester
Monitoring
Renal Function
Resources
Bexagliflozin (DailyMed)
https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=3cdf28fc-4194-4ad6-aa03-c9eaa68da83e
References
(2020) Presc Lett 27(12): 68
(2020) Presc Lett 27(5): 26
(2018) Presc Lett 25(2)
(2016) Presc Lett 23(2): 8-9
(2014) Presc Lett 21(10): 57
(2013) Presc Lett 20(5): 28
Tomaszewski (2022) Crit Dec Emerg Med 36(11): 32
Nisly (2013)Am J Health-Syst Pharm 70 (4):311-9 [PubMed]
Stenlof (2013) Diabetes Obes Metab 15(4): 372-82 [PubMed]
Vaughan (2024) Am Fam Physician 109(4): 333-42 [PubMed]
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