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Toronto Notes 2019 Common Medications Endocrinology E51
Diabetes Medications (continued)
Drug Class
Mechanism of Action
Generic Drug Name
Canada Name
US Name (if different)
Dosing
Indications
Contraindications
Side Effects
Comments
Sodium- glucose linked transporter 2 (SGLT2) Inhibitor
Enhances urinary glucose excretion by inhibiting glucose reabsorption in the proximal renal tubule
canagliflozin dapagliflozin
Invokana® Forxiga®
100 mg OD before first meal of the day
ABSOLUTE:
Severe renal impairment ESRD
Patients on dialysis
UTI, genital infections
Hypotension caution with concomitant loop diuretic use
Caution with renal dysfunction Hyperlipidemia (raises LDL and HDL) Dapagliflozin not to be used in patients with active or history of bladder cancer Rare diabetic ketoacidosis (may occur with no hyperglycemia)
HbA1c 0.7-1.0%
Negligible risk of hypoglycemia as
Sodium- glucose linked transporter 2 (SGLT2) Inhibitor
Enhances urinary glucose excretion by inhibiting glucose reabsorption in the proximal renal tubule
canagliflozin dapagliflozin
Invokana® Forxiga®
100 mg OD before first meal of the day
ABSOLUTE:
Severe renal impairment ESRD
Patients on dialysis
UTI, genital infections
Hypotension caution with concomitant loop diuretic use
Caution with renal dysfunction Hyperlipidemia (raises LDL and HDL) Dapagliflozin not to be used in patients with active or history of bladder cancer Rare diabetic ketoacidosis (may occur with no hyperglycemia)
HbA1c 0.7-1.0%
Negligible risk of hypoglycemia as
Dyslipidemia Medications
Drug Class
Mechanism of Action
Generic Drug Name
Canada Name
US Name (if different)
Dosing
Indications
Contraindications
Side Effects
HMG-CoA Reductase Inhibitor (statins)
Inhibits cholesterol biosynthesis,  LDL synthesis,  LDL clearance, modest  HDL, limitedVLDL
atorvastatin fluvastatin lovastatin pravastatin rosuvastatin simvastatin
Lipitor® Lescol® Mevacor® Pravachol® Crestor® Zocor®
10-80 mg/d 20-80 mg/d 20-80 mg/d 10-40 mg/d 5-40 mg/d 10-80 mg/d
1st line monotherapy Used for  LDL,  TG
Active liver disease
liver enzymes
Myositis ( risk if combined with fibrates) Rhabdomyolysis
Fibrates
Activate PPAR α Upregulate lipoprotein lipase + apo A1,  VLDL,  TG, modest  LDL, modest HDL
bezafibrate fenofibrate gemfibrozil
Bezalip® Lipidil® Lopid®
400 mg/d 48-200 mg/d 600-1200 mg/d
Used for  TG, hyperchylomicronemia
Hepatic disease Renal disease
GI upset
Skin rashes
 risk of gallstone formation
risk of rhabdomyolysis when combined with statins
Niacin
Inhibits secretion of hepatic VLDL via lipoprotein lipase (LPL) pathwaygdecreased VLDL and LDL; decreased clearance of HDL
nicotinic acid
Niaspan® generic niacin
Niacor®
0.5-2 g/d
Used for severe hypertriglyceridemia not controlled by fibrate
Hypersensitivity Hepatic dysfunction Active PUD Hyperuricemia Severe hypotension
Generalized flushing Abnormal liver enzymes Pruritus
IGT
Bile Acid Sequestrants
Resins that bind bile acids in intestinal lumen and prevent absorption thereby
LDL
cholestyramine
Questran®
2-24 g/d
Used for  LDL
Use as adjunct with statins or fibrates
Complete biliary obstruction TG >3.5 mmol/L
Constipation, nausea Flatulence
Bloating
Rise in TG
Cholesterol Absorption Inhibitors
Inhibitscholesterolabsorptionat thesmall intestine brush border
Zetia®
Used for  LDL
Hypersensitivity
Hepatic dysfunction (when used with statin) Do not combine with fibrates or bile acid resins
Fatigue Pharyngitis Sinusitis Abdominal pain Diarrhea Arthralgia
Anti-PCSK9
Inhibits degradation of the LDL receptor by PCSK9 enzyme
LDL clearance
evolocumab alirocumab
Repatha® Praluent®
140mg q2w or 420mg qmonthly
Add-on to maximally tolerated statin therapy in heterozygous FH (evolocumab, alirocumab) and homozygous FH (evolocumab)
Consider in patients with atherosclerotic CVD and LDL-C not at target despite maximally tolerated statin ±ezetimibe
Hypersensitivity
No studies regarding use in severe hepatic or renal impairment
Nasopharyngitis, URTI, influenza Sinusitis
Back pain
Myalgia
empagliflozin
Jardiance®
10 mg OD in the morning with or without food
empagliflozin
Jardiance®
10 mg OD in the morning with or without food
colestipol ezetimibe
Colestid® Ezetrol®
5-30 g/d 10 mg/d
Binds other medications
5 mg OD in the morning with or without food
monotherapy Cause weight loss
5 mg OD in the morning with or without food
monotherapy Cause weight loss
75mg q2w or 300mg qmo
Arthralgia Nausea
Watch glucose control with overt DM