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Diabetes Medications

Classification Index
Diabetes Medications

Diabetes Medications

Oral Agents to Treat Type 2 Diabetes *

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Agent Class Primary Action Typical Dosage Side Effects Precautions Critical Tests Comments
Tolbutamide (Ornase TM)

Tolazamide (Tolinase TM)

Chlorpropamide (Diabenese TM)
Sulfonylureas (1st generation) Increases insulin production in pancreas Tolbutamide: 0.25–2.0 g/day in divided doses; maximum, 3 g/day Tolazamide: 100–1,000 mg/day in divided doses; maximum, 1 g/day Chlorpropamide: 100–500 mg/day twice a day; maximum, 750 mg/day Hypoglycemia, weight gain, hyperinsulinemia Disulfiram reaction with alcohol Chlorpropamide remains active for up to 60 hours. Use extreme caution with elderly patients or patients with hepatic or renal impairment. Metabolized in liver. Periodic evaluation of liver function tests. Use of these agents is not recommended unless the patient has a well-established history of taking them. Second-generation sulfonylureas provide more predictable results with fewer side effects and more convenient dosing.
Glyburide (Micronase TM, Diabeta TM, Glynase TM) glipizide (Glucotrol, Glucotrol XL TM), glimepiride (Amaryl TM) Sulfonylureas (2nd generation) Increases insulin production in pancreas Glyburide: 1.25–2.50 mg/day twice a day; maximum 29 mg/day Glynase: 0.75–12.0 mg/day; maximum 20 mg/day Glipizide: 2.5–20.0 mg/day twice a day; Maximum, 40 mg/day; or XL* 2.5–10.0 mg/day twice a day; maximum, 20 mg/day Glimepiride: 1–8 mg/day; maximum, 8 mg/day Hypoglycemia, weight gain, hyperinsulinemia Clearance may be diminished in patients with hepatic or renal impairment. Metabolized in liver.Periodic evaluation of liver function tests. Glipizide is preferred with renal impairment. Doses >15 mg should be split.
Repaglinide (Prandin TM) Meglitinide Increases insulin release from pancreas New diagnosis or HbAlc <8% 0.5 mg before meals 2–4 times a day HbA1c >8: 1–2 mg, 15–30 min after each meal; increase weekly until results are obtained; maximum, 16 mg/day Hypoglycemia, weight gain, hyperinsulinemia Should not be used in patients with diabetic ketoacidosis and known hypersensitivity to drug or its inactive ingredients. Metabolized in liver.Periodic evaluation of liver function tests. Patients should be instructed to take medication ≤30 min before a meal. If meals are skipped or added, medication should be skipped or added as well.
Nateglinide (Starlix TM) Phenylalanine derivative Increases insulin release from pancreas 120, or 60 mg 3 times a day before meals Hypoglycemia, weight gain, hyperinsulinemia Should not be used in patients with diabetic ketoacidosis and known hypersensitivity to drug or its inactive ingredients. Metabolized in liver.Periodic evaluation of liver function tests. Patients should be instructed to take medication ≤30 min before a meal. If meals are skipped or added, medication should be skipped or added as well. Nateglinide is approved only as monotherapy or in combination with Metformin.
Metformin (Glucophage TM) Biguanide Increases insulin sensitivity 500 mg/day twice a day with meals increase by 500 mg every 1–3 wk, twice or three times a day; usually most effective at 2,000 mg/day; maximum, 2,550 mg/day Nausea, diarrhea, metallic taste, very rare lactic acidosis Should not be used in patients who use alcohol frequently, liver, kidney disease or CHF because of risk of lactic acidosis. Contraindicated if serum creatinine is: >1.5 mg/dL in men or >1.4 mg/dL women, or use if creatinine clearance is abnormal. Monitor hematological and renal function annually. Metformin is especially beneficial in obese patients due to potential for weight loss, improved lipid profile, and lack of potential for hypoglycemia requiring supplemental carbohydrate intake. Discontinue for 48 hr after procedure using contrast dye.
Rosiglitazone (Avandia TM) Thiazolidinedione Increases insulin sensitivity 4 mg/day in single or divided doses Increase to 8 mg/day in 12 wk, if needed; maximum, 8 mg/day with or without food Weight gain, fluid retention, edema Should not be used in patients with CHF or hepatic disease. Can cause mild-to-moderate edema. Avoid initiation with patients with increased baseline liver enzyme levels (ALT >2.5 times upper limit of normal). Liver enzymes monitored every 2 months for 12 months, then periodically. If ALT levels increase to >3 times the upper limit of normal, discontinue use and recheck liver enzyme levels. Rosiglitazone is approved for use as monotherapy and in combination with metformin or sulfonylureas.
Pioglitazone (Actos TM) Thiazolidinedione Increases insulin sensitivity 15 or 30 mg/day; Maximum with or without food 45 mg for monotherapy 30 mg for combination therapy Weight gain, fluid retention, edema Clearance may be diminished in patients with hepatic or renal impairment. Avoid initiation with patients who have liver disease or ALT levels >2.5 times the upper limit of normal. Patients with mildly elevated liver enzymes (ALT levels 1–2.5 times the upper limit of normal) should be evaluated. Discontinue if >3 times the upper limit of normal. Pioglitazone is approved for use as monotherapy or with metformin, sulfonylureas, or insulin.
Acarbose (Precose TM) Miglitol (Glyset TM) Alpha-glucosidase inhibitor Blocks gut absorption of complex sugars 25 mg/day; increase by 25 mg/day every 4–6 wk; maximum, split dose before meals with first bite of food 300 mg/day (150 mg/day for weight <60 kg) Gas and bloating, sometimes diarrhea for both drugs Should not be used if GI disorders are concurrent. Avoid if serum creatinine is >2.0 mg/dL. Monitor serum transaminase every 3 months for 1st year of therapy.  
Combinations
Glucovance TM glyburide and metformin Decreases hepatic glucose production and increases insulin secretion. Initial, 1.25 mg/250 mg once or twice a day with meals; increase every 2 wk by 1.25 mg/250 mg per day; 2nd line, 2.5mg/500 mg or 5 mg glyburide/ 500 mg twice a day with meals; maximum, 20 mg/2000 mg per day Possible hypoglycemia, nausea, diarrhea, abdominal pain for this combination drug Should not be used if frequent alcohol use, liver or kidney disease, or CHF is suspected. Contraindicated if serum creatinine is >1.5 mg/dL in men or 1.4 mg/dL in women, or if creatinine clearance is abnormal. Monitor hematological and renal function annually. May use 1.25mg/250mg and 2.5mg/500mg doses at different times of day for best glucose control. Incidence of hypoglycemia is higher for combination than for single agent use.
Metaglip TM glipizide and metformin Decreases hepatic glucose production and increases insulin secretion Initial, 2.5 mg/250 mg once or twice a day with meals. Increase every 2 wk to maximum of 10 mg/1000 mg or 10 mg/2000 mg per day. 2nd line, 2.5 mg/500 mg or 5 mg/500 mg twice a day with meals. Maximum, 20 mg/2000 mg per day Diarrhea, nausea/ vomiting, headache for this combination drug Should not be used if frequent alcohol use, liver or kidney disease, or CHF is suspected. Contraindicated if serum creatinine is >1.5 mg/dL in men, or >1.4 mg/dL in women, or if creatinine clearance <60–75 mL/min. Monitor hematologic and renal function annuallys. May use 1.25mg/250mg and 2.5mg/500mg doses at different times of day for best glucose control. Incidence of hypoglycemia is higher for combination than for single agent use.
Avandamet TM rosiglitazone and metformin Decreases hepatic glucose production, increases glucose uptake, and decreases insulin resistance 1 mg/500 mg, 2 mg/500 mg or 4 mg/500 mg twice a day; dosage individualized based on current therapy. Maximum, 8 mg/2000mg per day Diarrhea, edema, anemia for this combination drug Should be avoided in patients with hepatic disease, CHF, renal disease. Contraindicated if serum creatinine is >1.5 mg/dL in men or >1.4 mg/dL in women, or if creatinin clearance is abnormal. Agent is less expensive than its components separately. Decrease in GI upset is reported with metformin compared with rosiglitazone alone.
*Agents in a class of medicines share mechanisms of action, require similar precautions, and generally have similar side effects. For proper usage, please read label. Agents should not be used in patients with type 1 diabetes.


Important Insulin Information *

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Insulin Onset Peak Effective Duration Maximal Duration Comments
Human
Lispro (humalog) <15 min 1–2 hr 2–4 hr 3–5 hr Must be taken just before or immediately after eating.
Aspart (novalog) <15 min 1–3 hr 3–5 hr 4–6 hr
Regular 0.5–1 hr 2–4 hr 3–5 hr 4–8 hr Best if administered 30 min before meal.
NPH 2–4 hr 4–10 hr 10–16 hr 14–18 hr  
Lente 3–4 hr 4–12 hr 12–18 hr 16–20 hr Frequently used instead of NPH in children.
Ultralente 6–10 hr Minimal 18–20 hr 20–30 hr  
70/30 0.5–1 hr 2–10 hr 10–16 hr 14–18 hr  
Humalog mix 75/25 <15 min 1–2 hr 10–16 hr 14–18 hr Must be taken before or immediately after eating.
Insulin glargine (Lantus TM) 4–6 hr None 24 hr 24 hr Administered at bedtime once a day. Cannot be mixed in same syringe and should not be given with use of same needle in same place as previous injection.
Animal Source
Regular 0.5–2 hr 3–4 hr 4–6 hr 6–8 hr Change over to human insulin recommended. Dose changes required; consult physician.
NPH 4–6 hr 8–14 hr 16–20 hr 20–24 hr
Lente 4–6 hr 8–14 hr 16–20 hr 20–24 hr
*Site rotation for injections is necessary for all types of insulin.


Recommended Insulin Storage

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Recommended Insulin Storage Refrigerated (36°F–46°F) Room Temperature (59°F–86°F)
VIAL Opened Unopened Opened Unopened
Humalog, novolog, humulin, novolin 28 days until expiration date 28 days 28 days
Novalog (release pending)   until expiration date    
Lantus TM (10 mL) 28 days until expiration date 28 days 28 days
Lantus TM (5 mL) 28 days until expiration date 14 days 14 days
PENS/CARTRIDGES Not in use In use
Humalog Until expiration date 28 days
Humulin R (cartridge) Until expiration date 28 days
Humulin N Until expiration date 14 days
Humulin 70/30 Until expiration date 10 days
Humalog Mix 75/25 Until expiration date 10 days
Novolog Until expiration date 28 days
Novolin R (prefilled and 1.5-mL cartridge) Until expiration date 30 days
Novolin R (3-mL cartridge) Until expiration date 28 days
Novolin N (prefilled and 1.5-mL cartridge) Until expiration date 7 days
Novolin N (3-mL cartridge) Until expiration date 14 days
Novolin 70/30 (prefilled and 1.5-mL cartridge) Until expiration date 7 days
Novolin 70/30 (3-mL cartridge) Until expiration date 10 days
Lantus TM Until expiration date 28 days
Self-filled syringes 14 days* 7 days*
*Suggested, not clinically established


Glucose Lowering Activity-Oral Diabetes Agent

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Medication Blood Glucose Most Affected SMBG* Testing to Recommend Greatest Risk for Hypoglycemia
Sulfonylureas Fasting and postprandial 2–3 times per day,especially fasting 4–6 hr after meal and fasting
Meglitinide phenylalanine derivative Postprandial 2 hr after meal 2–3 hr after meal
Biguanide Fasting Fasting None if used as single agent
Alpha-glucosidase inhibitor Postprandial 2 hr after meal 2 hr after meal
Thiazolidinedione Fasting and postprandial 2–3 times per day, especially fasting After exercise when used with sulfonylureas or insulin
Glucovance Fasting and postprandial 2–3 times per day, especially fasting 4–6 hr after meal and fasting
SMBG = self-monitoring of blood glucose


Measures to Control Glycemia

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Biochemical Index Normal Goal Action Suggested
Before meals (mg/dL)
plasma whole blood
<110
<100
90–130
80–120
<90, >150
<80, >140
Bedtime (mg/dL)
plasma whole blood
<120
<110
110–150
100–140
<110, >180
<100, >160
HbA1c* <6 <7 >8
HbA1c = glycated hemoglobin


Medications to Treat High Blood Cholesterol

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Category Brand Name Generic Name Manufacturer Minimum Daily Dose Maximum Daily Dose Special Considerations*
HMG-CoA reductase inhibitors (statins)
Lipitor atorvastatin Pfizer 10 mg 80 mg Main action: Lowers LDL ("bad") cholesterol.
Have blood tests for liver enzyme concentrations.
Notify physician immediately of muscle pain.
Use caution if combining with fibric acid derivatives or bile acid sequestrants (described below).
(increased risk of rhabdomyolysis)
Lescol fluvastatin Novartis 20 mg 80 mg
Lescol XL fluvastatin Novartis 80 mg 80 mg
Mevacor lovastatin Merck 10 mg 80 mg
  lovastatin generic† 10 mg 80 mg
Altocor lovastatin (extended-release) Aura Labs 20 mg 60 mg
Pravachol pravastatin Bristol-Myers Squibb 10 mg 80 mg
Zocor simvastatin Merck 5 mg 80 mg
Cholesterol absorption inhibitors Zetia ezetimibe Merck Schering-Plough 10 mg 10 mg Main action: Lowers LDL cholesterol; inhibits absorption of cholesterol.
If used with a statin, take together.
If used with bile acid sequestrant,ezetimibe should be taken 2 hr before or 4 hr after bile acid sequestrant.
Nicotinic acid (niacin)
Niaspan nicotinic acid (extended release) Kos 300 mg (starting dose) 2,000 mg Main action: Lowers LDL cholesterol increases HDL ("good") cholesterol, lowers triglycerides.
Take with food.
May cause flushing.
May increase blood glucose levels.
Have blood tests for liver enzyme concentrations.
Long-acting forms may be more likely to cause liver malfunction.
  nicotinic acid generic† 300 mg 2,000 mg
Lipid combinations Advicor lovastatin niacin Kos 20 mg
500 mg
40 mg
2,000 mg
Main Action: Reduces LDL, TC, and TG and increases HDL due to the individual actions of niacin and lovastatin.
Fibric acid derivatives
Lopid gemfibrozil Pfizer 1,200 mg 1,200 mg Main action: Lowers triglycerides, increases HDL cholesterol.
Perform blood tests for liver enzyme concentrations.
Notify physician of muscle pain immediately.
  gemfibrozil generic† 1,200 mg 1,200 mg
Tricor fenofibrate Abbott 54 mg 160 mg
Bile acid sequestrants
LoCHOLEST cholestyramine Warner Chilcott 4 g 24 g Main action: Lowers LDL cholesterol.
May cause constipation and stomach upset.
May need to be taken at a different time than other medications to avoid drug interactions.
May increase triglycerides blood concentrations.
LoCHOLEST light cholestyramine light Warner Chilcott 4 g 24 g
Questran cholestyramine Par Pharmaceuticals 4 g 24 g
Questran light cholestyramine light Par Pharmaceuticals 4 g 24 g
Prevalite cholestyramine Upsher Smith 4 g 24 g
  cholestyramine generic† 4 g 24 g
  cholestyramine light generic† 4 g 24 g
Welchol colesevelam Sankyo 1,875 (3 tablets) 4,375 (7 tablets)
HMG-Coa = LDL = low-density lipoprotein, HDL = high-density lipoprotein, TC = total cholesterol, TG = plasma triglycerides, †generic = generic drug manufacturers


Medications to Lower High Blood Pressure*

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Category Brand Name Generic Name Manufacturer Minimum Daily Dose Maximum Daily Dose Special Considerations
Angiotensin-8 converting enzyme (ACE) inhibitors
Mavik trandolapril Abbot 1 8 May cause cough.
May increase potassium concentrations.
Do not use potassium or salt substitutes without consulting physician.
Do not use if pregnant or if trying to conceive.
Caution if creatinine >1.5.
Altace ramipril Monarch 1.25 20
Capoten captopril Apothecon 25 450
  captopril generic† 25 450
Univasc moexipril Schwarz 7.5 60
Monopril fosinopril Bristol-Myers Squibb 10 80
Lotensin benazepril Novartis 5 20
Prinivil lisinopril Merck 2.5 80
Zestril lisinopril AstraZeneca 2.5 80
  lisinopril generic† 2.5 80
Vasotec enalapril Merck 2.5 40
Vasotec enalapril Merck 2.5 40
  enalapril generic† 2.5 40
Accupril quinapril Pfizer 5 80
Aceon perindopril Solvay 4 16
Angiotensin II receptor blockers
Cozaar losartan Merck 25 100 May cause dizziness and upset stomach.
Do not use potassium or salt substitutes without consulting physician.
Do not use if pregnant or if trying to conceive.
Caution if creatinine >1.5.
Benicar olmesartan Sankyo 20 40
Diovan valsartan Novartis 80 320
Avapro irbesartan Bristol-Myers Squibb 150 300
Atacand candesartan AstraZeneca 15 32
Micardis telmisartan Boehringer-Ingelheim 20 80
Teveten eprosartan Biovail 400 800
Calcium channel blockers
Sular nisoldipine AstraZeneca 20 60 May cause constipation, dizziness, upset stomach, and flushing.
Call physician for shortness of breath, unusual heartbeat, or swelling of feet or hands.
Adalat CC* nifedipine Bayer 30 120
Procardia nifedipine Pfizer 30 120
Procardia XL* nifedipine Pfizer 30 120
  nifedipine generic† 30 120
Cardene nicardipine Roche 60 120
Cardene SR* nicardipine Roche 60 120
DynaCirc isradipine Reliant 2.5 20
DynaCirc CR* isradipine Reliant 2.5 20
Plendil felodipine AstraZeneca 5 20
Cardizem diltiazem Biovail 120 360
Cardizem CD* diltiazem Biovail 120 360
  diltiazem generic† 120 360
Dilacor XR* diltiazem Watson 180 540
Tiazac diltiazem Forest 120 540
Calan verapamil Searle 120 480
Calan SR* verapamil Searle 120 480
  verapamil generic† 120 480
Isoptin verapamil Abbott 120 480
Isoptin SR* verapamil Abbott 120 480
Verelan verapamil Schwarz 120 480
Verelan PM* verapamil Schwarz 100 400
Covera HS* verapamil Searle 180 480
Norvasc amlodipine Pfizer 5 10
Thiazides and related diuretics
Diuril chlorothiazide Merck 500 2,000 May increase blood glucose concentrations.
Take in morning to minimize diuretic effect at night.
May cause low potassium.
Need blood test to monitor level.
  chlorothiazide generic† 500 2,000
HydroDIURIL hydrochlorothiazide Merck 15 50
Microzide hydrochlorothiazide Watson 12.5 200
  hydrochlorothiazide generic† 12.5 200
Enduron methyclothiazide Abbott 2.5 10
Zaroxolyn metolazone Fisons 2.5 10
Hygroton chlorthalidone Aventis 2.5 100
Lozol indapamide Aventis 1.25 5
Loop diuretics
Lasix furosemide Aventis 80 80 May cause low potassium.
Need blood test to monitor level.
May cause photosensitivity:sunscreen recommended.
  furosemide generic† 80 80
Bumex bumetanide Roche 0.5 10
  bumetanide generic† 0.5 10
Demadex torsemide Roche 5 20
Potassium sparing diuretics
Aldactone spironolactone Searle 50 400 Do not use potassium or salt substitutes without consulting physician.
  spironolactone generic† 50 400
Dyrenium triamterene GlaxoSmithKline 50 300
Midamor amiloride amiloride 5 20
  amiloride generic† 5 20
Carbonic anhydrase inhibitors
Diamox acetazolamide Wyeth-Ayerst 250 1,000 May take with food if medicine upsets stomach.
May cause hand/foot tingling that can be confused with neuropathy.
  acetazolamide generic† 250 1,000
β-blockers
Tenormin atenolol AstraZeneca 25 100 May mask signs of low blood glucose levels.
May alter blood glucose.
Call physician for slow heart rate (<60),confusion, or swelling of feet or legs.
Can cause claudication.
  atenolol generic† 25 100
Kerlone betaxolol Searle 5 40
  betaxolol generic† 5 40
Levatol penbutolol Schwarz 10 40
Zebeta bisoprolol Lederle 2.5 20
Lopressor metoprolol Novartis 25 450
  metoprolol generic† 25 450
Toprol XL* metoprolol AstraZeneca 50 400
Corgard nadolol Bristol-Myers Squibb 40 320
  nadolol generic† 40 320
Inderal propranolol Wyeth-Ayerst 40 640
Inderal LA* propranolol Wyeth-Ayerst 40 640
    generic† 40 640
α-blockers
Minipress prazosin propranolol Pfizer 1 20 To prevent dizziness, avoid standing up suddenly, especially with the first few doses.
  prazosin generic† 2 40
Hytrin terazosin Abbott 1 40
  terazosin generic† 1 40
Cardura doxazosin Roerig 1 16
  doxazosin generic† 1 16
Combined α- and β-blockers
Trandate labetalol Faro 100 2,400 May mask signs of low blood glucose levels.
Take with food to avoid stomach upset.
Normodyne labetalol Key 100 2,400
  labetalol generic† 100 2,400
Coreg carvedilol GlaxoSmithKline 6.25 50
Direct vasodilators
Apresoline hydralazine Novartis 40 300 May cause headaches, fluid retention, or fast heart rate.
         
Central α-agonists
Catapres clonidine Boehringer-Ingelheim 0.1 2.4 Do not discontinue drug suddenly without consulting physician.
  clonidine generic† 0.1 2.4
Catapres TTS* (patch) clonidine Boehringer-Ingelheim 0.1 0.6
Aldomet methyldopa Merck 250 3,000
  methyldopa generic† 250 3,000
*Agents in a class of medicines share mechanisms of action, require similar precautions and generally have similar side effects.
CC = extended release, XL = extended release, SR = sustained release, CR = controlled release, CD = extended release, XR = extended release, PM = extended release, controlled onset, HS = extended release, controlled onset, †generic = generic drug manufacturers, TTS = transdermal therapeutic system, LA = long acting

For all anti-hypertensives Source: Centers for Disease Control and Prevention. Go Top