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Diabetes Medications                            See   Diabetes Mellitus

Protocol for acute Rx of hyperglycemia (2-2006 DM clinic)   

Oral Diabetic Medications   

- stimulate insulin secretion in response to glucose.  Watch for weight grain.
  • Glipizide/Glucotrol   (2nd generation)  - Preferred than Glyburide in elderly due to its shorter half-life of 2-4 hours.
    5-10 mg 1-2 tab 1-2x/d; 5-10 mg tab (Max 40 mg/day)
    Glucotrol XL 5-10mg tab once/day
  • Glyburide/Diabeta  | Micronase  |   (2nd generation)   - Half-life of 5-16 hours
    2.5-5mg 1-2 tab 1-2x/d; 1.25-2.5-5 mg tab  (Max 20 mg/day)
     Glynase 1.5-3 mg 1-2 tab 1-2x/d; 1.5-3 mg tab
  • Glimepiride/Amaryl  (3rd generation)
    1,2,4 mg tab/day.  Start 1-2 mg/d, usual maintenance dose is 1-4mg once/d (Max: 8mg/d)
  • Gliclazide/ Diamicron  80-160 mg daily, max 320 mg PO daily.
    Modified release Diamicron MR 30 mg PO daily, mas 120 mg daily  
  • Diabenese/Chlorpropamide  (1st generation)
    100-250 mg 1-3 tab/d; 100-250 mg tab
  • Orinase /Tolbutamide  (1st generation) 
    250-500 mg tab 1-3x/d
  • Tolinase/Tolazamide   (1st generation)
    100-500 mg tab -2x/d; 100-250-500 mg tab.
  • Dymelor/Acetohexamide 500-750 mg once or divided.
  • Thiazolidinediones (Glitazones)
    - enhance muscle sensitivity to insulin.
    - Side effects are weight gain and edema.  Also check liver function tests at baseline and when clinically indicated thereafter.
    Caution: Possible liver damage.
    Its primary action is to enhance insulin action in muscle, adipose tissue & liver; it also reduces excessive hepatic glucose output. It is for type II diabetes currently on insulin, yet not controlled (insulin >30 u/d) (Parke Davis)  
    Warning: Liver damage/failure. Check LFT baseline & monthly x6 months, then every 2 months x6 months. 
    • Pioglitazone/Actos  15-30-45 mg tablet once daily   
    • Rosiglitazone/Avandia  4 mg 1-2x/day    
      Avandamet (Rosiglitazone/metformine) 1-2-4 mg/500mg tablets
    • Troglitazone/Rezulin -200-400mg tab 1/d - discontinued!

- Primary action is reduction of excessive hepatic glucose output; it also has some activity on insulin resistance in skeleton muscle, though less than troglitazone.  Metformin may cause life-threatening lactic acidosis.  Hold this med prior to IV contrast agents and for for 48 hours after.  Avoid if ethanol abuse, heart failure, hepatic or renal insufficiency (Cr >1.4-1.5), or hypoxic states.
  • Glucophage/Metformin 500 - 850 mg tab 2-3x/day or 1000 mg bid with meals. (MAX 2550 mg/day)
    Takes about 2 wks to work well.  Do not use in renal or hepatic dysfunction, dehydrated, or hospital patients.  
  • Glumetza/ Extended Metformin 500-1,000 mg dosage strength
Non-Sulfonylurea Insulin Secretagogues  (Meglitinides)
- stimulate insulin production in response to post-meal hyperglycemia.  
- Side effects include hypoglycemia, while repaglinide can bring on headaches.
  • Repaglinide/Prandin  0.5 - 1 - 2 mg tab ac (Max 16 mg/day)
  • Starlix (Nataglinide)   120 mg ac
    Starlix (Nataglinide) is an oral prescription drug that lowers your overall level of blood sugar by reducing the high blood sugar levels following a meal. It works by helping your body release insulin right at the start of a meal, when you need it the most.
    Who can take Starlix?  Starlix is indicated as initial monotherapy or as add-on therapy to patients on metformin who are not at A1c goal.
Alpha-glucosidase Inhibitor  
- it delays the breakdown of complex carbohydrates in the intestine & reduces the postprandial rise in blood glucose.
- Side effects include bloating and diarrhea.
  • Acarbose/Precose
    25- 50- 100 mg tid with first bite of meal.  Initially 25 mg 1x/d x2wks, then bid x2wks, then tid x2months, then may increase to 50 mg tid.
    - It slows carbohydrate breakdown & glucose GI absorption.  It decreases postprandial glucose peaks.
    May cause GI upset, pain, diarrhea, flatulence.
  • Miglitol/Glyset 50 mg tid

  • Combination Oral Diabetic Medications
    Data suggest that combination treatment with once-daily metformin-rosiglitazone improves glycemic control, insulin sensitivity, and  Beta-cell function more effectively than treatment with metformin alone.
NEW  * Exenatide (Exendin-4) 5-10 mcg bid subc within 1 hour before breakfast & dinner.
Glucagon-like peptide-1 (GLP-1) type med that enhancse glucose-dependent insulin secretion & regulation of glucagon release and the rate of gastric emptying, thereby reducing hyperglycemia; it also enhances pancreatic Beta-cell function and promotes satiety, resulting in reduced caloric intake & weight reduction.   

Byetta (Exenatide) 5-10 mcg BID subc. injection within 1 hour before breakfast & dinner.
- is indicated as adjunctive therapy to improve glycemic controlin patients with type 2 diabetes who are taking metformin, a sulfonyluria, or a comgination of metformin and a sulfonylurea but have not achieved adequate glycemic control. 
- by improving acute beta-cell responsiveness
- not recommended for use in patients with end-stage renal disease, severe renal impairment, or severe GI disease.
- most common adverse event was nausea, excluding hypoglycemia.

Combination of Oral Diabetic Agent and Insulin

If oral diabetic agents do not achieve glycemic control, consider combining them with insulin.  Options include:

  • Bedtime insulin plus daytime sulfonyurea
  • Bedtime insulin plus metformin

  • Humalog insulin analog is faster but shorter duration action than Human regular insulin.  Use within 15 min before meals.
  • Humulin Lente, NPH, Regular, Ultralente, 70/30 (Lilly)
  • Novolin Lente, NPH, Regular, 70/30 (Novo Nordisk)
  • Mixtard Human 70/30 (Novo Nordisk)
  • Lantus (Insulin glargine - rDNA origin) once a day injection, start 10  IU daily (about the same dose as NPH)
  • Symlin (pramlintide) 15 mcg subc before meal, titrate by 15 mcg increments up to maintenance 30-60 mcg as tolerated in Type 1 diabetes.  In type 2 diabetes initiate 60 mcg subc before meals and increase upto 120 mcg as tolerated.
    - a synthetic analog of the human neuroendocrine hormone amylin, it is secreted from beta cells with insulin.  The drug slows gastric emptying and decreases appetite and glucagon secretion after meals.
  • Inhaled insulin (Exubera - Pfizer) 
    Jan. 27, 2006 — The first inhaled insulin (Exubera) was approved today by the US Food and Drug Administration (FDA) for the treatment of adult patients with type 1 and type 2 diabetes. An inhaled powder form of recombinant human insulin (rDNA), the drug and delivery system is the first new insulin formulation introduced since the discovery of insulin in the 1920s, according to the FDA.


Injection, solution, aspart, human:

  • NovoLog®: 100 units/mL (10 mL vial)

  • NovoLog® [PenFill®]: 100 units/mL (3 mL cartridge)

Injection, solution, lispro, human:

  • Humalog®: 100 units/mL (1.5 mL cartridge, 3 mL disposable pen, 10 mL vial)

Injection, solution

  • Apidra (insulin glulisine [rDNA origin] injection) subc.
    - rapid acting, short duration
    - when used as a mealtime insulin, the dose should be given withint 15 min before or immediately after a meal.


Injection, solution, regular, human:

  • Humulin® R: 100 units/mL (10 mL vial)

  • Novolin® R: 100 units/mL (1.5 mL prefilled syringe, 10 mL vial)

  • Novolin® R [PenFill®]: 100 units/mL (1.5 mL cartridge, 3 mL cartridge)

Injection, solution, regular, human, buffered :

  • * Velosulin® BR [Discontinued]: 100 units/mL (10 mL vial)

Injection, solution, regular, purified pork:

  • Regular Iletin® II: 100 units/mL (10 mL vial)


Injection, suspension, lente, human [zinc]:

  • Humulin® L, * Novolin® L [Discontinued]: 100 units/mL (10 mL vial)

  • Injection, suspension, lente, purified pork [zinc]:

  • Lente® Iletin® II: 100 units/mL (10 mL vial) [Discontinued]

Injection, suspension, NPH, human [isophane]:

  • Humulin®  N: 100 units/mL (3 mL disposable pen, 10 mL vial)

  • Novolin®  N: 100 units/mL (1.5 mL prefilled syringe, 10 mL vial)

  • Novolin®  N [PenFill®]: 100 units/mL (1.5 mL cartridge, 3 mL cartridge)

Injection, suspension, NPH, purified pork [isophane]:

  • NPH  Iletin® II: 100 units/mL (10 mL vial)


Injection, suspension, Ultralente®, human [zinc]:

  • Humulin  U  Ultralente®: 100 units/mL (10 mL vial)

Injection, solution, glargine, human:

  • Lantus®: 100 unit/mL (10 mL vial)


Injection, aspart protamine human suspension 70% and rapid-acting aspart human solution 30%

  • (NovoLog® Mix 70/30): 100 units/mL (3 mL cartridge, 3 mL prefilled syringe)

Injection, lispro protamine human suspension 75% and rapid-acting lispro human solution 25%

  • (Humalog® Mix 75/25™): 100 units/mL (3 mL disposable pen, 10 mL vial)

Injection, NPH human insulin suspension 50% and short-acting regular human insulin solution 50%

  • (Humulin® 50/50): 100 units/mL (10 mL vial)

Injection, NPH human insulin suspension 70% and short-acting regular human insulin solution 30%:

  • Humulin® 70/30: 100 units/mL (3 mL disposable pen, 10 mL vial)

  • Novolin® 70/30: 100 units/mL (1.5 mL prefilled syringe, 10 mL vial)

  • Novolin® 70/30 [PenFill®]: 100 units/mL (1.5 mL cartridge, 3 mL cartridge)


See also Medical Letter Sep. 2002 Diabetes Treatment Guidelines