Diabetes: Insulin Therapy Flashcards
Pharmacologic Therapy: Treatment Options
• Type 1 diabetes
- Insulin
- Symlin (pramlintide): Rx only
• Type 2 diabetes - Oral agents: Rx only • Sulfonylureas • Non-Sulfonylurea Secretagogues • Biguanide • Thiazolidinediones • Alpha-glucosidase inhibitors • DPP-4 Inhibitors • SGLT-2 Inhibitors
- Injectables: Insulin, Pramlintide (Rx only), Exenatide, dulaglutine, semaglutide (Rx only)
- Inhaled: Insulin
Actions of Insulin
STOP: gluconeogenesis, glucogenolysis, lipolysis, ketogenesis, proteolysis
GO: glucose uptake in muscle/ad tissue, glycolysis, glycogen synthesis, protein synthesis, uptake of ions
Insulin Appearance
• Rapid-Acting: Clear / Colorless
- Lispro, Aspart, Glulisine
• Short-Acting: Clear / Colorless
- Regular
• Long-Acting: Clear / Colorless
- Glargine, Detemir, Degludec
• Intermediate-Acting: Cloudy / White
- NPH
• Combinations: Cloudy / White
- Regular, Novolog, Humalog
Rapid-Acting Insulin: Ex, DF, Pros, Cons
• Examples
- Insulin lispro (Humalog®, Admelog®)
- Insulin aspart (Novolog®, Fiasp®)
- Insulin glulisine (Apidra®)
- Rx ONLY, vials and pens
- Produced through recombinant DNA technology
- Typical dosing frequency: BID-QID, 15 minutes before a meal
• Pros
- Closely mimics endogenous postprandial insulin
- Works very fast
- More flexibility with mealtimes
- Improves postprandial hyperglycemia
- Usually less hypoglycemia than regular insulin
• Cons
- Caution with CHO intake (if < than expected = hypoglycemia)
- Cost, insurance coverage, MDI
- RX only
Short-Acting Insulin: Ex, DF, Pros, Cons
• Example
- Regular insulin (Humulin® R or Novolin® R)
- Clear & colorless
• Typical dosing frequency
- BID-QID, 30 minutes before meal
• Pros
- Relatively inexpensive
- Available OTC
- May be given IV as well
• Cons
- Takes longer to work & may cause delayed hypoglycemia
- Less flexibility with mealtimes
Intermediate-Acting Insulin: Ex, DF, Pros, Cons
• Examples
- NPH (Humulin® N, Novolin® N) (Protamine suspension slows dissolution & absorption from the injection site) (Insulin of choice for mixing)
- Typical dosing frequency: Daily (at bedtime) or BID
- Pros
- Provides basal insulin coverage
- Relatively inexpensive
- Available OTC
• Cons
- Protamine & zinc may cause immunologic reactions such as urticaria at the injection site
- Action may be unpredictable leading to hypoglycemia
Insulin Glargine (Lantus®, Basaglar®): Type, DF, Pros, Cons
Long acting insulin
• Insulin analog, 28 days stable at RT
• Typical dosing frequency:
- Insulin glargine: QD
- Must only inject in subcutaneous tissue (not IM or IV)
• Pros
- Glargine provides more predictable, steady, long acting, “peakless” basal insulin for about 24 hours.
- Decrease nocturnal hypoglycemia and less weight gain compared with NPH
• Cons
- Cost
- Injection site stinging, cannot be mixed
- pH=4 for stability
- RX Only
Insulin glargine-yfgn (Semglee®)
Long-acting insulin
- New interchangeable biosimilar
- Think generic (but not really)
- Biosimilar to Lantus only
What Is an Interchangeable Biosimilar Product?
An interchangeable product is a biosimilar that may be substituted for a reference product without the intervention of the prescribing healthcare provider, depending on state pharmacy laws.
Insulin Glargine: Mechanism of Action
- Injection of an acidic solution (pH 4.0)
- Precipitation of glargine in subcutaneous tissue (pH 7.4)
- Slow dissolution of free glargine hexamers from precipitated glargine (stabilized aggregates)
- Protracted action
Insulin Detemir (Levemir®): Type, DF, Pros, Cons
Long-acting insulin
• Insulin analog, 42 days stable at RT
• Typical dosing frequency:
- Insulin detemir: QD-BID
- Must only inject in subcutaneous tissue (not IM or IV)
• Pros
- Detemir provides more predictable, steady, long acting, “peakless” basal insulin for about 24 hours at higher doses
- Does not cause stinging (neutral pH)
- Decrease nocturnal hypoglycemia and less weight gain compared with NPH
• Cons
- Cost
- RX Only
Insulin Degludec (Tresiba®): Type, DF, Pros, Cons
Long-acting insulin • Ultra-long-acting insulin • Available as U-100 and U-200 • Insulin analog, 8 weeks stable at RT • Typical dosing frequency: Once Daily
• Pros
- Predictable, steady, long acting, “peakless” basal insulin for 42 hours.
- Does not cause stinging (neutral pH)
• Cons
- Cost
- RX Only
Concentrated Insulins
- Humalog® (lispro) U-200
- Tresiba® (degludec) U-200
- Toujeo® (glargine) U-300
- Available in insulin pens
- Similar PK to U-100
• Regular U-500
- Vial and pen
- Pros: Less volume for injection
- Cons: Cost
Inhaled Insulin
• Examples
- Insulin (Afrezza®) inhalation powder
- Produced through recombinant DNA technology
- Typical dosing frequency: BID-QID, 5 minutes before or during a meal
- Pros
- Closely mimics endogenous postprandial insulin
- Works very fast (peak in 15 minutes)
- More flexibility with mealtimes
- Improves postprandial hyperglycemia
- Less hypoglycemia than rapid insulin
- Less weight gain
• Cons
- Multiple inhalations for large doses
- Cost, insurance coverage
- RX only
- Lung disease
Afrezza Inhaled Insulin
• Afrezza is available as cartridges with
- 4 units of insulin
- 8 units of insulin
• Must use with an inhalation device called a Dreamboat
• The cartridges and inhaler should be kept at room temperature for 10 minutes prior to use
- Storage in refrigerator is recommended