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29 Cards in this Set
- Front
- Back
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Biguanids (oral)
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metformin (Glucophage, Glucophage XL)
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Mechanism of Action
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• 1o Decrease hepatic glucose production (glyconeogenesis) by interfering with lactate oxidation
• 2o Enhances insulin sensitivity in hepatic and peripheral (muscle) tissues • Metformin may also increases glucose to lactate turnover |
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Efficacy/Therapeutic Uses
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• Only oral diabetes medication proven to reduce the risk of total mortality; therefore guidelines list it as the drug of choice for initial therapy along with lifestyle modification
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Adverse Effects
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• Decreased appetite, metallic taste, N/V, & diarrhea (30%)
• Decreased absorption of vitamin B12 & folic acid • Does not cause hypoglycemia when used alone |
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Contraindications/Precautions
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• Use caution in patients with impaired renal function
• Avoid excessive alcohol consumption and in patients with severe liver dysfunction |
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Secretagogues- Sulfonylureas (oral)
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glipizide (Glucotrol & Glucotrol XL) (GLIP i zide)
*glimepiride (Amaryl) (GLYE me pye ride) – better tolerated glyburide (Diaeta, Glynase, Micronase) (GLYE byoor ide) – lots of hypoglycemia |
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Mechanism of Action
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• 1deg Stimulates pancreas to release more insulin
• deg Decreases hepatic glucose production (liver senses the insulin release) |
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Efficacy/Therapeutic Uses/ ADR
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• 2nd line oral agents in treatment of T2DM
• ADRs: hypoglycemia, weight gain |
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Secretagogues- Meglitinides (oral)
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repaglinide (Prandin) (re pa GLYE nide)
nateglinide (Starlix) (na te GLYE nide) |
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Mechinism of action/Efficacy/Therapeutic Uses/Adverse Effects
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similar to the sulfonylureas
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Dipeptidyl Peptidase-4 inhibitors/ DPP4-inhibitors/ gliptins (oral)
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sitagliptin (Januvia) (SI ta glip tin)
linagliptin (Tragenta) (LIN a glip tin) saxagliptin (Onglyza) (SAX a glip tin) |
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Mechanism of Actions
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• Inhibits the enzyme DPP-4. DPP-4 normally breaks down glucagon-like peptide-1 (GLP-1). Thus, these drugs increase endogenous GLP-1 levels. Normally GLP-1 stimulates post-prandial insulin release which then inhibits the liver’s production of glucose
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Efficacy/ Therapeutic Effects/ Adverse Effects
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• 2nd line oral agents in treatment of T2DM
• Mild stomach discomfort, diarrhea, rarely pancreatitis (weight neutral) • Hypoglycemia does not occur because these drugs don’t directly stimulate the pancreas |
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Thiazolidinediones (TZDs or glitazones) oral
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pioglitazone (Actos) (pye oh GLI ta zone)
rosiglitazone (Avandia®) (roh si GLI ta zone) – restricted use only |
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Mechanism of Action
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• 1deg Increase insulin sensitivity in muscle, liver, and fat tissues by stimulating peroxisome proliferator-activated receptor gamma (PPAR-)
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Efficacy/Therapeutic Uses/ Adverse Effects
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• Not a primary drug; rarely used due to adverse effects
• Edema (peripheral and macular edema), especially if used with insulin; contraindicated in HF NYHA III & IV; precaution in HF, HTN, pulmonary edema • Weight gain (especially if used with insulin or combined with sulfonylureas) • Increased rates of bone fractures & bladder cancer • Possible increased risk of cardiovascular complications & myocardial infarction |
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Alpha-Glucosidase Inhibitors (oral)
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acarbose (Precose) (AY car bose)
miglitol (Glyset) (MIG li tol) |
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Mechanism of Action
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• a-glucosidase inhibitors inhibit enzymes in the small intestine which normally turn dietary starch & sucrose into an absorbable form. Causes delayed glucose absorption
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Efficacy/Therapeutic Uses/Adverse Effects
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• Not a primary drug
• Taken with the first bite of each meal three times daily • Does not cause hypoglycemia when used alone. If hypoglycemia occurs due to other medications, only glucose will increase blood sugar levels. Cane sugar is sucrose & will not be effective. Eating will not be effective. Only the oral glucose tablets or gel or glucagon injection or IV dextrose injection will work to reverse hypoglycemia |
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Adverse Effects
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• Fermentation leads to flatulence (50-75%), cramps/bloating (20%), rumbling bowel sounds, & diarrhea (30%). GI side effects cause about 60% of patients to discontinue therapy
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GLP-1 receptor agonists (subcutaneous)
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exenatide (ByettaÒ twice daily, ext release Bydureon once a week) (ex EN a tide)
liraglutide (VictozaÒ once daily) (lih rah GLOO tide) |
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Mechanism of Action
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• These drugs are synthetic versions of exendin, a substance found in Gila monster saliva. These drugs are glucagon-like peptide (GLP-1) agonists (stimulate GLP-1 receptors) which then stimulates glucose-dependent insulin secretion, inhibits release of glucagon after meals, slows rate of stomach emptying, and reduces appetite (increases satiety)
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Efficacy/Therapeutic Uses
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• 2nd line agents in treatment of T2DM
• Helps with weight loss. Sometimes used in patients without diabetes to help them lose weight (not FDA approved for weight loss) ~8lb average weight loss over 24 weeks |
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Adverse Effects
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• Nausea (40 – 50%), loss of appetite, diarrhea (13%), rarely pancreatitis
• Hypoglycemia is usually not a concern with monotherapy • Risk of hypoglycemia is increased when added to sulfonylurea; consider reducing dose of sulfonylurea when initiating therapy • Bydureon may cause small, temporary lumps at injection site (normal, not a concern) |
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Insulin
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Available Insulin Products
Insulin Type Onset* Very rapid-acting / short acting insulin Lispro (Humalog) Aspart (Novolog) Glulisine (Apidra) 15 – 30 min Rapid acting / Short acting insulin Regular (Humulin R & Novolin R) 30 – 60 min Intermediate-acting insulin NPH (Humulin N & Novolin N) 2 – 4 hrs Long-acting / Basal insulin Insulin Detemir (Levemir) 2 hrs Glargine insulin (Lantus) 4 – 5 hrs Premixed Insulin Combinations NPH / Regular (Humulin 70/30 & Novolin 70/30) 30 – 60 min NPH / Regular (Humulin 50/50) 30 – 60 min NPA / Aspart (Novolog Mix 70/30) 15 – 20 min NPL / Lispro (Humalog Mix 75/25) 15 – 20 min |
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Mechanism of Action
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• Insulin is a hormone normally synthesized in the pancreas
• Insulin secretion is stimulated primarily by glucose. Other stimulants include epinephrine, fatty acids, amino acids, and ketones. Insulin promotes conservation of energy & increases cellular uptake of glucose, amino acids, & potassium • All US insulin products contain only the active human insulin peptide • The most common concentration is 100 units/mL (U-100) |
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Efficacy/Therapeutic Uses
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• Required for all patients with T1DM
• Frequently used in patients with T2DM |
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Adverse Effects
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• Hypoglycemia is a serious risk
• Weight gain • Injection site reactions are generally mild (lipohypertrophy, infection) |
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Administration
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• Subcutaneous injections in upper arms, thighs, and abdomen. Rotate injection sites to minimize lipohypertrophy
• Rapid & intermediate acting insulins should be given 30 minutes before a meal or snack. Very rapid acting insulin should be given 15 minutes before a meal or snack • Vials & Syringes: Insulin sold in 10ml vials and packs of syringes sold separately • Jet Injectors: Needless syringe that uses air to inject into skin • Pen Injectors: Pre-filled device with disposable needle. Doses may be preset or dialed • Portable Insulin Pump: computerized device delivers a basal rate with mealtime boluses by pressing a button. Patients must be highly motivated & be able to comprehend the education required for safe care & maintenance of insulin pumps |
