Diabetes medications

(Redirected from Sulfonylurea)

Background

  • Hypoglycemics
    • Sulfonylureas
    • Benzoic acid derivatives
  • Antihyperglycemics
    • Biguanides
    • Alpha glucosidase inhibitors
    • Thiazolidinediones

Common Anti-hyperglycemic Drugs and Pharmacology

Drug Pharmacology
Onset Peak Duration
Rapid-acting insulin

  • Aspart (Novolog)
  • Lispro (Humalog)
15-30min 1-2h 3-5h
Short-acting insulin

  • Regular
30-60min 2-4h 6-10h
Intermediate-acting insulin

  • NPH (Humulin, Novolin)
1-3h 4-12h 18-24h
Long-acting insulin

  • Glargine (Lantus)
2-4h None 24h
Sulfonylurea

  • Glimepiride
  • Glipizide (Glucotrol)
  • Glyburide (Glycron, Micronase)
2-6h 12-24h

Insulin

Biguanides (Metformin)

Suppresses liver glucose production

Dose

Metformin 500mg PO BID is first-line agent for type II diabetics

  • Do not prescribe if creatinine > 1.4 (GFR <40), CHF, hepatic insufficiency, ETOH abuse
  • Should be withheld for 48hr after IV contrast

Side Effects

  • Lactic acidosis (due to increased lactate production)
    • Seen almost exclusively in patients with renal failure
  • Nausea, diarrhea, crampy abdominal pain

Toxicity

  • Almost never causes hypoglycemia when taken alone, but can exacerbate hypoglycemia when taken in combination with hypoglycemic agents
  • Toxic dose unknown
  • Management: Supportive care

Sulfonylureas

Alpha Glucosidase Inhibitors

  • Acarbose, miglitol, voglibose
  • Competitively and reversibly inhibit alpha glucosidase brush border hydrolase enzyme- makes postprandial decrease in carbohydrate absorption since complex polysaccharides not broken down into absorbable monosaccharides. Does not affect lactose absorption
  • Taken with first bite of each meal
  • Since limited absorption, stays in gut and side effects mostly GI- bloating, gas, diarrhea
    • acarbose- can cause transaminitis/ liver inj
  • Contraindications- cirrhosis, IBD, malabsorption syndrome
  • Do not cause hypoglycemia when used as monotherapy
    • If hypoglycemic- sucrose/ table sugar will not work- use glucose- PO or IV
  • Since minimal absorption- systemic toxicity from OD unlikely

Thiazolidinediones

  • Rosiglitazone and poiglitazone
  • Enhance insulin effect on muscle, fat, liver without increasing pancreatic insulin secretion
  • Protein bound and hepatic metabolism - avoid in patients with liver disease
  • Side effects- induces ovulation, decreases effectiveness of OCP's, increases plasma volume (bad if CHF)

Benzoic Acid Derivatives

  • Repaglinide- monotherapy or combined with metformin
  • binds to ATP dependent potassium channel like sulfonyls but at different site.
  • Unlike sulfonyls, it decreases insulin levels
  • Dose 30 min before meal to decrease postprandial hyperglycemia

GLP-1 agonists

  • Exanatide (Byetta and Bydureon), Liraglutide (Victoza)
  • Synthetic glucagon-like peptide-1 (GLP-1) receptor agonists
  • Stimulates insulin release from pancreatic islet cells
  • May promote weight loss by slowing gastric emptying and increasing satiety

DPP-4 inhibitors

  • Sitagliptin, saxagliptin, linagliptin, alogliptin
  • Block DPP-4, which leads to increased activity of incretins, which inhibit glucagon release, which in turn increase insulin secretion and slow gastric emptying, ultimately decreasing blood glucose levels
  • Potential serious adverse events include acute pancreatitis, anaphylaxis/angioedema, SJS

SGLT-2 inhibitors

  • Canagliflozin (Invokana), Dapagliflozin (Farxiga), Empagliflozin (Jardiance)
  • Inhibit sodium-glucose cotransporter 2, decreasing glucose reabsorption in the proximal tubule
  • Potential serious adverse event: euglycemic DKA

See Also

References

Authors:

Ross Donaldson