TYPE 1 DIABETES

Insulin Replacement Action Onset Peak Duration Uses

Lispro, Aspart, Glulisine Rapid -Acting ~20 min ~1 hr Up to 4 hrs Meals, acute hyperglycemia, acute diabetic ketoacidosis
Regular Short-Acting ~45 min ~ 2 hrs Up to 8 hrs Meals, acute hyperglycemia
NPH Intermediate ~2 hrs ~9 hrs Up to 24 hrs Basal insulin levels, overnight coverage
Glargine, Detemir Long-Acting ~2 hrs NONE Up to 24 hrs Basal insulin levels, overnight & 24 hr coverage
TYPE 2 DIABETES
MOA Side Effects Uses Other
α-glucosidase inhibitors →
NO hypoglycemia
Acarbose ↓cleavage of disaccharides in SI → MonoRx/ComboRx in Type 2 Additive effect in combo w/
GI side effects:
Miglitol ↓carbohydrate absorptions ↓Post-prandial hyperglycemia Sulfonylureas & Metformin
flatulent > diarrhea > nausea
SULFONYLUREAS Oral administration
st Hypoglycemia
1 Generation: Alcohol → ↑Effects
Chlorpropamide Drug interactions: Binds plasma
ND st
2 Generation: 1 gen = 24-48 hr half-life
proteins, P450 metabolism
Glyburide Less potent
ATP-dep. K+ channel blockers → Contraindications: pregnancy, nd
Glimepiride 2+ 2 gen = 3-5 hr half-life
cell depolarization → ↑Ca influx lactation, renal/hepatic MonoRx/ComboRx in Type 2
Glipizide More potent
→ ↑insulin release insufficiency
Diazoxide = opposite MOA,
Chlorpropamide - SIADH
Rx for hypoglycemia
MEGLINIDES
Less hypoglycemia Rapid absorption
Repaglinide
Caution: hepatic insuff. 1 hr half-life
Nateglinide
BIGUANIDES ↑AMP-dep. Kinase activation → NO hypoglycemia
Phenformin ↓Acetyl-CoA carboxylase → Metabolic (lactic) acidosis Overall Effects:
First line drug for Type 2
Metformin ↓lipogenesis → ↑fatty acid oxidation ↓Hepatic gluconeogenesis
Also ↓Triglyceride levels
↑GLUT4 & glycolytic enzymes Contraindications: ↑Muscle/Adipocyte glucose
↓Gluconeogenic enzymes Renal failure (Cr ≥1.5 / ≥1.4 ) uptake
Parenteral contrast media use
THIAZOLIDINEDIONES Activates PPAR- nuclear recept:
Pioglitazone Adipose: ↑fat synthesis, ↓lipolysis Heart failure Active metabolizes
MonoRx/ComboRx in Type 2
Adipose, muscle, liver: 99% Albumin bound
Also ↓HTN & atherosclerosis
↑GLUT4, ↑insulin sensitivity Weight gain GI excretion

AMYLIN ANALOG ↓Glucagon secretion BOTH Type 1 & Type 2

Amylin = co-secreted with
Pramlintide ↓Gastric emptying, Hypoglycemia ↓Post-prandial hyperglycemia
insulin by cells
↓Appetite Injected with major meals
GLP-1 ANALOGS ↑Insulin release
Injected: GLP-1 = incretin released
Exenatide ↓Glucagon secretion
Thyroid cancer Exenatide = 2x/day from gut, ↑glucose-induced
Bydureon ↓Gastric emptying
Pancreatitis Bydureon = 1x/week insulin secretion from
Liraglutide ↓Appetite
Liraglutide = 1x/day pancreas
↑β cell number
DDP-4 INHIBITORS
↓GLP-1 metabolism by DDP-4
Sitagliptin Contraindications: Renal failure MonoRx/ComboRx in Type 2 Oral administration
(same effects as GLP-1 analogs)
Linagliptin