Antidiabetics, Insulin, + Incretins Flashcards
Insulin maintenance therapy
- admin S.C.
- Afrezza inhalation
Hyperglycemia emergencies
IV regular insulin
Ultra-short insulins
- Insulin lispro (Humalog)
- Insulin aspart (Novolog)
- Insulin glulisine (Apidra)
- Inhaled Afrezza
- Prior to meals for post-prandial glucose
Short-acting insulin
- Regular insulin
- IV for DKA; SC for normal maintenance postprandial glucose
Intermediate acting insulin
- NPH Insulin (Humilin/Novolin)
- maintains fasting blood glucose levels
- given w/ regular/ultrafast insulin
Long-acting insulin
- insulin glargine (Lantus)
- insulin detemir (Levemir)
- insulin degludec (Tresiba)
- Once-daily maintenance insulin levels
Long-lasting Combo
- Insulin degludec/liraglutide
- Fasting + Postprandial glucose levels
- ONLY DMT2
Novolog 70/30 mix coverage
- Covers Postprandial AND fasting
Insulin Drug interactions
- B-Blockers: Reduce hyperglycemic action; inhibit GNG + Glycogenolysis
Which of the following statements is correct?
A. Insulin can be administered orally
B. Insulin is always required therapy in Type II diabetes
C. Protamine is added to insulin to decrease the rate of absorption of the hormone
D. Insulin is a steroid hormone
E. Insulin acts by binding to receptors in the nucleus of target tissues
C. Protamine is added to insulin to decrease the rate of absorption of the hormone
Insulin secretagogues
- Mech
- AE
- Drug interactions
- Sulfonylureas and
Meglitinides - Stimulate the release of insulin from b-cells in the pancreas by closing K Channels causing membrane depolarization; inhibit alpha cell secretion of glucagon
- AE: Hypoglycemia; Weight gain; N/V; Anemia
- DI: Highly bound to plasma proteins; Sulfonamides, Salicylates, clofibrate, phenylbutazone
First-Generation Sulfonylureas
- Use
- Tolbutamide; Tolazamide; Chlorpropamide
- Fasting + Postprandial hyperglycemia
Tolbutamide Duration + Breakdown
- Short (6-10 H)
- rapidly oxidized in liver -> Safest for geriatric diabetes
Tolazamide DOA
intermediate 10-14 H
Chlorpropamide
- DOA
- PK
- Contra
- DOA: Slow; 48-60 H
- PK: slowly metabolized in liver; 25% excreted in urine unchanged
- Contra: elderly + hepatic/renal insufficiency
Second Generation Sulfonylureas
- Use
- Caution
- Glipizide (XR), Glimepiride
- Use: Fasting + Postprandial;
- Caution: Elderly + CV
Meglitinides
- use
- Repaglinide
- Nateglinide
- Postprandial hyperglycemia
Biguanide
- MOA
- Use
- PK
- AE
- Contra
- Metformin
- does not involve b-cells; DEC hepatic GNG; DEC Glucose absorption
- Fasting + Postprandial
- Dur 10-12H; Excreted by kidneys unchanged
- GI disturbance; Lactic Acidosis
- Contra: Renal/hepatic Dx
Thiazolidinediones
- MOA
- USE
- AE
- Pioglitazone; Rosiglitazone
- MOA: Stimulate PPAR-y-receptor; INC sensitivity to insulin
- Use: Fasting and post-postprandial
- SE: Anemia, Edema, HF, + MI
a-Glucosidase Inhibitors
- MOA
- Use
- AE
- Acarbose; Miglitol
- inhibitors of a-glucosidase; delay absorption of Carbs
- Post-prandial
- AE: GI effects
Incretin Mimetics
- MOA
- AE
- Use
- Exenatide
- Liraglutide
- Dulaglutide
- Semaglutide
- Lixisenatide
- Use: Post-prandial + Basal glucose
- INC insulin; Inhibit glucagon
- AE: Hypoglycemial Pancratitis + P-Cancer??
Which Incretin Mimetic is only for postprandial hyperglycemia?
Exenatide (Byetta)
Dipeptidyl Peptidase-4 Inhibitors
- MOA
- AE
▪Sitagliptin (Januvia)
▪Saxagliptin (Onglyza)
▪Linagliptin (Tradjenta)
▪Alogliptin (Nesina)
- MOA: Inhibits DPP-4 -> INC Insulin release; inhibits glucagon
- AE: Upper RTI, Headache, Pancreatitis, Hypoglycemia, Allergic rxn, Lymphopenia
Sodium-Glucose Co-Transporter 2 Inhibitors
- MOA
- AE
▪Canagliflozin (Invokana) ▪Dapagliflozin (Farxiga) ▪Empagliflozin (Jardiance) ▪Ertugliflozin (Steglatro) - MOA: Inhibits sodium-glucose co-transporter 2; Decreases renal glucose reabsorption - AE: Hypoglycemia; Ketoacidosis
Biggest Goal of Diabetes management
- Reduces risk of vascular complications
Cardiac effects glucagon
- ionotrope
- chronotrope via INC cAMP
Clinical use Glucagon
- Severe hypoglycemia
- Radiology of Bowel
- B-blocker poisoning
