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Flashcards in Repro-Endo: Pancreas Deck (19)
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1

Insulin

  • Self-administered Subcu / IV (emergency)
  • Supplies Insulin for DM-1 or resistance DM-2, DKA
  • Leading to decreased Plasma Glucose
  • Tx: DM-1, DM-2, DKA, Insulin comes in Short, Intermediate, and Long-acting forms
  • SE: Hypoglycemia, Hypokalemia (K+ shift into intracellular compartment)

2

Ultrashort-acting Insulin Drugs?

  • Bind Insulin receptor (Tyrosine Kinase Activity)
  • Onset: 20 minutes
  • Duration: 4 hours
  • Tx: DM1, DM2, GDM (post-prandial glucose ctrl)
  • Synthetic Insulin - Lysine and Proline at end of β-chain
  • Does not dimerize upon injection --> 30 min. prior food
  • SE: Hypoglycemia, Rare Hypersensitivity rxn
  • Lispro
  • Aspart
  • Glulisine

3

Rapid Acting Insulin Drug?

  • Onset: 1 hour
  • Duration: 6 - 8 hours
  • Tx: DM1, DM2, GDM, DKA (IV), Hyperkalemia (+ glucose) and Stress Hyperglycemia
  • Does Not dimerize upon SubQ inj.--> 30 delay
  • Regular Insulin
  • Only type of Insulin given IV

4

Intermediate-acting Insulin Drugs?

  • Onset: 2 - 4 hours
  • Duration: 10 - 18 hours
  • Tx: DM1, DM2, GDM
  • Insulin and Zinc to react w/ Protamine (basic protein)
    --> Protamine-Insulin-Zinc
    --> Slow Release
  • NPH (Neutral Protamine Hagedorn)
  • Lente
  • Most widely used type of Insulin

5

Long-acting Insulin Drugs?

  • Tx: DM1, DM2, GDM
  • Glargine: 12 hours --> 24 hours
  • Protamine Zinc: 14 - 24 hours --> 36 hours
  • 3 Amino acid difference (2 Arg & Asp)
  • Glargine (soluble in the vial pH 4.0 to precipitate upon injection (at neutral pH)
  • Ultralente: 18 - 24 hours --> 36 hours
  • Detemir (Levemir)
  • Establishes Basal Insulin Level

6

Sulfonylureas

  • Closes K+ channels on β-cells and K+ efflux
    --> Leading to  Depolarization
    --> Ca2+ influx --> Insulin Release
    --> Decreased Glucagon release from α-cells and Increased tissue sensitivity to Insulin
    --> Increased Glucose Uptake (peripheral)
  • Tx: DM-2 (reqs. 30% B-cell function)
  • 1st Gen: Tolbutamide
  • 2nd Gen: Glyburide, Glipizide
  • SE: Risk of Hypoglycemia a/w Renal Failure, Weight gain, IV hypersensitivity rxn, Hypoglycemia w/ Cimetidine, Insulin Salicylates, Sulfonamides

7

Biguanides

(Metformin)

  • Inhibit Gluconeogenesis in Liver
  • Decrease Hepatic Glucose production (Liver)
  • Inscrease Peripheral Insulin sensitivity
  • Mechanism unknown
  • Decrease Postprandial glucose levels w/out weight gain or Hypoglycemia (euglycemic)
  • Tx: Obese diabetic, synergistic w/ Sulfonylureas in pts. w/ Renal failure, Can be used in Pts. w/out Islet function
  • Contraindicated in Pts. w/ Renal Impairment
  • SE: Lactic acidosis (rare), GI distress, avoid IV contrast

8

α-glucosidase inhibitors

(Acarbose, Miglitol)

  • α-glycosidase inhibitor
    --> Decreased carbohydrate absorption from GI tract
    --> inhibits Sucrose --> Glucose
    --> Decreased Insulin demand
    --> Delayed sugar hydrolysis and glucose absorption
    --> Decreased Postprandial Hyperglycemia
  • Tx: DM-2
  • SE: Hypoglycemic --> Glucose tablets or Food intake
  • SE: GI disturbances: Flatulence, Diarrhea, Abdominal Discomfort

9

Glitazones / Thiazolidinediones

(Rosiglitazone, Pioglitazone)

  • Decreases Insulin resistance
    --> Enhances Efficacy of Insulin in the Liver, Muscle, Fat
  • Binds nuclear Peroxisome Proliferator-activated Receptor (PPARγ) to control Transcritpion of Insulin-responsive genes
    --> Insulin sensitization and decreased Hepatic gluconeogenesis and Insulin receptor upregulation
    --> Translocation of Glucose Transporter in Muscle and Adipose tissue
  • Tx: DM-2 in the Absence of Liver Disease, CHF or Coronary artery disease
  • SE: Weight gain, Edema (peripheral or macular), Liver function abnormalities

10

Repaglinide

  • Oral Hypoglycemic
  • Works like Sulfonylureas by stimulating release of Insulin from the Pancreas
  • Tx: DM-2
  • SE: Hypoglycemia, Weight gain

11

First generation Sulfonylureas Drugs and SEs?

  • Tolbutamide
  • Chlorpropamide
  • SE 1st Gen: Disulfiram-like effects

12

2nd Generation Sulfonylureas Drugs and SEs?

  • Glyburide
  • Glimepiride
  • Glipizide
  • SE 2nd Gen: Hypoglycemia

13

Glitazone / Thiazolidinediones Drugs?

  • Pioglitazone
  • Rosiglitazone

14

α-glucosidase inhibitor drugs?

  • Acarbose
  • Miglitol

15

Amylin analogs?

  • Pramlintide
  • Decrease Gastric emptying
  • Decrease Glucagon
  • Tx: DM1, DM2
  • SE: Hypoglycemia, Nausea, Diarrhea

16

GLP-1 analogs?

  • Exenatide
  • Liraglutide
  • Increased Insulin
  • Decreased Glucagon release
  • Tx: DM2
  • SE: Nausea, Vomiting, Pancreatitis

17

DPP-4 inhibitors?

  • Linagliptin
  • Saxagliptin
  • Sitagliptin
  • Increased Insulin
  • Decreased Glucagon release
  • Tx: DM2
  • SE: Mild urinary or Respiratory Infections

18

Sitagliptin phosphate?

(DPP-4)

  • Orally active inhibitor of the 'Dipeptidyl peptidase-4' (DPP-4) enzyme, the enzyme that breaks down Endogenous Glucagon-like peptide-1 (GLP-1)
    --> 
    Increase of Endogenous GLP-1
    --> Stimulates Insulin release and Inhibits Glucagon release
  • Sitagliptin amplifies the action of GLP-1
  • Saxagliptin is a new version that acts the same way

19

SGLT2 Inhibitor

(Canagliflozin)

  • SGLT2 (Sodium-glucose cotransporter 2) inhibitor
    --> reduces the reabsorption of Glucose in the Proximal tubule
    --> Loss of Glucsoe and Water in Urine
  • SE: Genital mycotic infections (men and women), UTIs, Diuretic effects