Exam IV - Diabetes Flashcards Preview

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Flashcards in Exam IV - Diabetes Deck (48):
1

Insulin
Indications

Hyperglycemia

2

Insulin
Mechanism

Rapid: ↑ Gluc transport Intermediate: Activates glycolytic enzymes, glycogen synthase; Blocks posphorylase & gluconeogenesis Delayed: Gene transcription; cell growth

3

Insulin
ADME

1. Injected SQ, IV or IM in emergency 2. Ultra short acting: Lispro, Aspart, Glulisine 3. Rapid acting: standard, purified 4. Intermediate acting: Novolin-N, Humulin-N 5. Long Acting: Detemir, Glargine *use short acting at meals & longer for cont. effect

4

Insulin
Advantages

1. Therapy is individualized: multidose regimens, repeated monitoring 2. Now other admin forms: pen, nasal spray

5

Insulin
Adverse

1. "Dawn effect" - overnight dosing is important 2. Hypoglycemia (

6

Insulin
Contraindications

Pregnancy category B

7

Metformin (Biguanide)
Indications

Insulin sensitizer: blocks glucose release from liver
First line for DMII

8

Metformin
Mechanism

Activates AMPK in liver: ↑FA oxidation, ↑gluc uptake, ↓lipogenesis, ↓gluconeogenesis

9

Metformin
ADME

T½ 1.5-3H Non-protein binding Not metabolized Kidney excreted used in combo w/ PO antidiabetics: metformin+saxagliptin

10

Metformin
Advantages

1. Doesn't induce hypoglycemia 2. No weight gain 3. Inhibits microvascular complications

11

Metformin
Adverse

GI: N,V&D - dose dependent, transient, metallic taste

12

Metformin
Contraindications

1. Pregnancy Category B 2. Renal & Hepatic Dz
3. EtOH: lactic acidosis

13

Glipizide (Sulfonylurea)
Indications

Classic secretagogue: promotes pancreatic insulin secretion

14

Glipizide
Mechanism

1. Binds & blocks ATP sensetive K+ channel β-cell → depolarization → Ca2+ influx
2. Requires functional β-cells
3. No effect on insulin resistance / sensitvity

15

Glipizide
ADME

Protein bound liver metab renal excretion

16

Glipizide
Advantages

↓ A1C by 1-2% 2nd generation: fewer adverse effects

17

Glipizide
Adverse

1. Hypoglycemia 2. Weight gain

18

Glipizide
Contraindications

1. Pregnancy Category C 2. Hepatic & renal Dz 3. Caution in elderly pts

19

Glipizide
Drug-Drug

1. ↑ hypoglycemia: NSAIDS, MAOIs, sulfonamides, chloramphenicol, H2 antihistamines, EtOH 2. ↓hypoglycemia: β-blockers; thiazides, estrogens, rifampin

20

Pioglitazone (TZD)
Indications

Insulin sensitizer: blocks FFA release from adipose, promotes uptake in muscle

21

Pioglitazone
Mechanism

Peroxisome proliferator-activated receptor gamma (PPAR-γ) ligands: ↓ hepatic glucose output ↑ Glucose use in muscle ↓FFA ↓A1C 1-1.5%

22

Pioglitazone
ADME

4-14 weeks to achieve optimal effect Rapid abs CYP2C/CYP3A4 liver metabolism Biliary excretion

23

Pioglitazone
Adverse

1. Fluid retention: peripheral edema, macular edema, anemia 2. ↑ risk HF 3. Weight gain 4. ↓ Bone density 5. ↑ risk bladder cancer Black Box: rosiglitazone had one then repealed 3 years later

24

Pioglitazone
Contraindications

1. Pregnancy Category C 2. Liver DZ 3. Heart DZ

25

Exenatide
Indications

↑ cAMP: slows gastric emptying, ↑satiety

26

Exenatide
Mechanism

GLP-1 Receptor Agonist
↑ glucose dependent insulin secretion
↓post-prandial glucagon release

27

Exenatide
Advantages

1. Facilitates weight loss and ↓ hepatic fat 2. Potential ↑ beta cell mass (↓ apoptosis) 3. ↓ A1C ~1.5%

28

Exenatide
Adverse

1. GI: N,V&D in 44% pts that ↓ w/ continued use 2. ↓ GI absorption of other Rx 3. Acute pancreatitis

29

Exenatide
Drug-Drug

Risk of hypoglycemia when combined w/ insulin secretagogues

30

Sitaglitpin
Indications

secretagogue: promotes pancreatic insulin secretion

31

Sitaglitpin
Mechanism

DPP4 inhibitor
Cleavage not specific to incretins
1. Prolongs endogenous GLP-1 activation by creating inactive metabolites 2. ↑ glucose mediate insulin secretion 3. ↓ Post prandial glucagon release

32

Sitaglitpin
ADME

Non-protein binding no/minimal hepatic metab renal excretion

33

Sitaglitpin
Advantages

1. Weight neutral 2.↓ A1C 0.5-0.7%

34

Sitaglitpin
Adverse

1. Acute pancreatitis 2. Hepatic failure 3. Hypersensetivity reaction (urticaria, vasculitis) 4. Long term safety unknown

35

Sitaglitpin
Contraindications

Pregnancy category B

36

Sitaglitpin
Drug-Drug

Risk of hypoglycemia in combo w/ insulin secretagogues

37

Acarbose
Indications

Slow digestion of carbs

38

Acarbose
Mechanism

a-glucosidase inhibitor
Facilitates oligo/disaccharide digestion

39

Acarbose
ADME

Take w/ meal

40

Acarbose
Advantages

1. ↓ A1C 0.5-1% 2. ↓post prandial glycemia

41

Acarbose
Adverse

1. GI: Abd pain, farts: alleviated w/ dose titration & cont use 2. ↑ LFTs/Hepatic failure

42

Acarbose
Contraindications

1. Category B in Pregnancy 2. Chronic Intestinal DZ

43

Acarbose
Drug-Drug

Risk of hypoglycemia w/ sulfonylureas / insulin - Tx w/ oral glucose

44

Canagliflozin
Mechanism

PCT Renal SGLT-2 Inhibitor (Na+ dependent)
Inhibition suppresses renal glucose reabs

45

Canagliflozin
Advantages

Metabolized by UDP-GT

46

Canagliflozin
Adverse

1. Genital mycotic infections 2. Long term safety unknown

47

Canagliflozin
Contraindications

Pregnancy Category C

48

Canagliflozin
Drug-Drug

1. Can ↑ serum digoxin levels 2. UDP-GT inducers ↓ blood level: rifampin, phenobarb, phenytoin, ritonavir