Exam IV - Diabetes Flashcards

1
Q

Insulin

Indications

A

Hyperglycemia

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2
Q

Insulin

Mechanism

A

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

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3
Q

Insulin

ADME

A
  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
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4
Q

Insulin

Advantages

A
  1. Therapy is individualized: multidose regimens, repeated monitoring 2. Now other admin forms: pen, nasal spray
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5
Q

Insulin

Adverse

A
  1. “Dawn effect” - overnight dosing is important 2. Hypoglycemia (
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6
Q

Insulin

Contraindications

A

Pregnancy category B

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7
Q

Metformin (Biguanide)

Indications

A

Insulin sensitizer: blocks glucose release from liver

First line for DMII

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8
Q

Metformin

Mechanism

A

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

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9
Q

Metformin

ADME

A

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

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10
Q

Metformin

Advantages

A
  1. Doesn’t induce hypoglycemia 2. No weight gain 3. Inhibits microvascular complications
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11
Q

Metformin

Adverse

A

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

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12
Q

Metformin

Contraindications

A
  1. Pregnancy Category B 2. Renal & Hepatic Dz
  2. EtOH: lactic acidosis
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13
Q

Glipizide (Sulfonylurea)

Indications

A

Classic secretagogue: promotes pancreatic insulin secretion

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14
Q

Glipizide

Mechanism

A
  1. Binds & blocks ATP sensetive K+ channel β-cell → depolarization → Ca2+ influx
  2. Requires functional β-cells
  3. No effect on insulin resistance / sensitvity
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15
Q

Glipizide

ADME

A

Protein bound liver metab renal excretion

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16
Q

Glipizide

Advantages

A

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

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17
Q

Glipizide

Adverse

A
  1. Hypoglycemia 2. Weight gain
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18
Q

Glipizide

Contraindications

A
  1. Pregnancy Category C 2. Hepatic & renal Dz 3. Caution in elderly pts
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19
Q

Glipizide

Drug-Drug

A
  1. ↑ hypoglycemia: NSAIDS, MAOIs, sulfonamides, chloramphenicol, H2 antihistamines, EtOH 2. ↓hypoglycemia: β-blockers; thiazides, estrogens, rifampin
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20
Q

Pioglitazone (TZD)

Indications

A

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

21
Q

Pioglitazone

Mechanism

A

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

22
Q

Pioglitazone

ADME

A

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

23
Q

Pioglitazone

Adverse

A
  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
Q

Pioglitazone

Contraindications

A
  1. Pregnancy Category C 2. Liver DZ 3. Heart DZ
25
Q

Exenatide

Indications

A

↑ cAMP: slows gastric emptying, ↑satiety

26
Q

Exenatide

Mechanism

A

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

27
Q

Exenatide

Advantages

A
  1. Facilitates weight loss and ↓ hepatic fat 2. Potential ↑ beta cell mass (↓ apoptosis) 3. ↓ A1C ~1.5%
28
Q

Exenatide

Adverse

A
  1. GI: N,V&D in 44% pts that ↓ w/ continued use 2. ↓ GI absorption of other Rx 3. Acute pancreatitis
29
Q

Exenatide

Drug-Drug

A

Risk of hypoglycemia when combined w/ insulin secretagogues

30
Q

Sitaglitpin

Indications

A

secretagogue: promotes pancreatic insulin secretion

31
Q

Sitaglitpin

Mechanism

A

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
Q

Sitaglitpin

ADME

A

Non-protein binding no/minimal hepatic metab renal excretion

33
Q

Sitaglitpin

Advantages

A
  1. Weight neutral 2.↓ A1C 0.5-0.7%
34
Q

Sitaglitpin

Adverse

A
  1. Acute pancreatitis 2. Hepatic failure 3. Hypersensetivity reaction (urticaria, vasculitis) 4. Long term safety unknown
35
Q

Sitaglitpin

Contraindications

A

Pregnancy category B

36
Q

Sitaglitpin

Drug-Drug

A

Risk of hypoglycemia in combo w/ insulin secretagogues

37
Q

Acarbose

Indications

A

Slow digestion of carbs

38
Q

Acarbose

Mechanism

A

a-glucosidase inhibitor

Facilitates oligo/disaccharide digestion

39
Q

Acarbose

ADME

A

Take w/ meal

40
Q

Acarbose

Advantages

A
  1. ↓ A1C 0.5-1% 2. ↓post prandial glycemia
41
Q

Acarbose

Adverse

A
  1. GI: Abd pain, farts: alleviated w/ dose titration & cont use 2. ↑ LFTs/Hepatic failure
42
Q

Acarbose

Contraindications

A
  1. Category B in Pregnancy 2. Chronic Intestinal DZ
43
Q

Acarbose

Drug-Drug

A

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

44
Q

Canagliflozin

Mechanism

A

PCT Renal SGLT-2 Inhibitor (Na+ dependent)

Inhibition suppresses renal glucose reabs

45
Q

Canagliflozin

Advantages

A

Metabolized by UDP-GT

46
Q

Canagliflozin

Adverse

A
  1. Genital mycotic infections 2. Long term safety unknown
47
Q

Canagliflozin

Contraindications

A

Pregnancy Category C

48
Q

Canagliflozin

Drug-Drug

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