DM drugs Flashcards

1
Q

Metformin

(Glucophage)

A
  • first line for T2DM
  • -Dosing: 500mg-2000mg/day
  • Max CLINICAL dose: 2000mg/day (1000mg PO BID)
  • BBW : Lactic Acidosis
  • Common ADE: diarrhea (self-limiting), cramping, nausea, taste disorder
  • Take with food
  • XR should be used in patients that don’t tolerate IR with BID dosing
  • D/C prior to iodinated contrast procedures
  • potential B12 deficiency
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2
Q

Metformin MOA

A

**suppression of hepatic glucose production

** ↑ insulin-mediated muscle glucose uptake

**↑ intestinal glucose utilization

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3
Q

Sulfonylurea (2nd) generation

A
  • Glimepiride (Amaryl)
  • Glipizide (Glucotrol, Glucotrol XL)
  • Glyburide (Diabeta)
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4
Q

Sulfonylurea (2nd) generation

A
  • -Take 30 min prior to meals
    • Test G6PD deficiency for hemolytic anemia
  • -Prolong use may result in worsening beta cell function (“beta cell burnout”
  • -Not effective in pt with long duration of T2DM
    • Glimepiride (Amaryl)- preferred in liver dysfunction
    • Glipizide (Glucotrol) – preferred in renal insufficiency (short t1/2)
  • -Rapid onset of action/shorter durability vs. metformin
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5
Q

Sulfonylurea (2nd) generation MoA

A

** Close 𝐾𝐴𝑇𝑃channels on beta cell plasma membranes

Physiologic action:

**↑ insulin secretion

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6
Q

TZD

A
  • Pioglitazone (Actos)
  • Rosiglitazone (Avandia)
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7
Q

TZD

A
  • -Take with or without food
  • -BBW: may cause or worsen heart failure
  • -CI in patients with class III/IV HF
  • -ADE: fluid retention, peripheral edema, weight gain, risk of bone fracture/atypical fracture
  • -Onset: 3 weeks (long onset of action)
  • -d/c if signs of hepatitis, AST/ALT > 3x normal
  • -Monitor: AST/ALT, visual exam
  • -check LFT Q3-6 months
  • -Bladder cancer (pioglitazone)
  • -↑ LDL cholesterol (rosiglitazone)
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8
Q

TZD MoA

A
  • activates the nuclear transcription factor PPAR-y (gamma)
  • Physiologic action: ↑ insulin sensitivity
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9
Q

DDP-4 inhibitors

A
  • Sitagliptin (Januvia)
  • Saxagliptin (Onglyza)
  • Linagliptin (Trajenta)
  • Alogliptin (Nesina)
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10
Q

DDP-4 inhibitors

A
    • Start sitagliptin at 100mg PO daily (25mg and 50mg are renal dose, no need for titration)
  • -Not associated with hypoglycemia or weight gain
  • -Monotherapy when metformin is CI or in dual/triple tx
  • -ADE: nasopharyngitis, pancreatitis, upper respiratory infection, HA, joint pain
  • -Saxagliptin, linagliptin-preferred in severe hepatic failure
  • -linagliptin- no renal adjustment required
  • -DO not combined with GLP-1 receptor inhibitors
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11
Q

DDP-4 inhibitors MOA

A
  • MOA: inhibit DDP-4 activities
  • Physiologic action:
    • ↑ postprandial incretin (GLIP-1) concentration
    • ↑ insulin secretion and ↓ glucagon secretion (glucose dependent)
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12
Q

GLP-1 receptor agonist

A
  • Long acting
    • Exenatide extended release (Bydureon), Liraglutide(Victoza), Dulaglutide (Trulicity)
    • Semaglutide (Ozempic)
  • Short acting
    • Exenatide (Byetta)
    • Lixisenatide (Adlyxin)
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13
Q

GLP-1 receptor agonist

A
  • – Take within 60 minutes prior to a meal
  • –ADE: Nausea (40-44%) diarrhea, vomiting, constipation (slow gastric emptying)
  • -Not recommended in combination with SGLT-2 or bonus insulin
  • –GLP-1 decrease FBG, PPBG, weight, and insulin requirement when combined with basal insulin or bonus insulin (not FDA approved, but clinically safe and effective- 2016 ACCP GLP-1 addon to bolus insulin)
  • –BBW: thyroid C-cell tumors
  • –Precaution: risk of acute pancreatitis
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14
Q

GLP-1 receptor agonist MOA

A
  • Activated GLP-1 receptor
  • Physiologic action:
    • ↑ insulin secretin (glucose dependent)
    • ↓ glucagon secretion (glucose dependent)
    • slow gastric emptying
    • ↑ satiety
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15
Q

SGLT-2 inhibitors

A
  • Canagliflozin (Invokana)
  • Dapagliflozin (Farxiga)
  • Empagliflozin (Jardiance)
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16
Q

SGLT-2 inhibitors

A
  • -↓ body weight 1.6-2.8kg, ↓ SBP 3.6- 5.1mm Hg
  • -Drink plenty of water to prevent dehydration
  • -Difference in efficacy (glycemic control) between empagliflozin 10mg and 25mg is < 1%
  • BBW: risk of AMPUTATION (canagliflozin)
  • -Risk of bone fractures (canagliflozin)
    • DKA risk (all agents, rare in T2DM)
    • Genitourinary infections
  • -Risk of volume depletion, hypotention
  • -↑ LDL cholesterol
  • CVD benefit: Empagliflozin > canagliflozin (no CVD benefit in dapagliflozin)
17
Q

SGLT-2 inhibitors

A
  • MOA: inhibit SGLT-2 in the proximal nephron
  • Primary physiologic actions:
    • Blocks glucose reabsorption by the kidney
    • ↑ glucososuria
18
Q

ASCVD benefits

A

liraglutide > semaglutide > exenatide ER

19
Q

Weight lost:

A

semaglutide > liraglutide > dulaglutide > exenatide > lixisenatide

20
Q

“ DO NOT USE” combinations

(due to therapy duplications)

A
  • SU + meglitinide
  • GLP-1 RA + DDP-4 inhibitors
  • Two basal/intermediate insulins
  • Two rapid/short-acting insulins
  • SU/meglitinide + rapid/short-acting insulin
21
Q
A