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NRS 271B > Diabetes Mellitus Oral Agents > Flashcards

Diabetes Mellitus Oral Agents Flashcards

1
Q

Definition of DM

A
  • abnormal carbohydrate metabolism → hyperglycemia
    • due to relative or absolute impairment of insulin secretion
    • due to peripheral resistance to the action of insulin
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2
Q

What does the Pancreas Produce

A
  • insulin
  • amylin
  • glucagon
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3
Q

Insulin resistance associated with CV risks such as?

A
  • abd obestiy
  • HTN
  • dyslipidemia
  • hypercoag
  • hyperinsulinemia
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4
Q

What cells are located in the Islet of Langerhans?

A
  • Alpha Cells
    • release glucagon
      • increases blood glucose
  • Beta Cells
    • release insulin and amylin
      • decreases blood glucose
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5
Q

Fasting stage: insulin levels

A

43-186pMol/L

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6
Q

Type II DM definition

A
  • 90% of patients
  • partial loss of insulin secretion
    • variable degree of deficiency
  • peripheral insulin resistance
    • mostly in skeletal muscles & liver
      • not responsive to glucose uptake
      • can’t stop hepatic glucose production
  • Present years before dx
  • often asymptomatic
  • hyperglycemia
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7
Q

Type I DM

A
  • 5-10% of pts
  • absolute loss of insulin
    • due to autoimmune beta cell destruction
    • at time of diagnosis = 80-95% have been destroyed
    • Complete insulin dependency
  • Honeymoon period:
    • Days to weeks after diagnosis experience remission
    • Lasts weeks – months
    • May need very low insulin supplementation
  • DKA = initial presentation in 25% of adults
  • genetic link: HLA-DR and HLA-DQ
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8
Q

Vicious cycle of Type II DM

A
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9
Q

Renal Glucose Threshold

A

180 mg/dL

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10
Q

Diagnosis of Diabetes Mellitus WHO & ADA guidelines

A
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11
Q

Medications that Affect Blood Glucose

A
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12
Q

When to Screen for Type II DM: ADA guidelines

A
  • adults without risk factors:
    • start at age 45
    • repeat q 3 yrs
    • more frequent if BMI ≥ 25 plus ≥ 1 risk factor
    • Fasting plasma glucose and A1C preferred over OGTT
  • Children. at 10yo or onset of puberty with:
    • BMI > 85th percentile for age and sex
    • Wt for height > 85th percentile
    • wt > 120% of ideal height
    • plus ≥ risk factors
    • Screen Q 2yrs
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13
Q

Glycemic Goals for DM patients: ADA

A
  • A1C < 7% (normal 4-6%)
  • preprandial plasma gluc: 70-130 mg/dL
  • Postprandial plasma gluc: < 180mg/dL
  • BP < 130/80
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14
Q

Non-Pharm Tx of DM

A
  • Diet:
    • counting carbs
    • reducing trans fat; cholesterol intake < 200mg/day
    • protein – 15-20% of daily caloric intake (animal and vegetables)
    • sodium: + CHF <2g/day
    • alcohol: NTE 2 drink/day; 1 drink = 12 oz of beer, 5oz wine, 1.5 oz of distilled alcohol
  • Exercise:
    • starting goal = 150 min/week
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15
Q

Categories for Oral Antihyperglycemics for DM II & A1C reduction %

A
  • Biguanides: 1.5-2%
  • Sulfonylureas: 1-1.5%
  • Thiazolidinediones (TZD): 1-1.5%
  • Non-sulfonylurea Secretagogues: 0.8-1%
    • (“Glinides” or Meglitinides)
  • SGLT2 inhibitor: 0.8-1%
  • Dipeptidyl Peptidase-4 (DPP-4) Inhibitors: 0.7-1%
  • Alpha-Glucosidase Inhibitors 0.3-1%
  • Bile Acid Sequestrant: 0.4% with metformin
  • Dopamine Receptor agonists: 0.1-0.4%
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16
Q

Sulfonylureas MOA

A

Block the ATP-sensitive K channels on beta cells → insulin secretion

  • first class of PO antihyperglycemic agents approved in US
  • Cross sensitivity with sulfa allergy
  • all require renal adjustment, except tolbutamide
  • hepatic metabolism - 2C9
  • can’t stimulate insulin secretion at extremely high glucose levels (i.e. glucose toxicity)
17
Q

Sulfonylureas 1st generation

A
  • Meds:
    • Chlorpropamide (Diabinese)
      • Avoid in Renal dysfunction or elderly
    • Tolazamide (Tolinase)
    • Tolbutamide (Orinase)
  • SEs:
    • Hypoglycemia
    • weight gain
    • reduce efficacy over time
    • lower A1c by 1-1.5%
    • Not preferred by ADA or AACE
18
Q

Sulfonylureas 2nd Generation

A
  • Meds:
    • Glyburide
      • more hypoglycemia
        • not recommended by ADA
    • Glipizide
      • less weight gain than glyburide
    • Glimepiride
      • less weight gain than glyburide
  • SEs:
    • weight gain
    • hypoglycemia
    • 2nd line tx (ADA) after metformin
    • add on therapy
    • inexpensive
    • start low & slow in elderly
19
Q

Non-Sulfonylurea Secretagogues (Glinides): Overview

A
  • block ATP-sensitive K channels
  • produce same effect as sulfonylureas,
    • but shorter onset & duration
  • bind to receptor adjacent to the sulfonylureas receptor
  • cannot be used together with sulfonylureas
  • Advantage:
    • reduce post-meal gluc level
  • **Lowers A1C 0.8-1%**
  • take 15-30min before meal
20
Q

Non-Sulfonylurea Secretagogues (Glinides): Meds

A
  • Lowers A1C by 0.8-1%
  • Meds:
    • Meglitinide
    • Nateglinide (Starlix)
    • Repaglinide (Prandin) + Metformin (PrandiMet)
      • more effective for lowering A1C than Starlix
  • SEs:
    • weight neutral
    • hypoglycemia
    • 2nd line according to ADA
      • 1st line if metformin contraindicated
  • can use instead of sulfonylureas
  • used in combo with others
21
Q

Biguanide

A

Metformin

lowers A1C by 1.5-2% and FBG by 60-80mg/dL

  • MOA:
    • unclear
    • decreases hepatic glucose production & increases insulin sensitivity → liver, fat, & muscles
    • does not affect insulin release
  • used as monotherapy
  • reduced LDL by 18.7%; TG by 12%
    • increased HDL by 1.2%
  • SEs:
    • GI: N/Diarrhea (=most common)
      • decreased appetite
    • Lactic Acidosis → rare
    • inhibits mitochondrial oxidation of lactic acid
    • Renal impairment elderly :
      • CrCl ≤ 30ml/min
      • hypoxemia, sepsis, dehydration
    • interferes with B12 absorption
      • monitor B12 levels
  • Considerations:
    • withhold tx when pt undergoes surgery or radiocontrast dye
    • renal fxn: assess within 48 hours after procedure → normal → restart
    • avoid in liver disease:
      • Check LFTs
22
Q

Alpha-Glucosidase Inhibitors MOA & Meds

A

lowers A1C by 0.3-1%

  • MOA: delay absorption of carbohydrates (by inhibiting alpha-glucoside at the brush border of the small intestine)
    • →reduce post-prandial BG
    • act as osmotic to draw water into GI lumen
    • pt can skip dose if they skip a meal/do not eat carbs
  • Meds:
    • Acarbose (Precose)
      • not as effective as Miglitol
      • 3rd line – ADA
    • Miglitol (Glyset)
    • **GIVEN WITH MEALS** (BOTH)
  • SEs:
    • GI:
      • flatulence, abd discomfort, diarrhea
  • contraindicated:
    • short bowel syndrome
    • irritable bowel syndrome
    • SCr >2mg/dL
  • Wt neutral
  • take with Meals
23
Q

Dosage of Metformin

A
  • 500mg PO BID or 850mg Qday
  • Max: 2550 mg/day (Glucophage)
  • Max: 2000mg/day (Glucophage XR)
24
Q

Thiazolidinediones: MOA, Considerations, SEs

A

lowers A1C by 1-1.5%; reduce FPG by 60-70mg/dL

aka TZDs or “glitazones”

  • MOA:
    • stimulate peroxisome proliferator-activated receptor gamma (PPAR-gamma) → nuclear receptor
      • increase sensitivity to insulin
      • decrease plasma fatty acid levels
  • Onset: delayed → takes several weeks, up to 12 weeks for max effects
  • SEs:
    • fluid retention
      • increased when combined with insulin tx
      • contraindicated in HF
    • hepatotoxicity – reversible within weeks after d/c
      • check LFTs at baseline & PRN
      • if baseline ALT 2.5x UNL → do not start
      • if ALT 3x UNL after taking TZD → d/c
    • Promotes ovulation → unwanted pregnancy
    • increased incidence of upper & lower limb fracture
    • increases risk of bladder cancer after 1 yr → dose related
      • contraindicated with h/o bladder cancer
    • Weight gain
    • low risk of hypoglycemia
25
Q

Thiazolidinediones: Meds

A

lowers A1C by 1-1.5%

  • Meds:
    • Pioglitazone (Actos)
        • metformin
        • glimepiride
      • +alogliptin
    • Rosiglitazone (avandia)
        • metformin
      • +glimepiride
        • greater risk of MI
  • 2nd line according to ADA
  • SEs:
    • Fluid retention
    • increased ovulation
    • long bone fractures
    • hepatotoxicity
    • bladder cancer
26
Q

Functions of GIP & GLP-1

A
  • GLP-1:
    • increase insulin
    • decrease glucagon
    • decrease Beta cell apoptosis
    • increase beta cell proliferation
  • GIP:
    • increase insulin
    • increase glucagon
    • decrease beta cell apoptosis
    • increase beta cell proliferation
  • DDP-4 enzyme breaks down GLP-1 and GIP
27
Q

DPP-4 Inhibitors (dipeptidyl peptidase-4 inhibitors): MOA, SEs, general info

A

lowers A1C by 0.7-1%

  • MOA:
    • inhibit DDP-4 therefore less GIP & GLP-1 is broken down and more is available
  • General Info:
    • less hypoglycemia
    • weight neutral
    • 2nd line tx
  • SEs:
    • HA
    • nasopharyngitis
    • pancreatitis??
28
Q

DPP-4 Inhibitors: Meds

A

-gliptins

lowers A1C by 0.7-1%

  • Sitagliptin: case report of acute pancreatitis, including hemorrhagic and necrotizing
    • CrCl <50 mL/min → max dose: 50mg/d
    • CrCl <30 mL/min → max dose: 25mg/d
  • Saxagliptin:
    • CrCl <50 mL/min
    • Strong 3A4 inhibitor
  • Linagliptin
    • substrate of 3A4
    • no adjustment needed for renal/hepatic impairment
  • Alogliptin
    • CrCl 30-59: 12.5 mg/day
    • CrCl <30: 6.25mg/day
29
Q

Dopamine Receptor Agonist and DM

A

lowers A1C by 01-0.4%

  • Bromocriptine (Cycloset)
    • unknown MOA
    • AM admin improves insulin sensitivity
    • 3rd line tx
  • SEs:
    • rhinitis/sinusitis
    • HA/dizziness
    • syncope
    • nausea
    • hypotension
  • Contraindications
    • Lactation
    • Syncopal migraine
30
Q

Bile Acid Sequestrant and DM

A

lowers A1C by 0.4% when used with metformin

  • Colesevelam (Welchol)
    • binds to bile acid in GI lumen
    • unclear MOA for lowering glucose
    • lowers LDL by up to 20%
  • SEs:
    • nausea/bloating/constipation
    • increased TGs
    • dyspepsia
  • DDI:
    • prevents absorption of:
      • levothyroxine, OC, phenytoin
      • warfarin, digoxin
      • **separate by 4 hours**
  • Malabsorption of fat-soluble vitamins: A, D, E, K
31
Q

SGLT2 Inhibitor (Sodium-Glucose Co-transporter 2): MOA, general info, SEs

A
  • MOA:
    • reduce reabsorption of filtered glucose
  • benefits:
    • weight loss
    • BP reduction (slight)
    • less hypoglycemia
  • general info:
    • may increase LDL
    • expensive
    • only added onto metformin
  • SEs:
    • renal dysfunction do not use
    • fungal infx of genitals
    • UTI
    • increased urination
    • hypotension
32
Q

SGLT2 Inhibitor: Meds

A
  • “if you use SGLT2 inhibitors you may sucCEED in losing weight”
  • Canagliflozin (Invokana)
      • Metformin (invokamet)
    • Do Not Use if CrCl <45 mL/min
    • may increase risk of stroke
  • Dapagliflozin (Farxiga)
    • +Metformin (Xigduo XR)
    • Do Not Use if CrCl <60 mL/min
    • contraindicated with h/o bladder cancer
    • may increase risk of bladder cancer
  • Empagliflozin (Jardiance)
    • +Linagliptin (Glyxambi)
    • +Metformin (Synjardy)
    • Do Not Use if CrCl <45 mL/min
  • Ertugliflozin (Steglatro)
    • +sitagliptin (Steglujan)
    • +metformin (Segluromet)
    • Do Not Use if CrCl <30 mL/min
33
Q

Glycemic Goals of Tx in DM

A
  • Non-Pregnant:
    • A1C <7%
      • Preprandial BG: 80-130 mg/dL
      • Postprandial BG <180 mg/dL
    • May target A1C <6.5%:
      • DM2 tx with lifestyle mods or metformin only
      • long life expectancy
      • no significant CV disease
      • pregnancy (<6% = optimal without hypoglycemia)
    • May target A1C < 8%
      • H/o severe hypoglycemia
      • Limited life expectancy
      • Advanced micro or macrovascular
      • Complications extensive comorbidities
      • Long standing DM—difficult to achieve
      • Has been on appropriate doses on multiple agents and monitoring
34
Q

Summary of Glucose Lowering Interventions (Chart)

NRS 271B (10 decks)

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