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Diabetes Medications Flashcards

1
Q

Thiazolidienediones Tzdx MOA

A

Peroxisome proliferator-activated receptor-gama (PPAR-Gamma receptor ligand

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2
Q

PPAR-gamma receptors actions

A

Nuclear hormone receptor
Transcription factor
Glucose and lipid metabolism gene regulation

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3
Q

PPAR-gamma endogenous ligand

A

oxidized fatty acids

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4
Q

Current available Tzds

A

Rosiglitazone (Avandia)

Pioglitazone (Actos)

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5
Q

Tissue with largest ppar-gamma receptor

A

Adipose

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6
Q

activation of ppar-gamma in adipose

A

Decreased release of FFA –> reduced insulin resistance
Decreased TNF-alpha
–> reduced inflammatin
–> reduced TNFalpha dependant insulin resistance

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7
Q

Secondary actions of Tzds

A

Increased insulin dependant glucose uptake in muscle (skeletal)
Due to decreased FFA

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8
Q

Tzd adverse effects (Chronic Use)

A

**Heart failure (increased blood volume)
PPAR-gamma –>increased renal fluid retention
Contraindicated with patients at risk for heart failure

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9
Q

Pioglitazone (Actos) Addition effects

A
  • Slight reduction in plasma triglycerides and increase in HDL-cholesterol levels
  • -> Dual effect on PPAR-alpha and gamma
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10
Q

Rosiglitazone (Avandia) and triglycerides/HDL levels

A

No such effect shown. Not ppar-alpha

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11
Q

Metformin (Glucophage) Mechanism of Action

A

Increase AMPK activity

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12
Q

What does AMPK activity do?

A

Reduces Gluconeogenesis
Stimulates glucose uptake in skeletalmuscle
–>Increased glut4 transporters on membrane
–>Increases insulin sensitivity
Reduces Intestinal glucose absorption

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13
Q

Metformin and normal glycemia

A

Decreased effect

At low insulin levels, glut4 moves from cell membrane to intracellular vesicles

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14
Q

Metformin and insulin release

A

no effect

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15
Q

First line T2DM

A

Metformin

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16
Q

Metformin advantages

A 
No increase in plasma insulin
--> low hypoglycemia risk
Persistent efficacy (2-5 years)
Positive lipid profile
--> decreased TGs, LDL, and increased HDL
-->lower risk of CVD
Unlikely to gain weight
Delays DM progression
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17
Q

Metformin Adverse Effects

A

GI NVD, decreases w/ food
Lactic acidosis BBW

Renal failure (sub 50ml/min) –> Metformin overdose –> lactic acidosis

Contraindicated with tissue anoxia

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18
Q

Metformin counseling point

A

Take with food

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19
Q

Metformin DDI

A 
No plasma protein binding
excreted unchanged in the urine
renal tubular secretion
OCT 2
Cationic drugs compete for transport
**Dose adjustment recommended with concurrent cationic meds: Cimetidine, furosemide, nifeedipine
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20
Q

Sulfonylureas: Insulin Secretagogue MOA

A

Bind and inhibit K-ATP

  • -> cell membrane depolarization
  • -> voltage-gated CA2+ channels open
  • -> release of preformed insulin

**No increase in insulin production

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21
Q

Sulfonylureas Prolonged administration

A

Reduced hepatic glucose production
Enhansed insulin sensitivity
–> increased insulin receptor expression
–> increased insulin receptor signaling

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22
Q

1st generation Sulfonylureas (Drugs)

Rarely used

A

Tolbutamide (Orinase)
Tolazamide (Tolinase)
Chloropropamide (Diabinese)

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23
Q

1st gen sulfonylurea duration and primary side effect

A

Long acting

High incidence of hypoglycemia (particularly at night)

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24
Q

2nd gen sulfonylureas

Selling points

A

More Potent, fewer adverse effects

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25
2nd gen sulfonylureas | PK/PD & interactions
High plasma protein binding; effective dose | Elimination: Major elimination by hepatic metabolism, minor renal excretion
26
2nd gen sulfonylureas | Dosing
Same time every day, with breakfast Start with low dose Increase 1-2.5 mg/day every 1-2 weeks based on BG
27
2nd gen sulfonylureas | Drugs
Glyburide (Micronase, Diabeta) Micronized glyburide tablets (Glynase PresTab) Glipizide (Glucotrol) Glimepiride (Amaryl)
28
``` Glyburide (Micronase, Diabeta) Duration Doseing Bioavailability Elimination ```
~24 h QD or BID Poor and variable bioavailability Eliminated by liver, partially liver
29
Micronize glyburide tablets (Glynase PresTab) Tpeak compared Bioavailability Bioequivalent, result?
Quicker Tpeak improved and consistent bioavailability Not bioequivalent, must re-titrate dose
30
``` Glipizide (Glucotrol) Half life Duration of action, result Tabsoprtion/bioavailability Elimination ```
~3 h t1/2, shortest ~12 h duration, less hypoglycemia rapid absorption, consistent bioavailability Primarily Liver, minor renal
31
Glucotrol XL
Extended-release glipizide, more hypoglycemia
32
``` Glimepiride (Amaryl) Half-life Duration Dosing Elimination ```
10 h t1/2 24 h duration Once daily dosing Primarily liver, partly renal clearance
33
Glimepiride (Amaryl) compared to Glyburide (Micronase, Diabeta)
Equivalent in controlling hyperglycemia Lower plasma insulin and C-peptide values Increased glucose uptake
34
Temporal changes in plasma insulin levels with sulfonylurea treatment
Initial: increased fasting and respons insulin levels Chronic (>1yr): Insulin levels decrease below original levels; downregulation of sulfonylurea cell surface receptors **Reduction of plasma glucose levels are maintained
35
Sulfonylurea long term effectiveness
Develop hyperglycemia >1yr | Results from progressive beta cell failure
36
Sulfonylurea contraindications
T1DM, pregnancy, severe hepatic or renal dysfunction
37
Sulfonylurea Adverse Effects
Late postprandial or fasting hypoglycemia Most common with longer-acting in class Caution in Hepatic impairment --> dose adjustment Caution in Renal impairment **Weight Gain**
38
Sulfonylurea DDIs
Ethanol increases action Plasma protein binding displaced by other drugs Nonselective beta-blockers mask symptoms of hypoglycemia Hyperglycemia inducing drugs: lower effectivenes (Diuretics, HTCZ and beta blockers propanolol)
39
Meglitinide names | Secretagogues
Repaglinide (Prandin) | Nateglinide (Starlix)
40
Repaglinide and Nateglinide MOA
Selectively blocks beta cell Katp
41
Repaglinide and Nateglinide PK
``` Rapid onset ~30 min Peak ~1h t0.5 ~1h Take 5 min pre meal restores insulin release Less effect in normal glycemia ```
42
Thiazolidinedione PK
Well absorbed from GI, No food effect | Metabolized by liver (Cyp2C8)
43
Thiazolidinedione Adverse Effects and Contraindications
Fluid retention Weight Gain Heart Failure
44
Which Drug Class(es) are useful in pt with renal insufficiency
``` Thiazolidinediones Metformin (down to 50 ml/min) ```
45
Incretin Effect
Control: Larger increase in insulin secretion with Glc PO compared to IV - In T2DM, small increase
46
GLP-1 and GIP | MOA
Increase AC --> inPKAcrease cAPM --> Amplified Glucose effect and insulin secretion (requires some level of Glc to be effective)
47
Why didn't GIP work as therapy?
Increased glucagon release = negated effect
48
Effects of GLP1
- Increased proinsulin transcription - Increased insulin biosynthesis - Direct stimulation of secretion - promotes satiety *Inhibition of Glucagon secretion
49
Effect of GLP1 decreased GI motility
Lowers post prandial glucose spike
50
GLP-1 Given IV
Normalizes Fasting and post prandial insulin secretion
51
How is GLP-1 deactivated in blood?
dipeptidyl peptidase IV (DPP-4)
52
Exenatide (Byetta) Structure and function
53% homology to GLP1, but not metabolized by DPP-4 * Glucose-dependent insulin secretion * Delayed GI, Reduced Glucagon, satiety
53
``` Exenatide PK Clearance Half life Dosing interval Extended release ```
-Entirely renal (No use
54
Exenatide immune reaction
Antibody development in 6-12%
55
Liraglutide (victoza) Structure
97% homology to GLP1 AA subs, with fatty acid to bind albumin -->extends t1/2 and prevents peptidase breakdown
56
albiglutide (Tanzeum) Structure
Recombinant protein: 2 copies of human GLP-1, covelantly fused to human albumin AA subs --> DPP-4 resistant, Albumin--> 5 days (1/week dosing
57
Liraglutide (Victoza) Dosing
SC QD independent of meals
58
Dulaglutide (Dulaglutide) Structure
2 Recombinant, disulfide linked chains of GLP-1 analog fused to h-IgG AA subs --> dpp4 resistant IgG ~5d (1/week dose)
59
DPP-4 inhibitors MOA (direct)
complete and long-lasting inhibition of dpp-4
60
DPP-4 inhibitor MOA downstream
Increase conc. GIP and GLP-1 - >increased insulin secretion - >Reduced glucagon levels - >Improvements in both fasting and postprandial hyperglycemia
61
DPP-4 inhibitor adverse effect
Rare
62
DPP-4 inhibitor Eg,
Sitagliptin (Januvia) Saxagliptin (Onglyza) Alogliptin (Nesina) Linagliptin (Tradjenta)
63
DPP-4 inhibitor administration
QD PO without regard to meals
64
DPP-4 inhibitor interactions
Additive effect with metformin, thazolidinediones, sulfonylureas, or insulin
65
What do DPP-4 inhibitors lack that GLP-1 analogs have?
- Delayed Gastric Emptying - Decreased food intake - Decreased weight - N/V side effects
66
Alpha-glucosidase inhibitor examples
Acarbose (precose) | Miglitol (Glyset)
67
Alpha glucosidase inhibitor MOA
inhibits metabolism of sucrose to Glc and Fru --> delays absorption of monosaccharides --> blunts rate post prandial glucose spike
68
Alpha-glucosidase approved use
T2DM as monotherapy and in combo with Sulfonylureas
69
AGluI counseling point
Diarrhea | Treat hypoglycemia with glucose, not sucrose
70
Pramlintide (SymlinPen)
Synthetic analog of amylin
71
Pramlinitide | MOA
Binds amylin receptors in brain: - >reduces glucagon release - >Delays GI emptying - >Produces satiety
72
Pramlintide | Use and Admin
T1 and T2 DM - Immediatly before eating - adjunct to insulin -->retitrate insulin
73
Pramlintide ADR
Hypoglycemia when used with insulin; particularily with T1DM

Endocrine (6 decks)

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