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Diabetes Drugs Flashcards

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1
Q

what drug class is metformin and what organs does it target?

A

Biguanide

Targets: liver, muscle, adipose tissue

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2
Q

what is metformin’s MOA?

A

decreases hepatic glucose production and increases insulin sensitivity

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3
Q

metformins A1C lowering?

A

1-2%

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4
Q

when is metformins maximum therapeutic effect?

A

within 2 weeks

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5
Q

what glucose does metformin effect? (FPG or PPG)

A

FPG & PPG (FPG > PPG)

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6
Q

what are the adrs of metformin?

A
  • low hypoglycemia
  • vit B12 deficiency (high dose & chronic use) (REQUIRES PERIODIC TESTING)
  • weight neutral or loss (frail elders)
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7
Q

what are some symptoms of vitamin B12 deficiency and who is at risk?

A
  • cognitive impairment or paresthesias (tingling or numbness)
  • people at risk: elderly, vegetarians, use of chronic PPIs
  • if pt has tingling or numbness could also be diabetic peripheral neuropathy
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8
Q

metformin dosing?

A

titrate over 4 wks to minimize GI effects (start low and go slow)

  • week 1: start 500mg daily
  • week 2: incr to 500mg BID
  • week 3: incr to 500mg in AM and 1000mg in PM
  • week4: incr to 1000mg BID (maximum clinical dose)
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9
Q

if GI effects are bothersome with metformin, what do you do?

A

do slower titration, lower doses, and or d/c

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10
Q

what form of metformin do you consider to minimize GI effects?

A

extended-release (ER) formulation

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11
Q

metformin dose adjustments in renal disease

A
  • Metformin is C/I if eGFR < 30

- do NOT initiate if eGFR ≥ 30-45

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12
Q

if patient is already on metformin:

  • eGFR ≥ 45-60
  • eGFR ≥ 30-45
A
  • eGFR ≥ 45-60 -> continue use, but monitor renal fxn routinely
  • eGFR ≥ 30-45 -> weigh the pros and cons of continued use (routine renal fxn monitoring & consider dose reduction of 50%)
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13
Q

what does metformin reduce in obese its?

A

CV death

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14
Q

what drug class are glyburide, glipizide, & glimeperide?

A

Sulfonylurea

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15
Q

Sulfonylurea drugs

A

glyburide, glipizide, & glimeperide

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16
Q

what organs do sulfonylurea’s target?

A

pancreas

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17
Q

mechanism of sulfonylurea’s?

A

enhance insulin secretion of beta cells (independent of glucose load)

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18
Q

what is the A1c lowering effect of sulfonylurea’s?

A

1-2%

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19
Q

what do sulfonylurea’s require to work?

A

requires functioning beta-cells
*CHECK DISEASE DURATION!
(diabetes for 20-30 years probably won’t have good beta-cell fxn)

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20
Q

what glucose do sulfonylurea’s effect? (FPG or PPG)

A

FPG

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21
Q

when is sulfonylureas max therapeutic effects?

A

max therapeutic effects at 50% max daily dose

-avoid high doses to avoid hypoglycemia

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22
Q

what sulfonylurea should you avoid the use of?

A

Glyburide
-it’s long acting, so has a higher risk of hypoglycemia
(try glipizide or glimeperide)

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23
Q

sulfonylurea adrs?

A
  • HIGH hypoglycemia risk (b/c stimulates pancreas to secrete insulin)
  • limited durability - usually good for 6 months with high secondary failure thereafter
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24
Q

sulfonylurea dosing (max daily dose & max therapeutic dose)?

A

Glyburide:

  • MDD = 10mg BID
  • Max therapeutic dose = 5mg BID

Glipizide:

  • MDD = 20mg BID
  • Max therapeutic dose = 10mg BID

Glimeperide:

  • MDD = 8mg daily
  • Max therapeutic dose = 4mg daily
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25
what drug class are repaglinide and nateglinide?
glinides
26
glinide drugs
repaglinide and nateglinide
27
what organs do the glinides target?
pancreas
28
Glinides MOA?
Enhance insulin secretion of B cells (independent of glucose load) *same as Sulfonylurea
29
what is the A1c lowering effect of glinides?
0.5-1.5%
30
what do glinides require to work?
functioning beta-cells (check disease duration) *same as sulfonylurea
31
what glucose do glinides effect? (FPG or PPG)
PPG | vs SU effect FPG
32
glinide dosing
- multiple daily doses - take before meals *not in ADA algorithm
33
glinide adrs?
- less hypoglycemia than SU | - short duration, rapid onset
34
what drugs are in thiazolidinediones (TZDs) class?
- Pioglitazone | - Rosilglitazone
35
Pioglitazone & Rosilglitazone are in what drug class?
TZDs
36
what organs do TZDs target?
liver, muscle, adipose tissue
37
TZD MOA?
activate PPAR in muscle, liver, fat -> increase glucose transporter expression
38
what is TZD A1c lowering effect?
0.5-1.4%
39
what glucose do TZDs effect? (FPG or PPG)
FPG
40
TZDs are ___ sensitizers
TZDs are insulin sensitizers
41
when are the max therapeutic effects for TZDs seen? why is titrating to max dose not recommended?
8-12 weeks (counsel pts) -titrating to max dose (45 mg/d) is NOT recommended b/c of side effects (edema, weight gain)
42
TZD adrs?
- low hypoglycemia risk - Pioglitazone: edema, weight gain (5-10kg), bone fracture, bladder cancer, macula edema - Rosilglitazone: was associated with CV risk and MI death
43
TZDs have good what and maintain what?
A1c durability | -maintain A1c lowering effect
44
Alpha-glucosidase inhibitor drugs?
- Acarbose | - Miglitol
45
Arcarbose & Miglitol are in what drug class?
Alpha-glucosidase inhibitor
46
Alpha-glucosidase inhibitor MOA?
inhibit enzymes in small intestine that digest carbs -> delay carb absorption & inhibit breakdown of dietary carbohydrates
47
what organs do Alpha-glucosidase inhibitor target?
GIT (small intestine)
48
A1c lowering effect of Alpha-glucosidase inhibitor?
0.5-0.8%
49
what glucose do Alpha-glucosidase inhibitor effect? (FPG or PPG)
effect PPG
50
when are Alpha-glucosidase inhibitor most effective?
most effective if diet contains large amounts of CHO | -watch for diet changes/low CHO diets
51
Alpha-glucosidase inhibitor dosing?
requires multiple daily doses - must be present in gut to exert its effects - max therapeutic effects are 1 hour after eating * take 30-60min before eating, so in gut before eating * not in ADA algorithm
52
Alpha-glucosidase inhibitor and titrating
tirate over 4-8 weeks to minimize GI side effects | -poor tolerability -> not used often clinically
53
Alpha-glucosidase inhibitor adrs?
- FLATULENCE - bloating - poorly tolerated
54
what drugs are in DPP-4 inhibitor class?
- sitagliptin - saxagliptin - linagliptin - alogliptin
55
Sitagliptin, saxagliptin, linagliptin, alogliptin are in what drug class?
DPP-4 inhibitors
56
DPP-4 inhibitors MOA
(sitagliptin, saxagliptin, linagliptin, alogliptin) - Inhibit enzyme responsible for breakdown of GLP-1 * GLP-1 promotes insulin secretion (dependent on glucose)
57
what is the A1c lowering effect of DPP-4 inhibitors?
(sitagliptin, saxagliptin, linagliptin, alogliptin) 0. 5-0.8% - modestly effective at lowering A1c b/c T2DM pas already have less endogenous GLP-1 hormone
58
what glucose do DPP-4 inhibitors effect? (FPG or PPG)
(sitagliptin, saxagliptin, linagliptin, alogliptin) effect PPG
59
DPP-4 inhibitor max therapeutic effects are when?
(sitagliptin, saxagliptin, linagliptin, alogliptin) -max therapeutic effects within 2 weeks
60
DPP-4 inhibitor adrs?
(sitagliptin, saxagliptin, linagliptin, alogliptin) - weight neutral - well-tolerated - low hypoglycemia risk
61
DPP-4 inhibitor dosing
may need to reduce dose of SU if given in combination | -b/c SU's also help to stimulate insulin secretion
62
what drugs are in SGLT-2 inhibitor class?
- canagliflozin - empagliflozin - dapagliflozin
63
canagliflozin, empagliflozin, dapagliflozin are in what drug class?
SGLT-2 inhibitors
64
what organ DPP-4 inhibitors target?
(sitagliptin, saxagliptin, linagliptin, alogliptin) -target GIT
65
what organ do SGLT-2 inhibitors target?
(canagliflozin, empagliflozin, dapagliflozin) -target kidneys
66
SGLT-2 inhibitors MOA
(canagliflozin, empagliflozin, dapagliflozin) - inhibit SGLT-2 in kidney, increase urinary glucose excretion * SGLT-2 normally reabsorbs glucose in kidney
67
what is the A1c lowering effect of SGLT-2 inhibitors?
(canagliflozin, empagliflozin, dapagliflozin) 0.5-0.8%
68
can you use SGLT-2 inhibitors at any point in disease?
(canagliflozin, empagliflozin, dapagliflozin) YES! they are useful for all durations of diabetes (but are expensive) -not dependent on beta cell for efficacy
69
what glucose do SGLT-2 inhibitors effect? (FPG or PPG)
(canagliflozin, empagliflozin, dapagliflozin) effect FPG
70
SGLT-2 inhibitors adrs?
(canagliflozin, empagliflozin, dapagliflozin) - weight loss (b/c peeing out sugars) - low risk of hypoglycemia - UTI risk & genital infections - decreased BP (check for volume depletion & routinely monitor BP) - risk of amputations - acute kidney injury (AKI)
71
what do you need to routinely monitor for SGLT-2 inhibitors?
(canagliflozin, empagliflozin, dapagliflozin) -routinely monitor BP & check for volume depletion b/c decreases BP
72
if a pt has a hx of recurrent UTIs, can you give them SGLT-2 inhibitors?
probably wouldn't want to b/c one of their adrs is increased risk of UTIs
73
what drug class is colesevelam in?
bile acid sequesterant
74
what organs does colesevelam effect?
GIT, liver?
75
colesevelam A1c lowering effect?
0.3-0.5%
76
colesevelam adrs & DDIs?
- bad GI (poorly tolerated) - no weight effect - lowers LDL but may incr TG DDIs: warfarin, levo, phenytoin, digoxin, fat vitamins - A, D, E, K (take interacting meds 4 hours prior to administering colesevelam) *not in ADA algorithm
77
when do you take interacting meds when also taking colesevelam? what are the interacting meds?
take interacting meds 4 hours prior to administering colesevelam Interacting meds are: warren, levo, phenytoin, digoxin, fat vitamins - A, D, E, K
78
what drug class is bromocriptine in?
dopa agonist
79
what drug is a dopa agonist?
bromocriptine
80
what organs does bromocriptine target?
brain, muscle, adipose?
81
bromocriptine A1c lowering effect?
0.1-0.4%
82
bromocriptine adrs?
- N/V - HA, dizziness *not in ADA algorithm
83
what drugs are in GLP-1 agonist class?
- exenatide - liraglutide - abiglitide - dulaglitide - liexenitide
84
exenatide, liraglutide, abiglitide, dulaglitide, liexenitide are in what drug class?
GLP-1 agonists
85
what organs do the GLP-1 agonists target?
(exenatide, liraglutide, abiglitide, dulaglitide, liexenitide) -GIT, brain, liver, pancreas (beta-cells)
86
GLP-1 agonists MOA?
(exenatide, liraglutide, abiglitide, dulaglitide, liexenitide) - enhance glucose dependent insulin secretion - slow gastric emptying - increase satiety - suppress post-prandial glucagon release - suppress hepatic glucose production
87
what is the A1c lowering effect of GLP-1 agonists?
(exenatide, liraglutide, abiglitide, dulaglitide, liexenitide) 0.5-1.6%
88
what glucose do the GLP-1 agonists effect?
(exenatide, liraglutide, abiglitide, dulaglitide, liexenitide) short-acting effect PPG more long-acting effect FPG more
89
GLP-1 agonists adrs?
(exenatide, liraglutide, abiglitide, dulaglitide, liexenitide) - weight loss of ~2-4kg over 12 wks - low hypoglycemia risk
90
what are GLP-1 agonists approved to be used with?
(exenatide, liraglutide, abiglitide, dulaglitide, liexenitide) most are approved to be used with basal insulin -no approval for use with prandial insulin
91
administration of GLP-1 agonists?
injectables only | -not good for needle phobia
92
exenatide dosing
(GLP-1 agonist) daily: BID, short-acting (PPG coverage) weekly: long-acting & extended release
93
liraglutide dosing
(GLP-1 agonist) daily: long-acting (FPG > PPG coverage)
94
lixisenatide dosing
(GLP-1 agonist) daily: short-acting (PPG coverage)
95
dulaglutide dosing
weekly: long-acting (FPG)
96
albiglutide dosing
weekly: long-acting (FPG)
97
which GLP-1 agonists are good for patients that are non-adherent?
- exenatide ER - dulaglutide - albiglutide weekly dosing & long acting
98
what drug is in the amylin analogue class?
pramlintide
99
pramlintide is in what drug class?
amylin analogue
100
amylin analogue MOA?
(pramlintide) - slows gastric emptying - increases satiety - suppresses post-prandial glucagon release - suppresses hepatic glucose production
101
amylin analogue A1c lowering effect?
(pramlintide) 0.5-1%
102
what organs does the amylin analogue effect?
(pramlintide) -GIT, liver, brain
103
what glucose does the amylin analogue effect? (FPG or PPG)
(pramlintide) -effects PPG
104
what MUST the amylin analogue be used with?
(pramlintide) must be used with intensive insulin regimens (basal-bolus)
105
amylin analogue dosing?
(pramlintide) -reduce dose of bolus insulin by 50% to avoid hypoglycemia (risk is higher in T1DM vs T2DM b/c T2 is insulin resistant and T1 is insulin sensitive) - requires multiple daily doses * not in ADA algorithm
106
what does amylin analogue work to complement?
(pramlintide) -works to complement the action of insulin
107
amylin analogue adrs?
- injection - expensive - high risk of hypoglycemia if don't reduce dose of bolus insulin by 50%
108
when do you intensify regimen?
- every 3 months until glycemic goals are met | - start at low doses and titrate until max doses or max tolerated doses are reached before intensifying
109
what medication is usually kept on board even when transitioning over to insulin therapy?
metformin is usually kept on board to reduce weight gain from insulin
110
what combinations of drugs should you avoid?
SU + glinide -duplicate MOA (increased risk of hypoglycemia, increased beta-cell "burnout" GLP-1 + DPP-4 inhibitor - some overlap w/MOA - GLP-1 agonist does everything a DPP-4 inhibitor does (and more) and is more eficacious
111
what drugs should you consider using in patients with CVD?
- liraglutide - empagliflozin - canagliflozin - metformin (obese patients)
112
what drugs should you consider avoiding or use with caution in patients with CVD?
- saxagliptin/alogliptin (incr hospitalizations for HF) - TZDs (increased risk of HF) - SU? (conflicting data)
113
what medications need to be avoided or dose reduced in renal disease?
- metformin - SUs (especially glyburide) - DPP-4 inhibitors (except linagliptin) - exenatide, exenatide ER - SGLT-2 inhibitors
114
canaglifozin dosing - usual dose - renal dosing - other renal notes
Usual dose: 100 or 300mg daily Renal dosing: eGFR 45-59 give 100mg daily -AVOID if eGFR < 45 Renal notes: AKI reported (requiring dialysis) -monitor for: edema, decreased urine production
115
empagliflozin dosing - usual dose - renal dosing - other renal notes
Usual dose: 10 or 25mg daily Renal dosing: AVOID if eGFR < 45 Renal notes: reduction in AKI
116
dapagliflozin dosing - usual dose - renal dosing - other renal notes
Usual dose: 5 ot 10 mg daily Renal dosing: AVOID if eGFR < 60 Renal notes: AKI reported (requiring dialysis) -monitor for: edema, decreased urine production
117
when should you avoid the use of canaglifozin in terms of eGFR?
avoid if eGFR < 45
118
when should you avoid the use of empagliflozin in terms of eGFR?
avoid if eGFR < 45
119
when should you avoid the use of dapagliflozin in terms of eGFR?
avoid if eGFR < 60
120
what medications have the highest risk of hypoglycemia (monotherapy)?
- insulin - SUs - glinides (less than SUs) - amylin analogue
121
how do you reduce the risk of hypoglycemia when using insulin?
use rapid & long or ultra-long acting analogues
122
how do you reduce the risk of hypoglycemia when using SUs?
take with food | *avoid glyburide!
123
how do you reduce the risk of hypoglycemia when using glinides?
take with food
124
how do you reduce the risk of hypoglycemia when using amylin analogue?
reduce dose of bolus insulin by 50%
125
what increases when anti diabetic drugs are used in combo?
risk of hypoglycemia increases when any of the anti diabetic drugs are used in combo - Monitor! - consider dose reduction if needed
126
is age a C/I for use of any anti diabetic agent?
no
127
if older in age, what should you watch for/monitor/be careful of?
- watch for agents that cause hypoglycemia - monitor renal function - be careful of medications that can cause weight loss
128
what medications cause weight loss?
- GLP-1 agonists - Amylin analogue - SGLT-2 inhibitors
129
what medications are weight neutral?
- metformin - DPP-4 inhibitors - alpha-glucosidase inhibitors
130
what medications cause weight gain?
- TZDs - SUs - Glinides - Insulin
131
what medications come in generic form?
- metformin - SUs - glinides - TZDs - AGIs *insulin glargine U-100 (Basaglar is not "generic", but is a lot cheaper than Lantus*
132
what medications come in brand form?
- DPP-4 inhibitors - SGLT-2 inhibitors - GLP-1 agonists - Amylin analogue - Insulin (basal, bolus, inhaled)
133
what medications are SQ injectables?
- GLP-1 agonists - Amylin analogue - Insulin (Basal, bolus) *all others are oral*

Therapeutics (6 decks)

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