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9

Endocrine Learning Objectives

Drug Class

Mechanism of action

Insulin lispro
Insulin aspart
Insulin glulisine

ShortActing Insulins

Short acting insulin


analogues

Bolus dosing

Match carbo content


of meals

Regular insulin

NPH insulin
Insulin glargine

Interme
diate/LongActing Insulins

Insulin detimir

Glipizide
Glyburide
Glimepiride

Nateglinide
Repaglinide

ureas

ides

Sulfonyl

Meglitin

Biguani

Intermediate/long
acting insulin analogues

Basal dosing

Taken regularly
independent of food intake

Bind to the
sulfonylurea receptor
(SUR1), closing the ATPdependent potassium channel
Kir6.2

Depolarizing the cell

Increased insulin
secretion.

Expected decrease in
A1c 1 to 2%

Similar MOA as
sulfonylureas, but shorter
acting. (bolus)

Decrease in A1c 0.5


to 1.5%

1st line drug in obese


pts w DM2

Increases insulin
sensitivity, esp liver.

Pharmacokinetics

Onset in 5-15 min

Duration 2-4 hr

Commonly used in
insulin pumps

Onset in 5-15 min

Duration 2-4 hr

Onset in 30 min

Duration 2-4 hr

Used IV in hospital

2x day dosing

Onset in 2 hr

Duration 18-28 hr

Peak 6-10 hr

1x day dosing

Onset in 2 hr

Duration 20-24 hr

1 or 2x day dosing

Onset in 2 hr

Duration 6-24 hr

Dosed orally once or


twice daily

meal

Short acting.
Dosed orally with each

Adverse effects

Hypoglycemia
Local injection reactions
Weight gain

Contraindications

None

None

Hypoglycemia

Weight gain

Use with caution in elderly,


and in renal and liver failure

Hypoglycemia (mild)

Weight gain (mild)

Use with caution in renal and


liver failure

GI symptoms (metallic taste,

Causes weight loss or is nausea, diarrhea, cramping dose


weight neutral
dependent)

Renal insuff (cr > 1.41.5 mg/dL)

Liver disease, alcohol

10
Endocrine Learning Objectives

Rosiglitazone
Pioglitazone

Thiazoli
dinediones

TZD

Acarbose

aGlucosidase
Inhibitors

Exenatide
Liraglutide

Incretin
Mimetics

Sitaglipin
Saxaglipin

DPP-4
Inhibitors

Glucagon

Agonist @ PPAR g
receptor

Sensitizes skeletal
muscle to insulin

Increased glucose
uptake incr GLUT-4
transporters

Decr hepatic glucose


production

Decrease in A1c 0.5


to 1.4%

Inhibits aglucosidase, delaying


digestion and absorption of
carbs

Decrease in A1c 0.5


to 0.8%

Promotes glucosemediated insulin secr GLP-1


mimetics

Decr hepatic glucose


production

Slows gastric
emptying

Decrease in A1c 0.5


to 1%

Inhibits DDP-4 which


breaks down GLP-1

Incr GLP-1 levels and


insulin secr

Decrease in A1c 0.5


to 0.8%

cAMP, gluconeo &


glycogeno & increased blood
glucose levels

Delayed onset and


offset of action

May take 6-12 weeks to


see peak effect Does not cause

hypoglycemia

Pioglitizone improves
lipid profile

used

Weight gain
Edema/fluid retention
Risk of osteoporosis/fractures

Contra in HF, caution


in LF

Rosiglitizone may be
associated with increased risk of
CV events

Flatulence/diarrhea
Not well tolerated, not widely

Reduces appetite and


improves satiety.

Does not cause


hypoglycemia

May support beta cell


mass/survival

GI symptoms (nausea,
vomiting)

Use with caution in renal


insufficiency

None

None

None

None