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75 Cards in this Set
- Front
- Back
- 3rd side (hint)
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Insulin Release:
Activators, inhibitors |
Activated by: Glucose, β2 agonists [other sugars, AA's, FA's, ketones & vagal stim]
Inhitibited by α2 agonists (SNS activating conditions: hypoxia, hypothermia, surgery, severe burns) |
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Actions of Insulin
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Glucose uptake into SkM & Cardiac Muscle, Adipose & WBC's
Inhibits catabolic processes, induces anatolism Upregulates GLUT4 channels in muscle in adipose NB: affinity of GLUT4 higher than affinity of GLUT2 in β cells not req'd for transport into brain, liver & RBC's injected insulin will ↓ [glucose], [phosphate], [K+] ↑ [pyruvate], [lactate] |
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[Glucose Transporters]
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GLUT2: β cells 15
GLUT4: 5, inducable on muscle & adipose by insulin GLUT1: Brain 1mmol/L affinity GLUT3: Brain <1 GLUT5: Fructose Absorption in Gut & Kidney (2 mmol) |
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Insulin Adverse Reactions
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HYPOGLYCEMIA: SSx disappear after repeated events!
[Local allergy to injected protin Lipodystrophy & lipohypertrophy at injx sites IR Rx interactions] |
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Metabolism of Inssulin
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liver and kidney hydrolyze disulfide bonds
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Hypoglycemia
Causes, Tx |
Causes fairly obvious slide 20, include alcohol
Tx: 50-100 ml 50% glucose IV w/ 0.5-1 mg glucagon injx |
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Allergic reactions to insulin
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mostly local
may presist for days inflam & infx from unhygenic technique/impurities |
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Factors that increase insuline requirement
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[Nothing bolded on this slide]
↑ metabolic activity: Fever, thyrotoxicosis, pregnancy, states of stress, surgery, trauma, infx, etc Acromegacly (excessive GH) Cushings: excessive adrenocortical hormone Altered sensitivity of muscle &adipose: ie IR |
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Duration of insulin preparations
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rapid acting: lispro, aspart, glulisine --OK for IV
Regular Intermediate: NPH, Isophane Long acting: |
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Sulfonylurea
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block K+ channel on β cells → depolarize → ↑ insulin release
weight gain, 20% non-responders, ↓ efficacy w/ time hypoglycemia -- esp ↑λ or interaxn w/ other Rx's Contrad: severe renal/hepatic dz, [sulfa allergy relative] 1st gen: Tolbutamide, Chlorpropamide, Tolazamide ie Orinase, Diabinese, Tolinase 2nd gen: Glyburide, Glipizide, Glimepiride ie Micronase, Glucotrol, Amaryl |
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Tolbutamide
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Orinase: 1st gen SU
special for being safest in the elderly; [shortest λ at 4h] |
Sulfonylureas: block β cell K+ channels → depolarize → ↑ insulin release
weight gain, 20% non-responders, ↓ efficacy w/ time hypoglycemia -- esp ↑λ or interaxn w/ other Rx's Contrad: severe renal/hepatic dz, [sulfa allergy relative] |
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Chlorpropamide
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Diabinese: 1st gen SU
special for long (32h) λ & disulfiram-like effect |
Sulfonylureas: block β cell K+ channels → depolarize → ↑ insulin release
weight gain, 20% non-responders, ↓ efficacy w/ time hypoglycemia -- esp ↑λ or interaxn w/ other Rx's Contrad: severe renal/hepatic dz, [sulfa allergy relative] |
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Tolazamide
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A first generation sulfonylurea with no strikingly unique features
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Sulfonylureas: block β cell K+ channels → depolarize → ↑ insulin release
weight gain, 20% non-responders, ↓ efficacy w/ time hypoglycemia -- esp ↑λ or interaxn w/ other Rx's Contrad: severe renal/hepatic dz, [sulfa allergy relative] |
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Oral Insulin Agents
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Seems like there should be a lot more about these guys; make sure this is all right.
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Glyburide
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Micronase: 2nd Gen SU
special for 24h effect (like Glimepiride), far greater risk of hypoglycemia than Glimepiride |
Sulfonylureas: block β cell K+ channels → depolarize → ↑ insulin release
weight gain, 20% non-responders, ↓ efficacy w/ time hypoglycemia -- esp ↑λ or interaxn w/ other Rx's Contrad: severe renal/hepatic dz, [sulfa allergy relative] |
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Glipizide
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Glucotrol: 2nd Gen SU
special short (3h) λ → least likely to cause hypoglycemia |
Sulfonylureas: block β cell K+ channels → depolarize → ↑ insulin release
weight gain, 20% non-responders, ↓ efficacy w/ time hypoglycemia -- esp ↑λ or interaxn w/ other Rx's Contrad: severe renal/hepatic dz, [sulfa allergy relative] |
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Glimepiride
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Amaryl: 2nd Gen SU
special for 24h effect (like Glyburide), far less risk of hypoglycemia than Glyburide |
Sulfonylureas: block β cell K+ channels → depolarize → ↑ insulin release
weight gain, 20% non-responders, ↓ efficacy w/ time hypoglycemia -- esp ↑λ or interaxn w/ other Rx's Contrad: severe renal/hepatic dz, [sulfa allergy relative] |
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Meglitinides
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aka "Glinides" Repaglinide (Prandin), Nateglinide (Starlix)
Glinides best for pt w/ good FS, bad post-prandial control block β cell K+ channels → depolarize → ↑ insulin release rapid onset/short acting(1hλ) → take orally <1h before eating; hypoglycemia for sure if ∅ food vs. SUs: ↓ weight gain, ✓ in ∅-sulfa-pts $$ Expensive $$ Contras: combo w/ SU's, hepatic dysfnx (CYP3A4 metzm) |
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Nateglinide
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Starlix: a "Glinide" Meglitinides (sibling of Repaglinide "Prandin")
Glinides best for pt w/ good FS, bad post-prandial control block β cell K+ channels → depolarize → ↑ insulin release rapid onset/short acting(1hλ) → take orally <1h before eating; hypoglycemia for sure if ∅ food vs. SUs: ↓ weight gain, ✓ in ∅-sulfa-pts $$ Expensive $$ Contras: combo w/ SU's, hepatic dysfnx (CYP3A4 metzm) |
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Repaglinide
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Prandin: a Meglitinide aka "glinide" (sibling of Nateglinide "Starlix")
Glinides best for pt w/ good FS, bad post-prandial control block β cell K+ channels → depolarize → ↑ insulin release rapid onset/short acting(1hλ) → take orally <1h before eating; hypoglycemia for sure if ∅ food vs. SUs: ↓ weight gain, ✓ in ∅-sulfa-pts $$ Expensive $$ Contras: combo w/ SU's, hepatic dysfnx (CYP3A4 metzm) |
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Metformin
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ativates hepatic & SkM AMP-activated protein kinase AMPK
↓ glucagon, GNG, GI sugar absorptn, TAGs & LDL ↑ glucose uptake Awesomeness: euglycemia w/o hypoglycemia ∅ ↑ weight ↓ macrovascular events safe in children >10 yo oral, 1/day available S-efx: Dose dpt lactic acidosis --rare but ±fatal nausea & DIARRHEA from GI non-absoprtion Contrad: lactic acidosis prone conditns: renal, hepatic dz, etohism, hypoxia (CHF, COPD, etc) |
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Thiazoladinediones
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Pioglitazone (Actos) & Rosiglitazone (Avandia):
PPARγ ligands → post-receptor insulin mimetic action 1° ↓ IR → ↓ GNG, ↑ Peripheral Glucose Uptake/Use ↓ TAGs, ↑ HDL (& LDL) S-efx: slow onset (weeks), weight gain, edema → edema will ↑ heart failure in CHF! Black Label: Rosiglitazone ± 2x risk MI & angina Contras: CHF & Hepatic dz (hepatic metzm) |
adipocytes: ↑ glucose transporter synth, differentatn, NEFA deposition, adiponectin secretn
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Rosiglitazone
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Avandia: A Thiazoladindione like Pioglitazone (Actos)
PPARγ ligands → post-receptor insulin mimetic action 1° ↓ IR → ↓ GNG, ↑ Peripheral Glucose Uptake/Use ↓ TAGs, ↑ HDL (& LDL) S-efx: slow onset (weeks), weight gain, edema → edema will ↑ heart failure in CHF! Black Label: Rosiglitazone ± 2x risk MI & angina Contras: CHF & Hepatic dz (hepatic metzm) |
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Pioglitazone
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Actos: a thiazoladinedione (like Rosiglitazone "Avandia")
PPARγ ligands → post-receptor insulin mimetic action 1° ↓ IR → ↓ GNG, ↑ Peripheral Glucose Uptake/Use ↓ TAGs, ↑ HDL (& LDL) S-efx: slow onset (weeks), weight gain, edema → edema will ↑ heart failure in CHF! Black Label: Rosiglitazone ± 2x risk MI & angina Contras: CHF & Hepatic dz (hepatic metzm) |
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Alpha-glucosidase inhibitors
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Acarbose (Precose) & Miglitol (Glyset): ↓ α glycosidase fnx → delay intestinal CHO dgestn
↓ postprandial [glucose] w/o ↓ FS ie no hypoglycemia ∅ Δ weight also good for T1DM SEfx: Flatulence $$ Expensive $$ Contrad: Hepatic Dz |
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Acarbose
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Alpha-glucosidase inhibitor like Miglitol: ↓ α glycosidase fnx → delayed CHO dgest'n & absoprt'n from the intestine
used off-label Rx for T1DM nice because they ↓ postprandial [glucose] w/o ↓ fasting glucose no significant effects on weight SEfx: Flatulence [general GI Sx, ↑ hepatic enzymes, jaundice] [PhK: oral admin 2hλ, met'd by intestinal enzymes & bacteria] [Contras: GI, Hepatic, or Renal problems] |
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Miglitol
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Alpha-glucosidase inhibitor like Acarbose: ↓ α glycosidase fnx → delayed CHO dgest'n & absoprt'n from the intestine
used off-label Rx for T1DM nice because they ↓ postprandial [glucose] w/o ↓ fasting glucose no significant effects on weight SEfx: Flatulence [general GI Sx, ↑ hepatic enzymes, jaundice] [PhK: oral admin 2hλ, met'd by intestinal enzymes & bacteria] [Contras: GI, Hepatic, or Renal problems] |
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Incretin Mimetics
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Exenatide, Liraglutide: Synthetic exendin-4 GLP1 analog resistant to DPP4 degradation
Exenatide PhK: Subcu 1h before two main meals [2hλ, renal met'sm] Liraglutide: 1 daily Subcu [12hλ] ↓ postprandial & fasting glucose potential ↑ β cell # & fnx slows gastric emptying: weight loss (contrast to -gliptin DPP4 inhibitors) [SEfx: GI, hypoglycemia when combined, hyperesensitivity to injx, ± acute pancreatitis] Contras: Thyroid CA: Liraglutide [Renal, GI impariments. Oral meds which cannot be exposed to somach acid too long] |
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DPP 4 inhibitors
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Sitagliptin, Saxagliptin
potentiate effects of incretins ↓ postprandial & fasting glucose no effect on weight (contrast to incretin mimetics) PhK: oral [12hλ 1/day, renal met'sm] SEfx: Sitagliptin ± ≈ acute pancreatitis/pancreatic CA; [hypersensitivity rxns] Contras: [slow GI, renal impairment] |
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Amylin-like peptide
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Pramlintide: synthetic analogue of amylin, a hormone co-secreted w/ insulin
Only an adjunct to insulin therapy in T1&2DM ↓ gastric emptying w/o Δabsorption centrally mediated Δappetitie ↓ caloric intake ↓ glucagon secretion Fnx: weight loss [PhK: S.c. 3x w/ meal bolus of insulin, renal met'sm, ~45mλ, 3h fnx SEfx: GI, hypoglycemia, lipodystrophy at injx Contras: slow GI] |
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Exenatide
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Incretin Mimetic like Liraglutide: Synthetic exendin-4 GLP1 analog resistant to DPP4 degradation
Exenatide PhK: Subcu 1h before two main meals [2hλ, renal met'sm] Liraglutide: 1 daily Subcu [12hλ] ↓ postprandial & fasting glucose potential ↑ β cell # & fnx weight loss: slows gastric emptying [SEfx: GI, hypoglycemia when combined, hyperesensitivity to injx, ± acute pancreatitis] Contras: Thyroid CA: Liraglutide [Renal, GI impariments. Oral meds which cannot be exposed to somach acid too long] |
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Liraglutide
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Incretin Mimetic like Exenatide: Synthetic exendin-4 GLP1 analog resistant to DPP4 degradation
Exenatide PhK: Subcu 1h before two main meals [2hλ, renal met'sm] Liraglutide: 1 daily Subcu [12hλ] ↓ postprandial & fasting glucose potential ↑ β cell # & fnx weight loss: slows gastric emptying [SEfx: GI, hypoglycemia when combined, hyperesensitivity to injx, ± acute pancreatitis] Contras: Thyroid CA: Liraglutide [Renal, GI impariments. Oral meds which cannot be exposed to somach acid too long] |
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Saxagliptin
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DPP 4 inhibitor like Saxagliptin: potentiate effects of incretins
↓ postprandial & fasting glucose no effect on weight (contrast to incretin mimetics) PhK: oral [12hλ 1/day, renal met'sm] SEfx: Sitagliptin ± ≈ acute pancreatitis/pancreatic CA; [hypersensitivity rxns] Contras: [slow GI, renal impairment] |
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Sitagliptin
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DPP 4 inhibitors Sitagliptin: potentiate effects of incretins
↓ postprandial & fasting glucose no effect on weight (contrast to incretin mimetics) PhK: oral [12hλ 1/day, renal met'sm] SEfx: Sitagliptin ± ≈ acute pancreatitis/pancreatic CA; [hypersensitivity rxns] Contras: [slow GI, renal impairment] |
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Orinase
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Tolbutamide: 1st gen SU
special for being safest in the elderly; [shortest λ at 4h] |
Sulfonylureas: block β cell K+ channels → depolarize → ↑ insulin release
weight gain, 20% non-responders, ↓ efficacy w/ time hypoglycemia -- esp ↑λ or interaxn w/ other Rx's Contrad: severe renal/hepatic dz, [sulfa allergy relative] |
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Diabinese
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Chlorpropamide: 1st gen SU
special for long (32h) λ & disulfiram-like effect |
Sulfonylureas: block β cell K+ channels → depolarize → ↑ insulin release
weight gain, 20% non-responders, ↓ efficacy w/ time hypoglycemia -- esp ↑λ or interaxn w/ other Rx's Contrad: severe renal/hepatic dz, [sulfa allergy relative] |
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Tolinase
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Tolazamide: 1st gen SU
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Sulfonylureas: block β cell K+ channels → depolarize → ↑ insulin release
weight gain, 20% non-responders, ↓ efficacy w/ time hypoglycemia -- esp ↑λ or interaxn w/ other Rx's Contrad: severe renal/hepatic dz, [sulfa allergy relative] |
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Micronase
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Glyburide: 2nd Gen SU
special for 24h effect (like Glimepiride), far greater risk of hypoglycemia than Glimepiride |
Sulfonylureas: block β cell K+ channels → depolarize → ↑ insulin release
weight gain, 20% non-responders, ↓ efficacy w/ time hypoglycemia -- esp ↑λ or interaxn w/ other Rx's Contrad: severe renal/hepatic dz, [sulfa allergy relative] |
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Glucotrol
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Glipizide: 2nd Gen SU
special short (3h) λ → least likely to cause hypoglycemia |
Sulfonylureas: block β cell K+ channels → depolarize → ↑ insulin release
weight gain, 20% non-responders, ↓ efficacy w/ time hypoglycemia -- esp ↑λ or interaxn w/ other Rx's Contrad: severe renal/hepatic dz, [sulfa allergy relative] |
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Amaryl
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Glimepiride: 2nd Gen SU
special for 24h effect (like Glyburide), far less risk of hypoglycemia than Glyburide |
Sulfonylureas: block β cell K+ channels → depolarize → ↑ insulin release
weight gain, 20% non-responders, ↓ efficacy w/ time hypoglycemia -- esp ↑λ or interaxn w/ other Rx's Contrad: severe renal/hepatic dz, [sulfa allergy relative] |
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Starlix
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Nateglinide: a "Glinide" Meglitinides (sibling of Repaglinide "Prandin")
Glinides best for pt w/ good FS, bad post-prandial control block β cell K+ channels → depolarize → ↑ insulin release rapid onset/short acting(1hλ) → take orally <1h before eating; hypoglycemia for sure if ∅ food vs. SUs: ↓ weight gain, ✓ in ∅-sulfa-pts $$ Expensive $$ Contras: combo w/ SU's, hepatic dysfnx (CYP3A4 metzm) |
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Prandin
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Repaglinide: a "Glinide" Meglitinides (sibling of Nateglinide aka "Starlix")
Glinides best for pt w/ good FS, bad post-prandial control block β cell K+ channels → depolarize → ↑ insulin release rapid onset/short acting(1hλ) → take orally <1h before eating; hypoglycemia for sure if ∅ food vs. SUs: ↓ weight gain, ✓ in ∅-sulfa-pts $$ Expensive $$ Contras: combo w/ SU's, hepatic dysfnx (CYP3A4 metzm) |
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Glinides
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ie Meglitinides: Repaglinide (Prandin), Nateglinide (Starlix)
Glinides best for pt w/ good FS, bad post-prandial control block β cell K+ channels → depolarize → ↑ insulin release rapid onset/short acting(1hλ) → take orally <1h before eating; hypoglycemia for sure if ∅ food vs. SUs: ↓ weight gain, ✓ in ∅-sulfa-pts $$ Expensive $$ Contras: combo w/ SU's, hepatic dysfnx (CYP3A4 metzm) |
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Januvia
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Sita"gliptin"
DPP 4 inhibitors Sitagliptin: potentiate effects of incretins ↓ postprandial & fasting glucose no effect on weight (contrast to incretin mimetics) PhK: 100 mg po qd; 12hλ Rnl metzm SEfx: Sitagliptin ± ≈ acute pancreatitis/pancreatic CA; [hypersensitivity rxns] Contras: [slow GI, renal impairment] |
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Tradjenta
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Lina"gliptin"
DPP 4 inhibitor: potentiate effects of incretins ↓ postprandial & fasting glucose no effect on weight (contrast to incretin mimetics) PhK: 5 mg po qd [12hλ, Rnl metzm] SEfx: Sitagliptin ± ≈ acute pancreatitis/pancreatic CA; [hypersensitivity rxns] Contras: [slow GI, renal impairment] |
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Linagliptin
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Tradjenta
"gliptin" DPP 4 inhibitor: potentiate effects of incretins ↓ postprandial & fasting glucose no effect on weight (contrast to incretin mimetics) PhK: 5 mg po qd [12hλ, Rnl metzm] SEfx: Sitagliptin ± ≈ acute pancreatitis/pancreatic CA; [hypersensitivity rxns] Contras: [slow GI, renal impairment] |
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Byetta
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Exenatide
Incretin Mimetic like Liraglutide/Victoza: Synthetic exendin-4 GLP1 analog resistant to DPP4 degradation ↓ postprandial & fasting glucose potential ↑ β cell # & fnx weight loss: slows gastric emptying PhK: 5 mCg sc 1h two main meals, NLT 6h apart [2hλ, renal met'sm] [SEfx: GI, hypoglycemia when combined, hypersensitivity to injx, ± acute pancreatitis] Contras: Thyroid CA: Liraglutide [Renal, GI impariments. Oral meds which cannot be exposed to somach acid too long] |
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Victoza
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Liraglutide
GLP1 analog resistant to DPP4 degradation 0.6-1.2 mg qd sc (12hλ) ↓ postprandial & fasting glucose potential ↑ β cell # & fnx weight loss: slows gastric emptying [SEfx: GI, hypoglycemia when combined, hyperesensitivity to injx, ± acute pancreatitis] Contras: Thyroid CA: Liraglutide [Renal, GI impariments. Oral meds which cannot be exposed to somach acid too long] |
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Onglyza
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Saxagliptin
"gliptin" DPP 4 inhibitor like Januvia, Tradjenta 2.5-5 mg po qd ↓ postprandial & fasting glucose no effect on weight (contrast to incretin mimetics) PhK: oral [12hλ, Rnl mtzm] SEfx: Sitagliptin ± ≈ acute pancreatitis/pancreatic CA; [hypersensitivity rxns] Contras: [slow GI, renal impairment] |
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Actos
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Pio"glitazone": a thiazoladinedione (like Rosiglitazone "Avandia")
PPARγ ligands → post-receptor insulin mimetic action 1° ↓ IR → ↓ GNG, ↑ Peripheral Glucose Uptake/Use ↓ TAGs, ↑ HDL (& LDL) S-efx: slow onset (weeks), weight gain, edema → edema will ↑ heart failure in CHF! Black Label: Rosiglitazone ± 2x risk MI & angina Contras: CHF & Hepatic dz (hepatic metzm) |
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Avandia
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Rosi"glitazone": A Thiazoladindione like Pioglitazone (Actos)
PPARγ ligands → post-receptor insulin mimetic action 1° ↓ IR → ↓ GNG, ↑ Peripheral Glucose Uptake/Use ↓ TAGs, ↑ HDL (& LDL) SEfx: slow onset (weeks), weight gain, edema → edema will ↑ heart failure in CHF! Black Label: Rosiglitazone ± 2x risk MI & angina Contras: CHF & Lvr Dz (hepatic metzm) |
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TZDD + Metformin
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Actoplus Met
Pioglitazone + metformin (Pioglitazone = Actos, TZDD) Avandamet Avandamet |
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SU+ TZDD
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Avandaryl: Rosiglitazone + glimeperide
rosiglitazone = avandia, TZDD Glimepiride = Amaryl, SU Duetact: Pioglitazone + glimepiride Pioglitazone = Actos, TZDD |
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SU + Metformin
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Glucovance: Glyburide + metformin
Glyburide = Diabeta/Micronase, SU Metaglip: Glipizide + Metformin Glipizide = Glucotrol |
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DPP4 Inhibitor + Metformin
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Janumet: Sitagliptin + metformin
Sitagliptin = Januvia, Kobiglyze XR: Saxagliptin + Metformin Saxagliptin = Onglyza |
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Meglinide + Metformin
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Prandimet: Repaglinide + Metformin
Repaglinide = Prandin |
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Symlin
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Pramlintide: synthetic analogue of amylin, a hormone co-secreted w/ insulin
Only an adjunct to insulin therapy in T1&2DM ↓ gastric emptying w/o Δabsorption centrally mediated Δappetitie ↓ caloric intake ↓ glucagon secretion Fnx: weight loss [PhK: S.c. 3x w/ meal bolus of insulin, renal met'sm, ~45mλ, 3h fnx SEfx: GI, hypoglycemia, lipodystrophy at injx Contras: slow GI] |
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Actoplus Met
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Pioglitazone + metformin
(Pioglitazone = Actos, TZDD) |
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Avandamet
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rosiglitazone + metformin
(rosiglitazone = avandia, TZDD) |
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Avandaryl
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Rosiglitazone + glimeperide
rosiglitazone = avandia, TZDD Glimepiride = Amaryl, SU |
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Duetact
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Pioglitazone + glimepiride
Pioglitazone = Actos, TZDD Glimepiride = Amaryl, SU |
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Glucovance
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Glyburide + metformin
Glyburide = Diabeta/Micronase, SU |
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Janumet
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Sitagliptin + metformin
Sitagliptin = Januvia, DPP4I |
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Kobiglyze XR
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Saxagliptin + Metformin
Saxagliptin = Onglyza, DDP4I |
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Metaglip
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Glipizide + Metformin
Glipizide = Glucotrol, SU |
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Prandimet
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Repaglinide + Metformin
Repaglinide = Prandin, a Meglinide (Non-Sulfa SU-like) |
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NovoLog
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Insulin Aspart
Onset: 10 min (fastest) Peak: 2 h Lasts: 4h |
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Apidra
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Insulin glolisine
Onset: 20 min Peak: 1 h Lasts: 4h |
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Humalog
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Insulin Lispro
Onset: 20 min Peak: 1 h Lasts: 4h |
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Novalin N
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NPH: Novalin N, Humulin N
Onset: 3 h Peak: 7 h Lasts: 12h |
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Humalin N
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NPH: Novalin N, Humulin N
Onset: 3 h Peak: 7 h Lasts: 12h |
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Levemir
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Onset: n/a
peak: flat action Lasts: dose dpt 6-23 |
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Latnus
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Onset: 3h
Peak: None Lasts: 24h |
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Novolog Mix
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Insulin aspart protamine suspension + non-suspended aspart
Onset: 20 min Peak: 1-4 biphasic Duration: up to 24 |
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Humalog Mix
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Insulin lispro protamine suspension + non-suspended lispro
Onset: 20 min Peak: 1-4 biphasic Duration: ~16h |
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