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Pharmacology- Test 4 Material > Insulin/Oral Anti-diabetic Agents > Flashcards

Insulin/Oral Anti-diabetic Agents Flashcards

1
Q

rosiglitazone

A

thiazolidinedione

  • Agonist of PPAR gamma leading to an increase in in insulin sensitivity (liver, fat, and muscle).
  • Adverse Rxn: cardiac disturbances, edema, fluid retention, wt gain, liver toxicity, and increased risk for bladder CA
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2
Q

pioglitazone

A

thiazolidinedione

  • Agonist of PPAR gamma leading to an increase in in insulin sensitivity (liver, fat, and muscle).
  • Adverse Rxn: cardiac disturbances, edema, fluid retention, wt gain, liver toxicity, and increased risk for bladder CA
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3
Q

acarbose

A

alpha-glucosidase inhibitor

  • decrease intestinal absorption of carbs
  • Adverse Rxn: flatulence, diarrhea, and abd pain.
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4
Q

miglitol

A

alpha-glucosidase inhibitor

  • decrease intestinal absorption of carbs
  • Adverse Rxn: flatulence, diarrhea, and abd pain.
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5
Q

canagliflozin

A

glucose reabsorption inhibitor

  • prevents reabsorption of glucose in the kidneys, thus increasing the body’s excretion of glucose.
  • S/E: UTI’s and increased urinary frequencies
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6
Q

empagliflozin

A

glucose reabsorption inhibitor

  • prevents reabsorption of glucose in the kidneys, thus increasing the body’s excretion of glucose.
  • S/E: UTI’s and increased urinary frequencies
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7
Q

insulin aspart

A

rapid acting
modification of the amino acid sequence (B28 changed from Pro to Asp) that promotes absorption by preventing self association
-adverse effects: hypoglycemia, lipodystrophy at injection site, allergy/resistance

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8
Q

insulin detemir

A

long acting
modification of amino acid sequence (c-terminal Thr B chain was deleted & myristic acid attached to new c-terminal Lys) that increases self aggregation and binding to albumin
-adverse effects: hypoglycemia, lipodystrophy at injection site, allergy/resistance

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9
Q

insulin glargine

A

long acting
modification of the amino acid sequence (A21 changed from Asn to Gly and two Arg added to positions B31 & B32) that makes insulin soluble at acidic pH but precipitates at neutral pH thus slowing down absorption
-adverse effects: hypoglycemia, lipodystrophy at injection site, allergy/resistance

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10
Q

insulin glulisine

A

rapid acting
modification of the amino acid sequence (B3 & B29 changed from Asn to Lys & Lys to Glu) that promote absorption by preventing self association
-adverse effects: hypoglycemia, lipodystrophy at injection site, allergy/resistance

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11
Q

insulin lispro

A

rapid acting
modification of the amino acid sequence (residues B28 & B29 changed from Pro-Lys to Lys-Pro) that promotes absorption by preventing self association
-adverse effects: hypoglycemia, lipodystrophy at injection site, allergy/resistance

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12
Q

NPH

A

Intermediate acting
wild-type amino acid sequence
cloudy suspension with protamine added to give 1:6 molar ratio to insulin– all protamine and insulin are in a complex
-clinical use now waning in favor of long-acting insulins
-adverse effects: hypoglycemia, lipodystrophy at injection site, allergy/resistance

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13
Q

regular crystalline insulin

A

short acting
wild-type amino acid sequence
-adverse effects: hypoglycemia, lipodystrophy at injection site, allergy/resistance

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14
Q

exenatide

A

incretin agonist
increases insulin and decreases glucagon
SQ injection
side effects: nasuea, anorexia, headaches, diarrhea, pancreatitis

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15
Q

liraglutide

A

incretin agonist
increases insulin and decreases glucagon
SQ injection
side effects: nasuea, anorexia, headaches, diarrhea, pancreatitis

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16
Q

saxagliptin

A

inhibitor of incretin degradation
increases insulin and decrease glucagon
oral
side effects: headache, increased rate of infections and pnacreatitis

17
Q

sitaglitpin

A

inhibitor of incretin degradation
increases insulin and decrease glucagon
oral
side effects: headache, increased rate of infections and pnacreatitis

18
Q

pramlintide

A

amylin analog (hormone made in the beta cells, it acts on the alpha cells to inhibit glucagon secretion, also has CNS mediated anorectic effect)

  • can increase the effectiveness of insulin therapy in type 1 DM
  • SQ
  • useful in type 2 when given alone
  • side effects: hypoglycemia, nausea, vomiting, anorexia
19
Q

chlorpropamide (Drabinese)

A

Sulfonylurea- First generation

  • oral anti-diabetic, ~60 hr half-life
  • inc. insulin secretion by decreasing K+ efflux from beta cells in the pancreas
  • S/Fx: hypoglycemia, tachyphylaxis
  • no longer readily available and rarely used
20
Q

glipizide (Glucotrol)

A

Sulfonylurea- Second generation

  • oral anti-diabetic, 10-24 h duration
  • generally more potent, more readily available, and commonly used
  • S/fx: hypoglycemia, tachyphylaxis
21
Q

glyburide (Micronase)

A

Sulfonylurea- Second generation

  • oral anti-diabetic, 10-24 h duration
  • generally more potent, more readily available, and commonly used
  • S/fx: hypoglycemia, tachyphylaxis
22
Q

glimepiride (Amaryl)

A

Sulfonylurea- Second generation

  • oral anti-diabetic, 10-24 h duration
  • generally more potent, more readily available, and commonly used
  • S/fx: hypoglycemia, tachyphylaxis
23
Q

tolbutamide (Orinase)

A

Sulfonylurea- First generation

  • oral anti-diabetic, ~60 hr half-life
  • inc. insulin secretion by decreasing K+ efflux from beta cells in the pancreas
  • S/Fx: hypoglycemia, tachyphylaxis
  • no longer readily available and rarely used
24
Q

repaglinide (Prandin)

A

Meglitinide- oral anti-diabetic

  • like sulfonylureas, prevent K+ efflux from beta cells, ultimately leading to inc. insulin secretion
  • chemically unrelated to and have greater binding affinity to K+ channels then sulfonylureas
  • more potent then second gen. sulfonylureas but shorter DOA
  • used to control postpandrial glucose levels
  • S/Fx: hypoglycemia, need to use cautiously in patients with renal or hepatic insufficiency
25
Q

nateglinide (Starlix)

A

Pheylalanine analog- oral anti-diabetic

  • chemically unrelated to sulfonylureas and meglitinides but stimulate insulin secretion by same mechanism
  • effect is faster but less sustained then with meglitinides
  • S/Fx: hypoglycemia
  • safer in those with reduced renal function
26
Q

metformin (Glucophage)

A

Biguanide- oral anti-diabetic

  • inactivate mitochondrial glycerophosphate dehydrogenase, antagonize the action of glucagon and/or activate the AMP-activated protein kinase
  • actions occur in liver and lead to reduction in gluconeogenesis and thus hepatic glucose output
  • commonly used as first line therapy in DM type II
  • S/Fx: GI discomfort, lactic acidosis, Vitamin B12 deficiency

Pharmacology- Test 4 Material (12 decks)

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