Rapid - Endocrine Flashcards Preview

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Flashcards in Rapid - Endocrine Deck (80):
1

Chlorpropamide

  • 1st gen sulfonylurea
    • Closes K+ channel in β-cell memb → depolarization → Ca2+ influx → insulin release
  • Use: T2DM
  • S/E:
    • disulfiram-like effects
    • hypoglycemia
    • weight gain
    • C/I in sulfa allergy

2

Tolbutamide

  • 1st gen sulfonylurea
    • Closes K+ channel in β-cell memb → depolarization → Ca2+ influx → insulin release
  • Use: T2DM
  • S/E:
    • disulfiram-like effects
    • hypoglycemia
    • weight gain
    • C/I in sulfa allergy

3

Glimepiride

  • 2nd gen sulfonylurea
    • Closes K+ channel in β-cell memb → depolarization → Ca2+ influx → insulin release
  • Use: T2DM
  • S/E:
    • hypoglycemia
    • weight gain
    • C/I in sulfa allergy

4

glipizide

  • 2nd gen sulfonylurea
    • Closes K+ channel in β-cell memb → depolarization → Ca2+ influx → insulin release
  • Use: T2DM
  • S/E:
    • hypoglycemia
    • weight gain
    • C/I in sulfa allergy

5

glyburide

  • 2nd gen sulfonylurea
    • Closes K+ channel in β-cell memb → depolarization → Ca2+ influx → insulin release
  • Use: T2DM
  • S/E:
    • hypoglycemia
    • weight gain
    • C/I in sulfa allergy 

6

Metformin

  • Biguanide
    • Exact MOA unknown
  • Decreases gluconeogenesis, increases glycolysis & peripheral glucose uptake
  • Use: 1st line in T2DM (oral)
    • can be used in pts w/o islet fcn
  • S/E:
    • lactic acidosis
    • weight loss -- good for obese pts
    • GI upset
  • C/I in renal insufficiency

7

Pioglitazone

  • Glitazone
    • Binds to PPAR-γ nuclear transcription regulator → increases peripheral tissue insulin sensitivity
  • Use: mono- or combo therapy in T2DM
  • S/E:
    • weight gain
    • edema
    • hepatotoxicity
    • HF
    • increased risk fractures

8

rosiglitazone

  • Glitazone
    • Binds to PPAR-γ nuclear transcription regulator → increases peripheral tissue insulin sensitivity
  • Use: mono- or combo therapy in T2DM
  • S/E:
    • weight gain
    • edema
    • hepatotoxicity
    • HF
    • increased risk fractures

9

PPAR-γ

  • Genes activated by PPAR-γ regulate FA storage and glucose metabolism
  • Activation of PPAR-γ increases insulin sensitivity and adiponectin levels

10

Lispro

  • Rapid-acting insulin
    • Binds insulin receptor (tyrosine kinase activity)
  • Use:
    • T1DM
    • T2DM
    • GDM - postprandial
  • S/E:
    • hypoglycemia
    • lipodystrophy
    • hypersensitivity (rare)

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11

Aspart

  • Rapid-acting insulin
    • Binds insulin receptor (tyrosine kinase activity)
  • Use:
    • T1DM
    • T2DM
    • GDM - postprandial
  • S/E:
    • hypoglycemia
    • lipodystrophy
    • hypersensitivity (rare)

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12

Glulisine

  • Rapid-acting insulin
    • Binds insulin receptor (tyrosine kinase activity)
  • Use:
    • T1DM
    • T2DM
    • GDM - postprandial
  • S/E:
    • hypoglycemia
    • lipodystrophy
    • hypersensitivity (rare)

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13

Regular insulin

  • short-acting
  • Use:
    • T1DM
    • T2DM
    • GDM
    • DKA
    • Hyperkalemia
    • Stress hyperglycemia

14

NPH Insulin

  • Intermediate-Acting
  • Use:
    • T1DM
    • T2DM
    • GDM

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15

Detemir

  • Long-acting insulin
  • Use:
    • T1DM
    • T2DM
    • GDM - basal control

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16

glargine

  • Long-acting (24h) insulin
  • Use:
    • T1DM
    • T2DM
    • GDM - basal control

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17

Nateglinide

  • Meglitinide
    • Binds K+ channels on β-cell memb (different site than sulfonylureas) → postprandial insulin release
  • Rapid-acting, short duration -- take only w/meal
  • Use:
    • T2DM monotherapy
    • T2DM + metformin
  • S/E:
    • hypoglycemia
    • weight gain

18

repaglinide

  • Meglitinide
    • Binds K+ channels on β-cell memb (different site than sulfonylureas) → postprandial insulin release
  • Rapid-acting, short duration -- take only w/meal
  • Use:
    • T2DM monotherapy
    • T2DM + metformin
  • S/E:
    • hypoglycemia
    • weight gain

19

Exenatide

  • GLP-1 analog
    • increases glucose-dependent insulin release + satieity
    • decreases glucagon release + gastric emptying
  • Use: T2DM
  • S/E:
    • Nausea/vomiting
    • Pancreatitis
    • modest weight loss

20

liraglutide

  • GLP-1 analog
    • increases glucose-dependent insulin release + satieity
    • decreases glucagon release + gastric emptying
  • Use: T2DM
  • S/E:
    • Nausea/vomiting
    • Pancreatitis
    • modest weight loss

21

Linagliptin

  • DPP-4 inhibitor
    • Inhibits DPP-4 enzyme (which deactivates GLP-1) →
      • inc glucose-dependent insulin release
      • dec glucagon release
      • dec gastric emptying
      • inc satiety
  • Use: T2DM
  • S/E:
    • Mild urinary or respiratory infections
    • weight neutral

22

saxagliptin

  • DPP-4 inhibitor
    • Inhibits DPP-4 enzyme (which deactivates GLP-1) →
      • inc glucose-dependent insulin release
      • dec glucagon release
      • dec gastric emptying
      • inc satiety
  • Use: T2DM
  • S/E:
    • Mild urinary or respiratory infections
    • weight neutral

23

sitagliptin

  • DPP-4 inhibitor
    • Inhibits DPP-4 enzyme (which deactivates GLP-1) →
      • inc glucose-dependent insulin release
      • dec glucagon release
      • dec gastric emptying
      • inc satiety 
  • Use: T2DM
  • S/E:
    • Mild urinary or respiratory infections
    • weight neutral

24

Pramlintide

  • Amylin analog
    • Decreases glucagon + gastric emptying
  • Use:
    • T1DM
    • T2DM
  • S/E:
    • Hypoglycemia (w/mistimed prandial insulin)
    • nausea

25

Canagliflozin

  • SGLT-2 inhibitor
    • Blocks glucose reabsorption in PCT
  • Use: T2DM
  • S/E:
    • Glucosuria
    • UTI
    • vaginal yeast infxn
    • hypERkalemia
    • dehydration (→ orthostatic hypOtension)

26

dapagliflozin

  • SGLT-2 inhibitor
    • Blocks glucose reabsorption in PCT
  • Use: T2DM
  • S/E:
    • Glucosuria
    • UTI
    • vaginal yeast infxn
    • hypERkalemia
    • dehydration (→ orthostatic hypOtension)

27

empagliflozin

  • SGLT-2 inhibitor
    • Blocks glucose reabsorption in PCT
  • Use: T2DM
  • S/E:
    • Glucosuria
    • UTI
    • vaginal yeast infxn
    • hypERkalemia
    • dehydration (→ orthostatic hypOtension)

28

Acarbose

  • α-glucosidase inhibitor
    • Inhibits intestinal brush-border α-glucosidases → delays carb hydrolysis, glucose absorption → decreases postprandial hypERglycemia
  • Use: T2DM
  • S/E: GI upset

29

miglitol

  • α-glucosidase inhibitor
    • Inhibits intestinal brush-border α-glucosidases → delays carb hydrolysis, glucose absorption → decreases postprandial hypERglycemia
  • Use: T2DM
  • S/E: GI upset

30

T1DM Rx Strategies

low-carb diet + insulin replacement

31

T2DM Rx Strategies

  • dietary modification and exercise for weight loss
  • oral agents
  • non-insulin injectables
  • insulin replacement

32

GDM Rx Strategies

  • dietary modifications
  • exercise
  • insulin replacement if lifestyle modification fails

33

Propylthiouracil (PTU)

  • Thionamide
    • Blocks thyroid peroxidase → inhibits oxidation of iodide, organification (coupling) of iodine → inhibits thyroid hormone synth
    • Blocks 5′-deiodinase → decreases periph T4 to T3 conv
  • Use: HypERthyroidism
    • Can be used in Pregnancy
  • S/E:
    • Skin rash
    • agranulocytosis (rare)
    • aplastic anemia
    • hepatotoxicity

34

Methimazole

  • Thionamide
    • Blocks thyroid peroxidase → inhibits oxidation of iodide, organification (coupling) of iodine → inhibits thyroid hormone synth
  • Use: HypERthyroidism
  • S/E:
    • Teratogenesis (aplasia cutis)
    • Skin rash
    • agranulocytosis (rare)
    • aplastic anemia
    • hepatotoxicity

35

Levothyroxine

  • Synthetic T4
  • Use:
    • HypOthyroidism
    • Myxedema
    • Weight loss (off-label)
  • S/E:
    • Tachycardia
    • heat intolerance
    • tremors
    • arrhythmias
  • Interactions:
    • Rifampin, Carbamazepine, Phenytoin (enzyme inducers)
    • Soy, fiber, coffee (dec absorp)
    • Amiodarone (inhib T4 → T3)

36

Triiodothyronine

  • Synthetic T3
  • Use:
    • HypOthyroidism
    • Myxedema
    • Weight loss (off-label)
  • S/E:
    • Tachycardia
    • heat intolerance
    • tremors
    • arrhythmias

37

Radioactive iodine (RAI, 131I)

  • Concentrates in thyroid gland → follicular necrosis
  • Use: most common Rx for hypERthyroidism
  • C/I: children, pregnancy/lactation
  • S/E: hypOthyroidism

38

Rx Thyroid Storm

  • PTU
  • iodides
  • propranolol
  • corticosteroids
  • supportive measures

39

Thyroid Storm

  • Life-threatening medical emergency
  • Precipitated by infection, trauma, surgery, withdrawal of antithyroid meds
  • Severe thyrotoxicosis, high fever, tachycardia, tachypnea, dehydration, delirium, N/V/D
  • Average duration ~72 hours w/treatment
  • W/aggressive treatment, mortality is 20%

40

Iodine

  • Lugol’s solution OR saturated potassium iodide solution
    • Acutely blocks thyroid hormone release
    • inhibits thyroid hormone synth
    • decreases gland vascularity
  • Use: pre-op before thyroid surgery or after RAI treatment
  • Adverse effects:
    • hypersensitivity reactions
    • iodism (metallic taste, burning mouth, GI upset)

41

Potassium Iodide

  • Competitively inhibits uptake of radioactive iodine
  • Use: decrease risk of developing thyroid cancer after exposure to radioactive iodine

42

Myxedema Coma

  • End stage of uncontrolled, long-standing hypOthyroidism
  • Advanced hypothyroid symptoms, hypothermia, delirium, and coma
  • Mortality 60-70%

43

Rx Myxedema Coma

  • Aggressive treatment:
    • IV thyroxine
    • glucocorticoids
    • supportive measures
  • Improvement of symptoms within 24 hrs
  • Switch to oral levothyroxine once pt is stable

44

conivaptan

  • ADH antagonist
    • Blocks action of ADH at collecting duct V2-receptor
  • Use: SIADH

45

tolvaptan

  • ADH antagonist
    • Blocks action of ADH at collecting duct V2-receptor
  • Use: SIADH

46

Desmopressin acetate

  • Synthetic ADH
    • Regulates aquaporin channel insertion in principal cells of collecting duct
    • Stimulates endothelial release of vWF → augmentation of platelet binding
    • Stabilizes & increases Factor 8 levels
  • Use:
    • Central DI
    • Nocturnal Enuresis
    • Type 1 Von Willebrand's Disease
    • Mild Hemophilia A

47

GH

Use:

  • GH deficiency
  • Turner Syndrome

48

Oxytocin

Use:

  • Stimulates labor, uterine contractions, milk let-down
  • Controls uterine hemorrhage

49

Somatostatin (octreotide)

  • Inhibits GH
  • Use:
    • Acromegaly
    • carcinoid syndrome
    • gastrinoma
    • glucagonoma
    • esophageal varices

50

Demeclocycline

  • ADH antagonist (tetracycline family)
  • Use: SIADH
  • S/E:
    • Nephrogenic DI
    • photosensitivity
    • abnormalities of bone and teeth

51

Beclomethasone

  • Glucocorticoid
    • Inhibits PLA2 → decreases PG & LT synth
    • Inhibits NF-kB → inhibits transcription of cytokines & adhesion proteins → decreases leukocyte recruitment & activation
  • Use:
    • Adrenal insufficiency
    • inflammation
    • immunosuppression
    • asthma
  • S/E:
    • Iatrogenic Cushing syndrome
    • adrenocortical atrophy
    • peptic ulcers
    • steroid diabetes / hyperglycemia
    • steroid psychosis
    • cataracts
    • osteoporosis/pathologic fractures
    • Adrenal insufficiency when stopped abruptly after chronic use

52

dexamethasone

  • Glucocorticoid
    • Inhibits PLA2 → decreases PG & LT synth
    • Inhibits NF-kB → inhibits transcription of cytokines & adhesion proteins → decreases leukocyte recruitment & activation
  • Use:
    • Adrenal insufficiency
    • inflammation
    • immunosuppression
    • asthma
  • S/E:
    • Iatrogenic Cushing syndrome
    • adrenocortical atrophy
    • peptic ulcers
    • steroid diabetes / hyperglycemia
    • steroid psychosis
    • cataracts
    • osteoporosis/pathologic fractures
    • Adrenal insufficiency when stopped abruptly after chronic use

53

hydrocortisone

  • Glucocorticoid
    • Inhibits PLA2 → decreases PG & LT synth
    • Inhibits NF-kB → inhibits transcription of cytokines & adhesion proteins → decreases leukocyte recruitment & activation
  • Use:
    • Adrenal insufficiency
    • inflammation
    • immunosuppression
    • asthma
  • S/E:
    • Iatrogenic Cushing syndrome
    • adrenocortical atrophy
    • peptic ulcers
    • steroid diabetes / hyperglycemia
    • steroid psychosis
    • cataracts
    • osteoporosis/pathologic fractures
    • Adrenal insufficiency when stopped abruptly after chronic use

54

methylprednisolone

  • Glucocorticoid
    • Inhibits PLA2 → decreases PG & LT synth
    • Inhibits NF-kB → inhibits transcription of cytokines & adhesion proteins → decreases leukocyte recruitment & activation
  • Use:
    • Adrenal insufficiency
    • inflammation
    • immunosuppression
    • asthma
  • S/E:
    • Iatrogenic Cushing syndrome
    • adrenocortical atrophy
    • peptic ulcers
    • steroid diabetes / hyperglycemia
    • steroid psychosis
    • cataracts
    • osteoporosis/pathologic fractures
    • Adrenal insufficiency when stopped abruptly after chronic use

55

Prednisone

  • Glucocorticoid
    • Inhibits PLA2 → decreases PG & LT synth
    • Inhibits NF-kB → inhibits transcription of cytokines & adhesion proteins → decreases leukocyte recruitment & activation
  • Use:
    • Adrenal insufficiency
    • inflammation
    • immunosuppression
    • asthma
  • S/E:
    • Iatrogenic Cushing syndrome
    • adrenocortical atrophy
    • peptic ulcers
    • steroid diabetes / hyperglycemia
    • steroid psychosis
    • cataracts
    • osteoporosis/pathologic fractures
    • Adrenal insufficiency when stopped abruptly after chronic use

56

triamcinolone

  • Glucocorticoid
    • Inhibits PLA2 → decreases PG & LT synth
    • Inhibits NF-kB → inhibits transcription of cytokines & adhesion proteins → decreases leukocyte recruitment & activation
  • Use:
    • Adrenal insufficiency
    • inflammation
    • immunosuppression
    • asthma
  • S/E:
    • Iatrogenic Cushing syndrome
    • adrenocortical atrophy
    • peptic ulcers
    • steroid diabetes / hyperglycemia
    • steroid psychosis
    • cataracts
    • osteoporosis/pathologic fractures
    • Adrenal insufficiency when stopped abruptly after chronic use

57

Fludrocortisone

  • Synthetic aldosterone analog
    • Few glucocorticoid effects
  • Use: Mineralocorticoid replacement in 1° adrenal insufficiency
  • S/E:
    • edema
    • HF exacerbation
    • hyperpigmentation
    • Others similar to glucocorticoids

58

Cinacalcet

  • Sensitizes parathyroid gland Ca2+-sensing receptor to circulating Ca2+ → decreases PTH
  • Use: 1° or 2° hyperparathyroidism
  • S/E: HypOcalcemia

59

Liothyronine

  • Synthetic T3
  • Use:
    • HypOthyroidism
    • Myxedema
    • Weight loss (off-label)
  • S/E:
    • Tachycardia
    • heat intolerance
    • tremors
    • arrhythmias

60

1st gen sulfonylureas

Close K+ channel in β-cell memb → depolarization → Ca2+ influx → insulin release

  • Chlorpropamide
  • Tolbutamide

Note: Disulfiram-like effects; C/I in sulfa allergy

61

2nd gen sulfonylureas

Close K+ channel in β-cell memb → depolarization → Ca2+ influx → insulin release

  • Glimepiride
  • Glyburide
  • Glipizide

Note: Hypoglycemia

62

Biguanides

Stimulate AMPK → Decrease gluconeogenesis / increase glycolysis + periph glucose uptake

  • Metformin

Note: lactic acidosis; C/I in renal insufficiency

63

Glitazones

Bind to PPAR-γ → increase periph tissue insulin sensitivity

  • Pioglitazone
  • Rosiglitazone

Note: weight gain; edema

64

Rapid-Acting Insulin

Bind insulin receptor → tyrosine kinase activity

  • Lispro
  • Aspart
  • Glulisine

Note: use w/meals

65

Short-Acting Insulin

Bind insulin receptor → tyrosine kinase activity

  • Regular insulin

Note: use for DKA

66

Intermediate-Acting Insulin

Bind insulin receptor → tyrosine kinase activity

  • NPH

67

Long-Acting Insulin

Bind insulin receptor → tyrosine kinase activity

  • Detemir (2x/day)
  • Glargine (1x/day)

Note: use for basal control

68

Meglitinides

Bind K+ channels on β-cell memb (different site than sulfonylureas) → postprandial insulin release

  • Nateglinide
  • Repaglinide

Note: hypoglycemia; weight gain

69

GLP-1 Agonists

decrease glucagon release + gastric emptying → increase glucose-dependent insulin release + satieity

  • Exenatide
  • Liraglutide

Note: weight loss

70

GLP-1

  • Neuropeptide and incretin derived from transcription product of proglucagon gene
  • Produced by intestinal L cells and nucleus of solitary tract
  • Activated by selective cleavage of proglucagon molecule
  • decreases glucagon release + gastric emptying → increases glucose-dependent insulin release + satieity

71

DPP-4 Inhibitors

Inhibit DPP-4 enzyme → allow activation of GLP-1

  • Linagliptin
  • Saxagliptin
  • Sitagliptin

Note: weight-neutral

72

Amylin Analogs

Decrease glucagon + gastric empyting

  • Pramlintide

Note: hypoglycemia

73

Amylin

  • peptide hormone that is cosecreted with insulin from pancreatic beta-cell
  • inhibits glucagon secretion, delays gastric emptying, and acts as a satiety agent

74

SGLT-2 inhibitors

Block glucose reabsorption in PCT

  • Canagliflozin
  • Dapagliflozin
  • Empagliflozin

Note: UTIs; C/I in renal insufficiency

75

SGLT-2

Low-affinity, high-capacity transport protein responsible for reabsorbing 90% of filtered glucose in proximal tubule (cotransport w/Na+)

76

α-Glucosidase Inhibitors

Inhibit intestinal brush-border α-glucosidases → delay carb hydrolysis, glucose absorption → decrease postprandial hyperglycemia

  • Acarbose
  • Miglitol

77

Thioamides

Block thyroid peroxidase → inhibit oxidation of iodide, organification (coupling) of iodine → inhibit thyroid hormone synth

PTU also blocks 5′-deiodinase → decreases periph T4 to T3 conv

  • Propylthiouracil (PTU)
  • Methimazole

Note: aplastic anemia; PTU can be used in pregnancy

78

Synthetic Thyroid Hormones

Act at thyroid hormone nuclear receptors

  • Levothyroxine (T4)
  • Triiodothyronine (T3)
  • Liothyronine (T3)

Note: tachycardia; heat intolerance

79

ADH Antagonists

Block action of ADH at collecting duct V2-receptor

  • Conivaptan
  • Tolvaptan
  • Demeclocycline

Note: demeclocycline → tetracycline S/E

 

80

Glucocorticoids

Inhibit PLA2 → decreased PG & LT synth

Inhibit NF-kB → inhibit transcription of cytokines & adhesion proteins → decrease leukocyte recruitment & activation

  • Beclomethasone
  • Dexamethasone
  • Hydrocortisone
  • Methylprednisolone
  • Prednisone
  • Triamcinolone

Note: osteoporosis/pathologic fractures; iatrogenic Cushing's; hyperglycemia