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Flashcards in Endocrine Deck (73):
1

What are the treatment strategies for Diabetes Mellitus Type 1?

Low-sugar diet, insulin replacement

2

What are the treatment strategies for Diabetes Mellitus Type 2?

Dietary modification and exercise for weight loss; oral agents, non-insulin injectables, insulin replacement

3

Diabetes Drugs - What are the treatment strategies for Gestational Diabetes Mellitus?

Dietary modifications, exercise, insulin replacement if lifestyle modification fails

4

Diabetes Drugs - What is the mechanism of the rapid acting Insulin drugs (Lispro, Aspart, Glulisine)?

Bind insulin receptor (tyrosine kinase activity).
Liver: ↑ glucose stored as glycogen.
Muscle: ↑ glycogen, protein synthesis; ↑ K+ uptake.
Fat: ↑ TG storage.

5

Diabetes Drugs - What is the clinical use of the rapid acting Insulin drugs (Lispro, Aspart, Glulisine)?

DM1, DM2, GDM (postprandial glucose control)

6

Diabetes Drugs - What are the toxicities of the rapid acting Insulin drugs (Lispro, Aspart, Glulisine)?

Hypoglycemia, rare hypersensitivity reactions

7

Diabetes Drugs - What is the clinical use of the short acting Insulin drugs (Regular)?

DM1, DM2, GDM, DKA (IV), hyperkalemia (+ glucose), stress hyperglycemia

8

Diabetes Drugs - What is the clinical use of the intermediate acting Insulin drugs (NPH)?

DM1, DM2, GDM

9

Diabetes Drugs - What is the clinical use of the long acting Insulin drugs (Glargine, Detemir)?

DM1, DM2, GDM (basal glucose control)

10

Diabetes Drugs - What is the mechanism of Biguanides (Metformin)?

Exact mechanism is unknown. ↓ gluconeogenesis, ↑ glycolysis, ↑ peripheral glucose uptake (insulin sensitivity).

11

Diabetes Drugs - What is the clinical use of Biguanides (Metformin)?

Oral. First-line therapy in type 2 DM.
Can be used in patients without islet function.

12

Diabetes Drugs - What are the toxicities of Biguanides (Metformin)?

GI upset; most serious adverse effect is lactic acidosis (thus contraindicated in renal failure)

13

Diabetes Drugs - What is the mechanism of Sulfonylureas (First generation: Tolbutamide, Chlorpropamide; Second generation: Glyburide, Glimepiride, Glipizide)?

Close K+ channel in β-cell membrane, so cell depolarizes → triggering of insulin release via ↑ Ca2+ influx

14

Diabetes Drugs - What is the clinical use of Sulfonylureas (First generation: Tolbutamide, Chlorpropamide; Second generation: Glyburide, Glimepiride, Glipizide)?

Stimulate release of endogenous insulin in type 2 DM. Require some islet function, so useless in type 1 DM.

15

Diabetes Drugs - What are the toxicities of Sulfonylureas (First generation: Tolbutamide, Chlorpropamide; Second generation: Glyburide, Glimepiride, Glipizide)?

Risk of hypoglycemia ↑ in renal failure.
First generation: disulfiram-like effects.
Second generation: hypoglycemia.

16

Diabetes Drugs - What is the mechanism of Glitazones/thiazolidinediones (Pioglitazone, Rosiglitazone)?

↑ insulin sensitivity in peripheral tissue. Binds to PPAR-γ nuclear transcription regulator.
Genes activated by PPAR-γ regulate fatty acid storage and glucose metabolism. Activation of PPAR-γ ↑ insulin sensitivity and levels of adiponectin.

17

Diabetes Drugs - What is the clinical use of Glitazones/thiazolidinediones (Pioglitazone, Rosiglitazone)?

Used as monotherapy in type 2 DM or combined with above agents.

18

Diabetes Drugs - What are the toxicities of Glitazones/thiazolidinediones (Pioglitazone, Rosiglitazone)?

Weight gain, edema.
Hepatotoxicity, heart failure.

19

Diabetes Drugs - What is the mechanism of α-glucosidase inhibitors (Acarbose, Miglitol)?

Inhibit intestinal brush-border α-glucosidases.
Delayed sugar hydrolysis and glucose absorption → ↓ postprandial hyperglycemia.

20

Diabetes Drugs - What is the clinical use of α-glucosidase inhibitors (Acarbose, Miglitol)?

Used as monotherapy in type 2 DM or in combination with above agents.

21

Diabetes Drugs - What are the toxicities of α-glucosidase inhibitors (Acarbose, Miglitol)?

GI disturbances

22

Diabetes Drugs - What is the mechanism of Amylin analogs (Pramlintide)?

↓ gastric emptying, ↓ glucagon

23

Diabetes Drugs - What is the clinical use of Amylin analogs (Pramlintide)?

Type 1 and type 2 DM

24

Diabetes Drugs - What are the toxicities of Amylin analogs (Pramlintide)?

Hypoglycemia, nausea, diarrhea

25

Diabetes Drugs - What is the mechanism of GLP-1 analogs (Exenatide, Liraglutide)?

↑ insulin, ↓ glucagon release.

26

Diabetes Drugs - What is the clinical use of GLP-1 analogs (Exenatide, Liraglutide)?

Type 2 DM

27

Diabetes Drugs - What are the toxicities of GLP-1 analogs (Exenatide, Liraglutide)?

Nausea, vomiting; pancreatitis

28

Diabetes Drugs - What is the mechanism of DPP-4 inhibitors (Linagliptin, Saxagliptin, Sitagliptin)?

↑ insulin, ↓ glucagon release.

29

Diabetes Drugs - What is the clinical use of DPP-4 inhibitors (Linagliptin, Saxagliptin, Sitagliptin)?

Type 2 DM

30

Diabetes Drugs - What are the toxicities of DPP-4 inhibitors (Linagliptin, Saxagliptin, Sitagliptin)?

Mild urinary or respiratory infections

31

What is the mechanism of Propylthiouracil and methimazole?

Block thyroid peroxidase, inhibiting the oxidation of iodide and the organification (coupling) of iodine → inhibition of thyroid hormone synthesis. Propylthiouracil also blocks 5′-deiodinase, which ↓ peripheral conversion of T4 to T3

32

What is the clinical use of Propylthiouracil and methimazole?

Hyperthyroidism. PTU blocks Peripheral conversion, used in Pregnancy.

33

What is the toxicity of Propylthiouracil and methimazole?

Skin rash, agranulocytosis (rare), aplastic anemia, hepatotoxicity (propylthiouracil). Methimazole is a possible teratogen (can cause aplasia cutis).

34

What is the mechanism of Levothyroxine and triiodothyronine?

Thyroxine replacement

35

What is the clinical use of Levothyroxine and triiodothyronine?

Hypothyroidism, myxedema

36

What is the toxicity of Levothyroxine and triiodothyronine?

Tachycardia, heat intolerance, tremors, arrhythmias

37

Hypothalamic/pituitary drugs - What is the clinical use of GH?

GH deficiency, Turner syndrome

38

Hypothalamic/pituitary drugs - What is the clinical use of Somatostatin (octreotide)?

Acromegaly, carcinoid, gastrinoma, glucagonoma, esophageal varices

39

Hypothalamic/pituitary drugs - What is the clinical use of Oxytocin?

Stimulates labor, uterine contractions, milk let-down; controls uterine hemorrhage

40

Hypothalamic/pituitary drugs - What is the clinical use of ADH (DDAVP)?

Pituitary (central, not nephrogenic) DI

41

What is the mechanism of Demeclocycline?

ADH antagonist (member of the tetracycline family)

42

What is the clinical use of Demeclocycline?

SIADH

43

What are the toxicities of Demeclocycline?

Nephrogenic DI, photosensitivity, abnormalities of bone and teeth

44

What are the glucocorticoids?

Hydrocortisone, prednisone, triamcinolone, dexamethasone, beclomethasone, fludrocortisone (mineralocorticoid and glucocorticoid activity)

45

What is the mechanism of Glucocorticoids?

Metabolic, catabolic, anti-inflammatory, and immunosuppressive effects mediated by interactions with glucocorticoid response elements and inhibition of transcription factors such as NF-κB

46

What is the clinical use of Glucocorticoids?

Addison disease, inflammation, immune suppression, asthma

47

What are the toxicities of Glucocorticoids?

Iatrogenic Cushing syndrome—buffalo hump, moon facies, truncal obesity, muscle wasting, thin skin, easy bruisability, osteoporosis (treat with bisphosphonates), adrenocortical atrophy, peptic ulcers, diabetes (if chronic).
Adrenal insufficiency when drug stopped abruptly after chronic use.

48

What is the mechanism of Clomiphene?

Inhibits the hypothalamus

49

What do oral contraceptives and danazol do?

Inhibit the anterior pituitary

50

What do ketoconazole and danzol do?

Inhibit P-450c17

51

What do Anastrozole and others do?

Inhibit aromatase

52

What does Fulvestrant do?

Inhibit estradiol from interacting with the estrogen response element

53

What do ketoconazole and spironolactone do?

Inhibit the testis from producing testosterone

54

What does Finasteride do?

5α-reductase

55

What do Flutamide, cyproterone, and spironolactone do?

Inhibit testosterone and dihydrotestosterone from becoming an androgen-receptor complex

56

What can Dopamine antagonists (e.g., antipsychotics) cause?

Galactorrhea

57

What is used in the treatment of prolactinoma?

Dopamine agonists (bromocriptine or cabergoline) inhibit prolactin secretoin and thus can be used to treat prolactinoma.

58

What do dopamine antagonists (most antipsychotics) and estrogens (OCPs, pregnancy) do?

Stimulate prolactin secretion

59

What is used for the treatment of central Diabetes Insipidus?

Desmopressin (ADH analog; intranasal DDAVP)

60

What can exogenous corticosteroids cause?

Reactivation of TB and candidiasis (blocked IL-2 production)

61

What is the difference between Propylthiouracil and Methimazole?

Propulthiouracil inhibits both peroxidase and 5'-deiodinase. Methimazole inhibits peroxidase only.

62

What can be used to interfere with trapping of Iodide?

Anions (perchlorate, pertechnetate, and thiocyanate)

63

What is the treatment for Primary Hyperaldosteronism?

Surgery to remove the tumor and/or spironolactone, a K+ sparing diuretic that acts as an aldosterone antagonist

64

What is the treatment for Secondary Hyperaldosteronism?

Spironolactone

65

What is used in the treatment of Pheochromocytoma?

Irreversible α-antagonists (phenoxybenzamine) and β-blockers followed by tumor resection. α-blockade must be achieved before giving β-blockers to avoid a hypertensive crisis.

66

How do you treat a Thyroid storm?

3 P's: β-blockers (e.g., Propranolol), Propylthiouracil, corticosteroids (e.g., Prednisolone)

67

How do you treat Acromegaly?

Octreotide (somatostatin analog) or pegvisomant (growth hormone receptor antagonist)

68

What do you treat Nephrogenic Diabetes Insipidus with?

HCTZ, indomethacin, amiloride
Hydration

69

What drugs can cause Nephrogenic Diabetes Insipidus?

Lithium, democlocycline (ADH antagonist)

70

What drug can cause SIADH?

Cyclophosphamide

71

What is the treatment for SIADH?

Conivaptan, tolvaptan, demeclocycline

72

What is the treatment for hypopituitarism?

Hormone replacement therapy (corticosteroids, thyroxine, sex steroids, human growth hormone)

73

What is the treatment for Carcinoid syndrome?

Resection, somatostatin analog (e.g., octreotide)