Pharmacology: Endocrine drugs Flashcards

1
Q

Lispro

A

Rapid-acting insulin

  • Binds insulin R (cell surface receptor tyrosine kinase with intrinsic activity, MAP kinase)
  • Liver: incr glycogen storage
  • Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
  • Fat: incr TG storage
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2
Q

Aspart

A

Rapid-acting insulin

  • Binds insulin R (receptor tyrosine kinase with intrinsic activity, MAP kinase)
  • Liver: incr glycogen storage
  • Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
  • Fat: incr TG storage
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3
Q

Regular insulin

A

Short-acting insulin

  • Binds insulin R (receptor tyrosine kinase with intrinsic activity, MAP kinase)
  • Liver: incr glycogen storage
  • Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
  • Fat: incr TG storage
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4
Q

NPH

A

Intermediate-acting insulin

  • Binds insulin R (receptor tyrosine kinase with intrinsic activity, MAP kinase)
  • Liver: incr glycogen storage
  • Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
  • Fat: incr TG storage
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5
Q

Detemir

A

Long-acting insulin

  • Binds insulin R (receptor tyrosine kinase with intrinsic activity, MAP kinase)
  • Liver: incr glycogen storage
  • Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
  • Fat: incr TG storage
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6
Q

Glargine

A

Long-acting insulin

  • Binds insulin R (receptor tyrosine kinase with intrinsic activity, MAP kinase)
  • Liver: incr glycogen storage
  • Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
  • Fat: incr TG storage
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7
Q

Tolbutamide

A

First generation sulfonylurea

  • Close K+ATP channel => cell depolarization => Ca2+ influx => insulin release
  • Disulfiram-like effects
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8
Q

Chlorpropamide

A

First generation sulfonylurea

  • Close K+ATP channel => cell depolarization => Ca2+ influx => insulin release
  • Disulfiram-like effects
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9
Q

Glyburide

A

Second generation sulfonylurea

  • Close K+ATP channel on pancreatic beta cells => cell depolarization => Ca2+ influx => insulin release
  • Hypoglycemia
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10
Q

Glimepiride

A

Second generation sulfonylurea

  • Close K+ATP channel on pancreatic beta cells => cell depolarization => Ca2+ influx => insulin release
  • Hypoglycemia
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11
Q

Glipizide

A

Second generation sulfonylurea

  • Close K+ATP channel on pancreatic beta cells => cell depolarization => Ca2+ influx => insulin release
  • Hypoglycemia
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12
Q

Metformin

A

Biguanide

  • Unk mechanism: DECR gluconeogenesis, incr glycolysis and peripheral glucose uptake/insulin sensitivity
  • Lactic acidosis! *Don’t give in RF, check BUN/Cr
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13
Q

Pioglitazone

A

Glitazone/thiazolidinedione

  • Bind to nuclear PPAR-gamma (peroxisome proliferator-activated receptor), in family of steroid and thyroid nuclear receptors, affects transcription
  • Effects: 1) incr adiponectin, 2) incr FA transport protein, 3) incr insulin R substrate, 4) incr Glut4
  • SEs: weight gain (from fluid), edema (caution in CHF), hepatotoxity (check LFTs!), heart failure.
  • NO hypoglycemia
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14
Q

Rosiglitazone

A

Glitazone/thiazolidinedione

  • Bind to nuclear PPAR-gamma (peroxisome proliferator-activated receptor), in family of steroid and thyroid nuclear receptors, affects transcription
  • Effects: 1) incr adiponectin, 2) incr FA transport protein, 3) incr insulin R substrate, 4) incr Glut4
  • SEs: weight gain, edema, hepatotoxity, heart failure.
  • NO hypoglycemia
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15
Q

Acarbose

A

alpha-glucosidase inhibitor

  • Inhibits intestinal brush border alpha-glucosidases
  • Decreases post-prandial hypergly
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16
Q

Miglitol

A

alpha-glucosidase inhibitor

  • Inhibits intestinal brush border alpha-glucosidases
  • Decreases post-prandial hypergly
17
Q

Pramlintide

A

Mimetic

- Mimics amylin (secreted with insulin): decr glucagon and inh gastric mobility

18
Q

Exenatide

A

GLP-1 analog
- Incr insulin, decr glucagon release

GLP-1 (cAMP-coupled R)

  • incretin hormone secreted by intestinal L cells in response to food intake
  • decreases blood glucose by incr satiety, decr gastric emptying, incr insulin release from pancreatic beta cells
19
Q

Repaglinide

A

Meglitinide

- Similar to sulfonylureas; bind to different spot on K+ channel

20
Q

Nateglinide

A

Meglitinide

- Similar to sulfonylureas; bind to different spot on K+ channel

21
Q

Sitagliptine

A

DD4 inhibitor
- DD4 normally degrades GLP-1 (an incretin hormone secreted by intestinal L cells in response to food intake–incr insulin and decr gastric motility and glucagon)

22
Q

Vildagliptine

A

DD4 inhibitor
- DD4 normally degrades GLP-1 (an incretin hormone secreted by intestinal L cells in response to food intake–incr insulin and decr gastric motility and glucagon)

23
Q

PTU vs. Methimazole

A

PTU: inhibits both peroxidase (thyroid) and 5’-deiodinase (peripheral T4 to T3 conversion), heptatotoxic
Methimazole: inhibits peroxidase only, possible teratogen

24
Q

Levothyroxine

A

Hypothyroid

25
Q

Perchlorate

A

Anion, competitively inhibits basolateral Na-I symporter on thyroid follicular cells
- Tx: Hyperthyroid

26
Q

Pertechnetate

A

Anion, competitively inhibits basolateral Na-I symporter on thyroid follicular cells
- Tx: Hyperthyroid

27
Q

Which diabetic drug requires some islet cell function?

A

Sulfonylureas, because they increase endogenous insulin secretion from beta cells

28
Q

GH

A

Tx: GH deficiency, Turner’s

29
Q

SST

A

AKA Octreotide

Tx: Acromegaly, carcinoid, gastrinoma, glucaconoma

30
Q

Oxytocin

A

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

31
Q

ADH (desmopressin)

A

Pituitary/central DI

32
Q

Demeclocycline

A

A tetracycline, used to treat SIADH but can cause nephrogenic DI, photosensitivity, bone and teeth abnormalities

33
Q

Hydroxycortisone

A

Glucocorticoid
Indications: Addison’s disease, immunosuppression, inflammation, asthma
SE: Iatrogenic Cushing’s; adrenal insufficiency, >3 weeks of use/more potent GCs increase risk of insufficiency after d/c

34
Q

Prednisone

A

Glucocorticoid
Indications: Addison’s disease, immunosuppression, inflammation, asthma
SE: Iatrogenic Cushing’s; adrenal insufficiency, >3 weeks of use/more potent GCs increase risk of insufficiency after d/c

35
Q

Triamcinolone

A

Glucocorticoid
Indications: Addison’s disease, immunosuppression, inflammation, asthma
SE: Iatrogenic Cushing’s; adrenal insufficiency, >3 weeks of use/more potent GCs increase risk of insufficiency after d/c

36
Q

Dexamethasone

A

Glucocorticoid
Indications: Addison’s disease, immunosuppression, inflammation, asthma
SE: Iatrogenic Cushing’s; adrenal insufficiency, >3 weeks of use/more potent GCs increase risk of insufficiency after d/c

37
Q

Beclomethasone

A

Glucocorticoid
Indications: Addison’s disease, immunosuppression, inflammation, asthma
SE: Iatrogenic Cushing’s; adrenal insufficiency, >3 weeks of use/more potent GCs increase risk of insufficiency after d/c