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Block 7 Flashcards

1
Q

Chlorpropamide

A
  • 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
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2
Q

Tolbutamide

A
  • 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
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3
Q

Glimepiride

A
  • 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
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4
Q

glipizide

A
  • 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
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5
Q

glyburide

A
  • 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
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6
Q

Metformin

A
  • Biguanide
    • Stimulates AMPK
    • 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 (check creatinine)
    • weight loss – good for obese pts
    • GI upset
  • C/I in renal insufficiency
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7
Q

Pioglitazone

A
  • Glitazone / TZD
    • Binds to PPAR-γ nuclear transcription regulator → increases periph tissue insulin sensitivity
  • Use: mono- or combo therapy in T2DM
  • S/E:
    • weight gain
    • edema
    • hepatotoxicity
    • HF
    • increased risk fractures
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8
Q

rosiglitazone

A
  • Glitazone / TZD
    • Binds to PPAR-γ nuclear transcription regulator → increases periph tissue insulin sensitivity
  • Use: mono- or combo therapy in T2DM
  • S/E:
    • weight gain
    • edema
    • hepatotoxicity
    • HF
    • increased risk fractures
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9
Q

PPAR-γ

A
  • Nuclear transcription regulator
  • Genes activated by PPAR-γ regulate FA storage and glucose metabolism
  • Activation of PPAR-γ increases insulin sensitivity and adiponectin levels
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10
Q

Lispro

A
  • 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
Q

Aspart

A
  • 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
Q

Glulisine

A
  • 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
Q

Regular insulin

A
  • Short-acting
  • Use:
    • T1DM
    • T2DM
    • GDM
    • DKA
    • Hyperkalemia
    • Stress hyperglycemia
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14
Q

NPH

A
  • Intermediate-Acting Insulin
  • Use:
    • T1DM
    • T2DM
    • GDM
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15
Q

Detemir

A
  • Long-acting insulin
  • Use:
    • T1DM
    • T2DM
    • GDM - basal control
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16
Q

glargine

A
  • Long-acting (24h) insulin
  • Use:
    • T1DM
    • T2DM
    • GDM - basal control
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17
Q

Nateglinide

A
  • 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
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18
Q

repaglinide

A
  • 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
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19
Q

Exenatide

A
  • GLP-1 analog
    • increases glucose-dependent insulin release + satieity
    • decreases glucagon release + gastric emptying
  • Use: T2DM
  • S/E:
    • Nausea/vomiting
    • Pancreatitis
    • modest weight loss
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20
Q

liraglutide

A
  • GLP-1 analog
    • increases glucose-dependent insulin release + satieity
    • decreases glucagon release + gastric emptying
  • Use: T2DM
  • S/E:
    • Nausea/vomiting
    • Pancreatitis
    • modest weight loss
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21
Q

Linagliptin

A
  • DPP-4 inhibitor
    • Inhibits DPP-4 enzyme → active GLP-1
    • inc glucose-dependent insulin release & satiety
    • dec glucagon release & gastric emptying
  • Use: T2DM
  • S/E:
    • Mild urinary or respiratory infections
    • weight neutral
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22
Q

saxagliptin

A
  • DPP-4 inhibitor
    • Inhibits DPP-4 enzyme → active GLP-1
    • inc glucose-dependent insulin release & satiety
    • dec glucagon release & gastric emptying
  • Use: T2DM
  • S/E:
    • Mild urinary or respiratory infections
    • weight neutral
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23
Q

sitagliptin

A
  • DPP-4 inhibitor
    • Inhibits DPP-4 enzyme → active GLP-1
    • inc glucose-dependent insulin release & satiety
    • dec glucagon release & gastric emptying
  • Use: T2DM
  • S/E:
    • Mild urinary or respiratory infections
    • weight neutral
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24
Q

Pramlintide

A
  • Amylin analog
    • Decreases glucagon + gastric emptying
  • Use:
    • T1DM
    • T2DM
  • S/E:
    • Hypoglycemia (w/mistimed prandial insulin)
    • nausea
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25
Q

Canagliflozin

A
  • SGLT-2 inhibitor
    • Blocks glucose reabsorption in PCT
  • Use: T2DM
  • S/E:
    • Glucosuria
    • UTI
    • vaginal yeast infxn
    • hypERkalemia
    • dehydration (→ orthostatic hypOtension)
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26
Q

dapagliflozin

A
  • SGLT-2 inhibitor
    • Blocks glucose reabsorption in PCT
  • Use: T2DM
  • S/E:
    • Glucosuria
    • UTI
    • vaginal yeast infxn
    • hypERkalemia
    • dehydration (→ orthostatic hypOtension)
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27
Q

empagliflozin

A
  • SGLT-2 inhibitor
    • Blocks glucose reabsorption in PCT
  • Use: T2DM
  • S/E:
    • Glucosuria
    • UTI
    • vaginal yeast infxn
    • hypERkalemia
    • dehydration (→ orthostatic hypOtension)
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28
Q

Acarbose

A
  • α-glucosidase inhibitor
    • Inhibits intestinal brush-border α-glucosidases → delays carb hydrolysis, glucose absorption → decreases postprandial hypERglycemia
  • Use: T2DM
  • S/E: GI upset
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29
Q

miglitol

A
  • α-glucosidase inhibitor
    • Inhibits intestinal brush-border α-glucosidases → delays carb hydrolysis, glucose absorption → decreases postprandial hypERglycemia
  • Use: T2DM
  • S/E: GI upset
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30
Q

T1DM Rx Strategies

A

low-carb diet + insulin replacement

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31
Q

T2DM Rx Strategies

A
  • dietary modification and exercise for weight loss
  • oral agents
  • non-insulin injectables
  • insulin replacement
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32
Q

GDM Rx Strategies

A
  • dietary modifications
  • exercise
  • insulin replacement if lifestyle modification fails
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33
Q

Propylthiouracil (PTU)

A
  • Thioamide
    • 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
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34
Q

Methimazole

A
  • Thioamide
    • 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
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35
Q

Levothyroxine

A
  • 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, Ca2+ (dec absorp)
    • Amiodarone (inhib T4 → T3)
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36
Q

Triiodothyronine

A
  • Synthetic T3
  • Use:
    • HypOthyroidism
    • Myxedema
    • Weight loss (off-label)
  • S/E:
    • Tachycardia
    • heat intolerance
    • tremors
    • arrhythmias
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37
Q

Radioactive iodine (RAI, 131I)

A
  • Concentrates in thyroid gland → follicular necrosis
  • Use: most common Rx for hypERthyroidism
  • C/I: children, pregnancy/lactation
  • S/E: hypOthyroidism
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38
Q

Rx Thyroid Storm

A
  • PTU
  • iodides
  • propranolol
  • corticosteroids
  • supportive measures
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39
Q

Thyroid Storm

A
  • 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%
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40
Q

Iodine

A
  • 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)
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41
Q

Potassium Iodide

A
  • Competitively inhibits uptake of radioactive iodine
  • Use: decrease risk of developing thyroid cancer after exposure to radioactive iodine
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42
Q

Myxedema Coma

A
  • End stage of uncontrolled, long-standing hypOthyroidism
  • Advanced hypothyroid symptoms, hypothermia, delirium, and coma
  • Mortality 60-70%
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43
Q

Rx Myxedema Coma

A
  • Aggressive treatment:
    • IV thyroxine
    • glucocorticoids
    • supportive measures
  • Improvement of symptoms within 24 hrs
  • Switch to oral levothyroxine once pt is stable
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44
Q

conivaptan

A
  • ADH antagonist
    • Blocks action of ADH at collecting duct V2-receptor
  • Use: SIADH
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45
Q

tolvaptan

A
  • ADH antagonist
    • Blocks action of ADH at collecting duct V2-receptor
  • Use: SIADH
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46
Q

Desmopressin acetate

A
  • 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
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47
Q

GH

A

Use:

  • GH deficiency
  • Turner Syndrome
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48
Q

Oxytocin

A

Use:

  • Stimulates labor, uterine contractions, milk let-down
  • Controls uterine hemorrhage
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49
Q

Somatostatin (octreotide)

A
  • Inhibits GH
  • Use:
    • Acromegaly
    • carcinoid syndrome
    • gastrinoma
    • glucagonoma
    • esophageal varices
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50
Q

Demeclocycline

A
  • ADH antagonist (tetracycline family)
  • Use: SIADH
  • S/E:
    • Nephrogenic DI
    • photosensitivity
    • abnormalities of bone and teeth
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51
Q

Fludrocortisone

A
  • Synthetic aldosterone analog
    • Few glucocorticoid effects
  • Use: Mineralocorticoid replacement in 1° adrenal insufficiency
  • S/E:
    • edema
    • HF exacerbation
    • hyperpigmentation
    • Others similar to glucocorticoids
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52
Q

Cinacalcet

A
  • Sensitizes parathyroid gland Ca2+-sensing receptor to circulating Ca2+ → decreases PTH
  • Use: 1° or 2° hyperparathyroidism
  • S/E: HypOcalcemia
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53
Q

Lovastatin

A
  • HMG-CoA Reductase inhibitor
    • Inhibits conversion of HMG-CoA → mevalonate
    • Up-regulates LDL receptors
  • Decreases LDL, increases HDL, decreases TG
  • Use: Hypercholesterolemia
    • Decreases mortality in CAD pts
  • S/E:
    • Hepatotoxicity / elevated LFTs
    • Myopathy (+fibrates or niacin)
  • C/I in pregnancy
  • CYP3A4 metab
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54
Q

atorvastatin

A
  • HMG-CoA Reductase inhibitor
    • Inhibits conversion of HMG-CoA → mevalonate
    • Up-regulates LDL receptors
  • Decreases LDL, increases HDL, decreases TG
  • Use: Hypercholesterolemia
    • Decreases mortality in CAD pts
  • S/E:
    • Hepatotoxicity / elevated LFTs
    • Myopathy (+fibrates or niacin)
  • C/I in pregnancy
  • CYP3A4 metab
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55
Q

simvastatin

A
  • HMG-CoA Reductase inhibitor
    • Inhibits conversion of HMG-CoA → mevalonate
    • Up-regulates LDL receptors
  • Decreases LDL, increases HDL, decreases TG
  • Use: Hypercholesterolemia
    • Decreases mortality in CAD pts
  • S/E:
    • Hepatotoxicity / elevated LFTs
    • Myopathy (+fibrates or niacin)
  • C/I in pregnancy
  • CYP3A4 metab
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56
Q

Pravastatin

A
  • HMG-CoA Reductase inhibitor
    • Inhibits conversion of HMG-CoA → mevalonate
    • Up-regulates LDL receptors
  • Decreases LDL, increases HDL, decreases TG
  • Use: Hypercholesterolemia
    • Decreases mortality in CAD pts
  • S/E:
    • Hepatotoxicity / elevated LFTs
    • Myopathy (+fibrates or niacin)
  • C/I in pregnancy
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57
Q

Cholestyramine

A
  • Bile Acid Resin
    • Anion exchg in bowel removes bile acids from circ → liver uses cholesterol to make more bile acids + up-regulates LDL receptors
  • Decreases LDL, slightly increases HDL + TG
  • Use: Hypercholesterolemia
    • works best in combo w/statin
  • S/E:
    • GI upset
    • Decreased absorption of other drugs, fat-soluble vitamins
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58
Q

Colestipol

A
  • Bile Acid Resin
    • Anion exchg in bowel removes bile acids from circ → liver uses cholesterol to make more bile acids + up-regulates LDL receptors
  • Decreases LDL, slightly increases HDL + TG
  • Use: Hypercholesterolemia
    • works best in combo w/statin
  • S/E:
    • GI upset
    • Decreased absorption of other drugs, fat-soluble vitamins
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59
Q

Colesevalam

A
  • Bile Acid Resin
    • Anion exchg in bowel removes bile acids from circ → liver uses cholesterol to make more bile acids + up-regulates LDL receptors
  • Decreases LDL, slightly increases HDL + TG
  • Use: Hypercholesterolemia
    • works best in combo w/statin
  • S/E:
    • GI upset
    • Decreased absorption of other drugs, fat-soluble vitamins
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60
Q

Ezetimibe

A
  • Prevents cholesterol absorption at small intestine brush border
    • inhibits NPC1L1 transporter protein
  • Decreases LDL
  • Use: Hypercholesterolemia
  • S/E:
    • Rare increase in LFTs
    • Diarrhea
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61
Q

Gemfibrozil

A
  • Fibrate
    • Upregulates LPL → increases TG clearance
    • Activates PPAR-α → induces HDL synth
  • Decreases TG, slightly decreases LDL, increases HDL
  • Use: Hypercholesterolemia
  • S/E:
    • Myopathy (+statins)
    • Cholesterol gallstones
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62
Q

bezafibrate

A
  • Fibrate
    • Upregulates LPL → increases TG clearance
    • Activates PPAR-α → induces HDL synth
  • Decreases TG, slightly decreases LDL, increases HDL
  • Use: Hypercholesterolemia
  • S/E:
    • Myopathy (+statins)
    • Cholesterol gallstones
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63
Q

fenofibrate

A
  • Fibrate
    • Upregulates LPL → increases TG clearance
    • Activates PPAR-α → induces HDL synth
  • Decreases TG, slightly decreases LDL, increases HDL
  • Use: Hypercholesterolemia
  • S/E:
    • Myopathy (+statins)
    • Cholesterol gallstones
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64
Q

Niacin / Vitamin B3

A
  • Inhibits lipolysis (hormone-sensitive lipase) in adipose → reduces hepatic VLDL synth
  • Decreases LDL, increases HDL, slightly decreases TG
  • Use: Hypercholesterolemia
  • S/E:
    • PG release → Red, flushed face (decreased by NSAIDs, long-term use)
    • HypERglycemia
    • HypERuricemia
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65
Q

Cyclosporine

A
  • Calcineurin inhibitor
    • binds cyclophilin → prevents IL-2 transcription → blocks T-cell activation
  • Use:
    • Transplant rejection prophylaxis
    • psoriasis
    • rheumatoid arthritis
  • S/E:
    • Nephrotoxicity
    • HTN
    • hyperlipidemia
    • neurotoxicity
    • gingival hyperplasia
    • hirsutism
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66
Q

Tacrolimus (FK506)

A
  • Calcineurin inhibitor
    • Binds FK506 binding protein (FKBP) → prevents IL-2 transcription → blocks T-cell activation
  • Use: Transplant rejection prophylaxis.
  • S/E:
    • Nephrotoxicity
    • increased risk of diabetes and neurotoxicity
    • HTN
    • hyperlipidemia
    • NO gingival hyperplasia or hirsutism
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67
Q

Sirolimus

A
  • aka Rapamycin
  • Binds FKBP → inhibits mTOR
  • Use: Kidney transplant rejection prophylaxis
  • S/E:
    • Pan”Sirtopenia” (pancytopenia)
    • insulin resistance
    • hyperlipidemia
    • NOT nephrotoxic
  • Synergistic w/cyclosporine
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68
Q

Rapamycin

A
  • aka Sirolimus
    • Binds FKBP → inhibits mTOR
  • Use: Kidney transplant rejection prophylaxis
  • S/E:
    • Pan”Sirtopenia” (pancytopenia)
    • insulin resistance
    • hyperlipidemia
    • NOT nephrotoxic
  • Synergistic w/cyclosporine
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69
Q

Daclizumab

A
  • Monoclonal Ab
    • Blocks IL-2R
  • Use: Kidney transplant rejection prophylaxis
  • S/E:
    • Edema
    • HTN
    • tremor
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70
Q

basiliximab

A
  • Monoclonal Ab
    • Blocks IL-2R
  • Use: Kidney transplant rejection prophylaxis
  • S/E:
    • Edema
    • HTN
    • tremor
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71
Q

Azathioprine

A
  • Antimetabolite precursor of 6-mercaptopurine
    • Blocks nucleotide synthesis → inhibits lymphocyte prolif
  • Use:
    • Transplant rejection prophylaxis
    • rheumatoid arthritis
    • Crohn disease
    • glomerulonephritis
    • other autoimmune conditions
  • S/E:
    • Leukopenia
    • anemia
    • thrombocytopenia
  • Toxicity increased by allopurinol (xanthine oxidase degrades 6-MP)
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72
Q

Mycophenolate mofetil

A
  • Reversibly inhibit IMP dehydrogenase → prevent purine synthesis → inhibit B and T cell responses
  • Use:
    • Transplant rejection prophylaxis
    • lupus nephritis
  • S/E:
    • GI upset
    • pancytopenia
    • HTN
    • hypERglycemia
    • Less nephrotoxic and neurotoxic
  • Assoc w/invasive CMV infxn
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73
Q

Corticosteroids

A
  • Multiple fcns
    • Inhibit NF-κB
    • decrease transcription of many cytokines → Suppress both B- and T-cell fcn
    • Induce apoptosis of T lymphocytes
  • Use:
    • Transplant rejection prophylaxis
    • many autoimmune and inflamm d/o
  • S/E:
    • Hyperglycemia
    • osteoporosis
    • central obesity
    • muscle breakdown
    • psychosis
    • acne
    • HTN
    • cataracts
    • avascular necrosis (femoral head)
    • iatrogenic Cushing syndrome.
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74
Q

Aldesleukin

A
  • Recombinant cytokine: IL-2
  • Use:
    • Renal cell carcinoma
    • metastatic melanoma
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75
Q

Epoetin alfa

A
  • Recombinant cytokine: EPO
  • Use: Anemias (especially in renal failure)
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76
Q

Filgrastim

A
  • Recombinant cytokine: G-CSF
  • Use: Recovery of bone marrow
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77
Q

Sargramostim

A
  • Recombinant cytokine: GM-CSF
  • Use: Recovery of bone marrow
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78
Q

IFN-α

A
  • Recombinant cytokine
  • Use:
    • Chronic hepatitis B and C
    • Kaposi sarcoma
    • malignant melanoma
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79
Q

IFN-β

A
  • Recombinant cytokine
  • Use: Multiple sclerosis
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80
Q

IFN-γ

A
  • Recombinant cytokine
  • Use: Chronic granulomatous disease
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81
Q

Romiplostim

A
  • Recombinant cytokine
    • thrombopoietin receptor agonist
  • Use: Thrombocytopenia
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82
Q

eltrombopag

A
  • Recombinant cytokine
    • thrombopoietin receptor agonist
  • Use: Thrombocytopenia
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83
Q

Oprelvekin

A
  • Recombinant cytokine: IL-11
  • Use: Thrombocytopenia
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84
Q

Immunosuppression targets

A
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86
Q

Alemtuzumab

A
  • Target: CD52
  • Use:
    • CLL
    • MS
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87
Q

Bevacizumab

A
  • Target: VEGF
  • Use:
    • Colorectal cancer
    • renal cell carcinoma
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88
Q

Cetuximab

A
  • Target: EGFR
  • Use:
    • Stage IV colorectal cancer
    • head and neck cancer
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89
Q

Rituximab

A
  • Target: CD20 (B cells)
  • Use:
    • B-cell non-Hodgkin lymphoma
    • CLL
    • rheumatoid arthritis
    • ITP
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90
Q

Trastuzumab

A
  • Target: HER2/neu
  • Use: Breast cancer
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91
Q

Adalimumab

A
  • Target: Soluble TNF-α
  • Use:
    • IBD
    • rheumatoid arthritis
    • ankylosing spondylitis
    • psoriasis
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92
Q

certolizumab

A
  • Target: Soluble TNF-α
  • Use:
    • IBD
    • rheumatoid arthritis
    • ankylosing spondylitis
    • psoriasis
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93
Q

infliximab

A
  • Target: Soluble TNF-α
  • Use:
    • IBD
    • rheumatoid arthritis
    • ankylosing spondylitis
    • psoriasis
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94
Q

Eculizumab

A
  • Target: Complement protein C5
  • Use: Paroxysmal nocturnal hemoglobinuria
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95
Q

Natalizumab

A
  • Target: α4-integrin (WBC adhesion)
  • Use:
    • Multiple sclerosis
    • Crohn disease
  • S/E: Risk of PML in pts w/JC virus
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96
Q

Abciximab

A
  • Target: Platelet GPIIb/IIIa
  • Use: Antiplatelet agent for prevention of ischemic complications in patients undergoing percutaneous coronary intervention
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97
Q

Denosumab

A
  • Target: RANKL
    • inhibits osteoclast maturation (mimics osteoprotegerin)
  • Use: Osteoporosis
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98
Q

Digoxin immune Fab

A
  • Target: Digoxin
  • Use: Antidote for digoxin toxicity
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99
Q

Omalizumab

A
  • Target: IgE
    • prevents IgE binding to FcεRI
  • Use: Allergic asthma
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100
Q

Palivizumab

A

Target: RSV F protein

Use: RSV prophylaxis for high-risk infants

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101
Q

Ranibizumab

A
  • Target: VEGF
  • Use: Neovascular age-related macular degeneration
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102
Q

bevacizumab

A
  • Target: VEGF
  • Use: Neovascular age-related macular degeneration
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103
Q

Hyperacute Transplant Rejection

A
  • Within minutes
  • Pre-existing recipient antibodies react to
  • donor antigen (T2HS) → activate complement.
  • Widespread thrombosis of graft vessels → ischemia/necrosis.
  • Graft must be removed.
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104
Q

Acute Transplant Rejection

A
  • Weeks to months
    • Cellular: CD8+ T cells activated against donor MHCs (T4HS)
    • Humoral: similar to hyperacute, except Ab’s develop after transplant.
  • Vasculitis of graft vessels with dense interstitial lymphocytic infiltrate.
  • Prevent/reverse with immunosuppressants.
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105
Q

Chronic Transplant Rejection

A
  • Months to years
  • CD4+ T cells respond to recipient APCs presenting donor peptides, including allogeneic MHC.
  • Has both cellular and humoral components (T2HS and T4HS).
  • Recipient T cells react and secrete cytokines → proliferation of vascular smooth muscle, parenchymal atrophy, interstitial fibrosis.
  • Dominated by arteriosclerosis.
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106
Q

Graft-vs-Host Disease

A
  • Timing varies
  • Grafted T cells proliferate in immunocompromised host and reject host cells with “foreign” proteins (T4HS) → severe organ dysfcn
  • Maculopapular rash, jaundice, diarrhea, hepatosplenomegaly.
  • Usually in bone marrow and liver transplants (rich in lymphocytes).
  • Potentially beneficial in bone marrow transplant for leukemia (graft-versus-tumor effect).
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107
Q

Bronchiolitis obliterans

A

Chronic lung graft rejection

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108
Q

Accelerated atherosclerosis

A

Chronic heart transplant rejection

109
Q

Chronic graft nephropathy

A

Chronic kidney graft rejection

110
Q

Vanishing bile duct syndrome

A

Chronic liver graft rejection

111
Q

Methotrexate

A
  • Folate analog
    • competitively inhibits dihydrofolate reductase → decreases dTMP → decreases pyrimidine & DNA synthesis
  • Use: malignancy
  • S/E:
    • Oral, GI ulcers
    • Pancytopenia / BM suppresssion (reversible w/leucovorin)
    • Alopecia
    • Hepatotoxicity
    • Pulmonary fibrosis
112
Q

Leflunomide

A
  • Reversibly inhibits dihydroorotate dehydrogenase → prevents pyrimidine synth
    • Suppresses T-cell proliferation
  • Use:
    • Rheumatoid arthritis
    • psoriatic arthritis
  • S/E:
    • Diarrhea
    • HTN
    • hepatotoxicity
    • teratogenicity
113
Q

trimethoprim

A
  • Folate analog
    • inhibits bacterial dihydrofolate reductase → decreases pyrimidine & DNA synthesis
  • Use: + sulfamethazole for various bacterial infxns
  • S/E:
    • Megaloblastic anemia
    • leukopenia
    • granulocytopenia
    • (May alleviate with supplemental folinic acid).
114
Q

pyrimethamine

A
  • inhibits protozoan dihydrofolate reductase → decreases pyrimidine & DNA synthesis
  • Use: Toxoplasmosis
115
Q

Cyclophosphamide

A
  • Alkylating agent
    • Cross-links DNA at guanine N-7.
    • Requires bioactivation by liver.
  • Use:
    • Solid tumors
    • leukemia
    • lymphomas
  • S/E:
    • Myelosuppression
    • hemorrhagic cystitis: prevent w/mesna (thiol group binds toxic metabolites) or N-acetylcysteine
116
Q

Anakinra

A
  • Recombinant cytokine: IL-1 receptor antagonist
  • Use: rheumatoid arthritis
117
Q

Tocilizumab

A
  • Recombinant cytokine: IL-6 receptor antagonist
  • Use:
    • Giant cell arteritis
    • Rheumatoid arthritis
118
Q

Muromonab

A
  • aka OKT3
  • mouse monoclonal antibody against human CD3 (co-receptor for T-cell receptor activation)
  • S/E: cytokine release syndrome (Fever, myalgias, nausea, diarrhea)
119
Q

OKT3

A
  • aka muromonab
  • mouse monoclonal antibody against human CD3 (co-receptor for T-cell receptor activation)
  • S/E: cytokine release syndrome (Fever, myalgias, nausea, diarrhea)
120
Q

Levamisole

A
  • “Restores” depressed immune function of B & T cells, monocytes, and macrophages.
  • Its only clinical indication is as adjuvant therapy w/5-FU after surgical resection in patients with colon cancer
121
Q

Thalidomide

A
  • Available only under a restricted distribution program and can be prescribed only by specially licensed physicians
  • Indicated for the treatment of erythema nodosum leprosum (decreases TNF-α)
    • In HIV patients it is known to increase TNF-α
  • S/E: Teratogenicity – Limb defects (phocomelia, micromelia; “flipper” limbs)
122
Q

Bacillus Calmette-Guerin (BCG)

A
  • Attenuated, live culture of the bacillus of Calmette and Guerin strain of Mycobacterium bovis
  • Mechanism unclear
  • Use: prophylaxis/Rx of carcinoma in situ of urinary bladder
  • Can cause positive PPD
123
Q

Rho(D) Immune Globulin

A
  • IgG containing high titer of Ab’s against Rh(D) Ag
    • binds Rho antigens → prevents sensitization
  • Use: prevents maternal anti-D IgG production in Rh- mothers (prev exposed to Rh+ blood) w/Rh+ baby
124
Q

Kleihauer-Betke test

A

Postnatal maternal blood sample is analyzed to see how much fetal blood has entered maternal circulation so we can determine dose of RhoD immune globulin

125
Q

Methylphenidate

A
  • Stimulant
  • Inhibits DAT and NET → decreases reuptake of DA and NE
  • Use: ADHD
  • S/E
    • Tic disorders (transient and chronic)
    • DA elevation – may worsen pre-existing psychosis
    • Abuse potential
  • Interactions
    • CYP 2D6 inhibitors (SSRIs)
    • MAOIs
    • TCAs
    • Phenytoin
    • Clonidine
126
Q

Amphetamines

A
  • Stimulants
  • Inhibit DAT and NET → decrease reuptake of DA and NE and enhance DA release
  • Use: ADHD
  • S/E:
    • CV events
127
Q

Atomoxetine

A
  • NON-stimulant
  • Selective NE reuptake inhibitor
  • Use: ADHD
  • S/E:
    • Severe liver disease
    • Potential suicidal ideation
128
Q

ADHD Rx Preference

A
  1. Stimulants
  2. Non-stimulants
  3. TCAs, Bupropion
  4. Clonidine, Guanfacine
129
Q

Calcium Salts

A
  • Use:
    • HypOcalcemia
    • Prevention/Rx Osteoporosis
  • S/E:
    • MI
    • Constipation
    • Decreased absorption of ciprofloxacin, phenytoin, levothyroxine and tetracyclines
130
Q

Vitamin D

A
  • Increases bone formation
    • Increases calcibindin (Ca2+ carrier protein) synth
    • Increases Ca2+ and PO43- absorption from intestines, kidney, bone
  • Use: Osteoporosis
131
Q

ergocalciferol

A

Vitamin D2

132
Q

cholecalciferol

A

Vitamin D3

133
Q

calcitriol

A

1,25-dihydroxyvitamin D3 (most active form)

134
Q

calcifediol

A

25-hydroxycholecalciferol

135
Q

Teriparatide

A
  • Recombinant human PTH
  • Use: Osteoporosis
    • Short-term: stim osteoBlasts > osteoclasts
    • Long-term: stim osteoClasts
  • S/E:
    • Increased risk osteosarcoma
    • Transient hypERcalcemia
136
Q

Alendronate

A
  • Bisphosphonate
    • Pyrophosphate analog → binds hydroxyapatite in bone → inhibits osteoClast activity
  • Use:
    • Osteoporosis
    • HypERcalcemia
    • Paget bone
    • Metastatic bone disease
    • Osteogenesis imperfecta
  • S/E:
    • Esophagitis
    • osteonecrosis of jaw
    • atypical stress fractures
137
Q

Ibandronate

A
  • Bisphosphonate
    • Pyrophosphate analog → binds hydroxyapatite in bone → inhibits osteoClast activity
  • Use:
    • Osteoporosis
    • HypERcalcemia
    • Paget bone
    • Metastatic bone disease
    • Osteogenesis imperfecta
  • S/E:
    • Esophagitis
    • osteonecrosis of jaw
    • atypical stress fractures
138
Q

Risedronate

A
  • Bisphosphonate
    • Pyrophosphate analog → binds hydroxyapatite in bone → inhibits osteoClast activity
  • Use:
    • Osteoporosis
    • HypERcalcemia
    • Paget bone
    • Metastatic bone disease
    • Osteogenesis imperfecta
  • S/E:
    • Esophagitis
    • osteonecrosis of jaw
    • atypical stress fractures
139
Q

Zoledronate

A
  • Bisphosphonate
    • Pyrophosphate analog → binds hydroxyapatite in bone → inhibits osteoClast activity
  • Use:
    • Osteoporosis
    • HypERcalcemia
    • Paget bone
    • Metastatic bone disease
    • Osteogenesis imperfecta
  • S/E:
    • Esophagitis
    • osteonecrosis of jaw
    • atypical stress fractures
140
Q

Calcitonin

A
  • Keeps bone in
    • Inhibits osteoClast bone resorption
    • Promotes osteoBlast Ca2+ deposition
  • Use: HypERcalcemic states
    • Postmenopausal osteoporosis
    • Paget’s disease
  • Used only short-term–long-term fx unclear
141
Q

Denosumab

A
  • Human IgG2 monoclonal antibody
    • Binds to and inactivates RANKL → RANK → NF-kB pathway inhibits gene exp req for osteoClast fcn
  • Use: Osteoporosis
  • S/E: Hypocalcemia may be worsened
142
Q

Leflunomide

A
  • Reversibly inhibits dihydroorotate dehydrogenase → prevents pyrimidine synth
  • Suppresses T-cell prolif
  • Use:
    • Rheumatoid arthritis
    • Psoriatic arthritis
  • S/E:
    • Diarrhea
    • HTN
    • hepatotoxicity
    • teratogenicity
143
Q

Acute Gout Rx

A
  • Pain is the major concern → use NSAIDs (indomethacin, naproxen, sulindac) and Colchicine
  • Avoid:
    • Allopurinol, febuxostat (can cause flares)
    • Aspirin / salicylates (dec urate excretion)
    • Diuretics (vol depletion increases urate levels in blood)
144
Q

Chronic Gout Rx

A

Target: get blood uric acid below 4-5 mg/dl

  • Probenecid / rasburicase (in underexcretors)
  • Febuxostat (in overproducers)
  • Lesinurad (SURI)
145
Q

Colchicine

A
  • Gouty inflammation suppressant
    • Binds / stabilizes tubulin → inhibits microtubule polymerization in neutrophils → impairs neutrophil chemotaxis / degranulation
  • Use: Gout, acute and prophylaxis
  • S/E:
    • Diarrhea / GI upset
    • Alopecia
    • Hematuria
    • BM suppression
    • Peripheral neuropathy
146
Q

Probenecid

A
  • Inhibits PCT uric acid reabsorption
  • Use: Chronic Gout
  • S/E:
    • Can precipitate uric acid calculi
    • Prolonged duration of action of penicillins, cephalosporins
147
Q

Allopurinol

A
  • Competitive xanthine oxidase inhibitor
    • Decreases conversion of hypoxanthine and xanthine → urate
  • Use:
    • Chronic Gout
    • Lymphoma / leukemia (prevent tumor lysis-assoc urate nephropathy)
    • Increases conc of azathioprine and 6-MP (metabolized by xanthine oxidase)
  • S/E: SJS
148
Q

Febuxostat

A
  • Xanthine oxidase inhibitor
    • Decreases conversion of hypoxanthine and xanthine → urate
  • Use:
    • Chronic Gout
    • Increases conc of azathioprine and 6-MP (metabolized by xanthine oxidase)
  • S/E: SJS
149
Q

Pegloticase

A
  • Recombinant uricase
    • Catalyzes metab of uric acid → allantoin (a more water-soluble product)
  • Use: Chronic Gout
150
Q

Glucocorticoids

A
  • Oral, intra-articular, or parenteral.
  • Use: Acute Gout
  • See endocrine cards
151
Q

TNF-α Inhibitor S/E

A

All TNF-α inhibitors predispose to infection, including reactivation of latent TB, since TNF is important in granuloma formation and stabilization.

152
Q

Etanercept

A
  • TNF-α Inhibitor
    • Fusion protein (TNF-α + IgG1 Fc) → decoy receptor
  • Use:
    • Rheumatoid arthritis
    • psoriasis
    • ankylosing spondylitis
  • S/E: Infxn
153
Q

Infliximab

A
  • TNF-α Inhibitor
    • Anti-TNF-α monoclonal antibody
  • Use:
    • Inflammatory bowel disease
    • rheumatoid arthritis
    • ankylosing spondylitis
    • psoriasis
  • S/E: Infxn
154
Q

Adalimumab

A
  • TNF-α Inhibitor
    • Anti-TNF-α monoclonal antibody
  • Use:
    • Inflammatory bowel disease
    • rheumatoid arthritis
    • ankylosing spondylitis
    • psoriasis
  • S/E: Infxn
155
Q

Rasburicase

A
  • Recombinant uricase
    • catalyzes metab of uric acid → allantoin (a more water-soluble product)
  • Use: Prevention and treatment of tumor lysis syndrome
156
Q

Purine Metabolism

157
Q

Liothyronine

A
  • Synthetic T3
  • Use:
    • HypOthyroidism
    • Myxedema
    • Weight loss (off-label)
  • S/E:
    • Tachycardia
    • heat intolerance
    • tremors
    • arrhythmias
158
Q

Beclomethasone

A
  • 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
159
Q

dexamethasone

A
  • 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
160
Q

hydrocortisone

A
  • 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
161
Q

methylprednisolone

A
  • 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
162
Q

Prednisone

A
  • 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
163
Q

triamcinolone

A
  • 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
164
Q

1st gen sulfonylureas

A

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

  • Chlorpropamide
  • Tolbutamide

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

165
Q

2nd gen sulfonylureas

A

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

  • Glimepiride
  • Glyburide
  • Glipizide

Note: Hypoglycemia

166
Q

Biguanides

A

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

  • Metformin

Note: lactic acidosis; C/I in renal insufficiency

167
Q

Glitazones / TZDs

A

Bind to PPAR-γ → increase periph tissue insulin sensitivity

  • Pioglitazone
  • Rosiglitazone

Note: weight gain; edema

168
Q

Rapid-Acting Insulin

A

Bind insulin receptor → tyrosine kinase activity

  • Lispro
  • Aspart
  • Glulisine

Note: use w/meals

169
Q

Short-Acting Insulin

A

Bind insulin receptor → tyrosine kinase activity

  • Regular insulin

Note: use for DKA

170
Q

Intermediate-Acting Insulin

A

Bind insulin receptor → tyrosine kinase activity

  • NPH
171
Q

Long-Acting Insulin

A

Bind insulin receptor → tyrosine kinase activity

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

Note: use for basal control

172
Q

Meglitinides

A

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

  • Nateglinide
  • Repaglinide

Note: hypoglycemia; weight gain

173
Q

GLP-1 Agonists

A

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

  • Exenatide
  • Liraglutide

Note: weight loss

174
Q

GLP-1

A
  • 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
175
Q

DPP-4 Inhibitors

A

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

  • Linagliptin
  • Saxagliptin
  • Sitagliptin

Note: weight-neutral

176
Q

Amylin Analogs

A

Decrease glucagon + gastric empyting

  • Pramlintide

Note: hypoglycemia

177
Q

Amylin

A
  • peptide hormone that is cosecreted with insulin from pancreatic beta-cell
  • inhibits glucagon secretion, delays gastric emptying, and acts as a satiety agent
178
Q

SGLT-2 inhibitors

A

Block glucose reabsorption in PCT

  • Canagliflozin
  • Dapagliflozin
  • Empagliflozin

Note: UTIs; C/I in renal insufficiency

179
Q

SGLT-2

A

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

180
Q

α-Glucosidase Inhibitors

A

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

  • Acarbose
  • Miglitol
181
Q

Thioamides

A

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

182
Q

Synthetic Thyroid Hormones

A

Act at thyroid hormone nuclear receptors

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

Note: tachycardia; heat intolerance

183
Q

ADH Antagonists

A

Block action of ADH at collecting duct V2-receptor

  • Conivaptan
  • Tolvaptan
  • Demeclocycline

Note: demeclocycline → tetracycline S/E

184
Q

1st gen sulfonylureas

A

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

  • Chlorpropamide
  • Tolbutamide

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

185
Q

1st gen sulfonylureas

A

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

  • Chlorpropamide
  • Tolbutamide

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

186
Q

Intermediate-Acting Insulin

A

Bind insulin receptor → tyrosine kinase activity

  • NPH
187
Q

α-Glucosidase Inhibitors

A

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

  • Acarbose
  • Miglitol
188
Q

ADH Antagonists

A

Block action of ADH at collecting duct V2-receptor

  • Conivaptan
  • Tolvaptan
  • Demeclocycline

Note: demeclocycline → tetracycline S/E

189
Q

Synthetic Thyroid Hormones

A

Act at thyroid hormone nuclear receptors

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

Note: tachycardia; heat intolerance

190
Q

Thioamides

A

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

191
Q

SGLT-2

A

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

192
Q

SGLT-2 inhibitors

A

Block glucose reabsorption in PCT

  • Canagliflozin
  • Dapagliflozin
  • Empagliflozin

Note: UTIs; C/I in renal insufficiency

193
Q

Amylin

A
  • peptide hormone that is cosecreted with insulin from pancreatic beta-cell
  • inhibits glucagon secretion, delays gastric emptying, and acts as a satiety agent
194
Q

Amylin Analogs

A

Decrease glucagon + gastric empyting

  • Pramlintide

Note: hypoglycemia

195
Q

DPP-4 Inhibitors

A

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

  • Linagliptin
  • Saxagliptin
  • Sitagliptin

Note: weight-neutral

196
Q

GLP-1

A
  • 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
197
Q

GLP-1 Agonists

A

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

  • Exenatide
  • Liraglutide

Note: weight loss

198
Q

Meglitinides

A

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

  • Nateglinide
  • Repaglinide

Note: hypoglycemia; weight gain

199
Q

Long-Acting Insulin

A

Bind insulin receptor → tyrosine kinase activity

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

Note: use for basal control

200
Q

Short-Acting Insulin

A

Bind insulin receptor → tyrosine kinase activity

  • Regular insulin

Note: use for DKA

201
Q

Rapid-Acting Insulin

A

Bind insulin receptor → tyrosine kinase activity

  • Lispro
  • Aspart
  • Glulisine

Note: use w/meals

202
Q

Glitazones

A

Bind to PPAR-γ → increase periph tissue insulin sensitivity

  • Pioglitazone
  • Rosiglitazone

Note: weight gain; edema

203
Q

Biguanides

A

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

  • Metformin

Note: lactic acidosis; C/I in renal insufficiency

204
Q

2nd gen sulfonylureas

A

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

  • Glimepiride
  • Glyburide
  • Glipizide

Note: Hypoglycemia

205
Q

Rapid-Acting Insulin

A

Bind insulin receptor → tyrosine kinase activity

  • Lispro
  • Aspart
  • Glulisine

Note: use w/meals

206
Q

Glitazones

A

Bind to PPAR-γ → increase periph tissue insulin sensitivity

  • Pioglitazone
  • Rosiglitazone

Note: weight gain; edema

207
Q

Biguanides

A

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

  • Metformin

Note: lactic acidosis; C/I in renal insufficiency

208
Q

2nd gen sulfonylureas

A

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

  • Glimepiride
  • Glyburide
  • Glipizide

Note: Hypoglycemia

209
Q

1st gen sulfonylureas

A

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

  • Chlorpropamide
  • Tolbutamide

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

210
Q

NSAIDs

A

Reversibly inhibit COX → block PG synth

  • Ibuprofen
  • Naproxen
  • Indomethacin
  • Ketorolac
  • Sulindac
  • Diclofenac
  • Meloxicam
  • Piroxicam

Note: gastric ulceration; renal ischemia; interstitial nephritis

211
Q

TNF-α Inhibitors

A

Anti-TNF-α monoclonal Ab

  • Adalimumab
  • Certolizumab
  • Infliximab

Note: Etanercept is a decoy receptor, NOT a mab

212
Q

Bisphosphonates

A

Pyrophosphate analogs → bind hydroxyapatite in bone → inhibit osteoClast activity

Also promote osteoClast apoptosis and decrease development/recruitment of osteoClast precursors

  • Alendronate
  • Ibandronate
  • Risedronate
  • Zoledronate

Note: esophageal erosion; jaw osteonecrosis

213
Q

Xanthine Oxidase Inhibitors

A

Decrease conversion of hypoxanthine / xanthine → urate

  • Allopurinol
  • Febuxostat

Note: increase conc of Azathioprine and 6-MP; do NOT use for acute gout

214
Q

Recombinant Uricases

A

Catalyze metab of uric acid → allantoin (a more water-soluble product)

  • Pegloticase
215
Q

Meds that can cause Osteoporotic Fractures

A
  • CYP450-inducing anticonvulsants
  • Aromatase inhibitors
  • Medroxyprogesterone
  • GnRH Agonists
  • Proton Pump Inhibitors
  • Glucocorticoids
  • Unfractionated Heparin
  • Thiazolidinediones
216
Q

Low Ca2+ / Low PTH

A

1° HypOparathyroidism

217
Q

Low Ca2+ / High PTH

A

2° hypERparathyroidism

218
Q

High Ca2+ / Low PTH

A

PTH-Independent HypERcalcemia

219
Q

High Ca2+ / High PTH

A

1° HypERparathyroidism

220
Q

Significantly decrease LDL, slightly decrease TG, increase HDL

221
Q

Significantly decrease LDL, slightly increase HDL & TG

A

Bile Acid Resins

222
Q

Significantly decrease LDL

223
Q

Significantly decrease TG, slightly decrease LDL, increase HDL

224
Q

Significantly decreases LDL, significantly increases HDL, slightly decreases TG

225
Q

HMG-CoA Reductase Inhibitors

A

Inhibit conversion of HMG-CoA → mevalonate

Up-regulate LDL receptors

  • Lovastatin
  • Atorvastatin
  • Simvastatin
  • Pravastatin

Note: myopathy; C/I in pregnancy

226
Q

Bile Acid Resins

A

Anion exchg in bowel removes bile acids from circ → liver uses cholesterol to make more bile acids + up-regulates LDL receptors

  • Cholestyramine
  • Colestipol
  • Colesevalam

Note: malabsorption

227
Q

Cholesterol Absorption Inhibitors

A

Inhibit NPC1L1 transporter protein → prevent cholesterol absorption at small intestine brush border

  • Ezetimibe

Note: diarrhea

228
Q

Fibrates

A

Upregulate LPL → increase TG clearance

Activate PPAR-α → induce HDL synth

  • Gemfibrozil
  • Bezafibrate
  • Fenofibrate

Note: Cholesterol gallstones

229
Q

HSL Inhibitors

A

Inhibit lipolysis (hormone-sensitive lipase) in adipose → reduce hepatic VLDL synth

  • Niacin

Note: Flushing; HypERglycemia; HypERuricemia

230
Q

PTH Analog

A

Short-term: stim osteoBlasts > osteoclasts

Long-term: stim osteoClasts

  • Teriparatide

Note: osteosarcoma; transient hypERcalcemia

231
Q

TNF-α Decoy Receptor

A

Fusion protein (TNF-α + IgG1 Fc)

  • Etanercept

Note: Infxn

232
Q

COX-2 Inhibitors

A

Reversibly inhibit COX-2 in inflamm cells and vascular endothelium (mediates inflamm/pain) → no GI corrosion, no antiplatelet agg fx

  • Celecoxib

Note: Thrombosis; C/I in sulfa allergy

233
Q

Etanercept

A
  • TNF-α Inhibitor
    • Fusion protein (TNF-α + IgG1 Fc) → decoy receptor
  • Use:
    • Rheumatoid arthritis
    • psoriasis
    • ankylosing spondylitis
  • S/E: Infxn
234
Q

Calcineurin Inhibitors

A

Prevent IL-2 transcription → block T-cell activation

  • Cyclosporine → cyclophilin
  • Tacrolimus → FK506

Note: gingival hyperplasia + hirsutism w/cyclosporine but NOT tacrolimus

235
Q

mTOR Inhibitors

A

Bind FKBP → inhibit mTOR

  • Sirolimus / Rapamycin

Note: Pancytopenia; NOT nephrotoxic; synergistic w/cyclosporine

236
Q

mTOR

A
  • serine/threonine protein kinase
  • regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, autophagy, transcription
  • PI3 family
  • Inhibited by sirolimus/rapamycin
237
Q

IL-2R Inhibitors

A
  • Daclizumab
  • Basiliximab

Note: use for kidney transplant rejection prophylaxis

238
Q

6-MP Precursor

A

Antimetabolite precursor → blocks nucleotide synth → inhibits lymphocyte prolif

Activated by HGPRT; Degraded by xanthine oxidase

  • Azathioprine

Note: leukopenia; thrombocytopenia; conc increased by xanthine oxidase inhibitors

239
Q

IMP Dehydrogenase Inhibitors

A

Reversibly inhibit IMP dehydrogenase → prevent purine synthesis → inhibit B and T cell responses

  • Mycophenolate Mofetil

Note: pancytopenia; invasive CMV

240
Q

IL-2 Recombinant Cytokine

A

Aldesleukin

Use: Renal cell carcinoma; metastatic melanoma

241
Q

EPO Recombinant Cytokine

A

Epoetin Alfa

Use: Anemias (especially in renal failure)

242
Q

G-CSF Recombinant Cytokine

A

Filgrastim

Use: Recovery of bone marrow

243
Q

GM-CSF Recombinant Cytokine

A

Sargramostim

Use: Recovery of bone marrow

244
Q

IFN-α Recombinant Cytokine

A

IFN-α

Use: Chronic Hep B / C; Kaposi sarcoma; malignant melanoma

245
Q

IFN-β Recombinant Cytokine

A

IFN-β

Use: Multiple sclerosis

246
Q

IFN-γ Recombinant Cytokine

A

IFN-γ

Use: Chronic granulomatous disease

247
Q

Thrombopoietin Receptor Agonists

A
  • Romiplostim
  • Eltrombopag

Use: Thrombocytopenia

248
Q

IL-11 Recombinant Cytokine

A

Oprelvekin

Use: Thrombocytopenia

249
Q

CD52 Blocker

A

Alemtuzumab

Use: CLL; MS

250
Q

VEGF Blocker

A
  • Bevacizumab
    • Use: Colorectal cancer; renal cell carcinoma
  • Ranibizumab
    • Use: Neovascular age-related macular degeneration
251
Q

EGFR Blocker

A

Cetuximab

Use: Stage IV colorectal cancer; head and neck cancer

252
Q

CD20 Blocker

A

Rituximab

Use: B-cell non-Hodgkin lymphoma; CLL; rheumatoid arthritis; ITP

253
Q

HER2/neu Blocker

A

Trastuzumab

Use: Breast cancer

254
Q

C5 Blocker

A

Eculizumab

Use: Paroxysmal nocturnal hemoglobinuria

255
Q

α4-Integrin Blocker

A

Natalizumab

Use: Multiple sclerosis; Crohn disease

256
Q

Platelet GPIIb/IIIa Blocker

A

Abciximab

Use: Antiplatelet agent for prevention of ischemic complications in patients undergoing percutaneous coronary intervention

257
Q

RANKL Blocker

A

Denosumab

Use: Osteoporosis

258
Q

Digoxin Blocker

A

Digoxin immune Fab

Use: Antidote for digoxin toxicity

259
Q

IgE Blocker

A

prevents IgE binding to FcεRI

Omalizumab

Use: Allergic asthma

260
Q

RSV F Protein Blocker

A

Palivizumab

Use: RSV prophylaxis for high-risk infants

261
Q

Dihydrofolate Reductase Inhibitors

A

Decrease dTMP → decrease pyrimidine & DNA synthesis

  • Methotrexate
  • Trimethoprim (bacteria)
  • Pyrimethamine (protozoa)

Note: mucosal ulcers; reversible BM suppression (leucovorin)

262
Q

Dihydroorotate Dehydrogenase Inhibitors

A

Prevent pyrimidine synth

  • Leflunomide

Note: hepatotoxicity; teratogenicity

263
Q

Alkylating Agents

A

Cross-link DNA at guanine N-7

  • Cyclophosphamide

Note: Myelosuppression; reversible hemorrhagic cystitis (mesna)

264
Q

IL-1 receptor antagonist

A

Anakinra

Use: rheumatoid arthritis

265
Q

IL-6 receptor antagonist

A

Tocilizumab

Use: Giant cell arteritis; Rheumatoid arthritis

266
Q

Anti-CD3 Ab

A

Muromonab / OKT3

267
Q

Immune Boosters

A
  • Levamisole
  • Thalidomide
  • Bacillus Calmette-Guerin (BCG)

M2 - Pharm (10 decks)

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