Final Exam Flashcards

1
Q

MOA of ACE inhibitors

A

Blocks ACE which directly prevents:

  1. conversion of AT`1 to AT2
  2. breakdown of bradykinin

Pts with HT have more renin and AT in blood so ACE inhibitors work really well in these pts

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2
Q

Angiotensin II receptor:

  • G-protein coupled receptor located on plasma membrane
  • Mediates major biological function of AT2
  • Located in vascular smooth muscle of vessels, brain, and adrenal gland
A

Antiotensin II type 1 receptor

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3
Q

Angiotensin II receptor:

  • mainly present in fetus
  • less abundant in adults
  • functions are poorly understood
A

Angiotensin II type 2 receptor

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4
Q

Renin-Angiotensin Cycle

Describe the resulting effects after kidneys respond to decreased BP and renal blood flow…

A

Kidney’s sense decreased renal blood flow, decreased BP, or triggered by Beta -1 activation and kidneys release renin. Renin converts angiotensinogen to angiotensin I and ACE converts angiotensin I –> angiotensin II which results in:

Blood vessels - increase smooth muscle contraction & PR

Adrenal Gland (medulla) - increase release of NE & Epi (mostly Epi) which causes same effects as in blood vessels above AND increase HR, contractility, & CO

Adrenal Gland (cortex) - increases aldosterone release –> increases Na+ & H2O reabsorption (increases K+ secretion)

Post Pituitary Gland - increase vasopressin release –> increases water reabsorption

Hypothalamus - increases thirst

ALL THESE EFFECTS LEAD TO INCREASED BLOOD VOLUME AND BLOOD PRESSURE

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5
Q

ACE inhibitor AE

A
  1. dry cough
  2. angioedema
  3. rash
  4. hyperkalemia-from reduction in aldosterone (b/c aldosterone responsible for increasing secretion of K+)
  5. inflammation
  6. fetotoxicity-crosses placenta, don’t give during pregnancy
  7. taste dysfunction
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6
Q

Captopril

A
  • ACE inhibitor

- Tx of HT (not 1st option), HF (1st line drug), MI

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7
Q

Lisinopril

A
  • ACE inhibitor

- Tx of HT (not 1st option), HF (1st line drug), MI

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8
Q

Fosinopril, Enalapril, Moexipril

A
  • ACE inhibitor
  • Tx of HT (not 1st option), HF (1st line drug), MI
  • Prodrug
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9
Q

Losartan

A
  • Angiotensin II Receptor Blocker
  • Tx of HT
  • Prototype one of the 1st marketed AII antagonists
  • orally active
  • less dry cough SE b/c bradykinin and PGE2 levels not affected
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10
Q

Valsartan

A
  • Angiotensin II Receptor Blocker
  • Tx of HT
  • one of the 1st marketed AII antagonists
  • orally active
  • less dry cough SE b/c bradykinin and PGE2 levels not affected
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11
Q

Telmisartan, Irbesartan, Candesartan, Eprosartan

A
  • Angiotensin II Receptor Blocker
  • Tx of HT
  • less dry cough SE b/c bradykinin and PGE2 levels not affected
  • newer and longer DOA than Losartan & Valsartan
  • better PK profile
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12
Q

Aliskiren

A
  • Renin inhibitor
  • Tx of essential HT
  • -Effective in lowering BP (esp in combo with hydrochlorothiazide)
  • no effect on bradykinin metabolism
  • no evidence of bradykinin-mediated SE (dry cough, angioedema, rash, etc.)
  • orally active
  • long DOA
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13
Q

Fibroblast Growth Factor 23 (FGF-23)

A

-protein produced by osteoblasts and osteoclasts

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14
Q

Vitamin D

A

-steroid produced in the skin from UV radiation; found in food & supplements

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15
Q

Etidronate

A
  • older Bisphosphonate
  • Tx of Osteoporosis
  • inhibits osteoclast activity
  • has affinity for areas of active remodeling
  • Bisphosphonates are the most appropriate INITIAL TX for women with osteoporosis
  • less GI problems than other bisphosphonates
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16
Q

Pamidronate

A
  • older Bisphosphonate
  • Tx of Osteoporosis
  • inhibits osteoclast activity
  • has affinity for areas of active remodeling
  • Bisphosphonates are the most appropriate INITIAL TX for women with osteoporosis
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17
Q

Alendronate (Fosamax)

A
  • older Bisphosphonate
  • Tx of Osteoporosis
  • inhibits osteoclast activity
  • has affinity for areas of active remodeling
  • Bisphosphonates are the most appropriate INITIAL TX for women with osteoporosis
  • contraindicated in pts with active upper GI disease; risk of esophageal irritation
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18
Q

Risedronate

A
  • newer Bisphosphonate
  • Tx of Osteoporosis
  • inhibits osteoclast activity
  • has affinity for areas of active remodeling
  • Bisphosphonates are the most appropriate INITIAL TX for women with osteoporosis
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19
Q

Tiludronate

A
  • newer Bisphosphonate
  • Tx of Osteoporosis
  • inhibits osteoclast activity
  • has affinity for areas of active remodeling
  • Bisphosphonates are the most appropriate INITIAL TX for women with osteoporosis
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20
Q

Ibandronate (Boniva)

A
  • newer Bisphosphonate
  • Injection (~3x/yr); potent
  • Tx of Osteoporosis
  • inhibits osteoclast activity
  • has affinity for areas of active remodeling
  • Bisphosphonates are the most appropriate INITIAL TX for women with osteoporosis
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21
Q

Zoledronate

A
  • newer Bisphosphonate
  • Injection (once per year)
  • Tx of Osteoporosis
  • inhibits osteoclast activity
  • has affinity for areas of active remodeling
  • Bisphosphonates are the most appropriate INITIAL TX for women with osteoporosis
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22
Q

Raloxifene

A
  • Selective estrogen receptor modulators (SERMS)
  • approved for prevention & Tx of osteoporosis
  • protects against spine, but not hip fractures
  • reduces breast cancer risk
  • more activity in bone than breast tissue
  • best choice for pts susceptible to vertebral fractures
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23
Q

Estrogen/Progestin therapy

A
  • No longer 1st line Tx for osteoporosis
  • only moderately effective in Tx osteoporosis (used more for pre/postmenopausal women)
  • still option for pts contraindicated from or intolerant to bisphosphonates or raloxifene
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24
Q

PTH (Teriparatide)

A
  • represents a portion of PTH
  • stimulates new bone formation and reduces risk of fractures
  • requires expensive, daily SQ Inj
  • stops working as soon as you stop taking it
  • Increase effectiveness of PTH by taking Thiazide diuretic/restricting Na+ intake which can reduce renal Ca+2 excretion
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25
Calcitonin
- lowers plasma Ca+2 (by using available Ca+2 in blood to form more bone) - inhibits osteoclast bone reabsorption (breakdown of bone) - unique role in acute Tx of osteoporotic fracture - may speed up healing; analgesic
26
Ergonovine
- Ergot alkaloid - Tx of postpartum bleeding - MOA: 5-HT agonist > alpha agonist
27
Ergotamine
- Ergot alkaloid - Tx of migraine HA (given just prior to onset) - MOA: 5-HT agonist, alpha agonist
28
Bromocriptine
- Ergot alkaloid - Tx of parkinson's, reduce prolactin secretion - MOA: DA agonist
29
Methysergide
- Ergot alkaloid - Used for migraine prophylaxis - MOA: 5-HT antagonist
30
Pergolide
- Ergot alkaloid - Tx of parkinson's, reduce prolactin secretion - MOA: DA agonist
31
Dimenhydrinate (Dramamine)
- 1st generation H1 antagonist | - Tx motion sickness
32
Diphenhydramine (Benadryl)
- 1st generation H1 antagonist - Tx allergic rhinitis, hyper-sensitivity reactions, pruritis - nonselective H1 & H2 antagonist - produces sedation in most adults
33
Cetirizine (Zyrtec)
- 2nd generation H1 antagonist - Tx allergic rhinitis, urticaria - less BBB penetration, longer DOA
34
Fexofenadine (Allegra)
- 2nd generation H1 antagonist - Tx allergic rhinitis, urticaria - less BBB penetration, longer DOA
35
Azelastine (Asteline)
- 2nd generation H1 antagonist - Tx allergic rhinitis, urticaria - less BBB penetration, longer DOA
36
Loratadine (Claritin)
- 2nd generation H1 antagonist - Tx allergic rhinitis, urticaria - less BBB penetration, longer DOA
37
Cimetidine (Tagamet)
- H2 antagonist - Tx of duodenal and gastric ulcers, GERD, heartburn, indigestion - inhibits gastric acid secretion
38
Ranitidine (Zantac)
- H2 antagonist - Tx of duodenal and gastric ulcers, GERD, heartburn, indigestion - inhibits gastric acid secretion
39
Famotidine (Pepcid)
- H2 antagonist - Tx of duodenal and gastric ulcers, GERD, heartburn, indigestion - inhibits gastric acid secretion
40
Buspirone
- 5-HT1A agonist | - anxiolytic
41
Dexfenfluramine
- 5-HT1A agonist | - appetite suppressant
42
Ketanserin
- 5-HT2 antagonist - Tx of carcinoid tumor - controls symptoms until tumor is surgically removed
43
Cyproheptadine
- 5-HT2 antagonist - Tx of carcinoid tumor - controls symptoms until tumor is surgically removed - also has some histamine blocking activity
44
Phenoxybenzamine
- 5-HT2 antagonist - Tx of carcinoid tumor - controls symptoms until tumor is surgically removed - also has alpha 1 & 2 blocking activity
45
Ondansetron
- 5-HT3 antagonist - antinausea and antiemetic - 5-HT3 receptor is the only ion channel in this class
46
PGD2
-Prostanoid (products of oxygenation of AA by COX-1 & 2 Action @: Airway SM - bronchoconstriction -platelet antagonists (prevents aggregation)
47
LTC4 and LTD4
-Leukotrienes Action @: Airway SM - bronchoconstriction
48
PGI2
``` -Prostanoid (prostacyclin) Action @: Airway SM - bronchdilation Vascular SM - vasoconstriction -used for pulmonary HT (not asthma) ```
49
PGE2
-Prostanoid Action @: Vascular SM - vasoconstriction Reproductive - ovulation, uterine contractions Eye - lowers intraocular pressure -platelet antagonists (prevents aggregation)
50
PGF2alpha
- Prostanoid - uterine contraction, labor inducer or abortion (dep. on when given during pregnancy) - lower intraocular pressure - contraindicated for asthmatics
51
PGE1
- Prostanoid - penile erection - lower intraocular pressure
52
TXA
-promotes platelet aggregation
53
Corticosteroids
- block all known eicosanoid synthesis pathways | - very potent anti-inflammatory action
54
Indomethacin
- NSAID - reversibly and non-selectively inhibit COX activity (blocks prostaglandin and thromboxane formation which you need for platelet aggregation)
55
Ibuprofen
- NSAID - reversibly and non-selectively inhibit COX activity (blocks prostaglandin and thromboxane formation which you need for platelet aggregation)
56
Zileuton
- 5-lipoxygenase (LOX) inhibitor - inhibits synthesis of leukotrienes - Tx mild to moderate asthma
57
Alprostadil
- Eicosanoid (PGE1) - Tx of erectile dysfunction by producing vasodilation in penis via insert or ink (not orally active) - AE: algesia (pain near inj), priapism (long lasting erections)
58
Misoprostol
-Eicosanoid (PGE1 analogue) -used for termination of early pregnancies by causing dramatic contractions to expel fetus AE: cramping, diarrhea
59
Dinoprostone
- Eicosanoid (PGE2) | - induction of labor (topical application)
60
Carboprost tromethamine
- Eicosanoid (PGF2alpha analogue) - 2nd trimester abortion - controls postpartum hemorrhage - AE: vomiting and diarrhea
61
Epoprostenol
- Eicosanoid (PGI2 analogue) | - Tx of primary pulmonary HT via inhaler/nebulizer
62
Iloprost
- Eicosanoid (PGI2 analogue) | - Tx of primary pulmonary HT via inhaler/nebulizer
63
Treprostinil
- Eicosanoid (PGI2 analogue) | - Tx of primary pulmonary HT via inhaler/nebulizer
64
Denosumab
monoclonal antibody for Tx of osteoporosis | -binds to and inhibits RANKL, a protein that normally acts as the primary signal for breakdown of bone
65
Strontium Ranelate
blocks osteoclast differentiation and stimulates apoptosis in pre-osteoclast, which has an anti-resorption effect -not available in the US
66
Latanoprost
PGF2 alpha analogue -ophthalmic solution for controlling progression of glaucoma by reducing intraocular pressure by increasing outflow of aqueous humor from eye
67
Sumatriptan
5-HT agonist used for Tx of migraines
68
Tegaserod
Used for management of IBS and constipation | -taken off the market in 2007