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Pharmacology I > Final Exam > Flashcards

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
Q

Calcitonin

A
  • 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
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26
Q

Ergonovine

A
  • Ergot alkaloid
  • Tx of postpartum bleeding
  • MOA: 5-HT agonist > alpha agonist
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27
Q

Ergotamine

A
  • Ergot alkaloid
  • Tx of migraine HA (given just prior to onset)
  • MOA: 5-HT agonist, alpha agonist
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28
Q

Bromocriptine

A
  • Ergot alkaloid
  • Tx of parkinson’s, reduce prolactin secretion
  • MOA: DA agonist
29
Q

Methysergide

A
  • Ergot alkaloid
  • Used for migraine prophylaxis
  • MOA: 5-HT antagonist
30
Q

Pergolide

A
  • Ergot alkaloid
  • Tx of parkinson’s, reduce prolactin secretion
  • MOA: DA agonist
31
Q

Dimenhydrinate (Dramamine)

A
  • 1st generation H1 antagonist

- Tx motion sickness

32
Q

Diphenhydramine (Benadryl)

A
  • 1st generation H1 antagonist
  • Tx allergic rhinitis, hyper-sensitivity reactions, pruritis
  • nonselective H1 & H2 antagonist
  • produces sedation in most adults
33
Q

Cetirizine (Zyrtec)

A
  • 2nd generation H1 antagonist
  • Tx allergic rhinitis, urticaria
  • less BBB penetration, longer DOA
34
Q

Fexofenadine (Allegra)

A
  • 2nd generation H1 antagonist
  • Tx allergic rhinitis, urticaria
  • less BBB penetration, longer DOA
35
Q

Azelastine (Asteline)

A
  • 2nd generation H1 antagonist
  • Tx allergic rhinitis, urticaria
  • less BBB penetration, longer DOA
36
Q

Loratadine (Claritin)

A
  • 2nd generation H1 antagonist
  • Tx allergic rhinitis, urticaria
  • less BBB penetration, longer DOA
37
Q

Cimetidine (Tagamet)

A
  • H2 antagonist
  • Tx of duodenal and gastric ulcers, GERD, heartburn, indigestion
  • inhibits gastric acid secretion
38
Q

Ranitidine (Zantac)

A
  • H2 antagonist
  • Tx of duodenal and gastric ulcers, GERD, heartburn, indigestion
  • inhibits gastric acid secretion
39
Q

Famotidine (Pepcid)

A
  • H2 antagonist
  • Tx of duodenal and gastric ulcers, GERD, heartburn, indigestion
  • inhibits gastric acid secretion
40
Q

Buspirone

A
  • 5-HT1A agonist

- anxiolytic

41
Q

Dexfenfluramine

A
  • 5-HT1A agonist

- appetite suppressant

42
Q

Ketanserin

A
  • 5-HT2 antagonist
  • Tx of carcinoid tumor
  • controls symptoms until tumor is surgically removed
43
Q

Cyproheptadine

A
  • 5-HT2 antagonist
  • Tx of carcinoid tumor
  • controls symptoms until tumor is surgically removed
  • also has some histamine blocking activity
44
Q

Phenoxybenzamine

A
  • 5-HT2 antagonist
  • Tx of carcinoid tumor
  • controls symptoms until tumor is surgically removed
  • also has alpha 1 & 2 blocking activity
45
Q

Ondansetron

A
  • 5-HT3 antagonist
  • antinausea and antiemetic
  • 5-HT3 receptor is the only ion channel in this class
46
Q

PGD2

A

-Prostanoid (products of oxygenation of AA by COX-1 & 2
Action @:
Airway SM - bronchoconstriction
-platelet antagonists (prevents aggregation)

47
Q

LTC4 and LTD4

A

-Leukotrienes
Action @:
Airway SM - bronchoconstriction

48
Q

PGI2

A 
-Prostanoid (prostacyclin)
Action @:
Airway SM - bronchdilation
Vascular SM - vasoconstriction
-used for pulmonary HT (not asthma)
49
Q

PGE2

A

-Prostanoid
Action @:
Vascular SM - vasoconstriction
Reproductive - ovulation, uterine contractions
Eye - lowers intraocular pressure
-platelet antagonists (prevents aggregation)

50
Q

PGF2alpha

A
  • Prostanoid
  • uterine contraction, labor inducer or abortion (dep. on when given during pregnancy)
  • lower intraocular pressure
  • contraindicated for asthmatics
51
Q

PGE1

A
  • Prostanoid
  • penile erection
  • lower intraocular pressure
52
Q

TXA

A

-promotes platelet aggregation

53
Q

Corticosteroids

A
  • block all known eicosanoid synthesis pathways

- very potent anti-inflammatory action

54
Q

Indomethacin

A
  • NSAID
  • reversibly and non-selectively inhibit COX activity (blocks prostaglandin and thromboxane formation which you need for platelet aggregation)
55
Q

Ibuprofen

A
  • NSAID
  • reversibly and non-selectively inhibit COX activity (blocks prostaglandin and thromboxane formation which you need for platelet aggregation)
56
Q

Zileuton

A
  • 5-lipoxygenase (LOX) inhibitor - inhibits synthesis of leukotrienes
  • Tx mild to moderate asthma
57
Q

Alprostadil

A
  • 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
Q

Misoprostol

A

-Eicosanoid (PGE1 analogue)
-used for termination of early pregnancies by causing dramatic contractions to expel fetus
AE: cramping, diarrhea

59
Q

Dinoprostone

A
  • Eicosanoid (PGE2)

- induction of labor (topical application)

60
Q

Carboprost tromethamine

A
  • Eicosanoid (PGF2alpha analogue)
  • 2nd trimester abortion
  • controls postpartum hemorrhage
  • AE: vomiting and diarrhea
61
Q

Epoprostenol

A
  • Eicosanoid (PGI2 analogue)

- Tx of primary pulmonary HT via inhaler/nebulizer

62
Q

Iloprost

A
  • Eicosanoid (PGI2 analogue)

- Tx of primary pulmonary HT via inhaler/nebulizer

63
Q

Treprostinil

A
  • Eicosanoid (PGI2 analogue)

- Tx of primary pulmonary HT via inhaler/nebulizer

64
Q

Denosumab

A

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
Q

Strontium Ranelate

A

blocks osteoclast differentiation and stimulates apoptosis in pre-osteoclast, which has an anti-resorption effect
-not available in the US

66
Q

Latanoprost

A

PGF2 alpha analogue
-ophthalmic solution for controlling progression of glaucoma by reducing intraocular pressure by increasing outflow of aqueous humor from eye

67
Q

Sumatriptan

A

5-HT agonist used for Tx of migraines

68
Q

Tegaserod

A

Used for management of IBS and constipation

-taken off the market in 2007

Pharmacology I (10 decks)

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