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Old Gastrointestinal Cards > GI Pharmacology-A > Flashcards

GI Pharmacology-A Flashcards

1
Q

Glyburide: Drug Class

A

Sulfonylurea

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2
Q

Sulfonylureas: Mechanism of action

A

They bind to specific receptors on the insulin producing pancreatic beta cells and close a certain K+ channel. This causes depolarization and triggers an increase of intracellular calcium which, in turn, augments the release of granules of insulin

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3
Q

Name the three Sulfonylureas

A

Glipizide, Glyburide, and Glimepiride

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4
Q

Glipizide: Drug Class

A

Sulfonylurea

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5
Q

Sulfonylureas: Side Effects

A

Dominant adverse effect is hypoglycemia (risk factors are age, poor nutrition, and renal failure). It also causes weight gain and elevation of triglycerides & LDL cholesterol (further aggravating coronary risk factors of DM II)

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6
Q

Glimepiride: Drug Class

A

Sulfonylurea

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7
Q

Repaglinide: Drug Class

A

Glinide

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8
Q

Glinides: Side Effects

A

Dominant adverse effect is hypoglycemia

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9
Q

Glinides: Mechanism of action

A

They bind to specific receptors on the insulin producing pancreatic beta cells and close a certain K+ channel. This causes depolarization and triggers an increase of intracellular calcium which, in turn, augments the release of granules of insulin

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10
Q

Nateglinide: Drug Class

A

Glinide

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11
Q

Name the two Glinides

A

Repaglinide and Nateglinide

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12
Q

Metformin: Drug Class

A

Biguanide

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13
Q

Metformin: Mechanism of action

A

It enhances insulin’s suppression of gluconeogenesis by the liver (thus decreasing hepatic glucose output), and it enhances glucose uptake and utilization primarily in skeletal muscle

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14
Q

Which Diabetes drug(s) reduce(s) triglycerides and LDL cholesterol levels

A

Metformin

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15
Q

Metformin: Side Effects

A

Early (Transient): Nausea, abdominal discomfort, and diarrhea. Late: Lactic acidosis (rare but increased in renal failure, liver failure, CHF or shock and has 50% mortality rate)

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16
Q

Metformin is contraindicated in what condition(s)

A

Renal failure, liver failure, CHF or shock

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17
Q

Pioglitazone: Drug Class

A

Thiazolidinedione

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18
Q

This drug class acts by activating PPARs (especially PPAR?) which, when activated, increases transcription of a number of specific genes (and decreases transcription of others). This all results in increased peripheral (muscle) sensitivity to glucose

A

Thiazolidinediones

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19
Q

Pioglitazone is the only remaining Thiazolidinedione on the market because

A

It does not cause hepatic and cardiac toxicity like troglitazone and rosiglitazone do respectively

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20
Q

This diabetes drug class takes 4-6 weeks to exert its affects on the patient

A

Thiazolidinediones

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21
Q

Which Diabetes drug(s) reduce(s) triglycerides and raise HDL cholesterol levels

A

Pioglitazone

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22
Q

Which diabetes drug(s) can cause fluid retention and thus are contraindicated in CHF

A

Pioglitazone

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23
Q

Acarbose: Drug Class

A

Alpha-Glucosidase Inhibitor

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24
Q

Name the two Alpha-Glucosidase Inhibitors

A

Acarbose and Miglitol

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25
Q

Which diabetes drug class will reduce post-prandial hyperglycemia

A

Alpha-Glucosidase Inhibitors

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26
Q

Miglitol: Drug Class

A

Alpha-Glucosidase Inhibitor

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27
Q

Alpha-Glucosidase Inhibitors: Mechanism of action

A

They inhibit Alpha-Glucosidase at the jejunal brush border, preventing it from cleaving oligosaccharides for rapid carbohydrate absorption. As a result, carbohydrates are absorbed more slowly

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28
Q

Alpha-Glucosidase Inhibitors: Side Effects

A

Abdominal discomfort, diarrhea, and flatulence (symptoms ameliorate or subside after 4-8 weeks). It can cause liver toxicity

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29
Q

Sitagliptin: Drug Class

A

Dipeptidyl-peptidase 4 (DPP4) Inhibitor

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30
Q

Dipeptidyl-peptidase 4 (DPP4) Inhibitors: Mechanism of action

A

They inhibit DPP4, an enzyme that breaks down GLP-1 and GIP. GLP-1 increases insulin secretion, decreases glucagon secretion, and delays gastric emptying (in a glucose dependent manner). Thus by inhibiting DPP4, GLP-1 levels increase and their function is enhanced

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31
Q

Saxagliptin: Drug Class

A

Dipeptidyl-peptidase 4 (DPP4) Inhibitor

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32
Q

Name the two Dipeptidyl-peptidase 4 (DPP4) Inhibitors

A

Sitagliptin, Saxagliptin

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33
Q

Methimazole: Drug Class and function

A

Anti-thyroid agent used to treat hyperthyroidism

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34
Q

Anti-thyroid agents: Mechanism of action

A

Inhibit thyroid peroxidase-mediated iodination of thyroglobulin to form T4 and T3 in thyroid gland. Propylthiouracil also partially inhibits the peripheral deiodination of T4 and T3

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35
Q

Anti-thyroid agents: Uses

A

Used to shrink the thyroid, decrease friability (ability to be broken into bits), and control until thyroidectomy. Rarely used chronically. Also used in Pts in whom iodine 131 is planned (methimazole is prefered)

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36
Q

Propylthiouracil: Drug Class and function

A

Anti-thyroid agent used to treat hyperthyroidism

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37
Q

Name the two Anti-thyroid agents

A

Methimazole and Propylthiouracil

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38
Q

Anti-thyroid agents: Side Effects

A

Agranulocytosis (manifests as sore throat and fever), hepatotoxicity, jaundice, and angioneurotic edema

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39
Q

Calcitriol: Drug Class and function

A

Bone mineral hormone that increases the level of calcium and phosphate in the blood

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40
Q

Calcitriol: Mechanism of action

A

It decreases kdney excretion of calcium and phosphate, increases calcium and phosphate absorption in GI tract, and increases calcium and phosphate resorption in bone

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41
Q

PTH: Drug Class and function

A

Bone mineral hormone that increases the level of calcium and decreases the level of phosphate in the blood

42
Q

PTH: Mechanism of action

A

It decreases calcium excretion by the kidney, increases phosphate excretion by the kidney, increases calcium and phosphate resorption in bone, and increases the production of Vitamin D (Calcitriol) which increases calcium and phosphate absorption in GI tract

43
Q

Calcitonin: Drug Class and function

A

Bone mineral hormone that decreases the level of calcium and phosphate in the blood

44
Q

Calcitonin: Mechanism of action

A

It decreases calcium and phosphate resorption in the kidney, and inhibits bone osteoclasts thus reducing bone resorption of calcium and phosphate

45
Q

Which tissue/organ produces Calcitonin

A

The thyroid

46
Q

Calcium Chloride: Drug Class

A

Calcium mineral supplement

47
Q

Calcium Chloride: Side Effects

A

It can act as an irritant by desiccating moist skin. Solid calcium chloride dissolves exothermically, and burns can result in the mouth and esophagus if it is ingested. Ingestion of concentrated solutions or solid products may cause gastrointestinal irritation or ulceration

48
Q

Calcium gluconate: Side Effects

A

Nausea, constipation, upset stomach. Rapid intravenous injections of calcium gluconate may cause hypercalcaemia, which can result in vasodilation, cardiac arrhythmias, decreased blood pressure, and bradycardia. Extravasation of calcium gluconate can lead to cellulitis. Intramuscular injections may lead to local necrosis and abscess formation

49
Q

Calcium Gluconate: Drug Class

A

Calcium mineral supplement

50
Q

Calcium Gluconate: Uses

A

Used in the treatment of hypocalcemia and to counteract an overdose of magnesium sulfate

51
Q

Alendronate: Drug Class

A

Bisphosphonate

52
Q

Alendronate: Uses

A

Tx for Paget Dx (excessive breakdown and formation of bone). Most potent Bisphosphonate and used for osteoporosis in post-menopausal women

53
Q

Ibandronate: Drug Class

A

Bisphosphonate

54
Q

Pamindronate: Drug Class

A

Bisphosphonate

55
Q

Pamindronate: Uses

A

Tx for Paget Dx (excessive breakdown and formation of bone).

56
Q

Resendronate: Drug Class

A

Bisphosphonate

57
Q

Which Bisphosphonates are available for weekly oral dosing regimens

A

Alendronate and Resendronate

58
Q

Which Bisphosphonates are available for monthly oral dosing regimens

A

Ibandronate and Resendronate

59
Q

Bisphosphonates: Mechanism of action

A

Inhibit the activity of osteoclasts

60
Q

Bisphosphates: Side Effects

A

Significant esophageal and gastric irritation. Risk of bone fractures with chronic use.

61
Q

Name the four Bisphosphates

A

Alendronate, Ibandronate, Pamindronate, Resendronate

62
Q

Food interferes with absorption of which drug class

A

Bisphosphonates

63
Q

Which Bisphosphonate is available for IV dosing every 3 months

A

Ibandronate

64
Q

Raloxifene: Drug Class [and mechanism of action]

A

Selective Estrogen Receptor Modulator (SERM) [Inhibits nuclear binding of the estrogen receptor, decreasing secretion of stimulatory growth factor TGF-alpha and increasing inhibitory growth factor TGF-Beta, thus blocking estrogen stimulation of breast cancer cells. It has a static effect on Tumor cell growth]

65
Q

Name the two Selective Estrogen Receptor Modulators (SERMs)

A

Raloxifene and Tamoxifen

66
Q

How does Raloxifene differ from Tamoxifen

A

It has a better adverse event profile (lower risk of uterine cancer) but tamoxifen is superior in breast cancer risk reduction. I also can only be used in post-menpausal women

67
Q

Tamoxifen: Drug Class [and mechanism of action]

A

Selective Estrogen Receptor Modulator (SERM) [Inhibits nuclear binding of the estrogen receptor, decreasing secretion of stimulatory growth factor TGF-alpha and increasing inhibitory growth factor TGF-Beta, thus blocking estrogen stimulation of breast cancer cells. It has a static effect on Tumor cell growth]

68
Q

In what tissues does Tamoxifen act as an estrogen agonist and an estrogen antagonist

A

Agonist: Endometrium. Antagonist: Breast cancer cells and vaginal mucosa

69
Q

Tamoxifen: Uses

A

Adjuvant Tx of breast cancer alone or following chemo in pre & post menopausal women (only hormonal therapy for premenopausal women), Tx of metastatic breast cancer, and prophylaxis in high risk women/women with ductal carcinoma in situ

70
Q

Tamoxifen: Side Effects

A

Improves bone density, improves lipid profile, Hot flashes, nausea/vomiting, edema, thromboembolism, endometrial cancer (3x incidence), cataracts, vaginal discharge and bleeding

71
Q

Tamoxifen should not be given concurrently with what

A

CYP2D6 converts Tamoxifen to the much more potent metabolite endoxifen. Tamoxifen should not be given concurrently with a potent CYP2D6 inhibitor

72
Q

Anastrozole: Drug Class

A

Aromatase Inhibitor

73
Q

Aromatase Inhibitor: Mechanism of action

A

Selectively Inhibits aromatase which converts androstenedione and testosterone to estrone and estradiol respectively

74
Q

Name the three Aromatase Inhibitors

A

Anastrozole, Exemestane, and Letrozole

75
Q

Exemestane: Drug Class

A

Aromatase Inhibitor

76
Q

Aromatase Inhibitors: Uses

A

Tx of locally advanced or metastatic breast cancer (hormone receptor positive or unknown) in post menopausal women, Tx of advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy, adjuvant Tx of early hormone receptor positive breast cancer in post menopausal women.

77
Q

Why are Aromatase Inhibitors not used in premenopausal women

A

Because in premenopausal women, 95% of estrogen is produced by the ovary not by aromatase conversion

78
Q

Letrozole: Drug Class

A

Aromatase Inhibitor

79
Q

Which drug class is never given concurrently with chemotherapy (always given sequentially)

A

Aromatase Inhibitors

80
Q

Aromatase Inhibitors: Side Effects

A

Fatigue, arthralgias/myalgias, osteoporosis/osteopenia, hot flashes, vaginal dryness.

81
Q

Which Aromatase Inhibitor does not have a lower incidence of endometrial cancer and thromboembolic events compared with tamoxifen.

A

Letrozole

82
Q

Which Aromatase Inhibitor may cause less bone turnover than the others

A

Exemsestane

83
Q

Goserelin: Drug Class

A

Gonadotropin Releasing Hormone Agonist (synonymous with LHRH agonist)

84
Q

Gonadotropin Releasing Hormone Agonists: Mechanism of Action

A

Inhibit the synthesis of sex steroids in both men and women: after initial surge, supresses LH, FSH, and subsequently testosterone (males & females) and estrogen (premenopausal females)

85
Q

Which Gonadotropin Releasing Hormone Agonist can cause headache, vaginitis, and diaphoresis

A

Goserelin

86
Q

Histrelin: Drug Class

A

Gonadotropin Releasing Hormone Agonist (synonymous with LHRH agonist)

87
Q

Name the four Gonadotropin Releasing Hormone Agonists

A

Goserelin, Histrelin, Leuprolide, Triptorelin

88
Q

Which Gonadotropin Releasing Hormone Agonist can cause urinary retention

A

Histrelin

89
Q

Leuprolide: Drug Class

A

Gonadotropin Releasing Hormone Agonist (synonymous with LHRH agonist)

90
Q

Gonadotropin Releasing Hormone Agonists: Side Effects

A

Initial tumor flare (lasts a week), Gynecomastia/breast tenderness, hot flashes, and longterm use can lead to osteoporosis (bisphosphonates can be used to help)

91
Q

Gonadotropin Releasing Hormone Agonists are started with what in order to avoid tumor flare

A

An antiandrogenic agent

92
Q

Triptorelin: Drug Class

A

Gonadotropin Releasing Hormone Agonist (synonymous with LHRH agonist)

93
Q

Bicalutamide: Drug Class

A

Anti-androgenic Agent

94
Q

Name the three traditional (Non-steroidal) Anti-androgenic Agents

A

Bicalutamide, Flutamide, and Nilutamide

95
Q

What are the Uses of the traditional Anti-androgenic Agents (Bicalutamide, Flutamide, and Nilutamide)

A

Inferior to LHRH agonists and so are not used alone. Used in combination with LHRH agonists for prostate cancer and to prevent tumor flare, used to prevent hot flashes associated with castration, all agents are equally efficacious but differ in toxicity

96
Q

Flutamide: Drug Class

A

Anti-androgenic Agent

97
Q

Name the two new Anti-androgenic Agents

A

Abiraterone and Enzalutamide

98
Q

What are the side effects of the traditional Anti-androgenic Agents (Bicalutamide, Flutamide, and Nilutamide)

A

Gynecomastia, hot flashes, increase in liver enzymes, nausea/vomiting, diarrhea (most severe with flutamide), disulfuram type reaction with nilutamide

99
Q

Nilutamide: Drug Class

A

Anti-androgenic Agent

100
Q

What is the mechanism of action of the traditional Anti-androgenic Agents (Bicalutamide, Flutamide, and Nilutamide)

A

Bind to androgen receptors and competitively inhibit the binding of dihydrotestosterone and testosterone

Old Gastrointestinal Cards (4 decks)

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