Endocrine/Reproductive Drugs Flashcards Preview

Pharmacology > Endocrine/Reproductive Drugs > Flashcards

Flashcards in Endocrine/Reproductive Drugs Deck (144):
1

Rapid-acting insulin (name 3)

Lispro
Aspart
Glulisine

2

Rapid-acting insulin (use)

Postprandial glucose control in DM1, 2, GDM

3

Short-acting insulin (name 1)

regular insulin

4

Short-acting insulin (3 uses)

1. DM1, 2, GDM
2. DKA (IV)
3. Hyperkalemia (+ glucose)

5

Intermediate-acting insulin (name 1)

NPH

6

Long-acting insulin (name 2)

Glargine
Detemir

7

Long-acting insulin (use)

Basal glucose control in DM1, 2, GDM

8

Metformin (mechanism)

Biguanides
Alteration of intracellular microsomal enzyme -> decreases hepatic glucose production, increases peripheral insulin sensitivity
Euglycemic and doesn't cause weight gain

9

Metformin (use)

1st line in DM2, can use w/out islet fx

10

Metformin (side effect)

Lactic acidosis -> can't use in renal&hepatic failure, CHF, alcoholism, sepsis

11

Tolbutamide (mechanism)

Sulfonylureas
Closes K+ channel in beta cells -> depolarization -> increased Ca2+ influx -> insulin release

12

Tolbutamide (use)

Sulfonylureas
DM2 (useless in DM1 bc requires some islet fx)
Good in renal dysfx

13

Tolbutamide (side effects)

1st gen sulfonylureas
Disulfiram-like effects

14

Chlorpropamide (mechanism)

Sulfonylureas
Closes K+ channel in beta cells -> depolarization -> increased Ca2+ influx -> insulin release

15

Chlorpropamide (use)

Sulfonylureas
DM2 (useless in DM1 bc requires some islet fx)

16

Chlorpropamide (side effects)

1st gen sulfonylureas
Disulfiram-like effects, increased risk of hypoglycemia in renal failure, don't use in CHF

17

Glyburide (mechanism)

Sulfonylureas
Closes K+ channel in beta cells -> depolarization -> increased Ca2+ influx -> insulin release

18

Glyburide (use)

Sulfonylureas
DM2 (useless in DM1 bc requires some islet fx)

19

Glyburide (side effect)

2nd gen sulfonylureas
Increased risk of hypoglycemia in renal failure

20

Glimepiride (mechanism)

Sulfonylureas
Closes K+ channel in beta cells -> depolarization -> increased Ca2+ influx -> insulin release

21

Glimepiride (use)

Sulfonylureas
DM2 (useless in DM1 bc requires some islet fx)

22

Glimepiride (side effect)

2nd gen sulfonylureas
Increased risk of hypoglycemia in renal failure

23

Glipizide (mechanism)

Sulfonylureas
Closes K+ channel in beta cells -> depolarization -> increased Ca2+ influx -> insulin release
Short acting

24

Glipizide (use)

Sulfonylureas
DM2 (useless in DM1 bc requires some islet fx)

25

Glipizide (side effect)

2nd gen sulfonylureas
Increased risk of hypoglycemia in renal failure

26

-glitazone (mechanism)

Thiazolidinediones
Binds PPAR-g (INTRACELLULAR RECEPTOR) -> transactivation -> increases insulin sensitivity in peripheral tissue (increasing GLUT-4 transporter expression), also increases level of adiponectin and promotes adipocyte differentiation (PPAR-g regulates FA storage)
Takes days-weeks to take effects

27

-glitazone (use)

DM2

28

-glitazone (side effects)

Hepatotoxicity (monitor liver fx), HF, weight gain, edema (fluid retention worse when used w/ insulin)
Don't use in liver disease, CHF, CAD!

29

Acarbose (mechanism)

Inhibits brush-border alpha-glucosidase (surface membrane-bound enzyme) -> decreases absorption

30

Acarbose (use)

DM2

31

Acarbose (side effect)

GI disturbances -> don't use in IBS or intestinal blockage

32

Miglitol (mechanism)

Inhibits brush-border alpha-glucosidase (surface membrane-bound enzyme) -> decreases absorption

33

Miglitol (use)

DM2

34

Miglitol (side effect)

GI disturbances

35

Pramlintide (mechanism)

Amylin analog
Decreases gastric emptying and glucagon

36

Pramlintide (use)

DM1, 2

37

Pramlintide (side effects)

Nausea, diarrhea, hypoglycemia

38

Exenatide, Liraglutide (mechanism)

GLP-1 analog -> acts thru G-protein linked adenylyl cyclase -> increases insulin, decreases glucagon

39

Exenatide, Liraglutide (use)

DM2

40

Exenatide, Liraglutide (side effects)

Pancreatitis, n/v

41

-gliptin (mechanism)

DPP-4 inhibitors -> inhibits metab of GLP-1 -> increases insulin, decreases glucagon

42

-gliptin (use)

DM2

43

-gliptin (side effects)

Mild urinary/respiratory infections

44

Propylthiouracil (mechanism)

Thionamides
Blocks thyroid peroxidase (decreases thyroid synthesis) and 5'-deiodinase (decreases peripheral conversion to T3)

45

Propylthiouracil (use)

For hyperthyroidism in pregnancy (1st trimester only, see side effects for why -> change to methimazole later in pregnancy)

46

Propylthiouracil (side effects)

Liver toxicity (why methimazole preferred unless pregnant in first trimester), agranulocytosis, aplastic anemia, skin rash
ANCA develops in half the pts taking this med

47

Methimazole (mechanism)

Thionamides
Blocks thyroid peroxidase (decreases thyroid synthesis). Doesn't block 5'-deiodinase like propylthiouracil

48

Methimazole (use)

First line for hyperthyroidism unless pregnant

49

Methimazole (side effects)

Teratogen and can cause aplasia cutis (only used after 1st trimester), agranulocytosis, aplastic anemia, skin rash

50

Levothyroxine (mechanism)

T4 analog

51

Levothyroxine (use)

First line for hypothyroidism

52

Levothyroxine (side effects)

Signs of hyperthyroidism -> tachycardia, heat intolerance, tremors, arrhythmias

53

Liothyronine (mechanism)

T3 analog

54

Liothyronine (use)

Myxedema coma (not routinely used for hypothyroidism, see side effects for why)

55

Liothyronine (side effects)

Arrhythmogenic and can precipitate HF

56

Demeclocycline (mechanism)

ADH antagonist
Member of tetracycline family

57

Demeclocycline (use)

SIADH

58

Demeclocycline (side effects)

Nephrogenic DI, photosensitivity, abnormality of bone and teeth

59

Octreotide (mechanism)

Somatostatin analog -> inhibits GH, glucagon, insulin, gastrin, VIP

60

Octreotide (2 main uses)

eso varices (by reducing splanchnic blood flow by inhibiting hormones responsible for splanchnic vasodilation), conditions characterized by oversecretion of hormones it inhibits (acromegaly, carcinoid, gastrinoma, glucagonoma)

61

Octreotide (side effects)

Gallbladder disease, pancreatitis, cardiac arrhythmias, hyper or hypothyroidism

62

Leuprolide (mechanism)

GnRH agonist

63

Leuprolide (2 uses)

Pulsatile release (mimic normal release) -> increases LH & FSH -> fertility
Continuous release -> decreases LH & FSH -> suppress growth of prostate cancer, leiomyomas, endometriosis, and halts precocious puberty

64

Leuprolide (side effects)

Bone pain, feet/ankle swelling

65

Somatotropin/Somatotrem (mechanism)

GH analog

66

Somatotropin/Somatotrem (2 uses)

Dwarfism/short stature
Wasting (assc w/ AIDS or malignancy)

67

Somatotropin/Somatotrem (side effects)

DM (from decreased insulin sensitivity and hyperglycemia), carpal tunnel syndrome, leukemia, slipped capital femoral epiphyseal plate, edema (hand/foot), thickening of bones

68

Bromocriptine (mechanism)

D2 agonist

69

Bromocriptine (2 uses)

Pituitary adenoma (prolactinoma, acromegaly)
Parkinson disease (high dose)

70

Bromocriptine (side effects)

Psychotic sx, dizziness, headache, nausea, confusion

71

Cabergoline (mechanism)

D2 agonist

72

Cabergoline (2 uses)

Pituitary adenoma (prolactinoma, acromegaly)
Parkinson disease (high dose)

73

Cabergoline (side effects)

Psychotic sx, dizziness, headache, nausea, confusion

74

Desmopressin (mechanism)

ADH analog (DDAVP) -> likes V2 receptors (collecting tubules) more than V1 (vascular SMC)
Stimulates vWF release from endothelium

75

Desmopressin (3 uses)

Central DI
vWF disease
Bedwetting

76

Desmopressin (side effects)

Hyponatremia, headache, flushing

77

Oxytocin (3 uses)

Induces labor
Decreases postpartum bleeding (by inducing contractions)
Stimulates breast milk letdown

78

Oxytocin (side effects)

Chest pain, confusion, vaginal bleeding, palpitations, seizures

79

Iodine (2 uses)

Thyroid storm (inhibits thyroid hormone release when used in large dose)
Before thyroidectomy (to prevent thyroid storm)

80

Radioiodine (2 uses)

Hyperthyroidism
Adjunctive for thyroid cancer

81

Iodine/Radioiodine (side effects)

Metallic taste, excessive salivation, diarrhea, rash

82

Alendronate and other "-dronate" (mechanism)

Bisphosphonates
Pyrophosphate analog which is a component of hydroxyapatite -> prevent bone resorption (decreased osteoclast activity)

83

Alendronate and other "-dronate" (3 uses)

Bisphosphonates
Postmenopausal osteoporosis
Paget disease (reduces bone turnover)
Pt on long-term high-dose glucocorticoid (prevent accelerated bone loss)

84

Alendronate and other "-dronate" (side effects)

Osteonecrosis of jaw, joint/back pain, GI stuff (heartburn, erosive esophagitis, stomach upset - so take on empty stomach)

85

Calcitriol (mechanism)

Active vit D
Increases Ca2+ absorption from small intestines

86

Calcitriol (use)

Hypocalcemia from all causes

87

Calcitriol (side effects)

Hypercalcemia (so constipation follows), polyuria, weakness, somnolence, headache

88

Repaglinide (mechanism)

Closes K+ channel in beta cells (at a diff site from sulfonylureas tho) -> depolarization -> increased Ca2+ influx -> insulin release
Unlike sulfonylureas, doesn't stimulate insulin release when extracellular glucose is low

89

Repaglinide (use)

DM2 to prevent postprandial hyperglycemia (taken before meals)
CAN use in renal insufficiency (unlike sulfonylureas which have the same mechanism) -> met by liver and excreted by gut

90

-sone (mechanism)

Glucocorticoids
Also triamcinolone

91

-sone (2 uses)

Addison disease
Immune suppression (inflammation, asthma, etc)

92

-sone (side effects)

Iaotrogenic Cushing syndrome
Adrenal insufficiency if stopped abruptly after chronic use

93

Ethinyl estradiol (mechanism)

Estrogen, most common form in OCP

94

Estrogen (side effects)

Procoagulation, increased risk of endometrial cancer

95

DES (mechanism)

Estrogen

96

DES (side effects)

Clear cell adenocarcinoma of vagina in females exposed to DES in utero -> so pulled from market

97

Mestranol (mechanism)

Estrogen

98

Clomiphene (mechanism)

SERMs
Anti-estrogen in HYPOTHALAMUS -> increases LH and FSH release

99

Clomiphene (use)

Infertility due to anovulation (PCOS in women desirous of pregnancy)

100

Clomiphene (side effects)

Hot flashes, visual disturbances, multiple pregnancies, ovarian enlargement

101

Tamoxifen (mechanism)

SERMs
Anti-estrogen in BREAST
Agonist in UTERUS and bone

102

Tamoxifen (use)

ER+ breast cancer (pre-menopausal)

103

Tamoxifen (side effects)

Endometrial cancer, thrombi

104

Raloxifene (mechanism)

SERMs
Anti-estrogen in BREAST and UTERUS
Agonist in bone

105

Raloxifene (2 uses)

ER+ breast cancer (postmenopausal)
Osteoporosis prevention in postmenopausal

106

Raloxifene (side effects)

Thrombi

107

Anastrozole (mechanism)

Aromatase inhibitor -> decreases estrogen

108

Anastrozole (use)

Postmenopausal w/ breast cancer

109

Exemestane (mechanism)

Aromatase inhibitor -> decreases estrogen

110

Exemestane (use)

Postmenopausal w/ breast cancer

111

Progestins (3 uses)

OCP
Endometrial cancer
AUB

112

Mifepristone/RU-486 (mechanism)

Competitive inhibitor of progestins

113

Mifepristone/RU-486 (use)

Abortion (used w/ misoprostol - PGE1)

114

Mifepristone/RU-486 (side effects)

heavy bleeding, GI effects (n/v, anorexia), abd pain

115

OCP (3 contraindications)

smokers > 35 yo (increased risk of cardiovascular events)
hx of thromboembolism and stroke
hx of estrogen-dependent tumor

116

Danazol (mechanism)

Partial agonist of androgen

117

Danazol (2 uses)

Endometriosis
Hereditary angioedema

118

Danazol (side effects)

Hepatotoxicity, decreased HDL, androgen effects (acne, hirsutism, masculinization), weight gain, edema

119

Testosterone (2 uses)

Promotes recovery after burn/injury (anabolic effect)
Replete testosterone (fix sexual dysfx 2ndary to testosterone deficiency -> like after mumps orchitis)

120

Testosterone (side effects)

Reduces intratesticular testosterone (neg feedback to LH) -> get gonadal atrophy in males
Premature epiphyseal plate closure
Increases LDL and decreases HDL

121

Finasteride (mechanism)

5a-reductase inhibitor (so get less conversion from testosterone to DHT)

122

Finasteride (3 uses)

BPH
Male pattern baldness
Hirsutism

123

Flutamide (mechanism)

Competitive inhibitor of androgens
Nonsteroidal

124

Flutamide (2 uses)

Prostate carcinoma
Hirsutism

125

Ketoconazole (mechanism)

Inhibits 17,20-desmolase -> inhibits steroid synthesis (so affects multiple pathways leading to decreased androgen synthesis)

126

Spironolactone (mechanism)

Anti-androgen (inhibits steroid binding, 17,20-desmolase, 17a-hydroxylase)

127

Ketoconazole (use)

PCOS to prevent hirsutism

128

Spironolactone (use)

PCOS to prevent hirsutism

129

Ketoconazole (side effects)

Gynecomastia, amenorrhea

130

Spironolactone (side effects)

Gynecomastia, amenorrhea

131

-enafil (mechanism)

Inhibits cGMP-specific PDE-5 -> increases cGMP -> SMC relaxation in corpus cavernosum -> erection

132

-enafil (2 uses)

ED
Pulm HTN (prolongs vasodilation)

133

-enafil (side effects)

Life-threatening hypotension in pts taking nitrates
Impaired blue-green color vision
Headache, flushing, dyspepsia

134

Fulvestrant (mechanism)

Anti-estrogen

135

Fulvestrant (use)

ER+ breast cancer (postmenopausal)

136

Cyproterone (mechanism)

Anti-androgen (at receptor)

137

Mitotane (mechanism and use)

Adrenocorticolytic drug
For adrenocortical carcinoma

138

Medroxyprogesterone (use)

Progesterone-only contraceptive IM injection

139

Pegvisomant (mechanism and use)

GH receptor antagonist
For acromegaly

140

Podophyllin (mechanism and use)

Inhibits topoisomerase II
Topically for genital warts

141

"-gliflozin" (mechanism and use)

Canagliflozin and dapagliflozin
Inhibits SGLT2 (transporters in renal tubule lumen) -> urinary glucose loss
For DM2

142

"-gliflozin" (3 side effects)

UTI, genital mycotic infections
Hypotension
Avoided in pts w/ renal impairment!

143

Danazole (mechanism and 3 uses)

Androgen used to suppress LH and FSH release by pituitary
Endometriosis, hemophilia, ITP

144

Nandrolone (mechanism and use)

Anabolic steroids
For anemia caused by kidney failure