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Pharmacology > Endocrine/Reproductive Drugs > Flashcards

Endocrine/Reproductive Drugs Flashcards

1
Q

Rapid-acting insulin (name 3)

A

Lispro
Aspart
Glulisine

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2
Q

Rapid-acting insulin (use)

A

Postprandial glucose control in DM1, 2, GDM

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3
Q

Short-acting insulin (name 1)

A

regular insulin

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4
Q

Short-acting insulin (3 uses)

A
  1. DM1, 2, GDM
  2. DKA (IV)
  3. Hyperkalemia (+ glucose)
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5
Q

Intermediate-acting insulin (name 1)

A

NPH

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6
Q

Long-acting insulin (name 2)

A

Glargine

Detemir

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7
Q

Long-acting insulin (use)

A

Basal glucose control in DM1, 2, GDM

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8
Q

Metformin (mechanism)

A

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

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9
Q

Metformin (use)

A

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

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10
Q

Metformin (side effect)

A

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

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11
Q

Tolbutamide (mechanism)

A

Sulfonylureas

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

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12
Q

Tolbutamide (use)

A

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

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13
Q

Tolbutamide (side effects)

A

1st gen sulfonylureas

Disulfiram-like effects

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14
Q

Chlorpropamide (mechanism)

A

Sulfonylureas

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

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15
Q

Chlorpropamide (use)

A

Sulfonylureas

DM2 (useless in DM1 bc requires some islet fx)

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16
Q

Chlorpropamide (side effects)

A

1st gen sulfonylureas

Disulfiram-like effects, increased risk of hypoglycemia in renal failure, don’t use in CHF

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17
Q

Glyburide (mechanism)

A

Sulfonylureas

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

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18
Q

Glyburide (use)

A

Sulfonylureas

DM2 (useless in DM1 bc requires some islet fx)

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19
Q

Glyburide (side effect)

A

2nd gen sulfonylureas

Increased risk of hypoglycemia in renal failure

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20
Q

Glimepiride (mechanism)

A

Sulfonylureas

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

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21
Q

Glimepiride (use)

A

Sulfonylureas

DM2 (useless in DM1 bc requires some islet fx)

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22
Q

Glimepiride (side effect)

A

2nd gen sulfonylureas

Increased risk of hypoglycemia in renal failure

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23
Q

Glipizide (mechanism)

A

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

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24
Q

Glipizide (use)

A

Sulfonylureas

DM2 (useless in DM1 bc requires some islet fx)

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25
Q

Glipizide (side effect)

A

2nd gen sulfonylureas

Increased risk of hypoglycemia in renal failure

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26
Q

-glitazone (mechanism)

A

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

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27
Q

-glitazone (use)

A

DM2

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28
Q

-glitazone (side effects)

A

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

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29
Q

Acarbose (mechanism)

A

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

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30
Q

Acarbose (use)

A

DM2

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31
Q

Acarbose (side effect)

A

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

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32
Q

Miglitol (mechanism)

A

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

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33
Q

Miglitol (use)

A

DM2

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34
Q

Miglitol (side effect)

A

GI disturbances

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35
Q

Pramlintide (mechanism)

A

Amylin analog

Decreases gastric emptying and glucagon

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36
Q

Pramlintide (use)

A

DM1, 2

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37
Q

Pramlintide (side effects)

A

Nausea, diarrhea, hypoglycemia

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38
Q

Exenatide, Liraglutide (mechanism)

A

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

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39
Q

Exenatide, Liraglutide (use)

A

DM2

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40
Q

Exenatide, Liraglutide (side effects)

A

Pancreatitis, n/v

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41
Q

-gliptin (mechanism)

A

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

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42
Q

-gliptin (use)

A

DM2

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43
Q

-gliptin (side effects)

A

Mild urinary/respiratory infections

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44
Q

Propylthiouracil (mechanism)

A

Thionamides

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

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45
Q

Propylthiouracil (use)

A

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

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46
Q

Propylthiouracil (side effects)

A 
Liver toxicity (why methimazole preferred unless pregnant in first trimester), agranulocytosis, aplastic anemia, skin rash
ANCA develops in half the pts taking this med
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47
Q

Methimazole (mechanism)

A

Thionamides

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

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48
Q

Methimazole (use)

A

First line for hyperthyroidism unless pregnant

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49
Q

Methimazole (side effects)

A

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

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50
Q

Levothyroxine (mechanism)

A

T4 analog

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51
Q

Levothyroxine (use)

A

First line for hypothyroidism

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52
Q

Levothyroxine (side effects)

A

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

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53
Q

Liothyronine (mechanism)

A

T3 analog

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54
Q

Liothyronine (use)

A

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

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55
Q

Liothyronine (side effects)

A

Arrhythmogenic and can precipitate HF

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56
Q

Demeclocycline (mechanism)

A

ADH antagonist

Member of tetracycline family

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57
Q

Demeclocycline (use)

A

SIADH

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58
Q

Demeclocycline (side effects)

A

Nephrogenic DI, photosensitivity, abnormality of bone and teeth

59
Q

Octreotide (mechanism)

A

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

60
Q

Octreotide (2 main uses)

A

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
Q

Octreotide (side effects)

A

Gallbladder disease, pancreatitis, cardiac arrhythmias, hyper or hypothyroidism

62
Q

Leuprolide (mechanism)

A

GnRH agonist

63
Q

Leuprolide (2 uses)

A 
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
Q

Leuprolide (side effects)

A

Bone pain, feet/ankle swelling

65
Q

Somatotropin/Somatotrem (mechanism)

A

GH analog

66
Q

Somatotropin/Somatotrem (2 uses)

A

Dwarfism/short stature

Wasting (assc w/ AIDS or malignancy)

67
Q

Somatotropin/Somatotrem (side effects)

A

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

68
Q

Bromocriptine (mechanism)

A

D2 agonist

69
Q

Bromocriptine (2 uses)

A 
Pituitary adenoma (prolactinoma, acromegaly)
Parkinson disease (high dose)
70
Q

Bromocriptine (side effects)

A

Psychotic sx, dizziness, headache, nausea, confusion

71
Q

Cabergoline (mechanism)

A

D2 agonist

72
Q

Cabergoline (2 uses)

A 
Pituitary adenoma (prolactinoma, acromegaly)
Parkinson disease (high dose)
73
Q

Cabergoline (side effects)

A

Psychotic sx, dizziness, headache, nausea, confusion

74
Q

Desmopressin (mechanism)

A 
ADH analog (DDAVP) -> likes V2 receptors (collecting tubules) more than V1 (vascular SMC)
Stimulates vWF release from endothelium
75
Q

Desmopressin (3 uses)

A

Central DI
vWF disease
Bedwetting

76
Q

Desmopressin (side effects)

A

Hyponatremia, headache, flushing

77
Q

Oxytocin (3 uses)

A

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

78
Q

Oxytocin (side effects)

A

Chest pain, confusion, vaginal bleeding, palpitations, seizures

79
Q

Iodine (2 uses)

A 
Thyroid storm (inhibits thyroid hormone release when used in large dose)
Before thyroidectomy (to prevent thyroid storm)
80
Q

Radioiodine (2 uses)

A

Hyperthyroidism

Adjunctive for thyroid cancer

81
Q

Iodine/Radioiodine (side effects)

A

Metallic taste, excessive salivation, diarrhea, rash

82
Q

Alendronate and other “-dronate” (mechanism)

A

Bisphosphonates

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

83
Q

Alendronate and other “-dronate” (3 uses)

A

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

84
Q

Alendronate and other “-dronate” (side effects)

A

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

85
Q

Calcitriol (mechanism)

A

Active vit D

Increases Ca2+ absorption from small intestines

86
Q

Calcitriol (use)

A

Hypocalcemia from all causes

87
Q

Calcitriol (side effects)

A

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

88
Q

Repaglinide (mechanism)

A

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
Q

Repaglinide (use)

A

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
Q

-sone (mechanism)

A

Glucocorticoids

Also triamcinolone

91
Q

-sone (2 uses)

A 
Addison disease
Immune suppression (inflammation, asthma, etc)
92
Q

-sone (side effects)

A

Iaotrogenic Cushing syndrome

Adrenal insufficiency if stopped abruptly after chronic use

93
Q

Ethinyl estradiol (mechanism)

A

Estrogen, most common form in OCP

94
Q

Estrogen (side effects)

A

Procoagulation, increased risk of endometrial cancer

95
Q

DES (mechanism)

A

Estrogen

96
Q

DES (side effects)

A

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

97
Q

Mestranol (mechanism)

A

Estrogen

98
Q

Clomiphene (mechanism)

A

SERMs

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

99
Q

Clomiphene (use)

A

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

100
Q

Clomiphene (side effects)

A

Hot flashes, visual disturbances, multiple pregnancies, ovarian enlargement

101
Q

Tamoxifen (mechanism)

A

SERMs
Anti-estrogen in BREAST
Agonist in UTERUS and bone

102
Q

Tamoxifen (use)

A

ER+ breast cancer (pre-menopausal)

103
Q

Tamoxifen (side effects)

A

Endometrial cancer, thrombi

104
Q

Raloxifene (mechanism)

A

SERMs
Anti-estrogen in BREAST and UTERUS
Agonist in bone

105
Q

Raloxifene (2 uses)

A

ER+ breast cancer (postmenopausal)

Osteoporosis prevention in postmenopausal

106
Q

Raloxifene (side effects)

A

Thrombi

107
Q

Anastrozole (mechanism)

A

Aromatase inhibitor -> decreases estrogen

108
Q

Anastrozole (use)

A

Postmenopausal w/ breast cancer

109
Q

Exemestane (mechanism)

A

Aromatase inhibitor -> decreases estrogen

110
Q

Exemestane (use)

A

Postmenopausal w/ breast cancer

111
Q

Progestins (3 uses)

A

OCP
Endometrial cancer
AUB

112
Q

Mifepristone/RU-486 (mechanism)

A

Competitive inhibitor of progestins

113
Q

Mifepristone/RU-486 (use)

A

Abortion (used w/ misoprostol - PGE1)

114
Q

Mifepristone/RU-486 (side effects)

A

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

115
Q

OCP (3 contraindications)

A

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

116
Q

Danazol (mechanism)

A

Partial agonist of androgen

117
Q

Danazol (2 uses)

A

Endometriosis

Hereditary angioedema

118
Q

Danazol (side effects)

A

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

119
Q

Testosterone (2 uses)

A 
Promotes recovery after burn/injury (anabolic effect)
Replete testosterone (fix sexual dysfx 2ndary to testosterone deficiency -> like after mumps orchitis)
120
Q

Testosterone (side effects)

A

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

121
Q

Finasteride (mechanism)

A

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

122
Q

Finasteride (3 uses)

A

BPH
Male pattern baldness
Hirsutism

123
Q

Flutamide (mechanism)

A

Competitive inhibitor of androgens

Nonsteroidal

124
Q

Flutamide (2 uses)

A

Prostate carcinoma

Hirsutism

125
Q

Ketoconazole (mechanism)

A

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

126
Q

Spironolactone (mechanism)

A

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

127
Q

Ketoconazole (use)

A

PCOS to prevent hirsutism

128
Q

Spironolactone (use)

A

PCOS to prevent hirsutism

129
Q

Ketoconazole (side effects)

A

Gynecomastia, amenorrhea

130
Q

Spironolactone (side effects)

A

Gynecomastia, amenorrhea

131
Q

-enafil (mechanism)

A

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

132
Q

-enafil (2 uses)

A 
ED
Pulm HTN (prolongs vasodilation)
133
Q

-enafil (side effects)

A

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

134
Q

Fulvestrant (mechanism)

A

Anti-estrogen

135
Q

Fulvestrant (use)

A

ER+ breast cancer (postmenopausal)

136
Q

Cyproterone (mechanism)

A

Anti-androgen (at receptor)

137
Q

Mitotane (mechanism and use)

A

Adrenocorticolytic drug

For adrenocortical carcinoma

138
Q

Medroxyprogesterone (use)

A

Progesterone-only contraceptive IM injection

139
Q

Pegvisomant (mechanism and use)

A

GH receptor antagonist

For acromegaly

140
Q

Podophyllin (mechanism and use)

A

Inhibits topoisomerase II

Topically for genital warts

141
Q

“-gliflozin” (mechanism and use)

A

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

142
Q

“-gliflozin” (3 side effects)

A

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

143
Q

Danazole (mechanism and 3 uses)

A

Androgen used to suppress LH and FSH release by pituitary

Endometriosis, hemophilia, ITP

144
Q

Nandrolone (mechanism and use)

A

Anabolic steroids

For anemia caused by kidney failure

Pharmacology (12 decks)

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