Endocrine/Reproductive Drugs Flashcards
1
Q
Rapid-acting insulin (name 3)
A
Lispro
Aspart
Glulisine
2
Q
Rapid-acting insulin (use)
A
Postprandial glucose control in DM1, 2, GDM
3
Q
Short-acting insulin (name 1)
A
regular insulin
4
Q
Short-acting insulin (3 uses)
A
- DM1, 2, GDM
- DKA (IV)
- Hyperkalemia (+ glucose)
5
Q
Intermediate-acting insulin (name 1)
A
NPH
6
Q
Long-acting insulin (name 2)
A
Glargine
Detemir
7
Q
Long-acting insulin (use)
A
Basal glucose control in DM1, 2, GDM
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
9
Q
Metformin (use)
A
1st line in DM2, can use w/out islet fx
10
Q
Metformin (side effect)
A
Lactic acidosis -> can’t use in renal&hepatic failure, CHF, alcoholism, sepsis
11
Q
Tolbutamide (mechanism)
A
Sulfonylureas
Closes K+ channel in beta cells -> depolarization -> increased Ca2+ influx -> insulin release
12
Q
Tolbutamide (use)
A
Sulfonylureas
DM2 (useless in DM1 bc requires some islet fx)
Good in renal dysfx
13
Q
Tolbutamide (side effects)
A
1st gen sulfonylureas
Disulfiram-like effects
14
Q
Chlorpropamide (mechanism)
A
Sulfonylureas
Closes K+ channel in beta cells -> depolarization -> increased Ca2+ influx -> insulin release
15
Q
Chlorpropamide (use)
A
Sulfonylureas
DM2 (useless in DM1 bc requires some islet fx)
16
Q
Chlorpropamide (side effects)
A
1st gen sulfonylureas
Disulfiram-like effects, increased risk of hypoglycemia in renal failure, don’t use in CHF
17
Q
Glyburide (mechanism)
A
Sulfonylureas
Closes K+ channel in beta cells -> depolarization -> increased Ca2+ influx -> insulin release
18
Q
Glyburide (use)
A
Sulfonylureas
DM2 (useless in DM1 bc requires some islet fx)
19
Q
Glyburide (side effect)
A
2nd gen sulfonylureas
Increased risk of hypoglycemia in renal failure
20
Q
Glimepiride (mechanism)
A
Sulfonylureas
Closes K+ channel in beta cells -> depolarization -> increased Ca2+ influx -> insulin release
21
Q
Glimepiride (use)
A
Sulfonylureas
DM2 (useless in DM1 bc requires some islet fx)
22
Q
Glimepiride (side effect)
A
2nd gen sulfonylureas
Increased risk of hypoglycemia in renal failure
23
Q
Glipizide (mechanism)
A
Sulfonylureas
Closes K+ channel in beta cells -> depolarization -> increased Ca2+ influx -> insulin release
Short acting
24
Q
Glipizide (use)
A
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
