Endocrine Uni 1 pharm Flashcards
(250 cards)
1
Q
GHRH analog
A
sermorelin
2
Q
somatostatin analog
A
octreotide
3
Q
dopamine agonists (derivatives)
A
bromocriptine, cabergoline
4
Q
recombinant HGH
A
somatrem, somatropin
5
Q
GH antagonist
A
pegvisomant
6
Q
recombinant IGF-1
A
mecasermin
7
Q
vasopressin antagonist
A
conivaptan
8
Q
somatropin moa
A
recombinant form of HGH; acts thru GH receptors -> inc IGF-1 -> promote protein deposition, enhance fat use, dec carb use, inc cartilage/bone growth
9
Q
somatropin pk
A
sub-q 6-7x/wk; continues until adequate height reached, epiphyses close, or response stops
10
Q
somatropin clinical uses
A
replace in GH deficiency: Turner’s, Prader-Willi, chronic kidney disease; idiopathic short stature; wasting in HIV infection; short bowel syndrome
11
Q
somatropin adverse effects
A
rare in kids; scoliosis, edema, gynecomastia, intracranial hypertension, myalgia, arthralgia, carpal tunnel syndrome, inc CYP450 activity
12
Q
somatropin contradictions
A
closed epiphyses, active intracranial lesion, active malignancy, proliferative diabetic retinopathy
13
Q
somatropin overview
A
replacement therapy; must be subQ - short half-life; GH agonist
14
Q
pegvisomant moa
A
blocks GH receptors - antagonist
15
Q
pegvisomant pk
A
daily subQ
16
Q
pegvisomant clinical apps
A
acromegaly for pt’s unresponsive to somatostatin analogs
17
Q
pegvisomant adverse effects
A
elevated liver enzymes; hypertension, peripheral edema, paresthesias, dizziness
18
Q
pegvisomant characteristics
A
pt’s should have yearly MRI to exclude enlarging adenoma; effective, but costly drug
19
Q
mecasermin moa
A
recombinant IGF-1 -> stimulates IGF-1 receptors
20
Q
mecasermin pk
A
subQ 2x/day, after food
21
Q
mecasermin clinical uses
A
Laron dwarfism; GH deficiency w/neutralizing antibodies; IGF-1 deficiency unresponsive to exogenous GH
22
Q
mecasermin adverse effects
A
HYPOGLYCEMIA -> inc adipose, intracranial hypertension, inc liver enzymes; tonsillar hypertrophy (less common); contraindicated in pt’s w/closed epiphyses or neoplasm
23
Q
sermorelin characteristics
A
GHRH - shortest pharmaco active analogue -> used for diagnostic purposes; orphan drug for GH def treatment; used in athletic doping, “youthful rejuvenation”
24
Q
octreotide moa
A
somatostatin receptor agonist
25
octreotide clinical uses
acromegaly; flushing and diarrhea from carcinoid tumors; carcinoid crisis; TSH-producing adenomas; diarrhea from vasoactive intestinal peptide-secreting tumors
26
octreotide pk
45x more potent than somatostatin; 80 min t1/2; subQ 3x/day or IM 1x/mo; in a biodegradable polymer
27
octreotide adverse effects
ab pain; constipation; diarrhea; nausea; vomiting; arrhythmias; bradycardia; hypoglycemia; gallstones
28
lanreotide
similar long acting drug to octreotide; mostly in Europe
29
gonadotropins moa
continuous stimulation -> inhibit LH, FSH; pulsatile stimulation -> stim LH, FSH
30
FSH characteristics
direct follicle development in women; regulates spermatogenesis in men
31
LH characteristics
works w/FSH to regulate ovarian steroidogenesis; main stimulus for testicular, androgen production
32
human chorionic gonadotropin
produced by fertilized egg, placenta, some tumors
33
GnRH
can be pulsatile -> mimic normal release - short t1/2 -> very effective; GnRH to suppress sex hormone - longer t1/2
34
gonadorelin moa
synthetic human GnRH
35
gonadorelin clinical uses
diagnose hypogonadism; stimulate ovulation (pulsatile form)
36
gonadorelin adverse effects
anaphylaxis w/multiple administrations; headache, flushing, lightheadedness
37
leuprolide, goserelin, histrelin, nafarelin, triptorelin moa
GnRH receptor agonist
38
leuprolide, goserelin, histrelin, nafarelin, triptorelin pk
IV, subQ, IM, intranasally (nafarelin); depot forms available -> dec gonadal steroid production
39
leuprolide, goserelin, histrelin, nafarelin, triptorelin clinical uses
ovarian suppression (controlled ovarian hyperstimulation); endometriosis, uterine fibroids; acute intermittent porphyria; central precocious puberty; advanced breast/prostate cancer (androgen-dependent)
40
leuprolide, goserelin, histrelin, nafarelin, triptorelin adverse effects
hot flushes, gynecomastia, osteoporosis, transient pain, sexual dysfunction; DVT (leuprolide, goserelin)
41
leuprolide, goserelin, histrelin, nafarelin, triptorelin therapeutic considerations
gonadotropin suppression not immediate -> initial flare, then longterm suppression
42
ovarian induction basic steps
1. inhibit endogenous gonadotropin production (use continuous GnRH agonist or antagonist); 2. induce follicle development (use daily injections of menotropins, FSH/analogue); 3. induce oocyte maturation (use LH/analogue - hCG injection; or GnRH agonist - less risk)
43
ovarian induction major side effects
multiple pregnancies; ovarian hyperstimulation syndrome -> enlarged ovary, ascites, hypovolemia, shock
44
ganirelix moa
GnRH receptor antagonist
45
ganirelix pk
subQ
46
ganirelix clinical uses
prevent premature LH surges during controlled ovulation hyperstimulation
47
ganirelix adverse effects
headache, nausea; ovarian hyperstimulation syndrome; ectopic pregnancy, thrombotic disorder, spontaneous abortion
48
cetrorelix moa
GnRH receptor antagonist
49
cetrorelix adverse effects
potential for anaphylaxis
50
cetrorelix clinical uses
controlled ovarian hyperstimulation; hormone sensitive breast/prostate cancer; endometriosis
51
degarelix moa
GnRH receptor antagonist
52
degarelix clinical uses
only in advanced prostate cancer
53
follitropin (rFSH), urofollitropin (FSH) moa
stimulate gonadal maturation, steroid production
54
follitropin, urofollitropin clinical uses
ovulation induction; male hypogonadotropic hypogonadism (with hCG)
55
follitropin, urofollitropin adverse effects
possible multiple fetuses; ovarian cysts, hypertrophy; URI, ARDS; embolism, thrombosis, ovarian hyperstimulation syndrome
56
human chorionic gonadotropin characteristics
LH analogs/receptor agonists; others: choriogonadotropin alfa - recombinant hCG, lutropin alfo - recombinant LH, menotropins (hMG) - FSH, LH activity
57
hCG clinical uses
initiate ovulation during controlled ovulation stimulation; ovarian follicle development for hypogonadotropic hypogonadism; hypogonadotropic hypogonadism in males
58
hCG moa
agonist of LH receptor
59
hCG pk
IM injection 2-3x/wk
60
hCG adverse effects
headache, depression, edema; ovarian hyperstimulation (women); gynecomastia (men)
61
bromocriptine characteristics
PROTOTYPE DRUG; treats hyperprolactinemia - dec prolactin, GH (at higher doses)
62
bromocriptine moa
dopamine analog; dopamine receptor agonist; affinity for D2>>D1
63
bromocriptine other clinical uses
Parkinson's (w/L-dopa); NOT to be used in women to stop lactation after stillbirth, abortion
64
bromocriptine pk
oral (only 7% makes it past liver), vaginal
65
bromocriptine adverse effects
GI disturbances; orthostative hypertension; headache, dizziness; psychiatric disturbances; vasospasm, pulmonary infiltrates (high doses); link to valvular heart disease (in high-dose parkinson's)
66
cabergoline characteristics
bromocriptine derivative w/similar effects (less GI disturbances); weekly/bi-weekly dosing
67
oxytocin moa
oxytocin receptor agonist
68
oxytocin pk
IV; can be intranasally
69
oxytocin clinical uses
induce, augment labor; control hemorrhage after delivery
70
oxytocin adverse effects
fetal distress; placental abruption; uterine rupture; fluid retention; hypotension
71
atosiban moa
oxytocin receptor antagonist
72
atosiban pk
IV
73
atosiban clinical uses
tocolysis for preterm birth
74
atosiban notables
growing concern over inc rates of infant death
75
vasopressin pharmacological effects
dec urine; dec water loss in sweat, vasoconstriction -> inc blood pressure
76
vasopressin clinical uses
treat diabetes insipidus; control bleeding from esophageal varices - V1-mediated vasoconstriction of splanchnic arterials; advanced cardiac life support in emergencies to activate V1 pressor
77
desmopressin moa
vasopression V2 receptor agonist
78
desmopressin pk
longer acting synthetic vasopressin analogue; oral, IV, subQ, INTRANASAL
79
desmopressin clinical uses
pituitary diabetes insipidus; hemophilia A; von Willebrand disease; sometimes for nocturnal bedwetting
80
desmopressin adverse effects
GI disturbances; headache; hyponatremia; allergic reactions
81
conivaptan moa
vasopressin V1a, V2 receptor antagonist
82
conivaptan pk
IV infusion
83
conivaptan clinical uses
hyponatremia in hospitalized pt's
84
conivaptan adverse effects
infusion site rxns; hypertension, orthostatic hypotension, hypokalemia, inc thirst, polyuria
85
conivaptan contraindications
P450 3A4 inhibitors i.e. ketoconazole, itraconazole, ritonavir, clarithromycin, indinavir
86
thyroid hormone replacements
levothyroxine; liothyronine
87
thioamines
propylthiouracil; methimazole
88
iodide uptake inhibitors
perchlorate; thiocyanate; pertechnetate
89
iodides
potassium iodide; radioactive iodine
90
levothyroxine (T4) characteristics
CHOICE treatment for replacement therapy in hypothyroid pt's; long t1/2; circulates bound to thyroxine-binding globulin (TBG) binding protein -> depot for tissues to make T3
91
liothyronine (T3) characteristics
active hormone; short t1/2; expensive
92
levothyroxine, liothyronine moa
activate nuclear receptors -> protein synth; act as exogenous thyroid hormone
93
levothyroxine, liothyronine pk
T4 converts to T3 in target cells (liver, kidney); T3 - 10x>potent (preferred in MYXEDEMA COMA - rapid onset w/IV)
94
levothyroxine adverse effects
hyperthyroidism symptoms; osteopenia, pseudotumor cerebri, seizure (rare); MI/CV events (inc BMR/O2 consumption)
95
levothyroxine, liothyronine contraindications
ACUTE MI; uncorrected adrenal cortical insufficiency; untreated thyrotoxicosis
96
levothyroxine, liothyronine drug interactions
cholestyramine (sequesters bile; can sequester T4/3 too); sodium polystyrene sulfonate - dec absorption of T3/4 (sequesters); rifampin, phenytoin inc met of T3/4; concomitant DM may need inc insulin dosing
97
Factors that increase TBG binding (requires increase dosing)
estrogens, pregnancy; chronic/severe liver disease; HIV
98
Factors that decrease TBG binding (requires decrease dosing)
acute liver disease; glucocorticoids; androgens; acute/chronic illness
99
iodide uptake inhibitors moa
compete w/iodide for uptake into thyroid via sodium-iodide symporter -> dec intrathyroidal iodide for thyroid synth; effectiveness is unpredictable
100
iodide uptake inhibitors clinical uses
hyperthyroidism (limited use); radiocontrast agents
101
idodide uptake inhibitors adverse effects
GI irritation; aplastic anemia?
102
radioactive iodine clinical uses
131I - only isotope used in treatment of thyrotoxicosis; same as nuclear powerplants
103
radioactive iodine moa
emits beta, gamma particles -> destroys thyroid gland tissue
104
radioactive iodine pk
t1/2 of 8 days; >99% of radioactivity gone after 56 days
105
radioactive iodine adverse effects
hypothyroidism (managed w/T4); common: sore throat
106
radioactive iodine contraindications
pregnancy, lactation
107
123I characteristics
used to measure iodine uptake, thyroid imaging; emits gamma particles; t1/2 13 hrs
108
potassium iodide, inorganic iodide characteristics
dec circulating thyroid hormone by: inhibit release, inhibit organification, dec size, vascularity of hyperplastic gland
109
potassium iodide, inorganic iodide pk
oral (high doses); acute onset; reversible, transient effect -> not for long-term
110
potassium iodide, inorganic iodide clinical uses
prep for surgical thyroidectomy; temp suppression of thyroid gland fxn
111
potassium iodide, inorganic iodide adverse effects
rare; may worsen toxic goiter symptoms
112
potassium iodide, inorganic iodide contraindications
pregnancy: fetal goiter
113
Lugol's solution
iodine and potassium iodide solution
114
Lugol's solution moa
competitively inhibits radioactive iodine absorption
115
Lugol's solution uses
as antiseptic or purify drinking water
116
thioamines - propylthiouracil and methimazole moa
inhibit thyroid peroxidase -> block iodine organification, coupling rxns; PTU inhibits conversion of T4 to T3
117
propylthiouracil and methimazole pk
oral, slow onset
118
propylthiouracil, methimazole clinical uses
hyperthyroidism, mild thyrotoxicosis; prep pt's for subtotal thyroidectomy
119
propylthiouracil and methimazole adverse effects
nausea, GI disturbances, rash, hepatitis, hypothyroidism; arthralgias (should consider stop drug use); immune-mediated agranulocytosis
120
propylthiouracil and methimazole considerations
meth preferred (less side effects); class D
121
beta-blockers for hyperthyroidism
treat the symptoms (tachy, tremor, sweating); propranolol (prototype), but esmolol is CHOICE - rapid onset, short t1/2
122
vitamin D
cholecalciferol, calcifediol, calcitriol, doxercalciferol, ERGOCALCIFEROL, paricalcitol
123
vitamin D supplements - cholecalciferol, ergocalciferol
cholecalciferol - vit D3 - animal form; ergocalciferol - vit D2 - plant form - used in food for fortification, high dose vit D injection; equally potent, efficacious
124
vitamin D moa
regulate gene transcription via vit D receptor
125
vitamin D clinical uses
oral to treat vit D def; secondary hyperparathyroidism (inc PTH from hypocalcemia); hypoparathyroidism (high doses w/ca supplements); rickets/osteomalacia; osteoporosis (w/ca)
126
vitamin D adverse effects
hypercalcemia (bypassing feedback regulation of ca); hyperphosphatemia; hypercalciuria
127
vitamin D drug interactions
aluminum (antacids); atorvastatin (vit D can dec plasma conc); can dec effectiveness of CYP 3A4 meds; thiazide antidiuretics (can cause severe hypercalcemia); some CV drugs (digoxin, diltiazem, verapamil)
128
calcitriol (D3 analogue) clinical uses
manage secondary hyperparathyroidism in pt's w/chronic kidney disease; manage hypocalcemia in pt's w/hypoparathyroidism; could cause more hypercalcemia than paricalcitol/doxercalciferol
129
doxercalciferol (D2 analogue) clinical uses
manage secondary hyperparathyroidism in pt's w/chronic kidney disease
130
paricalcitol (D3 analogue) clinical uses
analog of calcitriol; manage secondary hyperparathyroidism in pt's w/chronic kidney disease on DIALYSIS
131
calcipotriene clinical uses
calcitriol analog for psoriasis; can't put on face; flammable - smokers can burn their hand
132
bisphosphonates characteristics
most widely used anti-resorptive drugs; analogues of pyrophosphates
133
bisphosphonates pk
poor oral absorption; sit upright/stand for 30-60 mins
134
alendronate pk
oral daily/weekly
135
alendronate moa
suppresses osteoclast activity; inhibit bone resorption
136
alendronate clinical uses
osteoporosis; paget's disease; increases bone density
137
alendronate adverse effects
adynamic bone; ESOPHAGEAL IRRITATION; rare: osteonecrosis of jaw
138
other bisphosphanates
risedronate, ibandronate, pamidronate, zoledronate
139
pamidronate, zoledronate other clnical uses
osteolytic lesions of multiple myeloma (overexpression of RANKL), breast cancer; hypercalcemia w/malignancy
140
pamidronate, zoledronate pk
IV only; fast
141
pamidronate, zoledronate adverse effects
common: osteocrenosis of jaw
142
RANKL antagonists - denosumab moa
monoclonal antibody that targets RANKL; dec bone resorption (block osteoclast activation)
143
denosumab clinical uses
osteoporosis prevention/treatment
144
denosumab adverse effects
jaw osteonecrosis in cancer pt's; hypocalcemia
145
raloxifene pk
oral
146
raloxifene moa
estrogen agonist effect in bone; estrogen antagonist effects in breast, endometrium
147
raloxifene clinical uses
osteoporosis in postmenopausal women; BONUS: dec breast cancer incidence
148
raloxifene adverse effects
hot flushes; thromboembolism
149
raloxifene contraindications
women w/history/presence of thromboembolism
150
teriparatide pk
subQ
151
teriparatide moa
PTH analogue; inc bone formation by osteoblasts
152
teriparatide clinical uses
severe osteoporosis
153
teriparatide adverse effects
hypercalcemia; hypercalciuria; osteosclerosis, osteosarcoma; leg cramps
154
teriparatide contraindications
open epiphyses; prior radiation therapy; paget's disease; hypercalcemia
155
calcitonin pk
subQ (fast), intranasal
156
calcitonin moa
inhibit bone resorption by osteoclasts thru calcitonin receptors; inhibits ca absorption in intestines, reabsorption in kidneys
157
calcitonin clinical uses
postmenopausal osteoporosis (not 1st line); hypercalcemia
158
calcitonin adverse effects
rhinitis w/nasal spray; flushing, nausea, diarrhea
159
cinacalcet pk
oral
160
cinacalcet moa
inc sensitivity of calcium-sensing receptor to ca in parathyroid -> dec PTH secretion
161
cinacalcet clinical uses
chronic kidney disease/secondary hyperparathyroidism; hypercalcemia w/parathyroid carcinoma
162
cinacalcet adverse effects
nausea, vomiting, dizziness; hypocalcemia; adynamic bone
163
oral phosphate binders - sevelamer moa
dec GI absorption of dietary inorganic phosphate; dec serum cholesterol - binds to bile acids
164
sevelamer clinical uses
chronic kidney disease; hypoparathyroidism; vit D intoxication; tumoral calcinosis; hyperphosphatemia-hyperostosis syndrome (rare)
165
sevelamer adverse effects
constipation; thrombosis; hypertension
166
other oral phosphate binders
aluminum hydroxide (rarely used); calcium carbonate/calcium acetate - similar to sevelamer
167
calcium moa
essential for bone mineralization
168
calcium preparations
calcium gluconate (IV), calcium carbonate (oral); calcium citrate-malate (oral)
169
calcium clinical uses
secondary hyperparathyroidism; hypoparathyroidism; rickets; osteomalacia
170
calcium adverse effects
constipation, hypercalciuria, hypercalcemia, renal calculi
171
calcium considerations
take with food
172
inorganic phosphate moa
essential for bone mineralization
173
inorganic phosphate clinical uses
severe hypophosphatemia
174
inorganic phosphate adverse effects
diarrhea
175
inorganic phosphate preparations
potassium phosphate - preferred over sodium phosphate to minimize renal excretion of phosphate and/or to correct coexisting hypokalemia
176
estrogens
ethinyl estradiol; mestranol; estrogen esters
177
anti-estrogens
TAMOXIFEN; toremifene; clomiphene; raloxifene; FULVESTRANT
178
progestins
norgestrel; levonorgestrel; norethindrone; norethindrone acetate; ethynodiol; etonogestrel; norelgestromin; norgestimate; gestodene; desogestrel; drospirenone; noregestimate; medroxyprogesterone acetate (depo-provera)
179
androgens
DANAZOL; testosterone; fluoxymesterone; methyltestosterone; anabolic steroids (oxandrolone, nandrolone decanoate)
180
anti-androgens
FINASTERIDE; dutasteride; flutamide; biclumatide; nilutamide; SPIRONOLACTONE
181
estrogens characteristics
synthetic undergo less 1st pass than natural
182
estrogens moa
activate estrogen receptors
183
estrogens considerations
women w/uterus: must give w/progestin to prevent endometrial cancer; w/o uterus: can use for hormone therapy
184
estrogens clinical uses
contraception; hormone therapy - postmenopausal (inc breast cancer, CV events risk), or premature ovarian failure; hypogonadism in young females (estradiol cypionate - long-acting); prevention of bone loss, osteoporosis
185
mestranol
prodrug converted to ethinyl estradiol
186
estrogens adverse effects
minor: breakthrough bleeding, nausea, breast tenderness; serious: THROMBOEMBOLISM, GALLBLADDER DISEASE, hypertriglyceridemia, migraine headache, hypertension, DEPRESSION; in postmenopause - breast cancer, endometrial hyperplasia
187
estrogens drug interactions
combination with CYP450 inducer can lead to breakthrough bleedings, reduced contraceptive efficacy; RIFAMPIN (tx TB) - interact w/OCs; other antibiotics - maybe
188
progestins moa
activate progesterone receptors
189
progestins clinical uses
contraception (w or w/o estrogen); hormone deficiency; promote/maintain pregnancy; dysfunctional uterine bleeding; dysmenorrhea, endometriosis
190
progestins adverse effects
weight gain; reversible dec in BMD w/high doses; inc BP, dec HDL
191
progesterone
major progestin in humans; not used - rapidly met.
192
low dose progestin only pills (POP)
norplant, mirena; inhibit ovulation in 50% of cycles; thicken cervical mucus - reduce sperm viability, penetration
193
medium dose progestin only pills
nexplanon; inhibit ovulation in 97-99% of cycles; cervical mucus thickens
194
high dose progestin only pills
depo-provera; inhibit follicular development, ovulation; thicken cervical mucus
195
selective estrogen receptor modulators effects
mixed estrogen effects - agonist, partial agonist, antagonist in diff tissues
196
tamoxifen moa
estrogen antagonist in breast, CNS; estrogen agonist in liver, bone
197
tamoxifen clinical use
prevent, adjuvant treatment of hormone-responsive breast cancer
198
tamoxifen adverse effects
hot flushes, thromboembolism, endometrial hyperplasia; inc incidence of endometrial cancer
199
tamoxifen BONUS
inc BMD in postmenopause
200
toremifene
similar to tamoxifen
201
raloxifene moa
SERM; antagonist in breast, cns, endometrium
202
raloxifene clinical uses
osteoporosis, prevent breast cancer in postmenopause
203
clomiphene moa
SERM; antagonist in pituitary -> inc gonadotropin secretion
204
clomiphene clinical uses
ovulation induction
205
ormeloxifene characteristics
non-hormonal, non-steroidal oral contraceptive
206
ormeloxifene moa
SERM; agonist in bones, antagonist in uterus/breast; only in India
207
ormeloxifene adverse effects
uterine prolapse, urinary incontinence
208
lasofoxifene moa
SERM; agonist in bones; antagonist in breast/uterus; not marketed/FDA approved in US
209
selective estrogen down regulator (SERD) - fulvestrant pk
monthly IM
210
fulvestrant moa
estrogen receptor antagonist in all tissues
211
fulvestrant clinical uses
2nd-line treatment for hormone-responsive breast cancer that resists 1st line anti-estrogen therapy
212
fulvestrant adverse effects
hot flushes, headache, INJECTION SITE RXN; nausea, asthenia, pain; expensive
213
aromatase inhibitors characteristics
can inhibit extra-ovarian estrogen production (GnRH agonists cannot)
214
aromatase inhibitors moa
block aromatase enzyme - competitive (anastrozole, letrozole) or covalently bind to aromatase (exemestane, formestane)
215
aromatase inhibitors clinical apps
adjuvant treatment of hormone responsive breast cancer
216
aromatase inhibitors adverse effects
hot flushes, musculoskeletal disorders, reduced BMD, depression, dyspnea, arthralgia, bone pain, peripheral edema; serious adverse effects: OSTEOPOROTIC FRACTURES, thrombophlebitis, hypercholesterolemia, profuse vaginal bleeding
217
aromatase inhibitors considerations
may be more effective than SERMs; substantial risk of osteoporotic fractures
218
danazol moa
weak cytochrome P450 inhibitor; partial agonist of progestin, androgen receptors; synthetic derivative of 17-ethinyltestosterone; dec FSH/LH
219
danazol clinical uses
fibrocystic breast disease; endometriosis - induces anovulation, amenorrhea, endometrial atrophy (dec LH/FSH), high androgen, low estrogen
220
danazol adverse effects
acne, hirsutism, weight gain, irreversible virilization (clitoromegaly, voice changes), menstrual irregularities, dec breast size, hepatotoxicity, thromboembolism
221
danazol drug interactions
CYP450
222
anti-progestin - mifepristone moa
progestin, glucocorticoid receptor antagonist
223
mifepristone clinical uses
combo w/prostaglandin (misoprostol) for abortion
224
mifepristone adverse effects
GI disturbances, vaginal bleeding, atypical infection
225
androgens - testosterone pk
transdermal, buccal, subQ
226
testosterone moa
androgen receptor agonist
227
testosterone clinical uses
male hypogonadism; wasting syndrome (drug helps gain weight)
228
testosterone adverse effects
virilization in females (topical application users must use caution); gynecomastia (high doses); testicular shrinkage, infertility; headache
229
oral androgens
fluoxymesterone, methyltestosterone
230
testosterone esters
testosterone cypionate - long-acting, parenteral
231
anabolic steroids
oxandrolone, nandrolone decanoate -> liver toxicities
232
anti-androgens - 5alpha-reductase inhibitors - finasteride moa
inhibits conversion of testosterone to dihydrotesterone
233
finasteride clinical uses
benign prostatic hyperplasia; male pattern hair loss
234
finasteride adverse effects
rare: gynecomastia, impotence
235
dutasteride
similar to finasteride
236
flutamide moa
competitive inhibitor of androgen receptor
237
flutamide clinical uses
advanced prostate cancer
238
flutamide adverse effects
gynceomastia, hot flashes, impotence, hepatotoxicity
239
bicalutamide, nilutamide
similar to flutamide w/lower hepatotoxicity
240
spironolactone moa
mineralocorticoid receptor antagonist; androgen receptor antagonist
241
spironolactone clinical uses
k-sparing diuretic; others: hirsutism, acne, hypertension, hypokalemia, primary aldosteronism
242
spironolactone adverse effects
gynecomastia, dyspepsia, lethargy, abnormal menstruation, impotence, rash
243
pharmacotherapy for dysmenorrhea
CHOICE: NSAIDs; combined oral contraceptives; depot medroxyprogesterone; levonorgestrel IUD
244
pharmacotherapy for menorrhagia
combined oral contraceptives; levonorgestrel IUD; NSAIDs; tranexamic acid (used in surgeries)
245
pharmacotherapy for endometriosis
suppress ovarian fxn, endometrial tissue growth -> oral contraceptives (1st line) - progestins, GnRH agonists, danazol; NSAIDs for mild discomfort
246
pharmacotherapy for polycystic ovarian syndrome (PCOS)
1st line - combined oral contraceptives - alone or w/anti-androgens -> normalize dysfunctional uterine bleeding
247
treatment of hirsutism, acne in PCOS
spironolactone, finasteride, flutamide, GnRH agonists
248
treatment of infertility
clomiphene citrate (ovulation inducer); metformin
249
pharmacotherapies for uterine leiomyomas (fibroids/myomas)
GnRH agonists - most effective - limitations: uterus grows back to size after stopping therapy; levonorgestrel-releasing intrauterine device - reduce uterine vol, bleeding, inc hematocrit; mifepristone w/anti-progesterone if progesterone-responsive
250
postpartum contraception
progestin contraceptive preferred - POP, depot medroxyprogesterone acetate (injection/implants), levonorgestrel IUD; combined oral contraceptives may suppress lactation initially -> not recommended for 3wks, 6wks if thromboembolism risk
