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Endocrine Uni 1 pharm Flashcards

1
Q

GHRH analog

A

sermorelin

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2
Q

somatostatin analog

A

octreotide

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3
Q

dopamine agonists (derivatives)

A

bromocriptine, cabergoline

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4
Q

recombinant HGH

A

somatrem, somatropin

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5
Q

GH antagonist

A

pegvisomant

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6
Q

recombinant IGF-1

A

mecasermin

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7
Q

vasopressin antagonist

A

conivaptan

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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

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9
Q

somatropin pk

A

sub-q 6-7x/wk; continues until adequate height reached, epiphyses close, or response stops

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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

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11
Q

somatropin adverse effects

A

rare in kids; scoliosis, edema, gynecomastia, intracranial hypertension, myalgia, arthralgia, carpal tunnel syndrome, inc CYP450 activity

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12
Q

somatropin contradictions

A

closed epiphyses, active intracranial lesion, active malignancy, proliferative diabetic retinopathy

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13
Q

somatropin overview

A

replacement therapy; must be subQ - short half-life; GH agonist

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14
Q

pegvisomant moa

A

blocks GH receptors - antagonist

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15
Q

pegvisomant pk

A

daily subQ

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16
Q

pegvisomant clinical apps

A

acromegaly for pt’s unresponsive to somatostatin analogs

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17
Q

pegvisomant adverse effects

A

elevated liver enzymes; hypertension, peripheral edema, paresthesias, dizziness

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18
Q

pegvisomant characteristics

A

pt’s should have yearly MRI to exclude enlarging adenoma; effective, but costly drug

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19
Q

mecasermin moa

A

recombinant IGF-1 -> stimulates IGF-1 receptors

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20
Q

mecasermin pk

A

subQ 2x/day, after food

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21
Q

mecasermin clinical uses

A

Laron dwarfism; GH deficiency w/neutralizing antibodies; IGF-1 deficiency unresponsive to exogenous GH

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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

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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”

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24
Q

octreotide moa

A

somatostatin receptor agonist

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25
Q

octreotide clinical uses

A

acromegaly; flushing and diarrhea from carcinoid tumors; carcinoid crisis; TSH-producing adenomas; diarrhea from vasoactive intestinal peptide-secreting tumors

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26
Q

octreotide pk

A

45x more potent than somatostatin; 80 min t1/2; subQ 3x/day or IM 1x/mo; in a biodegradable polymer

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27
Q

octreotide adverse effects

A

ab pain; constipation; diarrhea; nausea; vomiting; arrhythmias; bradycardia; hypoglycemia; gallstones

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28
Q

lanreotide

A

similar long acting drug to octreotide; mostly in Europe

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29
Q

gonadotropins moa

A

continuous stimulation -> inhibit LH, FSH; pulsatile stimulation -> stim LH, FSH

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30
Q

FSH characteristics

A

direct follicle development in women; regulates spermatogenesis in men

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31
Q

LH characteristics

A

works w/FSH to regulate ovarian steroidogenesis; main stimulus for testicular, androgen production

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32
Q

human chorionic gonadotropin

A

produced by fertilized egg, placenta, some tumors

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33
Q

GnRH

A

can be pulsatile -> mimic normal release - short t1/2 -> very effective; GnRH to suppress sex hormone - longer t1/2

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34
Q

gonadorelin moa

A

synthetic human GnRH

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35
Q

gonadorelin clinical uses

A

diagnose hypogonadism; stimulate ovulation (pulsatile form)

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36
Q

gonadorelin adverse effects

A

anaphylaxis w/multiple administrations; headache, flushing, lightheadedness

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37
Q

leuprolide, goserelin, histrelin, nafarelin, triptorelin moa

A

GnRH receptor agonist

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38
Q

leuprolide, goserelin, histrelin, nafarelin, triptorelin pk

A

IV, subQ, IM, intranasally (nafarelin); depot forms available -> dec gonadal steroid production

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39
Q

leuprolide, goserelin, histrelin, nafarelin, triptorelin clinical uses

A

ovarian suppression (controlled ovarian hyperstimulation); endometriosis, uterine fibroids; acute intermittent porphyria; central precocious puberty; advanced breast/prostate cancer (androgen-dependent)

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40
Q

leuprolide, goserelin, histrelin, nafarelin, triptorelin adverse effects

A

hot flushes, gynecomastia, osteoporosis, transient pain, sexual dysfunction; DVT (leuprolide, goserelin)

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41
Q

leuprolide, goserelin, histrelin, nafarelin, triptorelin therapeutic considerations

A

gonadotropin suppression not immediate -> initial flare, then longterm suppression

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42
Q

ovarian induction basic steps

A
  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)
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43
Q

ovarian induction major side effects

A

multiple pregnancies; ovarian hyperstimulation syndrome -> enlarged ovary, ascites, hypovolemia, shock

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44
Q

ganirelix moa

A

GnRH receptor antagonist

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45
Q

ganirelix pk

A

subQ

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46
Q

ganirelix clinical uses

A

prevent premature LH surges during controlled ovulation hyperstimulation

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47
Q

ganirelix adverse effects

A

headache, nausea; ovarian hyperstimulation syndrome; ectopic pregnancy, thrombotic disorder, spontaneous abortion

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48
Q

cetrorelix moa

A

GnRH receptor antagonist

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49
Q

cetrorelix adverse effects

A

potential for anaphylaxis

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50
Q

cetrorelix clinical uses

A

controlled ovarian hyperstimulation; hormone sensitive breast/prostate cancer; endometriosis

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51
Q

degarelix moa

A

GnRH receptor antagonist

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52
Q

degarelix clinical uses

A

only in advanced prostate cancer

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53
Q

follitropin (rFSH), urofollitropin (FSH) moa

A

stimulate gonadal maturation, steroid production

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54
Q

follitropin, urofollitropin clinical uses

A

ovulation induction; male hypogonadotropic hypogonadism (with hCG)

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55
Q

follitropin, urofollitropin adverse effects

A

possible multiple fetuses; ovarian cysts, hypertrophy; URI, ARDS; embolism, thrombosis, ovarian hyperstimulation syndrome

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56
Q

human chorionic gonadotropin characteristics

A

LH analogs/receptor agonists; others: choriogonadotropin alfa - recombinant hCG, lutropin alfo - recombinant LH, menotropins (hMG) - FSH, LH activity

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57
Q

hCG clinical uses

A

initiate ovulation during controlled ovulation stimulation; ovarian follicle development for hypogonadotropic hypogonadism; hypogonadotropic hypogonadism in males

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58
Q

hCG moa

A

agonist of LH receptor

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59
Q

hCG pk

A

IM injection 2-3x/wk

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60
Q

hCG adverse effects

A

headache, depression, edema; ovarian hyperstimulation (women); gynecomastia (men)

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61
Q

bromocriptine characteristics

A

PROTOTYPE DRUG; treats hyperprolactinemia - dec prolactin, GH (at higher doses)

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62
Q

bromocriptine moa

A

dopamine analog; dopamine receptor agonist; affinity for D2»D1

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63
Q

bromocriptine other clinical uses

A

Parkinson’s (w/L-dopa); NOT to be used in women to stop lactation after stillbirth, abortion

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64
Q

bromocriptine pk

A

oral (only 7% makes it past liver), vaginal

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65
Q

bromocriptine adverse effects

A

GI disturbances; orthostative hypertension; headache, dizziness; psychiatric disturbances; vasospasm, pulmonary infiltrates (high doses); link to valvular heart disease (in high-dose parkinson’s)

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66
Q

cabergoline characteristics

A

bromocriptine derivative w/similar effects (less GI disturbances); weekly/bi-weekly dosing

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67
Q

oxytocin moa

A

oxytocin receptor agonist

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68
Q

oxytocin pk

A

IV; can be intranasally

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69
Q

oxytocin clinical uses

A

induce, augment labor; control hemorrhage after delivery

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70
Q

oxytocin adverse effects

A

fetal distress; placental abruption; uterine rupture; fluid retention; hypotension

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71
Q

atosiban moa

A

oxytocin receptor antagonist

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72
Q

atosiban pk

A

IV

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73
Q

atosiban clinical uses

A

tocolysis for preterm birth

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74
Q

atosiban notables

A

growing concern over inc rates of infant death

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75
Q

vasopressin pharmacological effects

A

dec urine; dec water loss in sweat, vasoconstriction -> inc blood pressure

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76
Q

vasopressin clinical uses

A

treat diabetes insipidus; control bleeding from esophageal varices - V1-mediated vasoconstriction of splanchnic arterials; advanced cardiac life support in emergencies to activate V1 pressor

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77
Q

desmopressin moa

A

vasopression V2 receptor agonist

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78
Q

desmopressin pk

A

longer acting synthetic vasopressin analogue; oral, IV, subQ, INTRANASAL

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79
Q

desmopressin clinical uses

A

pituitary diabetes insipidus; hemophilia A; von Willebrand disease; sometimes for nocturnal bedwetting

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80
Q

desmopressin adverse effects

A

GI disturbances; headache; hyponatremia; allergic reactions

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81
Q

conivaptan moa

A

vasopressin V1a, V2 receptor antagonist

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82
Q

conivaptan pk

A

IV infusion

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83
Q

conivaptan clinical uses

A

hyponatremia in hospitalized pt’s

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84
Q

conivaptan adverse effects

A

infusion site rxns; hypertension, orthostatic hypotension, hypokalemia, inc thirst, polyuria

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85
Q

conivaptan contraindications

A

P450 3A4 inhibitors i.e. ketoconazole, itraconazole, ritonavir, clarithromycin, indinavir

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86
Q

thyroid hormone replacements

A

levothyroxine; liothyronine

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87
Q

thioamines

A

propylthiouracil; methimazole

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88
Q

iodide uptake inhibitors

A

perchlorate; thiocyanate; pertechnetate

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89
Q

iodides

A

potassium iodide; radioactive iodine

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90
Q

levothyroxine (T4) characteristics

A

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

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91
Q

liothyronine (T3) characteristics

A

active hormone; short t1/2; expensive

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92
Q

levothyroxine, liothyronine moa

A

activate nuclear receptors -> protein synth; act as exogenous thyroid hormone

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93
Q

levothyroxine, liothyronine pk

A

T4 converts to T3 in target cells (liver, kidney); T3 - 10x>potent (preferred in MYXEDEMA COMA - rapid onset w/IV)

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94
Q

levothyroxine adverse effects

A

hyperthyroidism symptoms; osteopenia, pseudotumor cerebri, seizure (rare); MI/CV events (inc BMR/O2 consumption)

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95
Q

levothyroxine, liothyronine contraindications

A

ACUTE MI; uncorrected adrenal cortical insufficiency; untreated thyrotoxicosis

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96
Q

levothyroxine, liothyronine drug interactions

A

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

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97
Q

Factors that increase TBG binding (requires increase dosing)

A

estrogens, pregnancy; chronic/severe liver disease; HIV

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98
Q

Factors that decrease TBG binding (requires decrease dosing)

A

acute liver disease; glucocorticoids; androgens; acute/chronic illness

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99
Q

iodide uptake inhibitors moa

A

compete w/iodide for uptake into thyroid via sodium-iodide symporter -> dec intrathyroidal iodide for thyroid synth; effectiveness is unpredictable

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100
Q

iodide uptake inhibitors clinical uses

A

hyperthyroidism (limited use); radiocontrast agents

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101
Q

idodide uptake inhibitors adverse effects

A

GI irritation; aplastic anemia?

102
Q

radioactive iodine clinical uses

A

131I - only isotope used in treatment of thyrotoxicosis; same as nuclear powerplants

103
Q

radioactive iodine moa

A

emits beta, gamma particles -> destroys thyroid gland tissue

104
Q

radioactive iodine pk

A

t1/2 of 8 days; >99% of radioactivity gone after 56 days

105
Q

radioactive iodine adverse effects

A

hypothyroidism (managed w/T4); common: sore throat

106
Q

radioactive iodine contraindications

A

pregnancy, lactation

107
Q

123I characteristics

A

used to measure iodine uptake, thyroid imaging; emits gamma particles; t1/2 13 hrs

108
Q

potassium iodide, inorganic iodide characteristics

A

dec circulating thyroid hormone by: inhibit release, inhibit organification, dec size, vascularity of hyperplastic gland

109
Q

potassium iodide, inorganic iodide pk

A

oral (high doses); acute onset; reversible, transient effect -> not for long-term

110
Q

potassium iodide, inorganic iodide clinical uses

A

prep for surgical thyroidectomy; temp suppression of thyroid gland fxn

111
Q

potassium iodide, inorganic iodide adverse effects

A

rare; may worsen toxic goiter symptoms

112
Q

potassium iodide, inorganic iodide contraindications

A

pregnancy: fetal goiter

113
Q

Lugol’s solution

A

iodine and potassium iodide solution

114
Q

Lugol’s solution moa

A

competitively inhibits radioactive iodine absorption

115
Q

Lugol’s solution uses

A

as antiseptic or purify drinking water

116
Q

thioamines - propylthiouracil and methimazole moa

A

inhibit thyroid peroxidase -> block iodine organification, coupling rxns; PTU inhibits conversion of T4 to T3

117
Q

propylthiouracil and methimazole pk

A

oral, slow onset

118
Q

propylthiouracil, methimazole clinical uses

A

hyperthyroidism, mild thyrotoxicosis; prep pt’s for subtotal thyroidectomy

119
Q

propylthiouracil and methimazole adverse effects

A

nausea, GI disturbances, rash, hepatitis, hypothyroidism; arthralgias (should consider stop drug use); immune-mediated agranulocytosis

120
Q

propylthiouracil and methimazole considerations

A

meth preferred (less side effects); class D

121
Q

beta-blockers for hyperthyroidism

A

treat the symptoms (tachy, tremor, sweating); propranolol (prototype), but esmolol is CHOICE - rapid onset, short t1/2

122
Q

vitamin D

A

cholecalciferol, calcifediol, calcitriol, doxercalciferol, ERGOCALCIFEROL, paricalcitol

123
Q

vitamin D supplements - cholecalciferol, ergocalciferol

A

cholecalciferol - vit D3 - animal form; ergocalciferol - vit D2 - plant form - used in food for fortification, high dose vit D injection; equally potent, efficacious

124
Q

vitamin D moa

A

regulate gene transcription via vit D receptor

125
Q

vitamin D clinical uses

A

oral to treat vit D def; secondary hyperparathyroidism (inc PTH from hypocalcemia); hypoparathyroidism (high doses w/ca supplements); rickets/osteomalacia; osteoporosis (w/ca)

126
Q

vitamin D adverse effects

A

hypercalcemia (bypassing feedback regulation of ca); hyperphosphatemia; hypercalciuria

127
Q

vitamin D drug interactions

A

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
Q

calcitriol (D3 analogue) clinical uses

A

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
Q

doxercalciferol (D2 analogue) clinical uses

A

manage secondary hyperparathyroidism in pt’s w/chronic kidney disease

130
Q

paricalcitol (D3 analogue) clinical uses

A

analog of calcitriol; manage secondary hyperparathyroidism in pt’s w/chronic kidney disease on DIALYSIS

131
Q

calcipotriene clinical uses

A

calcitriol analog for psoriasis; can’t put on face; flammable - smokers can burn their hand

132
Q

bisphosphonates characteristics

A

most widely used anti-resorptive drugs; analogues of pyrophosphates

133
Q

bisphosphonates pk

A

poor oral absorption; sit upright/stand for 30-60 mins

134
Q

alendronate pk

A

oral daily/weekly

135
Q

alendronate moa

A

suppresses osteoclast activity; inhibit bone resorption

136
Q

alendronate clinical uses

A

osteoporosis; paget’s disease; increases bone density

137
Q

alendronate adverse effects

A

adynamic bone; ESOPHAGEAL IRRITATION; rare: osteonecrosis of jaw

138
Q

other bisphosphanates

A

risedronate, ibandronate, pamidronate, zoledronate

139
Q

pamidronate, zoledronate other clnical uses

A

osteolytic lesions of multiple myeloma (overexpression of RANKL), breast cancer; hypercalcemia w/malignancy

140
Q

pamidronate, zoledronate pk

A

IV only; fast

141
Q

pamidronate, zoledronate adverse effects

A

common: osteocrenosis of jaw

142
Q

RANKL antagonists - denosumab moa

A

monoclonal antibody that targets RANKL; dec bone resorption (block osteoclast activation)

143
Q

denosumab clinical uses

A

osteoporosis prevention/treatment

144
Q

denosumab adverse effects

A

jaw osteonecrosis in cancer pt’s; hypocalcemia

145
Q

raloxifene pk

146
Q

raloxifene moa

A

estrogen agonist effect in bone; estrogen antagonist effects in breast, endometrium

147
Q

raloxifene clinical uses

A

osteoporosis in postmenopausal women; BONUS: dec breast cancer incidence

148
Q

raloxifene adverse effects

A

hot flushes; thromboembolism

149
Q

raloxifene contraindications

A

women w/history/presence of thromboembolism

150
Q

teriparatide pk

151
Q

teriparatide moa

A

PTH analogue; inc bone formation by osteoblasts

152
Q

teriparatide clinical uses

A

severe osteoporosis

153
Q

teriparatide adverse effects

A

hypercalcemia; hypercalciuria; osteosclerosis, osteosarcoma; leg cramps

154
Q

teriparatide contraindications

A

open epiphyses; prior radiation therapy; paget’s disease; hypercalcemia

155
Q

calcitonin pk

A

subQ (fast), intranasal

156
Q

calcitonin moa

A

inhibit bone resorption by osteoclasts thru calcitonin receptors; inhibits ca absorption in intestines, reabsorption in kidneys

157
Q

calcitonin clinical uses

A

postmenopausal osteoporosis (not 1st line); hypercalcemia

158
Q

calcitonin adverse effects

A

rhinitis w/nasal spray; flushing, nausea, diarrhea

159
Q

cinacalcet pk

160
Q

cinacalcet moa

A

inc sensitivity of calcium-sensing receptor to ca in parathyroid -> dec PTH secretion

161
Q

cinacalcet clinical uses

A

chronic kidney disease/secondary hyperparathyroidism; hypercalcemia w/parathyroid carcinoma

162
Q

cinacalcet adverse effects

A

nausea, vomiting, dizziness; hypocalcemia; adynamic bone

163
Q

oral phosphate binders - sevelamer moa

A

dec GI absorption of dietary inorganic phosphate; dec serum cholesterol - binds to bile acids

164
Q

sevelamer clinical uses

A

chronic kidney disease; hypoparathyroidism; vit D intoxication; tumoral calcinosis; hyperphosphatemia-hyperostosis syndrome (rare)

165
Q

sevelamer adverse effects

A

constipation; thrombosis; hypertension

166
Q

other oral phosphate binders

A

aluminum hydroxide (rarely used); calcium carbonate/calcium acetate - similar to sevelamer

167
Q

calcium moa

A

essential for bone mineralization

168
Q

calcium preparations

A

calcium gluconate (IV), calcium carbonate (oral); calcium citrate-malate (oral)

169
Q

calcium clinical uses

A

secondary hyperparathyroidism; hypoparathyroidism; rickets; osteomalacia

170
Q

calcium adverse effects

A

constipation, hypercalciuria, hypercalcemia, renal calculi

171
Q

calcium considerations

A

take with food

172
Q

inorganic phosphate moa

A

essential for bone mineralization

173
Q

inorganic phosphate clinical uses

A

severe hypophosphatemia

174
Q

inorganic phosphate adverse effects

175
Q

inorganic phosphate preparations

A

potassium phosphate - preferred over sodium phosphate to minimize renal excretion of phosphate and/or to correct coexisting hypokalemia

176
Q

estrogens

A

ethinyl estradiol; mestranol; estrogen esters

177
Q

anti-estrogens

A

TAMOXIFEN; toremifene; clomiphene; raloxifene; FULVESTRANT

178
Q

progestins

A

norgestrel; levonorgestrel; norethindrone; norethindrone acetate; ethynodiol; etonogestrel; norelgestromin; norgestimate; gestodene; desogestrel; drospirenone; noregestimate; medroxyprogesterone acetate (depo-provera)

179
Q

androgens

A

DANAZOL; testosterone; fluoxymesterone; methyltestosterone; anabolic steroids (oxandrolone, nandrolone decanoate)

180
Q

anti-androgens

A

FINASTERIDE; dutasteride; flutamide; biclumatide; nilutamide; SPIRONOLACTONE

181
Q

estrogens characteristics

A

synthetic undergo less 1st pass than natural

182
Q

estrogens moa

A

activate estrogen receptors

183
Q

estrogens considerations

A

women w/uterus: must give w/progestin to prevent endometrial cancer; w/o uterus: can use for hormone therapy

184
Q

estrogens clinical uses

A

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
Q

mestranol

A

prodrug converted to ethinyl estradiol

186
Q

estrogens adverse effects

A

minor: breakthrough bleeding, nausea, breast tenderness; serious: THROMBOEMBOLISM, GALLBLADDER DISEASE, hypertriglyceridemia, migraine headache, hypertension, DEPRESSION; in postmenopause - breast cancer, endometrial hyperplasia

187
Q

estrogens drug interactions

A

combination with CYP450 inducer can lead to breakthrough bleedings, reduced contraceptive efficacy; RIFAMPIN (tx TB) - interact w/OCs; other antibiotics - maybe

188
Q

progestins moa

A

activate progesterone receptors

189
Q

progestins clinical uses

A

contraception (w or w/o estrogen); hormone deficiency; promote/maintain pregnancy; dysfunctional uterine bleeding; dysmenorrhea, endometriosis

190
Q

progestins adverse effects

A

weight gain; reversible dec in BMD w/high doses; inc BP, dec HDL

191
Q

progesterone

A

major progestin in humans; not used - rapidly met.

192
Q

low dose progestin only pills (POP)

A

norplant, mirena; inhibit ovulation in 50% of cycles; thicken cervical mucus - reduce sperm viability, penetration

193
Q

medium dose progestin only pills

A

nexplanon; inhibit ovulation in 97-99% of cycles; cervical mucus thickens

194
Q

high dose progestin only pills

A

depo-provera; inhibit follicular development, ovulation; thicken cervical mucus

195
Q

selective estrogen receptor modulators effects

A

mixed estrogen effects - agonist, partial agonist, antagonist in diff tissues

196
Q

tamoxifen moa

A

estrogen antagonist in breast, CNS; estrogen agonist in liver, bone

197
Q

tamoxifen clinical use

A

prevent, adjuvant treatment of hormone-responsive breast cancer

198
Q

tamoxifen adverse effects

A

hot flushes, thromboembolism, endometrial hyperplasia; inc incidence of endometrial cancer

199
Q

tamoxifen BONUS

A

inc BMD in postmenopause

200
Q

toremifene

A

similar to tamoxifen

201
Q

raloxifene moa

A

SERM; antagonist in breast, cns, endometrium

202
Q

raloxifene clinical uses

A

osteoporosis, prevent breast cancer in postmenopause

203
Q

clomiphene moa

A

SERM; antagonist in pituitary -> inc gonadotropin secretion

204
Q

clomiphene clinical uses

A

ovulation induction

205
Q

ormeloxifene characteristics

A

non-hormonal, non-steroidal oral contraceptive

206
Q

ormeloxifene moa

A

SERM; agonist in bones, antagonist in uterus/breast; only in India

207
Q

ormeloxifene adverse effects

A

uterine prolapse, urinary incontinence

208
Q

lasofoxifene moa

A

SERM; agonist in bones; antagonist in breast/uterus; not marketed/FDA approved in US

209
Q

selective estrogen down regulator (SERD) - fulvestrant pk

A

monthly IM

210
Q

fulvestrant moa

A

estrogen receptor antagonist in all tissues

211
Q

fulvestrant clinical uses

A

2nd-line treatment for hormone-responsive breast cancer that resists 1st line anti-estrogen therapy

212
Q

fulvestrant adverse effects

A

hot flushes, headache, INJECTION SITE RXN; nausea, asthenia, pain; expensive

213
Q

aromatase inhibitors characteristics

A

can inhibit extra-ovarian estrogen production (GnRH agonists cannot)

214
Q

aromatase inhibitors moa

A

block aromatase enzyme - competitive (anastrozole, letrozole) or covalently bind to aromatase (exemestane, formestane)

215
Q

aromatase inhibitors clinical apps

A

adjuvant treatment of hormone responsive breast cancer

216
Q

aromatase inhibitors adverse effects

A

hot flushes, musculoskeletal disorders, reduced BMD, depression, dyspnea, arthralgia, bone pain, peripheral edema; serious adverse effects: OSTEOPOROTIC FRACTURES, thrombophlebitis, hypercholesterolemia, profuse vaginal bleeding

217
Q

aromatase inhibitors considerations

A

may be more effective than SERMs; substantial risk of osteoporotic fractures

218
Q

danazol moa

A

weak cytochrome P450 inhibitor; partial agonist of progestin, androgen receptors; synthetic derivative of 17-ethinyltestosterone; dec FSH/LH

219
Q

danazol clinical uses

A

fibrocystic breast disease; endometriosis - induces anovulation, amenorrhea, endometrial atrophy (dec LH/FSH), high androgen, low estrogen

220
Q

danazol adverse effects

A

acne, hirsutism, weight gain, irreversible virilization (clitoromegaly, voice changes), menstrual irregularities, dec breast size, hepatotoxicity, thromboembolism

221
Q

danazol drug interactions

222
Q

anti-progestin - mifepristone moa

A

progestin, glucocorticoid receptor antagonist

223
Q

mifepristone clinical uses

A

combo w/prostaglandin (misoprostol) for abortion

224
Q

mifepristone adverse effects

A

GI disturbances, vaginal bleeding, atypical infection

225
Q

androgens - testosterone pk

A

transdermal, buccal, subQ

226
Q

testosterone moa

A

androgen receptor agonist

227
Q

testosterone clinical uses

A

male hypogonadism; wasting syndrome (drug helps gain weight)

228
Q

testosterone adverse effects

A

virilization in females (topical application users must use caution); gynecomastia (high doses); testicular shrinkage, infertility; headache

229
Q

oral androgens

A

fluoxymesterone, methyltestosterone

230
Q

testosterone esters

A

testosterone cypionate - long-acting, parenteral

231
Q

anabolic steroids

A

oxandrolone, nandrolone decanoate -> liver toxicities

232
Q

anti-androgens - 5alpha-reductase inhibitors - finasteride moa

A

inhibits conversion of testosterone to dihydrotesterone

233
Q

finasteride clinical uses

A

benign prostatic hyperplasia; male pattern hair loss

234
Q

finasteride adverse effects

A

rare: gynecomastia, impotence

235
Q

dutasteride

A

similar to finasteride

236
Q

flutamide moa

A

competitive inhibitor of androgen receptor

237
Q

flutamide clinical uses

A

advanced prostate cancer

238
Q

flutamide adverse effects

A

gynceomastia, hot flashes, impotence, hepatotoxicity

239
Q

bicalutamide, nilutamide

A

similar to flutamide w/lower hepatotoxicity

240
Q

spironolactone moa

A

mineralocorticoid receptor antagonist; androgen receptor antagonist

241
Q

spironolactone clinical uses

A

k-sparing diuretic; others: hirsutism, acne, hypertension, hypokalemia, primary aldosteronism

242
Q

spironolactone adverse effects

A

gynecomastia, dyspepsia, lethargy, abnormal menstruation, impotence, rash

243
Q

pharmacotherapy for dysmenorrhea

A

CHOICE: NSAIDs; combined oral contraceptives; depot medroxyprogesterone; levonorgestrel IUD

244
Q

pharmacotherapy for menorrhagia

A

combined oral contraceptives; levonorgestrel IUD; NSAIDs; tranexamic acid (used in surgeries)

245
Q

pharmacotherapy for endometriosis

A

suppress ovarian fxn, endometrial tissue growth -> oral contraceptives (1st line) - progestins, GnRH agonists, danazol; NSAIDs for mild discomfort

246
Q

pharmacotherapy for polycystic ovarian syndrome (PCOS)

A

1st line - combined oral contraceptives - alone or w/anti-androgens -> normalize dysfunctional uterine bleeding

247
Q

treatment of hirsutism, acne in PCOS

A

spironolactone, finasteride, flutamide, GnRH agonists

248
Q

treatment of infertility

A

clomiphene citrate (ovulation inducer); metformin

249
Q

pharmacotherapies for uterine leiomyomas (fibroids/myomas)

A

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
Q

postpartum contraception

A

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

Pharmacology (15 decks)

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