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Repro Endo Drugs > edited drugs for repro_endo - Sheet1 > Flashcards

edited drugs for repro_endo - Sheet1 Flashcards

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1
Q

amiloride

A

blocks Na channels -> decr MC effects in hyperaldosteronism *weaker effect than spirolactone

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2
Q

spironolactone: action, use and dosage (3 doses for 6 diseases)

A

antagonist at MC receptors (also androgen and progesterone receptors); 25-50 mg daily as K sparing diuretic for HTN and edematous states (CHF, cirrhosis, nephoris); 400 mg daily in primary hyperaldosteronism; 200 mg daily in PCOS (used off label for anti-androgen effects)

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3
Q

spironolactone side effects (4)

A

hyperkalemia, volume depletion, men: gynecomastia, impaired libido, impotence; women: mest. irregularities

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4
Q

eplerenone

A

highly selective (and expensive) MC antagonist (not androgens nor progesterone)

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5
Q

contraindications for spironolactone (3)

A

renal impairment, hyperkalemia, pregnancy

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6
Q

metyrapone

A

blocks 11-beta enzyme that converts 11-DOC -> cortisol; doesn’t interfere with aldosterone or androgen production (dx adrenal insufficiency as primary or central by seeing relative ACTH/11-DOC levels)

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7
Q

hydrocortisone dosing

A

physiological: 20-30 mg/day in the am; stress: 50 mg every 6-8 hrs; acute: 100 mg IV/IM every 6-8 hrs (don’t need MC replacement b/c hydrocortisone works as MC above 100 mg)

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8
Q

dex dosing

A

physiological: .5 mg daily; stress: 2 mg every 12 hrs; acute: 4 mg IV/IM

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9
Q

ketoconazole

A

non-specific inhibitor of cortisol synthesis (inhibits at 3 steps)

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10
Q

cabergoline

A

DA agonist used to tx somatotroph adenoma -> paradoxical effect

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11
Q

octreotide

A

STT analog used to tx somatotroph or thyrotroph adenoma

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12
Q

pegvisomant

A

GH anatagonist used to tx somatotroph adenoma -> binds only 1/2 receptor and thus blocks it

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13
Q

metformin: action, MOA, effect, metab, adverse effects (4), benefits (3), contraindications (5), misc (1)

A

prevents gluconeogenesis (and poss glycogenolysis); phosphorylation (activation) of AMPK; improves fasting glucose (little effect on postprandial); not metabolized, renally excreted unchanged (can accum. if renal insuff); adverse: anorexia, nausea, diarrhea, lactic acidosis; benefits: immed onset (altho need to titrate slowly to avoid GI effects), no hypoglycemia, weight neutral (poss loss) -> first drug of choice; contraindications: prone to acidosis, hypoxic states, renal failure, cardiac ischemia, T1DM; need insulin to work!

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14
Q

TZDs: action, MOA, effect, duration/onset, contraindications (3), adverse effects (3), benefits (3)

A

incr. periph tissue sensitivity to insulin; binds to nuclear PPAR-gamma receptor (incr. GLUT4 transcription); lowers fasting and post-meal glucose; slow onset of action (fasting gluc begins to decr w/in 5-7 days but doesn’t completely decline until 2-3 mons); contraindications: liver disease, heart failure, renal insuff.; side effects: weight gain (improved glyc. control and incr water due to Na reabs), hepatocellular injury, incr LDL; benefits: reduces TGs, raises HDL, no hypoglycemia

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15
Q

secretagogues: types (2), differences

A

sulfonylurea and meglitinides; both bind the beta cell ATP-dep K channel but meglitinide binds more quickly and dissociates more quickly (shorter duration -> 3-4 hrs vs 12-24)

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16
Q

sulfonylurea: action, MOA, duration, effect, metab, contraindications (3), adverse effects (3)

A

secretagogue; binds to sulfonyl receptor in beta cell causing depolarization of ATP-dependent K channels; 12-24 hrs duration; effect on fasting glucose; metab: excreted via kidney w/ active metabs (careful w/ renal probs); contraind: T1DM, DKA, sulfa allergy; adverse effects: hypoglycemia, weight gain, hunger

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17
Q

meglitinides: action, MOA, duration and onset, metab, contraindications (4), adverse effects (2), aka

A

secretagogue; binds to sulfonyl receptor in beta cell causing depolarization of ATP-dependent K channels; 3-4 hrs duration w/ fast onset (give w/ every meal -> hard for compliance); metab: hepatic (P450) w/ most metabs excreted GI; contraind: T1DM, liver failure, DKA, sulfa allergy; adverse effects: low glucose 2-4 hrs after meal, weight gain; aka glinides

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18
Q

alpha-glucoside inhibitors: MOA, effects, side effects (2), contraindications (1), metab

A

delay carbohydrate absorption (inhibits intestinal enzymes ability to break down sugars) and thus incr GLP-1; effects postprandial glucose only; side effects: flatulence, bloating -> titrate slowly to minimize; contraindications: GI disorders (esp IBD); metab: renally excreted unchanged

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19
Q

GLP-1 mimetic: names (2), comparison, contraindications (2), effect, metab, benefits (2), side effects (1)

A

exenatide (from Gila monster) and liraglutide; liraglutide is once daily injection b/c binds albumin vs. exenatide is twice daily (60 mins before each meal); avoid in pts with severe GI disease or on drugs that need rapid GI abs; effect on postprandial glucose; metab: renal after DPP-4 breakdown; benefit: weight loss, no hypoglycemia; side effects: GI

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20
Q

biguanides: names (1)

A

metformin

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21
Q

incretin enhancers: MOA, duration, effect, metab, contraind, adverse effects, benefits (2)

A

DPP-4 inhibitors; 80% inhib at 24 hrs (take 1 daily); immed effect on postprandial glucose; metab: renally excreted unchanged (dose adj for renal probs); contraindications: none; adverse effects: GI; benefits: weight neutral, no hypoglycemia

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22
Q

glimeperide: what is it, brand name

A

aka Amaryl, a sulfonyurea

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23
Q

bolus insulin types (3) and peak times

A

rapid: Aspart, Lipro (1 hr to peak); short-acting: regular (2-4 hrs to peak -> complexed w/ zinc)

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24
Q

basal insulin types (3) and dosing

A

intermediate: NPH (once or twice/day); long acting: glargine (once/day), detemir (once or twice/day)

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25
rapid-acting insulin: names (3), kinetics (peak, onset, duration), vs. regular (2)
Aspart, Lispro, Glulisine; 1 hr peak (base substitutions disrupt monomer-monomer interactions and decr hexamer formation), 10-20 mins onset, 3-5 hr duration; 2x faster absorption and 2x higher peak concentration
26
NPH: what is it, duration, dosage, onset, peak
suspension of zinc insulin w/ protamine (positively charged peptide); 10-20 hrs duration; dosed once/twice daily; 1-2 hr onset, 4-8 hrs peak
27
glargine: what is it, dosage, onset
human analog insulin w/ base substitutions that cause it to exist at pH 4.0 -> when injected it forms microprecipate below skin that takes time to absorb (long lasting); dosed once daily; 1-2 hr onset (flat course)
28
detemir: what is it, dosage, duration, onset
insulin analog that is acylated w/ myristic acid (remains in solution after injection -> binds to albumin and slowly releases); dosed once or twice daily; duration is dose dependent (up to 24 hrs); .8-2 hr onset (flat course)
29
regular insulin kinetics (onset, peak, duration)
30-60 mins (complexed w/ zinc) onset, 2-4 hr peak, 6-10 hr duration
30
PARP inhibitors (olaparib)
used in BRCA1/2 mutation carriers to prevent ss break repair -> "two hit" hypothesis; tumors may restore BRCA1/2 function and thus become resistant to PARP inhibitors and cisplatin (but not taxane now!)
31
medical tx of impotence: what is it, how does it work, examples (3)
PDE5 inhibitors: sildenafil (Viagra) is prototype -> also vardenafil (Levitra) and tadalafil (Cialis); works by inhibiting breakdown of cGMP by PDE 5, thus incr cGMP and relaxing arteries/trabeculae smooth muscles; works to maintain vasodilatory response (cannot cause it)
32
PDE5 inhibitors pharmacokinetics: onset, metabolism, distribution, changes in metabolism due to... (4)
work quickly (peak plasma 30-90 mins after oral dose); metabolized by CYP3A4 to active metabolite (accounts for 20% activity); widely distributed throughout body tissues; incr. plasma levels (-> hypotension) in elderly (40% incr), liver disease (80%), severe renal disease (100%), w/ CYP3A4 inhibitors (100% incr -> macrolide antibiotics, antifungals, protease inhibitors, cimetidine - OOC for heartburn)
33
PDE5 inhibitors indications (4)
current: impotence, primary pulmonary hypertension; future: CF, BPH
34
PDE5 inhibitors side effects
PDE5 inhibitors prevent breakdown of cGMP, and cGMP is in several other pathways: sperm motility, test synthesis, vaginal smooth muscle, esophageal motility, retinal color vision, inhibition of platelet aggregation; side effects can be divided into four groups: vasodilation (headahce, flushing, rhinitis), CV (hypotension, tachycardia, platelet inhibition), GI (reflux), visual changes (blue green tinged vision, incr. light perception, blurred vision)
35
tx of female sexual dysfn (6)
educational: behavioral/sex therapy, anatomy arousal and response; HRT (estrogen, sometimes testosterone); vascular tx: PDE5 inhibitors (for SSRI induced dysfn only), Eros therapy (handheld device to incr clitoral blood flow), L-arginine tropical tx (Vigael, Sensua -> substrate for NO synthesis)
36
mifepristone
used for abortion up to 63 days (approved for 49 days); anti-progestin; take 4-6 hrs to complete abortion (needs 2 visits) * i think its approved longer now, up to ~10 weeks (70 d)
37
misoprostol
prostaglandin E1 analog (stimulates uterine contractions, softens/primes cervix); FDA approved for prevention and tx of gastric/duodenal ulcers; benefits: heat stable (no refrig), inexpensive, widely available; side effects: flu-like sx (diarrhea, nausea, vomiting, headaches); given vaginally or buccally
38
methotrexate
anti-folate (used off label for abortion - given IV); takes 3-45 days to complete abortion; slightly less effective than mifepristone (90-95% vs 93-98%); used where mifepristone isn't approved and to end ectopic pregnancies (vs mifepristone, which only ends uterine pregnancies)
39
dosing of LT4
start: if under age 60 w/o cardiac disease -> 50-100 mcg, if over 60 or w/ cardiac disease -> 25 mcg; avg final dose (for pts w/o thyroid) = 1.6 mcg/kg PO qd (lower in elderly); give 75% of oral dose if given IV
40
methimazole: half life, dosing, protein bound? how long to see effects? side effects
half life 4-6 hrs (need 1x daily); starting does 10-30 mg QD; 2-4 weeks for improvement w/ 6-12 weeks to euthyroid; freq of side effects is dose related and there are fewer side effects than PTU; rare teratogenic effects -> use instead of PTU unless in pregnancy or thyroid storm
41
PTU: half life, dosing, protein bound? how long to see effects? side effects
half life 1 hr (need 3x daily); starting dose 100 mg TID; 2-4 weeks for improvement w/ 6-12 weeks to euthyroid; worse side effects than methimazole (i.e. severe hepatitis only seen w/ PTU) and no dose relationship of side effects; not teratogenic -> use only in pregnancy
42
when to use PTU
use methimazole in all Grave's except: first trimester pregnancy, thyroid storm, adverse rxn to methimazole
43
side effects of antithyroid drugs (5)
most important side effect = agranulocytosis -> rare (.1-.5%) but severe -> can kill and can appear at any dose; severe hepatitis (PTU only at .1%, hence we don't use it); cholestasis (not as severe as PTU hepatitis, seen w/ methimazole rarely); vasculitis (rare), severe polyarthritis (rare)
44
special instructions with antithyroid drugs
agranulocytosis is dangerous side effect, so tell pts to stop drug and check WBC for fever or sore throat; if granulocytes <500, hospitalize and give broad spectrum antibiotics, if not, resume drug
45
amiodarone
anti-arrhytmia drug w/ 37% weight iodine -> can cause hypothyroidism due to Wolf-Chakoff effect, or hyperthryoidism: type 1 due to Jod-Basedow phenomenon in pts w/ underlying thyroid nodular or Graves' disease, type 2 due to toxic effect of amiodarone causing destructive thyroiditis in normal thyroids causing T3/4 release
46
raloxifene
type III SERM; competes with E2; acts as estrogen in bone and CVS but anti-estrogen in breast and uterus
47
type III SERM
raloxifene; competes with E2; acts as estrogen in bone and CVS but anti-estrogen in breast and uterus
48
tamoxifen
type IV SERM; competes with E2; acts as estrogen in bone, CVS, uterus, but anti-estrogen in breast
49
type IV SERM
tamoxifen; competes with E2; acts as estrogen in bone, CVS, uterus, but anti-estrogen in breast
50
RU-486 is what antagonist type?
type II antagonist
51
Equilin
ERT
52
Mestranol
estrogen -> inhibit lactation
53
letrozole
aromatase inhibitors -> use in breast cancer
54
Norethindrone
progestin -> use in endometriosis
55
finasteride
type II 5-alpha reductase inhibitor; used in BPH and baldness to prevent DHT from exerting its effects in the prostate and hair follicles (more dramatic effect on BPH then on baldness, however)
56
flutamide
non-steroidal androgen receptor antagonist
57
cyproterone acetate
steroidal androgen receptor antagonist
58
Medroxyprogesterone acetate
aka MPA, progesterone-derived progestin in Depo-Provera -> only prog-derived on market
59
Drosperinone
derived from 17-alpha spirolactone, used in Yaz/Yasmin b/c more mineralocorticoid activity
60
bromocriptine
dopamine agonist; can be used to inhibit lactogenesis, treat lactotroph/somatotroph adenoma
61
Herceptin
monoclonal antibody effective for breast cancer with HER-2/neu overexpression/amplification
65
pegvisomat
gh receptor antagonist - GH adenomas
66
eplereone
like spiralactone, exept only acts on MC -- more expensive
67
fludrocortisine
synthetic MC - side effect: hyperaldosteronism
68
mitotane
adrenal cytotoxic (sometimes used for cushings)
69
mifeprostone
GC receptor antagonist (also progesterone antagonist ) -s ometimes used for cushings
70
metyrapone, ketoocnazole
inhibit steroidognesis enzymes - hypercortisolism ** hepatotoxic
71
somatostatin analogue: pasireotide (anything ending in reotide)
inhibit ACTH secretion - used for hypercortisolism, doesnt work for acth-indepnedent adrenal adenomas
72
methimazole/PTU (propylthiouracil)
antithryoid - try these before iodone' 60% remissoin * do not use during pregnancy --- inhibit intrathyroidal iodine utilization AND iodotyrosine coupling ** same mechanism: inhibit oxidation via thyroiperoxidase of iodine for addition to tg .. -- use for graves disease (esp younger), acheive remission in adults, and to lwoer levels prior to surgery
73
thyroid surgery
when thyroid is compresion OR pregnancy
74
give T3
myxedema coma , thyroid cancer before radioactice iodine scans/therapy.. people with defects in enzyme st3-->t4
75
Lt 4
hypothyroidism - need more still with: noncompliance, decreased absorption (iron, PPIs, bowel disease)), increased metabolism (anti-seizure), increased TBG (estrogen, hepatitis), worsening disease ;;; need less with - heart disease (dont want to overdo it)
76
methimazole
preferred antithyroid - longer half life, fewer side effects more consistent dosing, NOT proteint bound - SE dose related - less drug inducedl upus, hepatits, vascultis
77
PTU
binds protein - doesnt cross placenta well - use in first trimester pregnancy, thyroid storm (slows t4--> t3) and adverse reactions to methimazole
78
anitthyroid side effects
AGRANULOCYTOSIS; ptu - hepatitis; both - cholestasis, vasculitis, skin rash, hives
79
PTU, glucocorticoids, pronalol (beta -blockers)
inhibits t4 --> t3 ;; so does potassium iodine -- faster effect -- thyrotoxicosis
80
amiadarone
used for arrthymias - lots of iodoine - causes hyper w/ graves, nodules; can cause hyper or hypo thyroidism --- causes destructive thyroidiitis of normal thyroid --> hormone leakage --> hyperthyroidism
81
rTSH
thyroid cancer diangosis and assessment - drives well differentiated thryoid cancers to take up more iodine - if you have I-131 can see where -- helps AVOID hypo
82
side effects from thyroid meds
inapporpriate dosing OR esnistivity to dyes
83
treat thyroid storm
PTU, propranolol, hydrocortisone, potassium iodide drops ((block conversion !!)
84
i-131
radioiodine - emits gamma rays/beta particles - higher doses for TX - kills off prolifeating cells (necrosis then fibrosis) - NOT pregnancy/KIDS
85
lupron, suprellin
GnRH agonists, treat precocious puberty
86
hypoPTH treament
give Calcium and Vitamin D .. target calcium level = low normal .. not REPLACING kidney effects so you dont want to spill too much into urine
87
5 meds that cause osteoporosis
anticonvulsants, PPIs, aromatase inhibitors, depo-medroxyprogesterone, GC
88
glucocrticoids...
cause fractures!
89
rPTH
increase osteoblasts (osteoporosis)
90
bisphosphobates, calcitonin, denosumab, Serm, estrogen
inhibit osteoclasts (osteoporosis!)
91
bisphosphonate
binds to bone and prevents osteoclasts from working (osteoclasts die too) -- short term effect: gi discomfort, ulcers constipation (ORAL) .. increase creatine (IV) .. flu like ilnness (IV) .. long term may actually weakne bones --> atypical femur fractures and osteonecrosis of jaw
92
denosumab
osteporosis - blocks osteoclasts - mAb, soaks up RANKL - giving OPG basically .. can cause hypocalcemia, infections, and skin reactions
93
teriparatide (rPTH)
OSTEOBLAST ACTIVATOR ! .. can only give 2 years , then stimulation of osteoclast > stimulation of osteoblast (don't know why it doesn't mimic hyperparathyroidism).. adverse effects; hypercalcemia, nausea, orthosatis - OSTEOSARCOMA (rats) .. dont give to people with exisitng bone prolif disease (ie pagets)
94
calcitonin
acute fracture and pain - not good for prevention (another osteoclast inhibitor)
95
raloxifene
SERM used for osteoporosis -- reduces risk of reproductive cancers.. adverse: thromboembolism, menopause symptoms
96
estrogen for osteoporosis
not really used anymore, risks > benefits
97
rPTH, denosumabmab, bisphonates
best 3
98
surgery for hyperPTH
younger than 50, severe hypercalcemia, reduced creatinie clearance (impaired kidney function); osteoporosis
99
risk of overtreating hypothyroidism
high T4, which can lead to atrial fibrillatin
100
reasons for high thyroid during thyroid treatment
doapmine, glucocorticoid, decreased binding protiens, taking more than they should for weight loss, reactivation of diseases like graves
101
t3 on bone marrow
erythropoeies
104
3 treatments for hypogonadism
Testosterone replacemnt (can worsen infertility), LH/FSH replacement, TESE
105
treatment for BPH
alpha adrenergic blocker; 5alpha reductase inhibitor; surgical
106
alkylating agents
do the worse damage to granulosa cells (chemo)
107
misoprostol
"miso soup" - nausea/vomiting, diarrhea, feever/chills .. stimualtes uterine contractions, softens cervixs.. FDA approved for ulcers
108
methotrexate
kills actively dividing cells - takes wayyyy longer than mifeprostone (blocks folate) - ..3-7 d for abotion, bleeding up to 45 d.
109
cardioprotective effects of ERT
increase HDL, decrease LDL; delayed intimal thickening (but arteries thicker), dec angiotensin II; reverse ACh-induced vasoconstriction of carotid arteries
110
aromatase inhibitors
block peripheral conversion of t--> e. ... used in ER-positive cancers (breast and uterine)
111
letrozole, anastrozole, exemestane
aromatase inhibitors
112
estrogen effect on bone
promotes apoptosis of osteoclasts --> maintenance of bone density (why postmenopausal women lose bone density) .. ALSO CLOSURE OF EPHYSEAL PLATES
113
ethinyl estradiol (EE)
used for hypogonadism and contraception
114
mestranol
an estrogen; used for hypogonadism and contraception
115
estradiol cypionate
longer duration than E2; used for ERT
116
metabolic effects of estrogen
increase lepin (inhibit appetide), increase serum proteins including binding proteins and fibrinogen
117
bisphenols, alkylphenols, phthalates (in plastic)
synthetic estrogenic compounds -- implicated in precocious puberty, maybe.
118
site of E1, E3 synthesis
liver (from E2), periphery (from andostenedione)
119
estrogen inc coagulability
inc II, VII, IX, X and decrease antithrombin II
120
non-genomic estrogen
binds uterine artery - promotes vasodilation - inc blood flow w/o transcriptional changes
121
raloxifene
SERM - antagonist in breast AND uterus; agonist in bone and CV .. big downside: strokes, DVTs
122
esterification in 17-beta - complete androgens
helps with cachexia to help gain lean mass , more like tesosterone - used for severe anorexia
123
2-3 anti androgen drugs for prostate cancer
flutamide, nilutamie, cyproterone acetate
124
flutamide
receptor antagonist
125
nilutamide
receptor antagonist
126
cyprotene acetate
receptor antagonist
127
prostaglandin D2
more important for causing buildness then DHT
128
aromatase locations
liver and periphery
129
DHEA
hair growth, bone maturation, sense of well being
130
finasteride
targets type 2 5a reductatse -- bph, mpb
131
alkylation at 17alpha
anabolic effects - commonly abused, in urine - increase RBC and muscle mass
132
pentoxphylline
used to activate sperms from tese/pese
133
clomiphene + FSH
treatment for intfertility in PCOS -- but risk of eclampsia, gestational diabetes, premie, and perinatal motality if do get pregnant
134
clomiphene
SERM (wikipedia: inhibits receptors in hypothalamus, releasing neg feedback, allowing FSH/LH to raise ..)
135
PCOS treatment
OCPS/cyclic progesterone; anti-androgens; weight loss; insulin sensitizers

Repro Endo Drugs (1 decks)

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