Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Repro Endo Drugs > ReproEndo Drugs - Sheet1 > Flashcards

ReproEndo Drugs - Sheet1 Flashcards

1
Q

amiloride

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

spironolactone side effects (4)

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

eplerenone

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

contraindications for spironolactone (3)

A

renal impairment, hyperkalemia, pregnancy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

dex dosing

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

ketoconazole

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

cabergoline

A

DA agonist used to tx somatotroph adenoma -> paradoxical effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

octreotide

A

STT analog used to tx somatotroph or thyrotroph adenoma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

pegvisomant

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

metformin: action, MOA

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!

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Metformin effect

A

improves fasting glucose (little effect on postprandial)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

metformin metabolism

A

not metabolized, renally excreted

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

metformin adverse effects (4)

A

anorexia, nausea, diarrhea, lactic acidosis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

metformin benefits (3)

A

immediate onsent, no hypoglycemia, weight neutral

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

metformin contraind (5)

A

prone to acidosis, hypoxic states, renal failure, cardiac ischemia, T1DM (need insulin to work)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

TZDs: action, MOA

A

incr. periph tissue sensitivity to insulin; binds to nuclear PPAR-gamma receptor (incr. GLUT4 transcription)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

TZD effect

A

decreases fasting and post-meal glucose

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

TZD duration/onset

A

slow onset of action (fasting gluc begins to decrease within 5-7 days but doesn’t completely decline until 2-3 months)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

TZD contraind (3)

A

liver disease, heart failure, renal insufficiency

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

TZD adverse effects (3)

A

weight gain (increased water due to Na reabsorption), hepatocellular injury, increased LDL

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

TZD benefits (3)

A

reduces TGs, raises HDL, no hypoglycemia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

sulfonylurea: action, MOA, duration

A

secretagogue; binds to sulfonyl receptor in beta cell causing depolarization of ATP-dependent K channels; 12-24 hrs duration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

sulfonylurea effect

A

effect on fasting glucose

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

sulfonylurea metabolism

A

excreted via kidney with active metabolites (careful w/ renal problems)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

sulfonylurea contraind (3)

A

T1DM, DKA (need fxning beta cells!), sulfa allergy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

sulfonyl adverse effects (3)

A

hypoglycemia, weight gain, hunger

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

meglitinides duration and onset

A

3-4 hour duration wtih fast onset (different from sulfonylureas)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

meglitinides metabolism

A

hepatic (P450) with most metabolites secreted via GI

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

meglitinides contraind (4)

A

T1DM, DKA (need fxning beta cells!), sulfa allergy, liver failure

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

meglitinides adverse effects (2)

A

low glucose 2-4 hours after meal, weight gain

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

alpha-glucoside inhibitors: MOA

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

alpha-glucosidase inhibitors effects

A

decreases post-prandial glucose

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

alpha-glucosidase side effects

A

flatulence, bloating

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

alpha-glucosidase contraindications

A

GI disorders

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

alpha-glucosidase metabolism

A

renally excreted unchanged

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
41
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

42
Q

GLP-1 mimetic contraindications (2)

A

GI disease or drugs that need rapid GI absorption

43
Q

GLP-1 mimetic effect

A

decrease post-prandial glucose

44
Q

GLP-1 mimetic metabolism

A

broken down by DPP-4 then renal

45
Q

GLP-1 mimetic benefits (2)

A

weight loss, no hypoglycemia (glucose dependent)

46
Q

GLP-1 mimetic side effects

A

GI

47
Q

biguanides: names (1)

A

metformin

48
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

49
Q

incretin enhancer effect

A

decrease post-prandial glucose

50
Q

incretin enhancer metabolism

A

renally excreted unchanged

51
Q

incretin enhancer contraindiaction

A

none

52
Q

incretin enhancer adverse effects

A

GI

53
Q

incretin enhancer benefits (2)

A

weight neutral, no hypoglycemia

54
Q

glimeperide: what is it, brand name

A

aka Amaryl, a sulfonyurea

55
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)

56
Q

basal insulin types (3) and dosing

A

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

57
Q

rapid-acting insulin: names (3), kinetics (peak, onset, duration), vs. regular (2)

A

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

58
Q

NPH: what is it, duration, dosage, onset, peak

A

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

59
Q

glargine: what is it, dosage, onset

A

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)

60
Q

detemir: what is it, dosage, duration, onset

A

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)

61
Q

regular insulin kinetics (onset, peak, duration)

A

30-60 mins (complexed w/ zinc) onset, 2-4 hr peak, 6-10 hr duration

62
Q

PARP inhibitors (olaparib)

A

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!)

63
Q

medical tx of impotence: what is it, how does it work, examples (3)

A

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)

64
Q

PDE5 inhibitors pharmacokinetics: onset, metabolism, distribution, changes in metabolism due to… (4)

A

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)

65
Q

PDE5 inhibitors indications (4)

A

current: impotence, primary pulmonary hypertension; future: CF, BPH

66
Q

PDE5 inhibitors side effects

A

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)

67
Q

tx of female sexual dysfn (6)

A

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)

68
Q

mifepristone

A

used for abortion up to 63 days (approved for 49 days); anti-progestin; take 4-6 hrs to complete abortion (needs 2 visits)

69
Q

misoprostol

A

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

70
Q

methotrexate

A

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)

71
Q

dosing of LT4

A

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

72
Q

methimazole: half life, dosing, protein bound? how long to see effects? side effects

A

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

73
Q

PTU: half life, dosing, protein bound? how long to see effects? side effects

A

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

74
Q

when to use PTU

A

use methimazole in all Grave’s except: first trimester pregnancy, thyroid storm, adverse rxn to methimazole

75
Q

side effects of antithyroid drugs (5)

A

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)

76
Q

special instructions with antithyroid drugs

A

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

77
Q

amiodarone

A

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

78
Q

raloxifene

A

type III SERM; competes with E2; acts as estrogen in bone and CVS but anti-estrogen in breast and uterus

79
Q

type III SERM

A

raloxifene; competes with E2; acts as estrogen in bone and CVS but anti-estrogen in breast and uterus

80
Q

tamoxifen

A

type IV SERM; competes with E2; acts as estrogen in bone, CVS, uterus, but anti-estrogen in breast

81
Q

type IV SERM

A

tamoxifen; competes with E2; acts as estrogen in bone, CVS, uterus, but anti-estrogen in breast

82
Q

RU-486 is what antagonist type?

A

type II antagonist

83
Q

Equilin

A

ERT

84
Q

Mestranol

A

estrogen -> inhibit lactation

85
Q

letrozole

A

aromatase inhibitors -> use in breast cancer

86
Q

Norethindrone

A

progestin -> use in endometriosis

87
Q

finasteride

A

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)

88
Q

flutamide

A

non-steroidal androgen receptor antagonist

89
Q

cyproterone acetate

A

steroidal androgen receptor antagonist

90
Q

Medroxyprogesterone acetate

A

aka MPA, progesterone-derived progestin in Depo-Provera -> only prog-derived on market

91
Q

Drosperinone

A

derived from 17-alpha spirolactone, used in Yaz/Yasmin b/c more mineralocorticoid activity

92
Q

bromocriptine

A

dopamine agonist; can be used to inhibit lactogenesis, treat lactotroph/somatotroph adenoma

93
Q

Herceptin

A

monoclonal antibody effective for breast cancer with HER-2/neu overexpression/amplification

94
Q

pegvisomat

A

gh receptor antagonist - GH adenomas

95
Q

eplereone

A

like spiralactone, exept only acts on MC – more expensive

96
Q

fludrocortisine

A

synthetic MC - side effect: hyperaldosteronism

97
Q

mitotane

A

adrenal cytotoxic (sometimes used for cushings)

98
Q

mifeprostone

A

GC receptor antagonist (also progesterone antagonist ) -s ometimes used for cushings

99
Q

metyrapone, ketoocnazole

A

inhibit steroidognesis enzymes - hypercortisolism ** hepatotoxic

100
Q

somatostatin analogue: pasireotide (anything ending in reotide)

A

inhibit ACTH secretion - used for hypercortisolism, doesnt work for acth-indepnedent adrenal adenomas

101
Q

methimazole/PTU

A

antithryoid - try these before iodone’ 60% remissoin * do not use during pregnancy

102
Q

thyroid surgery

A

when thyroid is compresion OR pregnancy

Repro Endo Drugs (1 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions