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Endocrine > Pharm > Flashcards

Pharm Flashcards

1
Q

somatropin

A

hGH
most effective in first 2 yrs of life
continue Tx until growth stops
children AE: few, intracranial HTN, papilledema, visual changes, LEUKEMIA
adult AE: peripheral edema, carpal tunnel, arthralgia, myalgia
men: increased muscle and bone, decreased fat (athlete abuse: no evidence that it improves performance)
CI: 1-2 yrs following Tx of pediatric tumors

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2
Q

somatomedin C

A

hIGF-1

mediator of GH effects

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3
Q

mecasermin

A

complex of hIGF-1 and hIGFBP-3
longer T1/2
Tx: IGF-1 deficiency

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4
Q

pegvisomant

A

growth hormone receptor antagonist: decreases IGF-1
PEG: increase T1/2 by decreasing renal clearance
Tx: acromegaly

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5
Q

octreotide

A

somatostatin analog
short T1/2: 3x daily injections
Tx: GH excess, insulinomas, glucagonomas
AE: GI
LAR: long-acting, slow release: injected every 4 weeks
inhibits: TSH, GH, insulin, glucagon release

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6
Q

lanreotide

A

somatostatin analog

Tx: GH excess

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7
Q

cabergoline

A

dopamine receptor agonist to decrease prolactin
higher affinity for D2; longer T1/2
Tx: hyperprolactinemia

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8
Q

bromocriptine

A

dopamine receptor agonist
not well tolerated
Tx: hyperprolactinemia

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9
Q

protirelin

A

TRH
stimulates TSH release from thyroid
use: test thyroid function

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10
Q

thyrotropin alpha

A

TSH, hTRH

use: diagnostics for thyroglobulin levels

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11
Q

levothyroxine

A

L-T4

Tx: hypothyroid

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12
Q

liothyronine sodium

A

L-T3

Tx: hypothyroid

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13
Q

liotrix

A

mix of L-T4 and L-T3

Tx: hypothyroid

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14
Q

propylthiouracil (PTU)

A

antithyroid
1. inhibit iodine organification (peroxidase catalyzed rxns: iodination and coupling)
2. inhibits peripheral conversion of T4 to T3
shorter T1/2 than methimazole
AE: rare (agranulocytosis)
can use in pregnancy
Tx: hyperthyroidism

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15
Q

methimazole

A 
antithyroid
inhibit iodine organification (peroxidase catalyzed rxns: iodination and coupling)
more potent than PTU
CI: PREGNANCY (crosses placenta)
Tx: hyperthyroidism
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16
Q

carbimazole

A

antithyroid
inhibit iodine organification (peroxidase catalyzed rxns: iodination and coupling)
Tx: hyperthyroidism

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17
Q

iodine (potassium iodide, iodized salt)

A

large doses: blocks release of thyroid hormone
Tx: thyroid storm, pre-op treatment (reduce size, vascularity, fragility)
CI: prior to radioactive iodide Tx (dilutes)
long-term Tx fails; works best for pre-op or with other antithyroid drugs

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18
Q

radioactive iodine (Na131I)

A

oral
concentrates in thyroid: B radiation destroys all or part of parenchymal cells in weeks but not other tissues
use: 35 yrs or older; NOT in women of child bearing age

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19
Q

propranolol

A

B blocker
blocks T4 to T3 (potent effects on heart)
Tx: hyperthyroidism, thyrotoxicosis

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20
Q

How are T3 and T4 metabolized? Excretion?

A

liver
glucuronide conjugation, sulfate conjugation
excretion: bile, subject to enterohepatic cycling: glucoronidases (from microorganisms) in lower intestine hydrolyze conjugates and release free hormone to be absorbed

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21
Q

What factors inhibit thyroid releasing hormone (TRH) production?

A
  1. somatostatin
  2. DA
  3. Rx glucocorticoids
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22
Q

What factors stimulate thyroid releasing hormone (TRH) production?

A

catecholamines

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23
Q

What factors inhibit thyroid hormone release?

A

HIGH iodine

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24
Q

thyroid stimulating hormone (TSH)

A

immediate increases thyroid hormone secretion
later: effects iodide uptake, hormone synthesis, proteolysis
last: hypertrophy and hyperplasia of thyroid cells
TSH receptor: GPCR that stimulates AC
high TSH levels: TSH receptor: GPCR that stimulates PLC and therefore increase Ca

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25
Q

iodinated contrast media

A

used for improved contrast in CT scans, cardiac cath, etc.

AE: hyperthyroidism (in euthyroid), thyroid storm (in hyperthyroid pts.)

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26
Q

animal insulin

A

bovine, porcine, ovine

only available by special permission from FDA

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27
Q

Can animal become diabetic without glucagon receptors?

A

no

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28
Q

insulin pump

A 
into abdominal fat
must use regular insulin
Tx: T1DM
meal bolus, continuous infusion, variable infusion rates
still requires glucose monitoring
useful in: children, infants
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29
Q

insulin powder

A 
inhaled into lungs
short acting
CI: lung probs
ONLY replaces mealtime injections
easier to use but EXPENSIVE
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30
Q

glucagon

A

Tx: severe hypoglycemia

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31
Q

What drug is CI with sulfonylureas

A

NSAID

causes severe hypoglycemia

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32
Q

meglitinides

A

-GLINIDE
increase insulin secretion (different receptor than sulfonylureas)
short T1/2 (take before each meal)
AE: WEIGHT GAIN, hypoglycemia

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33
Q

repaglinide

A

meglitinide

34
Q

nateglinide

A

meglitinide

35
Q

mitiglinide

A

meglitinide

36
Q

diazoxide

A

anti-HTN antidiuretic
inhibits insulin secretion (but NOT synthesis)
insulin builds up in B cells
Tx: hypoglycemia, insulinomas

37
Q

SGLT2 inhibitors SE

A

hypotension, hyperkalemia, hypoglycemia, increased LDL

CI: renal disease, dialysis

38
Q

teriparatie

A

hPTH
short T1/2
Tx: hypoparathyroid
low dose: cause bone formation: tx: osteoporosis

39
Q

full length hPTH

A

parathyroid hormone

40
Q

synthetic human calcitonin hCT

A

MOA: decrease ruffle border of osteoclast, direct renal effects
does NOT inhibit PTH
decrease syn./secretion of PTH (causes Ca excretion)
decreased bone resorption
shift to inactive Vit. D
Tx: hypercalcemia, hyperparathyroidism, Paget’s, osteoporosis (injection/ nasal spray)
SHORT TERM: Ab form

41
Q

natural calcitonin from salmon

A

MOA: decrease ruffle border of osteoclast, direct renal effects
does NOT inhibit PTH
decrease syn./secretion of PTH (causes Ca excretion)
decreased bone resorption
shift to inactive Vit. D
Tx: hypercalcemia, hyperthyroidism, Paget’s, osteoporosis (injection/ nasal spray)
SHORT TERM: Ab form

42
Q

cholecalciferol

A

Vit. D3

remains in lipid for months

43
Q

ergosterol

A

Vit. D

44
Q

ergocalciferol after irradiation

A

Vit. D2

45
Q

25-OH cholecalciferol

A

Vit. D

46
Q

calcipotriol

A

Vit. D

Tx: Psoriasis (topical, better than glucocorticoids)

47
Q

dihydrotachysterol

A

reduced Vit. D2
not as active as calcitriol, more effective in high doses
Tx: osteoporosis (injection, nasal spray)

48
Q

22-oxacalcitriol

A

Vit. D

suppress PTH gene expression

49
Q

calcitriol (vit. 1,25 dihydroxy-D3)

A

active form of Vit. D
increase Ca and Pi uptake from GI
syn. of calbindin, increase mRNA
also at pharm dose: increase kidney reabsorption, increase bone resorption (paradoxical)
give with Ca to reverse bone resorption
Tx: rickets, osteomalacia, hypoparathyroidism, prevent and tx osteoporosis

50
Q

etidronate

A

first generation bisphosphonate
oral: not effective against hypercalcemia, but 4-24 hr infusion can lower Ca for weeks
Tx: Paget’s

51
Q

alendronate

A

second generation bisphosphonate

Tx: osteoporosis, Paget’s

52
Q

pamidronate

A

second generation bisphosphonate

oral: not effective against hypercalcemia, but 4-24 hr infusion can lower Ca for weeks

53
Q

ibandronate

A

second generation bisphosphonate

54
Q

risedronate

A

third generation bisphosphonate

Tx: Paget’s

55
Q

zoledronate

A

third generation bisphosphonate

56
Q

fluoride

A

binds Ca
dental caries prevention
AE: mottled enamel, osteosclerosis
potential agent for osteoporosis prevention

57
Q

paricalcitol

A

Vit. D

reduce PTH secretion

58
Q

tiludronate

A

3rd generation bisphosphonate

59
Q

Ca supplements

A

take with Vit. D

60
Q

hydrocortisone

A

glucocorticoid

short duration, less potent

61
Q

cortisone acetate

A

glucocorticoid

short duration, less potent

62
Q

prednisone

A

glucocorticoid
potent
weak mineralocorticoid

63
Q

prednisolone

A

glucocorticoid
potent
weak mineralocorticoid

64
Q

methylprednisolone

A

glucocorticoid

NO mineralocorticoid effect

65
Q

dexamethasone

A

glucocorticoid
long duration, potent
NO mineralocorticoid effect
inhibits pituitary ACTH
NO direct effect on cortisol from adrenals
use: test for cushings, acute Addison’s crisis

66
Q

betamethasone

A

glucocorticoid
potent, long acting
NO mineralocorticoid effect

67
Q

cosyntropin

A

ACTH

68
Q

mifepristone (RU-486)

A

glucocorticoid antagonist: binds GC receptor (functionally inactive GC-receptor complex)
Tx: Cushing (high dose) in inoperable patients that have failed other therapies, progesterone antagonist (abortion pill)

69
Q

fludrocortisone

A

mineralocorticoid: mimics aldosterone
renal DCT: Na reabsorption, K excretion
Tx: Addison’s, adrenocortical insufficiency, adrenogenital syndrome
AE: fluid imbalance, hypokalemia, edema, CHF, cardiomegaly, HTN, glucocorticoid effects with long term Tx

70
Q

spironolactone

A

mineralocorticoid antagonist
K sparing diuretic (block Na channels in collecting tubule), aldosterone receptor antagonists
Tx: hyperaldosteronism
AE: hyperkalemia (arrhythmias,), gynecomastia

71
Q

eplerenone

A

mineralocorticoid antagonist
K sparing diuretic (block Na channels in collecting tubule), aldosterone receptor antagonists
Tx: hyperaldosteronism
AE: hyperkalemia (arrhythmias,), gynecomastia
LESS anti-androgen effect

72
Q

Ca sensing receptor

A

GPCR: Gq and Gi
allows both PTH and calcitonin secreting cells to respond to extracellular calcium
expressed in: parafollicular cells, PTH (also: kidney, osteoblasts, hematopoietic cells, GI mucosa)

73
Q

Vit. D

A

Tx: hypoparathyroid

give with/out Ca supplements

74
Q

raloxifene

A

SERM
estrogen effects without breast CA risk
Tx: osteoporosis

75
Q

denosumab

A

Ab to RANKL

Tx: osteoporosis

76
Q

FGF23

A

inhibits production of 1,25-(OH2)D3: opposes PTH in kidney

produced by osteoblasts and osteoclasts

77
Q

bisphosphonates

A

pyrophosphate analog
inhibit bone resorption
poorly absorbed: taken after OVERNIGHT FAST with full glass of WATER, NO FOOD 30 min (sit up, don’t bend over to prevent esophagus irritation)
Tx: Paget’s, osteoporosis
potency increases as generation increases: high potency given IV
AE: OSTEONECROSIS of JAW (most common in 3rd generation, mainly in CA patients), strongest point of femur breaks
ONLY take for 5 years

78
Q

glucocorticoids

A

MOA: inhibit PLA2, inhibit production/release of cytokines, inhibit histamine release
AE: osteoporosis, infection, myopathy, neuropsychiatric (HPA deficient), hirsutism, cataract, glaucoma, increase CV risk, weight gain, Cushing, insulin resistance (DIABETIC probs), thin fragile skin, impaired wound healing, HTN, edema
gastric ulcer: if with NSAIDs
men: hypogonadism
women: stop ovulation, dysmenorrhea, dysfunctional uterine bleeding
children: decrease GH and IGF
SUPPRESSION of endogenous ACTH/cortisol and TSH: up to 12 months to fully recover (doesn’t happen with low doses or short term)
TAPER down: prevent acute adrenal insufficiency

79
Q

plicamycin

A

Tx: Paget’s, hypercalcemia

80
Q

estrogen therapy

A

can cause blood clots

81
Q

how do you evaluate for HPA axis suppression due to glucocorticoids?

A

stop GC for 24 hours
take morning cortisol
less than 5 mug/dL (138nmol/L): impaired HPA
5-10 (138-275): ACTH stimulation test or empiric perioperative GC therapy
greater than 10: HPA not impaired, continue on current glucocorticoid replacement dose on day of surgery
greater than 18: adequate adrenal reserve, no need for GC coverage perioperatively

Endocrine (7 decks)

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