Pharm Flashcards
somatropin
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
somatomedin C
hIGF-1
mediator of GH effects
mecasermin
complex of hIGF-1 and hIGFBP-3
longer T1/2
Tx: IGF-1 deficiency
pegvisomant
growth hormone receptor antagonist: decreases IGF-1
PEG: increase T1/2 by decreasing renal clearance
Tx: acromegaly
octreotide
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
lanreotide
somatostatin analog
Tx: GH excess
cabergoline
dopamine receptor agonist to decrease prolactin
higher affinity for D2; longer T1/2
Tx: hyperprolactinemia
bromocriptine
dopamine receptor agonist
not well tolerated
Tx: hyperprolactinemia
protirelin
TRH
stimulates TSH release from thyroid
use: test thyroid function
thyrotropin alpha
TSH, hTRH
use: diagnostics for thyroglobulin levels
levothyroxine
L-T4
Tx: hypothyroid
liothyronine sodium
L-T3
Tx: hypothyroid
liotrix
mix of L-T4 and L-T3
Tx: hypothyroid
propylthiouracil (PTU)
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
methimazole
antithyroid inhibit iodine organification (peroxidase catalyzed rxns: iodination and coupling) more potent than PTU CI: PREGNANCY (crosses placenta) Tx: hyperthyroidism
carbimazole
antithyroid
inhibit iodine organification (peroxidase catalyzed rxns: iodination and coupling)
Tx: hyperthyroidism
iodine (potassium iodide, iodized salt)
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
radioactive iodine (Na131I)
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
propranolol
B blocker
blocks T4 to T3 (potent effects on heart)
Tx: hyperthyroidism, thyrotoxicosis
How are T3 and T4 metabolized? Excretion?
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
What factors inhibit thyroid releasing hormone (TRH) production?
- somatostatin
- DA
- Rx glucocorticoids
What factors stimulate thyroid releasing hormone (TRH) production?
catecholamines
What factors inhibit thyroid hormone release?
HIGH iodine
thyroid stimulating hormone (TSH)
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
iodinated contrast media
used for improved contrast in CT scans, cardiac cath, etc.
AE: hyperthyroidism (in euthyroid), thyroid storm (in hyperthyroid pts.)
animal insulin
bovine, porcine, ovine
only available by special permission from FDA
Can animal become diabetic without glucagon receptors?
no
insulin pump
into abdominal fat must use regular insulin Tx: T1DM meal bolus, continuous infusion, variable infusion rates still requires glucose monitoring useful in: children, infants
insulin powder
inhaled into lungs short acting CI: lung probs ONLY replaces mealtime injections easier to use but EXPENSIVE
glucagon
Tx: severe hypoglycemia
What drug is CI with sulfonylureas
NSAID
causes severe hypoglycemia
meglitinides
-GLINIDE
increase insulin secretion (different receptor than sulfonylureas)
short T1/2 (take before each meal)
AE: WEIGHT GAIN, hypoglycemia
repaglinide
meglitinide
nateglinide
meglitinide
mitiglinide
meglitinide
diazoxide
anti-HTN antidiuretic
inhibits insulin secretion (but NOT synthesis)
insulin builds up in B cells
Tx: hypoglycemia, insulinomas
SGLT2 inhibitors SE
hypotension, hyperkalemia, hypoglycemia, increased LDL
CI: renal disease, dialysis
teriparatie
hPTH
short T1/2
Tx: hypoparathyroid
low dose: cause bone formation: tx: osteoporosis
full length hPTH
parathyroid hormone
synthetic human calcitonin hCT
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
natural calcitonin from salmon
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
cholecalciferol
Vit. D3
remains in lipid for months
ergosterol
Vit. D
ergocalciferol after irradiation
Vit. D2
25-OH cholecalciferol
Vit. D
calcipotriol
Vit. D
Tx: Psoriasis (topical, better than glucocorticoids)
dihydrotachysterol
reduced Vit. D2
not as active as calcitriol, more effective in high doses
Tx: osteoporosis (injection, nasal spray)
22-oxacalcitriol
Vit. D
suppress PTH gene expression
calcitriol (vit. 1,25 dihydroxy-D3)
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
etidronate
first generation bisphosphonate
oral: not effective against hypercalcemia, but 4-24 hr infusion can lower Ca for weeks
Tx: Paget’s
alendronate
second generation bisphosphonate
Tx: osteoporosis, Paget’s
pamidronate
second generation bisphosphonate
oral: not effective against hypercalcemia, but 4-24 hr infusion can lower Ca for weeks
ibandronate
second generation bisphosphonate
risedronate
third generation bisphosphonate
Tx: Paget’s
zoledronate
third generation bisphosphonate
fluoride
binds Ca
dental caries prevention
AE: mottled enamel, osteosclerosis
potential agent for osteoporosis prevention
paricalcitol
Vit. D
reduce PTH secretion
tiludronate
3rd generation bisphosphonate
Ca supplements
take with Vit. D
hydrocortisone
glucocorticoid
short duration, less potent
cortisone acetate
glucocorticoid
short duration, less potent
prednisone
glucocorticoid
potent
weak mineralocorticoid
prednisolone
glucocorticoid
potent
weak mineralocorticoid
methylprednisolone
glucocorticoid
NO mineralocorticoid effect
dexamethasone
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
betamethasone
glucocorticoid
potent, long acting
NO mineralocorticoid effect
cosyntropin
ACTH
mifepristone (RU-486)
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)
fludrocortisone
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
spironolactone
mineralocorticoid antagonist
K sparing diuretic (block Na channels in collecting tubule), aldosterone receptor antagonists
Tx: hyperaldosteronism
AE: hyperkalemia (arrhythmias,), gynecomastia
eplerenone
mineralocorticoid antagonist
K sparing diuretic (block Na channels in collecting tubule), aldosterone receptor antagonists
Tx: hyperaldosteronism
AE: hyperkalemia (arrhythmias,), gynecomastia
LESS anti-androgen effect
Ca sensing receptor
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)
Vit. D
Tx: hypoparathyroid
give with/out Ca supplements
raloxifene
SERM
estrogen effects without breast CA risk
Tx: osteoporosis
denosumab
Ab to RANKL
Tx: osteoporosis
FGF23
inhibits production of 1,25-(OH2)D3: opposes PTH in kidney
produced by osteoblasts and osteoclasts
bisphosphonates
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
glucocorticoids
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
plicamycin
Tx: Paget’s, hypercalcemia
estrogen therapy
can cause blood clots
how do you evaluate for HPA axis suppression due to glucocorticoids?
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
