Endocrine Flashcards
Somatropin (Genotropin, Humatrope)
Octreotide
Pegvisomant
are all examples of what type of medications
growth hormone release modulators
Corticotropin
Cosyntropin
are all examples of what type of medications
ACTH release modulators
Leuprolide
Groserelin
Nafarelin
Histrelin
are all examples of what type of medications
FSH-LH release modulators
Bromocriptine
Cabergoline
Octreotide
Pegvisomant
Somatropin
are all examples of what type of medications
prolactin release modulators
Oxytocin
vasopressin
Desmopressin
are all examples of what type of medications
posterior pituitary hormones
Growth hormone has an effect on the
liver
ACTH has an affect on the
adrenal gland to make cortisol
TSH has an affect on
the thyroid gland - producing T4 and T3
FSH/LH has affects on
the gonads to produce estrogen, progesterone or testosterone
PRL has effects on
the breast to produce milk
GH is required for normal
growth
GH target tissues (BALM)
bone
adipose - reduction
liver - somatomedins
muscle
growth plates
Somatropin (GH) indications
GH deficiency
growth failure
HIV patients with cachexia
Somatropin (GH) adverse effects
pain at injection site
edema
arthralgia and myalgia
nausea
glucose tolerance - insulin insensitivity
Somatropin (GH) warning
do not use in peds pts with closed epiphyses
increased intracranial pressure
Somatostatin is an
inhibitory hormone that suppresses GH and TSH release in the hypothalamus (anterior pituitary gland)
suppresses secretions and motility in the GI tract
Octreotide (long acting synthetic somatostatin analog) indications
acromegaly
severe diarrhea caused by carcinoid tumors
bleeding esophageal varices
Octreotide MOA
long acting synthetic somatostatin analog to suppress GH release
Octreotide (long acting synthetic somatostatin analog) adverse effects
CVS - bradycardia and conduction disturbances
GI - diarrhea, abdominal pain, flatulence, nausea and steatorrhea (fatty stool)
Gallbladder emptying is delayed
Pegvisomant MOA
GH receptor antagonist - modified GH with receptor blocking properties
Pegvisomant (GH receptor antagonist) indications
acromegaly that is refractory to other pharm, surgical or radiological intervention
Pegvisomant (GH receptor antagonist) adverse effects
diarrhea and nausea
CNS - pain
abnormal hepatic function tests
Corticotropin MOA
anterior pituitary hormone stimulates steroid biosynthesis - naturally occurring hormone
Cosyntropin MOA
Synthetic ACTH - stimulates adrenal cortex to secrete adrenal steroids (cortisol), androgenic substances and a small amount of aldosterone
Cosyntropin (synthetic ACTH) indications
diagnostic tool - ACTH stimulation test - screening for adrenocorticosteroid deficiency
cortisol is like
adrenaline
Cosyntropin (synthetic ACTH) Adverse effects
excess glucocorticoid toxicities -
HTN, peripheral edema, hypokalemia, osteoporosis
Cosyntropin is a precursor to _____ essentially
steroids - like prednisone
Gonadotropin - releasing hormone is secreted from
the hypothalamus - binds to receptors in anterior pituitary gland
FSH-LH release modulators adverse effects: males and females
male - transient increase in testosterone, hot flashes, sweats, edema, gynecomastia, decreased libido, decreased HCT and bone density
female - generalized menopausal symptoms, ovarian cysts
Leuprolide (FSH-LH release modulator) indications
used to treat prostate cancer, breast cancer, endometriosis, uterine fibroids, early puberty
can delay onset of puberty in transgender youth prior to HRT
can delay or prevent early ovulation to allow for development of mature eggs for retrieval in IVF
Goserelin (FSH-LH release modulator) indications
suppress production of the sex hormones, particularly in the treatment of breast and prostate cancer
Nafarelin (FSH-LH release modulator) indications
used in the treatment of endometriosis and early puberty
Histrelin (FSH-LH release modulator) indications
used to treat advanced prostate cancer in adults - will reduce levels of testosterone
Prolactin is a hormone secreted from the
anterior pituitary
Prolactin stimulates and maintains
lactation
Prolactin is increased by _____ and is also stimulated to release by _______
dopamine antagonists
TRH
Prolactin release modulators include
Bromocriptine and Cabergoline
Bromocriptine and Cabergoline MOA
Dopamine D2 receptor agonists - suppress prolactin release
Bromocriptine and Cabergoline indications
lactotroph adenomas (prolactinomas) - hyperprolactinemia
T2DM (theoretically)
Bromocriptine and Cabergoline adverse effects
HA, dizziness, psychosis
Nausea
When giving FSH-LH release modulators
Continuous =
Pulsatile =
will decrease production
will increase/ stimulate production
Posterior Pituitary gland hormones are not
regulated by releasing hormones
Target tissues of:
Oxytocin
Vasopressin (ADH)
Oxytocin = uterus and breast
Vasopressin = nephron and vascular smooth muscle
Oxytocin acting on breast and uterus causes
contraction and milk production
Vasopressin acting on nephron and vascular smooth muscle causes
water reabsorption, hyponatremia
vasoconstriction
Oxytocin indications
labor induction
postpartum hemorrhage
Oxytocin adverse effects
hypotension and arrhythmias
fluid retention
placental abruption or uterine rupture
fetal distress and death
oxytocin MOA
binds to oxytocin receptors
Vasopressin MOA
stimulates arginine vasopressin receptors
desmopressin = selective V2 activity (minimal V1)
V1 receptor =
V2 receptor =
V1 = vascular smooth muscle
V2 = nephron
Vasopressin indications
central diabetes insipidus
nocturnal enuresis
Vasopressin adverse effects
water intoxication and hyponatremia
HA, bronchoconstriction and tremor
clots because of the extra renal V2 receptors that increase blood coag factors
Vasopressin warnings
caution when using vasopressin in pts with CAD, epilepsy and asthma
nasal spray has been linked to increased seizures in children
Naturally occurring Glucocorticoids
Cortisol (hydrocortisone)
Cortisone (less potent)
Primary action of naturally occurring glucocorticoids
stress hormone
betamethasone
Cortisone
dexamethasone
hydrocortisone
prednisone
methylprednisone
triamcinolone
are all examples of what type of medication
corticosteroids
Fludrocortisone
spironolactone
eplerenone
are examples of what type of medications
mineralocorticoid agonist and antagonists
Short acting (1-12 hours) glucocorticoids
hydrocortisone
cortisone
intermediate acting (12-35 hours) glucocorticoids
prednisone
prednisolone
methylprednisone
triamcinolone
long acting (36-55 hours) glucocorticoids
betamethasone
dexamethasone
mineralocorticoid properties - high salt retaining effect
fludrocortisone
similar glucocorticoid and mineralocorticoid properties
short acting steroids - hydrocortisone and cortisone
more glucocorticoid activity and minimal to no mineralocorticoid activity
intermediate acting steroids - prednisone, prednisolone, methylprednisolone, triamcinolone (no mineralocorticoid effect)
Glucocorticoid activity and no mineralocorticoid activity
long acting steroids - betamethasone and dexamethasone
Therapeutic use of steroids:
Adrenal use - replacement therapy or dx of cushing’s syndrome
replacement therapy = hydrocortisone
dx of cushing’s = dexamethasone
Therapeutic use:
non adrenal therapy - anti inflammatory, anti-allergy =
acceleration of lung maturation-antenatal (surfactant production) =
anti inflammatory, anti allergy = several
acceleration of lung maturation-antenatal = betamethasone and dexamethasone
Low dose dexamethasone suppression test
positive low dose test dx/confirms hypercortisolemia (cushing’s syndrome) = no suppression of cortisol - normal or high
negative test = decreased/ suppressed cortisol production after administration
Naturally occuring Mineralocorticoids
aldosterone
Action of aldosterone
regulate salt and water metabolism
- increase salt reabsorption
- increase potassium excretion
- increase hydrogen ion excretion
Fludrocortisone MOA
synthetic mineralocorticoid
salt and water retaining properties
some glucocorticoid activity
Fludrocortisone indications
treatment of addison’s disease and associated mineralocorticoid deficiency
Hypothyroidism drugs
T4- Levothyroxine
T3- Liothyronine
T3+T4 LioTrix
Hyperthyroidism drugs
Methimazole
Propylthiouracil
Propranolol
Iodine and potassium iodide
T4 - Levothyroxine absorption
stable, well absorbed (taken on an empty stomach) with some exceptions - aluminum, magnesium containing antacids may decrease absorption
Levothyroxine is synthetic
T4
T4- Levothyroxine has a half life of
7 days
T4- Levothyroxine is associated with
toxicity (increased levels of T4)
Liothyronine is
synthetic T3
T3- Liothyronine has _______ oral absorption
rapid
T3- Liothyronine has a ______ half life
short
T3- Liothyronine has an increased risk of
cardiotoxicity
T3 + T4 Liotrix was developed to
try and mimic normal, physiologic hormone levels
T3 + T4 Liotrix is made up of
12.5 mcg levothyroxine and 3.1 mcg liothyronine
Indications for what drug = tried and failed levothyroxine, have no thyroid left or has gone through radioiodine
T3 + T4 Liotrix
Thioamides include
Propylthiouracil
Methimazole
Propylthiouracil MOA
Inhibits thyroid hormone synthesis - inhibits thyroperoxidase and D1 (iodothyronine deiodinase) which decreases T4 to T3 conversion
Propylthiouracil has a ______ half life
fast
Propylthiouracil toxicity
teratogenic - preferred early in pregnancy
hepatotoxicity
bone marrow suppression - agranulocytosis
Methimazole MOA
inhibits thyroid hormone synthesis - inhibits thyroperoxidase, does not affect D1
Methimazole toxicity
teratogenic - preferred in the 2nd and 3rd trimester
hepatotoxicity
bone marrow suppression - agranulocytosis
Propanolol MOA
non-selecetive b-blocker
symptomatic control in thyroid storm
inhibits deiodination of T4 - reduces circulation of T3
Propanolol is administered in
IV in emergency setting for thyroid storm symptom control
Iodine and KI MOA
inhibition of biosynthesis - inhibition of the iodination of tyrosine
inhibition of secretion/ release of T4/T3
Iodine and KI effects on serum thyroid hormone are maximal at
10 days
Iodine and KI adverse effects
exacerbation of hyperthyroidism
mucosal injury - mouth, pharynx, esophageal or duodenal lesions
Potassium Iodide used to treat
severe hyperthyroidism and to protect the thyroid gland when using radiopharmaceuticals
preoperative preparation for thyroidectomy in graves disease to decrease gland vascularity
thyroid storm
short term control of graves disease
Radioactive Iodine MOA
administered orally as sodium iodine in solution or capsule, rapidly absorbed into the thyroid gland causing local tissue destruction
Thyroid is rendered inactive over 6-18 wks
Indications for radioactive iodine
graves disease
toxic adenoma
multinodular goiter
Bisphosphonates MOA
Inhibit osteoclast activity, reducing bone resorption and turnover
Alendronate indications
osteoporosis, pagets disease of bone, osteopenia (in non-ambulatory patients)
Risedronate indications
osteoporosis, pagets disease of the bone
Hypercalcemia clinical presentation
bones, moans, stones and muscle psychiatric overtones
ECG - shorted QT, ST depression, AV blocks
Ibandronate indications
Osteoporosis
Zoledronic Acid indications
Osteoporosis, malignant hypercalcemia, bone metastases, multiple myeloma
Common causes of Hypercalcemia
hyperparathyroidism, malignancy, granulomatous disease, thiazides, lithium, pancreatitis
Hypercalcemia interventions
IV hydration, calcitonin, bisphosphonates, loop diuretics, glucocorticoids, denosumab, dialysis
Bisphosphonates side effects
bone, joint, muscle pain
GI upset
HA
atypical femur fractures, osteonecrosis of the jaw
Irritation to upper GI mucosa - take and remain upright for at least 30 min
hypocalcemia - Ca and Vit D supplementation recommended
Contraindications of Bisphosphonates
esophageal disorders
renal insufficiency
hypocalcemia
food interferes with absorption - take with water on empty stomach and wait 30-60 min before eating
Calcitonin MOA
antagonizes the effects of PTH, inhibits osteoclast activity and promotes the renal excretion of Ca2+
Calcitonin indications
hypercalcemia
pagets disease of the bone
postmenopausal osteoporosis
pain from osteoporotic fracture
Calcitonin adverse effects
rhinitis
epistaxis
back pain
n/v
bronchospasms
hypocalcemia
anaphylaxis (rare)
Vit D MOA
Cholecalciferol is a provitamin
stimulates Ca absorption from the small intestines, promotes bone mineralization
Indications for Vit D
Vit D deficiency
Osteoporosis
Hypoparathyroidism
Contraindications to Vit D
hypercalcemia
primary hyperparathyroidism
sarcoidosis
Calcitrol MOA
Vit D analog - stimulates intestinal Ca and P aborption, decrease PTH synthesis, stimulates bone mineralization
Calcitrol indications
renal failure
hypoparathyroidism
rickets
hypophosphatemia
Adverse effects of Calcitriol
hypercalcemia
hyperphosphatemia
N/V
Contraindications of Calcitriol
pancreatitis
soft tissue calcifications
arrhythmias
Denosumab MOA
recombinant antibody that inhibits RANK-ligand to bind to RANK (antiresorptive)
Denosumab indications
osteoporosis, cannot tolerate or unresponsive to bisphosphonates, renal impairment
Side effects of Denosumab
osteonecrosis of the jaw, atypical subtrochanteric fracture, bone pain
Contraindications to denosumab
hypocalcemia
Teriparatide - recombinant PTH MOA
anabolic effect on bone metabolism by stimulating bone formation and activating bone remodeling
treatment duration < 2 years in lifetime
Teriparatide indications
osteoporosis (not used often), if they have failed bisphosphonates and other options
Side effects of Teriparatide
generally well tolerated
hypercalcemia and hypercalciuria
orthostatic hypotension
BLACK BOX WARNING - potential risk of osteosarcoma
Contraindications of teriparatide
hypercalcemia
severe renal impairment
Raloxifene MOA
selective estrogen receptor modifier
acts like an estrogen agonist in the bone thereby decreasing bone resorption and overall bone turnover
bone density is increased
indications for raloxifene
osteoporosis in postmenopausal women
Adverse effects of raloxifene
hot flashes, leg cramps, peripheral edema, DVT/PE
Contraindications for raloxifene
history of DVT/PE, pregnancy
Effects of diuretics on calcium levels
Thiasizes (HCTZ) - decreased urinary Ca excretion, inhibits secretion of Ca sometimes leading to elevated levels of Ca in blood
Loop diuretics (furosemide) - increased urinary Ca concentration, useful in treatment of hypercalcemia because it stimulates tubular Ca excretion
therapeutic and toxic effects of fluoride ion
appears to increase osteoblast activity, increase bone density but fracture risk is not reduced
toxicity sxs - Gi effects such as N/V, diarrhea, severe cases renal or cardiac dysfunction