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