Pituitary hormone ligands bind ____ receptor and dimerizes, and phosphorylates ____ would lead to regulating ______ in the nucleus.
JAK-2
STAT
Transcription
GH receptors in the _______, would lead to stimulation and secretion of IGF-1. What could IGF-1 do once it is stimulated?
Liver
Linear bone growth
Oxidation of free fatty acid
Protein synthesis for muscle
And decrease GH level once it is high enough
Somatropin is used to treat which hormone deficiency?
Growth hormone
What used for growth hormone deficiency?
Somatropin
Which drug is a recombinant form of GH?
Somatropin
Therapeutic indication for somatropin:
GH deficiency
Pediatric patients short stature
Which drug does Kaydee need to be on that isn’t Adderall?
Somatropin, iono maybe it'll help her get taller?
ADR somatropin:
Arthralgia
Myalgia
Peripheral edema
Slipped capital femoral epiphysis (children)
What drug is contraindicated when there is active malignancy?
Somatropin
Which drug has adverse effects that include joint, muscle ache and peripheral edema?
Somatropin
Which hormonal drug can increase P450 activity?
Somatropin (recombinant GH)
Contraindications for somatropin:
Acute critical illness
Active malignancy
Somatropin pharmacokinetics:
IM or subcutaneous
Increase P450 enzymes
T/F: Recombinant IGF-1 can be used for chronic renal insufficiency, in addition to GH deficiency
False; recombinant growth hormone (ie somatropin) is used to treat chronic renal insufficiency, as well as Prader-willi, Turner, in addition to GH deficiency
Prader-Willi Syndrome, Turner syndrome and chronic renal insufficiency can be treated with______
Recombinant human growth hormone – somatropin (recombinant GH)
MOA for Mecasermin:
Recombinant human IGF-1, bound to IGFBP-3
What is an agent of IGF-1 agonist?
Mecasermin
T/F: Mecasermin primarily binds to IGFBP-1 binding protein
False; it is an IGF-1 agonist that mostly (80%) binds to IGFBP-3 binding protein
Short children not responding to somatropin, use:
Mecasermin (recombinant human IGF-1)
Therapeutic Indications for Mecasermin?
Severe IGF-1 deficiency / GH therapy ineffective
ADR mecasermin (recombinant human IGF-1)?
Intracranial hypotension
Hypoglycemia
What needs/should be done to patient on mecasermin to avoid hypoglycemia?
Eat carbohydrates 20 minutes before/after drug administration
Which drug can have adverse effect hypotension and hypoglycemia?
Mecasermin (recombinant human IGF-1)
What typically shows up on MRI in patients with acromegaly?
Pituitary tumors
What is acromegaly?
Disorder of IGF-1 which causes excessive growth of the hands, feet, jaw, and internal organs in adulthood
T/F: Acromegaly is a disorder of GH deficiency which occurs in childhood
False; acromegaly is a disorder of IGF-1 and occurs in adulthood. Symptoms include excessive growth of the hands, feet, jaw, and internal organs
Large pituitary adenomas can lead to what CNS effect?
Disturbance of visual field
What is the negative feedback for pituitary secretion of growth hormone?
IGF-1
Somatostatin inhibits release of which 5 hormones?
GH, TSH, glucagon, insulin and gastrin
T/F: somatostatin analogs have longer half-live than somatostatin, and it targets only GH inhibition
False; somatostatin has inhibition effects on multiple hormones (not just GH), including GH, TSH, Glucagon, insulin and gastrin. It's true that it does have longer half-live, though
What are some somatostatin analogs?
Octreotide – potent somatostatin, not as much effect on release of insulin than endogenous somatostatin
Lanreotide (just know that this also exists)
Which medication can be used to locate neuroendocrine tumors?
octreotide
(somatostatin analog)
What are the therapeutic indications for octreotide?
Which drug should Kaydee definitely avoid taking, especially long term, for reason other than that she is already vertically challenged?
Octreotide (somatostatin analog)
Because if on this for over a year, can lead to B12 deficiency, and we don't want that since she's vegan and might already be on her way to developing that?
That, and also we don't want more somatostatin in her, inhibiting GH
Which medication when on it for over 1 year, can lead to B12 deficiency?
Octreotide (a somatostatin analog)
Which medication when on it for over 6 months can lead to biliary sludge and gallstones?
Octreotide (a somatostatin analog)
What is pegvisomant?
GH receptor antagonist
What is an agent for GH receptor antagonist?
Pegvisomant
T/F: Pegvisomant is a growth receptor agonist
False; it is a growth receptor antagonist
Which drug is used to treat acromegaly?
Pegvisomant, (GH receptor antagonist)
Somatostatin analogs: ie Octreotide
Dopamine agonist
ADR for pegvisomant?
Elevated GH and liver enzymes
Adenoma growth
(GH receptor antagonist)
Which drug could potentially lead to adenoma growth?
pegvisomant (a GH antagonist)
Hyperprolactinemia is treated with ____ agonist
Dopamine
What are agents of dopamine agonist:
Ergot derivatives
Bromocriptine
Cabergoline
Therapeutic use for dopamine agonist (ie Bromocriptine)
Acromegaly
Hyperprolactinemia
Which drug could be given either orally or vaginally?
dopamine agonist ie Bromocriptine
ADR for Dopamin agonists (Bromocriptine)?
Nausea, HA
Orthostatic hypotension, fatigue
Contraindication for dopamine agonist?
Small adenomas during pregnancy
Which drug is contraindicated when you are pregnant and have small adenomas?
