Flashcards in Pituitary drugs Deck (43)
Which drug is a direct agonist of the GH receptor?
Which drug directly activates IGF-1 receptors?
What is this more detailed drug's MoA?
Is a downstream effector of GH
Bypasses GHR defects and/or anti-GH ABs
Activates the IGF1R
Name two SS analogues.
Indications for Somatotropin (rGH)?
- HRT for children w/ GH deficiency
- Other conditions of small stature: Prader-willi syndrome; Turner’s syndrome; Noonan’s syndrome; Chronic renal insufficiency; Idiopathic short stature
Which drug is an antagonist of the GH receptor?
Indications for Mecasermin (rIGF1)?
Children with impaired growth
non-responsive to GH: e.g. mutations in GHR or downstream signaling pathway, neutralizing antibodies to GH, or IGF-1 gene defects (v. rare)
Indications for octreotide, lanreotide?
- GH excess: gigantism, acromegaly.
- Other clinical uses: Esophageal varices; Carcinoid syndrome; Gastrinoma; glucagonoma
- [sketchy: insulinoma, VIPoma, ZE syndrome]
Indications for pegvisomant?
GH excess; gigantism; acromegaly
Adverse effects of somatotropin (rGH)? (adults, children)
- Idiopathic intracranial HTN
- Increased intraocular pressure
- Development of insulin resistance
- Peripheral edema
- Carpal tunnel
- Worsening glucose intolerance
- Acute pancreatitis
Adverse effects of mecasermin (rIGF1)?
- Hypoglycemia (insulin-like)
- Intracranial HTN
- Increased liver enzymes
Adverse effects of octreotide, lanreotide?
Suppresses TSH (monitor for hypothyroidism low risk- typically only transient effect)
Bradycardia & cardiac arrhthymias
Adverse effects of Pegvisomant?
Contraindications for somatotropin? (rGH)
- Active malignancy
- Uncontrolled diabetes
- Proliferative retinopathy
- Children with closed epiphyseal plates (won't be effective)
- Prader-willi with severe obesity and/or respiratory obstruction
Contraindications for mecasermin?
- Active neoplasm
- Children with closed epiphyseal plates
What drugs are GnRH agonists?
Lewd-pro (Jeremy) 'Lin' activates the gonads.
How do GnRH agonists affect gonadotropin release?
Sustained activation of GnRH receptor inhibits release of gonadotropins (even though they're agonists)
Indications for GnRH agonists?
- Controlled ovarian stimulation.
- Palliative therapy of hormone-dependent tumors.
- Suppression of inappropriate growth of hormone-dependent tissues (e.g. endometriosis and fibroids).
- Tx of precocious puberty.
- Suppression of endogenous puberty in gender dysmorphic adolescents.
What drugs are GnRH antagonists?
'Relax' the gonads.
How do GnRH antagonists affect gonadotropin release?
Antagonize GnRH receptors, reduce gonadotropin release. (as expected)
What are the indications for ganirelix + cetrorelix?
What are the indications for degarelix?
Ganirelix + cetrorelix: controlled ovarian stimulation.
Degarelix: advanced prostate cancer
"D" = dick (prostate).
When are ALL GnRH agonists and antagonists contraindicated?
What are the SE's of ALL GnRH agonists and antagonists?
Side effects associated with gonadal hormone deprivation:
- Hot flashes
- Decreased bone density
- Vaginal dryness/atrophy
Although both GnRH agonists and antaognists ultimately inhibit release of gonadotropins, which provides an initial gonadotropin "flair"?
AKA Lewd-pro (Jeremy) 'Lin' activates the gonads.
What does hMG stand for?
Human menopausal gonadotropin
What is hMG made up of?
What is urofollitropin and follitropin (alpha/beta)?
FSH and rFSH
What is FSH (urofollitropin, follitropin) and hMG used for?
Female: FSH and hMG used to stimulate follicular development.
What is hCG used for in females? Males?
- Females: hCG used to trigger ovulation via the LH receptor.
- Males: hCG used to trigger endogenous testosterone synthesis via the LH receptor.
What are hMG, urofollitropin, follitropin, and hCG indicated for in females? Males?
Females: Infertility treatment in anovulatory women.
Ovarian hyperstimulation (in assisted reproductive surgery).
Male: infertility in hypogonadotopic hypogonadism.