Lecture 7 - Hypothalamic and Pituitary Pharm Flashcards
While Peptide hormones and drugs can have both genomic and non-genomic responses, ________ take much longer (on the order of a couple hours up to 24 hours). _______ responses can be almost instantaneous.
Genomic –> longer
High levels of Prolactin can suppress _______ levels –> this causes “Lactational _______” (no ovulation.)
GnRH
Lactational Amenorrhea
_______ is a drug given orally (so it’s not a peptide) to treat hyperprolactemia. It is a ______ agonist and can cause ______ ______ via D2 receptor mediated vasodilation.
Cabergoline
Dopamine
Orthostatic Hypotension
GH can be used to treat growth failure in children with ______ _____ disease. However, Supraphysiological levels of GH can lead to diabetes and _____ cancer.
Chronic Kidney Disease
Colon
______ is an SST analog. It is used instead of SST bc it has a half-life of about _____hrs, while SST’s is about 1/2hr.
It can be given subQ (which allows for slow release) every _____hrs. It can cause AP adenomas to shrink in some patients, but it can also inhibit release of _____ and _____ (some patients with hyper- some with hypoglycemia). It also inhibits release of _____ –> leads to abdominal side effects, including nausea, diarrhea, and flatulence.
Though the mech is unknown, it can also lower portal HTN, so it’s used to treat esophageal _______.
Octreotide
1.5hrs
8hrs
Insulin
Glucagon
CCK
Varices
______, a dopaminergic agonist, can be given for the treatment of Acromegaly (high GH). It is effective in about _____% of patients not responding to Octreotide.
Cabergoline
50%
_______ is given subQ to treat Acromegaly (high GH). It acts via receptor antagonism (binds active site but does not activate the receptor). It has shown about 90% response when used in combo with ______.
Pegvisomant
Octreotide
Gonadorelin = synthetic _______. Therapeutically, it has to be administered via an infusion pump. Why?
GnRH
This is so it can mimic release of endogenous GnRH, which is pulsatile.
______ is a long-acting GnRH agonist, but bc it’s long-acting, it works to ______ (increase or decrease?) FSH and LH after an initial “flare” period (typically after a couple days.) It does so by causing down-regulation of GnRH receptors.
Leuprolide
Decrease
Because Leuprolide decreases FSH and LH, it can be given to treat _______ cancer in men. Just keep in mind it would have to be co-administered with an ______ antagonist at first, given the initial Leuprolide-induced “flare up” of FSH and LH. before receptor down-regulation.
Prostate cancer
Androgen antagonist
Leuprolide is also used to treat _______ in women, as it will decrease ______ levels, causing partial regression.
In combination with an _______ inhibitor, it may also be used to treat breast cancer.
It can also be used to treat ______ puberty.
Endometriosis
Estrogen
Aromatase inhibitor
Precocious Puberty
______ is a GnRH antagonist. It competitively inhibits GnRH. What advantage does this have over Leupirolide?
Ganirelix
It won’t cause the initial flare-up.
FSH and LH analogs are both used in treatment of infertility.
Recombinant FSH is more expensive than _____ _____ _____, which is isolated from the urine of post-menopausal women and is a combo of FSH and LH (these will be high in post-menopausal women bc no ovulation/menses).
Recombinant LH has a similar relationship to _____ _____ _____, which is isolated from placentas.
Human Menopausal Gonadotropin (hMG)
Human CHorionic Gonadotropin (hCG)
What is the big advantage to using a long-acting GnRH agonist vs a GnRH antagonist?
A missed dose of the long-acting agonist will not likely have adverse effects given it’s long action.
Desmopressin’s half-life is about ____hrs, compared to the 1/2hr half-life of Vasopressin. Also, although Desmopressin is a peptide, it can be given ______ (the small amount absorbed is enough to have the therapeutic effect.)
2hrs
Orally
