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53 Cards in this Set

  • Front
  • Back
what are some FSH drugs
a) Follitropin alfa
b) Follitropin beta
c) Urofollitropin
what is a LH drug
a) Lutropin alfa
what is an hcg drug
a) Choriogonadotropin alfa
what are some gonadotropin releaseing hormone analogues
a) Leuprolide (prototype)
b) Gonadorelin
c) Goserelin
d) Histrelin
e) Nafarelin
f) Triptorelin
what are some6) Gonadotropin-releasing hormone antagonists
a)
Abarelix
b) Cetrorelix
c) Degarelix
d) Ganirelix
what are some dopamine agonists
a) Bromocriptine
b) Cabergoline
(a) Used in conjunction with hCG to induce ovulation and pregnancy in infertile females experiencing oligoanovulation or anovulation when the cause of anovulation is functional and not caused by primary ovarian failure
(b) Stimulation of multiple follicle development in ovulatory patients as part of an ART
menotropins
is purified human FSH extracted from the urine of postmenopausal women (no LH activity)
(1) Urofollitropin (uFSH
(1) Purified extract of FSH and LH extracted from the urine of postmenopausal women
(2) Contains an FSH-like substance (4% of the potency of FSH) and an LH-like substance
menotropins
are recombinant forms of FSH with amino acid sequences identical to that of human FSH
(2) Follitropin alfa and follitropin beta (rFSH)
what is the diff between rfsh and ufsh
(3) rFSH preparations have a shorter half-life but stimulate estrogen secretion equal to or greater than uFSH (rFSH preparations are considerably more expensive)
what are the clinical uses of FSH drugs
(a) Ovulation induction in patients who previously received pituitary suppression (uFSH)
(b) Ovulation induction in patients in whom the cause of infertility is functional and not caused by primary ovarian failure (rFSH alfa and beta)
(c) Spermatogenesis induction (rFSH alfa)
(d) Development of multiple follicles with ART (uFSH, rFSH alfa and beta)
recombinant form of human LH
(2) Only approved for use in combination with follitropin alfa for stimulation of follicular development in infertile women with profound LH deficiency
Lutropin
induce ovulation and pregnancy in anovulatory, infertile females; treatment of hypogonadotropic hypogonadism, prepubertal cryptorchidism; spermatogenesis induction with follitropin alfa
extracted hcg
induces ovulation in infertile females who have been pretreated with follicle stimulating hormones; induces ovulation and pregnancy in infertile females when the cause of infertility is functional
rhcg
how are all gonadotropins administered
IM or SQ
what are the contraindications and toxicity
Overstim of ovary> uncomplicated ovarian enlargement,Ovarian hyperstimulation syndrome: ovarian enlargement, ascites, hydrothorax, and hypovolemia, shock, Multiple pregnancies, Risk of multiple pregnancy is 15-20% in ART patients, Multiple preg incr the risk for gestational diabetes, preeclampsia, and preterm labor
what is the prototypical Gnrh analogue
leuprolide ( iv admin every 1-4 hours)
what happens to the mech of action of leuptolide in the fist 7-10 days and then after that
first 7-10 days of admin, an agonist effect results in increased concentrations of gonadal hormones (referred to as a flare), After the first 7-10 days, the continued presence of GnRH (or analog) results in an inhibitory action that manifests as a drop in the concentration of gonadotropins and gonadal steroids (due to receptor down-regulation and changes in the signaling pathways activated by GnRH)
what is leuprolide that supresses used to treat
(1) Controlled ovarian hyperstimulation (e.g., to prevent premature ovulation by endogenous LH in IVF patients)
(2) Endometriosis
(3) Uterine leiomyomata (uterine fibroids)
(4) Prostate cancer
(5) Central precocious puberty
what is leuprlide used for stimulation used to treat
(1) Female infertility
(2) Male infertility
(3) Diagnosis of LH responsiveness
v) Continuous GnRH agonist administration in men cause
hot flushes, sweats, edema, gynecomastia, decreased libido, decreased hematocrit, reduced bone density, and asthenia
i) Continuous treatment of women with a GnRH analog causes
menopause, which include hot flushes, sweats, and headaches, depression, diminished libido, generalized pain, vaginal dryness, breast atrophy, and decreased bone density and osteoporosis with long-term use If ovarian cysts do not resolve after 3-4 months
what is moa of gnrh recpetor antagonist
synthetic competitive antagonists of GnRH receptors that inhibit the secretion of FSH and LH in a dose-dependent manner
what is the role of gnrh antagonist in prostate cancer
ii) Advanced prostate cancer (GnRH antagonists reduce concentrations of gonadotropins and androgens significantly more rapidly than GNRH agonists and avoids the testosterone surge)
d) Ganirelix and cetrorelix are used in
controlled ovarian hyperstimulation procedures
e) Abarelix and degarelix are used to
treat advanced prostate cancer
6) DOPAMINE AGONISTS
a) Bromocriptine and cabergoline are ergot derivatives used to treat
hyperprolactinemia (bromocriptine is also used to treat acromegaly and Parkinson disease)
i) Dopamine agonists are the standard medical treatment for
hyperprolactinemia as they shrink pituitary PRL-secreting tumors, lower circulating PRL levels, and restore ovulation in 70% of women with microadenomas and 30% of women with macroadenomas
what are toxicities and contraindications of dopamine agonists
Nausea, headache, light-headedness, orthostatic hypotension, fatigue are most common, Psychiatric manifestations occur occasionally and can take months to resolve,Pulminfiltrates may occur with chronic high-dose therapy not recommended to suppress postpartum lactation due to increased incidence of stroke or coronary thrombosis
what is moa of oxytocin
stimulates uterine muscle contraction after activating oxytocin receptors (G-protein coupled receptors linked to Gq, phosphoinositide-calcium second-messenger system)
c) Stimulates the release of prostaglandins and leukotrienes that augment uterine contraction
d) Causes contraction of myoepithelial cells surrounding mammary alveoli, which leads to milk ejection
e) Indications include induction of labor at term; control of postpartum bleeding; adjunctive therapy in management of abortion
oxytocin
what are toxicities assoc with oxytocin
(toxicity that does occur is due either to excessive stimulation of uterine contractions or to inadvertent activation of vasopressin receptors at high concentrations of oxytocin)
ii) Anterior pituitary hormones are positively regulated by
hypothalamic releasing hormones, which are released from hypothalamic neurons and reach the anterior pituitary through the hypothalamic-adenohypophyseal portal system
iii) Anterior pituitary hormones are negatively regulated by
hypothalamic peptides (somatostatin) and catecholamines (dopamine)
where are hormones that are released by the post pit made
hypothalamus
i) Growth hormone (GH) and prolactin (PRL) are single-chain protein hormones that activate
kinase-linked receptors of the JAK/STAT superfamily
ii) Thyroid-stimulating hormone (TSH, thyrotropin), follicle-stimulating hormone (FSH), and luteinizing hormone (LH) are dimeric proteins that activate
G-protein coupled receptors (GPCRs)
iii) Adrenocorticotropic hormone (ACTH) is a single peptide, cleaved from a larger precursor containing the peptide β-endorphin, that also binds ____
GPCRa
ii) LH and FSH release is regulated by
gonadotropin-releasing hormone
iii) ACTH release is regulated by
corticotropin-releasing hormone (CRH)
i) TSH and TRH production is inhibited by
thyroxine (tetraiodothyronine, T4) and triiodothyronine (T3)
ii) FSH and LH (gonadotropins) and GnRH production is inhibited by
estrogen and progesterone in women and androgens in men
iii) ACTH and CRH production is inhibited by
cortisol
growth hormone Production is stimulated by growth hormone-releasing hormone (GHRH) and inhibited by
the peptide somatostatin (SST)
ii) GH and _____ feedback to inhibit GH release
insulin-like growth factor-1 (IGF-1)
(2) FSH stimulates the conversion of
androgens to estrogens by granulosa cells
(1) LH stimulates androgen production by
theca cells in the follicular stage of the menstrual cycle
iv) hCG is a placental protein nearly identical with LH and its actions are mediated through
Lh receptors
concentrations in the vicinity of developing sperm by stimulating
the production of androgen-binding protein by Sertoli cells
(2) FSH stimulates the conversion of testosterone to estrogen by
sertoli cell
g) Receptors selective for estrogens, progestins, and androgens are __ __
nuclear receptors
ii) LH is the main stimulus for the production of testosterone by
leydig cells