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53 Cards in this Set
- Front
- Back
what are some FSH drugs
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a) Follitropin alfa
b) Follitropin beta c) Urofollitropin |
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what is a LH drug
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a) Lutropin alfa
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what is an hcg drug
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a) Choriogonadotropin alfa
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what are some gonadotropin releaseing hormone analogues
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a) Leuprolide (prototype)
b) Gonadorelin c) Goserelin d) Histrelin e) Nafarelin f) Triptorelin |
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what are some6) Gonadotropin-releasing hormone antagonists
a) |
Abarelix
b) Cetrorelix c) Degarelix d) Ganirelix |
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what are some dopamine agonists
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a) Bromocriptine
b) Cabergoline |
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(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
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is purified human FSH extracted from the urine of postmenopausal women (no LH activity)
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(1) Urofollitropin (uFSH
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(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
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are recombinant forms of FSH with amino acid sequences identical to that of human FSH
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(2) Follitropin alfa and follitropin beta (rFSH)
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what is the diff between rfsh and ufsh
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(3) rFSH preparations have a shorter half-life but stimulate estrogen secretion equal to or greater than uFSH (rFSH preparations are considerably more expensive)
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what are the clinical uses of FSH drugs
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(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) |
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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
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induce ovulation and pregnancy in anovulatory, infertile females; treatment of hypogonadotropic hypogonadism, prepubertal cryptorchidism; spermatogenesis induction with follitropin alfa
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extracted hcg
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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
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rhcg
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how are all gonadotropins administered
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IM or SQ
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what are the contraindications and toxicity
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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
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what is the prototypical Gnrh analogue
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leuprolide ( iv admin every 1-4 hours)
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what happens to the mech of action of leuptolide in the fist 7-10 days and then after that
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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)
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what is leuprolide that supresses used to treat
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(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 |
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what is leuprlide used for stimulation used to treat
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(1) Female infertility
(2) Male infertility (3) Diagnosis of LH responsiveness |
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v) Continuous GnRH agonist administration in men cause
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hot flushes, sweats, edema, gynecomastia, decreased libido, decreased hematocrit, reduced bone density, and asthenia
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i) Continuous treatment of women with a GnRH analog causes
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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
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what is moa of gnrh recpetor antagonist
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synthetic competitive antagonists of GnRH receptors that inhibit the secretion of FSH and LH in a dose-dependent manner
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what is the role of gnrh antagonist in prostate cancer
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ii) Advanced prostate cancer (GnRH antagonists reduce concentrations of gonadotropins and androgens significantly more rapidly than GNRH agonists and avoids the testosterone surge)
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d) Ganirelix and cetrorelix are used in
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controlled ovarian hyperstimulation procedures
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e) Abarelix and degarelix are used to
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treat advanced prostate cancer
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6) DOPAMINE AGONISTS
a) Bromocriptine and cabergoline are ergot derivatives used to treat |
hyperprolactinemia (bromocriptine is also used to treat acromegaly and Parkinson disease)
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i) Dopamine agonists are the standard medical treatment for
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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
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what are toxicities and contraindications of dopamine agonists
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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
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what is moa of oxytocin
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stimulates uterine muscle contraction after activating oxytocin receptors (G-protein coupled receptors linked to Gq, phosphoinositide-calcium second-messenger system)
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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
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what are toxicities assoc with oxytocin
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(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)
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ii) Anterior pituitary hormones are positively regulated by
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hypothalamic releasing hormones, which are released from hypothalamic neurons and reach the anterior pituitary through the hypothalamic-adenohypophyseal portal system
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iii) Anterior pituitary hormones are negatively regulated by
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hypothalamic peptides (somatostatin) and catecholamines (dopamine)
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where are hormones that are released by the post pit made
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hypothalamus
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i) Growth hormone (GH) and prolactin (PRL) are single-chain protein hormones that activate
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kinase-linked receptors of the JAK/STAT superfamily
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ii) Thyroid-stimulating hormone (TSH, thyrotropin), follicle-stimulating hormone (FSH), and luteinizing hormone (LH) are dimeric proteins that activate
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G-protein coupled receptors (GPCRs)
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iii) Adrenocorticotropic hormone (ACTH) is a single peptide, cleaved from a larger precursor containing the peptide β-endorphin, that also binds ____
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GPCRa
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ii) LH and FSH release is regulated by
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gonadotropin-releasing hormone
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iii) ACTH release is regulated by
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corticotropin-releasing hormone (CRH)
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i) TSH and TRH production is inhibited by
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thyroxine (tetraiodothyronine, T4) and triiodothyronine (T3)
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ii) FSH and LH (gonadotropins) and GnRH production is inhibited by
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estrogen and progesterone in women and androgens in men
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iii) ACTH and CRH production is inhibited by
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cortisol
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growth hormone Production is stimulated by growth hormone-releasing hormone (GHRH) and inhibited by
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the peptide somatostatin (SST)
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ii) GH and _____ feedback to inhibit GH release
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insulin-like growth factor-1 (IGF-1)
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(2) FSH stimulates the conversion of
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androgens to estrogens by granulosa cells
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(1) LH stimulates androgen production by
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theca cells in the follicular stage of the menstrual cycle
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iv) hCG is a placental protein nearly identical with LH and its actions are mediated through
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Lh receptors
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concentrations in the vicinity of developing sperm by stimulating
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the production of androgen-binding protein by Sertoli cells
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(2) FSH stimulates the conversion of testosterone to estrogen by
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sertoli cell
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g) Receptors selective for estrogens, progestins, and androgens are __ __
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nuclear receptors
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ii) LH is the main stimulus for the production of testosterone by
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leydig cells
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