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Drugs for hypothalamic disorders Flashcards

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1
Q

What is the primary function of Gonadotropin-Releasing Hormone (GnRH)?

A

Activates pituitary GnRH receptors, influencing the secretion of gonadotropins (LH and FSH) from the anterior pituitary

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2
Q

What are the effects of continuous administration of GnRH?

A

Downregulates GnRH receptors, leading to decreased LH and FSH release and decreased sex hormone production

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3
Q

What therapeutic use does pulsatile administration of GnRH have?

A

Infertility treatment through stimulation of LH and FSH secretion, leading to ovulation in females and increased testosterone production in males

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4
Q

Name two clinical applications of GnRH analogs.

A
  • Prostate Cancer
  • Endometriosis
  • Uterine Fibroids
  • Precocious Puberty
  • Hormone-Sensitive Breast Cancer
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5
Q

What is Leuprolide?

A

A synthetic GnRH analog that acts as an agonist when given continuously, initially causing a transient increase in LH and FSH

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6
Q

List some side effects of Leuprolide.

A
  • Appetite decreased
  • Arthralgia
  • Bone pain
  • Depression
  • Dizziness
  • Fatigue
  • Gynecomastia
  • Hot flush
  • Insomnia
  • Sexual dysfunction
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7
Q

What is Goserelin used for?

A

Prostate cancer, breast cancer, endometriosis, and precocious puberty

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8
Q

What is the route of administration for Nafarelin?

A

Nasal spray

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9
Q

What does the ‘flare effect’ refer to in GnRH therapy?

A

Initial temporary rise in LH and FSH caused by GnRH analogs, which can exacerbate symptoms before eventual suppression

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10
Q

True or False: Continuous GnRH administration is used for infertility treatment.

A

False

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11
Q

What is the mechanism of action of GnRH analogs like Leuprolide and Goserelin?

A

Provides continuous GnRH stimulation, leading to reduced LH and FSH secretion

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12
Q

Fill in the blank: GnRH is a __________ peptide.

A

hypothalamic

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13
Q

What is the primary reason for using GnRH analogs in prostate cancer treatment?

A

To decrease testosterone levels, which can slow the growth of testosterone-sensitive prostate tumors

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14
Q

What is the purpose of using GnRH analogs in children with precocious puberty?

A

To delay puberty and ensure adequate final height by inhibiting gonadotropin release

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15
Q

What is the route of administration for Histrelin?

A

Subcutaneous implant that lasts for 12 months

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16
Q

What side effect is commonly associated with GnRH analogs?

A

Bone density loss

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17
Q

What is the effect of GnRH on gonadotropin release when administered in a pulsatile manner?

A

Stimulates gonadotropin release

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18
Q

What condition can GnRH analogs help alleviate symptoms for in women?

A

Endometriosis

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19
Q

What is the mechanism of action of anti-androgens like flutamide?

A

Blocks androgen (testosterone and DHT) receptors in prostate cells

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20
Q

What is the mechanism of action of ketoconazole in prostate cancer treatment?

A

Blocks testosterone synthesis directly in the testes

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21
Q

What is the role of 5-alpha reductase inhibitors in prostate cancer?

A

Blocks the conversion of testosterone to its more potent form, dihydrotestosterone (DHT)

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22
Q

What enzyme do aromatase inhibitors block in hormone-sensitive breast cancer treatment?

A

Aromatase

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23
Q

What hormone levels are decreased by GnRH analogs in the treatment of endometriosis?

A

Estrogen levels

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24
Q

What is the mechanism of action of GnRH analogs like leuprolide and goserelin?

A

They provide continuous GnRH stimulation, reducing LH and FSH secretion

These analogs downregulate GnRH receptors in the pituitary gland, leading to decreased estrogen production in the ovaries.

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25
What are the effects of lowered estrogen levels?
* Alleviate symptoms in endometriosis * Delay puberty in precocious puberty * Slow the growth of hormone-sensitive breast cancers
26
What do selective estrogen receptor modulators (SERMs) do?
They block estrogen receptors in certain tissues but do not reduce estrogen production ## Footnote Examples include tamoxifen and raloxifene.
27
What is the action of aromatase inhibitors?
They block the conversion of androgens to estrogen in peripheral tissues ## Footnote Examples include anastrozole, letrozole, and exemestane.
28
What conditions are aromatase inhibitors ineffective for?
* Endometriosis * Precocious puberty
29
What is the primary use of GnRH antagonists like ganirelix and cetrorelix?
They prevent premature LH surges in women undergoing ovarian stimulation.
30
What is the mechanism of action of GnRH antagonists?
They act as competitive antagonists at GnRH receptors in the pituitary gland.
31
What is the indication for degarelix?
Treatment of advanced prostate cancer in men.
32
What are the major side effects of GnRH antagonists?
* Hypersensitivity reactions * Anaphylaxis
33
What hormones do FSH and LH stimulate in females?
* FSH stimulates ovarian follicle maturation and estrogen production * LH induces ovulation and stimulates the corpus luteum to produce progesterone and androgens.
34
What is the purpose of administering menotropins?
Treatment of infertility and hypogonadism in men and women.
35
What preparations of FSH are available?
* Follitropin alfa * Follitropin beta * Urofollitropin
36
What is the role of chorionic gonadotropin in fertility treatment?
Induces ovulation after FSH administration.
37
What is the explanation for administering Ganirelix during IVF?
To prevent a premature LH surge.
38
True or False: Ganirelix increases the secretion of FSH and LH.
False
39
What is the action of estrogen receptor antagonists like fulvestrant?
They directly block estrogen receptors in breast tissue to prevent estrogen-driven tumor growth.
40
What does the term 'gonadotropins' refer to?
Hormones that stimulate the gonads, such as FSH and LH.
41
Fill in the blank: Aromatase inhibitors reduce estrogen production in _______ tissues.
peripheral
42
What is the function of FSH in males?
Stimulates spermatogenesis.
43
What is the effect of using GnRH agonists like leuprolide?
They stimulate the release of gonadotropins (LH and FSH).
44
What is the role of LH in males?
Stimulates Leydig cells in the testes to produce testosterone.
45
What is the role of Ganirelix?
It inhibits GnRH receptors in the pituitary ## Footnote Ganirelix is an antagonist, not blocking progesterone receptors.
46
What type of receptors do agonists at GnRH receptors initially stimulate?
LH and FSH release ## Footnote Agonists like leuprolide and goserelin cause initial stimulation before downregulation.
47
What is the function of Growth Hormone (GH)?
Stimulates lipolysis and antagonizes insulin to elevate blood glucose levels ## Footnote GH has direct and indirect actions on target organs.
48
What is IGF-1 and its role?
A protein produced in the liver and cartilage that stimulates skeletal growth, amino acid transport, protein synthesis, nucleic acid synthesis, and cell proliferation.
49
What stimulates the secretion of growth hormone?
Growth hormone-releasing hormone (GHRH) ## Footnote Secretion is inhibited by somatostatin.
50
What does excessive prolactin secretion cause?
Hyperprolactinemia, galactorrhea, hypogonadism, and infertility.
51
What is the use of Recombinant somatropin?
Idiopathic growth hormone deficiency, Turner syndrome, chronic renal failure, Prader-Willi syndrome ## Footnote It improves height velocity and final height.
52
What is the primary action of Somatostatin?
Inhibits the secretion of growth hormone and certain hormones of the pancreas, pituitary, and gastrointestinal tract.
53
What is the route of administration for Lanreotide?
Deep subcutaneous injection every 4 weeks.
54
What is Pegvisomant?
A pegylated growth hormone receptor antagonist ## Footnote It normalizes serum IGF-1 concentrations in 97% of persons with acromegaly.
55
What is the mechanism of action (MOA) of Cabergoline?
Stimulates dopamine receptors in the pituitary gland, inhibiting prolactin release.
56
What are common side effects of Cabergoline?
Nausea, dizziness, headache, and orthostatic hypotension.
57
What is the main function of Oxytocin?
Increases the strength of uterine contractions and causes milk ejection.
58
What triggers the release of Oxytocin?
Dilation of the uterine cervix, uterine contractions, or breast suckling.
59
What condition is characterized by excessive water excretion and increased water intake?
Diabetes insipidus.
60
What is desmopressin used for?
Treatment of diabetes insipidus, nocturnal enuresis, and certain bleeding conditions.
61
What does Conivaptan do?
Increases free water clearance and decreases urine osmolality by blocking V2 receptors.
62
What is the use of Tolvaptan?
Treatment of hypervolemic and euvolemic hyponatremia.
63
What are the side effects of Terlipressin?
Arrhythmias, abdominal cramps, diarrhea, peripheral ischemia ## Footnote It is associated with increased mortality from respiratory disorders.
64
What is the primary action of Vasopressin?
Causes vasoconstriction and has antidiuretic effects.
65
What is the mechanism of action of desmopressin?
It has potent antidiuretic activity but causes less vasoconstriction than natural vasopressin.
66
Fill in the blank: Growth hormone is also known as _______.
somatotropin.
67
True or False: Bromocriptine has a longer half-life than Cabergoline.
False.
68
What is the primary use of desmopressin?
Treatment of diabetes insipidus and nocturnal enuresis ## Footnote Desmopressin retains antidiuretic activity but has less vasoconstrictive effect.
69
What condition does cosyntropin help diagnose?
Adrenal insufficiency ## Footnote Cosyntropin is a synthetic corticotropin analog.
70
What is the mechanism of action of desmopressin?
Stimulates V2 receptors to concentrate urine ## Footnote Desmopressin is a synthetic analog of vasopressin.
71
What is the role of octreotide?
Used in the treatment of acromegaly, carcinoid syndrome, and pituitary adenomas ## Footnote Octreotide is a somatostatin analog.
72
Which drug is a growth hormone receptor antagonist used to treat acromegaly?
Pegvisomant ## Footnote Pegvisomant is a growth hormone analog.
73
List three gonadotropin preparations used to induce ovulation.
* Menotropins * Chorionic gonadotropin * Follitropin
74
What is the effect of goserelin and leuprolide?
Suppress gonadotropin secretion ## Footnote These are synthetic GnRH preparations administered continuously.
75
What is the function of dopamine agonists like cabergoline and bromocriptine?
Suppress prolactin secretion ## Footnote Hyperprolactinemia is often associated with galactorrhea and infertility.
76
True or False: Desmopressin is administered orally.
False ## Footnote Desmopressin is administered parenterally and intranasally.
77
What condition is treated with conivaptan and tolvaptan?
Hypervolemic and euvolemic hyponatremia ## Footnote These are arginine vasopressin receptor antagonists.
78
Fill in the blank: __________ is used to prevent postpartum uterine hemorrhage.
Oxytocin ## Footnote Oxytocin stimulates uterine contractions.
79
What is the primary indication for recombinant somatropin?
Growth hormone deficiency in children ## Footnote Recombinant somatropin is a growth hormone preparation.
80
What is the mechanism of action for the drug used to treat patients with syndrome of inappropriate antidiuretic hormone (SIADH)?
Stimulates V2 receptors in the kidney ## Footnote This action promotes water reabsorption and increases urine concentration.
81
Which hormone is used to treat endometriosis in women?
Nafarelin ## Footnote Nafarelin is a GnRH preparation administered as a nasal spray.
82
What is the purpose of using competitive GnRH receptor antagonists like ganirelix?
Treat prostate cancer and suppress premature LH surge ## Footnote These antagonists are used during ovulation induction.

Drugs for ENDOCRINE (2 decks)

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