Hypothalamic and Pituitary Hormones

Question 1

Recombinant human GH

Acts through GH receptors to increase production of IGF-1 (liver and cartilage)

Answer 1

GROWTH HORMONE

Somatropin
Somatrem

Question 2

Indications of GH

Answer 2

for long term treatment in GH deficiency in children (DWARFISM)

for non GH deficient short children (2 cm/year)

promotes growth in children w/ Turner syndrome (XO) or chronic renal failure

helps combat AIDS-associated wasting syndrome

Question 3

Recombinant IGF-1

Answer 3

IGF-1 AGONIST

Mecasermin

for children unresponsive to GH therapy

Question 4

Somatostatin receptor agonist

Suppresses release of GH, glucagon, insulin, gastrin, IGF-1, serotonin, GI peptides

USES:
acromegaly
pituitary adenoma
variceal bleeding
gastrinoma
glucagonoma

Answer 4

SOMASTATIN ANALOG

Octreotide - 45x more potent than GHIH

Lanreotide - longer duration of action

Question 5

Blocks GH receptor signaling

USES:
acromegaly

Answer 5

GH RECEPTOR ANTAGONIST

Pegvisomant

Question 6

Activates Follicle-stimulating hormone (FSH) receptor

Mimics effects of endogenous FSH

USES:
controlled ovulation hyperstimulation in women

infertility d.t. hypogonadotropic hypogonadism in men

Answer 6

FSH RECEPTOR AGONIST

Follitropin alfa
Follitropin beta
Urofollitropin
Menotropins (hMG)

Question 7

Recombinant product w/ the same peptide sequence as follitropin alfa but differs in its carbohydrate side chains

Answer 7

Follitropin beta

Question 8

Human FSH purified from the urine of POSTmenopausal women

Answer 8

Urofollitropin

Question 9

Extract of the urine of postmenopausal women; contains both FSH and LH activity

Answer 9

Menotropin

Question 10

Activates LH receptor agonist

Mimics effects of endogenous LH

USES:
ovarian induction

ovarian follicle devt in women with hypogonadotropic hypogonadism

hypogonadotropic hypogonadism in men

Answer 10

LH ANALOGS

Human Chorionic Gonadotropin (hCG)
Choriogonadotropin alfa
Lutropin
Menotropins (hMG)

Question 11

Recombinant form of hCG

Answer 11

Choriogonadotropin alfa

Question 12

Recombinant form of human LH

Answer 12

Lutropin

Question 13

Extract of the urine of postmenopausal women; contains both FSH and LH activity

Answer 13

Menotropins (hMG)

Question 14

GnRH Receptor Agonist

PULSATILE - inc FSH and inc LH

CONTINUOUS - inc initially – dec sa last

USES:

ovarian suppression
controlled ovarian stimulation
central precocious puberty
advanced prostate cancer

Answer 14

GnRH ANALOGS

Leuprolide
Gonadorelin - synthetic human GnRH
Goserelin
Buserelin
Histrelin
Nafarelin
Triptorelin

Question 15

Antagonist of GnRH Receptors

USES:

prevention of premature LH surges during controlled ovarian stimulation

Answer 15

GnRH Receptor Antagonists
-RELIX

Ganirelix

Cetrorelix - similar to ganirelix, approved for controlled ovarian hyperstimulation

Degarelix, Abarelix -approved for advanced prostate cancer

SE:
hypersensitivity - Abarelix

Question 16

Dopamine D2 receptor agonist

USES:
hyperprolactinemia
pituitary adenoma (prolactin secreting)
Parkinson's disease
acromegaly

Answer 16

DOPAMINE AGONIST

Bromocriptine
Cabergoline
Pergolide
Quinagolide

Question 17

Oxytocin receptor agonist

USES:
induction and augmentation of labor
control of uterine hemorrhage after delivery

Answer 17

Oxytocin

Demoxytocin

Question 18

Antagonist of Oxytocin Receptor

USES:
tocolysis for preterm labor

Answer 18

OXYTOCIN RECEPTOR ANTAGONIST

Atosiban

Question 19

Agonist of Vasopressin V2 receptors

relatively selective for V2 receptors

USES:
central diabetes insipidus
hemophilia A
vWF disease
esophageal bleeding
primary nocturnal enuresis

Answer 19

VASOPRESSIN RECEPTOR AGONIST

Desmopressin

pituitary diabetes insipidus
hemophilia A and vWD

Vasopressin - for diabetes insipidus and control bleeding from esophageal varices

Question 20

Antagonist of vasopressin V1a and V2 receptors

USES:
SIADH
hyponatremia

Answer 20

VASOPRESSIN RECEPTOR ANTAGONIST

Conivaptan

Tolvaptan - more selective for vasopressin V2 receptors

Question 21

A young couple (25-year-old male, 23-year-old female) wants to start a family. They have not conceived after 1 year of unprotected intercourse. Infertility evaluation revealed no abnormalities in the female partner and low sperm count in the male. Which of the following is a drug that is purified from the urine of postmenopausal women and is used to promote spermatogenesis in infertile men?

(A) Desmopressin
(B) Gonadorelin
(C) Goserelin
(D) Somatropin
(E) Urofollitropin

Answer 21

(E) Urofollitropin

Spermatogenesis in males requires the action of FSH and LH.

Urofollitropin, which is purified from the urine of postmenopausal women, is used clinically to provide FSH activity

Question 22

A 29-year-old woman in her 41st week of gestation had been in labor for 12 h.
Although her uterine contractions had been strong and regular initially, they had diminished in force during the past hour. Which of the following agents would be used to facilitate this woman’s labor and delivery?

(A) Dopamine
(B) Leuprolide
(C) Oxytocin
(D) Prolactin
(E) Vasopressin

Answer 22

(C) Oxytocin

Question 23

A 3-year-old boy with failure to thrive and metabolic disturbances was found to have an inactivating mutation in the gene that encodes the growth hormone receptor. Which of the following drugs is most likely to improve his metabolic function and promote his growth?

(A) Atosiban
(B) Bromocriptine
(C) Mecasermin
(D) Octreotide
(E) Somatropin

Answer 23

(C) Mecasermin

This child’s condition is due to the inability of GH to stimulate the production of insulin-like growth factors, the ultimate mediators of GH effects. Mecasermin, a combination of recombinant IGF-1 and the binding protein that protects IGF-1 from immediate destruction, will help correct the IGF deficiency. Because of the inactive GH receptors, somatropin will not be effective.

Question 24

An important difference between leuprolide and ganirelix is that ganirelix

(A) Can be administered as an oral formulation
(B) Can be used alone to restore fertility to hypogonadal men and women
(C) Immediately reduces gonadotropin secretion
(D) Initially stimulates pituitary production of LH and FSH
(E) Must be administered in a pulsatile fashion

Answer 24

(C) Immediately reduces gonadotropin secretion

Leuprolide is an agonist of GnRH receptors, whereas ganirelix is an antagonist.

Although both drugs can be used to inhibit gonadotropin release, ganirelix does so immediately, whereas leuprolide does so only after about 1 week of sustained activity

Question 25

A 27-year-old woman with amenorrhea, infertility, and galactorrhea was treated with a drug that successfully restored ovulation and menstruation. Before being given the drug, the woman was carefully questioned about previous mental health problems, which she did not have. She was advised to take the drug orally. Which of the following is most likely to be the drug that was used to treat this patient? ``` (A) Bromocriptine (B) Desmopressin (C) Human gonadotropin hormone (D) Leuprolide (E) Octreotide ```

Answer 25

(A) Bromocriptine Bromocriptine, a dopamine receptor agonist, is used to treat the amenorrhea-galactorrhea syndrome, which is a consequence of hyperprolactinemia. Because of its central dopaminergic effects, the drug should not be used in patients with a history of schizophrenia or other forms of psychotic illness

Question 26

A 3-year-old girl was referred to the genetic counselor by her pediatrician. She presents with short stature (height is 85 cm, –3 standard deviations) and appears to have loose skin on her neck. Cytogenetic testing reveals an XO karyotype. Which of the following drugs will allow her to achieve a higher adult height? (A) Adrenocorticotropin (ACTH) (B) Corticotropin-releasing hormone (CRH) (C) Growth hormone-releasing hormone (GHRH) (D) Gonadotropin-releasing hormone (GnRH) (E) Somatropin

Answer 26

(E) Somatropin recombinant human GH, promotes growth in children with Turner syndrome (an XO genetic genotype) or chronic renal failure helps combat the AIDS-associated wasting syndrome

Question 27

A 3-year-old girl presented with hirsutism, breast enlargement, and a height and bone age that was consistent with an age of 9. Diagnostic testing revealed precocious puberty. Which of the following is the most appropriate drug for treatment of this patient’s precocious puberty? ``` (A) Atosiban (B) Follitropin (C) Leuprolide (D) Octreotide (E) Pegvisomant ```

Answer 27

(C) Leuprolide In precocious puberty, the hypothalamic-pituitary-gonadal axis becomes prematurely active for reasons that are not understood. Treatment involves suppressing gonadotropin secretion with continuous administration of a long-acting GnRH agonist such as leuprolide

Question 28

A 47-year-old man exhibited signs and symptoms of acromegaly. Radiologic studies indicated the presence of a large pituitary tumor. Surgical treatment of the tumor was only partially effective in controlling his disease. At this point, which of the following drugs is most likely to be used as pharmacologic therapy? ``` (A) Cosyntropin (B) Desmopressin (C) Leuprolide (D) Octreotide (E) Somatropin ```

Answer 28

(D) Octreotide a somatostatin analog, has some efficacy in reducing the excess GH production that causes acromegaly

Question 29

A 37-year-old woman with infertility due to obstructed fallopian tubes was undergoing ovulation induction in preparation for in vitro fertilization. After 10 d of treatment with leuprolide, the next step in the procedure is most likely to involve 10–14 d of treatment with which of the following? ``` (A) Bromocriptine (B) Follitropin (C) Gonadorelin (D) hCG (E) Pergolide ```

Answer 29

(B) Follitropin

Question 30

A 7-year-old boy underwent successful chemotherapy and cranial radiation for treatment of acute lymphocytic leukemia. One month after the completion of therapy, the patient presented with excessive thirst and urination plus hypernatremia. Laboratory testing revealed pituitary diabetes insipidus. To correct these problems, this patient is likely to be treated with which of the following? ``` (A) Corticotropin (B) Desmopressin (C) hCG (D) Menotropins (E) Thyrotropin ```

Answer 30

(B) Desmopressin Pituitary diabetes insipidus results from deficiency in vasopressin. It is treated with desmopressin, a peptide agonist of vasopressin V2 receptors

Question 31

SE of GH Agonists - Somatropin

Answer 31

``` Intracranial HPN Pseudotumor cerebri Slipped capital femoral epiphysis Scoliosis HYPERglycemia ```

Question 32

SE of GH Agonists - Mecasermin

Answer 32

HYPOglycemia increased LFT intracranial HPN

Question 33

Syndrome of POLYURIA, POLYDIPSIA and HYPERNATREMIA Excessive urination d.t. an inability of the kidney to resorb water properly from the urine

Answer 33

DIABETES INSIPIDUS Central - deficient secretion of ADH Nephrogenic - end organ resistance to the effects of ADH