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Pharm #3 - Endocrine/Repro > Pharm #1 - Hypothalamus and Pituitary > Flashcards

Pharm #1 - Hypothalamus and Pituitary Flashcards

1
Q

Which two hormones act through the JAK/ STAT pathway?

A

GH and prolactin

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2
Q

What is the major target tissue of GH?

What are its 2 functions overall?

A

LIVER

2 basic functions
catabolic – on the fat cells –> lipolysis

anabolic - in MUSCLE cells and responsible for protein synthesis

(The effects of GH are primarily mediated by insulin-like growth factor 1 (IGF-1) released from liver in response to GH)

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3
Q

State the function of GH

  1. In childhood
  2. In adulthood
A

In childhood: Promotes linear growth (in 2 years of age), growth of long bones, cartilage, muscle, organ systems

In adulthood: Metabolic effects:
1. increases protein synthesis and bone density
promotes lipolysis and inhibits lipogenesis
promotes gluconeogenesis and glucose release
opposes insulin-induced glucose uptake in adipose tissue
reduces insulin sensitivity.
GH is released in a pulsatile manner, mostly during sleep.
Pulses are generated by interplay of GHRH and Somatostatin (GH inhibitor)

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4
Q

State the following drug names used in GH deficiency:

  1. Synthetic GHRH
  2. Recombinant GH
  3. Recombinant IGF1
A
  1. Synthetic GHRH
    Sermorelin (used if defective GHRH release but normally functioning anterior pituitary somatotrophs)
  2. Recombinant human growth hormone
    Somatropin
    Somatrem
  3. Recombinant IGF1
    Mecasermin (used in children where IGF1 deficiency is due to mutations of GH receptor- Laron dwarfism or development of neutralizing antibodies against GH.
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5
Q

What drug is used in baron dwarfism?

A

Mecasermin

used in children where IGF1 deficiency is due to mutations of GH receptor-

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6
Q

What drug can be used for short bowel syndrome in patients receiving specialized nutritional support?

A

Somatropin, Somatrem

  • recombinant human GH

ALSO used for:

Documented growth failure in pediatric patients associated with:
GH deficiency, chronic renal failure, Prader-Willi syndrome, Turner syndrome
Small-for-gestational-age condition with failure to catch up by age 2
Idiopathic short stature, non GH-deficient (>2.25 S.D. below mean height for age/sex)

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7
Q

What are the 6 main side effects of somatropin, sometime?

A
  1. Leukemia
  2. rapid growth of melanocytic lesions
  3. hypothyroidism*
  4. Insulin resistance
  5. Arthralgia (joint pain)
  6. increase in cytochrome P450 activity (can reduce the serum level of drugs)
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8
Q

What are the contraindication of SOmatropin and sometime? (4)

A

Contraindications:

  1. Pediatric patients with closed epiphyses (long bones already closed)
  2. Active underlying intracranial lesion
  3. Active malignancy
  4. Proliferative diabetic retinopathy
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9
Q

Somatropin and sometime should definitely NOT be used in what disease?

A

Diabetes

  • insulin action is non-functioning and GH increases glucose
  • would result in hyperglycemia
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10
Q

For the treatment of Smaller pituitary adenomas:
A) Somatostatin analogues
- state 2

B) GH receptor antagonist
Pegvisomant

C) Dopamine receptor agonist

A
  1. Octreotide
  2. Lanreotide (in Europe)

Pegvisomant

Bromocriptine

Larger adenomas need surgery

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11
Q

What drug is used for the following:

  1. used to control pituitary adenoma growth in acromegalic patients
  2. Carcinoid crisis- flushing, diarrhea and all symptoms of carcinoid syndrome
  3. Secretory diarrhea from vasoactive intestinal peptide (VIP)-secreting tumors.
  4. To control acute GI bleeding
A

OCTREOTIDE

  • somatostatin analog

synthetic long-lasting peptide analogue of somatostatin (45 times more potent)

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12
Q

What drug can cause sinus bradycardia, conduction disturbances, and gallstones and hypoglycemia?

A

Side Effects of Octreotide

  1. Nausea, vomiting, abdominal cramps, GI discomfort
  2. Cardiac effects-sinus bradycardia and conduction disturbances
  3. Hypoglycemia
  4. Gallstones

Contraindications:
Hypersensitivity to octreotide

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13
Q

Cyclosporine levels are inc/dec with octreotide?

Bromocriptine bioavailability is inc/dec with octreotide?

A

Decreased

INCREASED

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14
Q

MOA of pegvisomant?

A

Pegvisomant: GH receptor antagonist, recombinant protein of 191 amino acid residues.

Pegvisomant does not bind appropriately to the second GH receptor - blocks signal transduction and acts as a competitive antagonist of GH activity

  • NO receptor dimerization of GH!!! (blocks it)
  • decreases serum IGF-1 levels
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15
Q

Indication of Pegvisomant

2 main side effects

A

Drug Indications:
used for the treatment of acromegaly that is refractory to other modes of surgical, radiologic, or pharmacologic intervention.

  1. Increased pituitary adenoma size
  2. Elevated serum aminotransferase levels

Therapeutic Considerations:
Patients should have yearly MRI to exclude enlarging adenoma
Liver function tests should be performed periodically

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16
Q

Main function of FSH in women___

Main function of FSH in men?

A

ovarian follicle development

Spermatogenesis

In the follicular stage of the menstrual cycle, LH stimulates androgen production in the ovary (Thecal cells), whereas FSH stimulates conversion of androgens to estrogens (Granulosa cells).

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17
Q

In the luteal phase, estrogen and progesterone production is primarily controlled by ___, and during pregnancy controlled by hCG (human chorionic gonadotropin) produced by the placenta.

A

LH

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18
Q

MEN:

___ stimulates production of testosterone by the testicular Leydig cells
In Sertoli cells

___ produces androgen binding protein, which helps to maintain high testicular levels of testosterone.

A
  1. LH

2. FSH

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19
Q

______ are obtained from the urine of menopausal women and contain FSH and LH

____ is a placental hormone and an LH agonist

______ is purified FSH isolated from the urine of postmenopausal women

_____ is a recombinant from of human FSH

FX of all?

A
  1. Menotropins
  2. hCG
  3. Urofollitropin
  4. Follitropin

MOA: replace FSH and LH

20
Q

Drug indications for Gonadotropin stimulants

A

Drug Indications:

  1. Ovulation induction in women with anovulation due to hypogonadotropic hypogonadism,
  2. polycystic ovary syndrome
  3. obesity

Controlled ovarian hyperstimulation in assisted reproductive technology procedures (example IVF)

  1. Infertility in male
  2. hypogonadotropic hypogonadism
21
Q

SIDE EFFECTS of Gonadotropin stimulators (4, 1 main)

A
  1. Ovarian hyperstimulation syndrome (associated with ovarian enlargement, ascites, hydrothorax, hypovolemia, sometimes resulting in shock)
  2. Increase in multiple pregnancies (15-20% chance)
  3. Increased risk of gynecomastia in men
  4. Ovarian cancer
  5. Ovarian cysts and hypertrophy
22
Q

___ is a synthetic human GnRH

MOA

A

Gonadorelin

Mechanism of Action:

Pulsatile GnRH secretion or Gonadorelin stimulate the gonadotroph cells to produce and release LH and FSH (Stimulation of gonadal axis): mimicking physiology

23
Q

3 indications for Gonadorelin

3 side effects

A
  1. Mostly for diagnosis of hypogonadism
  2. Stimulate Ovulation (less cost effective, occasional use)
  3. Infertility in men with hypothalamic hypogonadotropic hypogonadism (less cost effective, occasional use)

SIDE EFFECTS:
1.Anaphylaxis with multiple administrations

  1. Lightheadedness, flushing
  2. Generalized hypersensitivity dermatitis
24
Q

What drug is used for the diagnosis of hypogonadism?

A

Gonadorelin

25
Q

Sustained GnRH agonists result in what?

What are drugs that fall in this category? (5)

A

Sustained, nonpulsatile administration of GnRH or GnRH analogs inhibits the release of FSH and LH in both men and women –
(Inhibition of gonadal axis).
Desensitizes GnRH receptors

  1. Goserelin
  2. Histrelin
  3. Leuprolide
  4. Nafarelin
  5. Triptorelin

-More potent and longer-lasting than native GnRH or gonadorelin

26
Q

What is the result of goserelin, histrelin, leuprolife, nafarelin, triptorelin?

A

Produces biphasic response:

  1. first there is a transient (7-10 days) increase in gonadal hormone levels (flare) – agonist effect
  2. followed by a long-lasting suppression of gonadotropins and gonadal hormones – inhibitory action
27
Q

What drugs are used for the following:

  1. To keep the LH surge low in controlled ovarian hyperstimulation that provides multiple mature oocytes for assisted reproductive technologies (like IVF)
  2. Endometriosis & Uterine fibroids
  3. Adjunctive in prostate cancer
  4. Central precocious puberty
A
  1. leuprolide, nafarelin
  2. Leuprolide, nafarelin, goserelin
  3. Leuprolife goserelin, histrelin, triptorelin
  4. Leuprolide, nafarelin
28
Q

side effects of GnRH sustained agonists
(5)

Contra (3)

A
  1. Hot flashes, sweats, headache (symptoms of menopause)
  2. Osteoporosis (monitoring) – estrogen needed for bone density
  3. Urogenital atrophy
  4. Temporary worsening of precocious puberty during the initial weeks of treatment

CONTRA:

  1. Hypersensitivity to GnRH or GnRH analogs
  2. Pregnancy
  3. Breast feeding
29
Q

3 drugs to inhibit gonadal axis

A

Ganirelix,
Cetrorelix and
Abarelix are used to inhibit gonadal axis

NO X’s for sex

  • Ganirelix and Cetrorelix produce immediate antagonistic effect, and so their duration of administration during IVF is shorter compared to GnRH agonists.
30
Q

Ganireliz, Ceftrorelix, Abarelix

MOA

  • key point
A

They function as competitive antagonists of GnRH receptors

Inhibits the secretion of FSH and LH in a dose dependent manner

Does not produce the flare effect (increased FSH/LH) as GnRH agonists

31
Q

Drug for metastatic prostate cancer in patients with extensive metastases

A

Abarelix

32
Q

___ and ___ keeps LH surge low in controlled ovarian hyperstimulation for assisted reproductive technologies (such as IVF), resulting in improved rates of implantation and pregnancy

A

Ganirelix

Ceftrorelix

33
Q

SE of GnRH antagonists

Ganirelix, Ceftrorelix, Abarelix

A

Side Effects:

  1. ovarian hyperstimulation syndrome
  2. QT interval prolongation (abarelix)
  3. Ectopic pregnancy,
  4. thrombotic disorder,
  5. spontaneous abortion (ganirelix)
  6. Anaphylaxis (cetrorelix)
34
Q
  1. drug that causes anaphylaxis
A
  1. Ceftrorelix
35
Q
  1. drug that causes spontaneous abortion
A

Ganirelix

36
Q
  1. drug that prolongs QT
A

Abarelix

37
Q

____ inhibits prolactin secretion

____ increases prolactin secretion

A
  1. dopamine
  2. TRH

Prolactin does-not stimulate hormone secretion in its target organ (mammary gland) and so there is no negative feedback regulation.

Increased estrogen levels during pregnancy stimulate prolactin release. However, during pregnancy estrogen antagonizes prolactin action in the breast, thus preventing lactation until after parturition.

38
Q

Increased prolactin inhibits ____ release and estrogen synthesis, suppressing ovulation during lactation.

A

GnRH

Prolactin: Regulates mammary gland development, milk protein biosynthesis and secretion.

39
Q

State the 4 dopamine receptor agonists

Indications?

A
  1. Bromocriptine
  2. Cabergoline
  3. Pergolide
  4. Quinagolide

Indications:

Amenorrhea, galactorrhea, infertility from hyperprolactinemia, premenstrual syndrome (Bromocriptine, Cabergoline)

Acromegaly:- requires high doses, and effective only if pituitary tumor secretes both prolactin and GH; otherwise combination therapy with Octreotide is effective (Bromocriptine)

Parkinson’s disease (Bromocriptine, Pergolide, Cabergoline)

40
Q

3 drugs for parkinson

A
  1. bromocriptine
  2. pergolide
  3. carbegoline
41
Q

SE of Dopamine receptor agonists

A
  1. Orthostatic hypotension
  2. Cerebral vascular accident, seizure, acute myocardial infarction (Bromocriptine)
  3. Arrhythmia, myocardial infarction, heart failure (Pergolide)
  4. Pulmonary fibrosis and pleural effusion (Cabergoline)
42
Q

Drug that causes pulmonary fibrosis and pleural effusion

A

Cabergoline

  • dopamine agonist for prolactinoma
43
Q

Drug that causes:Arrhythmia, myocardial infarction, heart failure

A

Pergolide

  • makes your heart pur
  • dopamine agonist
44
Q

Drug that causes cerebral vascular accident, seizure, and acute MI

A

Bromocriptine

45
Q

3 contra for dopamine agonists

A

Hypersensitivity to ergot derivatives

Uncontrolled hypertension

Toxemia of pregnancy (Bromocriptine)

Pharm #3 - Endocrine/Repro (3 decks)

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