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DERS Pharm > Hypothalamic and Pituitary Hormones > Flashcards

Hypothalamic and Pituitary Hormones Flashcards

1
Q
  • required during childhood and adolescence
  • Effects mediated mainly by IGF-1
  • Mediates effects via cell surface receptors that activate JAK/STAT signaling cascades
A

Growth Hormone: Somatotropin

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2
Q

Physiological effects of somatotropin

A
  • Stimulation of longitudinal growth of bones
  • Increased bone mineral density
  • Increased muscle mass (in GH deficient persons)
  • Increased GFR (Glomerular filtration rate)
  • Stimulation of preadipocyte differentiation into adipocytes
  • Anti-insulin actions (decreased glucose utilization & increased lipolysis)
  • Development & increased function of the immune system
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3
Q

Criteria for Diagnosis with growth hormone deficiency

A

(1) A growth rate < 4cm per year, and

(2) the absence of a serum GH response to two GH secretagogues

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4
Q

Recombinant growth hormones

A

Somatropin: Recombinant GH
Somatrem: GH analog

  • Active blood levels = persist for ~ 36 h
  • Given subcutaneously 3-7 times a week
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5
Q

Clinical Use of Recombinant Growth Hormone

A
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6
Q

Adverse effects of recombinant growth hormone in children

A
  • Scoliosis (during rapid growth)
  • Diabetic syndrome (chronic use)
  • Intracranial hypertension (rare)
  • Otitis media (increased risk for Turner Syndrome patients)
  • Pancreatitis, gynecomastia & nevus growth
  • Hypothyroidism
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7
Q

Adverse effects of recombinant growth hormone in adults

A
  • Peripheral edema, myalgias & arthralgias (hands & wrists especially)
  • Carpal tunnel syndrome
  • Proliferative retinopathy (rare)
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8
Q

Contraindications of Recombinant Growth Hormone

A
  • Cytochrome P450 inducer

* Patients with a known malignancy

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9
Q

IGF-1 deficiency in children is due mutations in gene that encodes for GH receptor and development of neutralizing antibodies to GH. Which drug should be used ?

A

IGF-1 Analog: Mecasermin: Complex of recombinant human IGF-1 and recombinant human IGF-binding protein-3

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10
Q

AE of mecasermin

A
  • Hypoglycemia (eat 20 minutes before or after administration)
  • Intracranial hypertension (rare)
  • Asymptomatic elevation of liver enzymes (rare)
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11
Q

Growth Hormone Secreting Tumors

A
  • Acromegaly (abnormal growth of cartilage, bone tissue, skin, muscle, heart, liver & GI tract)
  • Gigantism (if occurs before long bone epiphyses close)
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12
Q

Small GH-secreting adenomas can be treated with

A
  • GH receptor antagonists- Pegvisomant
  • Somatostatin analogs- Octreotide
  • Dopamine receptor agonists- Bromocriptine and Cabergoline

• Larger pituitary adenomas require surgery or radiation

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13
Q
  • Reduces symptoms caused by hormone-secreting tumors: acromegaly, carcinoid syndrome, gastrinoma, glucagonoma, nesidioblastosis, watery diarrhea, hypokalemia, achlorhydria syndrome & diabetic diarrhea.
  • Localizing neuroendocrine tumors
  • Acute control of bleeding from esophageal varices
A

Somatostatin Analog: Octreotide

  • 45x more potent in inhibiting GH release than somatostatin
  • 2x more potent in reducing insulin secretion
  • t 1⁄2 = ~ 80 min (30x somatostatin)
  • Octreotide acetate long-acting suspension can be given at 4-week intervals
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14
Q

AE OF Octreotide

A

*****Vit B 12 deficiency

  • Nausea, vomiting, abdominal cramps, flatulence, steatorrhea (with bulky bowel movements)
  • Constipation
  • Biliary sludge & gallstones (20-30% patients after 6-month use)
  • Sinus bradycardia (25%) & conduction disturbance (10%)
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15
Q

Treatment of hyperprolactinemis and acromegaly

A

Dopamine Agonists: Bromocriptine and Cabergoline
- Dopamine agonists shrink pituitary prolactin- secreting tumors, lower circulating prolactin levels, and restore ovulation in ~70% of women with microadenomas & ~30% with macroadenomas

  • Oral or as vaginal inserts
  • Bromocriptine t1/2 = ~7 h
  • Cabergoline t1/2 = ~65 h
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16
Q

AE OF Dopamine Agonists: Bromocriptine and Cabergoline

A
  • Nausea (bromocriptine>cabergoline), headache, light-headedness, orthostatic hypotension, fatigue
  • Psychiatric manifestations occasionally occur
  • High doses = cold-induced peripheral digital vasospasm • Chronic high-dosage therapy = pulmonary infiltrates
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17
Q

Gonadotropins in women

A

FSH: ovarian follicle development
• FSH & LH: ovarian steroidogenesis
• Luteal stage of menstrual cycle: estrogen & progesterone production is primarily under control of LH. (During pregnancy hCG takes over.)

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18
Q

Gonadotropins in men

A

• FSH: Spermatogenesis, conversion of testosterone to estrogen.
- Maintains high local androgen concentrations in vicinity of developing cells
• LH: Stimulus for production of testosterone

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19
Q

Act through GPCRs and is used for

  • ovulation induction
  • male infertility
  • female infertility
A

Gonadotropins

Male Infertility
• Treatment of hypogonadal men requires both FSH and LH.
- Treatment can consist of hCG alone or alternative protocols using urofollitropin, rFSH and rLH
• Stimulate spermatogenesis
Female Infertility: induce ovulation in women (IVF)

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20
Q

Gonadotropins

A
21
Q

AE OF GONADOTROPINS IN WOMEN

A
  • Ovarian hyperstimulation syndrome
  • Multiple pregnancies (15-20%)
  • Headache
  • Depression
  • Edema
  • Precocious puberty
22
Q

AE OF GONADOTROPINS IN MEN

A

Gynecomastia

23
Q

gonadotropin-releasing hormone
synthetic human GnRH
Given IV or SC
Half life of 4 mince

A

Gonadorelin

24
Q

gonadotropin-releasing hormone analogs
more potent & longer-lasting than gonadorelin
Given SC, IM, nasal spray (Nafarelin) or as SC implant

A

Gonadotropin analogs- Goserelin, leuprolide, nafarelin

25
Q

Continuous administration of Gonadotropin-Releasing Hormone & Analogs gives biphasic response:

A
  • First 7 days = agonist response ‘flare’

* Chronic effects (> 1 week) = inhibitory action (due to receptor down-regulation & changes in signaling pathways)

26
Q

Gonadotropin-Releasing Hormone & Analogs stimulates

A
  • Female infertility
  • Male infertility: In men with hypothalamic hypogonadotropic hypogonadism (pulsatile gonadorelin)
  • Diagnosis of LH responsiveness: Whether delayed puberty is due to constitutional delay or hypogonadotropic hypogonadism
27
Q

• Controlled ovarian hyperstimulation : Critical to suppress endogenous LH surge that could prematurely trigger ovulation

A

leuprolide, nafarelin

28
Q

Endometriosis: Pain often decreased by abolishing exposure to cyclical changes in estrogen & progesterone concentrations during menstrual cycle.
- Treatment limited to 6 months

A

(leuprolide, goserelin, nafarelin)

29
Q 
Uterine Leiomyomata (fibroids): - Can reduce fibroid size and combined with supplemental iron can
improve anemia
A

(leuprolide, goserelin, nafarelin)

30
Q

Prostate Cancer:
- Combined therapy with continuous GnRH agonist and an androgen receptor antagonist is effective as castration in reducing serum testosterone

A

(leuprolide, goserelin)

31
Q

Gonadotropin-Releasing Hormone & Analogs other suppression effects

A
  • Central Precocious Puberty (leuprolide, nafarelin)
  • Advanced Breast & Ovarian Cancer
  • Treatment of Amenorrhea in women with Polycystic Ovary Disease
  • Thinning of Endometrial lining: Preparation for endometrial ablation procedure in women with dysfunctional uterine bleeding
32
Q

Adverse effects of Gonadotropin-Releasing Hormone & Analogs

A
  • Headache, light-headedness, nausea, flushing
  • Swelling at SC injection site
  • Generalized hypersensitivity dermatitis (long-term administration)
  • Rare acute hypersensitivity reactions
  • Sudden pituitary apoplexy & blindness
33
Q

Adverse effects of Gonadotropin-Releasing Hormone & Analogs for continuous treatment

A

Women
• Menopausal symptoms (hot flushes, sweats, headaches)
• Depression, diminished libido, generalized pain, vaginal dryness & breast atrophy can occur
• Ovarian cysts (generally resolve)
• Reduced bone density & osteoporosis (long treatment)
Contraindications
- Pregnant and breast-feeding women

Men
• Hot flushes, sweats, edema, gynecomastia, decreased libido, decreased hematocrit, reduced bone density, asthenia, & injection site reactions

34
Q

These drugs suppress Gonadotropin Production: Prevent LH surge during controlled ovarian hyperstimulation

A

Cetrorelix, ganirelix = Competitive antagonists of GnRH receptors

35
Q

These drugs
- Act via MC2R (GPCR → cAMP) to stimulate adrenal cortex to secrete glucocorticoids, mineralocorticoids & androgen precursor
• Diagnostic tool for differentiating between primary adrenal insufficiency (Addison’s disease) and secondary adrenal insufficiency (inadequate ACTH secretion)
• Infantile spasm (West Syndrome) treatment

A

Corticotropin, cosyntropin = ACTH analogs

36
Q
  • Acts on GPCRs → stimulates release of prostaglandins & leukotrienes that augment uterine contraction
  • Small doses increase force & frequency of contractions
  • Higher doses evoke sustained contractions. Weak antidiuretic & pressor activity (vasopressin R activation)
  • Contraction of myoepithelial cells surrounding mammary alveoli → milk ejection
A

Oxytocin

  • IV: initiation & augmentation of labor
  • IM: control of postpartum bleeding
  • t1/2=5min
37
Q

Clinical applications of oxytocin

A

• Labor Induction: When early vaginal delivery is required
(Rh problems, maternal diabetes, preeclampsia, ruptured membranes)
• Augment Normal Labor: When labor is protracted or displays arrest disorder
• Control of uterine hemorrhage

38
Q

AE of oxytocin

A
  • Excessive stimulation of uterine contractions
  • Inadvertent activation of vasopressin receptors: Excessive fluid retention, water intoxication → hyponatremia, heart failure, seizure, death
  • Bolus injections can lead to hypotension: Administer IV as dilute solution at a controlled rate
39
Q

Oxytocin contraindications

A
  • Fetal distress
  • Prematurity
  • Abnormal fetal presentation
  • Cephalopelvic disproportion
  • Uterine rupture predisposition
40
Q

Oxytocin antagonist used for treatment of preterm labor

A

Atosiban

41
Q

Long-acting synthetic analog of vasopressin
Minimal V1 activity
Antidiuretic-to-vasopressor ratio 4000 x vasopressin

A

Desmopressin (Vasopressin (ADH) Agonists)

42
Q

V1R

A

vascular smooth muscle→vasoconstriction

43
Q

V2R

A

renal tubule cells→increased water permeability & water reabsorption

44
Q

Drugs of choice for Diabetes Insipidus

A

Vasopressin (ADH) Agonists

45
Q

Used for Esophageal variceal bleeding & colonic diverticular bleeding

A

Vasopressin

46
Q

Used for Coagulopathy treatment in Hemophilia A and von Willebrand’s disease

A

Desmopressin

47
Q

This drug is • Approved for use in patients with hyponatremia (due to elevated vasopressin)
• High affinity for V1 & V2 R’s

A

Conivaptan

48
Q

Adverse effects of vassopressin agonists

A
  • Headache, nausea, abdominal cramps, allergic reactions

* Overdosage = hyponatremia & seizures

DERS Pharm (9 decks)

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