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Chapter 26: Introduction to Endocrinology: The Hypothalamic–Pituitary Axis

INTRODUCTION

This chapter will be most useful after having a basic understanding of the material in Chapter 38, Introduction to Endocrinology: The Hypothalamic Pituitary Axis in Goodman & Gilman’s The Pharmacological Basis of Therapeutics, 12th Edition. In addition to the material presented here, the 12th Edition includes:

  • A detailed discussion of the hypothalamic-pituitary-endocrine axis

  • A description of the pituitary hormones and their releasing factors

  • A discussion of the therapy of growth hormone (GH) deficiency

  • A discussion of the glycoprotein hormones: thyroid stimulating hormone (TSH) and gonadotropins

  • A discussion of the posterior pituitary hormones: oxytocin and vasopressin

LEARNING OBJECTIVES

  • Understand the functioning of the hypothalamic-pituitary axis.

  • Describe the pharmacotherapy of GH excess and GH deficiency.

  • Develop knowledge of the clinical uses of gonadotropin-releasing hormone (GnRH) and its analogs.

DRUGS INCLUDED IN THIS CHAPTER

Bromocriptine (PARLODEL, CYLOSERT, others)

Cabergoline (CABERLIN, DOSTINEX, CABASER)

Cetrorelix (CETROTIDE)

Choriogonadotropin alfa (OVIDREL)

Follitropin α (GONAL-F)

Follitropin β (FOLLISTIM, PUREGON)

Ganirelix (ANTAGON)

Gonadorelin (FACTREL, LUTREPULSE)

Goserelin (ZOLADEX)

Histrelin (VANTAS, SUPPRELIN LA)

Lanreotide (SOMATULINE LA, SOMATULINE DEPOT)

Leuprolide (LUPRON, ELIGARD)

Lutropin alfa (LUVERIS, LHADI)

Mecasermin (INCRELEX)

Menotropins (REPRONEX)

Nafarelin (SYNAREL)

Octreotide (SANDOSTATIN, SANDOSTATIN-LAR DEPOT)

Oxytocin

Pegvisomant (SOMAVERT)

Pergolide (PERMAX)

Quinagolide (NORPROLAC)

Recombinant human growth hormoneGH (ACCRETRTROPIN, GENOTROPIN, HUMATROPE, NORDITROPIN, NUTROPIN, OMNITROPE, SAIZEN, SERPSTIM, TEV-TROPIN, ZORBTIVE, NUTROPINE DEPOT)

Triptorelin (TRELSTAR DEPOT LA)

Urine-derived human chorionic gonadotropin (hCG; NOVAREL, PREGNYL, PROFASI)

Urofollitropin (uFSH; BRAVELLE, MENOPUR)

MECHANISMS OF ACTION OF DRUGS THAT ACT ON THE HYPOTHALAMIC-PITUITARY AXIS
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MECHANISMS OF ACTION OF DRUGS THAT ACT ON THE HYPOTHALAMIC-PITUITARY AXIS
DRUG CLASS DRUG MECHANISM OF ACTION
Somatostatin (SST) Analogs Octreotide SST analog that inhibits the release of GH from the pituitary (see Figures 26-1 and 26-2)
Lanreotide SST analog that inhibits the release of GH from the pituitary (see Figures 26-1 and 26-2)
Growth Hormone (GH) Antagonist Pegvisomant GH receptor antagonist (see Figure 26-3)
Dopamine (DA) Receptor Agonists Quinagolide DA receptor agonist; inhibits release of prolactin (see Figure 26-4)
Bromocriptine DA receptor agonist; inhibits release of prolactin (see Figure 26-4)
Cabergoline DA receptor agonist; inhibits release of prolactin (see Figure 26-4)
Recombinant GH Recombinant GH Binds to GH receptor (see Figure 26-3)
Insulin-like Growth Factor-1 (IGF-1) Mecasermin Mimics effects of GH (see Figure 26-2)
Gonadotropin-Releasing Hormone (GnRH) Agonists GnRH Signals through a specific GPCR on gonadotropic cells in the anterior pituitary to release follicle-stimulating hormone (FSH) and luteinizing hormone (LH) (see Figure 26-5)
Goserelin GnRH agonist
Naferelin GnRH agonist
Triptorelin GnRH agonist
Histrelin GnRH agonist
Leuprolide GnRH agonist
GnRH Antagonists Cetrorelix Antagonizes the effect of GnRH on gonadotropic cells
Ganirelix Antagonizes the effect of GnRH on gonadotropic cells
Follicle-Stimulating Hormone (FSH) Menotropin FSH preparation that acts on the FSH receptor
Urofollitropin (uFSH) FSH preparation that acts the FSH receptor
Follitropin α Recombinant FSH that acts on the FSH receptor
Follitropin ...

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