PHRM 4430: Pituitary Hormones (GH and LH/FSH)

somatotropin

GH

Uses: short stature, muscle wasting

somatropin

rGH; recombinant GH

Uses: short stature, muscle wasting

mecasermin

rhIGF-1 (recombinant human insulin-like growth factor-1)

Uses: short stature, muscle wasting

mecasermin rinfabate

rhIGF1 + IGFBP-3 (recombinant human IGF-1 + IGF binding protein)

Uses: short stature, muscle wasting

semorelin

GHRH analogue

Uses: short stature, muscle wasting

Octreotide

Somatostatin analog; negative regulation of GH release from pituitary

Brand name: Sandostatin

Use: Acromegaly and tumors

ADR: gallstones, cardiac abnormalities, GI

Lanreotide

Somatostatin analog; negative regulation of GH release from pituitary

Use: block acromegaly and tumors

Parlodel/bromocriptine

D2 receptor agonist

Use:

• High doses block acromegaly (normally, dopamine stimulates GH in healthy, but in those with acromegaly, dopamine inhibits GH)

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Pegvisomant

GH receptor antagonist

Urofollitropin

FSH from urine of postmenopausal women (uFSH)

Use: helps infertility in conjunction with LH, trigger ovulation

Follitropin alfa and follitropin beta

Synthetic forms of FSH (recombinant) (rFSH)

• Similar to natural, just different carb side chains

Use: Fertility treatment in conjunction with LH

Lutropin alfa

Synthetic LH

Fertility treatment (IVF), diagnostic use for distinguishing between retained/undescended testes from retracted in prepubertal boys

Menotropins (Menopur)

Mixture of FSH/LH

Purified from urine of postmenopausal women

Use: Fertility treatments

rhCG

Recombinant human chorionic gonadotropin alfa

• Binds LH receptor and helps induce follicular development, ovulation, and stabilizes corpus luteum (which secretes estradiol/progesterone)

• Supports fertilized egg implantation and luteal phase

• Recombinant — more consistent, inc purity, high specific activity

Use: fertility treatment (final follicular development/ovulation)

Gonadorelin

Acetate salt of synthetic form of GnRH

Uses: ovarian hyperstimulation, infertility, ovarian cancer, endometriosis, prostate cancer, precocious puberty

Leuprolide

GnrH analogue

Uses: ovarian hyperstimulation, infertility, ovarian cancer, endometriosis, prostate cancer, precocious puberty

Histrelin

GnRH analogue

Uses: ovarian hyperstimulation, infertility, ovarian cancer, endometriosis, prostate cancer, precocious puberty

Nafarelin

GnRH analogue

Uses: ovarian hyperstimulation, infertility, ovarian cancer, endometriosis, prostate cancer, precocious puberty

Triptorelin

GnRH analogue

Uses: ovarian hyperstimulation, infertility, ovarian cancer, endometriosis, prostate cancer, precocious puberty

Goserelin

GnRH analogue

Uses: ovarian hyperstimulation, infertility, ovarian cancer, endometriosis, prostate cancer, precocious puberty

GnRH analogues

• Histrelin

• Goserelin

• Triptorelin

• Nafarelin

• Leuprolide

Ganirelix

GnRH antagonist

Use: ovarian hyperstimulation, prostate cancer

Cetrorelix

GnRH antagonist

Use: ovarian hyperstimulation, prostate cancer

Degarelix

GnRH antagonist

Use: men with prostate cancer