Growth hormone releasing hormone (GHRH) analog

↑GH produced by pituitary gland.

Diagnostic test for GH response

Intermittent: ↑FSH/LH secretion

Continuous: ↓ FSH/LH secretion

Headache, light-headedness, nausea, ↓libido, ↓bone density

 Women: menopausal symptoms, depression, pain, vaginal dryness, breast atrophy, osteoporosis  

Men: gynecomastia, asthenia

Stimulation: infertility, diagnosis of LH responsiveness

 Suppression: prevent premature LH surge in controlled ovarian hyperstimulation, endometriosis, uterine leiomyomata, advanced prostate cancer, central precocious puberty

Intermittent: ↑FSH/LH secretion

Continuous: ↓ FSH/LH secretion

Headache, light-headedness, nausea, ↓libido, ↓bone density

Women: menopausal symptoms, depression, pain, vaginal dryness, breast atrophy, osteoporosis

Men: gynecomastia, asthenia

Stimulation: infertility, diagnosis of LH responsiveness

Suppression: prevent premature LH surge in controlled ovarian hyperstimulation, endometriosis, uterine leiomyomata, advanced prostate cancer, central precocious puberty

Agonist of GnRH receptors

Intermittent: ↑FSH/LH secretion

Continuous: ↓ FSH/LH secretion

Headache, light-headedness, nausea, ↓libido, ↓bone density

Women: menopausal symptoms, depression, pain, vaginal dryness, breast atrophy, osteoporosis

Men: gynecomastia, asthenia

Stimulation: infertility, diagnosis of LH responsiveness

Suppression: prevent premature LH surge in controlled ovarian hyperstimulation, endometriosis, uterine leiomyomata, advanced prostate cancer, central precocious puberty

Agonist of GnRH receptors

Blocks GnRH receptors

↓ production of LH and FSH

Nausea, headache

Prevention of premature LH surges during controlled ovulation hyperstimulation

Activate dopamine D₂ receptors

Suppress pituitary secretion of prolactin, dopaminergic effects on CNS motor control and behavior

orthostatic hypotension, headache, psychiatric disturbances, vasospasm and pulmonary infiltrates in high doses

Hyperprolactinemia, acromegaly

Parkinson’s disease

Activate dopamine D₂ receptors

Suppress pituitary secretion of prolactin, dopaminergic effects on CNS motor control and behavior

orthostatic hypotension, headache, psychiatric disturbances, vasospasm and pulmonary infiltrates in high doses

Hyperprolactinemia, acromegaly

Parkinson’s disease

Women: direct ovarian follicle development, conversion of androgens to estrogens by granulosa cells

Men: regulates spermatogenesis, converstion of testosterone to estrogen by Sertoli cells

Women: ovarian hyperstimulation syndrome (ovarian enlargement, hydrothorax, hypovolemia, shock) multiple pregnancies 

Men: gynecomastia

 headache, depression, edema

Women: anovulation (due to hypogonadotropic hypogonadism, polycystic ovary, obesity, etc.) controlled ovulation hyperstimulation (ART procedure)

 Men: infertility due to hypogonadism

Dimerization of GH receptors activates JAK/STAT pathway to ↑insulin-like growth factor 1 (IGF-1) production

Scoliosis, edema, gynecomastia, intracranial hypertension, myalgia, arthralgia, carpal tunnel syndrome, ↑CYP450 activity

↑ Height in children with GH-deficiency, Prader-Willi, Turner, small-for-gestational age

Wasting in AIDS

Short bowel syndrome

Recombinant form of IGF-1 that stimulates IGF-1 receptors

Hypoglycemia, intracranial hypertension, ↑liver enzymes

Replacement in IGF-1 deficiency not responsive to exogenous GH

Somatostatin analog

Inhibits production of GH and to a lesser extent, of glucagon, insulin, and gastrin

GI disturbances, gallstones, bradycardia (25%), and other cardiac conduction problems, vitamin B₁₂ deficiency

Hormone-secreting tumors: acromegaly and gigantism (GH-secreting adenomas), gastrinoma, glucagonoma, WDHA syndrome

Acute control of bleeding from esophageal varices

GH receptor antagonist

↑ liver enzymes

acromegaly

↑ uterine contractions

↑prostaglandins and leukotrienes  that augment uterine contraction;

Contraction of myoepithelial cells surrounding mammary alveoli for milk ejection

Fetal distress, placental abruption, uterine rupture, fluid retention, hypotension

Induction and augmentation of labor, control of uterine hemorrhage after delivery

Blocks oxytocin receptors; decreased uterine contractions

Concern about rates of infant death

Tocolysis for preterm labor

Activates both V1 & V2 receptors (G protein-coupled)

V1: vasoconstriction

V2: anti-diuresis, regulate release of factor VIII & vWF

CI: coronary artery disease due to ↑ vasoconstriction (but not desmopressin)

Rx: pituitary diabetes insipidus

Activates vasopressin V₂ receptors much more than V₁ receptors

 Acts in the kidney to ↓ excretion of water, acts on extrarenal V₂ receptors to ↑ factor VIII and von Willebrand factor

GI disturbances, headache, hyponatremia, allergic reactions

Pituitary diabetes insipidus

Hemophilia A and von Willebrand disease

Antagonist of vasopressin V₁ and V₂ receptors

↑ renal excretion of water in conditions associated with increased vasopressin

Infusion site reactions

Hyponatremia in hospitalized patients