PANCREATIC HORMONES & ANTIDIURETIC

Somatostatin

Octreotide is a drug used for the treatment of such
conditions as acromegaly, gastrinoma, and
glucagonoma. What Hormone is Octreotide an
analog of?

I and III

Which of the following is/are appropriate indications
for Oxytocin?
I. Control of Postpartum uterine bleeding
II. Stimulate initial milk production

■ Agonist (Somatropin, Mecasermin)
■ Antagonist (Octreotide, Pegvisomant)

Growth Hormone (GH)

■ Mixed LH and FSH (Menotropin)
■ LH Agonist (Lutropin, B hCG)
■ FSH Agonist (Urofollitropin, Follitropin alpha, Follitropin Beta)

Gonadotrophs

■ Agonist (Gonadorelin, Goserelin,Histrelin, Nafarelin, Leuprolide)
■ Antagonist
(Gonadorelix,Ganirelix,Degarelix,
Cetrorelix)

GnRH

Hormones

Are chemical messengers that circulates in the body fluids and produces specific effects on cells distant from the hormone's point or origin

Insulin and Glucagon

Pancreas (an endocrine gland) produces __________ and __________ and exert effects on adipose tissue or skeletal muscles distant to the pancreas

Exocrine gland

contains ducts, stimulate adjacent to an organ or themselves

Endocrine gland

do not have any ducts

○ Regulation of energy storage, production, and utilization
○ Adaptation to new environments or conditions of stress
○ Facilitation of growth and development
○ Maturation and function of reproductive system

Major functions (GGP)

GROUP I HORMONES

○ Acts via a nuclear receptors to modulate signal transduction in target
○ Steroid hormones, Thyroid hormones, Vitamin D

GROUP II HORMONES

○ Acts via a membrane receptor to exert rapid effect on signal transduction
○ Ex: GPCR (classified based on subunit like Gs, Gi, Gq), ion channels, cytokine receptors, receptor tyrosine kinase)
○ Peptide and amino acid hormones

PITUITARY GLAND

Aka master gland (and hypophysis) because it is directly involved in the production signals involved in the peripheral tissues

600 mg

Pituitary gland weight

Where is the pituitary gland located?

Sits on top the Sella Turcica = Holds and protects your PG

Anterior lobe (aka. Adenohypophysis) and Posterior lobe (aka. Neurohypophysis)

PG is consist of...

Anterior lobe

connected to the hypothalamus via a portal venous system and neurosecretory fibers

hypothalamus

Posterior lobe (P) pituitary hormones (Oxytocin and ADH) are synthesized in the

Hypothalamus

acts as your smart control coordinating center (keeps your body in a stable state)

Portal venous system (aka. Hypothalamic Pituitary Portal Venous System)

Your Anterior lobe is connected to the Hypothalamus via:

Neurosecretory Axons & Fibers

Posterior lobe is connected to the Hypothalamus via:

hypothalamus

Posterior pituitary hormones (Oxytocin and ADH) are synthesized in?

posterior pituitary gland

Posterior pituitary hormones (Oxytocin and ADH) are stored in?

Hypothalamus

facilitates the release of Anterior Pituitary Gland Hormones except prolactin

SOMATROPIN (recombinantGH) MOA

stimulates IGF-1 release in the liver and cartilage

SOMATROPIN (recombinantGH) USES

GH Deficiency (Genetic/Acquired), Idiopathic Short Stature, AIDS-associated wasting [almost all px=malnutrition], ↑ Athletic performance and ↑ muscle mass [banded in tournaments]

SOMATROPIN (recombinantGH) TOXICITY

○ CHILDREN: Pseudotumor cerebri, Slipped capital femoral epiphysis, Scoliosis, Edema
○ ADULTS: Peripheral edema, Myalgia (muscle pain), and Arthralgia (joint pain; not same with arthritis=has inflammation)

Turner Syndrome, Prader-Willi Syndrome

Examples of Genetic GH Deficiency

Prader-Willi Syndrome

deletion of chromosome 15 (short stature)

Turner Syndrome

Instead of 46XX chromosome, it's only 45XX (missing X; short stature)

● Presence or formation of tumor that can affect pituitary gland production
● Infection that can damage pituitary gland ⬇️GH

Examples of Acquired GH deficiency

MECASERMIN (rhIGF-1) MOA

mimics the action of IGF-1

MECASERMIN (rhIGF-1) USES

given to children unresponsive to GH therapy

MECASERMIN (rhIGF-1) TOXICITY

Hypoglycemia - Addressed by giving snacks prior to administration

OCTREOTIDE, LANREOTIDE

SOMATOSTATIN ANALOG

SOMATOSTATIN ANALOG (O, L) MOA

inhibits the release of GH, Glucagon, Insulin, Gastrin, Serotonin

SOMATOSTATIN ANALOG (O, L) USES

Acromegaly, GH-secreting pituitary adenoma, Carcinoid tumor, Gastrinoma, Glucagonoma

SOMATOSTATIN ANALOG (O, L) TOXICITY

GI disturbances, Gallstone, Arrhythmia

Acromegaly

excess GH production in adults

Carcinoid Tumor

excess secretion of serotonin

Gastrinoma

(pancreatic tumor) excess secretion of gastrin

Glucagonoma

(pancreatic tumor) excess secretion of glucagon

PEGVISOMANT MOA and USE

MOA: GH receptor antagonist
USES: Acromegaly

BROMOCRIPTINE

DOPAMINE (D2) RECEPTOR AGONIST

BROMOCRIPTINE MOA

inhibits prolactin release more than growth hormone

FOLLICLE-STIMULATING HORMONE (FSH),
LUTEINIZING HORMONE (LH)

GONADOTROPHS

Ovarian Follicle Development (egg cell) and Estrogen production

FSH IN WOMEN

Androgen production (progesterone and testosterone)

LH IN WOMEN

Primary regulator of spermatogenesis

FSH IN MEN

Main stimulus for testicular androgen production

LH IN MEN

MENOTROPIN

FSH AND LH MIXED ANALOGS

MENOTROPIN

Mixture of FSH and LH purified from the urine of
postmenopausal women

Follitropin alpha, Urofollitropin, Follitropin beta

FSH AGONIST

FSH AGONIST MOA

stimulates FSH Receptor (mimics endogenous FSH)

FSH AGONIST USES

Initiation of ovulation during controlled Ovarian
Hyperstimulation, Infertility secondary to
Hypogonadotropic hypogonadism

FSH AGONIST SE

HA, Ovarian hyperstimulation syndrome (Ovarian
enlargement, Ascites, Hypovolemic shock), Multiple
pregnancies, Gynecomastia (only in males)

Controlled Ovarian Hyperstimulation

protocol for female infertility

Hypogonadism

gonads do not produce your sex hormones,
secondary to a problem in the hypothalamus

Ascites

excessive bloating/ edema in the abdomen

LEUTROPIN, B hCG, CHORIOGONADOTROPIN

LH AGONIST

GONADOTROPIN-RELEASING HORMONE (GnRH)

Hypothalamic hormone that facilitates the release of
gonadotrophs

(+) FSH and LH

If GnRh is released through a Pulsatile secretion =

(-) FSH and LH

If GnRh is released through a Sustained secretion =

LEUPROLIDE, GOSERELIN,
GONADORELIN, HISTRELIN, NAFARELIN, TRIPTORELIN

GnRH AGONIST

GnRH AGONIST MOA

inhibits Gonadotropin (FSH & LH) release
through steady continuous dosing (sustained secretion)

GnRH AGONIST USES

Ovarian Suppression, Endometriosis, Uterine
leiomyomata (fibroids), Central Precocious puberty,
Advanced Prostate CA

GnRH AGONIST TOXICITY

Menopausal symptoms, Bone loss and
osteoporosis (estrogen is needed in normal bone homeostasis), ↓ libido

GnRH AGONIST

Can cause temporary exacerbation of prostate
cancer (tumor flare at first 10 days of administration)

Androgen Receptor Antagonist (Flutamide)

temporary exacerbation of prostate
cancer TX

(GANIRELIX, CETRORELIX,
ABARELIX, DEGARELIX)
Ends in -relix

GnRH ANTAGONIST

GnRH ANTAGONIST MOA

directly blocks GnRH receptor → (-)
gonadotropin release

GnRH ANTAGONIST USES

Controlled ovarian hyperstimulation, Advance
prostate CA

GnRH ANTAGONIST TOXICITY

Menopausal symptoms, Bone loss and
osteoporosis, Libido, Hypersensitivity reaction (Abarelix)

GnRH ANTAGONIST NOTE

since it is an antagonist, there is no temporary
exacerbation of symptoms (no tumor flare) for prostate
CA; no need for flutamide

PROLACTIN (PRL)

Major hormone responsible for Lactogenesis

Stimulates milk production in breast

inhibits ovulation in females and spermatogenesis in
males by inhibiting GnRH synthesis and release.
(Natural contraception)

(Bromocriptine, Pergolide, Cabergoline)

PROLACTIN ANTAGONIST

PROLACTIN ANTAGONIST MOA

(-) PRL release from the pituitary gland and
also (-) GH release

PROLACTIN ANTAGONIST USES

Hyperprolactinemia (PRL secreting pituitary
adenoma), Acromegaly, Parkinson's Disease
(primary use of Dopamine Agonists)

PROLACTIN ANTAGONIST TOXICITY

Nausea/Vomiting, GI disturbances,
Behavioral changes