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Anterior & posterior

pituitary hormones

Dr. Karun Kumar


JR – III
Dept. of Pharmacology
What is a hormone ?
• Hormone (hormaein to stir up)
• is a substance of
• intense biological activity
• produced by specific cells in the body
• transported through circulation
• to act on its target cells
Growth hormone
• Acts on cell surface JAK-
STAT PKR
• Somatomedins or Insulin-
like growth factors (mainly
IGF-1, also IGF-2)
• Like insulin, IGF-1
promotes lipogenesis and
glucose uptake by muscles.
• GH acts directly as well to
induce lipolysis in adipose
tissue, gluconeogenesis
and glycogenolysis in liver
and decreased glucose
utilization by muscles
Use
1. Pituitary dwarfism
2. Constitutional short stature (only if epiphyses are
open)
3. Catabolic states (severe burns, bedridden
patients, chronic renal failure, osteoporosis, etc.)
4. AIDS related wasting
Abuse by athletes is banned, and it is one of the
drugs included in ‘dope testing’.
GH inh.(Somatostatin, Octreotide)

• Uses of Octreotide

1. Acromegaly

2. Secretory diarrhoeas associated with carcinoid,


AIDS, cancer chemotherapy or diabetes

3. Esophageal variceal bleeding


Bromocriptine (Actions)
1. ↓ Prl release from pituitary by activating
dopaminergic receptors on lactotrope cells
2. ↑ GH release in normal individuals, but ↓ GH in
pituitary tumours that cause acromegaly
3. Has levodopa like actions in CNS—
antiparkinsonian and behavioural effects.
4. Produces nausea and vomiting by stimulating
dopaminergic receptors in the CTZ.
5. Hypotension
6. ↓ GI motility
Uses
1. Hyperprolactinemia (microprolactinomas)
2. Acromegaly (small pit. tumours & inop. cases)
3. Parkinsonism
4. Diabetes mellitus (DM) [Adjunctive drug]
5. Hepatic coma (Arousal)

Cabergoline  Newer D2 agonist; more potent;


more D2 selective and longer acting (t½ > 60 hours)
FSH & LH
Uses

1. Amenorrhoea and infertility

2. Hypogonadotrophic hypogonadism in males

3. Cryptorchidism

4. To aid in vitro fertilization


GnRH analogues

• GnRH injected i.v.  ↑ LH & FSH (test HPG axis)

• ONLY pulsatile exposure to GnRH induces FSH/LH


secretion, continuous exposure desensitizes
pituitary gonadotropes (not used in hypogonadism)

• Eg. Goserelin, Leuprolide, Nafarelin, Triptorelin


Mechanism of action
Agonists act continuously & initially ↑ Gn secretion
After 1–2 weeks ↓
Desensitization and down regulation of GnRH receptors

Inhibition of FSH & LH secretion

Suppression of gonadal function

Spermatogenesis or ovulation cease & T/E levels ↓
Uses

1. Assisted reproduction technique (ART)

2. Uterine fibroids

3. Endometriosis

4. Central precocious puberty


Oxytocin (Actions)

1. Uterus  ↑ force & freq. of uterine contractions


Estrogens sensitize the uterus to oxytocin (↑ OR)

2. Breast  Contraction of myoepithelial cells (‘milk


ejection reflex’) is initiated by suckling

3. Kidney  Oxytocin in high doses exerts ADH-like


action
Uses

1. Induction of labour  Slow i.v. infusion: 5 IU is


diluted in 500 ml of glucose or saline solution

2. Uterine inertia

3. Postpartum haemorrhage, Caesarean section

4. Breast engorgement (Intranasal spray)


Oxytocin (DOC) v/s Ergometrine
1. Because of its short t½ and slow i.v. infusion,
intensity of action can be controlled and action
can be quickly terminated.
2. Low concentrations allow normal relaxation
inbetween contractions—foetal oxygenation does
not suffer.
3. Lower segment is not contracted: foetal descent
is not compromised.
4. Uterine contractions are consistently augmented