How do somatostatin analogues work in acromegaly?

How do somatostatin analogues work in acromegaly?

The most extensively studied and used somatostatin analogue, octreotide, binds to the somatostatin receptor subtypes II and V, inhibiting GH secretion. Octreotide suppresses the serum GH level to less than 2.5 mcg/L in 65% of patients with acromegaly and normalizes circulating IGF-I levels in 70% of patients.

Why is somatostatin used in acromegaly?

Biology of somatostatin and somatostatin analogs In vitro, native somatostatin retains its inhibitory effect on GH secretion in many GH-secreting tumors, and this led to the development of analogs of somatostatin for clinical use in the treatment of acromegaly (4).

How are somatostatin analogues?

Initial dose and dose adjustment of somatostatin analogues (1) The initial dose of octreotide long-acting release (LAR) is 20 mg, administered by intramuscular injection at 4-week intervals.

What is the mechanism of action of octreotide?

Octreotide binds to somatostatin receptors coupled to phospholipase C through G proteins and leads to smooth muscle contraction in the blood vessels.

How does octreotide help acromegaly?

Octreotide acts through four mechanisms to decrease abnormal GH secretion in acromegaly. First, octreotide suppresses GH secretion from the pituitary gland and from GH-secreting adenomas. Second, it decreases GH binding to hepatocytes. Third, it inhibits hepatic IFG-1 production and finally it controls tumour growth.

What is the mechanism of action of somatostatin analogues?

Mechanisms of action of Somatostatin synthetic Analogs (SSAs). (A). The antisecretory effects occur through the inhibition of the enzyme adenylyl cyclase (AC), the inhibition of voltage-dependent calcium channels and the stimulation of voltage-dependent potassium channels.

How can I activate my pituitary gland naturally?

Here are 11 evidence-based ways to increase human growth hormone (HGH) levels naturally.

1. Lose body fat.
2. Fast intermittently.
3. Try an arginine supplement.
4. Reduce your sugar intake.
5. Don’t eat a lot before bedtime.
6. Take a GABA supplement.
7. Exercise at a high intensity.
8. Take beta-alanine and/or a sports drink around your workouts.

Are there any other analogues of somatostatin?

Lanreotide, another somatostatin analogue, became available in the mid-1990s initially as a prolonged-release formulation administered every 10 or 14 days.

Are there any side effects to depot somatostatin?

The side effects of depot somatostatin analogs are similar to those of short-acting octreotide (Table 3; Refs. 7, 35, 37, 38 – 47, 59). The most common side effects are gastrointestinal with up to half of patients initially experiencing diarrhea, nausea, or abdominal discomfort, but in most patients these are transient.

How often can I take octreotide in somatostatin SC form?

Importantly also, in somatostatin analog responsive patients, the suppressive effect on GH secretion does not wane with time. The typical dose of octreotide in its sc form is 100–250 μg thrice daily, but doses up to 1500 μg over a 24-h period can be given ( 18 ).

What is the role of GH in acromegaly?

Gastroenteropancreatic neuroendocrine tumours (GEP-NET) constitute a heterogeneous group o … Acromegaly is a hormonal disorder that arises when the pituitary gland secretes excess growth hormone (GH), which in turn stimulates a concomitant increase in serum insulin-like growth factor 1 (IGF-1) levels.