Somatostatina
Somatostatina Uses, Dosage, Side Effects, Food Interaction and all others data.
Somatostatina is a polypetide obtained synthetically or from the hypothalamus. It acts by inhibiting the release of growth hormone from the anterior pituitary. It also inhibits the release of thyrotrophin and corticotropin from the pituitary, glucagon and insulin from the pancreas. It also regulates duodenal and gastric secretions. It may also play a role in pain perception.
Somatostatina is an endogenous peptide hormone that is secreted by the central nervous system, gastrointestinal tract, retina, peripheral neurons and pancreatic D cells of the islets of Langerhans. It exhibits several biological roles but predominantly exerts an inhibitory effect on secretion of other hormones and transmitters . While distribution of two active isoforms of somatostatin is similar, SST-14 is more predominant in the enteric neurons and peripheral nerves whereas SST-28 is more prominent in the retina and intestinal mucosal cells .
Anterior pituitary gland and brain: It inhibits the release of growth hormones and thyroid-stimulating hormones, such as thyroid stimulating hormone (TSH) and thyrotrophin, from the anterior pituitary while inhibiting the release of dopamine from the midbrain, norepinephrine, TRH and corticotrophin-releasing hormone in the brain .
Pancreas: In the pancreas, somatostatin reduces the secretion of glucagon and insulin as well as bicarbonate ions and other enzymes .
| Trade Name | Somatostatina |
| Generic | Somatostatin |
| Somatostatin Other Names | Somatostatin, Somatostatina, Somatostatine, Somatostatinum |
| Type | |
| Formula | C76H104N18O19S2 |
| Weight | Average: 1637.9 Monoisotopic: 1636.716655549 |
| Protein binding | This pharmacokinetic data is irrelevant. |
| Groups | Approved, Investigational |
| Therapeutic Class | Growth hormone antagonist |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Gastrointestinal haemorrhage, Growth hormone deficiency, Hypovolaemic shock
Somatostatina is also used to associated treatment for these conditions: Acromegaly, Biliary Fistula, Bleeding caused by Gastritis erosive, Diabetic Ketoacidosis, Duodenal ulcer haemorrhage, Fistula of small intestine, Gastric ulcer haemorrhage, Gastritis haemorrhagic, Oesophageal varices haemorrhage, Pancreatic Fistula, Postoperative Complications caused by Pancreatic Surgery, Restriction of Secretions
How Somatostatina works
Somatostatina binds to 5 subtypes of somatostatin receptors (SSTRs), which are all Gi-protein-coupled transmembrane receptors that inhibits adenylyl cyclase upon activation . By inhibiting intracellular cyclic AMP and Ca2+ and by a receptor-linked distal effect on exocytosis, SSTRs block cell secretion . The common pathway shared by the receptors involve the activation of phosphotyrosine phosphatase (PTP), and modulation of mitogen-activated protein kinase (MAPK) . With the exception of SSTR3, activation of SSTRs lead to activation of voltage-gated potassium channels accompanied by increased K+ currents. This result in membrane hyperpolarization and inhibits depolarization-induced Ca2+ influx through voltage-sensitive Ca2+ channels . Depending on the receptor subtype, signalling cascades involve activation of other downstream targets such as Na+/H+ exchanger, Rho GTPase, and nitric oxide synthase (NOS) . SSTRs 1 to 4 bind both somatostatin isoforms with equal nanomolar binding affinity whereas SSTR5 exhibits a 5- to 10-fold higher binding affinity for SST-28 .
Effects of SSTR1: Upon biding of somatostatin and activation, SSTR1 mediates an antisecretory effect on growth hormone, prolactin and calcitonin .
Effects of SSTR2: SSTR2 subtype dominates in endocrine tissues. By binding to SST2 receptors, somatostatin exerts paracrine inhibitory actions on gastrin release from G cells, histamine release from ECL cells, and directly on parietal cell acid output . SSTR2 receptor signalling cascades also inhibit the secretion of growth hormone and that of adrenocorticotropin, glucagon, insulin, and interferon-γ .
Effects of SSTR3: Activation of these receptors lead to reduction in cell proliferation . SSTR3 triggers PTP-dependent cell apoptosis accompanied by activation of p53 and the pro-apoptotic protein Bax . A study of the matrigel sponge assay suggests that through SSTR3-mediated inhibition of both NOS and MAPK activities may lead to the antitumor effects of somatostatin in inhibiting tumor angiogenesis .
Effects of SSTR4: The functions of SSTR4 remain largely unknown .
Effects of SSTR5: Like SSTR2, SSTR5 subtype also predominates in endocrine tissues. Upon activation, SSTR5 signalling cascades exert an inhibitory action on growth hormone, adrenocorticotropin, insulin, and glucagon-like peptide-1 as well as the secretion of amylase .
The presence of somatostatin receptors has been identified in most neuroendocrine tumours, endocrine gastroenteropancreatic (GEP) tumors, paragangliomas, pheochromocytomas, medullary thyroid carcinomas (MTC) and small cell lung carcinomas . The antitumor effects of somatostatin were also effective in various malignant lymphomas and breast tumours . Gastrointestinal hormones, such as gastrin, secretin, and cholecystokinin (CCK), as well as growth hormones and growth factors are thought to be elevated in gastrointestinal tract and neuroendocrine tumours and are inhibited by somatostatin . In vitro, somatostatin inhibited epidermal growth factor (EGF)-induced DNA synthesis and replication following which suggest that somatostatin may have direct anti-proliferative effects via SSTR signalling . Acromegaly is characterized as the endocrine disorder caused by a functioning tumour of cells that secrete growth hormone from the anterior pituitary . Somatostatina analogue therapies serve to normalize the elevated levels of GH and insulin-like growth factor 1 (IGF-1) and attenuate tumour growth.
In the vascular system this likely produces vasoconstriction by inhibiting adenylate cyclase leading to a lowering the concentration of cyclic adenosine monophosphate in the endothelial cells which ultimately blocks vasodilation through this pathway. This vasoconstriction is though the be responsible for reducing blood flow to the esophageal tissues and so reduces bleeding from esophageal varices .
Somatostatina mediates an analgesic activity by reducing vascular and nociceptive components of inflammation . Studies indicate that somatostatin may be present in nociceptive DRG neurons with C-fibers and primary afferent neurons to inhibit the release of transmitters at the presynaptic junctions of the sensory-efferent nerve terminals . Exogenous somatostatin has shown to inhibit the release of Substance P from central and peripheral nerve ending .
Dosage
Somatostatina dosage
Initially, 250 mcg as a bolus inj over 3-5 min, followed by a continuous infusion of 3.5 mcg/kg/hr until bleeding has ceased. May continue for a further 48-72 hr to prevent recurrent bleeding.
Side Effects
Rapid infusion may lead to abdominal discomfort, nausea, flushing, bradycardia.
Toxicity
Data is not available.
Precaution
Monitor blood glucose levels. May inhibit intestinal absorption thus concomitant parenteral nutrition may be recommended.
Interaction
Propranolol, phentolamine, barbiturates, pentetrazol.
Food Interaction
No interactions found.Volume of Distribution
This pharmacokinetic data is irrelevant.
Elimination Route
This pharmacokinetic data is irrelevant.
Half Life
The half-life of endogenous somatostatin is 1-3 minutes due to rapid degradation by peptidase enzymes present in the plasma and tissues .
Clearance
Following intravenous administration of 3H-labeld endogenous somatostatin, the total body clearance was approximately 50 mL/min . In man, the value was calculated to be as high as 3000 mL/minutes, which is greatly exceeds the hepatic blood flow. This suggests that rapid enzymatic breakdown in the circulation and other tissues serves as a critical route of elimination .
Elimination Route
As a polypeptide chain, somatostatin is primarily eliminated via metabolism by peptidase enzymes .
Pregnancy & Breastfeeding use
Pregnancy Category B. Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well-controlled studies in pregnant women OR Animal studies have shown an adverse effect, but adequate and well-controlled studies in pregnant women have failed to demonstrate a risk to the fetus in any trimester.
Contraindication
Pregnancy & lactation. Childn <16 yr (severe indication).
Innovators Monograph
You find simplified version here Somatostatina
Somatostatina contains Somatostatin see full prescribing information from innovator Somatostatina Monograph, Somatostatina MSDS, Somatostatina FDA label
FAQ
What is Somatostatina used for?
Somatostatina used to treat acute bleeding from esophageal varices, gastrointestinal ulcers, and gastritis; prevent pancreatic complications after surgery; and restrict secretions of the upper intestine, pancreas, and biliary tract.
How safe is Somatostatina?
Somatostatina analogs is generally well tolerated. Transitory adverse events frequently seen after initiating Somatostatina analog treatment include abdominal discomfort, diarrhea, steatorrhea, nausea, and bloating.
What are the common side effects of Somatostatina?
The common side effects of Somatostatina are include :
- gallbladder problems,
- slow heart rate,
- irregular heartbeat (arrhythmias),
- diarrhea,
- nausea,
- stomach pain,
- vomiting,
- gas (flatulence),
- abnormal stools,
- stomach distention,
- constipation,
- low and high blood glucose,
- low thyroid levels,
- headache, and
- injection site pain.
Does Somatostatina increase blood pressure?
During Somatostatina infusion, the mean blood pressure remained unaffected in all patients with EH and the normotensive subjects, while the PRA decreased slightly in the EH group.
Is Somatostatina safe in pregnancy?
Most of the limited experience with administration of octreotide during pregnancy comes from women being treated for acromegaly, and treatment with octreotide during pregnancy in these cases is generally considered safe.
Is Somatostatina safe during breastfeeding?
A pregnant woman with acromegaly started long-acting octreotide 10 mg monthly at 12 weeks gestation. After delivery, she breastfeed her until 6 weeks postpartum when she required an increase in Somatostatina LAR to 20 mg monthly. She continued to breastfeed successfully on Somatostatina.
What is the function of Somatostatina?
Somatostatina is a hormone that many different tissues produce, but it is found primarily in the nervous and digestive systems. The primary function of Somatostatina is to prevent the production of other hormones and also stop the unnatural rapid reproduction of cells such as those that may occur in tumors.
Does Somatostatina inhibit insulin?
Somatostatina potently inhibits insulin and glucagon release from pancreatic islets.
Does somatostatin increase blood glucose?
These results show that Somatostatina lowers blood glucose concentrations as a secondary effect of inhibition of glucagon secretion. Somatostatina is not suitable for therapy in diabetes.
What is Somatostatina secreted by?
In the pancreas, Somatostatina is produced by the delta cells of the islets of Langerhans, where it serves to block the secretion of both insulin and glucagon from adjacent cells. Insulin, glucagon, and Somatostatina act in concert to control the flow of nutrients into and out of the circulation.
What causes high Somatostatina?
Excessive Somatostatina levels in the bloodstream may be caused by a rare endocrine tumour that produces Somatostatina, called a 'somatostatinoma'. Too much Somatostatina results in extreme reduction in secretion of many endocrine hormones.
How do I test for Somatostatina?
Your doctor will usually start the diagnosis process with a fasting blood test. This test checks for an elevated Somatostatina level.
How Somatostatina causes diarrhea?
Diarrhea and steatorrhea are common symptoms of pancreatic somatostatin tumors and contribute to weight loss. In most patients, hypochlorhydria or achlorhydria occurs because of inhibited gastric acid secretion.
What type of protein is Somatostatina?
Somatostatina is an endogenous cyclic polypeptide with two biologically active forms. It is an abundant neuropeptide and has a wide range of physiological effects on neurotransmission, secretion and cell proliferation.
What is the half life of Somatostatina?
Its half-life is between 1 to 3 minutes.Somatostatina produces predominantly neuroendocrine inhibitory effects across multiple systems.
What is long-acting Somatostatina?
A long-acting Somatostatina analogue is used in the management of a diazoxide-unresponsive diffuse form of congenital hyperinsulinism.
How do I give Somatostatina?
Somatostatina continuous infusion of 3.5 mcg/kg/hr until bleeding has ceased. May continue for a further 48-72 hr to prevent recurrent bleeding. Monitor blood glucose levels.
Does Somatostatina activate gastric motility?
Moreover, SS exerts inhibitory effects on various gastrointestinal functions, including gastric acid secretion, gastric emptying, intestinal motility, and release of various gastrointestinal hormones.
How does Somatostatina regulate blood sugar?
Somatostatina blocks the production of insulin and glucagon to help regulate blood sugar levels.Somatostatina increases when either glucagon or insulin levels get too high.
What happens if I overdose dose of Somatostatina?
Seek emergency medical attention. Overdose symptoms may include severe upper stomach pain, diarrhea, weight loss, warmth or tingling, numbness or cold feeling, unexplained muscle pain, weakness, weak pulse, fainting, or slow breathing (breathing may stop).
What happens if I miss a dose?
Call your doctor for instructions if you miss a dose.
