Octreotide

	Email		Print
	Bookmark		Link

Octreotide

Octreotide (brand name Sandostatin, Novartis Pharmaceuticals

Novartis

Novartis International AG is a multinational corporation pharmaceutical company based in Basel, Switzerland that manufactures drugs such as clozapine , diclofenac , carbamazepine , valsartan , imatinib mesylate , ciclosporin , letrozole , methylphenidate , terbinafine , and others....
) is an octapeptide

Peptide

Peptides are short polymers formed from the linking, in a defined order, of a-amino acids. The link between one amino acid residue and the next is known as an amide chemical bond or a peptide bond....
that mimics natural somatostatin

Somatostatin

Somatostatin is a peptide hormone that regulates the endocrine system and affects neurotransmission and cell proliferation via interaction with G-protein-coupled somatostatin receptors and inhibition of the release of numerous secondary hormones....
pharmacologically, though it is a more potent inhibitor of growth hormone

Growth hormone

Growth hormone is a peptide hormone. It stimulates human development and cell reproduction in humans and other animals. It is a 191-amino acid, single chain polypeptide hormone which is synthesized, stored, and secreted by the somatotroph cells within the lateral wings of the anterior pituitary gland....
, glucagon

Glucagon

Glucagon is an important hormone involved in carbohydrate metabolism. Produced by the pancreas, it is released when the glucose level in the blood is low , causing the liver to convert stored glycogen into glucose and release it into the bloodstream....
, and insulin

Insulin

Insulin is a hormone with extensive effects on both metabolism and several other body systems . Insulin causes most of the body's cells to take up glucose from the blood , storing it as glycogen in the liver and muscle, and stops use of fat as an energy source....
than the natural hormone. It was first synthesized in 1979 by the chemist Wilfried Bauer.

e octreotide resembles somatostatin in physiological activities, it can:

of the formulations of this drug show some adverse effects, most important of which is the QT-Interval prolonging.

Discussion

Ask a question about 'Octreotide'

Start a new discussion about 'Octreotide'

Answer questions from other users

Full Discussion Forum

Encyclopedia

Octreotide (brand name Sandostatin, Novartis Pharmaceuticals

Novartis

Peptide

Somatostatin

Growth hormone

Glucagon

Insulin

Pharmaceutical Effects

Since octreotide resembles somatostatin in physiological activities, it can:

Inhibit secretion of many hormones, such as gastrin
Gastrin

In humans, gastrin is a hormone that stimulates secretion of gastric acid by the parietal cells of the stomach and aids in gastric motility. It is released by G cells in the stomach, duodenum, and the pancreas....
, cholecystokinin
Cholecystokinin

Cholecystokinin is a peptide hormone of the gastrointestinal system responsible for stimulating the digestion of fat and protein. Cholecystokinin, previously called pancreozymin, is synthesised by I-cells in the mucosal epithelium of the small intestine and secreted in the duodenum, the first segment of the small intestine, and ca...
, glucagon
Glucagon

Glucagon is an important hormone involved in carbohydrate metabolism. Produced by the pancreas, it is released when the glucose level in the blood is low , causing the liver to convert stored glycogen into glucose and release it into the bloodstream....
, growth hormone
Growth hormone

Growth hormone is a peptide hormone. It stimulates human development and cell reproduction in humans and other animals. It is a 191-amino acid, single chain polypeptide hormone which is synthesized, stored, and secreted by the somatotroph cells within the lateral wings of the anterior pituitary gland....
, insulin
Insulin

Insulin is a hormone with extensive effects on both metabolism and several other body systems . Insulin causes most of the body's cells to take up glucose from the blood , storing it as glycogen in the liver and muscle, and stops use of fat as an energy source....
, secretin
Secretin

Secretin is a peptide hormone produced in the S cells of the duodenum in the crypts of Lieberk?hn. Its primary effect is to regulate the pH of the duodenal contents via the control of gastric acid secretion and buffering with bicarbonate....
, pancreatic polypeptide
Pancreatic polypeptide

Pancreatic polypeptide is a polypeptide secreted by PP cells in the endocrine pancreas predominantly in the head of the pancreas. It consists of 36 amino acids and has molecular weight about 4200 Dalton_%28unit%29....
, TSH
TSH

TSH may refer to:*Serene Highness, a style used by some Royal houses.*Thyroid-stimulating hormone, a hormone synthesized and secreted by thyrotrope cells...
, and vasoactive intestinal peptide
Vasoactive intestinal peptide

Vasoactive intestinal peptide is a peptide hormone containing 28 amino acid residue s and is produced in many areas of the human body including the gut, pancreas and suprachiasmatic nuclei of the hypothalamus in the brain....
.
Reduce secretion of fluids by the intestine and pancreas
Pancreas

The pancreas is a gland Organ in the digestive system and endocrine system of vertebrates. It is both an endocrine gland , as well as an exocrine gland, secreting pancreatic juice containing Digestion enzymes that pass to the small intestine....
.
Reduce gastrointestinal motility and inhibits contraction of the gallbladder
Gallbladder

The gallbladder is a small non-vital Organ which aids in the digestive process and concentrates bile produced in the liver....
.
Inhibit the action of certain hormones from the anterior pituitary
Anterior pituitary

The anterior pituitary comprises the Anterior#Usage in human anatomy lobe of the pituitary gland and is part of the endocrine system. Unlike the posterior pituitary, the anterior lobe is genuinely glandular, hence the root adeno in its name....
.
Cause vasoconstriction
Vasoconstriction

Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels, particularly the large arteries, arterioles and veins....
in the blood vessels.
It has also been shown to produce analgesic
Analgesic

An analgesic is any member of the diverse group of Medication used to relieve pain . The word analgesic derives from Greek an- and algos ....
effects, most probably acting as a partial agonist
Partial agonist

Partial agonists bind and activate a given receptor, but have only partial efficacy#Pharmacology at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic effects - when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive...
at the mu opioid receptor
Mu Opioid receptor

The ? opioid receptors are a class of opioid receptors with high affinity for enkephalins and beta-endorphin but low affinity for dynorphins....
.

Adverse Effects

Some of the formulations of this drug show some adverse effects, most important of which is the QT-Interval prolonging. As a rule, a drug that causes prolonged QT-Interval shall have Drug-Drug Interaction possibilities. This indicates that giving such drug shall be of care so that no severe interactions can occur. Octreotide usually shows certain commonly observed adverse effects that differ in the frequency from patient to another:

Most Frequent Adverse Effects: Abdominal Pain with Cramps, Bradycardia, Conduction Disorder of the Heart, Constipation, Diarrhea, Disorder of the Digestive System, Injection Site Sequelae, Nausea, Vomiting

Less Frequent Adverse Effects: Discolored Feces, Dyspepsia, Flatulence, Hypothyroidism, Steatorrhea, Tenesmus

Rare Adverse Effects: Acute Pancreatitis, Alopecia, Biliary Calculus, Disease of Liver, Dizziness, Edema, Fatigue, Fever, Flushing, General Weakness, Headache Disorder, Hepatitis, Hyperbilirubinemia, Hyperglycemia, Hypoglycemic Disorder, Prolonged QT Interval

Uses

The Food and Drug Administration

Food and Drug Administration

The U.S. Food and Drug Administration is an Government agency of the United States Department of Health and Human Services and is responsible for regulating and supervising the safety of foods, dietary supplements, Medications, vaccines, Biopharmaceutical, blood transfusion, medical devices, Electromagnetic radiation-emitting devices, veteri...
(FDA) has approved the usage of a salt form of this peptide, octreotide acetate
Acetate

An acetate, or ethanoate, is either a salt or ester of acetic acid.In chemistry, the abbreviation Ac refers to the acetyl group. The anion and the functional group may be written as -OAc and AcO-, or OAc respectively....
, as an injectable depot formulation for the treatment of acromegaly

Acromegaly

Acromegaly is a syndrome that results when the pituitary gland produces excess human growth hormone after epiphyseal plate closure. A number of disorders may affect the pituitary to create this circumstance, although most commonly it involves a GH producing tumor derived from a distinct type of cells and called pituitary adenoma....
, the treatment of diarrhea

Diarrhea

In medicine, diarrhea, also spelled diarrhoea , is characterized by frequent loose or liquid bowel movements. The spelling of "diarrhea" is an appropriation of the Greek "diarrhoia" meaning "a flowing through." ....
and flushing

Flushing (physiology)

For a person to flush is to become markedly red in the face and often other areas of the skin, from various physiology conditions. Flushing is generally distinguished, despite a close physiological relation between them, from blushing, which is milder, generally restricted to the face or cheeks, and generally assumed to reflect embarrassment....
episodes associated with carcinoid syndrome

Carcinoid syndrome

Carcinoid syndrome refers to the array of symptoms that occur secondary to carcinoid.Carcinoid tumors are discrete, yellow, well-circumscribed tumors that can occur anywhere along the gastrointestinal tract and in the lung....
, and treatment of diarrhea in patients with vasoactive intestinal peptide

Vasoactive intestinal peptide

Vasoactive intestinal peptide is a peptide hormone containing 28 amino acid residue s and is produced in many areas of the human body including the gut, pancreas and suprachiasmatic nuclei of the hypothalamus in the brain....
-secreting tumors (VIPoma

VIPoma

A VIPoma is a rare endocrine tumor, usually originating in the pancreas, which produces vasoactive intestinal peptide .A syndrome caused by non-? islet cell tumors....
s).

Octreotide has also been used off-label

Off-label use

Off-label use is the practice of prescribing prescription drug for a purpose outside the scope of a drug's approved label, most often concerning the drug's indication ....
for the treatment of severe, refractory diarrhea from other causes. It is used in toxicology for the treatment of prolonged recurrent hypoglycemia after sulfonylurea

Sulfonylurea

Sulfonylurea derivatives are a class of antidiabetic drugs that are used in the management of diabetes mellitus Diabetes mellitus type 2 . They act by increasing insulin release from the beta cells in the pancreas....
overdose.

Octreotide has also been used with varying degrees of success in infants with nesidioblastosis to help decrease insulin hypersecretion.

In patients with suspected esophageal varices

Esophageal varices

In medicine , esophageal varices are extremely dilation sub-mucosal veins in the esophagus. They are most often a consequence of portal hypertension, such as may be seen with cirrhosis; patients with esophageal varices have a strong tendency to develop bleeding....
, octreotide can be given to help decrease bleeding.

Octreotide has been investigated for patients with pain from chronic pancreatitis

Chronic pancreatitis

Chronic pancreatitis is a long-standing inflammation of the pancreas that alters its normal structure and functions. It can present as episodes of acute inflammation in a previously injured pancreas, or as chronic damage with persistent pain or malabsorption....
.

Octreotide may be useful in the treatment of thymic neoplasms.

Octreotide has been used as an unlicensed drug, injected sub-cutaneously in the management of hypertrophic pulmonary osteoarthropathy (HPOA), secondary to non-small cell lung carcinoma. Although its mechanism is not known it appears to reduce the pain associated with HPOA

It has been used in the treatment of malignant bowel obstruction.

Octeotride is also used to treat diabetic drug toxicities.

Octreotide may be used in conjunction with midodrine to partially reverse periphreal vasodilation in the hepato-renal syndrome. By increasing systemic vascular resistance, these drugs reduce shunting and improve renal perfusion, prolonging survival until definitive treatment with liver transplant.

External links

Indevus Pharma and Octreotide