China
Africa
Explore chapters and articles related to this topic
Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Developed by Novartis, pasireotide (SigniforTM) (Figure 8.45) is the most recent somatostatin analog to be approved. Like octreotide and lanreotide, it is used to treat neuroendocrine (particularly carcinoid) and thyroid tumors, and acromegaly resulting from pituitary tumors. It has an advantage of a 40-fold increase in affinity for the Somatostatin Receptor 5 compared to the other two agents. Pasireotide is mainly used when a tumor cannot be removed surgically or fails to respond to other somatostatin analogues. Structure of pasireotide (SigniforTM).
The Endocrine Pancreas
Published in George H. Gass, Harold M. Kaplan, Handbook of Endocrinology, 2020
There are several other disease settings in which octreotide has definite or potential therapeutic uses. One of these is in the treatment of diabetes. In this case, its benefit would be associated with lowering growth hormone and IGF-I levels, rather than controlling serum glucose concentration. These two hormones are thought to be involved in the vascular proliferation that underlies both diabetic retinopathy and nephropathy. Another promising application for octreotide is in the treatment of bleeding esophageal varices in patients with cirrhosis. Octreotide reduces portal pressure and hepatic blood flow and has been shown to be of equal efficacy to vasopressin in randomized trials. Furthermore, octreotide is less costly and has fewer side effects than vasopressin, which can cause coronary artery spasm. Many types of diarrhea respond to octreotide therapy, such as those associated with short bowel syndrome, ileostomy, diabetes with autonomic neuropathy, and medullary thyroid carcinoma. Although somatostatin is thought to be a major regulator of pancreatic exocrine function, a clear role of octreotide in the treatment of acute or chronic pancreatitis has not been established. The use of octreotide is relatively safe, with complications mainly limited to gallstone formation, steatorrhea, and transient diarrhea.41
Endoscopic therapy of oesophageal and gastric varices
Published in David Westaby, Martin Lombard, Therapeutic Gastrointestinal Endoscopy A problem-oriented approach, 2019
The principal pharmacological therapies are the vasoconstrictor vasopressin, and glypressin (a synthetic analogue of vasopressin), vasopressin combined with nitroglycerine (to prevent the systemic side effects of vasopressin) and octreotide (a synthetic analogue of somatostatin). Dosages and administration are described in Table 7.3. Most evidence suggests that pharmacological therapy is better than no therapy in terminating haemorrhage [3], but initial trials with vasopressin had significant side effects. These can be partially abolished by adding a nitroglycerine infusion or using glypressin [16]. Octreotide, with few side effects, is also effective when administered over 5 days to try to avoid early rebleeding [17]. Trials comparing pharmacological with endoscopic therapy will be described below.
Octreotide and Octreotide-derived delivery systems
Published in Journal of Drug Targeting, 2023
Mingliang Fan, Yue Huang, Xinlin Zhu, Jiayu Zheng, Mingwei Du
The tetradecapeptide somatostatin is secreted by hypothalamus or delta cells in gastrointestinal tract and interacts with somatostatin receptors (SSTRs), which is a group of GPCRs (G-protein-coupled receptors) with five human receptor subtypes (SSTR 1-5). Somatostatin can inhibit the release of a series of hormones or neuropeptides in many organs, including growth hormone, insulin, glucagon, among others, thus taking important roles in many physiological functions. However, its clinical applications are remarkably restricted by poor circulation time (about 3 min) in the blood. Hence a variety of somatostatin analogs with longer circulation time have been developed for clinical use since 1970s [1]. Among them, Octreotide (SMS 201-995) is the most widely developed representative of somatostatin analog and stands the test of clinical application [2]. As a therapeutic agent and targeting ligand, Octreotide (OCT) has also been involved in the construction of many novel pharmaceutical systems for tumour targeted treatment. Given OCT-derived radionuclide therapy and radionuclide imaging were well reviewed by previous publication [3], we herein focus on the preclinical studies of some novel pharmaceutical delivery systems related to OCT, including microsphere, conjugate, liposome, polymeric nanoparticle, hydrogel and inorganic nanoparticle.
Current advances in the management of cluster headaches
Published in Expert Opinion on Pharmacotherapy, 2021
Theodoros Mavridis, Marianthi Breza, Christina Deligianni, Dimos D. Mitsikostas
Octreotide is a somatostatin analog that mimics natural somatostatin by inhibiting serotonin release, and the secretion of gastrin, VIP, insulin, glucagon, secretin, motilin, and pancreatic polypeptide. It provides more potent inhibition of growth hormone, glucagon, and insulin as compared to endogenous somatostatin. Octreotide has a level C recommendation for the acute treatment of CH [29]. Octreotide 100 mg given subcutaneously has shown effectiveness in improving headache response compared to placebo. In terms of response rate and time to initial relief, it is believed to be inferior to both subcutaneous and intranasal sumatriptan [42,43]. The adverse effects (AE) are nonserious and include injection site reactions, diarrhea, abdominal bloating, nausea, dull background headache and dizziness/somnolence [27,29].
Diagnosis and treatment of malignant-appearing arteriovenous malformation
Published in Baylor University Medical Center Proceedings, 2021
Rebekah John, Gurkarminder Sandhu, Christopher Naumann
The intermittent ischemia caused by contraction of the muscularis propria causes hypoxia, which is known to increase expression of proangiogenic factors. Vascular endothelial growth factor (VEGF) is one such growth factor that has been found in higher quantities in hypoxic environments.5 VEGF inhibitors have been studied in the treatment of AVMs; however, due to their extensive side effect profile, they are not commonly used for long-term treatment.6 Other therapies commonly employed in treatment of AVMs include endoscopic ligation and surgical intervention, as well as argon plasma coagulation. In argon plasma coagulation, an electrical current is combined with argon gas. The gas is ionized and allows a high-frequency electric current to be conducted to the tissue without direct contact. This method decreases tissue depth injury, especially when used in conjunction with a prior submucosal saline injection to the target area to form a cushion.7,8 Pharmacological therapy with octreotide is also commonly used. One study showed that administration of octreotide long-acting release for 6 months resulted in a significant reduction in bleeding episodes and transfusion requirements in patients who had mostly failed argon plasma coagulation therapy.9