Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P61278 (somatostatin)
 22,083 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Cyclic somatostatin was administered intravenously on eight occasions to five consecutive patients with massive haemalemesis due to oesophageal varices. The doses administered with 0--250 micrograms as bolus, followed by 100--250 micrograms per hr during 2--12 hrs. The source of bleeding was determined by endoscopy. The volume of bleeding was estimated from the clinical condition of the patient and by gastric irrigation and iced water. The bleeding stopped immediately on all occasions when somatostatin was administered. It is suggested that the effect is due to the ability of somatostatin to reduce regional splanchnic blood flows and portal pressure.
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PMID:Treatment of bleeding oesophageal varices with somatostatin. 31 31

The influence of octreotide and somatostatin on liver metabolic activity were studied in 16 patients with cirrhosis that was positive for hepatitis B surface antigen (HBsAg). In patients receiving a 50 micrograms bolus and a 50 micrograms/hr infusion of octreotide, the hepatic blood flow, hepatic clearance, and the maximum velocity/metabolic elimination rate constant (Vmax/km) were significantly reduced after octreotide infusion compared with basal values. Similarly, the hepatic blood flow, hepatic clearance, and Vmax/km were significantly decreased in patients receiving a 250 micrograms bolus and a 250 micrograms/hr infusion of somatostatin. The extraction ratio and the systemic hemodynamic values, including cardiac index, heart rate, mean arterial pressure, and systemic vascular resistance, showed no significant changes in patients receiving either octreotide or somatostatin. These findings suggest that, as with somatostatin, octreotide reduced hepatic blood flow and impaired liver metabolic activity in patients with HBsAg-positive cirrhosis. These effects may have important clinical implications in the management of bleeding esophageal varices in patients with cirrhosis.
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PMID:Octreotide decreased liver metabolic activity in patients with hepatitis B surface antigen-positive cirrhosis. 135 73

Successful pharmacological arrest of haemorrhage might avoid the risk of aspiration associated with tamponade and early studies have suggested that the vasoactive agent somatostatin may be as effective and perhaps safer than tamponade in controlling variceal haemorrhage. In our view, vasopressin has not established a role in management but we retain an open mind regarding the potential use of terlipressin in combination with nitroglycerin. It is unlikely that any of these agents can improve significantly our ability to control variceal haemorrhage when compared to balloon tamponade but they may reduce the incidence of pulmonary complications and thereby reduce subsequent mortality. Tamponade has proved successful in controlling acute haemorrhage from oesophageal varices in our hands. Late complications continue to give cause for concern but until effective safe alternatives to tamponade are developed, we continue to advocate its use for emergency control of acute variceal haemorrhage. Our own studies have shown that the high mortality seen in this patient population may reflect the severity of the underlying liver disease rather than failure of a management policy employing oesophageal tamponade for the initial control of acute variceal haemorrhage.
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PMID:Balloon tamponade and vasoactive drugs in the control of acute variceal haemorrhage. 135 76

1) Emergency treatment. The best treatment remains endoscopic sclerotherapy, which controls the bleeding in 90% of the cases. Pharmacologic management stops the variceal hemorrhage in 80% of the cases and is indicated before endoscopic treatment can be performed. Intravenous somatostatin administration may be prolonged for 5 days, even more, and may thus prevent early rebleeding, which is not achieved neither by vasopressin nor by glypressin, which administration is restricted to 24 hours. Esophageal tamponade is useful to arrest a massive variceal bleeding, if vasoactive drugs are not available or not efficient, before endoscopic management. If the bleeding persists after 2 sclerotherapy sessions, an alternative treatment is mandatory: the patient should be sent to the surgeon for a portosystemic shunt if the operative risk is acceptable (child A and B) or should become a candidate for a transjugular intrahepatic stent shunt, especially if transplantation is considered afterwards. 2) Prevention of recurrent hemorrhage. A) Early (within 5 days after the initial bleeding). Somatostatin probably prevents early rebleeding, as do sclerotherapy. B) Late. B blockade (+ nitrates) or long-term sclerotherapy have the same efficacy. Their association may improve their results. 3) Prevention of the first bleeding episode. Propranolol decrease the risk of variceal rupture from 20% to 9% during the first year after the diagnosis of esophageal varices and is the only treatment which may be proposed to cirrhotics who did not yet bled form their varices.
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PMID:[Prevention and treatment of digestive hemorrhage due to ruptured esophageal varices in patients with cirrhosis]. 136 Oct 90

Although the mechanism initiating and maintaining variceal hemorrhage is not completely understood, there has been general agreement in recent years on the concept that variceal rupture occurs when the tension on the wall of the varices reaches a critical value (the rupture point) that leads to the leakage of the elastic components of the wall. If this hypothesis is true, the aim of pharmacological treatment should be to reduce variceal wall tension or to prevent any abrupt increase in this parameter. Some vasoconstrictor drugs are currently used in order to achieve these goals and in the attempt to stop the acute bleeding episode. All these agents decrease either portal pressure and azygos blood flow. Vasopressin although effective, has significant cardiac and gastrointestinal adverse effects that discourage its use. Combination with nitroglycerin reduces its adverse effects while maintaining or even enhancing the reduction in portal pressure. Glypressin, which acts as a slow-release preparation of vasopressin, has a longer duration of action and can be administered as single intravenous injections instead of continuous infusion. However, the similarity of effects of these drugs on systemic circulation leads to an overlapping spectrum of untoward effects. Somatostatin and the synthetic octapeptide octreotide display similar pharmacological effects on splanchnic hemodynamics but have a better tolerability profile. Thanks to its longer duration of action and ease of administration, octreotide could become the drug of choice for the early, pre-hospital management of bleeding varices. A different approach to the pharmacological treatment of variceal bleeding may be the use of compounds, like metoclopramide and domperidone, that increase the lower esophageal sphincter pressure (LESP), thereby reducing the inflow of blood flow into the submucous venous plexus of the esophagus and hence into the esophageal varices. However, more studies are needed before these compounds be considered a real alternative to the above established drugs.
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PMID:Clinical pharmacology of active variceal bleeding. 136 76

Somatostatin was originally isolated from the hypothalamus, but has subsequently been found throughout the whole gastrointestinal tract. It exerts an inhibitory effect upon numerous functions of the body, and, therefore, increasing attention has been focused on its potential as a therapeutic agent with cytoprotective properties and a potent inhibitory action on a wide variety of functions in endocrine diseases, cancer and gastrointestinal haemorrhage, including bleeding from oesophageal varices. As somatostatin has a very short plasma half-life and requires administration by continuous infusion to maintain therapeutic levels, stable long-acting analogues have been developed. The analogue octreotide has been shown to have a plasma half-life of 113 minutes and to produce a profound selective inhibition of growth hormone. Hepatic excretion of octreotide has been estimated to be between 30 and 40% in healthy volunteers; no data are available in cirrhotic patients. A review of published data assessing systemic and hepatic haemodynamics in animals and humans over varying dosage regimens of somatostatin and octreotide reveals that cardiac output, arterial pressure and peripheral resistance are modified more in animals than in humans. Hepatic haemodynamics are significantly altered in animals as well as in humans in most of the studies. Circumstantial evidence is provided indicating that the mechanisms of action of somatostatin and octreotide in the therapy of bleeding oesophageal varices are mainly mediated by a splanchnic vasoconstrictive effect. Furthermore, gastric acid suppression and potential enhancement of platelet aggregation may contribute to the beneficial outcome after treatment of oesophageal varices with somatostatin.
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PMID:Somatostatin in acute bleeding oesophageal varices. Pharmacology and rationale for use. 138 68

This randomized controlled trial was conducted to compare the efficacy of intravenous infusion of octreotide (a synthetic long-acting somatostatin analogue) with vasopressin in 48 cirrhotic patients with endoscopically proven bleeding esophageal varices. Twenty-four patients received a continuous infusion of octreotide 25 micrograms/h for 24 h after an initial bolus of 100 micrograms and another 24 patients received a continuous infusion of vasopressin 0.4 U/min for 24 h. Bleeding was initially controlled after 6 h of drug infusion in 88% (21/24) and 54% (13/24) of the patients treated with octreotide and vasopressin respectively (p = 0.03). Complete control of bleeding after 24 h of drug infusion was achieved in 15 (63%) patients receiving octreotide and in 11 (46%) patients receiving vasopressin (p > 0.05). Side effects during drug infusion such as headache, chest pain and abdominal pain were significantly lower in the octreotide group (3/24) than in the vasopressin group (11/24). Serum gastrin and insulin levels fell significantly following octreotide infusion, but plasma glucose levels remained unchanged. Mortality related to bleeding esophageal varices was no different between the two groups. This report showed that octreotide infusion was more effective and had fewer side effects than vasopressin in initial controlling of acute esophageal variceal bleeding until an elective endoscopic sclerotherapy could be performed.
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PMID:A randomized controlled trial comparing octreotide and vasopressin in the control of acute esophageal variceal bleeding. 148 8

The long-acting somatostatin analogue octreotide is a synthetic cyclic peptide consisting of 8 amino acids. Depending on the organ, it acts either as a hormone or as a neurotransmitter. The effect on various physiological functions in the brain and the gastrointestinal tract is mainly inhibitory. Due to its inhibitory actions, the possibility of intravenous and subcutaneous administration and the lack of serious side-effects, octreotide offers a broad spectrum of possible indications. Today octreotide is recommended in acromegaly patients and for the treatment of hormone dependent symptoms in patients with gastroenteropancreatic tumours. New indications are enterocutaneous and pancreatic fistulas and the prevention of complications in major pancreatic surgery. In patients with dumping and short-bowel syndrome, octreotide may be helpful until dietary regimens are established. In Aids patients with severe diarrhea, octreotide can be used to stabilize patients with severe dehydration and malnutrition. The clinical effectiveness on upper GI-bleeding due to gastric ulcer and oesophageal varices is still controversial. Future studies must prove whether octreotide may be helpful in treating diabetic retino- and nephropathy because of the possibility of suppressing growth hormone and IGF-I. The antiproliferative effect of octreotide also allows its use in patients with somatostatin-receptor-positive, non-endocrine solid tumors (e.g. brain, breast and small-cell lung cancer). A promising area is the scintigraphic visualization of somatostatin-receptor-positive tumors with a radio-labelled octreotide analogue and the possible target irradiation of these tumors by beta-particle emitting isotopes attached to such analogues.
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PMID:[Somatostatin analog (octreotide) in clinical use: current and potential indications]. 162 Oct 78

In this study we evaluate the efficacy of somatostatin (ST) versus balloon tamponade (BT) in controlling bleeding from esophageal varices. Forty-four consecutive patients with active variceal bleeding were randomly assigned to treatment with a continuous infusion of ST at 250 micrograms/h after an initial bolus of 50 micrograms (group A) or to treatment with BT (group B). Five cases were excluded from the final analysis because of methodological issues. Nineteen patients were allocated to group A and twenty to group B. No differences in age, sex, alcohol intake, severity of bleeding or liver failure were found between the groups. Initial haemostasia within the first 4 h of treatment was obtained in 14 (74%) of the patients receiving ST and in 12 (60%) of those receiving BT. Three patients in group A and two in group B had early rebleeding. Bleeding was controlled over a 24-h period or until elective sclerotherapy could be performed in 11 (58%) and 10 (50%) of the patients, in groups A and B, respectively. One BT-treated patient developed aspiration pneumonia. No complications were observed in patients treated with ST. No significant differences in initial haemostasia, definite control of bleeding or complications were found between the two groups. In this study, somatostatin infusion was found to be as effective as Sengstaken BT in controlling acute variceal bleeding until an elective session of endoscopic sclerotherapy could be performed. However, larger studies are still needed to confirm this theory.
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PMID:Somatostatin versus Sengstaken balloon tamponade for primary haemostasia of bleeding esophageal varices. A randomized pilot study. 167 39

Variceal bleeding has a high mortality, as the majority of patients have cirrhosis, with hepatic coma, renal failure, ascites and clotting deficiencies as complicating factors. Bleeding varices must therefore be treated as an emergency. Resuscitation, endoscopic diagnosis and haemostasis are the cornerstones of treatment. Once bleeding varices have been identified, attempts to stop the bleeding must be made at once as this will lessen the chances of hepatic failure developing. Endoscopic sclerotherapy at the time of diagnosis is the best available treatment at present, although profusely bleeding varices can be difficult to see and inject. In these circumstances the passage of a Sengstaken tube should stop the bleeding, allowing later sclerotherapy to be successful. If rebleeding recurs and cannot be controlled, oesophageal transection with a stapling gun may be life-saving, although the varices may later recur and long-term endoscopic follow-up will be necessary. Portacaval shunting and the distal splenorenal shunt involve arduous surgery and are followed by a significant incidence of hepatic encephalopathy; they should be reserved for those few cases when simpler measures have failed, although shunts do lead to permanent decompression of the portal system. The acute variceal bleed may also be dealt with pharmacologically. Vasopressin, used in combination with nitroglycerin to lessen the harmful side-effects, is cheaper and as effective as terlipressin or somatostatin and its synthetic analogue octreotide. Several courses of injection sclerotherapy will be required to eliminate oesophageal varices. Thereafter, long-term follow-up will be necessary to deal with any recurrence. The place of non-selective beta-blockers is still contentious, but they do reduce portal pressure and may lessen the chance of rebleeding. There is also a growing role for hepatic transplantation, which not only eliminates the varices but also restores liver function to normal and greatly reduces the risk of subsequent hepatoma development.
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PMID:The management of variceal bleeding. 168 66


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