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Clinical Pharmacy Apr 1989The chemistry, pharmacology, pharmacokinetics, clinical uses, adverse effects and drug interactions, dosage, availability and cost, and indications for use of... (Review)
Review
The chemistry, pharmacology, pharmacokinetics, clinical uses, adverse effects and drug interactions, dosage, availability and cost, and indications for use of octreotide, a new synthetic analogue of the peptide hormone somatostatin (SS), are reviewed. Like SS, octreotide suppresses secretion of pituitary growth hormone (GH) and thyrotropin and decreases release of a variety of pancreatic islet cell hormones including insulin, glucagon, and vasoactive intestinal peptide (VIP). Octreotide also reduces splanchnic blood flow, gastric acid secretion, GI motility, and pancreatic exocrine function and alters the absorption of water, electrolytes, and nutrients from the GI tract. The elimination half-life of i.v. octreotide is 72-98 minutes, compared with 2-3 minutes for i.v. SS. Usual administration of octreotide is by the i.v. or s.c. route. Octreotide has been studied in the treatment of hormone-secreting pituitary tumors and pancreatic islet cell tumors. Octreotide therapy lowers GH secretion and improves clinical symptoms in patients with acromegaly and may suppress clinical symptoms to a greater degree than bromocriptine. Patients with carcinoid syndrome and VIP-secreting tumors (vipomas) have had substantial improvement in clinical symptoms with administration of octreotide. This agent does not appear to be effective in the treatment of nonvariceal upper GI bleeding and acute pancreatitis; its relative usefulness in the treatment of variceal bleeding is not established. Adverse effects associated with octreotide therapy generally have been mild, including pain or burning at the injection site, abdominal pain, and diarrhea. Octreotide has been shown to interfere with absorption of oral cyclosporine. Standard initial therapy is octreotide acetate 50-100 micrograms s.c. every 8-12 hours, with titration based on clinical and biochemical effects. Up to 3000 micrograms/day of octreotide acetate has been administered to patients with acromegaly without serious adverse effect. Octreotide is marketed under the brand name Sandostatin and is available in 1-mL ampuls containing 50, 100, and 500 micrograms of octreotide acetate. Because the conditions for which octreotide appears to be most effective are uncommon, the drug should be considered for addition to the formulary in tertiary-care institutions only; addition of octreotide to the formulary of a community hospital is probably unnecessary. The synthetic analogue octreotide is longer acting and more specific in pharmacologic action than SS.(ABSTRACT TRUNCATED AT 400 WORDS)
Topics: Animals; Humans; Octreotide
PubMed: 2653711
DOI: No ID Found -
Journal of Neonatal-perinatal Medicine 2021Being a rare condition, the incidence of chylothorax among neonates is low, but the mortality rate is high. In a dire effort to reduce the risk of death, octreotide... (Review)
Review
BACKGROUND
Being a rare condition, the incidence of chylothorax among neonates is low, but the mortality rate is high. In a dire effort to reduce the risk of death, octreotide treatment is used to effectively treat acquired and congenital chylothorax. Octreotide is proven to effectively treat chylothorax in pre-term and full-term neonates. However, previous studies have not consistently demonstrated the optimal dose of octreotide or the best mode of administration. The objectives of this work were to review previous literature to determine the outcomes of administering high doses of octreotide compared to lower dose regimens in neonates with chylothorax and to determine best practices.
METHODS
A literature search was performed using electronic databases using the key words neonates, chylothorax, and octreotide.
RESULTS
Octreotide has been administrated in doses ranging from 0.5μg/kg/h to > 20μg/kg/h. Both low- and high-doses of octreotide are effective in resolving chylothorax with little to no side effects. When side effects were reported, neonates experienced side effects that are less significant in nature and scope.
CONCLUSIONS
We recommend that the dose of octreotide in neonatal chylothorax can be titrated safely to a maximum of 20μg/kg/h without significant side effects.
Topics: Chylothorax; Humans; Infant, Newborn; Octreotide
PubMed: 33843702
DOI: 10.3233/NPM-200644 -
Critical Reviews in Oncology/hematology Sep 2012Malignant bowel obstruction (MBO) is a challenging complication of advanced cancer. Conservative treatment of inoperable MBO in terminal cancer patients has been found... (Review)
Review
Malignant bowel obstruction (MBO) is a challenging complication of advanced cancer. Conservative treatment of inoperable MBO in terminal cancer patients has been found to be effective in controlling the distressing symptoms caused by this complication in inoperable cancer patients. Twenty years ago, octreotide was proposed to treat symptoms related to malignant bowel obstruction. Since then several reports have confirmed the efficacy of octreotide in the management of gastrointestinal symptoms of MBO. Fifteen randomized controlled trials or observational reports with a significant number of patients treated with octreotide have been reviewed; 281 patients were surveyed. Authors reported a therapeutic success ranging between 60% and 90%. Despite the limited number of controlled studies, the large experience acquired through 20 years suggests that octreotide is the first-choice antisecretory agent for MBO. As such, octreotide is the only drug approved by the health-care system in Italy for this treatment.
Topics: Gastrointestinal Agents; Humans; Intestinal Obstruction; Neoplasm Staging; Neoplasms; Octreotide; Treatment Outcome
PubMed: 22277783
DOI: 10.1016/j.critrevonc.2011.12.006 -
Drug Intelligence & Clinical Pharmacy Oct 1988Octreotide is an investigational synthetic peptide exhibiting actions similar to those of endogenous somatostatin. It has a longer half-life than the native hormone and... (Review)
Review
Octreotide is an investigational synthetic peptide exhibiting actions similar to those of endogenous somatostatin. It has a longer half-life than the native hormone and can be administered by subcutaneous injection. Octreotide inhibits the secretion of growth hormone and numerous regulatory peptides of the gastroenteropancreatic system. Trials evaluating the clinical utility of octreotide indicate efficacy in the management of symptoms associated with acromegaly and hypersecretory neuroendocrine tumors, and in the control of nontumoral secretory diarrheas. Octreotide therapy is well tolerated. This agent should prove useful in the symptomatic control of a number of rare hypersecretory disorders.
Topics: Antineoplastic Agents; Humans; Octreotide
PubMed: 3068036
DOI: 10.1177/106002808802201001 -
Lancet (London, England) Sep 1989
Topics: Carcinoid Tumor; Diarrhea; Gastrinoma; Glucagonoma; Humans; Octreotide; Pancreatic Neoplasms; Syndrome
PubMed: 2570240
DOI: No ID Found -
Drugs Apr 1997Octreotide is a somatostatin analogue: a long-acting release (LAR) formulation of octreotide is designed for once-monthly intramuscular administration. As with native... (Review)
Review
Octreotide is a somatostatin analogue: a long-acting release (LAR) formulation of octreotide is designed for once-monthly intramuscular administration. As with native somatostatin, octreotide LAR exerts potent inhibitory effects on the secretion of growth hormone and on various peptides of the gastroenteropancreatic endocrine system. When patients with acromegaly who show a positive response to treatment with subcutaneous octreotide 300 to 600 micrograms/day are switched to octreotide LAR 20 or 30 mg, the resulting decrease in growth hormone levels is stable and sustained. Reductions in growth hormone levels to < 5 micrograms/L for about 4 weeks are seen in 86 to 100% of patients, to < 2 to 2.5 micrograms/L in 39 to 75% and to < 1 microgram/L in 24 to 40%. Levels of insulin-like growth factor-1 (IGF-1) decrease in parallel and are often normalised with repeated drug treatment. There is no evidence of tachyphylaxis with long term therapy (up to 34 months). Treatment with octreotide LAR improves facial appearance and soft tissue thickening, and eliminates or reduces the incidence of symptoms such as headache, fatigue, arthralgia and excessive perspiration. Tumour shrinkage has been noted in some, but not all, patients receiving octreotide LAR, although this has not been widely evaluated in clinical studies. Overall, octreotide LAR is well tolerated, and the mild to moderate gastrointestinal events experienced by up to 50% of patients are of short duration and often subside with continued drug administration. The incidence of gallbladder abnormalities (sediment, sludge, microlithiasis and gallstones) increases in patients receiving long term therapy with subcutaneous octreotide, although most patients remain asymptomatic. The incidence of gallbladder abnormalities in patients receiving octreotide LAR compares favourably with that during subcutaneous administration. Glycaemic control is not usually altered during octreotide LAR treatment. In summary, octreotide continues to be the principal pharmacological option for most patients with acromegaly. Octreotide LAR offers the convenience of once-monthly administration compared with daily subcutaneous drug administration. In addition, the good efficacy and tolerability profile of octreotide LAR should enhance patient compliance and acceptability of octreotide therapy and contribute to an improvement in patient quality of life.
Topics: Acromegaly; Delayed-Action Preparations; Humans; Octreotide
PubMed: 9098666
DOI: 10.2165/00003495-199753040-00009 -
Lancet (London, England) Apr 1992
Topics: Humans; Octreotide
PubMed: 1347860
DOI: No ID Found -
Drugs Nov 1989Octreotide is an analogue of somatostatin. Like endogenous somatostatin, it exerts a potent inhibitory effect on the release of anterior pituitary growth hormone and... (Review)
Review
Octreotide is an analogue of somatostatin. Like endogenous somatostatin, it exerts a potent inhibitory effect on the release of anterior pituitary growth hormone and thyroid-stimulating hormone, and peptides of the gastroenteropancreatic endocrine system, while overcoming some of the shortcomings of exogenously administered somatostatin, namely a short duration of action, a need for intravenous administration and postinfusion rebound hypersecretion of hormone. Clinical studies have shown that octreotide is effective in the treatment of acromegaly and thyrotrophinomas. In comparative trials octreotide was significantly superior to bromocriptine in patients with acromegaly. Octreotide also appears to provide a significant advantage over existing therapies in the management of the carcinoid syndrome and offers considerable therapeutic potential in reversing carcinoid crises which may be life-threatening. Trials in patients with tumours producing vasoactive intestinal peptide demonstrated that octreotide may be an effective first-line choice for this condition, which has usually metastasised and become refractory to traditional symptomatic therapy. In limited studies in patients with high-output secretory diarrhoea, including cryptosporidium-related diarrhoea associated with AIDS and in patients with small bowel fistulas, octreotide has been shown to be effective in reducing stool/fistula output. However, well-designed clinical trials are still required to confirm its long term usefulness in these disorders. Similarly, although the use of octreotide in other conditions such as neonatal hypoglycaemia caused by nesidioblastosis, reactive pancreatitis, insulin-dependent diabetes mellitus, postprandial hypotension and the dumping syndrome has provided encouraging preliminary results, more studies are needed to clarify the place of octreotide in their treatment. Overall, octreotide appears to be well tolerated with the most frequently reported reactions being pain at the site of injection and gastrointestinal symptoms such as abdominal cramps, nausea, bloating, flatulence, diarrhoea and steatorrhoea. These adverse effects usually abate with time. Additionally, octreotide, like endogenous somatostatin, may also result in cholelithiasis, presumably by altering fat absorption and possibly by decreasing motility of the gallbladder. Thus, octreotide represents a new departure from traditional therapies in the treatment of various pathophysiological states associated with excessive peptide production and secretion. It offers a significant advantage over existing therapies in the medical management of patients with acromegaly, thyrotrophinomas, the carcinoid syndrome, tumours producing vasoactive intestinal peptide and severe secretory diarrhoea in whom conventional management options have either become exhausted or have provided suboptimal symptomatic relief.
Topics: Animals; Humans; Octreotide; Peptides
PubMed: 2689136
DOI: 10.2165/00003495-198938050-00002 -
Digestive Diseases and Sciences Feb 1993Severe long-term complaints of dumping occur in a small number of patients after gastric surgery. Dietary modification, fiber preparations, and medical therapy are often... (Review)
Review
Severe long-term complaints of dumping occur in a small number of patients after gastric surgery. Dietary modification, fiber preparations, and medical therapy are often ineffective. In these severely affected patients administration of the somatostatin analog octreotide before meals appears to be a promising new strategy. The effects of octreotide on both gastrointestinal transit time and hormonal changes appear to contribute to the benefits seen in dumping syndrome. However, as the majority of studies conducted have employed only a single dose of octreotide, careful long-term assessment of the nutritional and metabolic effects will be required. Recent results suggest that octreotide may be administered up to 2 hr before a meal and therefore has a sufficiently long duration of action to be of practical long-term use. Moreover, general improvements in life-style, as well as beneficial effects on symptoms, have been reported with long-term treatment, although the potential development of diarrhea will require careful monitoring. The development of an oral or nasal formulation should further improve the practical application of octreotide as a treatment for dumping syndrome.
Topics: Clinical Trials as Topic; Dose-Response Relationship, Drug; Dumping Syndrome; Gastric Emptying; Humans; Octreotide; Time Factors
PubMed: 8425449
DOI: 10.1007/BF01307556 -
The American Journal of the Medical... Oct 1990One of the exciting recent developments in endocrinology research has been the introduction of the somatostatin analog, octreotide into clinical practice. Octreotide... (Review)
Review
One of the exciting recent developments in endocrinology research has been the introduction of the somatostatin analog, octreotide into clinical practice. Octreotide provides a new therapeutic tool for diseases in which somatostatin or somatostatin-like products are secreted abnormally. Unfortunately, early experience was obtained largely with uncontrolled, compassionate drug use. When clinical information regarding octreotide is critically reviewed, evaluation is hampered by the lack of long-term studies with adequate numbers of patients and controls. Nevertheless, the information available does indicate that octreotide is promising in the acute treatment of some of the manifestations of the carcinoid syndrome, including carcinoid crisis. Similarly, octreotide ameliorates symptoms of other gut neuroendocrine tumors, particularly vasoactive intestinal peptide (VIP)-secreting tumors. Octreotide also has potential in the management of growth-hormone-secreting tumors. Long-term treatment with octreotide for these diseases requires more information regarding alterations in disease progression and development of adverse effects including variable effects on blood sugar regulation and steatorrhoea. Octreotide also has been used in nonmalignant gastrointestinal disorders, but larger studies are necessary before recommendations regarding these applications can be made. The cost of octreotide, as may be expected, is high but is justified for patients with the specific indications outlined in this review. These indications may change as understanding of the drug increases. Octreotide offers promise, particularly as acute treatment for the troublesome symptoms of several neuroendocrine disorders.(ABSTRACT TRUNCATED AT 250 WORDS)
Topics: Drug Interactions; Humans; Octreotide
PubMed: 2248280
DOI: 10.1097/00000441-199010000-00011