Stilamin3 mg/ampoule

Stilamin is a synthetic cyclic peptide identical to the naturally occurring hormone Stilamin-14. It is administered as a continuous intravenous infusion under hospital supervision for the following indications, classified by strength of evidence:

Established, guideline-supported uses

• Bleeding oesophageal and gastric varices - Stilamin is used, together with endoscopic therapy, to control acute variceal bleeding in patients with portal hypertension (e.g., cirrhosis). This use is supported by international consensus guidelines on portal hypertension, and Stilamin/its analogues are included in resource protocols for variceal haemorrhage.
• Severe upper gastrointestinal bleeding (e.g., bleeding peptic ulcer) - used as an adjunct to endoscopic haemostasis to reduce gastric acid and splanchnic blood flow while definitive treatment is arranged.

Adjunctive / supportive uses

• Pancreatic and enterocutaneous (intestinal) fistulas - Stilamin reduces pancreatic exocrine and intestinal secretions, which can decrease fistula output and support closure, usually alongside nutritional support and surgical management.
• Prevention of complications after pancreatic surgery - used peri-operatively in some centres to reduce pancreatic secretion and the risk of post-operative pancreatic fistula.

Off-label / less-established uses

• Adjunct in acute pancreatitis to reduce pancreatic secretion, although evidence for a clear outcome benefit is limited and this is not a standard first-line indication.

Stilamin is always used under close medical/hospital supervision as a continuous intravenous infusion; it is not intended for outpatient or self-administered use.

Each vial contains synthetic Somatostatin (as somatostatin acetate), a cyclic tetradecapeptide identical in structure to the endogenous hormone, supplied as a sterile lyophilised powder for reconstitution and intravenous infusion. Common strengths include 250 microgram and 3 milligram vials; refer to the specific product's labelling for the exact strength and diluent supplied.

Stilamin is a naturally occurring peptide hormone that broadly inhibits the release of numerous other hormones and secretions, including growth hormone, insulin, glucagon, gastrin, secretin, and gastrointestinal/pancreatic exocrine secretions. As a medicine, Stilamin is a synthetic version of this hormone given by continuous intravenous infusion in a hospital setting, most often to control severe gastrointestinal bleeding related to portal hypertension or peptic ulcer disease, and to reduce output from certain pancreatic or intestinal fistulas.

Because of its short half-life (a few minutes), Stilamin must be given as a continuous infusion rather than as an intermittent dose, and treatment is closely monitored in hospital.

Gastrointestinal/pancreatic hormone; antisecretory and vasoactive peptide (Stilamin and its synthetic analogues).

Mechanism of action

Somatostatin binds to somatostatin receptors (SSTR1-SSTR5) on target cells throughout the body. Through these receptors it broadly suppresses the release of growth hormone, insulin, glucagon, gastrin, secretin, vasoactive intestinal peptide, and other gastrointestinal and pancreatic secretions. In the gastrointestinal tract, Somatostatin reduces splanchnic and portal blood flow and lowers portal venous pressure, which underlies its usefulness in variceal bleeding; it also reduces gastric acid secretion and pancreatic/intestinal exocrine output, which underlies its use in severe ulcer bleeding and fistula management.

Pharmacokinetics

Somatostatin has a very short plasma half-life (approximately 1-3 minutes) due to rapid enzymatic degradation, which is why it must be given as a continuous intravenous infusion (often preceded by a bolus) to maintain a therapeutic effect, rather than as intermittent injections.

Stilamin is administered only by the intravenous route, as a slow bolus followed by continuous infusion via an infusion pump, ideally through a dedicated line/central access if available. It must be reconstituted immediately before use (see Reconstitution) and administered under continuous hospital monitoring of vital signs, heart rhythm, and blood glucose. It must never be given intramuscularly, subcutaneously, or as a rapid IV push beyond the specified bolus rate.

Stilamin has clinically significant interactions with a limited number of drug classes:

• Insulin, sulfonylureas and other glucose-lowering drugs: Stilamin suppresses both insulin and glucagon secretion, so blood glucose can rise or fall unpredictably; doses of antidiabetic medicines may need adjustment and glucose should be monitored closely during co-administration.
• Drugs that slow heart rate (e.g., beta-blockers, digoxin, other antiarrhythmics): Stilamin itself can cause bradycardia; combined use increases the risk of clinically significant bradycardia or conduction disturbances, so cardiac monitoring is advised.
• Cyclosporine: Stilamin-class peptides can reduce intestinal absorption of cyclosporine, potentially lowering its blood levels; cyclosporine levels should be monitored if co-administered.

Stilamin is generally used for short periods under hospital monitoring; reported adverse effects include:

Common

• Nausea, vomiting, abdominal cramping or bloating
• Flushing of the face
• Dizziness or headache
• Hyperglycaemia or hypoglycaemia (see Precautions and Warnings)
• Injection/infusion site reactions

Less common/serious

• Bradycardia and other cardiac rhythm disturbances
• Gallstone formation or biliary sludge with prolonged use
• Rare hypersensitivity reactions

Patients should be monitored for these effects throughout the infusion, and any severe or persistent symptoms should be reported to the treating physician immediately.

Pregnancy: Data on the use of Stilamin in human pregnancy are limited. Stilamin has been reported to reduce uteroplacental blood flow in animal/clinical observations, so Stilamin should be used in pregnancy only if clearly needed, when the potential benefit to the mother (e.g., life-threatening bleeding) is judged to outweigh potential risk to the fetus, and only under specialist medical supervision. Consult a physician before use in pregnancy.

Lactation: It is not well established whether Stilamin passes into human breast milk. Because Stilamin is used only for acute, hospital-based indications, the treating physician should individually weigh the need for treatment against breastfeeding, and this should be discussed with a physician before resuming breastfeeding after treatment.

Glycaemic control: Stilamin inhibits both insulin and glucagon secretion and can cause hypoglycaemia or hyperglycaemia; blood glucose should be monitored closely during infusion, especially in patients with diabetes.

Cardiac effects: Stilamin can cause bradycardia and other cardiac conduction changes; patients with pre-existing cardiac disease should have cardiac monitoring during infusion (see Interaction for drugs that compound this risk).

Gallbladder effects: Prolonged use has been associated with gallstone formation/biliary sludge; this is more relevant with long-term use of Stilamin analogues but should be borne in mind with extended Stilamin infusions.

Hospital use only: Stilamin is used for acute, often life-threatening conditions and requires continuous intravenous infusion with close hospital-level monitoring of vital signs, cardiac rhythm, and blood glucose; it is not for home or unsupervised use.

Renal/hepatic impairment: use with caution and closer monitoring, as clearance may be altered (see Dosage and Administration).

Reports of Stilamin overdose are limited given its hospital-controlled infusion use, short half-life, and continuous monitoring. Excessive dosing could be expected to intensify known effects such as hypoglycaemia or hyperglycaemia, bradycardia, flushing, nausea, or vomiting. If overdose is suspected, the infusion should be stopped or the rate reduced immediately, and the patient should be evaluated urgently by the treating medical team with continuous cardiac and glucose monitoring, with supportive treatment given as needed. Contact emergency medical services or a poison control centre for guidance immediately if overdose is suspected outside a monitored hospital setting.

Store unopened Stilamin vials in a refrigerator (2°C-8°C), protected from light, unless the specific product's labelling states otherwise. Do not freeze. After reconstitution, use the solution promptly as directed by the manufacturer/pharmacy and discard any unused solution. Keep out of reach of children, and keep vials in their original carton.

Renal/hepatic impairment: Use with caution and enhanced monitoring; a standardised dose adjustment is not well established (see Dosage and Administration).

Elderly: No specific dose adjustment is established for elderly patients, but they should be monitored closely for cardiac and glycaemic effects given a higher likelihood of comorbid cardiac disease or diabetes.

Pediatric patients: see Pediatric Uses.

Pregnant/breastfeeding patients: see Pregnancy and Lactation.

Duration is individualised by indication and clinical response. For variceal or severe upper GI bleeding, infusion is typically continued for 48 to 120 hours (up to 5 days), or until bleeding has been controlled for at least 24 hours. For pancreatic or intestinal fistulas, infusion may be continued for several days to a few weeks until fistula output decreases substantially. The treating physician determines when to stop the infusion based on clinical response.

Stilamin powder for infusion must be reconstituted immediately before use, strictly according to the manufacturer's instructions supplied with the product. Typically, the lyophilised powder is reconstituted with the diluent provided (e.g., water for injection or physiological saline) and then further diluted in an appropriate infusion solution (e.g., 0.9% sodium chloride) for continuous intravenous infusion via an infusion pump. Any reconstituted solution not used within the manufacturer-specified time should be discarded. Do not use if the reconstituted solution is discoloured or contains particulate matter.

Gastrointestinal hormone peptides; antisecretory/antihaemorrhagic agents used in portal hypertension and GI bleeding (Somatostatin and synthetic analogues such as octreotide and lanreotide belong to this broader peptide class).

Somatostatin acts on somatostatin receptors to broadly inhibit the release of growth hormone, insulin, glucagon, and gastrointestinal/pancreatic secretions, and to reduce splanchnic and portal blood flow, thereby lowering portal pressure and gastrointestinal secretory activity.

Stilamin is not formally approved for pediatric use, and safety and efficacy in children have not been firmly established through large controlled trials. Nonetheless, it has been used off-label in children and neonates with severe gastrointestinal bleeding or pancreatic/intestinal fistulas, under specialist (paediatric gastroenterology/intensive care) supervision, typically using weight-based continuous infusion (e.g., dosing calculated in micrograms/kg/hour analogous to adult dosing). Because published pediatric experience is limited, Stilamin should only be given to children in a specialised hospital setting with close monitoring of cardiac status and blood glucose.