Anfarm Hellas




Full Prescribing Info
Somatostatin acetate.
Each vial contains: Somatostatin Acetate Hydrate eq. to Somatostatin 3 mg.
Pharmacology: Pharmacodynamics: Somatostatin is a synthetic cyclic 14 amino-acid peptide, which is identical in structure and action to natural somatostatin.
By IV infusion in humans, somatostatin causes inhibition of growth hormone, thyroid stimulating hormone, insulin and glucagon secretion as well as inhibition of gastric acid secretion. It also affects the absorption, motility, splanchnic blood flow and trophic functions of the gastrointestinal tract (GIT).
Physiologically, somatostatin is found mainly in the GIT and in the hypothalamus.
Somatostatin inhibits the release of gastrin, gastric acid and pepsin, which supports its indication in the treatment of upper gastrointestinal haemorrhage. Furthermore, somatostatin is capable of reducing remarkably splanchnic blood flow without causing significant variations in the systemic arterial pressure, which proves to be valuable for the management of oesophageal variceal haemorrhage.
Somatostatin reduces both pancreatic endocrine and exocrine secretion, which makes it effective in the prophylaxis and treatment of postoperative complications of pancreatic surgery.
The positive effect of somatostatin in the management of diabetic ketoacidosis can be ascribed to its suppression activity of glucagon secretion.
Mechanism of Action: Somatostatin is a 14-amino acid oligopeptide which was originally isolated from the hypothalamus of animals and, later, found in both epithelial cells and nerve fibers throughout the whole of the digestive system. Somatostatin is thought to act mainly as a local transport substance, thus having a role in both the regulation of endocrine and exocrine secretions and of gastrointestinal motility. When administered at pharmacological doses, somatostatin will inhibit gastrointestinal function and motility, as well as resorption within the digestive tract.
Pharmacokinetics: In healthy persons, the plasma level of endogenous somatostatin is low, generally well <175 ng/L.
Following IV administration, somatostatin shows a very short plasma half-life (t½) which, as measured by radioimmunoassay, lies between 1.1 and 3 min in normal subjects, between 1.2 and 4.8 min in subjects with liver disease, between 2.6 and 4.9 min in subjects with chronic renal failure.
Following an IV infusion at a rate of 75 mcg/hr, the plateau level was obtained within 15 min and reached 1250 ng/L. The metabolic clearance rate was around 1 L/min and the t½ around 2.7 min.
After IV injection of 2 mcg of 125 L-thyrosine somatostatin urinary excretion contained 40% of the radioactivity after 4 hrs and 70% after 24 hrs.
Somatostatin is rapidly metabolized in the liver through the action of endopeptidases and aminopeptidases, resulting in cleavage between the N-terminus and the cyclized portion of the molecule.
Treatment of acute gastrointestinal hemorrhage, resulting from gastric or duodenal ulcers, hemorrhagic gastritis and bleeding esophageal varices, whether suspected solely on clinical grounds or proven by endoscopy.
Treatment of intestinal and pancreatic fistulae.
Symptomatic treatment of excessive secretion from endocrine tumors of the gastrointestinal tract.
The prevention of complications after pancreatic surgery or endoscopic retrograde cholangiopancreatography (ERCP).
Dosage/Direction for Use
Adults: The recommended dose is 3.5 mcg/kg body weight/hr, or usually 6 mg/24 hrs for a 75-kg patient, given as a continuous infusion of 250 mcg/hr. The infusion rate should then be adjusted for 12 or 24 hrs (for 3 or 6 mg respectively).
Treatment of Gastrointestinal Hemorrhage: Somatostatin infusion should be initiated before endoscopy, as soon as possible after the first signs of bleeding, and continued during 5 days, the minimum duration being 48 hrs. In addition to the continuous infusion, a bolus injection of 3.5 mcg/kg body weight (1 vial of Somatostatin 0.25 mg for a 75-kg patient) should be given immediately after the start of the continuous infusion and another bolus about 1 min before endoscopy. The bolus must be given slowly (at least 1 min). After endoscopic treatment, similar boluses should also be given when the patient shows clinical signs of bleeding.
Treatment of Fistulae or Excessive Secretion from Endocrine Tumors: A bolus injection is not necessary. Healing of fistulae may be expected in most patients within 7-14 days, although longer (or shorter) periods are possible. After healing, only half the dose should be infused for the next 48 hrs, in order to avoid a possible rebound effect.
Elderly: Adjustment of the dose is recommended in elderly patients with severe renal impairment (see Renal Impairment as follows).
Renal Impairment: In patients with severe renal failure (CrCl ≤30 mL/min), the dose should be reduced to 1.75 mcg/kg body weight/hr for continuous infusion and 1.75 mcg/kg body weight for bolus dose.
Hepatic Impairment: No dose adjustment is needed in patients with solely hepatic impairment. The patient should be closely monitored after treatment discontinuation.
Administration: Due to its short plasma t½, 1-2 min, Somatostatin should be administered as a continuous IV infusion. It should be reconstituted immediately before use by adding the 1-mL ampule of sodium chloride solution (0.9%) for parenteral use.
Symptoms: Reported cases of somatostatin overdose did not reveal other safety hazard than the undesirable effects observed at recommended doses.
Treatment: Close monitoring of blood glucose level, cardiovascular parameters, renal function, and plasma electrolytes is recommended in case of somatostatin overdose.
After interruption of a somatostatin IV infusion given at therapeutic dose, the t½ of somatostatin in blood is about 2 min.
Treatment of overdose is symptomatic, no specific antidote is known.
Known hypersensitivity to somatostatin or somatostatin analogues.
Special Precautions
Somatostatin is intended for hospital use.
Half of the recommended dose should be given to patients with severe renal failure (CrCl ≤30 mL/min). Patients receiving Somatostatin should be kept under strict medical observation. The bolus doses should be given slowly over at least 1 min. The infusion must be given continuously. At the beginning of the infusion, hypoglycemia may occur, possibly followed 2-3 hrs later by a rise in blood sugar due to alterations in the balance between the counterregulatory hormones, insulin and glucagon. For this reason, blood sugar must be measured every 4-6 hrs.
Precaution is recommended in case of simultaneous administration of any form of sugar (see Interactions).
Somatostatin may induce the following pharmacodynamic cardiovascular effects: Transient systemic hypertension, transiently reduced cardiac output, increased pulmonary arterial pressure and central venous pressure, systemic hypotension, bradycardia, atrioventricular block.
Consequently, patient's vital signs should be monitored during the initial phase of somatostatin administration, especially after bolus injection. Caution should be exercised in patients with compromised cardiovascular status or history of cardiac arrhythmia, who may not be able to compensate for these effects.
As glomerular filtration rate, urine flow and sodium blood level may be decreased during somatostatin treatment, regular checks of the renal function and plasma electrolytes are recommended.
Somatostatin causes inhibition of the intestinal absorption of certain nutriments. It also inhibits other gastrointestinal hormone secretions. Abrupt interruption of infusion may result in a rebound effect, especially in patients treated for fistulae. Therefore, after healing of fistulae, only half of the dose should be infused for the next 48 hrs, in order to avoid a possible rebound effect.
The effects of somatostatin on vital signs, glycemia, and renal function should be taken into consideration for the patient's follow-up after treatment discontinuation.
Effects on Ability to Drive and Use Machines: Not applicable.
Use in Pregnancy & Lactation: There are no adequate data from the use of somatostatin in pregnant women. Animal reproduction studies were not performed. Somatostatin should not be used during pregnancy unless clearly necessary.
Somatostatin should not be used during lactation.
No studies have been reported concerning the pharmacokinetics of somatostatin in pregnancy and lactation in animals.
Use in Children & Adolescents: No adequate clinical studies establishing safety and efficacy of Somatostatin in children and adolescents have been done. Therefore, use is not recommended in this population of patients.
Use In Pregnancy & Lactation
There are no adequate data from the use of somatostatin in pregnant women. Animal reproduction studies were not performed. Somatostatin should not be used during pregnancy unless clearly necessary.
Somatostatin should not be used during lactation.
No studies have been reported concerning the pharmacokinetics of somatostatin in pregnancy and lactation in animals.
Adverse Reactions
Nausea, vertigo and flushing have been reported rarely. Nausea and vomiting have been reported when the infusion rate is >50 mcg/min.
Drug Interactions
Taking into account the wide range of somatostatin pharmacodynamic effects on various regulating systems, there is a potential for many pharmacodynamic interactions.
Pharmacodynamic interactions with possible clinical relevance have been observed with drugs that also influence blood glucose regulation, plasma renin level and arterial blood pressure, showing that somatostatin may modify the effects of these drugs on these parameters.
Simultaneous administration of any form of sugar (including glucose and fructose solutions or total parenteral nutrition) favors glycemic disturbances and requires a closer monitoring of blood sugar. Administration of insulin may be required.
Incompatibilities: None known.
Somatostatin is compatible with glucose (5% and 10%) and fructose solutions (40%).
Caution For Usage
Special Precautions for Disposal and Other Handling: Chemical in-use stability has been demonstrated for up to 48 hours at (25±2)°C and at (5±3)°C.
From a microbiological point of view, the product should be used immediately. If not used immediately, in-use storage times and conditions prior to use are the responsibility of the user and would normally not be longer than 24 hours at 2 to 8°C, unless reconstitution/dilution has taken place in controlled and validated aseptic conditions. Any unused solution should be discarded.
Store at temperatures not exceeding 30°C.
Store in the original container in order to protect from light.
ATC Classification
H01CB01 - somatostatin ; Belongs to the class of antigrowth hormone. Used in hypothalamic hormone preparations.
Powd for inj (vial) 3 mg (white cake with cylinder shape) x 1's.
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