Vials of SII SOMASTIN contain synthetic somatostatin (as the
acetate) as a white, freeze-dried, sterile and pyrogen-free
powder. Two strengths are available: 250 mcg and 3 mg.
Each vial of SII SOMASTIN contains:
Somatostatin 250 mcg or 3.0 mg*
D-Mannitol(excipient) 5.0 mg
*Corresponding to 300 µg and 3.6 mg of somatostatin
Each vial of the strength 250 mcg and 3.0 mg is accompanied
by a diluent ampoule containing 1 ml of isotonic, sterile
and pyrogen - free Sodium Chloride Injection solution.
INDICATIONS AND USE
SII SOMASTIN is indicated for:
- Severe acute haemorrhage from oesophageal varices.
- Severe acute haemorrhage from gastric or duodenal ulcers,
or accompanying acute erosive or haemorrhagic gastritis.
- Adjuvant treatment in pancreatic, biliary and intestinal
- Prophylaxis and treatment of postoperative complications
following pancreatic surgery.
- Adjuvant treatment in diabetic ketoacidosis.
- Treatment of acute pancreatitis.
SII SOMASTIN is a synthetic cyclic 14 amino-acid peptide,
which is identical in structure and action to natural somastin.
By i.v. 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 gastro-intestinal tract.
Physiologically, somatostatin is found mainly in the gastrointestinal
tract and in the hypothalamus.
Somatostatin inhibits the release of gastrin, gastric acid
and pepsin which supports its indication in the treatment
of upper G.I. 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
Somastin reduces both pancreatic endocrine and exocrine secretion
which makes it effective in the prophylaxis and treatment
of postoperative complications of pancreatic surgery and pancreatic
The positive effect of somatostatin in the management of diabetic
ketoacidosis can be ascribed to its suppression activity of
In healthy persons the plasma level of endogenous somatostatin
is low, generally well under 175 ng/L.
Following i.v. Administration, somatostatin shows a very short
plasma half-life which, as measured by radioimmunoassay, lies
between 1,1 and 3 minutes in normal subjects between 1, 2
and 4,8 minutes in subjects with liver disease, between 2,6
and 4,9 minutes in subjects with chronic renal failure.
Following an i.v. Infusion at a rate 75 µg/h, the plateau
level was obtained within 15 minutes and reached 1250 ng/L.
The metabolic clearance rate was around 1L/min. and the half-life
around 2,7 min.
After i.v. injection of 2µg of 125-I thyrosine somatostatin,
urinary excretion contained 40% of the radioactivity after
4 hours and 70% after 24 hours.
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
It has cyctoprotective activity at pancreatic parenchyma,
liver and stomach
DOSAGE AND ADMINISTRATION
SII SOMASTIN is given intravenously, by slow bolus injection(3
to 5 minutes) of 250 mcg or by continuous infusion at a rate
of 250 mcg/hour(equivalent of approximately 3,5 µg/kg
The lyophilised powder should be reconstituted with the physiological
sodium chloride solution immediately prior to use.
For continuous infusion one 3 mg SII SOMASTIN vial should
be used to prepare a 12 hours infusion. The solution may be
either saline or 5% dextrose and should be adjusted to guarantee
an outflow of 250 mcg somatostatin / hour. The use of a perfusion
syringe is recommended.
- Tr e a t m e n t o f s e v e r e a c u t e b l e e d i n
g f r o m t h e u p p e r gastrointestinal tract, including
from oesophageal varices.
It is recommended to start by a slow intravenous injection
of 250 mcg of SII SOMASTIN as loading dose, then immediately
followed by an intravenous infusion at a rate of 250 mcg/h.
In case of interruption of more than 3 to 5 minutes between
two infusions, an additional slow i.v. Injection of 250 mcg
is recommended to ensure a continuous treatment. Once the
haemorrhage has stopped(usually in less than 12 to 24 hours),
treatment should be continued for 48-72 hours in order to
Treatment up to 120 hours has been routinely performed in
- Adjuvant treatment in pancreatic, biliary and intestinal
A continuous infusion of SII SOMASTIN at a rate of 250 mcg/h
is recommended until closure of the fistula (2-20 days). This
infusion should be performed in addition to total parenteral
nutrition. Once the fistula has been closed, treatment should
be continued for 1 to 3 days and stopped progressively in
order to avoid rebound effect.
- Prophylactic treatment of postoperative complications following
SII SOMASTIN is administered at the beginning of the surgical
intervention at a rate of 250 mcg/h and treatment is continued
for 5 days.
Adjuvant treatment in diabetic ketoacidosis:
In patients with ketoacidosis, infusion of 100-500 µg/h
of somatostatin associated with insulin therapy (bolus of
Infusion of 1-4.8 I.U./h) was capable of restoring euglycemia
within 4 hours and resolving acidosis within 3 hours.
SII SOMASTIN is contra-indicated:
- During pregnancy and the immediate post-partum period (puerperium)
as well as during lactation. There is no evidence of the drug's
safety in human pregnancy nor is there evidence from animal
work that it is free from hazard. Avoid in pregnancy unless
there is no safer alternative.
- In states of proven hypersensitivity to somatostatin.
Due to its inhibitory effect on the secretion of insulin and
glucagon, the administration of SII SOMASTIN can, at the onset
of treatment, lead to a transient fall in blood glucose level.
Caution is, therefore, called for in insulin- dependent diabetic
patients in whom blood glucose should be measured every 3-4
hours. Simultaneous administration of insulin-requiring sugars
should, if possible, avoided. If necessary, insulin should
INTERACTION WITH OTHER DRUGS
Since somatostatin lengthens the time of hexobarbital-induced
sleep and potentiates the action of pentetrazol, SII SOMASTIN
should not be administered concomitantly with these drugs
or with drugs exerting the same effects.
Nausea, vertigo and flushing have been reported rarely. Nausea
and vomiting have been reported when the infusion rate is
greater than 50 µg/min.
Physical incompatibilities with other drugs have not been
tested, therefore SII SOMASTIN should be administered alone
in the syringe and in infusion solutions.
STABILITY AND STORAGE
Vials of SII SOMASTIN should be stored at 2 - 8°C and
should not be used after the expiry date stated on the package.
Solutions of SII SOMASTIN in physiological sodium chloride
are stable for 24 hours.
SII SOMASTIN 250 (250 mcg) vial plus 1 ml sodium chloride
injection (diluent) ampoule, sterile disposable syringe &
needle. Sii SOMASTIN 3000 (3 mg) vial plus 1 ml sodium chloride
injection (diluent) ampoule. Drugs should be stored out of
reach of children