Aminocaproic acid 5% 100ml

Pharmacological action:

Hormonal drug, a somatostatin analogue. Is a synthetic oktapeptid, which is a derivative of the natural hormone somatostatin and having similar pharmacological effects, but a much greater duration of action. The drug inhibits pathologically increased secretion of growth hormone and of peptides and serotonin, produced in the gastro-entero-pancreatic endocrine system.

The use of Octreotide during or after surgery on the pancreas reduces the incidence of typical postoperative complications (e.g. pancreatic fistula, abscess, sepsis, postoperative acute pancreatitis).

Pharmacokinetics:

Absorption

After p/to the introduction of octreotide is rapidly and completely absorbed. Cmax of octreotide in the blood plasma is achieved within 30 min.

Distribution

The plasma protein binding is 65%. The binding of Octreotide with formed elements of the blood is extremely low. Vd is 0.27 l/kg.

Excretion

Total body clearance is 160 ml/min, About 32% is excreted unchanged by the kidneys. After p/to the injection of the drug T1/2 of octreotide is 100 min. After the on/in the excretion of octreotide is carried out in 2 phases with T1/2 10 min and 90 min, respectively.

Pharmacokinetics in special clinical cases

In patients older reduced clearance, and T1/2 increases.

In severe renal insufficiency, clearance is decreased 2 times.

Indications:

– prevention and treatment of complications after operations on the abdominal organs

– stopping bleeding and prevention of rebleeding from esophageal varices in patients with cirrhosis of the liver

– treatment of acute pancreatitis

– peptic ulcer bleeding.

Dosing regimen:

In the treatment of acute pancreatitis the drug is injected p/to a dose of 100 µg 3 times/day for 5 days. You can assign up to 1200 mg/day.

For the prevention of complications after operations on the pancreas the first dose of 100 mcg administered s/C for 1 h before laparotomy then after the operation, enter n/a 100 µg 3 times/day for 7 consecutive days.

To stop bleeding from esophageal varices is injected in/in the dose of 2.5-50 µg/C in the form of prolonged infusions over 5 days. In elderly patients is not necessary to reduce the dose of Octreotide.

To stop ulcer bleeding administered at a dose of 25 mcg/h in a/V infusion for 5 days.

Side effects:

From the digestive system: possible anorexia, nausea, vomiting, spasticskie pains in the abdomen, feeling of bloating, excessive gas, loose stools, diarrhea, steatorrhea. Although the allocation of fat with faeces may increase, there is no indication that long-term treatment with octreotide may result in development of malabsorption (malabsorption). Rare – phenomena resembling acute intestinal obstruction. In some cases, acute pancreatitis without cholestasis, hyperbilirubinemia, combined with an increase in the activity of alkaline phosphatase, GGT, and to a lesser extent, other transaminases. Long-term use the formation of stones in the gallbladder. There are reports of rare cases of acute pancreatitis, which developed during the first hours or days of use and disappeared after discontinuation of octreotide.

From cardiovascular system: in single cases – arrhythmia, bradycardia.

From carbohydrate metabolism: possible violation of tolerance to glucose after a meal (due to suppression of the drug the secretion of insulin), hypoglycemia rarely with prolonged treatment of persistent hyperglycemia.

Local reactions: there may be pain, itching or burning, redness, swelling (usually disappear within 15 min).

Other: allergic reactions, alopecia.

Contraindications:

– hypersensitivity to the drug.

Caution should be used in case of cholelithiasis, diabetes, pregnancy, lactation.

Pregnancy and lactation:

Adequate and well-controlled clinical studies safety of the use of Octreotide was conducted. Use in pregnancy and lactation is possible only on the absolute indications, when the expected benefit of therapy for the mother outweighs the potential risk to the fetus. Category effects on the fetus B.

Special instructions:

In patients with diabetes treated with insulin, octreotide may reduce insulin requirements.

If gallstones are identified before treatment, the question of the use of octreotide is solved individually, depending on the ratio of the potential benefits of therapy and the possible risk associated with the presence of stones in the gallbladder.

Side-effects from the digestive system can be reduced if the injection of octreotide to produce in between meals or before bed.

To reduce the effects of discomfort at the injection site is recommended to bring the solution of the drug before administration to room temperature and enter the smaller amount of the drug. You should avoid multiple injection in the same place at short intervals of time.

Overdose:

Symptoms: short-term reduction in heart rate, feeling tide blood to a person, spastic abdominal pain, diarrhea, nausea, a feeling of emptiness in the stomach.

Treatment: symptomatic therapy.

Drug interactions:

Octreotide reduces the absorption of cimetidine, cyclosporine, diuretics, beta-adrenoblokatorov, antagonists of calcium, insulin and oral hypoglycemic drugs.

While the use of octreotide and bromocriptine increases the bioavailability of the latter.

Drugs, metabolized by the isoenzymes of cytochrome P450 and have narrow therapeutic range of doses should be administered with caution.

Terms and conditions of storage:

List B. the Drug should be stored out of the reach of children, protected from light place at a temperature of from 8° to 20°C.