Precautions for medication and usage and dosage are all in the instructions.
This is the specific instructions:
Chinese alias: octreotide acetate injection, sandostatin
Octreotide acetate injection
Drug category: Antitumor drugs from natural sources.
chemical composition
The active ingredient is octreotide acetate, whose chemical name is D- phenylalanine -L- cysteine -L- phenylalanine -D- trypyl -L- lysyl -L- threonyl -L- threonol ring 2→7) Disulfide acetate.
Excipients: lactic acid, mannitol
gender
This product is a colorless and clear liquid.
Pharmacology pharmacokinetics
The drug is a synthetic octapeptide derivative of natural somatostatin, which retains similar pharmacological effects to somatostatin and has a lasting effect. This product can inhibit the secretion of peptide and growth hormone in the endocrine system of gastrointestinal pancreas.
However, in animals, this product has stronger inhibitory effect on growth hormone, glucagon and insulin than somatostatin, and has higher selectivity for growth hormone and glucagon. Long-term (26 weeks) administration, the dose of rats reached 1 mg/kg/ day (intraperitoneal injection) and the dose of dogs reached 0.5 mg/kg/ day (intravenous injection), which was well tolerated.
Studies on healthy subjects show that this product can inhibit the following situations: the release of growth hormone (GH) caused by arginine, exercise and hypoglycemia of insulin; Postprandial secretion of insulin, glucagon, gastrin, other peptides in the gastrointestinal pancreatic system, and secretion of insulin and glucagon caused by arginine; The release of thyrotropin (TSH) caused by thyrotropin releasing hormone (TRH).
In patients with acromegaly (including patients who failed in surgery, radiotherapy or dopamine agonist treatment), the drug can reduce the plasma concentration of growth hormone and/or auxin mediator C. Almost all patients' serum growth hormone concentrations have been significantly reduced (50% or more), and half of them can reach normal (plasma GH
In patients with gastrointestinal pancreatic endocrine system tumor, the drug can improve many clinical symptoms because of its wide activity. For those who have undergone surgery, hepatic artery embolization and various chemotherapy (such as streptozotocin and 5- fluorouracil) but still have serious symptoms related to tumor, this product can improve the clinical condition and relieve symptoms.
The effects of this product on different tumors are as follows:
Carcinoid syndrome: it can improve the symptoms such as flushing and diarrhea, and the discharge of plasma 5- hydroxytryptamine and urine 5- hydroxyindoleacetic acid in some patients is reduced. In some cases where the curative effect is not obvious, the continuous treatment of this product should not exceed 1 week.
* Vasoactive intestinal peptide tumor syndrome: The main biochemical feature of the disease is the excessive production of vasoactive intestinal peptide (VIP), so the main clinical manifestation of vasoactive intestinal peptide tumor syndrome is severe secretory diarrhea. In most cases, this drug can relieve severe diarrhea, thus improving the quality of life of patients. This product can also improve the corresponding water and electrolyte deficiency, such as hypocalcemia. Therefore, gastrointestinal or parenteral replacement therapy can be stopped. Computed tomography showed that some patients' tumor growth was delayed or stopped, and some even shrank, especially some patients with liver metastasis. Clinical improvement is usually accompanied by the decrease of plasma vasoactive intestinal peptide concentration, even normal.
* Glucagon tumor: The disease is characterized by necrotizing wandering rash. This product has little effect on mild diabetes mellitus which is easy to be complicated by this kind of patients, and it is usually unnecessary to reduce the dosage of insulin or oral hypoglycemic drugs. The product can reduce the diarrhea of the affected patients, thus gaining weight. Although this product can rapidly reduce the plasma glucagon concentration in most cases, this phenomenon is not lasting. Despite this, the patient's clinical symptoms continued to improve.
* gastrinoma/Zhuo-Ai syndrome: For recurrent peptic ulcer caused by excessive gastric acid secretion caused by chronic gastrin stimulation, both selective H2 receptor antagonists and antacids are not effective, and some obvious diarrhea symptoms are rarely relieved. This product can be used together with H2 receptor antagonists to inhibit excessive gastric acid secretion, relieve the clinical symptoms (including diarrhea) of half patients, and relieve other symptoms (such as tidal waves) that may be caused by peptides produced by tumors.
* insulinoma: This drug can make the immune response insulin concentration in blood circulation short (about 2 hours), but it will not decrease permanently. For tumor patients who can be operated, preoperative use of this product can help them recover and maintain normal blood sugar. For patients with inoperable benign or malignant tumors, this product is also helpful for blood sugar control of some patients, even if it is not accompanied by a continuous decline in blood insulin concentration.
* Growth hormone releasing factor tumor: This rare tumor is characterized by only secreting growth hormone releasing factor (GRF) or other active peptides at the same time, which leads to acromegaly symptoms and somatic symptoms. Among the two cases of reactive acromegaly observed so far, this drug has improved the clinical manifestations of one case, which may be due to inhibiting the secretion of GRF and growth hormone, and may shrink the swollen pituitary gland.
* Prevention of postoperative complications of pancreas: In patients undergoing pancreatic surgery, using this product for perioperative and postoperative treatment can reduce the incidence of typical postoperative complications (such as pancreatic fistula, sepsis secondary to abscess and acute postoperative pancreatitis).
* Esophageal-gastric varices bleeding: The clinical trial results show that this product combined with sclerosing agent can improve the bleeding control rate, prevent early rebleeding, reduce blood transfusion and improve the 5-day survival rate. The exact mechanism of its action on the disease has not been determined, although there is evidence that the product can reduce visceral blood flow by preventing the secretion of vasoactive hormones (such as VIP and glucagon).
adapt to
For acromegaly patients who have failed in surgery, radiotherapy or dopamine agonist treatment, symptoms can be controlled and the concentrations of GH and auxin medium C can be reduced. This product is also suitable for acromegaly patients who are unable or unwilling to operate, and intermittent patients whose radiotherapy has not yet been effective.
Relieve symptoms and signs related to gastrointestinal pancreatic endocrine tumors. There is sufficient evidence that this product is effective for the following tumors: carcinoid tumor with carcinoid syndrome: VIP tumor, glucagon tumor. The effective rate of this product is 50% for the following tumors: gastrinoma/Zoroach-Aidan syndrome (usually used in combination with selective H2 receptor antagonists, and antacids can be added as appropriate); Islet tumor (used to prevent hypoglycemia and maintain normal blood sugar before islet tumor operation); Growth hormone releasing factor tumor. This product can only relieve symptoms and physical symptoms, but can't cure the cause.
Prevention of postoperative complications of pancreas.
Emergency treatment of esophageal and gastric varices bleeding caused by liver cirrhosis combined with special treatment (such as endoscopic sclerotherapy).
dosage
acromegaly
The initial dose was 50- 100 μg, and subcutaneous injection 1 time every 8 hours. Then adjust the dose according to the monthly assessment of growth hormone blood concentration, clinical response and tolerance. The optimal dose for most patients is 200-300 μ g/day, and the maximum dose cannot exceed 1.5 mg/day. Under the guidance of monitoring the plasma growth hormone level, it can be reduced as appropriate after several months of treatment. After one month of treatment, if the growth hormone concentration has not decreased and the clinical symptoms have not improved, the drug should be stopped.
* Gastrointestinal pancreatic endocrine tumor
The initial dose is 50 μg, subcutaneous injection, 1-2 times, daily/kloc-0 times, and then the dose can be gradually increased to 200 μg, three times a day according to tolerance and curative effect (clinical response and hormone concentration secreted by tumor). Larger doses can only be used under certain circumstances. Maintenance dose should be determined according to individual differences.
* Prevent postoperative complications of pancreas.
0. 1 mg subcutaneous injection, three times a day, continuous treatment for 7 days, the first injection should be at least 1 hour before operation.
* Esophageal-gastric variceal bleeding
After diluting the medicinal physiological saline, it was continuously administered intravenously at a rate of 25 μg/ hour for up to 5 days. For patients with liver cirrhosis and esophageal varices bleeding, this product can be continuously given intravenously at a dose of 50 μg/ hour for 5 days. Elderly patients do not need to change the dose.
Medication instructions
When intravenous drip is needed, this medicinal physiological saline is usually dissolved to the recommended concentration of 0.025 mg/mL. Injection should be continuously dripped by infusion pump for 20 hours. Repeat the above treatment until the required treatment cycle is reached. This product can also be dripped in low concentration or glucose solution.
Let the liquid reach room temperature before injection to reduce local discomfort and avoid short-term multiple injections at the same site. Multi-dose vial puncture should not exceed 10 times to prevent pollution. Prefabricated drops are stable within 24 hours.
counteraction
The main side effects of this product are local and gastrointestinal reactions. The local reactions after subcutaneous injection are pain or tingling, tingling or burning sensation at the injection site, accompanied by redness and swelling, rarely exceeding 15 minutes. If the liquid medicine is brought to room temperature before injection, or the concentration of the liquid medicine is increased by reducing the amount of solvent, local discomfort can be reduced.
Gastrointestinal side effects include loss of appetite, nausea, vomiting, spasmodic abdominal pain, abdominal distension, flatulence, loose stool, diarrhea and fatty dysentery. Although the measured fecal fat excretion may increase, there is no evidence that taking this product for a long time will lead to absorption disorder and malnutrition. In rare cases, gastrointestinal side effects can be similar to acute intestinal obstruction, accompanied by progressive epigastric pain, abdominal tenderness, muscle tension and abdominal distension. Eating should be avoided before administration (that is, injection between meals or bed rest) to reduce the occurrence of gastrointestinal side effects. Long-term use of this product may lead to gallstones.
Because this drug can inhibit the release of growth hormone, glucagon and insulin, it may lead to disorder of blood sugar regulation. Because it can reduce the postprandial glucose tolerance of patients, a few long-term drug users can cause persistent hyperglycemia. Hypoglycemia was observed.
It is reported that in rare cases, patients treated with this medicine will lose their hair.
A few cases of acute pancreatitis have been reported, but they usually occur within hours or days after starting treatment. It can gradually disappear after stopping the drug. People with gallstones may also have pancreatitis after long-term use of this product.
Some patients have abnormal liver function, including acute hepatitis without cholestasis. After stopping using this product, transaminase returns to normal. Chronic hyperbilirubinemia with elevated alkaline phosphatase, γ -glutamyltransferase and slightly elevated transaminase.
Contraindications
Allergic to octreotide or any excipient. Pregnant women, lactating women and children are prohibited.
Matters needing attention
Because pituitary adenoma secreting growth hormone may sometimes spread and cause serious complications (such as visual field defect), patients should be closely observed. If there are signs of tumor spread, other treatment methods should be considered.
It is reported that 10-20% of patients who use this product for a long time have gallstones, so gallbladder ultrasound should be performed every 6- 12 months before treatment and after medication.
In the treatment of gastrointestinal pancreatic endocrine tumors, symptoms occasionally get out of control, and serious symptoms recur quickly.
In patients with insulinoma, this product can inhibit the secretion of growth hormone and glucagon more than insulin, so it may increase the depth and time of hypoglycemia. Such patients should be closely observed, especially when starting to treat this product or changing the dose. The obvious fluctuation of blood sugar concentration can be reduced by giving small doses of this drug more frequently.
For diabetic patients receiving insulin therapy, the dosage of insulin can be reduced after using this product.
In the secondary bleeding stage of liver cirrhosis, the risk of adjusting insulin dose increases in insulin-dependent diabetes or diabetic patients, and the blood sugar level should be closely monitored.
Medication for pregnant and lactating women
Pregnant and lactating women are prohibited.
Children's medication
Child ban
drug interaction
It has been reported that the drug can reduce the absorption of cyclosporine in the intestine and delay the absorption of cimetidine.
overdose
No life-threatening reports of acute overdose were found. Up to now, the largest single dose for adults is 1.0 mg intravenous injection. The observed signs and symptoms are a brief slight decrease in heart rate, facial flushing, abdominal cramps, diarrhea, gastric emptying and nausea. Symptoms disappeared within 24 hours after drug withdrawal. There was once a patient who took an accidental overdose and continued intravenous drip (0.25 mg/ hour instead of 0.025 mg/ hour for 48 hours) without any side effects. Drug overdose should be treated symptomatically.
form of a drug
injection
Packaging/specifications
Instrument package price grid
100 μ g/ml glass ampoule, 5 pieces/box.
Storage; stock
2-8 c, dark storage. It can be stored at room temperature for 2 weeks.