Genfastat

Fasting is an analogue of the substance somatostatin. Used in intensive therapeutic procedures in gastroenterology.

Indications Genf

It is used in the following cases:

• acromegaly (if radiotherapy, surgical procedures and the use of dopamine agonists did not have the desired effect);
• neoplasms in which there is marked increased production of somatoliberin (GH-RF);
• elimination of manifestations arising from secreting neoplasms in the gastroenteropancreatic system (this includes carcinoid neoplasms accompanied by carcinoid syndrome and, in addition, insulomas with glucagonomas and gastrinomas);
• prevention of the development of postoperative complications in the pancreas;
• refractory diarrhea in other types of treatment in people with AIDS.

It is also used to stop bleeding and prevent its recurrence with varicose veins in the veins area of the esophagus in persons with hepatic cirrhosis (combined with endoscopic sclerotherapy).

[1]

Release form

The release of a therapeutic agent is in the form of a liquid for subcutaneous or intravenous injections, in glass bottles with a volume of 1 ml. Inside the box - 5 of these flakonchikov.

Pharmacodynamics

Genofastat is an artificial analogue of the element somatostatin, which has a long duration of therapeutic effect. The drug suppresses the release of growth hormone through the anterior pituitary lobe, and in addition, the secretion of TSH.

At the same time, it suppresses endocrine (glucagon with insulin) and exocrine pancreatic secretion, the process of excretion of hydrochloric acid with gastrin, secretin with cholecystokinin, vasointestinal peptide with certain other peptides, digestive enzymes and bioactive components, whose secretion is made through the gastrointestinal tract, through the gastrointestinal tract; The drug also inhibits the motor function of the gastrointestinal tract.

[2], [3], [4], [5]

Pharmacokinetics

After subcutaneous injection, the drug is rapidly absorbed into the circulatory system at high speed. The plasma level Cmax of the active element is noted after half an hour. Intraplasmic protein synthesis is 65%; binds to blood components very weakly. Vd values are 0.27 l / kg.

Values of total clearance - 160 ml / min. The half-life for a subcutaneous injection is 100 minutes. For intravenous injection, excretion is performed in 2 stages, with a half-life of 10 and 90 minutes, respectively.

[6], [7], [8], [9], [10]

Dosing and administration

The drug is used for intravenous and subcutaneous injections.

For endocrine neoplasms, the medicament is used subcutaneously, the initial dose is 50 mcg with a 1-2-fold administration per day. Further, taking into account the result obtained, the impact on the hormones produced by the formation (in carcinoid neoplasms - the effects on the secretion of 5-hydroxyindole acetic acid with urine), as well as tolerability, the portion is allowed to be gradually increased to 100-200 μg with 3-fold use day. To get a quick response, for example, in case of carcinoid formations, the initial dosage of drugs is administered in the form of a diluted bolus injection, while monitoring the level of heart rate.

In the absence of positive changes after 1 week of treatment for a carcinoid-type tumor, it can be stopped.

In the case of acromegaly, the medicament is used in the sc with the method in the initial portion of 50-100 mcg, which is used at 12-hour intervals. Next, the dosages are selected based on the results of the determination of blood indicators of GH, analysis of clinical signs and drug tolerance. Basically it is required to inject 200-300 μg of a substance per day. If the indicator of GH does not decrease to the required level after 3 months of therapy, and the clinical picture of the disease does not improve, treatment is canceled.

To prevent postoperative complications in the pancreatic region, the first portion of the drug (100 µg) is injected subcutaneously, 60 minutes before the laparotomy; then, after the operation is completed, 100 μg are administered 3 times a day for the next 7 days. Only in exceptional circumstances may require the introduction of higher portions. The selection of supporting dosages is done individually. In the absence of a result after a 1-week treatment with the introduction of the maximum allowable portions, the course is stopped.

The manufacture of fluids for intravenous procedures.

Immediately before the procedure, the medicinal substance from the vial for repeated use is dissolved in 0.9% NaCl. Drug should not be dissolved in glucose solution. In this case, the minimum limits for the dissolution of drugs are 1k1, and the maximum - 1k9. To prevent contamination by bacteria, the cork should be punctured a maximum of 10 times. The finished liquid must be applied during the next 8 hours, and the remaining unused substance must be disposed of.

The opened reusable bottle of medication (200 µg / ml) must be kept in the refrigerator (temperature values - within 2-8 ° C). Its shelf life is 15 days.

Before the introduction of the liquid is checked for the presence in it of sediment and particles, as well as a change in color, transparency and flow of the bottle.

It is forbidden to use a substance with a changed or muddy shade, as well as if there is a sediment with particles in it, and if there are traces of smudges on the vial.

[16], [17], [18]

Use Genf during pregnancy

It is possible to prescribe Genetic Fast to lactating or pregnant women only if there are strict vital indications.

Contraindications

It is contraindicated to use the drug for intolerance against octreotide.

[11], [12]

Side effects Genf

Drug administration leads to the following side effects:

• digestive disorders: vomiting, abdominal pain, anorexia, diarrhea, steatorrhea, nausea, and flatulence. There may be a disorder of tolerance towards glucose. Occasionally, pain occurs during palpation, a sharp pain in the epigastric zone, muscle tension in the peritoneum, hyperbilirubinemia and acute hepatitis, as well as increased activity of hepatic enzymes. Prolonged use sometimes leads to the formation of calculus inside the gallbladder;
• local signs: itching, burning sensation, pain, redness and swelling in the area of the injection.

[13], [14], [15]

Overdose

Portions of the medication up to 2000 mcg per day, used in the form of subcutaneous injections over several months, are often tolerated without complications.

With a maximum 1-fold bolus v / in an injection to an adult of 1000 µg of the drug, such manifestations as flushing to the skin on the face, a decrease in heart rate, and besides spastic pain in the abdominal area, nausea, diarrhea, and a feeling of emptiness inside the stomach. Similar signs disappear within 24 hours from the moment of using the drug.

In case of accidental use through prolonged infusion of too large portions of octreotide (250 µg / hour, not 25 µg / hour), no negative symptoms were observed. Acute intoxication also does not lead to the appearance of signs that are life-threatening. Symptomatic measures are taken to eliminate violations.

[19], [20], [21], [22], [23]

Interactions with other drugs

Substances similar to somatostatin are capable of lowering the clearance of components whose metabolism is carried out using the isoenzymes of the hemoprotein P450 system (this may be due to inhibition of growth hormone).

Combined use with bromocriptine causes an increase in its bioavailability.

The combination with insulin can potentiate the antidiabetic effect of drugs.

Introduction together with cyclosporin reduces the absorption of this element.

The use of Genfast and Cimetidine inhibits the absorption of the latter.

[24], [25], [26], [27], [28], [29]

Storage conditions

It must be kept in a dark and closed place for children. Do not freeze the drug. Temperature indicators - within the limits of 2-8 ° С.

[30]

Shelf life

Least can be used within a 36-month period from the date of manufacture of the drug substance.

[31]

Application for children

There is only limited information regarding the use of drugs in pediatrics, which is why it is not prescribed to children.

Analogs

Analogues of the drug are medicines Oktra with Octrestatin and Sandostatin.

[32]