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Last reviewed: 23.04.2024
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Firmagon is a substance from the category of hormonal antagonists and a drug used in oncology.
When using the drug in compliance with all instructions, there is a rapid decrease in luteotropin and follitropin, which as a result reduces the level of testosterone. The intraplasma values of dihydrotestosterone also decrease.
This medication demonstrates effectiveness in suppressing the release of testosterone below the indicators of medical castration (0.5 mg / ml), as well as maintaining these values. A standard monthly portion (administered 1-fold) causes sustained suppression of testosterone secretion for at least 12 months in 97% of treated men.
Indications Firmagona
It is used in men in the case of hormone - dependent prostate carcinoma, which is widespread.
Release form
The release of the medication is implemented in the form of a lyophilisate for injection, inside the vials with a capacity of 0.08 or 0.12 g. In addition, inside the box contains a solvent-filled syringe (injection fluid) having a volume of 3 or 4.2 ml, needles, adapters for the vials and piston rods.
Pharmacodynamics
A carcinoma that affects the prostate is sensitive to androgens, therefore, it is responsive to therapy that eliminates the source of these hormones.
The drug acts as a selective antagonist of gonadorelin. It is reversibly and competitively synthesized with the endings of pituitary gonadorelin, quickly reducing the volume of released luteotrophins, gonadropins and follitropins, which induces testosterone secretion by the testicles.
Gonadorelin blockers differ from its antagonists in that they do not lead to the development of a release of luteotropin with a subsequent release of the hormone testosterone and the stimulation of an increase in neoplasm. All this can potentially cause aggravation of signs of the disease after the start of the treatment course.
Pharmacokinetics
Suction.
When s / c injection of 0.24 g of degarelix with indicators of 40 mg / ml in patients with prostate carcinoma, the AUC level of 0-28 days equals 635 (in the range of 602-668) ng / ml; Cmax values are equal to 66 (in the range of 61–71) ng / ml and are recorded after 40 minutes (within 37–42 hours). The average indices are 11-12 ng / ml with the introduction of the 1st portion, as well as 11-16 ng / ml when using maintenance dosages (80 mg) with values of 20 mg / ml.
The plasma level of C max of degarelix decreases in 2 stages with an average half-life term of approximately 29 days in the maintenance portion. The long term half-life in s / c injections is associated with an extremely low rate of release of degarelix from the depots, which are formed in the areas of injections.
The pharmacokinetics of the drug is determined by its concentration inside the injection fluid. Since the values of bioavailability and Сmax decrease with increasing concentration, it is prohibited to use any other, not prescribed drug concentrations.
Distribution processes
The level of distribution in elderly volunteers was about 1 st l / kg. Intlasma protein synthesis is approximately 90%.
Exchange processes.
Degarelix is the subject of a standard peptide degradation during its passage through the hepatobiliary system; the main part of the substance is secreted together with the faeces in the form of peptide fragments.
When s / c injections with medicinal activity of metabolic elements inside the blood plasma are not observed. In vitro testing revealed that degarelix does not act as a substrate for the hemoprotein CYP450 structure in humans.
Excretion.
In men who do not have problems with the work of the kidneys, about 20-30% of degarelix is excreted through this system (the 1st intravenous injection). It is assumed that the remaining 70-80% are excreted by the hepatobiliary system.
The level of drug clearance after the application of a single dose (0.864-49.4 mg / kg) of the solution in elderly patients is 35-50 ml / hour / kg.
Dosing and administration
The drug begins to apply, introducing the patient the initial dosage. Further, it is used 1-fold per month. First, the drug is administered in portions of 0.24 g - after 2 p / c injection, each at 0.12 g.
With a supporting course, the size of the monthly portion is 0.08 g. It is necessary to perform the 1st support injection after the 1st month since the initial injection.
Injections should be carried out exclusively s / c method, in the abdominal area. The areas of injections should be periodically changed. It is necessary to select a site for carrying out the procedure, taking into account that it should not be compressed with clothing (it is impossible to prick the medicine at the site of wearing the belt, at the waist in the waist), and also it is not located near the ribs.
The result provided by the Firmmagon is checked by tracking the blood indicators of the hormones.
Because this medicine does not induce an increase in testosterone values, it is not necessary to prescribe anti-androgenic substances to protect against testosterone release at the beginning of treatment.
It is forbidden to use the solution in / in the method.
In severe stages of liver / kidney failure, the drug is used very carefully.
Use Firmagona during pregnancy
Firmagon is not intended for therapy in women.
Side effects Firmagona
The main adverse symptoms of a therapeutic agent are:
- febrile neutropenia or anemia;
- signs of allergies and intolerance in the form of anaphylaxis;
- hyperglycemia, reduction or increase in weight, increase in cholesterol, loss of appetite, diabetes and changes in blood values of Ca;
- headaches, decreased libido, insomnia, dizziness, and depression;
- dyspnea;
- deterioration of visual acuity;
- tachycardia or arrhythmia;
- an increase in blood pressure and tides;
- diarrhea, dry mouth, vomiting, obstipation and nausea;
- an increase in intrahepatic transaminase values;
- urticaria, hyperhidrosis, alopecia, night sweats, erythema and itching;
- myalgia, swelling or discomfort affecting the joints;
- nocturia, polakiuria, urinary incontinence or the urge to it, as well as renal failure;
- testicular atrophy, impotence and gynecomastia;
- manifestations in the area of the injection, severe fatigue, flu-like state, fever or chills.
With the development of uncharacteristic side effects when using the drug, it is necessary to consult with your doctor about possible changes in the treatment regimen.
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Overdose
Cases of poisoning with Firmagon have not yet been registered.
In case of intoxication, it is necessary to monitor the condition of the victim, conducting symptomatic or supportive measures when necessary.
Shelf life
A trademark is allowed to apply for a 36-month period from the time the therapeutic product is manufactured.
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Attention!
To simplify the perception of information, this instruction for use of the drug "The firm" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.