Index of drugs

Palliative treatment of advanced prostate cancer.

1 implant contains 50 mg of histrelin in the form of histrelin acetate.

Histrelin is a synthetic analogue of natural LHRH. After drug implantation, histrelin diffuses into the tissues, which leads to inhibition of LH secretion by the pituitary gland and a decrease in testosterone levels in men. This effect is reversible after discontinuation of treatment. Initially, the drug, like other LHRH agonists, may cause a transient increase in serum testosterone. Within one month after implant placement, the values ​​of testosterone levels decreased to the castration range and their level was reduced during the presence of the drug in the body. This inhibition leads to regression of the prostate tumor and improvement of symptoms in the majority of patients. The implant is implanted subcutaneously and left for 12 months, during this period the drug is released via a hydrogel cartridge at a rate of approximately 50 μg histrelin per day. The hydrogel implant insert determines the rate of diffusion into the aqueous environment. The hydrogel does not dissolve, but has a similar composition to the living tissue, which contributes to its biocompatibility, because it reduces the mechanical irritation of surrounding cells and tissues. It is also characterized by low surface tensionin vivo, which reduces the tendency for proteins to absorb and accumulate on the surface. This is important for the prevention of clots and other biological rejection processes.

Hypersensitivity to histrelin or any of the excipients of the implant, GnRH, GnRH agonists / analogs or stearic acid. There have also been reports of anaphylactic reactions to synthetic LH-RH or agonists / analogs of LH-RH. The use of the drug is contraindicated in women. The use of the drug is contraindicated children due to the lack of data on safety and efficacy of use.

Histrelin causes transient increases in serum testosterone levels during the first week of treatment. Patients may be more symptomatic or have new symptoms, including joint pain, bone pain, neuropathy, hematuria or features of ureteral obstruction or bladder outlet obstruction. Due to the use of LH-RH agonists, cases of ureteral stricture and spinal cord compression have been reported that may cause paralysis leading to death or not. Patients with metastatic lesions within the spine and / or with obstruction of urinary outflow should be closely monitored during the first few weeks of treatment. Prevention of antiandrogens should be considered. In the case of spinal cord compression or renal failure, standard treatment of these complications is necessary. It is recommended to strictly adhere to the recommended procedures for implanting and removing the implant to reduce the risk of complications and protrusion of the implant. In the case of difficulties with the palpation of the implant, ultrasound or computed tomography may be used. Treatment reactions should be monitored by regular measurements of serum testosterone and specific prostate antigen, especially if the expected clinical or biochemical response to treatment is not obtained. The immediate packaging contains latex - it can cause severe allergic reactions. There are no adequate studies in patients with hepatic impairment. No dosage adjustment is necessary for mild-to-moderate renal impairment (CLcr: 15-60 ml / min). The drug has not been studied in patients with prostate cancer with concomitant severe renal failure.

Due to the indication for the use of the drug, no studies have been carried out in pregnant women or during breast-feeding, as it is not intended for use in women.

Very often: hot flashes. Common: depression, decreased libido, insomnia; dizziness, headaches; redness of the face; effort dyspnoea; zapracia; liver disorders; excessive hair; pain in the joints, pain in the limbs; polyuria, impaired renal function, urinary retention; erectile dysfunction, testicular atrophy, gynecomastia; trauma at the implant site, redness at the implant site, weakness, fatigue, reaction at the implant site, pain tenderness; weight gain, increased blood glucose.Uncommon: anemia; fluid retention, hypercalcaemia, hypercholesterolemia, hunger pangs, increased appetite; muscle tremors, drowsiness; palpitations, additional ventricular contractions; hematoma; discomfort in the abdominal cavity, nausea; night sweats, pruritus, excessive sweating; back pain, muscle cramps, infiltration in the muscles, neck pain; renal failure, urolithiasis, diarrheal symptoms, hematuria; sexual dysfunction, breast pain, breast tenderness, pruritus in the genital area (men); peripheral edema, pain (exacerbation), edema, pains (non-specific), deterioration of well-being, feeling cold, irritability; stent obstruction, subcutaneous extravasation; increased activity of aspartate aminotransferase, increased activity of lactate dehydrogenase in the blood, increased testosterone concentration in the blood, decreased creatinine clearance, increased acid phosphatase activity in the prostate gland, weight loss. Rare: skin infections; inflammation. In the medical literature, cases of bone density decrease were reported in men after orchidectomy or treated with an agonist or LH-RH analogue. Long periods of pharmacological castration in men may have an adverse effect on bone density.

The recommended dose is 1 implant for 12 months. An average of 50 μg of histrelin acetate is delivered per day to the body. The implant is implanted subcutaneously on the inside of the arm. The implant should be removed after 12 months of treatment. At the time of its removal, it can be replaced with a new one to continue therapy. Please read the below-described procedure for implanting and removing the product.