Diphereline lyophilisate for suspension intramuscularly intravenously prolone. release bottle + comp. sol. 11.25mg N1
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Active ingredients
Triptorelin
Release form
Lyophilisate
Composition
1 bottle contains: triptorelin pamoat, in terms of triptorelin 11.25 mg (taking into account the characteristics of the dosage form, the preparation contains an excess of active substance to ensure the administration of an effective dose). Auxiliary substances: copolymer D, L-lactic and glycolic acids - 250 mg, mannitol - 85 mg, carmellose sodium (sodium carboxymethylcellulose) - 30 mg, polysorbate 80 - 2 mg. Solvent: mannitol 16 mg, water d / i (up to 2000 mg).
Pharmacological effect
Synthetic Decapeptide, an analogue of natural GnRH. After a short initial period of stimulation of the pituitary gonadotropic function, triptorelin has an inhibitory effect on the secretion of gonadotropins with subsequent suppression of the function of the testes and ovaries. In the initial period of use, Diphereline temporarily increases the concentration of LH and FSH in the blood, respectively, the concentration of testosterone increases in the blood, respectively and estradiol in women. Long-term treatment lowers the concentration of LH and FSH, which leads to a decrease in testosterone levels (to levels corresponding to the state after a testicular test) and to a decrease in estradiol values (to levels corresponding to the state of postovariectomy) approximately 20 days after the first injection and then remains constant throughout the period of administration of the drug. Prolonged treatment with triptorelin suppresses the secretion of estradiol in women and, thus, prevents the development of endometrioid ectopy.
Pharmacokinetics
Absorption and distribution When ip administration of Diphereline at a dose of 11.25 mg Cmax of triptorelin in the blood plasma (in men and women) is determined approximately 3 hours after injection. After the concentration reduction phase that lasts for the first month, up to 90 days, the concentration of circulating triptorelin remains constant (approximately from 0.04 to 0.05 ng / ml in the treatment of endometriosis and about 0.1 ng / ml in the treatment of prostate cancer).
Indications
Prostate cancer: - treatment of locally advanced prostate cancer in monotherapy or as an adjuvant with radiotherapy; - treatment of metastatic prostate cancer. Genital and extragenital endometriosis (stages I-IV).
Contraindications
- hypersensitivity to triptorelin, other components of the drug or other analogues of GnR.U men: - hormone-independent prostate cancer, the state after the previous surgical test of anesthesia. , women with polycystic ovary syndrome.
Use during pregnancy and lactation
Diphereline is contraindicated for use in pregnancy and lactation (breastfeeding). Since there are no data on the elimination of triptorelin in breast milk and its possible effects on the breastfed child, do not treat Dipherelin during breastfeeding. According to available data, found any teratogenic effects in experimental animal studies. In isolated cases of the use of GnRH analogues (through negligence), no defects in fetal development and fetotoxicity were found.
Dosage and administration
In prostate cancer, Diphereline is injected intramuscularly at a dose of 11.25 mg every 3 months. For treatment in combination with radiation therapy, long-term anti-androgen therapy (3 years) is preferable to short-term anti-androgen therapy (6 months). In endometriosis, the drug is administered intramuscularly at a dose of 11.25 mg every 3 months. Treatment must begin in the first 5 days of the menstrual cycle. The duration of treatment depends on the severity of endometriosis and the observed clinical picture (functional and anatomical changes) during therapy. As a rule, treatment is carried out for 3-6 months. It is not recommended to repeat the course of treatment with triptorelin or another GnRH analogue. Suspension preparation rules The dissolution of the lyophilisate in the attached solvent should be carried out immediately before the administration. The contents of the vial should be mixed with caution until a homogeneous suspension is obtained. In the event of incomplete injection, resulting in a loss of more suspension than is usually left in the syringe for injection, it is necessary to inform the attending physician. prone position. Disinfect the skin of the buttock.Break the neck of the ampoule (point on the front side above) .2. Draw the solvent in a syringe with a needle. Remove the green protective plastic cap from the top of the bottle. Transfer the solvent to the lyophilized vial. Pull the needle so that it remains in the bottle, but does not touch the suspension. Without turning the bottle, gently shake the contents until a homogeneous suspension is obtained.7. Check the absence of agglomerates before you put the suspension into the syringe (if there are no agglomerates, shake to complete homogeneity) .8. Without turning the vial over, draw the entire suspension into a syringe. Remove the needle used to prepare the suspension, and attach another needle tightly to the tip of the syringe. Hold only the colored tip. Remove air from syringe. Immediately give an injection to the gluteus 12. Dispose of needles in sharps containers.
Side effects
In men: At the beginning of treatment: dysuria (difficulty urinating, incomplete emptying of the bladder, pain), bone pain associated with metastases and compression of spinal cord metastases, which can be exacerbated by a temporary increase in plasma testosterone levels at the beginning of treatment. These symptoms disappear in 1-2 weeks. Also during this period, there may be a temporary increase in liver enzyme activity in the blood plasma. During treatment: hot flashes, decreased libido, gynecomastia, impotence, which is associated with a decrease in testosterone plasma levels. In women. At the beginning of treatment: symptoms associated with endometriosis (pelvic pain, dysmenorrhea), which may increase due to the initial transient increase in plasma estradiol concentration and disappear in 1-2 weeks. 1 month after the first injection, genital bleeding may occur, including both menorrhagia and metrorrhagia. During treatment: vaginal dryness, flushing, decreased libido, breast enlargement, dyspareunia, which is associated with a pituitary-ovarian blockade; rarely - headache, arthralgia, myalgia. In men and women, allergic reactions such as urticaria, rash, itching and very rarely - angioedema; mood disturbance, irritability, depression, fatigue, sleep disturbances, nausea, vomiting,weight gain, profuse sweat, arterial hypertension, paresthesia, blurred vision, pain at the injection site and feverish condition. Long-term use of GnRH analogues can lead to bone demineralization and is a possible risk factor for osteoporosis. According to data collected during the use of GnRH analogues, Patients may experience the following adverse reactions: erectile dysfunction, tinnitus, dizziness, diabetes mellitus (hyperglycemia), abdominal pain, constipation, diarrhea, abdominal distension, dry mucous membranes oral cavity, dysgeusia, flatulence, asthenia; drowsiness, flu-like syndrome, anaphylactic reactions; increased activity of ALT, AST, alkaline phosphatase; hypercreatininemia, increased blood urea, anorexia, gout, increased appetite, musculoskeletal pain, pain in the extremities, muscle cramps, muscle weakness, dizziness, memory loss, insomnia, confusion, anxiety, atrophy of the testes, shortness of breath, orthopnea, nasal bleeding , acne, alopecia, lowering blood pressure; at the injection site - erythema, inflammation, pain.
Overdose
To date, cases of overdose of drug Diphereline unknown.
Interaction with other drugs
Drug interaction drug Diphereline not described.
special instructions
When treating endometriosis. Before starting treatment, pregnancy should be excluded. Non-hormonal contraceptives should be used during the first month of therapy. V / m injection of the drug leads to persistent hypogonadotropic amenorrhea. Treatment should not be recommended for a period of more than 6 months. It is not recommended to repeat the course of therapy with triptorelin or another GnRH analogue. The occurrence of metrorrhagia during treatment, not counting the first month, is not the norm, and therefore it is necessary to determine the concentration of estradiol in the blood plasma. If the estradiol concentration is less than 50 pg / ml, other organic lesions may be present. Ovarian function is restored after completion of therapy. The first menstruation occurs on average 134 days after the last injection. Therefore, contraceptive measures should be started 15 days after discontinuation of treatment.that is, 3.5 months after the last injection. When treating prostate cancer, the most pronounced beneficial effect is observed in patients in the absence of other previously conducted hormone therapy. At the beginning of treatment, the appearance and increase of clinical symptoms (in particular, bone pain, dysuric events), of a transient nature. This implies careful observation of these patients during the first few weeks of therapy (plasma testosterone levels should not exceed 1 ng / ml). Therefore, patients with diagnosed compression of the spinal cord should be closely monitored at the beginning of treatment. In addition, a temporary increase in acid phosphatases may be observed at the beginning of treatment. Patients receiving GnRH agonists are at risk of developing hyperglycemia and diabetes. In addition, there may be a risk of developing cardiovascular diseases and, with long-term use, osteoporosis. Impact on the ability to drive motor vehicles and control mechanisms. There is no information.