Orgalutran injection solution syringe 0.25mg + 0.5ml N5
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Active ingredients
Ganirelix
Release form
Solution
Composition
1 syringe contains: Active substance: ganirelix (in the form of acetate) 250 mcg. Adjuvants: mannitol - 23.5 mg, glacial acetic acid 99% - 0.1 mg, glacial acetic acid and / or sodium hydroxide - to pH 5.0, water d / and - qs to 5.0 ml.
Pharmacological effect
Organutran is a competitive antagonist of GnRH receptors (gonadotropin-releasing hormone), controls the secretion of gonadotropins (luteinizing (LH) and follicle-stimulating (FSH) hormones), inhibits the secretion of LH and FSH by the pituitary (the effect depends on the dose). In the absence of prior stimulation, the onset of inhibition of the pituitary secretory function begins immediately after the administration of the drug and is maintained with the continuation of such treatment. Owing to the administration of volunteers with multiple doses of 0.25 mg of the drug Oralutran, the greatest decrease in serum LH, FSH and estradiol concentrations was observed in 74%, 32% and 25% at 4, 8 and 16 hours after the administration, respectively. The serum hormone level returned to baseline values within two days after the last injection. The average duration of use of the drug Oralutran at a dose of 0.25 mg / day for controlled stimulation of ovulation is 5 days. When using the drug Oralutran at a dose of 0.25 mg / day, the average frequency of increasing the level of LH (more than 10 IU / l) with a concomitant increase in the concentration of progesterone (more than 1 ng / ml) is 1.2%, which is comparable with the same indicator 0 , 8% for GnRH agonists. Sometimes, even before Orhalutran was started on therapy, by the 6th day of ovarian stimulation with gonadotropic drugs, women with a pronounced ovarian response had an increase in LH levels, which later did not significantly affect the clinical results. The secretion of LH in these patients was quickly suppressed immediately after the first injection of the drug Orgalutran.
Pharmacokinetics
1-2 hours after a single subcutaneous injection of 0.25 mg of the drug Orgalutran, the maximum concentration of ganirelix in the blood plasma is recorded (Cmax about 15 ng / ml). T1 / 2 is approximately 13 h and clearance is approximately 2.4 l / h. The drug is excreted through the intestines (about 75% as metabolites) and the kidneys (about 22%, ganirelix is the main compound found in the urine).The absolute bioavailability of the drug Oralutran after subcutaneous administration is 91%. The pharmacokinetic parameters after repeated subcutaneous administration of the drug Oralutran (once a day) are similar to those after a single injection. After repeated dosages of 0.25 mg / day, steady-state concentrations of approximately 0.6 ng / ml were achieved within 2-3 days. Pharmacokinetic analysis demonstrates an inverse relationship between body weight and drug concentrations of the drug Orgalutran in serum. Metabolic profile: The main compound circulating in plasma is ganirelix. Megabolized by enzymatic hydrolysis to form peptide fragments.
Indications
- Prevention of premature peak increase of LH secretion in women with induction of ovulation (superovulation) in infertility treatment programs using assisted reproductive technologies (ART).
Contraindications
- Hypersensitivity to the components of the drug; - Hypersensitivity to GnRH or any other GnRH analogue; - Renal or hepatic failure; - Pregnancy; - Lactation.
Use during pregnancy and lactation
The use of the drug Oralutran during pregnancy and lactation is contraindicated.
Dosage and administration
The drug Orgalutran can only be prescribed by a specialist gynecologist. Controlled stimulation of ovulation with FSH can be started on the 2nd or 3rd day of the menstrual cycle. Organutran (0.25 mg) is injected subcutaneously once a day, starting from the 6th day of the use of the FSH drug (in clinical studies Orhalutran was used in conjunction with the recombinant follicle-stimulating hormone drug Puregon). In case of an increased ovarian response to stimulation, to prevent premature elevation of LH levels, treatment with Orgalutran should be started from the 5th day of using FSH preparations. In the case of slow follicle growth, administration of the drug Orgalutran can be postponed (ie, start later than the 6th day of using FSH preparations). The instructions for administering the preparation Orgalutran are intended for subcutaneous administration (preferably in the thigh).Do not use the solution if it is opaque or contains impurities. Treatment of the injection site Wash your hands with soap and water. Treat the injection site (area of skin about 5 cm in diameter around the place where the needle should go) with a tampon soaked in alcohol and let it dry for at least 1 minute. Injecting the needle Remove the cap from the needle. Use your thumb and forefinger to fold the skin. Insert the needle into the base of the skin fold at an angle of 45 ° to its surface. After each injection, change the injection site. Checking the correct needle position Pull the plunger toward you to check that the needle is correctly inserted. If there is blood in the syringe, do not inject the drug, but remove the syringe, and attach a tampon soaked in alcohol for 1-2 minutes to the injection site. Do not use this syringe. Start the injection with a new syringe. Inject the solution. If the needle is positioned correctly, slowly push the plunger so that the solution is injected subcutaneously. Removing the syringe Remove the syringe and immediately apply a tampon soaked in alcohol, pressing it to the injection site. Use the syringe only once.
Side effects
Local reactions: Organalutran can cause a local skin reaction at the injection site (mainly redness, with or without swelling, and itching). In clinical trials, one hour after the injection, the frequency of moderate or severe local skin reactions to the course of treatment was 12% in patients treated with the drug Orgalutran. Local reactions usually disappear 4 hours after injection. Systemic reactions: The feeling of discomfort was noted in 0.3% of patients. On the immune system: Very rare cases of hypersensitivity reactions were observed among patients who received treatment with Orgalutran (<0.01% ) with the introduction of the first dose of the drug, including various symptoms, such as skin rash, swelling of the face and dyspnea. From the nervous system: Headache (0.4%), dizziness. From the gastrointestinal tract: Nausea (0.5% ), pain in the abdomen. Others - weakness .Drugie reported adverse reactions associated with treatment aimed at achieving a controlled ovarian stimulation using assisted reproductive activitiesespecially: pain in the pelvis, bloating, ovarian hyperstimulation syndrome (OHSS) (symptoms: lower abdominal pain, vomiting, diarrhea, ovarian enlargement, dyspnea, oliguria, weight gain), ectopic (ectopic) pregnancy and spontaneous abortion.
Overdose
An overdose of the drug Oralutran can lead to an increase in the duration of its action. In this case, the administration of the drug Orgalutran should be (temporarily) stopped and the patient should consult a doctor.
Interaction with other drugs
The combined use of the drug Orgalutran with other drugs has not been studied sufficiently, therefore the likelihood of drug interaction cannot be ruled out. Consequently, the attending physician should be informed about the drugs that the patient took shortly before the start of treatment with the drug Orguthrani continues to be taken along with his appointment.
special instructions
Ganirelix should be prescribed only by a doctor who has experience in treating infertility using assisted reproduction technologies. Women with signs or symptoms of active allergic conditions should be especially careful. In registered cases of hypersensitivity reactions, prn administration of the first dose of the drug occurred (see section Side effects). In the absence of clinical practice, treatment with Orgalutran is not indicated for women with severe allergic conditions. The packaging material for the drug contains natural rubber latex in its composition, which can cause allergic reactions. Organutran should be administered subcutaneously. The injection site should be changed. The patient can administer the drug independently, provided that she is properly instructed and can consult with a specialist. Orgutran and FSH should be administered at about the same time. The drugs should not be mixed in the same syringe, and for their introduction, you should use different parts of the body. The daily use of the drug Organalutran should continue until a sufficient number of preovulatory follicles are formed. The final maturation of the follicles can be initiated by administering human chorionic gonadotropin (hCG).Given the T1 / 2 ganirelix, the interval between injections of the drug Orgalutran, as well as the time between the last injection of the drug Orgalutran and the injection of hCG, should not exceed 30 hours, otherwise a premature peak of LH may occur. Consequently, with the introduction of the drug Orgalutran in the morning, its use should be continued, including, including the day of hCG administration. When prescribing Orhalutran in the evening, its last injection should be made in the evening of the day preceding the day of hCG administration. The luteal phase should be maintained in accordance with the methods adopted in the infertility clinic. The drug should be used during repeated courses of treatment only after a thorough assessment of the potential risk the effectiveness of treatment. Ovarian hyperstimulation syndrome (OHSS) may occur during or after stimulation of ovulation. The risk of this complication is always blowing into account during stimulation gonadotropinami.Pri moderate and severe OHSS severity of intensive therapy with intravenous techenieneskolkih days in the electrolyte and colloid solutions, geparina.Doklinicheskie data based on studies of general toxicity and genotoxicity, demonstrated the safety of the drug in humans. The drug has not revealed any teratogenic properties. The safety and efficacy of the drug has not been established for women weighing less than 50 kg or more than 90 kg. The incidence of congenital malformations after the use of assisted reproductive technologies (ART) may be slightly higher than in the population . It is believed that this slight increase is due to the characteristics of the parents (for example, the age of the mother, the characteristics of sperm) and the higher frequency of multiple pregnancies after ART. There is no indication that the increased risk of congenital malformations is associated with the use of GnRH antagonists during ART. It was shown that the incidence of congenital malformations in children (more than 1000 newborns) born after therapy of controlled stimulation of ovulation with Oralutran is comparable to the previously noted frequency after therapy of controlled stimulation of ovulation using GnRH agonists. An important ultrasound confirmation that The pregnancy is intrauterine.Since infertile women undergoing assisted reproductive technologies and especially extracorporeal fertilization (IVF) often have a fallopian tube pathology, therefore, the frequency of ectopic pregnancy can be increased. In controlled studies of the drug Orgalutran using the “long protocol” GnRH agonists (the beginning of the protocol from 21-23 days of the menstrual cycle, prior to stimulation) as a comparison, therapy with Orgalutran resulted in faster growth of follicles dyer's weed stimulation days, but the number of growing follicles at the end of the stimulation was somewhat smaller and the average estradiol levels in the blood were lower. This particular picture of follicular growth requires that dose adjustments of FSH be made based on the number and size of growing follicles, rather than on the amount of circulating estradiol. When skipping the time of drug administration: You can’t take a double dose of the drug in order to replenish the missed injection. If the patient remembers that she forgot to inject the drug, then the drug should be administered as soon as possible. If the delay in the administration of the drug Orgalutran is more than 6 hours (ie, the interval between injections of the drug is more than 30 hours), the patient should immediately enter the drug and consult a doctor as soon as possible. The effect on the ability to drive and work with mechanisms is not studied.