Orgalutran is an antagonist of GnRH (gonadotropin releasing hormone). GnRH binds to receptors on the pituitary cell membranes. Orgalutran has a competitive effect on the binding of endogenous GnRH to these receptors. Thanks to this mechanism of action, Orgalutran controls the secretion of gonadotropins (luteinizing hormone (LH) and follicle stimulating hormone (FSH) hormones). Orgalutran causes a dose-dependent inhibition of secretion of LH and FSH by the pituitary gland.
In the absence of pre-stimulation, early secretory suppression of pituitary function comes almost immediately after drug administration and is maintained by the continuation of such treatment. With repeated drug administration of 0.25 mg Orgalutran female volunteers, the concentration of luteinizing hormone (LH), follicle stimulating hormone (FSH) and estradiol in the serum was reduced by about 74%, 32% and 25% for 4, 8 and 16 hours after injection, respectively. The level of hormones in the blood serum returned to baseline values within two days after the last injection.
The average duration of application Orgalutran 0.25 mg / day procedure superovulation is 5 days. In applying the drug Orgalutran 0.25 mg / day, increasing the frequency of premature LH levels (more than 10 IU / l) with a concomitant increase in progesterone concentrations (above 1 ng / ml) was 1.2%, which is comparable with similar parameter for agonist GnRH. Sometimes, before the beginning of therapy Orgalutranom to 6 day gonadotropin stimulation drugs ovaries in women with advanced ovarian response was an increase in LH levels but did not significantly affect the clinical outcome in the future this fact. LH secretion in these patients rapidly suppressed after the first Orgalutran administration of the drug.
Orgalutran absolute bioavailability after subcutaneous administration was 91%.
In the first hours after a single subcutaneous injection of 0.25 mg Orgalutran ganirelix recorded maximum plasma concentration (C max of about 15 ng / ml). The half-life is about 13 hours. The drug is excreted in the feces (about 75%) and urine (about 22%). Pharmacokinetic parameters after multiple subcutaneous administration of Orgalutran treatment (once a day, every day) are similar to those of a single administration.
The active ingredient is :
acetic acid glacial,
acetic acid and / or sodium hydroxide,
water for injections
Prevention of premature ovulation in patients during treatment aimed at achieving a controlled ovarian stimulation, in treatment of infertility using assisted reproductive activities.
- Increased sensitivity to the drug;
- Increased sensitivity to GnRH or any other GnRH analogue;
- Renal or hepatic impairment;
- The period of lactation.
Local reactions: redness, itching, swelling at the injection site.
Systemic reactions: headache, nausea.
Less often – dizziness, weakness.
How to accept, acceptance rate and dosage
Orgalutran drug can be administered by a specialist gynecologist.
Controlled drug ovulation FSH stimulation may be started at day 2 or 3 of the menstrual cycle. Orgalutran (0.25 mg) is administered on day 6 of FSH preparation application (in clinical trials Orgalutran was used together with recombinant follicle stimulating hormone-drug Puregon). In case of increased ovarian response to the stimulation to prevent premature LH level increase, treatment should begin with Orgalutranom 5th day of the application of FSH preparations. In the case of the slow growth of follicles introduction Orgalutran can start later than the 6th day of the application of FSH preparations.
Orgalutran should be administered subcutaneously. The injection site should be changed. The patient can be administered the drug alone, provided that it is instructed accordingly and may consult a specialist.
Orgalutran and FSH be administered at about the same time. Drugs should not be mixed in the same syringe, and to introduce them to use different parts of the body.
Instructions for administering the drug
Orgalutran intended for subcutaneous administration (preferably in the thigh).
Do not use solution if it is opaque or contains impurities.
Processing introduction portion
Wash your hands with soap and water. Treat the injection site (skin diameter of approximately 5 cm around the point where the needle has to enter) with a tampon impregnated with alcohol and let dry for at least 1 minute.
Remove the cap from the needle. Forefinger and thumb, take the skin in the crease. Insert the needle into the base of the fold of skin at 45% of its surface. After each injection change the place of the drug.
Checking the correct needle position
Gently pull the piston itself, in order to check whether the needle is inserted correctly. In the case of the presence of blood in the syringe, the drug does not enter and remove the syringe and attach to the injection site swab soaked in alcohol for 1-2 min.
Start the administration of the drug with a new syringe.
Introduction of the solution
If the needle is correctly positioned, press down on the plunger slowly so that the solution was introduced subcutaneously.
Removing the syringe
Remove syringe and attach immediately swab impregnated with alcohol, pressing it against the injection site. Use the syringe only once.
Store at a temperature of 2-30 ° C, protected from light and the reach of children. Do not freeze.