Ganirelix Side Effects
Ganirelix is a decapeptide, better known as an antagonist of the natural gonadotropin-releasing hormone (GnRH). The primary function of this hormone is to regulate the release of two gonadotropins crucial for the functioning of the female reproductive system: luteinizing hormone (LH) and follicle-stimulating hormone (FSH).
The mechanism of action consists of blocking GnRH receptors, mostly in the anterior pituitary gland, thus reducing the release of these two gonadotropins. It is used in conditions where secretion (most often LH) reaches high levels and becomes harmful to the body, such as polycystic ovary syndrome, endometriosis, or various benign tumors such as leiomyomas. However, the most significant application of this peptide is in a medical procedure called controlled ovarian hyperstimulation, which increases the chance of pregnancy and reduces the chance of miscarriage.
About the Peptide
The main function of this peptide, on which all its effects on the body are based, is the blockade of the GnRH receptor by competitive binding. This results in a reduced secretion of LH and FSH, which can be used as a potential treatment for many conditions and diseases. Although this effect is achieved on both gonadotropins, the more significant is suppressing the secretion of luteinizing hormone. LH controls the process of ovulation (the release of an egg into the fallopian tube, preparing it for fertilization).
At the same time, FSH is crucial for the development of follicles in the ovaries (the sac-like formations that contain eggs). Both gonadotropins are crucial for achieving pregnancy, but in the case of excessive or uncontrolled secretion, primarily LH, premature ovulation most often occurs, which significantly reduces the chances of pregnancy due to hormonal imbalance. Also, high levels of this hormone appear in certain diseases and conditions such as endometriosis, polycystic ovary syndrome, or even benign uterine tumors such as leiomyomas and cause the appearance of various symptoms such as painful cycles, spontaneous abortions, insulin resistance, and low pregnancy rates.
By blocking further excessive secretion of LH, Ganirelix could potentially have positive effects on the aforementioned conditions, reduce the intensity of the symptoms, and, most importantly, it could restore hormone homeostasis and thus regulate the occurrence of ovulation at the expected time, which can result in a significant increase in the chance of pregnancy and a reduction in the rate of spontaneous miscarriages.
How Does This Peptide Work?
The mechanism of action of Ganirelix is reflected in the modulation of the hypothalamic-pituitary-gonadal mechanism and blocking of GnRH receptors by competitive binding, which then leads to a truly profound but still reversible suppression of gonadotropin release. Given that a very small, almost insignificant amount of histamine (a substance that is the main mediator of inflammation) is released during application, allergic reactions are almost impossible or extremely rare.
While many GnRH antagonists and agonists lead to an initial surge in LH and FSH, followed by suppression, Ganirelix is one of the few that does not cause an initial increase in levels. Due to this mechanism of action and results, this peptide in conditions of polycystic ovary syndrome could significantly reduce symptoms such as intensely painful and irregular menstruation, unexplained acne, and even insulin resistance.
In endometriosis, a condition in which uterine tissue appears in places where it does not naturally belong, Ganirelix could reduce the intensity of pelvis pain, and what is crucial in both diseases is the positive effect that the peptide has on conception. The pregnancy rate has increased significantly in researchers where Ganirelix has been studied, while the rate of spontaneous abortions has decreased significantly.
Controlled ovarian hyperstimulation is also a medical procedure where a GnRH antagonist could be used as part of drug therapy to increase the chance of pregnancy and regulate ovulation. Another potentially beneficial effect is the possibility of reducing the size of uterine tumors (such as leiomyoma).
Structure
The picture shows the structure of Ganirelix acetate. This peptide is derived from GnRH (a natural hormone) with substitution of amino acids at positions 1, 2, 3, 6, 8 and 10, and thus the molecular formula of the peptide was synthesized: N-acetyl-3-(2-naphthyl)-D-alanyl-4-chloro-Dphenylalanyl-3-(3-pyridyl)-D-alanyl-L-seryl-L tyrosyl-N9, N10-diethyl-D-homoarginyl-L-leucylN9, N10-diethyl-L-dethyl-l-dethyl acetate.
Side Effects
Gastrointestinal Symptoms
Some of the most common side effects after using Ganirelix are gastrointestinal symptoms such as bloating, profuse diarrhea, profuse non-menstrual vaginal bleeding, rapid weight gain, nausea, abdominal pain, or aggressive vomiting. These side effects are considered poor drug tolerance and occur about an hour after taking the peptide. Some other similar symptoms include upset stomach, dry mouth, and drowsiness, but these effects are not considered serious or dangerous for the patient.
Congenital Anomalies
Certain studies have followed pregnant women who received Ganirelix as part of hormone therapy and have examined the newborns. There have been a small number of cases in which children were born with serious congenital anomalies and a slightly larger number of cases with minor anomalies of the same type. Some of the most common were hydrocephalus, meningocele, omphalocele, and Beckwith-Wiedemann syndrome. Some of the minor anomalies that are not life-threatening have been nevus, skin tags, sacral sinus, hemangioma, torticollis, asymmetric skull, talipes, supernumerary toes, hip subluxation, high palate, abnormal arm crease, umbilical hernia, and hydronephrosis. While these may represent serious side effects, the association between the drug and the anomalies above has not been established, and the cause of their occurrence is still unknown.
Rapid Weight Gain
Ganirelix represents a hormonal treatment, and as mentioned, it works by suppressing further secretion of FSH and LH, which represents a change for the body. Hormones act on the body as a whole, so any level change can cause different hormonal symptoms. Since the most common reason for using Ganirelix is to increase the chances of pregnancy and conception, in combination with other methods such as in vitro fertilization, we can expect the peptide to interact with other hormones such as estradiol and progesterone. Therefore, fertility treatment can sometimes alter metabolic or hormonal pathways that cause weight gain.
Even in a normal menstrual cycle, when there is a change in hormone levels, there is an increase in appetite, and ovarian stimulation with medications like Ganirelix causes much larger surges in progesterone and estrogen levels than in a normal menstrual cycle. So it is expected to feel more hungry than usual.
Psychological Symptoms
If Ganirelix is used in cases of controlled ovarian hyperstimulation alone or in combination with a medical treatment known as in vitro fertilization, this process can bring with it other hormonal changes, both physical and psychological. Many patients have experienced symptoms such as mood swings, increased levels of anxiety, or even depression. Pregnant women in this process have also experienced panic attacks.
Other Side Effects
In addition to the above-mentioned side effects, others are usually not serious. Some of them are irritation, redness or pain at the injection site, headache, tiredness, or stomach pain similar to menstrual cramps. Swelling, decreased urination, rapid heartbeat, shortness of breath, and pain when breathing may also occur. An allergic reaction can be the case, but this is rare, given that very small amounts of histamine are released during the injection of Ganirelix.
Is It Safe to Use?
Based on research, this GnRH antagonist is safe to use with supervision and control by a doctor. Serious side effects are very rare and occur when the peptide is not dosed correctly or is not used according to indications. In the main, there are cases of mild side effects, but they are short and hormonal. The peptide is completely safe to use if dosed correctly and used for the above-mentioned indications.