Clomiphene Review | Buy Clomid Liquid
Also known as Clomiphene, it is a non-steroidal, ovulatory stimulant. It is the most commonly used compound for this purpose due to its relative affordability and high effectiveness. First synthesized in 1956, it became commercially available in 1961.
Clomiphene Citrate is widely used in infertility treatment to help individuals facing challenges in conceiving.
Clomiphene binds to oestrogen receptors but unlike what happens to estradiol, an endogenous estrogen, its binding is for a longer duration. This result in a net reduction is oestrogenic effect.
Clomiphene is a tri-phenylene derivative substituted with a chloride anion and an aminoalkoxy side chain. The dihydrogen citrate moiety denotes that the clinically used compound represents the dihydrogen citrate salt form.
What is Clomiphene Citrate?
Clomiphene citrate is a pharmacotherapeutic agent widely used to treat anovulatory or oligo-ovulatory infertility in women. As a selective estrogen receptor modulator (SERM), clomiphene citrate works by binding to estrogen receptors in various parts of the reproductive system, including the hypothalamus, ovary, endometrium, and cervix. This binding action produces both estrogenic and anti-estrogenic effects, which are crucial for its function in inducing ovulation. Clomiphene citrate is particularly beneficial for women with polycystic ovarian syndrome (PCOS), a condition that often leads to irregular ovulation. By stimulating the release of hormones necessary for ovulation, clomiphene citrate helps individuals aspiring to conceive by promoting the growth and release of mature eggs.
Structure of Clomiphene Citrate in Polycystic Ovary Syndrome
It possesses two isomeric forms – cis and trans, which current nomenclature refers to as zuclomiphene and euclomiphene respectively.
It is white to pale yellow, essentially odourless, crystalline powder. It is freely soluble in methanol, soluble in ethanol, slightly soluble in acetone, water and chloroform and insoluble in ether.
Understanding the Mechanism of Action of Clomiphene Citrate and Ovarian Hyperstimulation Syndrome
Studies in animal test subjects show that due to its structural similarity to oestrogen, clomiphene citrate can bind to oestrogen receptors through-out the reproductive system. Unlike oestrogen, clomiphene binds to the nuclear receptor for a much longer time spanning weeks instead of hours resulting in the depletion of oestrogen receptor concentrations by preventing its physiologic replacement.
Its actions occur at the level of the hypothalamus and depletion of the oestrogen receptors there impedes the proper interpretation of blood oestrogen concentration. A falsely low level is perceived which causes a negative feedback mechanism to be instituted. This triggers a compensatory system of altered pulsatile Gonadotropin-releasing hormone (GnRH) leading to higher levels of gonadotropin release from the anterior pituitary.
Increase pituitary gonadotropin release drives ovarian follicular activities. Experimental evidence points primary actions at pituitary levels also. Luteinizing and Follicle Stimulating hormones rise and typically fall after a 5-day administration is completed. This increase in gonadotropin levels is crucial for ensuring that ovulation occurs, which is a key indicator of the drug’s effectiveness.
Benefits of Taking Clomiphene Citrate
The benefits of taking clomiphene citrate are numerous, especially for women struggling with infertility. One of the primary advantages is its ability to induce ovulation in women who experience anovulatory or oligo-ovulatory infertility. This is particularly beneficial for those with polycystic ovarian syndrome (PCOS), as clomiphene citrate can significantly increase the chances of pregnancy. Additionally, clomiphene citrate helps regulate menstrual cycles, making them more predictable and regular. It also stimulates the growth and maturation of ovarian follicles, which are essential for ovulation. By increasing the production of follicle-stimulating hormone (FSH) and luteinizing hormone (LH), clomiphene citrate enhances the overall fertility potential in women, including those with unexplained infertility. These benefits make clomiphene citrate a valuable tool in the management and treatment of infertility.
Clomiphene Effects to Induce Ovulation
Treatment of adult rats with clomiphene citrate for 21 days results in transient cessation of estrous cycle.
Can induce amenorrhoea and oligomenorrhoea
Increased uterine growth
Clomiphene citrate use in men increases levels of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). LH encourages the release of testosterone in males
Histological section of ovary of control rat revealed that the developing follicles were well placed and embedded in ovarian stroma together with Graafian follicles, corpus lutea and atretic follicles.
Treating rats with 10mg clomid for one week caused degeneration of few follicles. After treatment with 50 mg, the ovary showed large number of degenerated follicles together with congestion of blood vessels. Ovaries of rats treated with 100 mg clomid revealed many deleterious histological changes.
In humans, ovulation typically occurs between 5 to 10 days after the last Clomid pill is taken, making it crucial to follow the prescribed dosage and timing.
Comparison between the animals treated with different doses indicates a general increase in inhibitory effect from 0·1 to 100 μg and the difference of antiestrogenic effect is notable between 0·1 and 1·0 and between 10 and 100 μg. No antiestrogenic activity was seen at doses 0·1 and 1·0 μg, but there was a considerable decrease in luminal epithelial cell height at doses 10 and 100 μg when compared to estradiol treated mice. The epithelial cell height of vehicle control and estradiol treated mice was 12·32 ± 0·51 and 35·28 ± l·60 respectively.
Although lots of benefits were discovered on animal laboratory studies, some theoretical side effects have also been brought to light and they include:
Visual symptoms: blurring or other visual symptom may occur occasionally during or after therapy which might be prolonged and possibly irreversible. Therapy should be discontinued if any unusual side effects occur.
Abdominal/Pelvic pain or distention: Ovarian hypertrophy could occur during or soon after administration. Weight gain or discomfort are warning signs.
Multiple pregnancy: There is increased risk of ovarian hyperstimulation that can lead to multiple pregnancy including bilateral tubal pregnancy and coexisting tubal and intrauterine pregnancy when conception occurs on clomiphene citrate therapy.
Spontaneous Abortion and congenital anomalies: Research shows increase rates of anomalies and spontaneous abortion among animal subjects administered clomiphene in contrast to the control.
Vasomotor flushes
Nausea and vomiting
Breast discomfort
Headache
Abnormal uterine bleeding: Intermenstrual spotting, menorrhagia
Drug interactions with clomiphene have not been documented. Long-term toxicity studies in animals have not been performed to evaluate the carcinogenic or mutagenic potential of clomiphene use.
Safety Precautions
Before starting clomiphene citrate therapy, it is crucial to discuss several safety precautions with your healthcare provider. One of the rare but serious side effects is ovarian hyperstimulation syndrome (OHSS), which can cause fluid accumulation in the heart, chest, and stomach. Abnormal vaginal bleeding may also occur during or after treatment, and it is essential to monitor any unusual bleeding patterns. Long-term use of clomiphene citrate has been associated with an increased risk of ovarian cancer, so it is vital to use the medication under strict medical supervision. Vision changes, although rare, can occur during or after treatment and should be reported to a doctor immediately. Additionally, there is a risk of liver damage, which, although uncommon, is a serious side effect. Clomiphene citrate is not recommended for use during pregnancy or breastfeeding, as it can have adverse effects on both the mother and the baby. Discussing these risks with your doctor will help ensure the safe and effective use of clomiphene citrate.
Drug Interactions and Contraindications
Clomiphene citrate may interact with several medications, which can affect its efficacy and safety. It is important to inform your healthcare provider if you are taking estrogen-containing medications, progesterone-containing medications, gonadotropin-releasing hormone (GnRH) agonists, or GnRH antagonists. These interactions can alter the effectiveness of clomiphene citrate and may lead to adverse effects.
There are also several contraindications for the use of clomiphene citrate. Individuals with hypersensitivity to clomiphene citrate or any components of the formulation should avoid its use. It is contraindicated during pregnancy and breastfeeding due to potential risks to the mother and baby. Those with a history of hepatic impairment or hepatic disease should not use clomiphene citrate, as it can exacerbate liver conditions. Abnormal uterine bleeding, uncontrolled adrenal dysfunction, non-PCOS-related ovarian cysts, organic intracranial lesions, uncontrolled thyroid disease, pituitary tumors, risk of hypertriglyceridemia, and endometrial cancer are also contraindications for clomiphene citrate use. Ensuring that these conditions are not present before starting treatment will help prevent complications and ensure the safe use of clomiphene citrate.
Looking for Where To Buy Clomiphene Citrate
Clomiphene Citrate can be bought from Loti labs. It is crucial to purchase USA made research liquids to be sure of the soundness of your research, Clomiphene citrate manufactured and sold by Loti labs is tested through high power liquid chromatography (HPLC) and mass spectrometry to ensure premium quality.
References
Kumar & Pakrasi, 1995: Estrogenic and antiestrogenic properties of clomiphene citrate on laboratory mice
Journal of American science 2013
Escobar & Fridhandler: Studies of clomiphene effects on rabbit embryo development and biosynthetic activity