Clomiphene Review | Buy Clomid LiquidAdmin
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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 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.
Structure of Clomiphene Citrate
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.
Mechanism of Action
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.
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.
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
- 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.
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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.
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