Blesifen
Blesifen Uses, Dosage, Side Effects, Food Interaction and all others data.
A triphenyl ethylene stilbene derivative which is an estrogen agonist or antagonist depending on the target tissue.
Blesifen (previously clomiphene) is an orally administered, non steroidal, ovulatory stimulant that acts as a selective estrogen receptor modulator (SERM). Blesifen can lead to multiple ovulation, and hence increase the risk of conceiving twins. In comparison to purified FSH, the rate of ovarian hyperstimulation syndrome is low. There may be an increased risk of ovarian cancer and weight gain. Blesifen is capable of interacting with estrogen-receptor-containing tissues, including the hypothalamus, pituitary, ovary, endometrium, vagina, and cervix. It may compete with estrogen for estrogen-receptor-binding sites and may delay replenishment of intracellular estrogen receptors. Blesifen initiates a series of endocrine events culminating in a preovulatory gonadotropin surge and subsequent follicular rupture. The first endocrine event, in response to a course of clomifene therapy, is an increase in the release of pituitary gonadotropins. This initiates steroidogenesis and folliculogenesis resulting in growth of the ovarian follicle and an increase in the circulating level of estradiol. Following ovulation, plasma progesterone and estradiol rise and fall as they would in a normal ovulatory cycle.
| Trade Name | Blesifen |
| Generic | Clomifene |
| Clomifene Other Names | Clomifene, Clomifeno, Clomifenum, Clomiphene |
| Weight | 50mg |
| Type | Tablet |
| Formula | C26H28ClNO |
| Weight | Average: 405.96 Monoisotopic: 405.18594223 |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | Sanbe Farma |
| Available Country | Indonesia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Blesifen is a medication used to induce ovulation.
Used mainly in female infertility due to anovulation (e.g. due to polycystic ovary syndrome) to induce ovulation.
Blesifen is also used to associated treatment for these conditions: Ovulatory Dysfunction
How Blesifen works
Blesifen has both estrogenic and anti-estrogenic properties, but its precise mechanism of action has not been determined. Blesifen appears to stumulate the release of gonadotropins, follicle-stimulating hormone (FSH), and leuteinizing hormone (LH), which leads to the development and maturation of ovarian follicle, ovulation, and subsequent development and function of the coprus luteum, thus resulting in pregnancy. Gonadotropin release may result from direct stimulation of the hypothalamic-pituitary axis or from a decreased inhibitory influence of estrogens on the hypothalamic-pituitary axis by competing with the endogenous estrogens of the uterus, pituitary, or hypothalamus. Blesifen has no apparent progestational, androgenic, or antrandrogenic effects and does not appear to interfere with pituitary-adrenal or pituitary-thyroid function.
Toxicity
The acute oral LD50 of clomifene is 1700 mg/kg in mice and 5750 mg/kg in rats. The toxic dose in humans is not known. Toxic effects accompanying acute overdosage of clomifene have not been reported. Signs and symptoms of overdosage as a result of the use of more than the recommended dose during clomifene therapy include nausea, vomiting, vasomotor flushes, visual blurring, spots or flashes, scotomata, ovarian enlargement with pelvic or abdominal pain.
Food Interaction
- Take with or without food. The absorption is unaffected by food.
Elimination Route
Based on early studies with 14 C-labeled clomifene, the drug was shown to be readily absorbed orally in humans.
Half Life
5-7 days
Elimination Route
Based on early studies with 14C-labeled clomiphene citrate, the drug was shown to be readily absorbed orally in humans and excreted principally in the feces. Mean urinary excretion was approximately 8% with fecal excretion of about 42%.
Innovators Monograph
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