Clomifene (INN) or clomiphene (USAN and former BAN) is a selective estrogen receptor modulator (SERM), used mainly in female infertility due to anovulation (e.g. due to polycystic ovary syndrome). In some countries, it is also registered for use in men. Clomifene citrate is marketed under various trade names including Clomid®, Serophene®, Milophene®, etc.
Mode of action
Clomifene acts by inhibiting the action of
estrogen on the
gonadotrope cells in the anterior
pituitary gland. "Sensing" low estrogen levels,
follicle-stimulating hormone (FSH) release is increased, leading to a higher rate of
ovulation and hence
pregnancy.
Clomifene can lead to multiple ovulation, and hence increasing the risk of 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.
Chemistry
Clomifene is a
racemic mixture of two
geometric isomers,
enclomifene (
E-clomifene) and
zuclomifene (
Z-clomifene).
Adverse effects
Common
adverse drug reactions associated with the use of clomifene (≥1% of patients) include:
hot flushes, abdominal discomfort, visual blurring, and/or reversible ovarian enlargement and cyst formation. Infrequent adverse effects (0.1–1% of patients) include: abnormal uterine bleeding, nausea, and/or vomiting. Rare adverse effects (<0.1% of patients) include: reversible
alopecia and/or
ovarian hyperstimulation syndrome.
[Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006. ISBN 0-9757919-2-3]
Use in bodybuilding
Clomifene is commonly used by male
anabolic steroid users to bind the estrogen receptors in their bodies, thereby blocking the effects of estrogen, ie
gynecomastia. It also restores the bodies natural production of
testosterone. It is commonly used as a "recovery drug" and taken toward the end of a
steroid cycle.
References
External links
Citrates | Selective estrogen receptor modulators
Clomifen | Clomifeen | Clomifeno