Clomiphene citrate (known as Clomid) is a selective estrogen receptor modulator (SERM). A SERM binds to estrogen receptors in the body. A SERM can either activate (agonist) or deactivate (antagonist) an estrogen receptor in the body.

Clomid acts as a weak estrogen receptor antagonist, meaning that it binds to the estrogen receptor and blocks the receptor from signaling. Clomiphene binds to estrogen receptors, in particular, at the level of the hypothalamus near the brain. This increases both LH and FSH secretion from the pituitary gland and drives an increase in testosterone secretion and spermatogenesis (sperm production) in the testicles in men.

The U.S. Food & Drug Administration (FDA) has not approved the use of Clomid for any purposes or indications in men. Instead, a physician may prescribe Clomid for off-label use as a safe and effective way for men to increase testosterone levels while maintaining fertility. Consult with a REGENX Health provider to see if you’re a candidate for therapy.

The use of Clomid in men is considered off-label, as Clomid’s FDA approval is intended for use in women to induce ovulation.

In addition to exogenous testosterone replacement therapies, other pharmacological strategies can be utilized to increase a man’s endogenous production of testosterone. SERMs, and more specifically Clomid, are medications used to raise testosterone naturally. Clomid is a safe alternative to raise testosterone levels for men who have Low-T who desire to increase their testosterone level while maintaining their fertility.

To find out if you are candidate for Clomid, schedule a consultation with a REGENX Health provider.

Clomid works by preventing the negative feedback that estrogen has on the hypothalamus. Clomid blocks the receptors on the hypothalamus. Normally these receptors are activated by estradiol in men to stop the production and secretion of FSH and LH from the pituitary. This then down regulates the testicles secretion and production of testosterone and sperm. When Clomid is taken, these estrogen receptors in the pituitary are blocked and estradiol is unable to prevent the pituitary from signalizing FSH and LH to the testicles. This results in a natural increase in both testosterone and spermatogenesis (sperm production).

In men aged 30 or above, testosterone levels decline naturally by 1% per year. Approximately 40% of men above age 45 in the U.S. have low testosterone levels.

Symptoms associated with low testosterone levels include poor performance, daily fatigue, daily naps, lack of libido, erectile dysfunction, decreased mental clarity, poor health, and/or an inability to maintain a healthy weight.

Exogenous testosterone replacement comes in many forms such as subcutaneous pellets, topical creams, topical gels and injectable medication. For men who desire to raise their testosterone levels while maintaining their reproductive function, Clomid is a great alternative. Many comparative studies have shown that Clomid is a viable to raise testosterone levels significant for men to feel the desired effect. A study, by Shabsigh et al., treated 36 men with T deficiency with clomiphene citrate for 4–6 weeks and observed increases of nearly 150% in serum testosterone levels. Other studies have shown improvement in erectile function with clomiphene citrate in men with secondary testosterone deficiency.

Though estrogen is commonly associated with female physiology, it also has a key role in male physiology, including libido, bone and vascular health, erectile function, and spermatogenesis.

The predominate form of male estrogen is called estradiol. Estradiol forms from aromatizing testosterone in primarily two areas: the peripheral tissues and the Leydig cells in the testicles. Adrenal glands play a small role in aromatizing androstenedione into estrone, which is then converted to estradiol.

Estradiol is essential to male bone development. Several studies indicate that low levels of both total estradiol and bioavailable estradiol are associated with an increased rate of bone loss, bone resorption, and an increased rate of osteoporotic fractures.

Estradiol is also important to cardiovascular health, particularly in assisting in the prevention of plaque building and preventing atherogenesis (formation of plaques in arteries).

Estrogen in humans is found in three forms: estrone (E1), estradiol (E2), and estriol (E3). Of these, estradiol (E2) has the most affinity for estrogen receptors and is therefore the most active biologically.

Men produce estradiol as a breakdown product of testosterone, primarily in fat cells and secondarily in the adrenal glands and testicles.

A variety of demographic factors can influence male estradiol levels, including age, race, and BMI (body mass index, a way to quantify fat, muscle, and bone).

• Estradiol levels typically decrease as men age, yet with a more significant decrease in testosterone.

• Estradiol levels often increase in men who are obese or have higher BMI.

• Estradiol levels are often heightened as much as 1016 percent in African American men compared to Asian or Caucasian men, regardless of age, BMI, or geography.

Clomid is an oral tablet. Swallow the medication whole, either daily or every other day, with or without food. Clomid comes in dosages of 25mg and 50mg. Your REGENX Health provider will determine your specific dosage and frequency of use to obtain your desired results.

Off-label use refers to the practice of prescribing a medication for a condition other than the medication is intended or approved to treat. A healthcare provider may prescribe a medication for a different condition or a different dosage other than what’s approved by the U.S. Food & Drug Administration (FDA), if medically appropriate for the patient.

Clomid is not right for everyone. Only your healthcare provider can decide if Clomid is right for you.

Do not take Clomid if you have any of the following conditions:

• Uncontrolled thyroid or adrenal dysfunction

• Liver disease or a history of liver dysfunction

• Hormone dependent tumors

• Organic intracranial lesion

• Hypersensitivity to clomiphene

Do not take Clomid if you have pre-existing mental depression of thrombophlebitis because Clomid may exacerbate these conditions.

Patients should be advised that blurring or other visual symptoms may occasionally occur during or shortly after therapy with clomiphene citrate. The significance of these visual symptoms is not understood. If the patient has any visual symptoms, treatment should be discontinued and complete ophthalmologic evaluation performed.

Only those who have specifically been prescribed Clomid should take it. Never share Clomid with others, even if their symptoms are similar, as it may cause serious harm.

Clomid can cause common side effects including:

• Cardiovascular conditions such as syncope

• Dermatologic conditions such as acne, dermatitis, dry hair, erythema (including multiforme and nodosum), vasomotor flushes, hypertrichosis, loss of hair, pruritus, rash, and urticaria

• Endocrine metabolic conditions such as disorder of thyroid gland and weight loss or gain

• Gastrointestinal conditions such as abdominalpelvic discomfort (distention, bloating), acute abdominal pain, constipation, diarrhea, gastrointestinal tract finding, increased appetite, nausea and vomiting

• Hepatic conditions such as increased liver enzymes

• Musculoskeletal conditions such as arthralgia, backache, myalgia

• Neurologic conditions such as asthenia, dizziness, headache, insomnia, lightheadedness, migraine, paresthesia, unsteadiness when walking, and vertigo

• Ophthalmic conditions such as eye/vision finding, temporary functional visual loss, pain in eye, and photopsia tinnitus

• Psychiatric conditions such as anxiety, depression, fatigue, irritability, and mood disorder

• Renal conditions such as polyuria

• Reproductive conditions such as ovary cyst, endometriosis, hyperstimulation of ovaries, pain of breast, urogenital finding, and vaginal dryness

• Other conditions such as fever

This is not a complete list of side effects. Other side effects may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Serious side effects of Clomid may include, but are not limited to, the following:

• Cardiovascular conditions such as cardiac dysrhythmia, chest pain, edema, hypertension, palpitations, phlebitis, pulmonary embolism, and tachycardia

• Endocrine metabolic conditions such as gynecomastia

• Gastrointestinal conditions such as pancreatitis

• Hematologic conditions such as leukocytosis and thrombophlebitis

• Hepatic conditions such as hepatitis and liver carcinoma

• Neurologic conditions such as cerebrovascular accident, neoplasm of nervous system, and seizure

• Ophthalmic conditions such as cataract, macular retinal edema, optic neuritis, posterior vitreous detachment, retinal hemorrhage, retinal vascular disorder, thrombosis of retinal artery, and thrombosis of retinal vein

• Psychiatric conditions such as a psychotic disorder

• Reproductive conditions such as disorder of menstruation, ectopic pregnancy, and endometrial carcinoma

• Gestational conditions such as trophoblastic neoplasm, hemorrhagic cyst of ovary, hypertrophy of ovary, neoplasm of ovary, ovarian cancer, testicular cancer, tubal pregnancy, and uterine hemorrhage

• Other conditions such as carcinoma of breast, fetal neoplasm, gestational trophoblastic neoplasm, malignant neoplasm of liver, neoplasm of breast, neoplasm of endometrium, neoplasm of nervous system, and neoplasm of ovary

Clomid may cause visual symptoms that make it difficult or dangerous to drive a car or operate machinery, particularly when lighting is varied.

Adverse effects of Clomid are typically related to the dose taken. Most exposures are mild and require only supportive care. In severe toxicity, support respiratory and cardiovascular function as needed. Contact your physician if you have questions about Clomid.

Mild to moderate overdose symptoms include:

• Flushing abdominal pain

• Pelvic pain

• Vomiting or nausea

• Visual blurring, spots, or flashes

• Scotomata

Severe overdose symptoms include:

• Ascites

• Dyspnea

• Oliguria

• Pleural effusion

• Pericardial effusion

• Acute abdominal pain

• Hypotension

• Renal failure

• Pulmonary edema

• Deep venous thrombosis

• Respiratory distress

• Electrolyte imbalances

• Hypovolemia

• Hypoproteinemia

• Hemoconcentration

• Shock

Your physician or healthcare provider must know all medications and non-prescription drugs or medicines you are currently taking. Before taking Clomid, tell your healthcare provider about all your medical problems.

The half-life of Clomid is generally reported as five days, though some traces of Clomid can be found in feces for up to six weeks.

The half-life of Clomid is 10 hours. This means that 10 hours after ingesting Clomid, half the concentration of the medication will be present in body. This is often the reason why Clomid is dosed as a daily medication.