How It Works
How It Works
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Anastrozole, Arimidex,
& Tamoxifen
Anastrozole, often called by its brand name Arimidex, is an aromatase inhibitor. When a male is undergoing testosterone replacement (TRT), the level of estradiol ( the predominant form of estrogen in men) can rise. The majority of estrogen in a man is the result of the aromatase enzyme complex converting testosterone to estradiol (E2) and Androstenedione to estrone.
Anastrozole can be used on its own to enhance GnRH release from the pituitary gland to promote FSH release to enhance fertility and endogenous testosterone production. This can be more beneficial than the increase in estrogen levels often witnessed with clomid use.
ABOUT
Anastrozole is the active ingredient in Arimidex, a drug that falls under the category of an aromatase inhibitor (AI).
Aromatase is an enzyme that converts testosterone into estradiol, the primary form of estrogen in men. An aromatase inhibitor, then, such as Anastrozole, can prevent the breakdown of testosterone by raising testosterone levels and reducing estradiol levels.
The U.S. Food & Drug Administration (FDA) has not approved the use of Anastrozole for any purposes or indications in men. Instead, a physician may prescribe Arimidex for off-label use as a safe and effective way to reduce elevated estradiol levels in men receiving testosterone replacement therapy (TRT). Consult with a REGENX Health provider to see if you’re a candidate for therapy.
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 (fat cells) 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.
Men on testosterone replacement therapy often experience an increase in estradiol levels. In such patients, elevated estradiol levels can result in decreased libido and breast tenderness and/or growth (gynecomastia).
While the use of an aromatase inhibitor (AI) such as Anastrozole during testosterone replacement therapy (TRT) is an off-label use, the drug can help reduce increased estradiol levels that result.
Studies indicate that men on testosterone replacement therapy who take an AI can see improvement in their sex drive and performance over men on TRT alone.
Yes. Men who do not want to take exogenous testosterone directly but do desire an increase in testosterone levels can take aromatase inhibitors (AIs) such as Anastrozole.
Anastrozole prevents or slows the breakdown of testosterone, which can result in decreased estradiol levels and increased testosterone levels. Anastrozole can also affect the activity of the estrogen receptors in the pituitary. The resulting reduction of estradiol levels prevents the negative feedback inhibition of estradiol on the hypothalamic-pituitary-gonadal axis, which can directly and indirectly increase serum levels of testosterone, follicle-stimulating hormone (FSH) and luteinizing hormone (LH) in men.
Several well-published studies indicate that using an AI alone can raise testosterone levels in hypogonadal men. A 2004 study by Leder et al looked at 37 hypogonadal men whose serum testosterone levels were lower than 350mg/dL. These men were given anastrozole 1mg/daily or 1mg twice weekly.
In men taking 1mg/daily, serum testosterone levels increased from 343 ± 61 to 572 ± 139 ng/dL
In men taking 1mg twice weekly, serum testosterone levels increased from 397 ± 106 to 520 ± 91 ng/dL
These results were illustrated again in a 2005 study by T’Sjoen et al. The study gave eligible men Letrozole 2.5mg/daily versus a placebo. After 28 days of treatment, testosterone levels increased by as much as 146%.
A 2016 longer-term study by Dias et al indicates that anastrozole 1mg/daily increased testosterone levels over three, six, and 12 months of therapy.
To find out if you are candidate for therapy, schedule a consultation with a REGENX Health provider.
Anastrozole is not right for everyone. Only your healthcare provider can decide if Anastrozole is right for you.
Anastrozole contains lactose. Therefore, patients with hereditary problems such as galactose intolerance, the Lapp lactase deficiency, or glucose-galactose malabsorption should not take this medicine.
Do not take Anastrozole if you have or have had the following conditions:
Severe renal impairment (defined as a creatinine clearance lower than 20ml/minute)
Moderate or severe hepatic disease
Known hypersensitivity to anastrozole or any history of reaction to Anastrozole
Lactoserelated hereditary problems, including galactose intolerance, the Lapp lactase deficiency, or glucose-galactose malabsorption
Do not take Anastrozole with estrogen-containing therapies, as the combination would negate any pharmacological action.
Clinical trials indicate an increased incidence of ischemic cardiovascular events in patients taking Anastrozole. Patients with pre-existing ischemic heart disease must discuss the risk-benefit ratio with their physician.
Children under the age of 18 should not take Anastrozole as safety and efficacy have not been established in such patients. Only those who have specifically been prescribed Anastrozole should take it. Never share Anastrozole with others, even if their symptoms are similar, as it may cause serious harm.
Taking Anastrozole with Tamoxifen may result in decreased Anastrozole plasma levels.
Clinical trials also indicate a mean decrease in lumbar spine bone mineral density and total hip bone mineral density in patients taking Anastrozole for 1224 months. Patients taking tamoxifen, conversely, saw an increase in lumbar spine BMD and total hip BMD.
The same trials also show that patients taking Anastrozole had elevated serum cholesterol compared to patients taking tamoxifen.
There is no evidence of clinically relevant interactions with other commonly prescribed drugs, including cytochrome P450 (such as antipyrine, cimetidine) or bisphosphonates.
Anastrozole has no significant effect on cortisol or aldosterone (at baseline or in response to ACTH), and has not induced increases in thyroid-stimulating hormone (TSH) in patients.
Anastrozole can cause serious side effects including:
Increased blood cholesterol (fat in the blood)
Skin reactions, including lesions, ulcers, and blisters
Severe allergic reactions
Liver problems
Seek medical help immediately if you experience:
Trouble breathing or swallowing
Swelling of your face, lips, throat, or tongue
Stop taking Anastrozole and seek help immediately if you experience:
General unwell feeling
Yellowing of skin or whites of the eyes
Pain in right side of the abdomen
Hot flashes
Weakness
General pain, joint pain, or back pain
Carpal tunnel syndrome, including tingling, pain, coldness, and weakness in your hand
Sore throat
Mood changes
High blood pressure
Depression
Nausea or vomiting
Thinning of the hair
Rash
Uncommon side effects of Anastrozole may include, but are not limited to, the following:
Cardiovascular conditions such as hypertension, vasodilation, peripheral edema, chest pain, ischemic heart disease, myocardial infarction, or thrombophlebitis
Psychiatric conditions such as anxiety, depression, or disturbance in mood
Respiratory conditions such as dyspnea, increased frequency of coughs, pharyngitis, bronchitis, rhinitis, or sinusitis
Hematologic conditions such as anemia, deep vein thrombosis, leukopenia, or thromboembolic disorder
Immunologic conditions such as immune hypersensitivity reaction or lymphedema
Neurologic conditions such as cerebral ischemia
Musculoskeletal, bone, and connective tissue conditions such as joint paint or stiffness, trigger finger, reductions in bone mineral density, arthralgia, arthritis, backache, osteoporosis, fracture of bone, or bone pain
Nervous system conditions such as asthenia, headache, insomnia, somnolence, carpal tunnel syndrome, dizziness, or sensory disturbances (including taste loss, taste perversion, and paresthesia)
Gastrointestinal conditions such as nausea, vomiting, or diarrhea
Skin and subcutaneous tissue conditions such as rash, allergic reactions, hair thinning (alopecia), urticaria, erythema multiforme, anaphylactic reaction, StevensJohnson Syndrome, or angioedema
Hepatobiliary disorders such as increases in alkaline phosphatase, alkaline aminotransferase, aspartate amino-transferase, gamma-GT and bilirubin, or hepatitis
Metabolism and nutritional conditions such as anorexia or hypercholesterolemia
Other conditions such as pain, cancer, tumor flare, urinary tract infections, or cataracts
REGENX Health is different from other online clinics. We take pride in educating you about the therapy you are undergoing. In our experience, the more you know about your health, the better results you will obtain.
Here’s what makes REGENX Health stand out:
Your healthcare is always expert. That’s because every virtual meeting you’ll have is with a boardcertified urologist who specializes in men’s health, including testosterone replacement therapy and related conditions. Other online men’s health clinics rely on mid-level health providers, nurse practitioners, or non-urologic physicians.
Your health and treatment are always physicianguided, in order to ensure your health and optimize your performance results. Each visit with a physician, scheduled every three months via video teleconference, provides a personable and convenient experience for our members, so we get to know you and you get to know us. (This timing is significantly more frequent than other providers.) Know that your therapy, management, and concerns will always be fully addressed.
Our pricing is always inclusive. Unlike other online men’s health clinics, there are no hidden fees or surprise prices. Your low, monthly investment includes everything you will need during your therapy:
Online physician visits
Medications
Supplies
Delivery
Comprehensive lab work
As always, there are no long-term commitment requirements, so you can cancel anytime. All medication and supplies are mailed discreetly to your home or office. Unlike other providers, you’ll never have to visit a clinic weekly to get an injection. Instead, your labs are performed on your time at a location most convenient to you and you’ll handle your personalized treatment in your own time and privacy.