Aromatase Inhibitors (AIs) For Men

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Aromatase Inhibitors For Men

There are innumerable categories of drugs such as aromatase inhibitors (AIs) available for human use. Drugs in the same group work nearly in the same manner, but with a slight difference in chemical makeup, side effects and dosage.


What is Aromatase Inhibitor?


Aromatase is an enzyme which synthesizes estrogen. The enzyme is located in the following areas:


  • Brain 
  • Adipose tissue 
  • Placenta 
  • Blood vessels 
  • Skin 
  • Bone


It may also be found in the tissue of:


  • Endometriosis 
  • Uterine fibroids 
  • Breast cancer
  • Endometrial cancer


Aromatase inhibitors are prescription drugs used to inhibit or prevent the synthesis of estrogen by blocking the actions of the enzyme. Males who have high estrogen levels and low testosterone levels may be given aromatase inhibitors for men.


AIs for Men


Many perceive estrogen hormone as a female hormone, however, a man’s body produce estrogen, but in minimal levels. A male will need estrogen to aid in the bone formation and blood clotting. Nonetheless, when the levels go higher than normal, it becomes problematic for a man and may result in:


  • Infertility
  • Gynecomastia
  • Cancer such as breast cancer
  • Obesity


There are many causes of elevated estrogen such as a high aromatase activity. The aromatase enzyme converts testosterone into estrogen. Aromatase enzyme in a male may be found in fat cells, particularly in the mid-section; thus if a man is obese, he may be at risk of low testosterone levels and high estrogen levels. Also, as a male age, testosterone starts to be converted to estrogen since aging is linked with an increase in the enzyme. Testosterone therapy (when a man is treated with man-made testosterone in the form of injections) may lead to too much estrogen. There are three AIs for men, namely:


  1. Arimidex (Anastrozole) – it blocks the enzyme, thus estrogen production is suppressed; the bond it forms with the enzyme is reversible and there is the likelihood of estrogen rebound when this AI is used.
  2. Aromasin (Exemestane) – it is considered a suicidal AI, this implies that once it binds to the enzyme, the bond is irreversible, there isn’t a chance for enzyme rebound, nevertheless, your body will rebuild the enzyme after a couple of weeks.
  3. Femara(Letrozole) – it works in a similar manner like Arimidex, though it is more powerful. The bond formed is reversible, although it’s competitive, so Letrozole crushes estrogen levels quickly; probably, this is an explanation why it’s the most commonly used AI


Uses of AIs for Males


Used in fertility treatments – a man dealing with infertility believed to be as a result of low testosterone or obesity is given an AI. The medication is given in low levels. The AI aids in stimulating the production of Luteinizing hormone (LH) and follicle-stimulating hormone (FSH) as estrogen production is suppressed. LH stimulates Leydig cells in your testes to produce testosterone, which supports sperm production, thus a male may be able to make a woman pregnant. While on fertility drugs, it’s important to eat healthy foods and exercise frequently, more so obese men, but exercise in moderation.


Used in bodybuilding – bodybuilders use anabolic steroids and hormonal imbalance may occur. The body has the ability to normalize or regulate the hormones; nonetheless, it can take a longer time. If a bodybuilder decides nature to take its course in normalizing the hormones, one will become vulnerable to some side effects which may significantly impact one’s bodybuilding goals, the longer the process takes. Also, an individual overall health may be at risk. Apart from being prone to gynecomastia (breast enlargement), you may be prone to spiking blood pressure levels and water retention. If this occurs, you will lose the admirable figure you have worked for tirelessly. To prevent all these side effects of anabolic use from happening, body builders use AIs, especially men as they are at risk of gyno. The AIs inhibits estrogen levels from increasing before the body regains back the ability to balance the hormones; the medication boosts the capability of the body to restore hormonal levels rapidly by preventing it from releasing elevated amounts of estrogen through aromatization. Apart from preventing a person from experiencing gyno, water retention, and hypertension, you are also guaranteed that you will not lose the gains (the muscles) you have worked hard for at the gym anytime soon, provided you take the AI as prescribed.


To treat breast cancer – Males are at risk of breast cancer since they have breast tissue, though the risk is low when compared to females. Some breast cancer depends on estrogen hormone (hormone receptor positive breast cancer) to grow and spread. Thus, when the drug (an AI) is taken, the tumors shrink and the growth of breast cancer is either slowed or stopped; the period of the therapy may range from three years to 10 years or as directed by the medical care provider. The AIs has been approved by the FDA to treat breast cancer in postmenopausal women.


Side Effects


Males on the medication are at risk of side effects which may be severe or minor. Men react differently to the medicine. Below are some unwanted effects, namely:


  • Joint pain and stiffness, especially the knees, ankles, and wrists. Also, you may feel discomfort in the hands. The good news is that your muscles or joint won’t be damaged.
  • Fatigue – you will be faced with fatigue within a couple of days once you start using the medications; it’s a natural reaction due to the changing hormonal levels in the body and will clear once the body adjust to the AI. The level of tiredness will be based on the level of testosterone levels.
  • Neurocognitive issues – the sudden rise of testosterone in the body will shock the neurocognitive capabilities for a short time. You may note a change in your ability to remember things temporally.
  • Hot flashes 
  • Night sweats 
  • Headaches
  • Nausea


If you are considering using an AI to treat gyno or to prevent it, to manage breast cancer or as a fertility drug, discuss with the health care provider the benefits versus the risks involved. The drugs have been of great help to many men, the most important thing is to take the drug as prescribed and contact the medical care provider if you experience unwanted bothersome effects

Article Name
Aromatase Inhibitors (AIs) For Men
Aromatase inhibitors are prescription drugs used to inhibit or prevent the synthesis of estrogen by blocking the actions of the enzyme.
Publisher Name
Fertility Drugs Online
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