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Medications induced Gynecomastia

Gynecomastia is a benign male breast enlargement (glandular enlargement with fat accumulation). Those who take medications that cause gynecomastia are more likely to develop drug-induced gynecomastia. If medicine-induced gynaecomastia is suspected, the medicine should be withdrawn or discontinued if possible.

Males can develop gynecomastia or breast tissue overgrowth for a variety of reasons. Some causes of gynecomastia are considered normal or physiologic and do not require treatment, while others are pathologic and require treatment. Pathologic Gynecomastia should be treated by surgery and eliminating the cause of male breast overgrowth. Patients are surgically treated with a combination of gland excision and liposuction.

Physiologic Gynecomastia

There are three peaks during a man life which physiologic gynecomastia happen: The first is caused by high materno-placental estrogen levels in infants and starts to decline within the first few weeks after birth.

The second peak occurs between the ages of 13 and 14, with a high rate of occurrence before the 17th year of life. This temporary form is linked to hormonal changes that occur during puberty, with estrogen levels peaking earlier than testosterone levels.

Also Read – How Much Does Liposuction Cost in India

The third peak occurs in men between the ages of 50 and 80, and is caused by a variety of factors.

Pathologic gynecomastia

The causes of pathological gynecomastia include persistent pubertal gynecomastia, drug-induced gynecomastia, cirrhosis or malnutrition, male hypogonadism, testicular tumours, hyperthyroidism, chronic renal insufficiency, and idiopathic gynecomastia.

Gynecomastia is caused by an increase in glandular tissue, adipose tissue (pseudogynecomastia), or a combination of the two. All causes share an androgen-estrogen imbalance with a decreased testosterone-to-estradiol ratio, which has a direct effect on breast tissue. Changes in androgen-estrogen ratios or increased sensitivity of breast tissue to normal circulating estrogen levels cause ductal hyperplasia, elongation and branching of the ducts, fibroblast proliferation, and neovascularization, all of which contribute to the clinical appearance of gynecomastia.

According to estimates, the following etiologies are present in males seeking medical attention for gynecomastia:

  • Persistent pubertal gynecomastia – 25%
  • No detectable abnormality             – 25%
  • Drugs                                                   – 10-25%
  • Primary hypogonadism                    – 8%
  • Cirrhosis or malnutrition                 – 8%
  • Testicular tumors                               – 3%
  • Secondary hypogonadism               – 2%
  • Hyperthyroidism                               – 1.5%
  • Chronic renal insufficiency              – 1%

In this blog we will discuss drug induced gynecomastia.

Drug induced Gynecomastia

Drugs and medications are one of the most common causes of gynecomastia, or breast tissue overgrowth in men. As a side effect of their intended use, several drugs and medications can cause estrogen and testosterone hormone imbalances.

The following drugs usually cause gynecomastia: 

  1. Antiandrogens: can cause gynecomastia by acting as an antagonist to testosterone and dihydrotestosterone on the mammary glands. Furthermore, because endogenous androgens inhibit the negative feedback mechanism on the hypothalamus-pituitary-gonad axis, antiandrogens increase the levels of circulating testosterone, which is converted to estradiol at the peripheral level, thereby increasing the estrogen /androgen ratio. Gynecomastia typically appears during the first year of antiandrogen therapy in 40-70 percent of long-term treatment patients.
  2. Antihypertensive: Spironolactone causes gynecomastia by inhibiting androgen production, inhibiting androgen binding to receptors, and increasing total and free estrogen levels.
  3. Antiretroviral: In HIV-infected men receiving highly active antiretroviral therapy, gynecomastia has been reported (HAART). However, there is a lack of data on the relationship between gynecomastia and any specific antiretroviral drug or hormonal abnormality.

The drug efavirenz has been linked to gynecomastia. Based on in vitro data, the proposed mechanism is that efavirenz mimics the effects of estrogen on breast tissue.

  1. Environmental exposure: Phenothrin is an insecticide that cause gynecomastia
  2. Exogenous hormones: Exogenous hormones are those that enter the body but are not produced by the patient’s own endocrine glands.
  3. Gastrointestinal drugs: Cimetidine-induced gynecomastia is thought to be caused by AR blockade in the breasts. As a result, estrogen acts in this tissue unopposed by androgens. However, increased estrogen levels as a result of estrogen metabolism inhibition is another possible mechanism.

Drugs frequently causing gynecomastia

Antiandrogens

Bicalutamide, flutamide, finasteride, dutasteride

Antihypertensive 

Spironolactone

Antiretroviral

Protease inhibitors (indinavir, saquinavir, nelfinavir, lopinavir, ritonavir), reverse transcriptase inhibitors (zidovudine,stavudine,  lamivudine)

Environmental exposure

Phenothrin (antiparasitical)

Exogenous hormones

Oestrogens, prednisone (male teenagers)

Gastrointestinal drugs

H2 histamine receptor blockers (cimetidine)

Following drugs effects are possible to cause gynecomastia: 

  1. Antifungal: In some patients, the antifungal drug ketoconazole causes gynecomastia. It also inhibits the synthesis of androgens and glucocorticoids.
  2. Chemotherapy drugs: Following chemotherapy Medication cause Gynecomastia: Methotrexate, carmustine, cyclophosphamide, etoposide, melphalan, bleomycin, cisplatin, cytarabine, vincristine, procarbazine
  3. Cardiovascular drugs: Angiotensin-converting enzyme inhibitors, amiodarone, spironolactone, digoxin, verapamil, diltiazem, and nifedipine are the medications commonly used in cardiology practise, and they have all been linked to gynecomastia.

Drugs possibly causing gynecomastia

Antifungal

Ketoconazole (prolonged oral use)

Antihypertensive

Calcium channel blockers (nifedipine, amlodipine, felodipine, verapamil, diltiazem)

Antipsychotic (first generation)

olanzapine, Haloperidol, ziprasidone, paliperidone (high doses), risperidone (high doses), 

Antiretroviral

Efavirenz

Chemotherapy drugs

cyclophosphamide, Methotrexate, carmustine, etoposide, melphalan, cytarabine, bleomycin, cisplatin, vincristine, procarbazine

Exogenous hormones

Androgens (athletes abuse)

Gastrointestinal drugs

Proton pump inhibitors (omeprazole)

Cardiovascular drugs

Angiotensin-converting enzyme inhibitors, digoxin, spironolactone, diltiazem, amiodarone, verapamil, and nifedipine

The following drugs effect are uncertain: 

There are some medications whose effects are Uncertain (reported but could be coincidental), like Nitrates, alpha-blockers, and diazepam. Other medication that has uncertain effect are as following: 

Amiodarone, amphetamine, aripiprazole, atorvastatin, digoxin, captopril, cetirizine, clonidine, cyproterone acetate, dasatinib, diazepam, diethylstilbestrol, domperidone, loratadine, entecavir, ethanol, fenofibrate, fluoxetine, gabapentin, heroin, imatinib, lisinopril, marijuana, methadone, metronidazole, misoprostol, My Tosterone, paroxetine, penicillamine, pravastatin, pregabalin, ranitidine, rosuvastatin, sulindac, phthalates, sulpiride, sunitinib, theophylline, venlafaxine

Also Read – Side Effects of Gynecomastia

Points to be noted while you are seeking to get rid of Gynecomastia by medication

  1. Anti-estrogen drugs

People who have developed gynecomastia frequently take anti-estrogen drugs, which were made popular by bodybuilders. Although the oestrogen blocker is intended to prevent testosterone from converting to the female hormone, its effectiveness is not guaranteed. Most importantly, once breast tissue has formed, these oral medications will not be able to remove it. They may reduce the amount of fat tissue in your body, and if this is your only concern, your condition is known as pseudogynecomastia and is treatable with medication.

  1. Proper Diet & Exercise

Online gimmicks can cause you to spend a lot of money with little return. Proper nutrition and a good workout routine can help you reduce the size of fat tissues in your chest to some extent. Gynecomastia surgery, on the other hand, is likely to produce better results in people who are already thin

To sum up

Long term use of medication that causes gynecomastia should be avoided to prevent gynecomastia. Always check your medication side effects to avoid further complications and new health issues.

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