mesterolone

Action and Spectrum

Actions and spectrum: 

Action: 

• Androgenic Activity: mesterolone has strong androgenic activity, meaning it exerts effects like testosterone in the body. Androgens are responsible for the development of male sexual characteristics and the maintenance of male secondary sexual traits. 
• Anabolic Activity: While it is primarily considered an androgen, mesterolone also has some weak anabolic properties. Anabolic agents promote muscle and tissue growth. 

Spectrum: 

• Androgen Deficiency: In cases of androgen deficiency, such as delayed puberty or andropause, mesterolone can be used to supplement androgens. 
• Muscle Wasting: While not as potent as some other anabolic steroids, mesterolone may be used to counteract muscle wasting conditions, such as those seen in certain chronic illnesses. 
• Libido Enhancement: mesterolone can improve libido and sexual function in men with low testosterone levels. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Priapism 

Hypernatremia 

Hyperphosphatemia 

Oedema 

Headache 

Depression 

Increased libido 

Hypercalcaemia 

Hyperkalaemia 

Weight gain 

Acne 

Anxiety 

Sleep apnea 

Black Box Warning

Black Box Warning: 

mesterolone does not have any black box warning. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: Individuals who have a known hypersensitivity or allergy to mesterolone or any of its components should not use this medication. 
• Prostate Cancer: mesterolone is contraindicated in individuals with prostate cancer can stimulate the growth of prostate tumors. 
• Breast Cancer: It is also contraindicated in individuals with breast cancer because it can have estrogenic effects on breast tissue. 
• Children and Adolescents: mesterolone is typically not prescribed to children and adolescents, as it can affect the development of secondary sexual characteristics and may have adverse effects on growth. 
• Pregnancy and Lactation: mesterolone should not be used during pregnancy or breastfeeding. It can harm developing fetus or be excreted into breast milk, leading to adverse effects in infants.

Caution: 

• Liver Function: While mesterolone is not considered hepatotoxic (toxic to the liver) like some other oral anabolic steroids. Therefore, individuals with pre-existing liver conditions or impaired liver function should use mesterolone cautiously and under medical supervision. Regular liver function tests may be recommended during treatment. 
• Cardiovascular Health: Anabolic steroids, including mesterolone, can potentially affect cardiovascular health. Individuals with cardiovascular disease, hypertension, or other heart-related conditions should use mesterolone with caution. Regular monitoring of blood pressure and cardiovascular health may be necessary. 
• Prostate Health: mesterolone has androgenic properties and can affect the prostate gland. It should be used cautiously in individuals with benign prostatic hyperplasia (BPH) or other prostate-related issues. Regular prostate examinations may be recommended during treatment. 
• Psychological Effects: Anabolic steroids can impact mood and behaviour. Some individuals may experience mood swings, increased aggression, and psychological dependence. If mood changes or psychological symptoms occur, they should be reported to a healthcare provider.

Comorbidities: 

• Hypogonadism: The primary indication for mesterolone is male hypogonadism, which can lead to a range of symptoms, including low libido, erectile dysfunction, fatigue, mood disturbances, and decreased muscle mass. mesterolone can help alleviate these symptoms by raising testosterone levels. 
• Depression: Low testosterone levels are sometimes associated with depressive symptoms, and mesterolone may have mood-enhancing effects in individuals with hypogonadism-related depression. 
• Osteoporosis: Low androgen levels can contribute to reduced bone density and risk of osteoporosis in men. mesterolone may help improve bone density and reduce the risk of fractures in individuals with hypogonadism. 
• Muscle Wasting: Individuals with low testosterone levels may experience muscle wasting or muscle weakness. mesterolone’s anabolic properties can potentially counteract muscle loss. 
• Libido and Sexual Function: The most common symptom of hypogonadism is a decrease in libido and sexual function. mesterolone can improve sexual desire and function in men with low testosterone levels. 

Pregnancy / Lactation

Pharmacology

Pharmacology: 

mesterolone exerts its pharmacological effects by mimicking the action of testosterone, the primary male sex hormone. It is administered orally and is well-absorbed from the gastrointestinal tract. Once in the body, mesterolone undergoes metabolism in liver, where it is converted into its active form, 1-methyl-dihydrotestosterone. This active metabolite binds to androgen receptors in various tissues, including the muscle, bone, and central nervous system.

By binding to these receptors, mesterolone can increase protein synthesis, leading to muscle growth and bone density improvement. It can also enhance libido, sexual function, and overall well-being. mesterolone is primarily used in the treatment of male hypogonadism, where it helps restore testosterone levels to alleviate symptoms associated with low androgen levels, such as low libido, erectile dysfunction, and fatigue.  

Pharmacodynamics: 

• Androgenic Activity: mesterolone is a synthetic derivative of dihydrotestosterone (DHT) and exhibits androgenic activity. It binds to androgen receptors in various tissues, including muscle, skin, and the central nervous system. This androgenic activity contributes to its effects on sexual function, libido, and the development of secondary sexual characteristics in males. 
• Anabolic Effects: While mesterolone is less potent in terms of anabolic effects compared to some other anabolic steroids, it still has mild anabolic properties. It can stimulate protein synthesis and muscle growth, which can be beneficial in conditions associated with muscle wasting. 
• Libido Enhancement: Mesterolone is known for its ability to increase libido and sexual function in men with low testosterone levels. It enhances sexual desire and can help address sexual dysfunction caused by hypogonadism or other factors. 
• Mood and Well-Being: mesterolone may have a positive impact on mood and overall well-being. Some individuals report improved mood, increased self-confidence, and reduced depressive symptoms when using this medication, especially in cases of hypogonadism-related mood disturbances. 
• Bone Health: mesterolone can have a positive effect on bone health by increasing bone density. This is particularly important in individuals with hypogonadism who may be at risk of osteoporosis.

Pharmacokinetics: 

Absorption 

mesterolone is typically administered orally in the form of tablets. It is absorbed from gastrointestinal tract after oral ingestion. Absorption can be variable among individuals, and it is influenced by factors such as the presence of food in the stomach. Taking mesterolone with food can slow down its absorption but may reduce the likelihood of gastrointestinal irritation. 

Distribution 

mesterolone, once absorbed, is distributed throughout the body via the bloodstream. It binds to serum proteins, including albumin and sex hormone-binding globulin (SHBG). This binding to proteins can influence its bioavailability and the extent to which it can exert its effects on target tissues. 

Metabolism 

mesterolone undergoes metabolism in the liver, where it is converted into its active form, 1-methyl-dihydrotestosterone (DHT). This active metabolite is responsible for the androgenic and anabolic effects of mesterolone. The metabolism of mesterolone may also involve conjugation reactions, such as glucuronidation. 

Elimination and excretion 

The metabolites of mesterolone are primarily excreted through the urine. The exact pathways of excretion and the duration of metabolite elimination can vary among individuals. The elimination half-life of mesterolone is short, typically ranging from 12 to 24 hours. 

Adminstartion

Pregnancy consideration: pregnancy Category X 

Lactation: excreted into human milk: unknown  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• <b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: mesterolone 

Pronounced: (MESS-teh-roe-lone)  

Why do we use mesterolone? 

mesterolone is commonly prescribed to treat male hypogonadism, a condition characterized by insufficient testosterone production by the testes. Hypogonadism can lead to a range of symptoms, including low libido, erectile dysfunction, fatigue, mood disturbances, and decreased muscle mass. mesterolone helps raise testosterone levels, alleviating these symptoms.

In cases of male infertility associated with low testosterone levels or inadequate sperm production, mesterolone may be used as part of fertility treatments to improve sperm quality and motility. mesterolone can help improve bone density in men with osteoporosis or low bone mass, reducing the risk of fractures. Individuals with muscle wasting conditions, such as HIV-related muscle wasting, may benefit from mesterolone’s mild anabolic effects, which can help counteract muscle loss.