Mesterolone

Mesterolone is a synthetic androgen belonging to the pharmacological class of androgen receptor agonists.

Mesterolone is approved for use by the FDA for treating hypogonadism and androgen deficiency conditions in males.

Mesterolone, when taken, gets rapidly absorbed and extensively binds to plasma proteins. Metabolism occurs in the liver, producing metabolites like 1α-methyl androsterone and excreting mainly via urine (80%) and faeces (13%) with a 12-13 hour half-life.

The most common side effects of Mesterolone include headache, breast enlargement, and acne.

Mesterolone is available in the form of oral tablets.

The molecule is available in India, the United States, Canada, the United Kingdom, Italy, Australia, Germany, France, Japan and Spain.

Mesterolone is a synthetic androgen belonging to the pharmacological class of androgen receptor agonists.

An oral androgen that is active, testosterone has a stronger influence on intrinsic testicular function than mesterolone. Mesterolone stimulates tissue receptors, which promote the growth of male sex organs and maintain secondary sex characteristics in androgen-deficient males. It works by simulating the effects of natural testosterone and supporting the maintenance of male sex organs, which helps with diseases associated with low hormone levels. It increases potency, strength, and bulk as an anabolic agent.

The data duration of Mesterolone action is between 8 to 12 hours after administration.

The onset of Mesterolone action typically occurs within a few days after its initial administration.

The Data of Cmax of Mesterolone typically reaches 3.8 ± 0.7 ng/mL within 2 hours post-dose.

The Data of Tmax of Mesterolone occurs around 2 hours after administration.

Mesterolone is available in the form of oral tablets.

Tablets: To be swallowed whole with water/liquid. Do not chew, crush or break it.

As the physician recommends, take the medication orally thrice daily; it can be taken with or without food as directed.

Mesterolone can be used for the following health conditions:

An inability to produce the sex hormones necessary for reproduction is known as hypogonadism. This condition is caused by malfunctioning reproductive organs, such as the ovaries in women and the testes in men. Because it functions similarly to the male sex hormone testosterone, testosterone methionine increases sperm generation in men. In addition to treating male hypogonadism, this can lessen infertility. For maximum advantage, strictly adhere to the physician's instructions.

Male infertility refers to a male's inability to cause pregnancy in a fertile female. Male insufficiency in sex hormones, which impacts both sperm count and health, could be the cause of this. Male infertility can be treated with testosterone, which functions similarly to the male sex hormone testosterone. Both the quantity and quality of sperm are increased. This improves a woman's chances of becoming pregnant and aids in the healthy functioning of a man's sexual organs. For best results, use it as prescribed by the physician.

It is indicated for treating male hypogonadism, a condition in which the testes fail to produce enough testosterone, androgen insufficiency or male infertility due to primary or secondary decreased gonadal activity. Men who are infertile owing to hypogonadism may benefit from it.

Orally: Mesterolone is usually administered orally as a tablet thrice daily, with or without food. It is advised to take this medication after meals to enhance absorption. Regular monitoring and dosage adjustments may be necessary for optimal therapeutic outcomes, and the treatment duration may generally last several weeks to months. The medication should be taken consistently as prescribed to ensure its effectiveness. Avoid abruptly stopping treatment; gradual tapering may be required under medical supervision to minimize potential withdrawal effects.

The dosage and duration of treatment should be as per the treating physician's clinical judgment.

Mesterolone is available in the form of oral tablets.

Initial dose: 75-100 mg daily in 3-4 divided doses for several months.

Maintenance: 50-75 mg daily.

If hypogonadism requires constant therapy: For several months, it is advised to take 1-2 pills of the medication Mesterolone three times a day to acquire secondary sexual characteristics.

Usually, a maintenance dose of two to three Mesterolone tablets per day is adequate.

Treatment for infertility: Enhancing sperm's quantitative and qualitative qualities.

Two to three mesterolone tablets per day should be utilized for around ninety days during the spermatogenesis cycle. After a few weeks off, testosterone treatment may be resumed if necessary.

To increase post-pubertal individuals' ejaculate fructose concentration Leydig cell failure: For several months, using a single tablet of the medication mesterolone twice a day will result in increased fructose concentrations.

The dietary restriction should be individualized as per patient requirements.

Mesterolone may be contraindicated in the following conditions:-

The adverse reactions related to Mesterolone can be categorized as

Common Adverse Effects: Mood swings, acne, changes in libido, hair loss.

Less Common Adverse Effects: GI disturbances (such as nausea), headache or changes in liver function tests.

Rare Adverse Effects: Liver abnormalities, jaundice, priapism (persistent and painful erection) or allergic reactions such as hives or swelling.

The clinically relevant drug interactions of Mesterolone are briefly summarized here.

The most common side effects of Mesterolone include:

Itching

Fever

Rash

Weight gain

Hives

Abdominal pain

Hot flashes

Indigestion

Nausea

Vomiting

Pregnancy Category X (FDA): The risks outweigh the potential benefits. Safer alternatives exist.

It is not indicated for women who are pregnant or may become pregnant to use Mesterolone tablets.

Mesterolone tablet is not indicated for women.

As per the FDA, safety and effectiveness in the pediatric population have not been established.

Renal impairment: Should be used only if the benefits outweigh the risks; Caution.

There is insufficient scientific evidence regarding the use and safety of Mesterolone in patients with hepatic impairment.

The physician should be vigilant about the knowledge pertaining to identifying and treating overdosage of Mesterolone.

Overconsumption of Mesterolone could lead to nausea, vomiting, and changes in libido.

There is no specific antidote or treatment for excessive Mesterolone intake, so treatment typically involves symptomatic and supportive measures. Mesterolone should be terminated immediately when an overdose is suspected or if any unusual symptoms occur after intake. In cases where ingestion occurred recently, gastric lavage may be intended, followed by supportive treatment to manage symptoms. At the same time, an activated charcoal may also be administered to reduce absorption if deemed appropriate within a short timeframe post-ingestion. It is essential to monitor vital signs, electrolytes, and organ function. Hospitalization and observation at a medical facility are required in severe cases, especially if extensive drug intake is suspected.

The unique characteristics of this steroid, which include not being converted into estrogen-like testosterone and its derivatives used in androgenic therapy, are determined by the presence of the C-1 methyl group in the drug's structure. This distinction thoroughly explains the observational data that mesterolone does not significantly suppress the pituitary gland's secretion of gonadotropins when given at the recommended therapeutic dose in healthy males. In this way, mesterolone differs from other androgens that limit the body's natural production of androgens to replenish testosterone levels by not affecting spermatogenesis or endogenous testosterone production. The liver tolerates meterolone better than other oral androgens, possibly because the steroid nucleus's C-17 position does not include an alkyl substitution.

Absorption of the substance occurs rapidly and almost entirely. Its bioavailability is measured at 3%, with the time to reach maximum plasma concentration being approximately 1.6 ± 0.6 hours.

The distribution of the compound shows high binding to plasma proteins, primarily to sex hormone-binding globulin (58%) and albumin (40%), totalling 98%.

In the liver, the substance undergoes swift metabolism, transforming into several metabolites, notably 1α-methyl androsterone and 1α-methyl-5α-androstane-3α, 17β-diol.

Following metabolism, the excretion of these metabolites primarily occurs through urine (80%) and, to a lesser extent, through faeces (13%). The elimination half-life is recorded at 12-13 hours.