Action and Spectrum

Actions and Spectrum: 

• Androgenic effects: methyltestosterone has potent androgenic effects, which means it can promote the development of male sexual characteristics such as deepening of the voice, facial and body hair growth, and increased muscle mass and strength. 
• Anabolic effects: methyltestosterone also has anabolic effects, meaning it can stimulate protein synthesis and promote muscle growth and repair. 
• Androgen replacement therapy: methyltestosterone can be used as a replacement therapy in men who have low testosterone levels due to a medical condition such as hypogonadism. 
• Delayed puberty: methyltestosterone can also be used to stimulate puberty in boys who have delayed puberty due to a medical condition. 
• Breast cancer: methyltestosterone can be used to treat advanced breast cancer in women, although it is not commonly used for this purpose due to the risk of masculinizing side effects. 
• Performance enhancement: methyltestosterone is sometimes used illicitly by athletes and bodybuilders to enhance muscle mass and athletic performance. However, its use is banned by many sports organizations and can lead to serious side effects and health risks. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Priapism 

Virilization 

Edema 

Breast soreness 

Acne 

Menstrual irregularities 

Frequency not defined 

Gynecomastia 

Anaphylaxis 

Cholestatic jaundice syndrome 

Neoplasm of liver 

Anaphylaxis 

Black Box Warning

Contraindication / Caution

Contraindication/Caution: 

methyltestosterone has several contraindications and cautions that should be considered before use. These include: 

• Hypersensitivity: methyltestosterone should not be used in individuals who are hypersensitive or allergic to the drug or its components. 
• Prostate cancer: methyltestosterone is contraindicated in men with prostate cancer or a history of prostate cancer. 
• Breast cancer: methyltestosterone is contraindicated in women with breast cancer or a history of breast cancer. 
• Pregnancy and breastfeeding: methyltestosterone should not be used during pregnancy or breastfeeding, as it can harm the developing fetus or nursing infant. 
• Liver disease: methyltestosterone should be used cautiously in individuals with liver disease, as it can worsen liver function and increase the risk of liver damage. 
• Cardiovascular disease: methyltestosterone can increase the risk of cardiovascular events such as heart attack, stroke, and blood clots, particularly in individuals with a history of cardiovascular disease. 
• Other medical conditions: methyltestosterone should be used with caution in individuals with high blood pressure, diabetes, kidney disease, and other medical conditions that androgens can worsen. 
• Drug interactions: methyltestosterone can interact with other medications, including blood thinners, insulin, and certain medications used to treat epilepsy. 

Pregnancy / Lactation

Pregnancy consideration:  

Category X 

Breastfeeding warnings:  

methyltestosterone is excreted in breastmilk; hence contraindicated 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: No evidence of risk to the fetus is found in animal reproduction studies, and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a human product; Pregnant women must take care of the potential risks. 
• Category D: There is adequate data with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergencies for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. The drug is not for pregnant women. 
• Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

Pharmacological properties of methyltestosterone include: 

• Androgenic activity: methyltestosterone has potent androgenic activity. It can bind to and activate androgen receptors in various tissues throughout the body, promoting the development of male sexual characteristics and increasing muscle mass and strength. 
• Anabolic activity: methyltestosterone also has anabolic activity, which can stimulate protein synthesis and promote muscle growth and repair. 
• Metabolism: methyltestosterone is metabolized in the liver by the cytochrome P450 enzyme system and is excreted primarily in the urine as metabolites. 
• Half-life: The half-life of methyltestosterone is relatively short, with a half-life of approximately 4 hours. 
• Bioavailability: methyltestosterone has variable bioavailability due to significant first-pass metabolism in the liver, and using enteric-coated formulations or other strategies to improve bioavailability may be necessary. 
• Androgen replacement therapy: methyltestosterone can be used as a replacement therapy in men with low testosterone levels due to a medical condition such as hypogonadism. 
• Delayed puberty: methyltestosterone can also stimulate puberty in boys who have delayed puberty due to a medical condition. 
• Breast cancer: methyltestosterone can be used to treat advanced breast cancer in women, although it is not commonly used for this purpose due to the risk of masculinizing side effects. 

Pharmacodynamics: 

• Androgenic effects: methyltestosterone has potent androgenic effects, which means it can promote the development of male sexual characteristics such as increased facial hair growth, deepening of the voice, and enlargement of the penis and testes. 
• Anabolic effects: methyltestosterone also has anabolic effects, stimulating protein synthesis and promoting muscle growth and repair. It helps treat delayed puberty and muscle-wasting conditions. 
• Hematologic effects: methyltestosterone can stimulate the production of red blood cells, which can increase the oxygen-carrying capacity of the blood. However, this effect can also increase the risk of polycythemia, a condition characterized by excessive red blood cells. 
• Lipid metabolism: methyltestosterone can alter lipid metabolism, increasing LDL cholesterol production and decreasing HDL cholesterol production. It can increase the risk of cardiovascular disease. 
• Reproductive effects: methyltestosterone can suppress the production of gonadotropins, hormones that stimulate the production of testosterone and sperm. It can lead to a decrease in endogenous testosterone production and testicular atrophy. 
• Masculinizing effects in women: methyltestosterone can cause masculinizing effects in women, including deepening of the voice, growth of facial hair, and clitoral enlargement. 
• Behavioral effects: methyltestosterone can affect mood and behavior, with potential effects including increased aggression and irritability. 

Pharmacokinetics: 

Absorption 

The half-life of the drug is 10-100 minutes 

The peak plasma concentration is achieved in 1-2 hours 

The drug is absorbed from the gastrointestinal tract & oral mucosa 

Distribution 

The protein-bound is 98% 

Metabolism 

It is less extensively undergoing first-pass hepatic metabolism than testosterone and is suitable for oral administration. 

Elimination and Excretion  

The drug is excreted 90% in urine and 6% in feces 

Adminstartion

Administration: 

methyltestosterone is a synthetic form of the male hormone testosterone, used to treat testosterone deficiency in men. It may also be prescribed to women for certain conditions, such as breast cancer, and to treat symptoms of menopause. 

methyltestosterone is usually taken orally as a tablet, and the dosage and duration of treatment will depend on the individual’s condition and medical history. It should be taken as prescribed by a healthcare provider. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: methyltestosterone 

Pronounced: METH-il-tes-TOS-te-rone 

Why do we use methyltestosterone? 

methyltestosterone is a synthetic form of testosterone, a male hormone naturally produced in the body. methyltestosterone is used to treat conditions in which there is a deficiency of testosterone in the body, such as hypogonadism (a condition in which the testes do not produce enough testosterone). 

In addition to treating testosterone deficiency in men, methyltestosterone may also be used to treat breast cancer in women and to relieve symptoms of menopause, such as hot flashes, night sweats, and vaginal dryness. 

methyltestosterone works by increasing the amount of testosterone in the body, which can help to improve symptoms associated with testosterone deficiency or menopause. However, it is essential to note that methyltestosterone has the potential to cause serious side effects and should only be used under the guidance of a healthcare provider.