estrogens esterified/methyltestosterone            

Actions and Spectrum: 

estrogens esterified 

• The mechanism of action of estrogens involves binding to estrogen receptors in target tissues, leading to changes in gene expression and cellular activity. estrogens have diverse effects on tissues, including the female reproductive organs, bones, cardiovascular, and central nervous systems. They contribute to developing secondary sexual characteristics, regulate menstrual cycles, promote bone density, and play a role in maintaining cardiovascular health. 

• The spectrum of activity of estrogens esterified primarily encompasses the treatment of symptoms associated with estrogen deficiency in menopausal women. It can help alleviate menopausal symptoms such as hot flashes, vaginal dryness, and mood changes. estrogens esterified can also be used for hormone replacement therapy in women with primary ovarian failure or those who have surgically removed the ovaries.

methyltestosterone: 

• methyltestosterone is a synthetic androgen or male sex hormone that exhibits both anabolic (tissue-building) androgenic (masculinizing) effects. It is a derivative of testosterone, the primary male sex hormone. 
• The mechanism of action of methyltestosterone involves binding to androgen receptors in various tissues, including skeletal muscle, bone, liver, and the central nervous system. Activation of androgen receptors leads to anabolic effects such as increased protein synthesis and muscle growth, and androgenic effects such as deepening of the voice, growth of facial and body hair, and promotion of secondary sexual characteristics in males. 

• The spectrum of methyltestosterone activity includes treating androgen deficiency in males, such as hypogonadism, delayed puberty, and certain forms of erectile dysfunction. It may also be used in females to treat certain hormone-related conditions, such as breast cancer or androgen-responsive inoperable metastatic mammary carcinoma. 

DRUG INTERACTION

Frequency not defined 

Headache 

Breast soreness, 

Bloating 

Hypercalcemia 

Cholestatic hepatitis 

Anaphylaxis 

Polycythemia 

Edema 

Acne, alopecia 

Menstrual irregularities 

Nausea 

Hypercholesterolemia 

Vomiting 

Suppression of clotting factors II, V, VII 

Paresthesia 

Black box warning: 

estrogens esterified: 

estrogens esterified has a black box warning, common to all estrogen products. The black box warning highlights the increased risks of endometrial cancer, cardiovascular disorders, breast cancer, and probable dementia associated with estrogen-alone or estrogen-plus-progestin therapy. It states that estrogens should be used at the lowest effective dose for the shortest duration necessary, and treatment should be re-evaluated regularly. 

methyltestosterone: 

methyltestosterone, as an androgen medication, does not have a black box warning specifically for its use. However, it is essential to note that androgens can have potential risks and side effects, including masculinization effects in females, adverse effects on the cardiovascular system, liver toxicity, psychiatric effects, and suppression of natural testosterone production. 

Contraindications/caution: 

Contraindications: 

estrogens esterified: 

• Known or suspected pregnancy: estrogens are contraindicated in pregnancy due to the risk of fetal harm. If pregnancy is detected during treatment, estrogen therapy should be discontinued immediately. 
• Known or suspected estrogen-dependent neoplasia (e.g., breast cancer): estrogens are contraindicated in individuals with known or suspected estrogen-dependent tumors. 
• Undiagnosed abnormal genital bleeding: estrogens should not be used in individuals with abnormal vaginal bleeding. A healthcare professional should evaluate any unexplained vaginal bleeding. 
• Known or suspected thromboembolic disorders: estrogens are contraindicated in individuals with active or history of thromboembolic disorders (e.g., deep vein thrombosis, pulmonary embolism). 

methyltestosterone: 

• Prostate cancer: methyltestosterone is contraindicated in individuals with prostate cancer or suspected prostate cancer. Androgens can stimulate the growth of prostate tissue and may worsen the condition. 
• Breast cancer in males: methyltestosterone is contraindicated in males with breast cancer or known or suspected breast carcinoma. 
• Known or suspected hypersensitivity: methyltestosterone should not be used in individuals with a known hypersensitivity to the drug or its components. 

Caution: 

• Cardiovascular disorders: estrogens esterified and methyltestosterone should be used cautiously in individuals with a history of cardiovascular disorders, such as heart disease, stroke, or blood clots. estrogens may increase the risk of cardiovascular events, including heart attack and stroke. 

• Endocrine disorders: The use of estrogens esterified and methyltestosterone should be approached with caution in individuals with endocrine disorders, such as diabetes or thyroid dysfunction. estrogens can affect glucose metabolism and thyroid hormone levels, requiring careful monitoring and adjustment of medications if necessary. 

• Liver dysfunction: Individuals with liver dysfunction or impaired liver function should use estrogens esterified and methyltestosterone with caution. These medications can affect liver function and may exacerbate liver disease. Regular monitoring of liver function tests is recommended in such cases. 

• Hypertension: estrogens esterified and methyltestosterone should be used cautiously in individuals with hypertension (high blood pressure) or a history of hypertension. estrogens can increase blood pressure in some individuals, requiring close monitoring and management of blood pressure levels. 

• History of breast disease: Individuals with a history of breast disease, such as breast cancer or benign breast tumors, should use estrogens esterified and methyltestosterone with caution. Regular breast examinations and mammograms are recommended during treatment. 

• Renal dysfunction: Individuals with renal dysfunction or impaired kidney function should use estrogens esterified and methyltestosterone with caution. Dose adjustments may be necessary in such cases. 

• Cholestatic jaundice: estrogens esterified and methyltestosterone should be used cautiously in individuals with a history of cholestatic jaundice (a liver condition characterized by impaired bile flow). These medications can affect liver function and may worsen the condition. 

Pregnancy consideration: estrogens are contraindicated due to the risk of fetal harm. If pregnancy is detected during treatment, estrogen therapy should be discontinued immediately. 

Pregnancy Category: X 

Lactation: Excretion of the drug in human breast milk is known, and it is contraindicated 

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 

Pharmacology: 

estrogens esterified, and methyltestosterone is a combination medication that contains two active ingredients: estrogens esterified and methyltestosterone. Each component has its pharmacology:  

estrogens esterified: 

estrogens esterified is a mixture of esterified estrogens and synthetic estrogens derived from natural sources. estrogens exert their effects by binding to estrogen receptors in various tissues throughout the body. The pharmacological actions of estrogens include: 

• Estrogenic Effects: estrogens promote the growth and development of female reproductive tissues and secondary sexual characteristics. They contribute to the uterus, fallopian tubes, and vagina maturation. estrogens also stimulate breast tissue growth and play a role in bone health by promoting calcium deposition and reducing bone resorption. 

• Hormone Replacement Effects: estrogens esterified can be used as hormone replacement therapy in menopausal women to alleviate symptoms associated with estrogen deficiency. They help relieve vasomotor symptoms (e.g., hot flashes) and genitourinary symptoms (e.g., vaginal dryness) and improve mood and overall well-being.

methyltestosterone: 

methyltestosterone is a synthetic androgen or male sex hormone. It is derived from testosterone, the primary male sex hormone. methyltestosterone exhibits both anabolic (tissue-building) and androgenic (masculinizing) effects. Its pharmacological actions include: 

• Androgenic Effects: methyltestosterone promotes the development and maintenance of male secondary sexual characteristics, such as the growth of facial and body hair, deepening of the voice, and enlargement of the genitalia. Androgens also play a role in the regulation of libido and sexual function. 
• Anabolic Effects: methyltestosterone has anabolic properties that promote protein synthesis and muscle growth. It is sometimes used to treat androgen deficiency in males, delay puberty, or support muscle growth in certain clinical conditions. 

The combination of estrogens esterified and methyltestosterone allows for supplementing estrogen and androgen hormones, providing a balanced hormonal replacement therapy option for individuals with specific clinical indications. 

Pharmacodynamics: 

The actions of their components mainly determine the pharmacodynamics of estrogens esterified and methyltestosterone: 

estrogens esterified: 

estrogens esterified exert their pharmacodynamic effects by binding to estrogen receptors in various tissues throughout the body. estrogen receptors are found in the cytoplasm or nucleus of target cells and modulate gene expression. The pharmacodynamic effects of estrogens esterified include: 

• Promotion of female secondary sexual characteristics: estrogens esterified promote the development and maturation of female reproductive tissues, such as the uterus, fallopian tubes, and vagina. They also contribute to the growth of breast tissue. 

• Maintenance of bone health: estrogens esterified help maintain bone health by promoting calcium deposition and reducing bone resorption. They have been used to prevent osteoporosis in postmenopausal women. 

• Relief of menopausal symptoms: estrogens esterified can be used as hormone replacement therapy in menopausal women to alleviate symptoms associated with estrogen deficiency, such as hot flashes, vaginal dryness, and mood swings.

methyltestosterone: 

methyltestosterone exerts its pharmacodynamic effects by binding to androgen receptors in various tissues throughout the body. Androgen receptors are found in the cytoplasm or nucleus of target cells and modulate gene expression. The pharmacodynamic effects of methyltestosterone include: 

• Promotion of male secondary sexual characteristics: methyltestosterone promotes the development and maturation of male reproductive tissues, such as the testes, epididymis, and prostate. It also contributes to the growth of facial and body hair, the deepening of the voice, and the enlargement of the genitalia. 
• Anabolic effects: methyltestosterone has properties that promote protein synthesis and muscle growth. It is sometimes used to treat androgen deficiency in males, delay puberty, or support muscle growth in certain clinical conditions. 

Pharmacokinetics: 

Absorption 

estrogens esterified, and methyltestosterone can be administered orally as tablets. After oral administration, they are absorbed from the gastrointestinal tract. The rate and extent of absorption may vary depending on the formulation and individual factors. 

Distribution 

Both estrogens esterified, and methyltestosterone are distributed throughout the body via the bloodstream. estrogens bind to sex hormone-binding globulin (SHBG) and albumin, while methyltestosterone binds primarily to albumin. They can cross cell membranes and enter target tissues where they exert their pharmacological effects. 

Metabolism 

estrogens esterified undergo hepatic metabolism, primarily through hydrolysis of the ester bonds to form free estrone, equilin, and other estrogens. These metabolites are metabolized by conjugation with glucuronic acid or sulfate and eventually excreted in the urine. 

methyltestosterone undergoes hepatic metabolism as well. The liver metabolizes it via various enzymatic pathways, including oxidation and conjugation reactions. The significant metabolites include 17α-methyl-5α-androstan-3α,17β-diol (which exhibits androgenic activity) and 17α-methyl-5β-androstan-3α,17β-diol (which exhibits estrogenic activity). 

Elimination and Excretion 

The metabolites of estrogens, esterified, and methyltestosterone are primarily excreted in the urine, and a smaller portion is eliminated in the feces. The elimination half-lives of these compounds can vary, and clearance rates are influenced by factors such as age, liver function, and renal function. 

Administration: 

• Dosage: The healthcare professional will determine the dosage of estrogens, esterified, and methyltestosterone based on the individual’s specific needs, medical condition, and response to treatment. It’s essential to take the medication as prescribed and not exceed the recommended dose. 

• Timing: The timing of administration may vary depending on the specific instructions provided. Sometimes, the medication must be taken with food or at specific intervals throughout the day. It’s essential to follow the prescribed schedule and timing of administration. 

• Swallowing: estrogens esterified and methyltestosterone tablets should be swallowed whole with a glass of water. Do not crush, chew, or break the tablets unless specifically instructed. 

• Duration of Treatment: The healthcare professional will determine the duration of treatment with estrogens esterified and methyltestosterone. It’s important to continue taking the medication for the prescribed duration unless otherwise instructed by a healthcare professional. 

• Compliance: It’s crucial to adhere to the prescribed dosing schedule and not miss any doses. If a dose is missed, it’s essential to take it as soon as remembered unless it’s close to the time for the next scheduled dose. The missed dose should be skipped, and the regular dosing schedule should be resumed. 

• Additional Instructions: It’s essential to consult the prescribing information, product labeling, or a healthcare professional for specific instructions or any additional considerations regarding the administration of estrogens esterified and methyltestosterone. They can provide detailed guidance based on the individual’s needs and medical conditions. 

Patient information leaflet 

Generic Name: estrogens esterified and methyltestosterone 

Why do we use estrogens esterified and methyltestosterone? 

estrogens esterified, and methyltestosterone is a combination medication primarily used for hormone replacement therapy in postmenopausal women. It provides a balanced supplementation of estrogen and androgen hormones to address specific symptoms and conditions. 

• Menopausal Hormone Therapy (HRT): estrogens esterified and methyltestosterone can be prescribed as hormone replacement therapy in postmenopausal women to alleviate symptoms associated with menopause. These symptoms may include hot flashes, night sweats, vaginal dryness, mood changes, and sleep disturbances. 
• Estrogen Deficiency: estrogens esterified, and methyltestosterone can supplement estrogen levels in women with low endogenous estrogen production. This may occur in women with ovarian failure, surgical menopause (removal of ovaries), or other conditions leading to estrogen deficiency. 
• Genitourinary Symptoms: estrogens esterified and methyltestosterone can help relieve genitourinary symptoms associated with menopause, such as vaginal dryness, itching, burning, and discomfort during sexual intercourse. Estrogen supplementation can improve vaginal lubrication and restore the health of vaginal tissues. 
• Osteoporosis Prevention: estrogens esterified and methyltestosterone can prevent osteoporosis in postmenopausal women at high risk of developing the condition. estrogen therapy helps maintain bone density and reduce the risk of fractures.