testosterone enanthate

Action and Spectrum

Actions and spectrum: 

Male sex organ development and maintenance of secondary sex characteristics are attributed to endogenous androgens, such as testosterone and dihydrotestosterone (DHT).

The development of male hair on the face, pubis, chest, and axillary hair, laryngeal enlargement, thickening of the vocal cord, and body musculature change and fat distribution are among these effects. The prostate, seminal vesicles, penis, and scrotum also grow and mature during this time. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Difficulty breathing 

Nausea 

Vomiting 

Urinary difficulty 

Swelling of feet, ankles, hands, or lower legs 

Frequent urination 

Depression 

Anxiety 

Headache 

Hypertension 

Pain in the abdomen 

Inflammation of prostate 

Infection of the urinary tract 

Sleep apnea 

Polycythemia  

Reactions at the site of injection 

Black Box Warning

Black Box Warning  

Use with caution in patients suffering from carcinoma 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

Hypersensitivity 

Precautions: 

Pulmonary embolism 

DVT (deep vein thrombosis) 

Polycythemia 

Risk of cardiovascular diseases 

Potential chances of prostate cancer 

Worsened BPH (Benign Prostate Hyperplasia) 

Suicidal risk associated with depression 

Pregnancy / Lactation

Pregnancy consideration:  

USFDA pregnancy category: X 

Lactation:  

It is contraindicated for use in lactating mothers as the drug is known to be excreted in human milk. 

Pregnancy category:  

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There was a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

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

Pharmacology: 

Pharmacodynamics: 

When testosterone ester derivatives, such as testosterone enanthate, are administered, the serum testosterone levels rise to 400% of the baseline within 24 hours. Three to five days following the first dosage, these androgen levels don’t go down.5. Serum dihydrotestosterone, serum PSA, HDL, and FSH are significantly suppressed when testosterone enanthate is administered continuously; serum estradiol is slightly elevated. Dihydrotestosterone and FSH levels can continue to be suppressed for up to 14 days following the end of treatment. The presence of testosterone enanthate does not alter mood or sexual behavior. 

Pharmacokinetics:  

Absorption 

After one day of the last dose, the testosterone level was found to exhibit a Cmax exceeding 1200 ng/dl, according to research on the pharmacokinetic profile of testosterone enanthate administered in a multiple-dosing regimen. After a week, the concentration gradually dropped until it reached 600 ng/dl. Depending on the dose given, the testosterone enanthate pharmacokinetic profile varied, shifting the peak half-life to a range of 36–48 hours. After three to four weeks, the plasma testosterone level peaked below the therapeutic range. According to this report, testosterone enanthate and testosterone cypionate have different formulations that produce different profiles, making them not therapeutically equivalent. 

Distribution 

After intravenous administration, the volume of distribution was found to be 1l/kg. 

Almost 98% of testosterone is known to be bound to plasma proteins 

Metabolism 

Enzymes in the bloodstream are required for the processing of testosterone enanthate. These enzymes will catalyze the molecule at the moiety’s ester location. Following this kind of processing, the testosterone enanthate molecule undergoes two distinct pathways of metabolism that result in different 17-keto steroids.

Estradiol and DHTd are the primary active metabolites that follow. The steroid 5α-reductase found in the skin, liver, and urogenital tract converts testosterone to DHT. DHT undergoes additional metabolism in reproductive tissues to produce androstanediol. 

Elimination and excretion 

90% of testosterone administered intramuscularly is known to be excreted in urine as conjugates of sulfuric acid glucuronide and other metabolites. 6% of the dose is eliminated as an unconjugated form through feces   

Half-life: 

7-9 days 

Adminstartion

Administration: 

Testosterone enanthate should be administered into the gluteal muscle slowly 

Patient Information Leaflet

Patient information leaflet 

Generic Name: testosterone enanthate 

Why do we use testosterone enanthate? 

In cases where there is a lack of endogenous testosterone, testosterone enanthate is recommended as a replacement medication for males. The following conditions are treated: hypogonadotropic hypogonadism, which results from an idiopathic gonadotropin or luteinizing hormone-releasing hormone deficiency.

It is essential to supplement the treatment with adrenal cortical and thyroid hormone replacement therapy, primary hypogonadism, and to stimulate puberty in patients whose delayed puberty is not caused by a pathological disorder. 

In females who are one to five years postmenopausal and have advanced, incurable metastatic breast cancer, testosterone enanthate is recommended as a secondary treatment. Additionally, it has been applied to premenopausal breast cancer patients who have undergone oophorectomy and are thought to have a tumor that responds to hormones.