Testosterone Cypionate

Endogenous testosterone plays a vital role in sexual maturation at all stages of life. It is synthetically derived from cholesterol. In males, androgens contribute to development starting in the fetal stage, become essential during puberty, and continue to influence various functions in adulthood. Women also produce small amounts of testosterone through the ovaries. However, androgen secretion from the adrenal cortex alone is insufficient to sustain male sexual characteristics.

Elevated androgen levels in the bloodstream suppress gonadotropin-releasing hormone (GnRH), reducing the production of endogenous testosterone, luteinizing hormone (LH), and follicle-stimulating hormone (FSH) through a negative feedback mechanism. Testosterone also plays a role in erythropoietin formation, calcium regulation, and blood glucose balance. Due to their high lipid solubility, androgens can quickly enter target tissue cells, where testosterone is enzymatically converted into 5-alpha-dihydrotestosterone (DHT). This transformed testosterone binds to cytosolic receptors, initiating changes in gene transcription and cellular activity within the nucleus.

Endogenous androgens typically stimulate RNA polymerase, leading to increased protein synthesis. These proteins regulate male sexual development, including the growth and maturation of the prostate, seminal vesicles, penis, and scrotum. During puberty, androgens trigger rapid muscle growth, redistribution of body fat, deepening of the voice due to changes in the larynx and vocal cords, and the development of body and facial hair. They also regulate the fusion of the epiphyseal plates, signaling the end of growth, and are essential for maintaining spermatogenesis. When natural androgen production is insufficient, exogenous androgens are required to support normal male development.

Testosterone is not recommended for children unless prescribed by a physician. Inform your healthcare provider if you have any of the following conditions:

• Cancer: Breast or prostate cancer
• Respiratory issues: Sleep apnea, lung disease
• Cardiovascular conditions: Heart disease, history of heart attack, stroke, or high blood pressure
• Metabolic disorders: Diabetes, kidney disease, liver disease
• Reproductive concerns: If you or your partner are pregnant or trying to conceive, breastfeeding
• Allergies: Soy, soya lecithin, benzyl alcohol, benzoic acid, castor oil, or other androgen-related sensitivities

Regular bloodwork is required while using testosterone. This medication is banned for use by most athletic organizations.

Special warnings & precautions

• Topical forms: Gels and solutions are flammable; avoid open flames and smoking. Accidental skin contact with others can cause hormone transfer.
• Injection risks: Must be administered intramuscularly, not intravenously. Improper injection may lead to respiratory issues or severe reactions.
• MRI caution: Some transdermal patches contain metals; remove before MRI scans.
• Prostate & cancer risk: May worsen benign prostatic hypertrophy (BPH) and increase the risk of prostate cancer. Older men should be screened before starting therapy.
• Cardiovascular risk: Studies suggest a possible increased risk of heart attacks and strokes. The FDA is investigating but has not confirmed a direct link.
• Sleep apnea & obesity: May worsen sleep apnea and is not well studied in men with BMI over 35.
• Polycythemia risk: Regular monitoring of hemoglobin and hematocrit levels is needed.
• Pregnancy & breastfeeding: Contraindicated due to potential harm to the fetus and risk of exposure through breast milk.
• Diabetes & calcium balance: Can affect blood sugar levels and exacerbate hypercalcemia in cancer patients.
• Severe reactions (POME & anaphylaxis): Some testosterone injections can cause serious lung reactions; medical monitoring is required.
• Intranasal testosterone: Not recommended for those with nasal conditions or chronic sinus issues.
• Pediatric use: May accelerate bone maturation and limit growth. Accidental exposure to children can cause early puberty symptoms.

Always follow your healthcare provider’s guidance when using testosterone therapy.

Endocrine & Reproductive Effects

• Feminization effects (gynecomastia, mastalgia) due to estrogen conversion, more common in hepatic disease.
• Libido changes (increase or decrease).
• Priapism, excessive sexual stimulation (more common in elderly males).
• Testicular effects: decreased testosterone, oligospermia, inhibition of spermatogenesis.
• Prostatic hypertrophy, increased PSA levels, prostate cancer risk.
• Epididymitis and urinary issues (urgency, retention, incontinence).
• Virilization in females (acne, facial hair, voice deepening, menstrual irregularities).

Dermatological Reactions

• Skin irritation from topical testosterone (redness, rash, itching, blistering).
• Acne, alopecia (male-pattern baldness).
• Hyperhidrosis (excessive sweating).

Cardiovascular Risks

• Hypertension (reported in 1-3% of patients).
• Increased risk of cardiovascular events (heart attack, stroke) in older men or those with pre-existing conditions.
• Potential impact on lipid profiles (increased LDL, decreased HDL).

Hepatic Effects

• Elevated liver enzymes, risk of cholestatic jaundice or hepatitis.
• Rare but severe liver complications (peliosis hepatis, hepatic neoplasms).

Neurological & Mood Effects

• Headaches (1-6%).
• Mood changes (depression, anxiety, aggression, confusion).
• Insomnia, abnormal dreams.

Gastrointestinal & Metabolic Effects

• Diarrhea, vomiting, nausea, abdominal pain.
• Weight gain due to fluid retention.
• Increased risk of hypercalcemia, especially in immobile patients.

Hematologic Effects

• Increased red blood cell count, hemoglobin, hematocrit → risk of polycythemia.
• Suppression of clotting factors → potential bleeding risk in anticoagulated patients.

Other Miscellaneous Effects

• Bone-related issues: Osteopenia, osteoporosis.
• Dental/gum irritation from buccal testosterone use.
• Risk of fetal harm if exposed during pregnancy.

Monitoring is advised for cardiovascular, prostate, liver, and blood-related complications.

Testosterone is strictly contraindicated during pregnancy due to its potential harmful effects on the fetus (FDA pregnancy category X). Women of childbearing potential undergoing testosterone therapy should use effective contraception. Since testosterone is not intended for use during pregnancy, there is no justification for its administration during labor or delivery, and its safety and efficacy in these scenarios have not been established.

Testosterone topical solutions, transdermal patches, and gels are contraindicated for breastfeeding women. Other testosterone formulations should also be avoided during lactation. While it is unknown whether testosterone transfers into breast milk, significant exposure could lead to androgenic effects in the infant and may disrupt lactation in the mother. Historically, androgens have been used to suppress lactation. Therefore, alternative feeding methods are recommended for breastfeeding women undergoing testosterone therapy.

• Store at 68°F to 77°F (20°C to 25°C), away from heat, moisture, and light.
• Keep out of reach of children.
• Discard any unused medication after the beyond use date.
• Do not flush or pour unused medicine down the sink or drain.
• If crystals form due to low temperatures, warm and shake the vial to redissolve them.