DEPO-TESTOSTERONE

Clinical safety rating: avoid

Corticosteroids may increase edema risk and anticoagulants may have increased effects Can cause polycythemia and increased risk of cardiovascular events.

How it works

Testosterone binds to androgen receptors, activating gene transcription that promotes development of male secondary sexual characteristics, anabolic effects, and erythropoiesis.

What the body does with it

Metabolism	Testosterone is extensively metabolized in the liver via reduction and conjugation, yielding androsterone, etiocholanolone, and dihydrotestosterone (DHT). The CYP3A4 enzyme is involved in oxidative metabolism.
Excretion	Testosterone is primarily excreted in urine as glucuronide and sulfate conjugates (90%) and in feces via bile (10%).
Half-life	The terminal elimination half-life of testosterone cypionate after intramuscular injection is approximately 8 days, allowing for dosing every 2-4 weeks.
Protein binding	Testosterone is 97-99% bound to sex hormone-binding globulin (SHBG) and albumin.
Volume of Distribution	Vd is approximately 0.6-1.0 L/kg, indicating distribution into total body water and tissues.
Bioavailability	Intramuscular: 100% (depot injection). Not available orally due to first-pass metabolism.
Onset of Action	Intramuscular: 2-3 days for initial clinical effect; maximal effects in 1-2 weeks.
Duration of Action	Intramuscular: 2-4 weeks depending on dose; sustained levels allow for biweekly to monthly dosing.

Classification & Brands

Dosing & administration

50-400 mg IM every 2-4 weeks

Dosage form	INJECTABLE
Renal impairment	No adjustment recommended; monitor fluid balance in severe impairment
Liver impairment	Contraindicated in Child-Pugh class C; use with caution in class A/B, reduce dose by 50%
Pediatric use	Not recommended for use in children; limited data
Geriatric use	Lower initial doses (50-100 mg IM every 4 weeks) due to increased risk of prostatic hypertrophy and cardiovascular events

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Corticosteroids may increase edema risk and anticoagulants may have increased effects Can cause polycythemia and increased risk of cardiovascular events.

FDA category	Contraindicated
Breastfeeding	Excretion into breast milk is unknown; however, testosterone is not expected to be present in significant amounts due to high protein binding and rapid metabolism. Theoretical risk of androgenic effects in infant. M/P ratio not established. Use during breastfeeding is not recommended unless clearly indicated and benefit outweighs risk.
Teratogenic Risk

Warnings & precautions

■ FDA Black Box Warning

Exogenous testosterone may cause virilization in pregnant women and is contraindicated in pregnant or breastfeeding women due to risk of fetal harm. Prolonged use of high doses has been associated with peliosis hepatis, hepatic neoplasms, and hepatocellular carcinoma.

Side Effect Profile

Common Effects	Acne
Serious Effects

Absolute Contraindications

Known or suspected prostate cancer, male breast cancer, pregnancy, breastfeeding, hypersensitivity to testosterone or components of the formulation, serious cardiac, hepatic, or renal disease.

Clinical Precautions

Precautions

Monitor prostate cancer risk, polycythemia (hematocrit increase), and sleep apnea. Use with caution in patients with cardiovascular disease, hepatic impairment, and fluid retention. Risk of venous thromboembolism and worsening of benign prostatic hyperplasia.

Clinical Tips & Counseling

Drug interactions

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DEPO-TESTOSTERONE

Clinical safety rating: avoid

Corticosteroids may increase edema risk and anticoagulants may have increased effects Can cause polycythemia and increased risk of cardiovascular events.

How it works

Testosterone binds to androgen receptors, activating gene transcription that promotes development of male secondary sexual characteristics, anabolic effects, and erythropoiesis.

What the body does with it

Metabolism	Testosterone is extensively metabolized in the liver via reduction and conjugation, yielding androsterone, etiocholanolone, and dihydrotestosterone (DHT). The CYP3A4 enzyme is involved in oxidative metabolism.
Excretion	Testosterone is primarily excreted in urine as glucuronide and sulfate conjugates (90%) and in feces via bile (10%).
Half-life	The terminal elimination half-life of testosterone cypionate after intramuscular injection is approximately 8 days, allowing for dosing every 2-4 weeks.
Protein binding	Testosterone is 97-99% bound to sex hormone-binding globulin (SHBG) and albumin.
Volume of Distribution	Vd is approximately 0.6-1.0 L/kg, indicating distribution into total body water and tissues.
Bioavailability	Intramuscular: 100% (depot injection). Not available orally due to first-pass metabolism.
Onset of Action	Intramuscular: 2-3 days for initial clinical effect; maximal effects in 1-2 weeks.
Duration of Action	Intramuscular: 2-4 weeks depending on dose; sustained levels allow for biweekly to monthly dosing.

Classification & Brands

Dosing & administration

50-400 mg IM every 2-4 weeks

Dosage form	INJECTABLE
Renal impairment	No adjustment recommended; monitor fluid balance in severe impairment
Liver impairment	Contraindicated in Child-Pugh class C; use with caution in class A/B, reduce dose by 50%
Pediatric use	Not recommended for use in children; limited data
Geriatric use	Lower initial doses (50-100 mg IM every 4 weeks) due to increased risk of prostatic hypertrophy and cardiovascular events

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Corticosteroids may increase edema risk and anticoagulants may have increased effects Can cause polycythemia and increased risk of cardiovascular events.

FDA category	Contraindicated
Breastfeeding	Excretion into breast milk is unknown; however, testosterone is not expected to be present in significant amounts due to high protein binding and rapid metabolism. Theoretical risk of androgenic effects in infant. M/P ratio not established. Use during breastfeeding is not recommended unless clearly indicated and benefit outweighs risk.
Teratogenic Risk

Warnings & precautions

■ FDA Black Box Warning

Side Effect Profile

Common Effects	Acne
Serious Effects

Absolute Contraindications

Known or suspected prostate cancer, male breast cancer, pregnancy, breastfeeding, hypersensitivity to testosterone or components of the formulation, serious cardiac, hepatic, or renal disease.