AVEED
Clinical safety rating: caution
Comprehensive clinical and safety monograph for AVEED (AVEED).
Testosterone replacement therapy; testosterone binds to androgen receptors, activating gene transcription and promoting development of male characteristics.
| Metabolism | Hepatic via oxidation and conjugation; not extensively metabolized by CYP450. |
| Excretion | Approximately 90% of testosterone metabolites are excreted in urine as glucuronide and sulfate conjugates, with about 6% excreted in feces via bile. |
| Half-life | The terminal elimination half-life of testosterone undecanoate following intramuscular injection is approximately 33.9 days (range 20-60 days), allowing for dosing intervals of 10-14 weeks. |
| Protein binding | Testosterone is approximately 98% bound in plasma, primarily to sex hormone-binding globulin (SHBG, ~40%) and albumin (~58%), with about 2% free. |
| Volume of Distribution | The apparent volume of distribution of testosterone is approximately 1.0 L/kg, reflecting extensive distribution into tissues and binding to androgen receptors. |
| Bioavailability | Testosterone undecanoate has an absolute bioavailability of approximately 100% following intramuscular injection due to complete absorption from the injection site. |
| Onset of Action | Following intramuscular injection, serum testosterone concentrations reach supraphysiological levels within 24-48 hours, with clinical effects (e.g., libido, energy) typically apparent within 1-2 weeks. |
| Duration of Action | A single intramuscular injection provides therapeutic testosterone levels for 10-14 weeks, with some patients maintaining levels for up to 16 weeks. The long duration is due to slow release from the oil depot. |
| Molecular Weight | 440.7 |
300 mg intramuscularly once at initiation and at 4 weeks, followed by 150 mg intramuscularly every 6 weeks thereafter.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for any degree of renal impairment. |
| Liver impairment | Contraindicated in patients with Child-Pugh Class B or C cirrhosis. No specific dose adjustment recommended for Child-Pugh Class A; use with caution. |
| Pediatric use | Not approved for use in pediatric patients; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment recommended; monitor for fluid retention and cardiovascular events due to age-related comorbidities. |
| 1st trimester | Contraindicated. Testosterone cypionate is a pregnancy category X drug; can cause virilization of female fetus and is not indicated for use in women. |
| 2nd trimester | Contraindicated. Same risks as t1; avoid use. |
| 3rd trimester | Contraindicated. Same risks as t1; avoid use. |
Clinical note
Comprehensive clinical and safety monograph for AVEED (AVEED).
| Placental transfer | Testosterone crosses the placenta and can cause virilization of the female fetus. Degree of transfer is significant with potential for teratogenicity. |
| Breastfeeding | Testosterone is excreted in human milk. Use during breastfeeding may cause virilization in the infant and suppress lactation. Contraindicated. |
| Lactation Rating |
■ FDA Black Box Warning
WARNING: PULMONARY OIL MICROEMBOLISM (POEM) AND ANAPHYLAXIS - Reported with testosterone undecanoate injection; can be fatal. Observe patients for 30 minutes after each injection.
| Serious Effects |
Hypersensitivity to testosterone cypionate or any componentMen with carcinoma of the breast or prostateWomen who are or may become pregnant (pregnancy category X)Nursing mothersSevere hepatic or renal impairment
| Precautions | Risk of POEM and anaphylaxis; monitor PSA and hematocrit; exacerbation of sleep apnea; gynecomastia; prostate cancer risk; edema; hypercalcemia. |
| Food/Dietary | No clinically significant food interactions reported. However, maintain a consistent diet with regard to fat intake as absorption is not affected by food. Avoid excessive alcohol consumption as it may exacerbate side effects such as liver toxicity and reduce therapeutic efficacy. |
Loading safety data…
| L5 - Contraindicated |
| Teratogenic Risk | Pregnancy category X. Testosterone undecanoate is contraindicated in pregnancy. First trimester: Virilization of female fetus. Second and third trimesters: Continued risk of fetal masculinization, growth abnormalities. |
| Fetal Monitoring | Monitor maternal blood pressure, lipid profile, liver function tests, and signs of virilization. Fetal monitoring for growth and development if inadvertent exposure. |
| Fertility Effects | May suppress spermatogenesis via negative feedback on gonadotropins. Reversible after discontinuation. Contraindicated in men with fertility concerns. |
| Clinical Pearls | AVEED (testosterone undecanoate) is an injectable testosterone replacement therapy with a long duration of action requiring careful monitoring of serum testosterone levels to avoid supraphysiologic concentrations. Due to risk of pulmonary oil microembolism (POME) and anaphylaxis, observe patient for 30 minutes post-injection. Do not use in patients with prostate carcinoma or male breast cancer. Monitor hematocrit, lipid profile, and liver function periodically. |
| Patient Advice | AVEED is injected into the gluteal muscle only by a healthcare professional. · Report any signs of allergic reaction (hives, difficulty breathing, swelling) or pulmonary oil microembolism (cough, shortness of breath, chest tightness) immediately. · Keep all follow-up appointments for blood tests to monitor testosterone levels and side effects. · Inform your doctor if you have a history of heart, kidney, or liver disease, or sleep apnea. · AVEED may increase the risk of blood clots; seek immediate care if you have leg pain/swelling, sudden chest pain, or trouble breathing. |