Oral testosterone is a treatment for men diagnosed with hypogonadism from specific medical conditions, not for the natural decline in testosterone that occurs with aging. This therapy provides a convenient, pill-based alternative to other delivery methods like injections or topical gels.
Modern Formulations of Oral Testosterone
Newer formulations of oral testosterone were developed to address the safety concerns of previous versions. Medications such as Jatenzo, Tlando, and Kyzatrex are forms of testosterone undecanoate designed for absorption through the body’s lymphatic system.
This lymphatic absorption bypasses the “first-pass effect” in the liver. When medications are swallowed, they are often metabolized by the liver before reaching the bloodstream, which can reduce effectiveness and cause liver stress. By avoiding this initial pass, modern formulations deliver testosterone more directly.
This design provides a safer profile concerning the liver compared to older options, making oral delivery a more viable choice for testosterone replacement. The capsules are taken twice daily.
Historical and Discontinued Oral Formulations
The history of oral testosterone is marked by safety issues related to liver health. Early formulations, most notably methyltestosterone, were associated with a high risk of liver damage (hepatotoxicity), giving oral testosterone a hazardous reputation.
Methyltestosterone is a synthetic form of testosterone chemically altered to survive digestion. This alteration, however, made it taxing on the liver as it was processed directly through the portal vein system. This direct exposure led to liver problems, including jaundice and other liver diseases.
Due to these risks, methyltestosterone and similar older oral androgens are no longer recommended. The development of testosterone undecanoate, which uses a different absorption pathway, was a direct response to the need for a safer oral alternative.
Cardiovascular and Blood Pressure Considerations
A primary concern with modern oral testosterone is its potential impact on cardiovascular health. The U.S. Food and Drug Administration (FDA) has mandated a boxed warning for these medications due to the risk of increased blood pressure. This elevation can increase the likelihood of major adverse cardiovascular events, such as a heart attack or stroke.
This risk is not limited to individuals with pre-existing heart conditions; it can also affect men without a history of cardiovascular problems. The warning underscores the need for careful patient selection and monitoring. Blood pressure should be assessed before starting treatment and checked regularly throughout therapy.
If a significant increase in blood pressure occurs, a physician may recommend medication to control it or discontinue the oral testosterone. Other potential cardiovascular risks noted with testosterone products include an increased risk of blood clots.
Administration and Required Monitoring
Oral testosterone undecanoate capsules should be taken with food to ensure proper absorption. The presence of dietary fat aids absorption through the lymphatic system. One formulation, Kyzatrex, is absorbable with any meal, not just one high in fat, due to its specific composition.
Medical supervision is a requirement for individuals undergoing oral testosterone therapy. Regular check-ups and open communication with a healthcare provider are important to ensure the safe use of these medications.
Periodic blood tests are also necessary to measure testosterone levels and check for changes in red blood cell counts (hematocrit). Testosterone can increase red blood cells, which elevates the risk for blood clots.