ORA-TESTRYL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ORA-TESTRYL (ORA-TESTRYL).
Testosterone replacement therapy; binds to androgen receptors, promoting protein synthesis, muscle growth, and secondary sexual characteristic development.
| Metabolism | Metabolized in liver via CYP3A4 and CYP2C9 to androsterone, etiocholanolone, and 17-ketosteroids. |
| Excretion | Renal (90% as glucuronide and sulfate conjugates, 10% unchanged); Biliary/fecal (10%) |
| Half-life | Terminal half-life 2.5-3.5 hours; clinical context: requires multiple daily dosing to maintain steady-state levels |
| Protein binding | 97-99% bound to sex hormone-binding globulin (SHBG) and albumin |
| Volume of Distribution | 0.5-1.0 L/kg; indicates extensive tissue distribution, including reproductive tissues |
| Bioavailability | Oral: 3-6% (extensive first-pass metabolism); Buccal/sublingual: 20-40% |
| Onset of Action | Oral: 1-2 hours; Buccal/sublingual: 15-30 minutes |
| Duration of Action | Oral: 6-8 hours; Buccal/sublingual: 4-6 hours; clinical notes: duration shorter with sublingual route due to first-pass avoidance |
| Molecular Weight | 288.42 |
Intramuscular injection: 50-100 mg every 2-4 weeks.
| Dosage form | TABLET |
| Renal impairment | No specific dose adjustment required for renal impairment; use with caution if GFR <30 mL/min. |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh class C). In moderate impairment (Child-Pugh class B), reduce dose by 50%. |
| Pediatric use | Not recommended in pediatric patients for androgen replacement; safety and efficacy not established. |
| Geriatric use | Use lowest effective dose (e.g., 50 mg IM every 4 weeks) due to increased risk of prostatic hypertrophy and cardiovascular events. |
| 1st trimester | Avoid; potential teratogenic effects due to androgenic activity. |
| 2nd trimester | Avoid; virilization of female fetus and potential adverse effects. |
| 3rd trimester | Avoid; may cause virilization of female fetus and premature closure of epiphyses. |
Clinical note
Comprehensive clinical and safety monograph for ORA-TESTRYL (ORA-TESTRYL).
| Placental transfer | Crosses placenta; androgenic effects on fetus documented. |
| Breastfeeding | Excreted in breast milk; may cause masculinization of female infants and other adverse effects. Use is contraindicated during breastfeeding. |
| Lactation Rating |
■ FDA Black Box Warning
Risk of blood clots, stroke, heart attack, and exacerbation of prostate cancer. Testosterone may be abused and cause serious health issues.
| Serious Effects |
PregnancyBreastfeedingKnown hypersensitivity to methyltestosteroneProstatic carcinomaMale breast carcinomaSevere hepatic impairment
| Precautions | Cardiovascular risk, polycythemia, benign prostatic hyperplasia, sleep apnea, and edema. Monitor hematocrit, lipids, and prostate-specific antigen. |
| Food/Dietary | No significant food interactions. However, avoid grapefruit juice as it may alter metabolism. Avoid alcohol as it may exacerbate hepatotoxic effects. |
| Clinical Pearls |
Loading safety data…
| L5 (Contraindicated) |
| Teratogenic Risk | Teratogenic risk profile: ORA-TESTRYL (testosterone undecanoate) is contraindicated in pregnancy. First trimester: virilization of female fetus; second and third trimesters: ongoing virilization, growth retardation. Class X. Transdermal testosterone has been associated with clitoromegaly, labial fusion, and urogenital sinus abnormalities in female fetuses. |
| Fetal Monitoring | If inadvertent exposure occurs, monitor fetal growth and anatomy via ultrasound. Assess for signs of virilization in female fetus. Monitor maternal blood pressure, liver function, lipid profile, and hematocrit. No specific fetal monitoring required if drug is avoided as recommended. |
| Fertility Effects | Testosterone suppresses endogenous gonadotropins, reducing spermatogenesis and potentially causing oligospermia or azoospermia. Reversible upon discontinuation. In females, may cause menstrual irregularities and anovulation. |
| ORA-TESTRYL (methyltestosterone buccal tablets) is an androgen replacement therapy for male hypogonadism. Buccal absorption avoids first-pass metabolism. Monitor liver function due to potential hepatotoxicity. Contraindicated in males with breast or prostate cancer. Avoid use in women due to virilization risks. |
| Patient Advice | Place tablet between cheek and gum and allow to dissolve; do not swallow or chew. · Do not eat, drink, or smoke while tablet is dissolving. · Use twice daily, once in morning and once in evening, at same times each day. · If you miss a dose, take it as soon as possible, but do not double up. · Report jaundice, dark urine, or abdominal pain immediately. · Regularly check liver function tests as directed by your doctor. · This medication may cause testicular shrinkage, gynecomastia, or worsening sleep apnea. · Not for use in women, especially those who are or may become pregnant. |